JP-7856360-B2 - Heterocyclic compounds with antitumor activity and their use

Inventors

• ワン，ジェンユィ
• ジュ，シンボ
• ワン，クアンレイ
• アン，ホォイ
• ホア，シンシン
• フゥ，ジィミン
• ガオ，ジュン
• リ，ズジェン
• ファン，リシュエ
• ヤン，インピン

Assignees

• 石薬集団中奇制薬技術（石家庄）有限公司

Dates

Publication Date

20260511

Application Date

20221216

Priority Date

20211217

Claims (20)

1. The following equation (A): (In the formula, below: The substructures in the above structural formula, represented as shown above, represent single or double bonds. Y and Z are both selected from C and N, and when Y is N, Z is C, and when Y is C, Z is N. Y and Z, together with the atoms connected to them, form ring A, and ring A is selected from 5-12 membered heterocyclyl groups and 5-12 membered heteroaryl groups. R2 is one, two, or three, each independently selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, formyl group, oxo group, C1-6 alkyl group, C1-6 alkoxy group, -C1-6 alkyl-NH( C1-6 alkyl), -C1-6 alkyl-N( C1-6 alkyl) 2 , C2-6 alkenyl group, C2-6 alkynyl group, C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group and 5-10 membered heteroaryl group, where the C1-6 alkyl group, C1-6 alkoxy group, -C1-6 alkyl-NH( C1-6 alkyl), -C1-6 alkyl-N( C1-6 alkyl) 2 , C2-6 alkenyl group, C2-6 alkynyl group, C The 3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may each be optionally substituted with one or more cyano groups, hydroxyl groups, or halogens. R3 is selected from hydrogen, halogen, hydroxyl group, amino group, cyano group, C1-6 alkyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, and 3-6 membered heterocyclyl group, where the C1-6 alkyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, and 3-6 membered heterocyclyl group may each be optionally substituted with one or more hydroxyl groups or halogens. Ring B is selected from C4-12 cycloalkyl groups, C4-12 cycloalkenyl groups, 4-12 membered heterocyclyl groups, C6-12 aryl groups, 5-12 membered heteroaryl groups, C6-12 aryl-condensed C4-12 cycloalkyl groups, C6-12 aryl-condensed 4-12 membered heterocyclyl groups, and C6-12 aryl-condensed C4-12 cycloalkenyl groups. Each R4 is independently selected from hydrogen, cyano group, halogen, amino group, hydroxyl group, oxo group, nitro group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, C1-6 haloalkyl group, C1-6 hydroxyalkyl group, C1-6 alkoxy group, -C0-6 alkyl-NH- C1-6 alkyl group, -C0-6 alkyl-N( C1-6 alkyl)( C1-6 alkyl), C3-6 cycloalkyl group, C3-6 halocycloalkyl group, and 3-6 membered heterocyclyl group, where the C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, C1-6 haloalkyl group, C1-6 hydroxyalkyl group, C1-6 alkoxy group, -C0-6 alkyl-NH- C1-6 alkyl group, and -C0-6 alkyl-N(C The 1-6 alkyl ( C1-6 alkyl), C3-6 cycloalkyl, C3-6 halocycloalkyl, and 3-6 membered heterocyclyl groups may all be optionally substituted with one or more substituents, which are halogens, hydroxyl groups, amino groups, -SO2- C1-4 alkyl groups, or oxo groups, where w is 0, 1, 2, 3 , or 4. below: When the substructure in the above structural formula is a double bond, X is C, and the R1 connected to it is selected from -O- RA , -N( RD ) RB and RC . If R1 is -O- RA , then R1 is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R1 . Each R a1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group . If R1 is -N( RD )R B , then R B is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R b1 . Each R b1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group . R D is selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl ) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group , and -N(C1-6 alkyl ) 2 . If R1 is R C , then R C is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 4 identical or different R c1 groups. Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, methanesulfonyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -COC3-6 cycloalkyl group , -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group, where the C1-6 alkyl group, C2-6 alkenyl group , C 2-6 alkynyl groups, -OC 1-6 alkyl groups, -SC 1-6 alkyl groups, -COC 1-6 alkyl groups, -COC 3-6 cycloalkyl groups, -CH2 COC 1-6 alkyl groups, -CH2 CON (C 1-6 alkyl) 2 , -CH2 CONHC 1-6 alkyl groups, -NHC 1-6 alkyl groups, -N (C 1-6 alkyl) 2 , C 3-10 cycloalkyl groups, C 6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may all be optionally substituted with one or more substituents selected from deuterium, hydroxyl groups, cyano groups, C 1-3 alkyl groups, C 1-3 alkoxy groups, and halogens. below: When the substructure in the above structural formula is a single bond, X is N, and R1 connected to it is selected from C3-10 cycloalkyl groups, C3-10 cycloalkenyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C3-10 cycloalkyl groups, C3-10 cycloalkenyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by one or more identical or different R a4 and/or R b4 . Each R a4 is independently selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by one or more identical or different R b4 and/or R c4 . Each R b4 is independently selected from -OR c4 , -NR c4 R c4 , halogen, -CN, -C(O)R c4 , -C(O)OR c4 , -C(O)NR c4 R c4 , -OC(O)R c4 , -S(O) 2 R c4 , -S(O) 2NR c4 R c4 , -NHC(O)R c4 , -N( C1-4 alkyl)C(O)R c4 , -NHC(O)OR c4 , and divalent substituents =O and =NH, where =O and =NH may be substituents in a non-aromatic ring system. Each R c4 is independently selected from hydrogen, C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by one or more identical or different R d4 and/or R e4 . Each R d4 is independently selected from -OR e4 , -NR e4 R e4 , halogen, -CN, -C(O)R e4 , -C(O)OR e4 , -C(O)NR e4 R e4 , -S(O) 2 R e4 , -S(O) 2NR e4 R e4 , -NHC(O)R e4 , -N( C1-4 alkyl)C(O)R e4 , and the divalent substituent =O, where =O may be only substituents in a non-aromatic ring system. Each R e4 is independently selected from hydrogen, C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted with one or more hydrogen, cyano groups, hydroxyl groups, or halogens. Here, Z and Y are included in the atoms or number of atoms of ring A, Unless otherwise specified, the heteroatoms in the heteroaryl group and heterocyclyl group are independently selected from O, N, and S, and the number of heteroatoms is one, two, three, or four. Compounds, or their stereoisomers, optical isomers, pharmaceutical salts, solvates, or isotopic derivatives.
2. The aforementioned compound is given by the following formula (A'): (In the formula, below: The substructures in the above structural formula, represented as shown above, represent single or double bonds. Y and Z are both selected from C and N, and when Y is N, Z is C, and when Y is C, Z is N. Y and Z, together with the atoms connected to them, form ring A, and ring A is selected from 5-12 membered heterocyclyl groups and 5-12 membered heteroaryl groups. R2 is one, two, or three, each independently selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, formyl group, oxo group, C1-6 alkyl group, C1-6 alkoxy group, -C1-6 alkyl-NH( C1-6 alkyl), -C1-6 alkyl-N( C1-6 alkyl) 2 , C2-6 alkenyl group, C2-6 alkynyl group, C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group and 5-10 membered heteroaryl group, where the C1-6 alkyl group, C1-6 alkoxy group, -C1-6 alkyl-NH( C1-6 alkyl), -C1-6 alkyl-N( C1-6 alkyl) 2 , C2-6 alkenyl group, C2-6 alkynyl group, C The 3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may each be optionally substituted with one or more cyano groups, hydroxyl groups, or halogens. R3 is selected from hydrogen, halogen, hydroxyl group, amino group, cyano group, C1-6 alkyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, and 3-6 membered heterocyclyl group, where the C1-6 alkyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, and 3-6 membered heterocyclyl group may each be optionally substituted with one or more hydroxyl groups or halogens. Ring B is selected from C4-12 cycloalkyl groups, C4-12 cycloalkenyl groups, 4-12 membered heterocyclyl groups, C6-12 aryl groups, 5-12 membered heteroaryl groups, C6-12 aryl-condensed C4-12 cycloalkyl groups, C6-12 aryl-condensed 4-12 membered heterocyclyl groups, and C6-12 aryl-condensed C4-12 cycloalkenyl groups. Each R4 is independently selected from hydrogen, cyano group, halogen, amino group, hydroxyl group, oxo group, nitro group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, C1-6 haloalkyl group, C1-6 hydroxyalkyl group, C1-6 alkoxy group, -C0-6 alkyl-NH- C1-6 alkyl group, -C0-6 alkyl-N( C1-6 alkyl)( C1-6 alkyl), C3-6 cycloalkyl group, C3-6 halocycloalkyl group, and 3-6 membered heterocyclyl group, where the C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, C1-6 haloalkyl group, C1-6 hydroxyalkyl group, C1-6 alkoxy group, -C0-6 alkyl-NH- C1-6 alkyl group, and -C0-6 alkyl-N(C The 1-6 alkyl ( C1-6 alkyl), C3-6 cycloalkyl, C3-6 halocycloalkyl, and 3-6 membered heterocyclyl groups may all be optionally substituted with one or more substituents, which are halogens, hydroxyl groups, amino groups, -SO2- C1-4 alkyl groups, or oxo groups, where w is 0, 1, 2, 3 , or 4. below: When the substructure in the above structural formula is a double bond, X is C, and the R connected to it is selected from -O- RA , -N( RD ) RB and RC . If R1 is -O- RA , then R1 is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R1 . Each R a1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group . If R1 is -N( RD )R B , then R B is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R b1 . Each R b1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group . R D is selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl ) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group , and -N(C1-6 alkyl ) 2 . If R1 is R C , then R C is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 4 identical or different R c1 groups. Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, methanesulfonyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -COC3-6 cycloalkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N (C1-6 alkyl ) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group, where the C1-6 alkyl group, C2-6 alkenyl group , C 2-6 alkynyl groups, -OC 1-6 alkyl groups, -SC 1-6 alkyl groups, -COC 1-6 alkyl groups, -COC 3-6 cycloalkyl groups, -CH2 COC 1-6 alkyl groups, -CH2 CON (C 1-6 alkyl) 2 , -CH2 CONHC 1-6 alkyl groups, -NHC 1-6 alkyl groups, -N (C 1-6 alkyl) 2 , C 3-10 cycloalkyl groups, C 6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may all be optionally substituted with one or more substituents selected from deuterium, hydroxyl groups, cyano groups, C 1-3 alkyl groups, C 1-3 alkoxy groups, and halogens. below: When the substructure in the above structural formula is a single bond, X is N, and R1 connected to it is selected from C3-10 cycloalkyl groups, C3-10 cycloalkenyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C3-10 cycloalkyl groups, C3-10 cycloalkenyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by one or more identical or different R a4 and/or R b4 . Each R a4 is independently selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by one or more identical or different R b4 and/or R c4 . Each R b4 is independently selected from -OR c4 , -NR c4 R c4 , halogen, -CN, -C(O)R c4 , -C(O)OR c4 , -C(O)NR c4 R c4 , -OC(O)R c4 , -S(O) 2 R c4 , -S(O) 2NR c4 R c4 , -NHC(O)R c4 , -N( C1-4 alkyl)C(O)R c4 , -NHC(O)OR c4 , and divalent substituents =O and =NH, where =O and =NH may be substituents in a non-aromatic ring system. Each R c4 is independently selected from hydrogen, C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by one or more identical or different R d4 and/or R e4 . Each R d4 is independently selected from -OR e4 , -NR e4 R e4 , halogen, -CN, -C(O)R e4 , -C(O)OR e4 , -C(O)NR e4 R e4 , -S(O) 2 R e4 , -S(O) 2NR e4 R e4 , -NHC(O)R e4 , -N( C1-4 alkyl)C(O)R e4 , and the divalent substituent =O, where =O may be only substituents in a non-aromatic ring system. Each R e4 is independently selected from hydrogen, C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted with one or more hydrogen, cyano groups, hydroxyl groups, or halogens. Here, Z and Y are included in the atoms or number of atoms of ring A, Unless otherwise specified, the heteroatoms in the heteroaryl group and the heterocyclyl group are independently selected from O, N, and S, and the number of heteroatoms is 1, 2, 3, or 4. ) The compound according to claim 1, or its stereoisomers, optical isomers, pharmaceutical salts, solvates, or isotopic derivatives.
3. The following equation (I): (In the formula, below: The substructures in the above structural formula, represented as shown above, represent single or double bonds. Y and Z are both selected from C and N, and when Y is N, Z is C, and when Y is C, Z is N. Y and Z, together with the atoms connected to them, form ring A, and ring A is selected from 5-12 membered heterocyclyl groups and 5-12 membered heteroaryl groups. R2 is one, two, or three, each independently selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, formyl group, oxo group, C1-6 alkyl group, C1-6 alkoxy group, -C1-6 alkyl-NH( C1-6 alkyl), -C1-6 alkyl-N( C1-6 alkyl) 2 , C2-6 alkenyl group, C2-6 alkynyl group, C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group and 5-10 membered heteroaryl group, where the C1-6 alkyl group, C1-6 alkoxy group, -C1-6 alkyl-NH( C1-6 alkyl), -C1-6 alkyl-N( C1-6 alkyl) 2 , C2-6 alkenyl group, C2-6 alkynyl group, C The 3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may each be optionally substituted with one or more cyano groups, hydroxyl groups, or halogens. R3 is selected from hydrogen, halogen, hydroxyl group, amino group, cyano group, C1-6 alkyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, and 3-6 membered heterocyclyl group, where the C1-6 alkyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, and 3-6 membered heterocyclyl group may each be optionally substituted with one or more hydroxyl groups or halogens. Ring B is selected from C4-12 cycloalkyl groups, C4-12 cycloalkenyl groups, C4-12 heterocyclyl groups, C6-12 aryl groups, C5-12 heteroaryl groups, C6-12 aryl-condensed C4-12 cycloalkyl groups, C6-12 aryl -condensed C4-12 heterocyclyl groups, and C6-12 aryl-condensed C4-12 cycloalkenyl groups. Each R4 is independently selected from hydrogen, cyano group, halogen, amino group, hydroxyl group, oxo group, nitro group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, C1-6 haloalkyl group, C1-6 hydroxyalkyl group, C1-6 alkoxy group, -C0-6 alkyl-NH- C1-6 alkyl group, -C0-6 alkyl-N( C1-6 alkyl)( C1-6 alkyl), C3-6 cycloalkyl group, C3-6 halocycloalkyl group, and 3-6 membered heterocyclyl group, where the C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, C1-6 haloalkyl group, C1-6 hydroxyalkyl group, C1-6 alkoxy group, -C0-6 alkyl-NH- C1-6 alkyl group, and -C0-6 alkyl-N(C The 1-6 alkyl ( C1-6 alkyl), C3-6 cycloalkyl, C3-6 halocycloalkyl, and 3-6 membered heterocyclyl groups may all be optionally substituted with one or more substituents, which are halogens, hydroxyl groups, amino groups, -SO2- C1-4 alkyl groups, or oxo groups, where w is 0, 1, 2, 3 , or 4. below: When the substructure in the above structural formula is a double bond, X is C, and the R1 connected to it is selected from -O- RA , -N( RD ) RB and RC . If R1 is -O- RA , then R1 is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R1 . Each R a1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group . If R1 is -N( RD )R B , then R B is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R b1 . Each R b1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group . R D is selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl ) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group , and -N(C1-6 alkyl ) 2 . If R1 is R C , then R C is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R c1 groups. Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group , 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group , where C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC 1-6 alkyl groups, -COC 1-6 alkyl groups, -CH2 COC 1-6 alkyl groups, -CH2 CON( C1-6 alkyl) 2 , -CH2 CONHC 1-6 alkyl groups, -NHC 1-6 alkyl groups, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups and 5-10 membered heteroaryl groups may all be optionally substituted with one or more substituents selected from hydroxyl groups, C1-3 alkyl groups, C1-3 alkoxy groups and halogens. below: When the substructure in the above structural formula is a single bond, X is N, and R1 connected to it is selected from C3-10 cycloalkyl groups, C3-10 cycloalkenyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C3-10 cycloalkyl groups, C3-10 cycloalkenyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by one or more identical or different R a4 and/or R b4 . Each R a4 is independently selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by one or more identical or different R b4 and/or R c4 . Each R b4 is independently selected from -OR c4 , -NR c4 R c4 , halogen, -CN, -C(O)R c4 , -C(O)OR c4 , -C(O)NR c4 R c4 , -OC(O)R c4 , -S(O) 2 R c4 , -S(O) 2NR c4 R c4 , -NHC(O)R c4 , -N( C1-4 alkyl)C(O)R c4 , -NHC(O)OR c4 , and divalent substituents =O and =NH, where =O and =NH may be substituents in a non-aromatic ring system. Each R c4 is independently selected from hydrogen, C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by one or more identical or different R d4 and/or R e4 . Each R d4 is independently selected from -OR e4 , -NR e4 R e4 , halogen, -CN, -C(O)R e4 , -C(O)OR e4 , -C(O)NR e4 R e4 , -S(O) 2 R e4 , -S(O) 2NR e4 R e4 , -NHC(O)R e4 , -N( C1-4 alkyl)C(O)R e4 , and the divalent substituent =O, where =O may be only substituents in a non-aromatic ring system. Each R e4 is independently selected from hydrogen, C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted with one or more hydrogen, cyano groups, hydroxyl groups, or halogens. Here, Z and Y are included in the atoms or number of atoms of ring A, Unless otherwise specified, the heteroatoms in the heteroaryl group and heterocyclyl group are independently selected from O, N, and S, and the number of heteroatoms is one, two, three, or four. Compounds, or their stereoisomers, optical isomers, pharmaceutical salts, solvates, or isotopic derivatives.
4. The aforementioned compound is of the following formulas: (II), (III), or (IV): (In the formula, below: The substructures in the above structural formula, represented as shown above, represent single or double bonds. Y and Z are both selected from C and N, and when Y is N, Z is C, and when Y is C, Z is N. Y and Z, together with the atoms connected to them, form ring A, and ring A is selected from 5-12 membered heterocyclyl groups and 5-12 membered heteroaryl groups. R2 is one, two, or three, each independently selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, formyl group, oxo group, C1-6 alkyl group, C1-6 alkoxy group, -C1-6 alkyl-NH( C1-6 alkyl), -C1-6 alkyl-N( C1-6 alkyl) 2 , C2-6 alkenyl group, C2-6 alkynyl group, C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group and 5-10 membered heteroaryl group, where the C1-6 alkyl group, C1-6 alkoxy group, -C1-6 alkyl-NH( C1-6 alkyl), -C1-6 alkyl-N( C1-6 alkyl) 2 , C2-6 alkenyl group, C2-6 alkynyl group, C The 3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may each be optionally substituted with one or more cyano groups, hydroxyl groups, or halogens. R3 is selected from hydrogen, halogen, hydroxyl group, amino group, cyano group, C1-6 alkyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, and 3-6 membered heterocyclyl group, where the C1-6 alkyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, and 3-6 membered heterocyclyl group may each be optionally substituted with one or more hydroxyl groups or halogens. Ring B is selected from C4-12 cycloalkyl groups, C4-12 cycloalkenyl groups, C4-12 heterocyclyl groups, C6-12 aryl groups, C5-12 heteroaryl groups, C6-12 aryl-condensed C4-12 cycloalkyl groups, C6-12 aryl -condensed C4-12 heterocyclyl groups, and C6-12 aryl-condensed C4-12 cycloalkenyl groups. Each R4 is independently selected from hydrogen, cyano group, halogen, amino group, hydroxyl group, oxo group, nitro group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, C1-6 haloalkyl group, C1-6 hydroxyalkyl group, C1-6 alkoxy group, -C0-6 alkyl-NH- C1-6 alkyl group, -C0-6 alkyl-N( C1-6 alkyl)( C1-6 alkyl), C3-6 cycloalkyl group, C3-6 halocycloalkyl group, and 3-6 membered heterocyclyl group, where the C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, C1-6 haloalkyl group, C1-6 hydroxyalkyl group, C1-6 alkoxy group, -C0-6 alkyl-NH- C1-6 alkyl group, and -C0-6 alkyl-N(C The 1-6 alkyl ( C1-6 alkyl), C3-6 cycloalkyl, C3-6 halocycloalkyl, and 3-6 membered heterocyclyl groups may all be optionally substituted with one or more substituents, which are halogens, hydroxyl groups, amino groups, -SO2- C1-4 alkyl groups, or oxo groups, where w is 0, 1, 2, 3 , or 4. below: When the substructure in the above structural formula is a double bond, X is C, and the R1 connected to it is selected from -O- RA , -N( RD ) RB and RC . If R1 is -O- RA , then R1 is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R1 . Each R a1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group . If R1 is -N( RD )R B , then R B is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R b1 . Each R b1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group . R D is selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl ) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group , and -N(C1-6 alkyl ) 2 . If R1 is R C , then R C is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R c1 groups. Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group , 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group , where C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC 1-6 alkyl groups, -COC 1-6 alkyl groups, -CH2 COC 1-6 alkyl groups, -CH2 CON( C1-6 alkyl) 2 , -CH2 CONHC 1-6 alkyl groups, -NHC 1-6 alkyl groups, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups and 5-10 membered heteroaryl groups may all be optionally substituted with one or more substituents selected from hydroxyl groups, C1-3 alkyl groups, C1-3 alkoxy groups and halogens. below: When the substructure in the above structural formula is a single bond, X is N, and R1 connected to it is selected from C3-10 cycloalkyl groups, C3-10 cycloalkenyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C3-10 cycloalkyl groups, C3-10 cycloalkenyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by one or more identical or different R a4 and/or R b4 . Each R a4 is independently selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by one or more identical or different R b4 and/or R c4 . Each R b4 is independently -OR c4 , -NR c4 R c4 , halogen, -CN, -C(O)R c4 , -C(O)OR c4 , -C(O)NR c4 R c4 , -OC(O)R c4 , -S(O) 2 R c4 , -S(O) 2NR c4 R c4 , -NHC(O)R c4 , -N( C1-4 alkyl)C(O)R c4 , -NHC(O)OR c4 , and a divalent substituent =O or =NH, where =O and =NH may be only substituents in a non-aromatic ring system. Each R c4 is independently selected from hydrogen, C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by one or more identical or different R d4 and/or R e4 . Each R d4 is independently selected from -OR e4 , -NR e4 R e4 , halogen, -CN, -C(O)R e4 , -C(O)OR e4 , -C(O)NR e4 R e4 , -S(O) 2 R e4 , -S(O) 2NR e4 R e4 , -NHC(O)R e4 , -N( C1-4 alkyl)C(O)R e4 , and the divalent substituent =O, where =O may be only substituents in a non-aromatic ring system. Each R e4 is independently selected from hydrogen, C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted with one or more hydrogen, cyano groups, hydroxyl groups, or halogens. Here, Z and Y are included in the atoms or number of atoms of ring A, Unless otherwise specified, the heteroatoms in the heteroaryl group and heterocyclyl group are independently selected from O, N, and S, and the number of heteroatoms is one, two, three, or four. (In the formula, below: The substructures in the above structural formula, represented as shown above, represent single or double bonds. Y and Z are both selected from C and N, and when Y is N, Z is C, and when Y is C, Z is N. Y and Z, together with the atoms connected to them, form ring A, and ring A is selected from 5-12 membered heterocyclyl groups and 5-12 membered heteroaryl groups. R2 is one, two, or three, each independently selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, formyl group, oxo group, C1-6 alkyl group, C1-6 alkoxy group, -C1-6 alkyl-NH( C1-6 alkyl), -C1-6 alkyl-N( C1-6 alkyl) 2 , C2-6 alkenyl group, C2-6 alkynyl group, C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group and 5-10 membered heteroaryl group, where the C1-6 alkyl group, C1-6 alkoxy group, -C1-6 alkyl-NH( C1-6 alkyl), -C1-6 alkyl-N( C1-6 alkyl) 2 , C2-6 alkenyl group, C2-6 alkynyl group, C The 3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may each be optionally substituted with one or more cyano groups, hydroxyl groups, or halogens. R3 is selected from hydrogen, halogen, hydroxyl group, amino group, cyano group, C1-6 alkyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, and 3-6 membered heterocyclyl group, where the C1-6 alkyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, and 3-6 membered heterocyclyl group may each be optionally substituted with one or more hydroxyl groups or halogens. Ring B is selected from C4-12 cycloalkyl groups, C4-12 cycloalkenyl groups, C4-12 heterocyclyl groups, C6-12 aryl groups, C5-12 heteroaryl groups, C6-12 aryl-condensed C4-12 cycloalkyl groups, C6-12 aryl -condensed C4-12 heterocyclyl groups, and C6-12 aryl-condensed C4-12 cycloalkenyl groups. Each R4 is independently selected from hydrogen, cyano group, halogen, amino group, hydroxyl group, oxo group, nitro group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, C1-6 haloalkyl group, C1-6 hydroxyalkyl group, C1-6 alkoxy group, -C0-6 alkyl-NH- C1-6 alkyl group, -C0-6 alkyl-N( C1-6 alkyl)( C1-6 alkyl), C3-6 cycloalkyl group, C3-6 halocycloalkyl group, and 3-6 membered heterocyclyl group, where the C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, C1-6 haloalkyl group, C1-6 hydroxyalkyl group, C1-6 alkoxy group, -C0-6 alkyl-NH- C1-6 alkyl group, and -C0-6 alkyl-N(C The 1-6 alkyl ( C1-6 alkyl), C3-6 cycloalkyl, C3-6 halocycloalkyl, and 3-6 membered heterocyclyl groups may all be optionally substituted with one or more substituents, which are halogens, hydroxyl groups, amino groups, -SO2- C1-4 alkyl groups, or oxo groups, where w is 0, 1, 2, 3 , or 4. below: When the substructure in the above structural formula is a double bond, X is C, and the R1 connected to it is selected from -O- RA , -N( RD ) RB and RC . If R1 is -O- RA , then R1 is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R1 . Each R a1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group . If R1 is -N( RD )R B , then R B is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R b1 . Each R b1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group . R D is selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl ) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group , and -N(C1-6 alkyl ) 2 . If R1 is R C , then R C is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R c1 groups. Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group , 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group , where C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC 1-6 alkyl groups, -COC 1-6 alkyl groups, -CH2 COC 1-6 alkyl groups, -CH2 CON( C1-6 alkyl) 2 , -CH2 CONHC 1-6 alkyl groups, -NHC 1-6 alkyl groups, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups and 5-10 membered heteroaryl groups may all be optionally substituted with one or more substituents selected from hydroxyl groups, C1-3 alkyl groups, C1-3 alkoxy groups and halogens. below: When the substructure in the above structural formula is a single bond, X is N, and R1 connected to it is selected from C3-10 cycloalkyl groups, C3-10 cycloalkenyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C3-10 cycloalkyl groups, C3-10 cycloalkenyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by one or more identical or different R a4 and/or R b4 . Each R a4 is independently selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by one or more identical or different R b4 and/or R c4 . Each R b4 is independently selected from -OR c4 , -NR c4 R c4 , halogen, -CN, -C(O)R c4 , -C(O)OR c4 , -C(O)NR c4 R c4 , -OC(O)R c4 , -S(O) 2 R c4 , -S(O) 2NR c4 R c4 , -NHC(O)R c4 , -N( C1-4 alkyl)C(O)R c4 , -NHC(O)OR c4 , and divalent substituents =O and =NH, where =O and =NH may be substituents in a non-aromatic ring system. Each R c4 is independently selected from hydrogen, C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by one or more identical or different R d4 and/or R e4 . Each R d4 is independently selected from -OR e4 , -NR e4 R e4 , halogen, -CN, -C(O)R e4 , -C(O)OR e4 , -C(O)NR e4 R e4 , -S(O) 2 R e4 , -S(O) 2NR e4 R e4 , -NHC(O)R e4 , -N( C1-4 alkyl)C(O)R e4 , and the divalent substituent =O, where =O may be only substituents in a non-aromatic ring system. Each R e4 is independently selected from hydrogen, C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted with one or more hydrogen, cyano groups, hydroxyl groups, or halogens. Here, Z and Y are included in the atoms or number of atoms of ring A, Unless otherwise specified, the heteroatoms in the heteroaryl group and heterocyclyl group are independently selected from O, N, and S, and the number of heteroatoms is one, two, three, or four. (In the formula, below: The substructures in the above structural formula, represented as shown above, represent single or double bonds. Y and Z are both selected from C and N, and when Y is N, Z is C, and when Y is C, Z is N. Y and Z, together with the atoms connected to them, form ring A, and ring A is selected from 5-12 membered heterocyclyl groups and 5-12 membered heteroaryl groups. R2 is one, two, or three, each independently selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, formyl group, oxo group, C1-6 alkyl group, C1-6 alkoxy group, -C1-6 alkyl-NH( C1-6 alkyl), -C1-6 alkyl-N( C1-6 alkyl) 2 , C2-6 alkenyl group, C2-6 alkynyl group, C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group and 5-10 membered heteroaryl group, where the C1-6 alkyl group, C1-6 alkoxy group, -C1-6 alkyl-NH( C1-6 alkyl), -C1-6 alkyl-N( C1-6 alkyl) 2 , C2-6 alkenyl group, C2-6 alkynyl group, C The 3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may each be optionally substituted with one or more cyano groups, hydroxyl groups, or halogens. R3 is selected from hydrogen, halogen, hydroxyl group, amino group, cyano group, C1-6 alkyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, and 3-6 membered heterocyclyl group, where the C1-6 alkyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, and 3-6 membered heterocyclyl group may each be optionally substituted with one or more hydroxyl groups or halogens. Ring B is selected from C4-12 cycloalkyl groups, C4-12 cycloalkenyl groups, C4-12 heterocyclyl groups, C6-12 aryl groups, C5-12 heteroaryl groups, C6-12 aryl-condensed C4-12 cycloalkyl groups, C6-12 aryl -condensed C4-12 heterocyclyl groups, and C6-12 aryl-condensed C4-12 cycloalkenyl groups. Each R4 is independently selected from hydrogen, cyano group, halogen, amino group, hydroxyl group, oxo group, nitro group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, C1-6 haloalkyl group, C1-6 hydroxyalkyl group, C1-6 alkoxy group, -C0-6 alkyl-NH- C1-6 alkyl group, -C0-6 alkyl-N( C1-6 alkyl)( C1-6 alkyl), C3-6 cycloalkyl group, C3-6 halocycloalkyl group, and 3-6 membered heterocyclyl group, where the C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, C1-6 haloalkyl group, C1-6 hydroxyalkyl group, C1-6 alkoxy group, -C0-6 alkyl-NH- C1-6 alkyl group, and -C0-6 alkyl-N(C The 1-6 alkyl ( C1-6 alkyl), C3-6 cycloalkyl, C3-6 halocycloalkyl, and 3-6 membered heterocyclyl groups may all be optionally substituted with one or more substituents, which are halogens, hydroxyl groups, amino groups, -SO2- C1-4 alkyl groups, or oxo groups, where w is 0, 1, 2, 3 , or 4. below: When the substructure in the above structural formula is a double bond, X is C, and the R1 connected to it is selected from -O- RA , -N( RD ) RB and RC . If R1 is -O- RA , then R1 is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R1 . Each R a1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group . If R1 is -N( RD )R B , then R B is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R b1 . Each R b1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group . R D is selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl ) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group , and -N(C1-6 alkyl ) 2 . If R1 is R C , then R C is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R c1 groups. Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group , 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group , where C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC 1-6 alkyl groups, -COC 1-6 alkyl groups, -CH2 COC 1-6 alkyl groups, -CH2 CON( C1-6 alkyl) 2 , -CH2 CONHC 1-6 alkyl groups, -NHC 1-6 alkyl groups, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups and 5-10 membered heteroaryl groups may all be optionally substituted with one or more substituents selected from hydroxyl groups, C1-3 alkyl groups, C1-3 alkoxy groups and halogens. below: When the substructure in the above structural formula is a single bond, X is N, and R1 connected to it is selected from C3-10 cycloalkyl groups, C3-10 cycloalkenyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C3-10 cycloalkyl groups, C3-10 cycloalkenyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by one or more identical or different R a4 and/or R b4 . Each R a4 is independently selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by one or more identical or different R b4 and/or R c4 . Each R b4 is independently selected from -OR c4 , -NR c4 R c4 , halogen, -CN, -C(O)R c4 , -C(O)OR c4 , -C(O)NR c4 R c4 , -OC(O)R c4 , -S(O) 2 R c4 , -S(O) 2NR c4 R c4 , -NHC(O)R c4 , -N( C1-4 alkyl)C(O)R c4 , -NHC(O)OR c4 , and divalent substituents =O and =NH, where =O and =NH may be substituents in a non-aromatic ring system. Each R c4 is independently selected from hydrogen, C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by one or more identical or different R d4 and/or R e4 . Each R d4 is independently selected from -OR e4 , -NR e4 R e4 , halogen, -CN, -C(O)R e4 , -C(O)OR e4 , -C(O)NR e4 R e4 , -S(O) 2 R e4 , -S(O) 2NR e4 R e4 , -NHC(O)R e4 , -N( C1-4 alkyl)C(O)R e4 , and the divalent substituent =O, where =O may be only substituents in a non-aromatic ring system. Each R e4 is independently selected from hydrogen, C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted with one or more hydrogen, cyano groups, hydroxyl groups, or halogens. Here, Z and Y are included in the atoms or number of atoms of ring A, Unless otherwise specified, the heteroatoms in the heteroaryl group and the heterocyclyl group are independently selected from O, N, and S, and the number of heteroatoms is 1, 2, 3, or 4. ) The compound according to claim 3, or its stereoisomers, optical isomers, pharmaceutical salts, solvates, or isotopic derivatives.
5. below: The substructure in the above structural formula is a double bond, where X is C, and the R1 connected to it is -O- RA . R A is selected from C1-6 alkyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R a1 groups. Each R a1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group , and -N(C1-6 alkyl ) 2 . Alternatively, R A is selected from C3-6 cycloalkyl groups, C6-10 aryl groups, 3-6 membered heterocyclyl groups, and 5-6 membered heteroaryl groups, where each of the C3-6 cycloalkyl groups, C6-10 aryl groups, 3-6 membered heterocyclyl groups, and 5-6 membered heteroaryl groups may be optionally substituted with 1 to 3 identical or different R a1 groups. Each R a1 is independently selected from halogen, hydroxyl group, cyano group, amino group, oxo group, formyl group, C1-6 alkyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, and -COC1-6 alkyl group. Alternatively, R A is selected from a 5-6 membered heterocyclyl group and a 5-6 membered heteroaryl group, where each of the 5-6 membered heterocyclyl group and the 5-6 membered heteroaryl group may be optionally substituted with 1 to 3 identical or different R a1 groups. Each R a1 is independently selected from halogen, hydroxyl group, cyano group, amino group, oxo group, formyl group, C1-4 alkyl group, -OC1-4 alkyl group, -SC1-4 alkyl group, and -COC1-4 alkyl group. Alternatively, R A is selected from a 5-6 membered heterocyclyl group, where the 5-6 membered heterocyclyl group may be optionally substituted with one or two identical or different R a1 groups. Each R a1 is independently selected from halogen, oxo group, formyl group, acetyl group, methyl group, ethyl group, n-propyl group, isopropyl group, and methoxy group. Alternatively, R A is selected from a 5-6 member monocyclic heterocyclyl group, where the 5-6 member monocyclic heterocyclyl group may be substituted with one or two identical or different R a1 groups, and each heteroatom in the 5-6 member monocyclic heterocyclyl group is independently selected from O, N, and S, with one heteroatom. Each R a1 is independently selected from halogen, oxo group, formyl group, acetyl group, methyl group, ethyl group, n-propyl group, isopropyl group, and methoxy group. Alternatively, R A is selected from a tetrahydrofuryl group, a tetrahydrothienyl group, a pyrrolidinyl group, a piperidinyl group, a tetrahydropyranyl group, and a tetrahydrothiopyranyl group, and each of the tetrahydrofuryl group, tetrahydrothienyl group, pyrrolidinyl group, piperidinyl group, tetrahydropyranyl group, and tetrahydrothiopyranyl group may be optionally substituted with one or two identical or different R a1 groups . Each R a1 is independently selected from halogen, oxo group, formyl group, acetyl group, methyl group, ethyl group, n-propyl group, isopropyl group, and methoxy group. Alternatively, R A is the following functional group: A compound selected from, according to claim 1, or a stereoisomer, optical isomer, pharmaceutical salt, solvate, or isotopic derivative thereof.
6. below: The substructure in the above structural formula is a double bond, where X is C, and the R1 connected to it is -N(R D )R B. R b1 is selected from C1-6 alkyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted with 1-3 identical or different R b1 groups . Each R b1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, and -COC1-6 alkyl group. Alternatively, R b1 is selected from C1-6 alkyl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted with 1-3 identical or different R b1 groups . Each R b1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, and -COC1-6 alkyl group. Alternatively, R B is selected from C1-6 alkyl groups and 5-6 membered monocyclic heterocyclyl groups, where each of the C1-6 alkyl groups and 5-6 membered monocyclic heterocyclyl groups may be optionally substituted with 1-2 identical or different R b1 groups, and the heteroatoms in the 5-6 membered monocyclic heterocyclyl group are independently selected from O, N, and S, with the number of heteroatoms being 1. Each R b1 is independently selected from halogen, oxo group, formyl group, C1-4 alkyl group, -OC1-4 alkyl group, and -COC1-4 alkyl group. Alternatively, R B is selected from a methyl group, an ethyl group, an n-propyl group, an isopropyl group, an oxetanyl group, a tetrahydrofuryl group, a tetrahydrothienyl group, a pyrrolidinyl group, a piperidinyl group, a tetrahydropyranyl group, and a tetrahydrothiopyranyl group, where each of the methyl group, ethyl group, n-propyl group, an isopropyl group, an oxetanyl group, a tetrahydrofuryl group, a tetrahydrothienyl group, a pyrrolidinyl group, a piperidinyl group, a tetrahydropyranyl group, and a tetrahydrothiopyranyl group may be optionally substituted by one or two identical or different R b1 groups . Each R b1 is independently selected from an oxo group, a formyl group, an acetyl group, a methyl group, an ethyl group, a methoxy group, and an ethoxy group. Alternatively, R B may be the following functional group: Selected from, R D is selected from hydrogen, C1-6 alkyl groups and -OC1-6 alkyl groups, or R D is hydrogen or C1-3 alkyl group, or R D is hydrogen or a methyl group, or R D is hydrogen. or, below: The substructure in the above structural formula is a double bond, where X is C, and the R1 connected to it is R C. R C is selected from C1-6 alkyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted with 1-3 identical or different R c1 groups . Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group , and 3-10 membered heterocyclyl group, where C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC The 1-6 alkyl groups, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC , 1-6 alkyl groups, -NHC , 1-6 alkyl groups, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl groups, and 3-10 membered heterocyclyl groups may all be optionally substituted with one or more substituents selected from hydroxyl groups, C1-3 alkyl groups, C1-3 alkoxy groups, and halogens. Alternatively, R C is selected from C1-6 alkyl groups, C3-10 cycloalkyl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C3-10 cycloalkyl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted with 1-3 identical or different R c1 groups. Each R c1 is independently selected from halogens, hydroxyl groups, cyano groups, amino groups, nitro groups, oxo groups, formyl groups, C1-4 alkyl groups, -OC1-4 alkyl groups, -SC1-4 alkyl groups, -COC1-4 alkyl groups, -CH2CON ( C1-4 alkyl ) 2 , -CH2CONHC1-4 alkyl groups, and 3-6 membered heterocyclyl groups, where each of the C1-4 alkyl groups, -OC1-4 alkyl groups, -SC1-4 alkyl groups, -COC1-4 alkyl groups, -CH2CON (C1-4 alkyl ) 2 , -CH2CONHC1-4 alkyl groups, and 3-6 membered heterocyclyl groups may be optionally substituted with one or more substituents selected from hydroxyl groups, methyl groups, methoxy groups, and halogens. Alternatively, R C is selected from a 3-10 membered heterocyclyl group and a 5-10 membered heteroaryl group, where each of the 3-10 membered heterocyclyl group and the 5-10 membered heteroaryl group may be optionally substituted with 1 to 3 identical or different R c1 groups. Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, oxo group, formyl group, C1-4 alkyl group, -OC1-4 alkyl group, -COC1-4 alkyl group, -CH2CON ( C1-4 alkyl) 2 and 3-6 membered heterocyclyl group, where the C1-4 alkyl group, -OC1-4 alkyl group, -COC1-4 alkyl group, -CH2CON ( C1-4 alkyl) 2 and 3-6 membered heterocyclyl group may be optionally substituted with one or more substituents selected from hydroxyl group , methyl group, methoxy group and halogen. Alternatively, R C is selected from a 5-6 member monocyclic heterocyclyl group, a 6-10 member spiroheterocyclyl group, a 6-8 member bridged heterocyclyl group, and a 5-6 member monocyclic heteroaryl group, where each of the 5-6 member monocyclic heterocyclyl group, the 6-10 member spiroheterocyclyl group, the 6-8 member bridged heterocyclyl group, and the 5-6 member monocyclic heteroaryl group may be optionally substituted with 1 to 3 identical or different R c1 groups. Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, oxo group, formyl group, acetyl group, propionyl group, methoxy group, ethoxy group, methyl group, ethyl group, n-propyl group, isopropyl group, -CH2CON ( CH3 ) 2 and a 6-membered heterocyclyl group, where each of the acetyl group, propionyl group, methoxy group, ethoxy group, methyl group, ethyl group, n-propyl group, isopropyl group, -CH2CON ( CH3 ) 2 and the 6-membered heterocyclyl group may be optionally substituted with one or more substituents selected from hydroxyl group, methyl group, methoxy group and halogen. Alternatively, R C is selected from a 6-membered monocyclic heterocyclyl group, a 4/6 spiroheterocyclyl group, a 4/4 spiroheterocyclyl group, a 7-membered bridged heterocyclyl group, and a 6-membered monocyclic heteroaryl group, where each of the 6-membered monocyclic heterocyclyl group, 4/6 spiroheterocyclyl group, 4/4 spiroheterocyclyl group, 7-membered bridged heterocyclyl group, and 6-membered monocyclic heteroaryl group may be optionally substituted with 1 to 3 identical or different R c1 groups. Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, oxo group, formyl group, acetyl group, -COCH₂CH₃ , -COCH₂OH , hydroxymethyl group, hydroxyethyl group, -CH₂OCH₃ , methoxy group , ethoxy group, methyl group, ethyl group, n-propyl group, isopropyl group, -CH₂CON ( CH₃ ) ₂ , and a 6-membered heterocyclyl group. Alternatively, R C is the basis of the following equation: Selected from, and each of the R Cs may be arbitrarily replaced by one or two identical or different R c1s . Each R c1 is independently selected from F, Cl, Br, hydroxyl group, cyano group, amino group, oxo group, acetyl group, -COCH₂CH₃ , -COCH₂OH , hydroxymethyl group, hydroxyethyl group, -CH₂OCH₃ , methoxy group, methyl group, ethyl group, isopropyl group, -CH₂CON ( CH₃ ) ₂ , and morpholinyl group. Alternatively, R C may be optionally substituted with R c1 , and the following functional groups: A compound selected from, according to claim 1, or a stereoisomer, optical isomer, pharmaceutical salt, solvate, or isotopic derivative thereof.
7. Ring A is a 5-10 membered heterocyclyl group or a 5-10 membered heteroaryl group, where the heteroatoms in the 5-10 membered heterocyclyl group and the 5-10 membered heteroaryl group are independently selected from O and N, and the number of heteroatoms is 1 to 4. Alternatively, ring A is selected from a 5-membered monocyclic heterocyclyl group, a 6-membered monocyclic heterocyclyl group, a 5-membered monocyclic heteroaryl group, a 6-membered monocyclic heteroaryl group, a 5/5-membered condensed heterocyclyl group, a 5/4-membered condensed heterocyclyl group, a 5/6-membered condensed heterocyclyl group, a 6/5-membered condensed heterocyclyl group, a 6/4-membered condensed heterocyclyl group, a 6/6-membered condensed heterocyclyl group, a 5/3-membered spiroheterocyclyl group, a 5/5-membered spiroheterocyclyl group, a 5/4-membered spiroheterocyclyl group, a 5/6-membered spiroheterocyclyl group, a 6/3-membered spiroheterocyclyl group, a 6/5-membered spiroheterocyclyl group, a 6/4-membered spiroheterocyclyl group, and a 6/6-membered spiroheterocyclyl group, where the 5-membered monocyclic heterocyclyl group is selected from the above. In the krill group, 6-membered monocyclic heterocyclyl group, 5-membered monocyclic heteroaryl group, 6-membered monocyclic heteroaryl group, 5/5-membered condensed heterocyclyl group, 5/4-membered condensed heterocyclyl group, 5/6-membered condensed heterocyclyl group, 6/5-membered condensed heterocyclyl group, 6/4-membered condensed heterocyclyl group, 6/6-membered condensed heterocyclyl group, 5/3-membered spiroheterocyclyl group, 5/5-membered spiroheterocyclyl group, 5/4-membered spiroheterocyclyl group, 5/6-membered spiroheterocyclyl group, 6/3-membered spiroheterocyclyl group, 6/5-membered spiroheterocyclyl group, 6/4-membered spiroheterocyclyl group, and 6/6-membered spiroheterocyclyl group, the heteroatoms are each independently nitrogen atoms, and the number of heteroatoms is 1 to 4. Alternatively, ring A is selected from a 5-membered monocyclic heterocyclyl group, a 6-membered monocyclic heterocyclyl group, a 5-membered monocyclic heteroaryl group, a 6-membered monocyclic heteroaryl group, a 5/5-membered condensed heterocyclyl group, a 5/6-membered condensed heterocyclyl group, and a 5/3-membered spiroheterocyclyl group, where the heteroatoms in the 5-membered monocyclic heterocyclyl group, 6-membered monocyclic heterocyclyl group, 5-membered monocyclic heteroaryl group, 6-membered monocyclic heteroaryl group, 5/5-membered condensed heterocyclyl group, 5/6-membered condensed heterocyclyl group, and 5/3-membered spiroheterocyclyl group are each independently nitrogen atoms, and the number of heteroatoms is 1 to 3. Alternatively, ring A is selected from a five-membered monocyclic heterocyclyl group and a five-membered monocyclic heteroaryl group, wherein the heteroatom in the five-membered monocyclic heterocyclyl group and the five-membered monocyclic heteroaryl group is N, and the number of heteroatoms is 1 to 3. Alternatively, ring A may have the following functional groups: Selected from, Alternatively, ring A may have the following functional groups: A compound selected from, according to claim 1, or a stereoisomer, optical isomer, pharmaceutical salt, solvate, or isotopic derivative thereof.
8. R2 is one, two, or three, each independently selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, formyl group, oxo group, C1-3 alkyl group, C1-3 alkoxy group, -C1-3 alkyl-NH( C1-3 alkyl) and -C1-3 alkyl-N( C1-3 alkyl) 2 , where each of the C1-3 alkyl group, C1-3 alkoxy group, -C1-3 alkyl-NH( C1-3 alkyl) and -C1-3 alkyl-N( C1-3 alkyl) 2 may be optionally substituted with one or more hydroxyl groups or halogens. Alternatively, R2 may be one, two, or three, each independently selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, formyl group, oxo group, methoxy group, methyl group, ethyl group, n-propyl group, and isopropyl group. Alternatively, R2 may be one or two, each independently selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, methoxy group, and methyl group. Alternatively, the compound according to claim 1 , or its stereoisomers, optical isomers, pharmaceutical salts, solvates, or isotopic derivatives.
9. R3 is selected from hydrogen, halogen, hydroxyl group, amino group, cyano group, C1-4 alkyl group, C1-4 alkoxy group, and C3-6 cycloalkyl group, where the C1-4 alkyl group, C1-4 alkoxy group, and C3-6 cycloalkyl group may each be optionally substituted with one or more hydroxyl groups or halogens. Alternatively, R3 may be selected from hydrogen, halogen, hydroxyl group, amino group, cyano group, methyl group, ethyl group, n-propyl group, isopropyl group, cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group and methoxy group. Alternatively, R3 is selected from hydrogen, halogen, hydroxyl group, amino group, cyano group, methyl group, ethyl group, n-propyl group, isopropyl group and cyclopropyl group. Alternatively, the compound according to claim 1 , or its stereoisomer, optical isomer, pharmaceutical salt, solvate, or isotopic derivative.
10. Ring B is selected from C4-12 cycloalkenyl groups, C4-12 heterocyclyl groups, C6-12 aryl groups, C6-8 aryl condensed C4-6 cycloalkyl groups, C6-8 aryl condensed C4-6 heterocyclyl groups, and C5-12 heteroaryl groups. Alternatively, ring B is selected from C6-10 aryl groups and C5-10 heteroaryl groups. Alternatively, the compound according to claim 1, wherein ring B is selected from a phenyl group and a pyridinyl group, or a stereoisomer, optical isomer, pharmaceutical salt, solvate, or isotopic derivative thereof.
11. Each R4 is independently selected from hydrogen, a cyano group, a halogen, an amino group, a nitro group, a C1-4 alkyl group, a C1-4 haloalkyl group, a C1-4 hydroxyalkyl group, a C3-6 cycloalkyl group, a C3-6 halocycloalkyl group, and a 3-6 membered heterocyclyl group, where each of the C1-4 alkyl group, C1-4 haloalkyl group, C1-4 hydroxyalkyl group, C3-6 cycloalkyl group, C3-6 halocycloalkyl group, and 3-6 membered heterocyclyl group may be optionally substituted with one or more substituents from among halogens, hydroxyl groups, amino groups, -SO2 -C1-4 alkyl groups, or oxo groups, and w is 0, 1, 2, or 3. Alternatively, each R4 is independently selected from hydrogen, a cyano group, a halogen, an amino group, a nitro group, a C1-4 alkyl group, a C1-4 haloalkyl group, and a C1-4 hydroxyalkyl group, where each of the C1-4 alkyl group, C1-4 haloalkyl group, and C1-4 hydroxyalkyl group may be optionally substituted with one or more substituents that are halogens, hydroxyl groups, or amino groups, and w is 1, 2, or 3. Alternatively, each R4 is independently selected from hydrogen, a cyano group, a halogen, an amino group, a nitro group, a methyl group, an ethyl group, an n-propyl group, and an isopropyl group, where the methyl group, ethyl group, n-propyl group, and isopropyl group may each be optionally substituted with one or more substituents that are halogens or hydroxyl groups, and w is 1, 2, or 3. Alternatively, each R4 is independently selected from hydrogen, halogen, amino group, methyl group, ethyl group, and isopropyl group, where the methyl group, ethyl group, and isopropyl group may each be optionally substituted with one or more substituents that are halogen or hydroxyl groups, and w is 1, 2, or 3. Alternatively, each R4 is independently selected from hydrogen, halogen, amino group, methyl group, trifluoromethyl group, difluoromethyl group, monofluoromethyl group, -CF2CH2OH , -C( CH3 ) 2OH , and -CF2CH3 , and w is 1 , 2, or 3 , the compound according to claim 1, or its stereoisomer, optical isomer, pharmaceutical salt, solvate, or isotopic derivative.
12. The following equation (B): (In the formula, R1 is selected from -O- RA , -N( RD ) RB and RC , If R1 is -O- RA , then R1 is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R1 . Each R a1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group . If R1 is -N( RD )R B , then R B is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R b1 . Each R b1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group . R D is selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl ) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group , and -N(C1-6 alkyl ) 2 . If R1 is R C , then R C is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 4 identical or different R c1 groups. Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, methanesulfonyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -COC3-6 cycloalkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N (C1-6 alkyl ) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group, where the C1-6 alkyl group, C2-6 alkenyl group , C 2-6 alkynyl groups, -OC 1-6 alkyl groups, -SC 1-6 alkyl groups, -COC 1-6 alkyl groups, -COC 3-6 cycloalkyl groups, -CH2 COC 1-6 alkyl groups, -CH2 CON (C 1-6 alkyl) 2 , -CH2 CONHC 1-6 alkyl groups, -NHC 1-6 alkyl groups, -N (C 1-6 alkyl) 2 , C 3-10 cycloalkyl groups, C 6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may all be optionally substituted with one or more substituents selected from deuterium, hydroxyl groups, cyano groups, C 1-3 alkyl groups, C 1-3 alkoxy groups, and halogens. R2 is one or two, each independently selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, formyl group, oxo group, C1-6 alkyl group, C1-6 alkoxy group, halo- C1-6 alkyl group and halo -C1-6 alkoxy group. R3 is selected from hydrogen, halogen, hydroxyl group, amino group, cyano group, C1-6 alkyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, and 3-6 membered heterocyclyl group, where the C1-6 alkyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, and 3-6 membered heterocyclyl group may each be optionally substituted with one or more hydroxyl groups or halogens. Ring B is selected from C4-12 cycloalkyl groups, C4-12 cycloalkenyl groups, C4-12 heterocyclyl groups, C6-12 aryl groups, C5-12 heteroaryl groups, C6-12 aryl-condensed C4-12 cycloalkyl groups, C6-12 aryl -condensed C4-12 heterocyclyl groups, and C6-12 aryl-condensed C4-12 cycloalkenyl groups. Each R4 is independently selected from hydrogen, cyano group, halogen, amino group, hydroxyl group, oxo group, nitro group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, C1-6 haloalkyl group, C1-6 hydroxyalkyl group, C1-6 alkoxy group, -C0-6 alkyl-NH- C1-6 alkyl group, -C0-6 alkyl-N( C1-6 alkyl)( C1-6 alkyl), C3-6 cycloalkyl group, C3-6 halocycloalkyl group, and 3-6 membered heterocyclyl group, where the C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, C1-6 haloalkyl group, C1-6 hydroxyalkyl group, C1-6 alkoxy group, -C0-6 alkyl-NH- C1-6 alkyl group, and -C0-6 alkyl-N(C The 1-6 alkyl ( C1-6 alkyl), C3-6 cycloalkyl, C3-6 halocycloalkyl and 3-6 membered heterocyclyl groups may all be optionally substituted with one or more substituents from among halogens, hydroxyl groups, amino groups, -SO2- C1-4 alkyl groups, and oxo groups, where w is 0, 1, 2, 3, or 4. Unless otherwise specified, the heteroatoms in the heteroaryl group and heterocyclyl group are independently selected from O, N, and S, and the number of heteroatoms is one, two, three, or four. Compounds, or their stereoisomers, optical isomers, pharmaceutical salts, solvates, or isotopic derivatives.
13. The aforementioned compound is given by the following formula (C): (In the formula, R1 is selected from -O- RA , -N( RD ) RB and RC , If R1 is -O- RA , then R1 is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R1 . Each R a1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group . If R1 is -N( RD )R B , then R B is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R b1 . Each R b1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group . R D is selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl ) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group , and -N(C1-6 alkyl ) 2 . If R1 is R C , then R C is selected from C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C2-6 alkenyl groups, C2-6 alkynyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 4 identical or different R c1 groups. Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, methanesulfonyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -COC3-6 cycloalkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N (C1-6 alkyl ) 2 , C3-10 cycloalkyl group, C6-10 aryl group, 3-10 membered heterocyclyl group, and 5-10 membered heteroaryl group, where the C1-6 alkyl group, C2-6 alkenyl group , C 2-6 alkynyl groups, -OC 1-6 alkyl groups, -SC 1-6 alkyl groups, -COC 1-6 alkyl groups, -COC 3-6 cycloalkyl groups, -CH2 COC 1-6 alkyl groups, -CH2 CON (C 1-6 alkyl) 2 , -CH2 CONHC 1-6 alkyl groups, -NHC 1-6 alkyl groups, -N (C 1-6 alkyl) 2 , C 3-10 cycloalkyl groups, C 6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may all be optionally substituted with one or more substituents selected from deuterium, hydroxyl groups, cyano groups, C 1-3 alkyl groups, C 1-3 alkoxy groups, and halogens. R2 is one or two, each independently selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, formyl group, oxo group, C1-6 alkyl group, C1-6 alkoxy group, halo- C1-6 alkyl group and halo -C1-6 alkoxy group. R3 is selected from hydrogen, halogen, hydroxyl group, amino group, cyano group, C1-6 alkyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, and 3-6 membered heterocyclyl group, where the C1-6 alkyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, and 3-6 membered heterocyclyl group may each be optionally substituted with one or more hydroxyl groups or halogens. Ring B is selected from C4-12 cycloalkyl groups, C4-12 cycloalkenyl groups, C4-12 heterocyclyl groups, C6-12 aryl groups, C5-12 heteroaryl groups, C6-12 aryl-condensed C4-12 cycloalkyl groups, C6-12 aryl -condensed C4-12 heterocyclyl groups, and C6-12 aryl-condensed C4-12 cycloalkenyl groups. Each R4 is independently selected from hydrogen, cyano group, halogen, amino group, hydroxyl group, oxo group, nitro group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, C1-6 haloalkyl group, C1-6 hydroxyalkyl group, C1-6 alkoxy group, -C0-6 alkyl-NH- C1-6 alkyl group, -C0-6 alkyl-N( C1-6 alkyl)( C1-6 alkyl), C3-6 cycloalkyl group, C3-6 halocycloalkyl group, and 3-6 membered heterocyclyl group, where the C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, C1-6 haloalkyl group, C1-6 hydroxyalkyl group, C1-6 alkoxy group, -C0-6 alkyl-NH- C1-6 alkyl group, and -C0-6 alkyl-N(C The 1-6 alkyl ( C1-6 alkyl), C3-6 cycloalkyl, C3-6 halocycloalkyl, and 3-6 membered heterocyclyl groups may all be optionally substituted with one or more substituents, which are halogens, hydroxyl groups, amino groups, -SO2- C1-4 alkyl groups, or oxo groups, where w is 0, 1, 2, 3 , or 4. Unless otherwise specified, the heteroatoms in the heteroaryl group and the heterocyclyl group are independently selected from O, N, and S, and the number of heteroatoms is 1, 2, 3, or 4. ) The compound according to claim 12, or its stereoisomers, optical isomers, pharmaceutical salts, solvates, or isotopic derivatives.
14. When R1 is -O- RA , R1 is selected from C1-6 alkyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different R1s . Each R a1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, C2-6 alkenyl group, C2-6 alkynyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group , and -N(C1-6 alkyl ) 2 . Alternatively, R A is selected from C3-6 cycloalkyl groups, C6-10 aryl groups, 3-6 membered heterocyclyl groups, and 5-6 membered heteroaryl groups, where each of the C3-6 cycloalkyl groups, C6-10 aryl groups, 3-6 membered heterocyclyl groups, and 5-6 membered heteroaryl groups may be optionally substituted with 1 to 3 identical or different R a1 groups. Each R a1 is independently selected from halogen, hydroxyl group, cyano group, amino group, oxo group, formyl group, C1-6 alkyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, and -COC1-6 alkyl group. Alternatively, R A is selected from a 5-6 membered heterocyclyl group and a 5-6 membered heteroaryl group, where each of the 5-6 membered heterocyclyl group and the 5-6 membered heteroaryl group may be optionally substituted with 1 to 3 identical or different R a1 groups. Each R a1 is independently selected from halogen, hydroxyl group, cyano group, amino group, oxo group, formyl group, C1-4 alkyl group, -OC1-4 alkyl group, -SC1-4 alkyl group, and -COC1-4 alkyl group. Alternatively, R A is a 5-6 membered heterocyclyl group, where the 5-6 membered heterocyclyl group may be optionally substituted with one or two identical or different R a1 groups. Each R a1 is independently selected from halogen, oxo group, formyl group, acetyl group, methyl group, ethyl group, n-propyl group, isopropyl group, and methoxy group. Alternatively, R A is a 5-6 member monocyclic heterocyclyl group, where the 5-6 member monocyclic heterocyclyl group may be substituted with one or two identical or different R a1 groups, and each heteroatom in the 5-6 member monocyclic heterocyclyl group is independently selected from O, N, and S, with one heteroatom. Each R a1 is independently selected from halogen, oxo group, formyl group, acetyl group, methyl group, ethyl group, n-propyl group, isopropyl group, and methoxy group. Alternatively, R A is selected from a tetrahydrofuryl group, a tetrahydrothienyl group, a pyrrolidinyl group, a piperidinyl group, a tetrahydropyranyl group, and a tetrahydrothiopyranyl group, and each of the tetrahydrofuryl group, tetrahydrothienyl group, pyrrolidinyl group, piperidinyl group, tetrahydropyranyl group, and tetrahydrothiopyranyl group may be optionally substituted with one or two identical or different R a1 groups . Each R a1 is independently selected from halogen, oxo group, formyl group, acetyl group, methyl group, ethyl group, n-propyl group, isopropyl group, and methoxy group. Alternatively, R A is the following functional group: Selected from, When R1 is -N( RD ) Rb , Rb is selected from C1-6 alkyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 3 identical or different Rb1 groups. Each R b1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, and -COC1-6 alkyl group. Alternatively, R b1 is selected from C1-6 alkyl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C1-6 alkyl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted with 1-3 identical or different R b1 groups . Each R b1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, C1-6 alkyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, and -COC1-6 alkyl group. Alternatively, R B is selected from C1-6 alkyl groups and 5-6 membered monocyclic heterocyclyl groups, where each of the C1-6 alkyl groups and 5-6 membered monocyclic heterocyclyl groups may be optionally substituted with 1-2 identical or different R b1 groups, and the heteroatoms in the 5-6 membered monocyclic heterocyclyl group are independently selected from O, N, and S, with the number of heteroatoms being 1. Each R b1 is independently selected from halogen, oxo group, formyl group, C1-4 alkyl group, -OC1-4 alkyl group, and -COC1-4 alkyl group. Alternatively, R B is selected from a methyl group, an ethyl group, an n-propyl group, an isopropyl group, an oxetanyl group, a tetrahydrofuryl group, a tetrahydrothienyl group, a pyrrolidinyl group, a piperidinyl group, a tetrahydropyranyl group, and a tetrahydrothiopyranyl group, where each of the methyl group, ethyl group, n-propyl group, an isopropyl group, an oxetanyl group, a tetrahydrofuryl group, a tetrahydrothienyl group, a pyrrolidinyl group, a piperidinyl group, a tetrahydropyranyl group, and a tetrahydrothiopyranyl group may be optionally substituted by one or two identical or different R b1 groups . Each R b1 is independently selected from an oxo group, a formyl group, an acetyl group, a methyl group, an ethyl group, a methoxy group, and an ethoxy group. Alternatively, R B may be the following functional group: Selected from, R D is selected from hydrogen, C1-6 alkyl groups and -OC1-6 alkyl groups, or R D is hydrogen or C1-3 alkyl group, or R D is hydrogen or a methyl group, or R D is hydrogen . When R1 is R C , R C is selected from C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C3-10 cycloalkyl groups, C6-10 aryl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted by 1 to 4 identical or different R c1 groups. Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, methanesulfonyl group, C1-6 alkyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -COC3-6 cycloalkyl group , -CH2COC1-6 alkyl group, -CH2CON ( C1-6 alkyl) 2 , -CH2CONHC1-6 alkyl group, -NHC1-6 alkyl group, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl group, and 3-10 membered heterocyclyl group, where C1-6 alkyl group, -OC1-6 alkyl group, -SC1-6 alkyl group, -COC1-6 alkyl group, -COC3-6 cycloalkyl group, -CH2COC1-6 alkyl group, -CH2CON ( C The 1-6 alkyl) 2 , -CH2CONHC 1-6 alkyl, -NHC 1-6 alkyl, -N( C1-6 alkyl) 2 , C3-10 cycloalkyl and 3-10 membered heterocyclyl groups may all be optionally substituted with one or more substituents selected from deuterium, hydroxyl groups, cyano groups, C1-3 alkyl groups, C1-3 alkoxy groups, and halogens. Alternatively, R C is selected from C3-10 cycloalkyl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups, where each of the C3-10 cycloalkyl groups, 3-10 membered heterocyclyl groups, and 5-10 membered heteroaryl groups may be optionally substituted with 1 to 4 identical or different R c1 groups . Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, nitro group, oxo group, formyl group, methanesulfonyl group , C1-4 alkyl group, -OC1-4 alkyl group, -SC1-4 alkyl group, -COC1-4 alkyl group, -COC3-6 cycloalkyl group, -CH2COC1-4 alkyl group, -CH2CON ( C1-4 alkyl ) 2 , -CH2CONHC1-4 alkyl group, C3-6 cycloalkyl group, and 3-6 membered heterocyclyl group, where C1-4 alkyl group, -OC1-4 alkyl group, -SC1-4 alkyl group, -COC1-4 alkyl group, -COC3-6 cycloalkyl group, -CH2COC1-4 alkyl group , -CH2CON(C1-4 alkyl)2 , -CH2CONHC1-4 alkyl group , C The 3-6 cycloalkyl groups and 3-6 membered heterocyclyl groups may each be optionally substituted with one or more substituents selected from deuterium, hydroxyl groups, cyano groups, C1-3 alkyl groups, C1-3 alkoxy groups, and halogens. Alternatively, R C is selected from a 3-10 membered heterocyclyl group and a 5-10 membered heteroaryl group, where each of the 3-10 membered heterocyclyl group and the 5-10 membered heteroaryl group may be optionally substituted with 1 to 4 identical or different R c1 groups. Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, oxo group, formyl group, methanesulfonyl group, C1-4 alkyl group, -OC1-4 alkyl group, -COC1-4 alkyl group, -COC3-6 cycloalkyl group, -CH2CON ( C1-4 alkyl) 2 and 3-6 membered heterocyclyl group, where the C1-4 alkyl group, -OC1-4 alkyl group, -COC1-4 alkyl group, -COC3-6 cycloalkyl group, -CH2CON ( C1-4 alkyl) 2 and 3-6 membered heterocyclyl group may be optionally substituted with one or more substituents selected from deuterium, hydroxyl group, cyano group, methyl group, methoxy group and halogen. Alternatively, R C is selected from a 5-6 member monocyclic heterocyclyl group, a 6-10 member spiroheterocyclyl group, a 6-8 member bridged heterocyclyl group, an 8-10 member condensed heterocyclyl group, and a 5-6 member monocyclic heteroaryl group, where each of the 5-6 member monocyclic heterocyclyl group, 6-10 member spiroheterocyclyl group, 6-8 member bridged heterocyclyl group, 8-10 member condensed heterocyclyl group, and 5-6 member monocyclic heteroaryl group may be optionally substituted with 1 to 4 identical or different R c1 groups. Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, oxo group, formyl group, acetyl group, propionyl group, methanesulfonyl group, methoxy group, ethoxy group, methyl group, ethyl group, n-propyl group, isopropyl group, -CH₂CON ( CH₃ ) ₂ , -CO-cyclopropyl group, -CO-cyclobutyl group, 4-membered heterocyclyl group, 5-membered heterocyclyl group, and 6-membered heterocyclyl group, where the acetyl group, propionyl group, methanesulfonyl group, methoxy group, ethoxy group, methyl group, ethyl group, n-propyl group, isopropyl group, -CH₂CON ( CH₃ ) ₂ The -CO-cyclopropyl group, -CO-cyclobutyl group, 4-membered heterocyclyl group, 5-membered heterocyclyl group, and 6-membered heterocyclyl group may each be optionally substituted with one or more substituents selected from deuterium, hydroxyl group, cyano group, methyl group, methoxy group, and halogen. Alternatively, R C is selected from a 6-membered monocyclic heterocyclyl group, a 4-membered/6-membered spiroheterocyclyl group, a 4-membered/4-membered spiroheterocyclyl group, a 6-membered/5-membered condensed heterocyclyl group, a 7-membered bridged heterocyclyl group, and a 6-membered monocyclic heteroaryl group, where the 6-membered monocyclic heterocyclyl group, the 4-membered/6-membered spiroheterocyclyl group, the 4-membered/4-membered spiroheterocyclyl group, the 6-membered/4-membered condensed heterocyclyl group, the 7-membered bridged heterocyclyl group, and the 6-membered monocyclic heteroaryl group may each be optionally substituted with 1 to 4 identical or different R c1 groups. Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, oxo group, formyl group, acetyl group, propionyl group, methanesulfonyl group, methoxy group, ethoxy group, methyl group, ethyl group, n-propyl group, isopropyl group, -CH2CON ( CH3 ) 2 , -CO-cyclopropyl group, 4-membered heterocyclyl group, 5-membered heterocyclyl group, and 6-membered heterocyclyl group, where the acetyl group, propionyl group, methanesulfonyl group, methoxy group, ethoxy group, methyl group, ethyl group, n-propyl group, isopropyl group, -CH2CON ( CH3 ) 2 , -CO-cyclopropyl group, 4-membered heterocyclyl group, 5-membered heterocyclyl group, and 6-membered heterocyclyl group may be optionally substituted with one or more substituents selected from deuterium, hydroxyl group, cyano group, methyl group, methoxy group, and halogen. Alternatively, R C is the basis of the following equation: Selected from, and each of the R Cs may be arbitrarily replaced by 1 to 4 identical or different R c1s . Each R c1 is independently F, Cl, Br, hydroxyl group, cyano group, amino group, oxo group, methanesulfonyl group, acetyl group, -COCH₂CH₃ , -COCH₂OH , -COCH₂CN , -CH(OH)( CH₃ ) ₂ , hydroxymethyl group, hydroxyethyl group, -CH₂OCH₃ , -CH₂CH₂OCH₃ , methoxy group, methyl group, CD₃ , ethyl group, isopropyl group, monofluoromethyl group, difluoromethyl group, trifluoromethyl group, monofluoroethyl group, difluoroethyl group, trifluoroethyl group, and the group shown in the following formula . - Selected from CH₂CON ( CH₃ ) ₂ and morpholinyl groups, Alternatively, R C may be optionally substituted with R c1 , and the following functional groups: A compound according to claim 12, selected from the above, or a stereoisomer, optical isomer, pharmaceutical salt, solvate, or isotopic derivative thereof.
15. R2 is one or two, each independently selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, formyl group, oxo group, methoxy group, methyl group, ethyl group, n-propyl group, and isopropyl group. Alternatively, R2 may be one or two, each independently selected from hydrogen, halogen, hydroxyl group, cyano group, amino group, nitro group, methoxy group, and methyl group. Alternatively, R2 may be one or two, each independently selected from hydrogen and a methyl group. Alternatively, the compound according to claim 12, or a stereoisomer, optical isomer, pharmaceutical salt, solvate, or isotopic derivative thereof, wherein R2 is hydrogen.
16. R3 is selected from hydrogen, halogen, hydroxyl group, amino group, cyano group, methyl group, ethyl group, n-propyl group, isopropyl group, cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group and methoxy group. Alternatively, R3 is selected from hydrogen, halogen, hydroxyl group, amino group, cyano group, methyl group, ethyl group, n-propyl group, isopropyl group and cyclopropyl group. Alternatively, the compound according to claim 12 , or its stereoisomer, optical isomer, pharmaceutical salt, solvate, or isotopic derivative.
17. Ring B is selected from C4-12 cycloalkenyl groups, 4-12 membered heterocyclyl groups, C6-12 aryl groups, C6-8 aryl condensed C4-6 cycloalkyl groups, C6-8 aryl condensed 4-6 membered heterocyclyl groups, and 5-12 membered heteroaryl groups. Alternatively, ring B may be selected from C6-10 aryl groups, 5-10 membered heteroaryl groups, and C6-8 aryl condensed 4-6 membered heterocyclyl groups. Alternatively, the compound according to claim 12, wherein ring B is selected from a phenyl group, a pyridinyl group, and a benzotetrahydrofuryl group, or a stereoisomer, optical isomer, pharmaceutical salt, solvate, or isotopic derivative thereof.
18. Each R4 is independently selected from hydrogen, a cyano group, a halogen, an amino group, a nitro group, a C1-4 alkyl group, a C1-4 haloalkyl group, a C1-4 hydroxyalkyl group, a C3-6 cycloalkyl group, a C3-6 halocycloalkyl group, and a 3-6 membered heterocyclyl group, where each of the C1-4 alkyl group, C1-4 haloalkyl group, C1-4 hydroxyalkyl group, C3-6 cycloalkyl group, C3-6 halocycloalkyl group, and 3-6 membered heterocyclyl group may be optionally substituted with one or more substituents from among halogens, hydroxyl groups, amino groups, -SO2 -C1-4 alkyl groups, or oxo groups, and w is 0, 1, 2, or 3. Alternatively, each R4 is independently selected from hydrogen, a cyano group, a halogen, an amino group, a nitro group, a C1-4 alkyl group, a C1-4 haloalkyl group, and a C1-4 hydroxyalkyl group, where each of the C1-4 alkyl group, C1-4 haloalkyl group, and C1-4 hydroxyalkyl group may be optionally substituted with one or more substituents that are halogens, hydroxyl groups, or amino groups, and w is 1, 2, or 3. Alternatively, each R4 is independently selected from hydrogen, a cyano group, a halogen, an amino group, a nitro group, a methyl group, an ethyl group, an n-propyl group, and an isopropyl group, where the methyl group, ethyl group, n-propyl group, and isopropyl group may each be optionally substituted with one or more substituents that are halogens or hydroxyl groups, and w is 1, 2, or 3. Alternatively, each R4 is independently selected from hydrogen, halogen, amino group, cyano group, methyl group, ethyl group, and isopropyl group, where the methyl group, ethyl group, and isopropyl group may each be optionally substituted with one or more substituents that are halogen or hydroxyl groups, and w is 1, 2, or 3. Alternatively, each R4 is independently selected from hydrogen, fluorine, amino group, cyano group, methyl group, trifluoromethyl group, difluoromethyl group, monofluoromethyl group, -CF2CH2OH , -C( CH3 ) 2OH , -CF2CH3 and -CH2CHF2 , and w is 1, 2 or 3 , the compound according to claim 12 , or its stereoisomers, optical isomers, pharmaceutical salts, solvates or isotopic derivatives.
19. The following equation (D): (In the formula, each R4 is independently selected from a cyano group, a halogen, an amino group, a C1-6 alkyl group, and a C1-6 haloalkyl group, where each of the C1-6 alkyl groups and C1-6 haloalkyl groups may be optionally substituted with one or more hydroxyl groups, and w is 1 or 2.) R1 is selected from -O- RA , -N( RD ) RB and RC , If R1 is -O- RA , then RA is selected from a 3- to 10-membered heterocyclyl group, where the 3- to 10-membered heterocyclyl group may be optionally substituted by 1 to 3 identical or different R a1 groups . Each R a1 is independently selected from C1-6 alkyl groups and -COC1-6 alkyl groups. If R1 is -N( RD ) RB , then RB is selected from C1-6 alkyl groups and 3-10 membered heterocyclyl groups, where each of the C1-6 alkyl groups and 3-10 membered heterocyclyl groups may be optionally substituted by 1-3 identical or different Rb1 groups . Each R b1 is independently a -OC1-6 alkyl group. R D is hydrogen, If R1 is R C , then R C is selected from a 3-10 membered heterocyclyl group and a 5-10 membered heteroaryl group, where the 3-10 membered heterocyclyl group and the 5-10 membered heteroaryl group may each be optionally substituted by 1 to 4 identical or different R c1 groups. Each R c1 is independently selected from halogens, hydroxyl groups, cyano groups, amino groups, methanesulfonyl groups, C1-6 alkyl groups, -OC1-6 alkyl groups, -COC1-6 alkyl groups, -COC3-6 cycloalkyl groups, -CH2CON ( C1-6 alkyl) 2 and 3-10 membered heterocyclyl groups, where each of the C1-6 alkyl groups, -OC1-6 alkyl groups, -COC1-6 alkyl groups, -COC3-6 cycloalkyl groups, -CH2CON ( C1-6 alkyl) 2 and 3-10 membered heterocyclyl groups may be optionally substituted with one or more substituents selected from deuterium, hydroxyl groups, cyano groups, C1-3 alkoxy groups and halogens. Unless otherwise specified, the heteroatoms in the heteroaryl group and the heterocyclyl group are independently selected from O, N, and S, and the number of heteroatoms is one, two, three, or four .) A compound represented by this symbol, or its stereoisomers, optical isomers, pharmaceutical salts, solvates, or isotopic derivatives.
20. When R1 is -O- RA , R1 is a 3- to 6-membered heterocyclyl group, where the 3- to 6-membered heterocyclyl group may be optionally substituted by 1 to 3 identical or different R1s . Each R a1 is independently selected from C1-6 alkyl groups and -COC1-6 alkyl groups. Alternatively, R A is a 5-6 membered heterocyclyl group, where the 5-6 membered heterocyclyl group may be optionally substituted with one or two identical or different R a1 groups. Each R a1 is independently selected from an acetyl group, a methyl group, an ethyl group, an n-propyl group, and an isopropyl group. Alternatively, R A is a 5-6 member monocyclic heterocyclyl group, where the 5-6 member monocyclic heterocyclyl group may be substituted with one or two identical or different R a1 groups, and each heteroatom in the 5-6 member monocyclic heterocyclyl group is independently selected from O, N, and S, with one heteroatom. Each R a1 is independently selected from an acetyl group, a methyl group, and an ethyl group. Alternatively, R A is selected from a tetrahydrofuryl group, a tetrahydrothienyl group, a pyrrolidinyl group, a piperidinyl group, a tetrahydropyranyl group, and a tetrahydrothiopyranyl group, and each of the tetrahydrofuryl group, tetrahydrothienyl group, pyrrolidinyl group, piperidinyl group, tetrahydropyranyl group, and tetrahydrothiopyranyl group may be optionally substituted with one or two identical or different R a1 groups . Each R a1 is independently selected from an acetyl group, a methyl group, and an ethyl group. Alternatively, R A is the following functional group: Selected from, When R1 is -N( RD ) Rb , Rb is selected from C1-6 alkyl groups and 3-6 membered monocyclic heterocyclyl groups, where each of the C1-6 alkyl groups and 3-6 membered monocyclic heterocyclyl groups may be optionally substituted with 1-2 identical or different Rb1 groups, and the heteroatoms in the 3-6 membered monocyclic heterocyclyl group are independently selected from O, N, and S, with the number of heteroatoms being 1. Each R b1 is independently a -OC1-4 alkyl group. Alternatively, R B is selected from a methyl group, an ethyl group, an n-propyl group, an isopropyl group, an oxetanyl group, a tetrahydrofuryl group, a tetrahydrothienyl group, a pyrrolidinyl group, a piperidinyl group, a tetrahydropyranyl group, and a tetrahydrothiopyranyl group, where each of the methyl group, ethyl group, n-propyl group, an isopropyl group, an oxetanyl group, a tetrahydrofuryl group, a tetrahydrothienyl group, a pyrrolidinyl group, a piperidinyl group, a tetrahydropyranyl group, and a tetrahydrothiopyranyl group may be optionally substituted by one or two identical or different R b1 groups . Each R b1 is independently selected from a methoxy group and an ethoxy group. Alternatively, R B may be the following functional group: Selected from, R D is selected from hydrogen, C1-6 alkyl groups and -OC1-6 alkyl groups, or R D is hydrogen or C1-3 alkyl group, or R D is hydrogen or a methyl group, or R D is hydrogen. When R1 is R C , R C is selected from a 3-10 membered heterocyclyl group and a 5-10 membered heteroaryl group, where the 3-10 membered heterocyclyl group and the 5-10 membered heteroaryl group may each be optionally substituted by 1 to 4 identical or different R c1 groups. Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, methanesulfonyl group, C1-4 alkyl group, -OC1-4 alkyl group, -COC1-4 alkyl group, -COC3-6 cycloalkyl group, -CH2CON ( C1-4 alkyl) 2 and 3-6 membered heterocyclyl group, where the C1-4 alkyl group , -OC1-4 alkyl group, -COC1-4 alkyl group, -COC3-6 cycloalkyl group, -CH2CON ( C1-4 alkyl) 2 and 3-6 membered heterocyclyl group may be optionally substituted with one or more substituents selected from deuterium, hydroxyl group, cyano group, methoxy group and halogen. Alternatively, R C is selected from a 5-6 member monocyclic heterocyclyl group, a 6-10 member spiroheterocyclyl group, a 6-8 member bridged heterocyclyl group, an 8-10 member condensed heterocyclyl group, and a 5-6 member monocyclic heteroaryl group, where each of the 5-6 member monocyclic heterocyclyl group, 6-10 member spiroheterocyclyl group, 6-8 member bridged heterocyclyl group, 8-10 member condensed heterocyclyl group, and 5-6 member monocyclic heteroaryl group may be optionally substituted with 1 to 4 identical or different R c1 groups. Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, methanesulfonyl group, methyl group, ethyl group, n-propyl group, isopropyl group, methoxy group, ethoxy group, acetyl group, propionyl group, -CO-cyclopropyl group, -CO-cyclobutyl group, -CH2CON ( CH3 ) 2 , 4-membered heterocyclyl group, 5-membered heterocyclyl group, and 6-membered heterocyclyl group, where the methanesulfonyl group, methyl group, ethyl group, n-propyl group, isopropyl group, methoxy group, ethoxy group, acetyl group, propionyl group, -CO-cyclopropyl group, -CO-cyclobutyl group, -CH2CON ( CH3 ) 2 , 4-membered heterocyclyl group, 5-membered heterocyclyl group, and 6-membered heterocyclyl group may be optionally substituted with one or more substituents selected from deuterium, hydroxyl group, cyano group, methoxy group, and halogen. Alternatively, R C is selected from a 6-membered monocyclic heterocyclyl group, a 4-membered/6-membered spiroheterocyclyl group, a 4-membered/4-membered spiroheterocyclyl group, a 7-membered bridged heterocyclyl group, a 6-membered/5-membered condensed heterocyclyl group, and a 6-membered monocyclic heteroaryl group, where the 6-membered monocyclic heterocyclyl group, the 4-membered/6-membered spiroheterocyclyl group, the 4-membered/4-membered spiroheterocyclyl group, the 7-membered bridged heterocyclyl group, the 6-membered/4-membered condensed heterocyclyl group, and the 6-membered monocyclic heteroaryl group may each be optionally substituted with 1 to 4 identical or different R c1 groups. Each R c1 is independently selected from halogen, hydroxyl group, cyano group, amino group, methanesulfonyl group, methyl group, ethyl group, n-propyl group, isopropyl group, methoxy group, ethoxy group, acetyl group, propionyl group, -CO-cyclopropyl group, -CH2CON ( CH3 ) 2 , 4-membered heterocyclyl group, 5-membered heterocyclyl group, and 6-membered heterocyclyl group, where the methanesulfonyl group, methyl group, ethyl group, n-propyl group, isopropyl group, methoxy group, ethoxy group, acetyl group, propionyl group, -CO-cyclopropyl group, 4-membered heterocyclyl group, 5-membered heterocyclyl group, and 6-membered heterocyclyl group may be optionally substituted with one or more substituents selected from deuterium, hydroxyl group, cyano group, methoxy group, and halogen. Alternatively, R C is the basis of the following equation: Selected from, and each of the R Cs may be arbitrarily replaced by 1 to 4 identical or different R c1s . Each R c1 independently contains F, Cl, Br, hydroxyl group, cyano group, amino group, methanesulfonyl group, methyl group, ethyl group, isopropyl group, CD3 , hydroxymethyl group, hydroxyethyl group (e.g., 2-hydroxyethyl group), -CH(OH)( CH3 ) 2 , -CH2OCH3 , -CH2CH2OCH3 , monofluoromethyl group, difluoromethyl group, trifluoromethyl group, monofluoroethyl group ( e.g., 2-fluoroethyl group), difluoroethyl group (e.g., 2,2 - difluoroethyl group), trifluoroethyl group ( e.g., 2,2,2-trifluoroethyl group), methoxy group, acetyl group, -COCH2CH3 , -COCH2OH , -COCH2CN , and the following groups: -CH₂CON ( CH₃ ) ₂ , and oxetanyl groups (for example, the following groups: ) and a morpholinyl group (for example, morpholin-4-yl) are selected, Alternatively, R C may be optionally substituted with R c1 , and the following functional groups: Selected from, Each R4 is independently selected from a cyano group, a halogen, an amino group, a C1-4 alkyl group, and a C1-4 haloalkyl group, where each of the C1-4 alkyl groups and C1-4 haloalkyl groups may be optionally substituted with one or more hydroxyl groups, and w is 1 or 2. Alternatively, each R4 is independently selected from a cyano group, fluorine, amino group, methyl group, trifluoromethyl group, difluoromethyl group, monofluoromethyl group, -CF2CH2OH , -CF2C ( CH3 ) 2OH , -CF2CH3 and -CH2CHF2 , and w is 1 or 2, the compound according to claim 19 , or its stereoisomer, optical isomer, pharmaceutical salt, solvate or isotopic derivative.

Description

This invention claims priority to the patent application filed in China on December 17, 2021, titled "Heterocyclic Compounds Having Antitumor Activity and Uses Thereof," application number 202111561282.9, and the patent application filed in China on June 7, 2022, titled "Heterocyclic Compounds Having Antitumor Activity and Uses Thereof," application number 202210634934.5, and incorporates these patent applications as a whole by reference. This invention relates to the field of medical technology, and more specifically to compounds as SOS1 inhibitors, as well as compositions, manufacturing methods, and uses of said compounds. Currently, three genes are known in the RAS family: KRAS (Kirsten rat sarcoma virus oncogene homolog), NRAS (neuroblastoma RAS virus oncogene homolog), and HRAS (Harvey rat sarcoma virus oncogene). RAS family proteins are low molecular weight GTPases and were the first oncogenes identified in human tumors. RAS family proteins have weak intrinsic GTPase activity and slow nucleotide exchange rates. For example, binding of NF1 to GTPase-activating protein (GAP) increases the GTPase activity of RAS family proteins. Mutations in RAS proteins are closely related to tumor development, and the type of RAS mutation varies depending on the tumor type. In human tumors, KRAS mutations (e.g., amino acids G12, G13, Q61, A146) are the most common, accounting for approximately 85%, while NRAS (e.g., amino acids G12, G13, Q61, A146) and HRAS (e.g., amino acids G12, G13, Q61) account for 12% and 3%, respectively. Changes in RAS family proteins (e.g., mutations, overexpression, gene amplification) have been described as mechanisms of resistance to the anticancer drugs EGFR antibodies cetuximab and panitumumab, and the EGFR tyrosine kinase inhibitor osimertinib. In oncogenic RAS mutants, GAP activity is weakened or significantly reduced, leading to persistent activation, which forms the basis of oncogenic RAS signaling. Direct inhibition of the RAS is already proven to be highly challenging and unpromising due to the picomolar affinity of GTP to its binding site, the lack of other clearly defined pockets, and the extended, flat protein-protein interactions of the RAS with GEF, GAP, and effectors. Therefore, targeting the upstream guanine nucleotide exchange factor, the SOS protein, to inhibit RAS activation is considered promising. There are two human isotypes of SOS, SOS1 and SOS2, but the vast majority of research focuses on SOS1. Human SOS1 contains 1333 amino acids (15 kDa) and its components include an N-terminal histone-like domain, a Dbl homolog (DH) domain, a pleckstrin homolog (PH) domain, a helical linker (HL), a Ras exchange motif (Rem) domain, a Cdc25 domain, and a C-terminal region. Of these, PH, Rem, and Cdc25 are components of the SOS cat core catalytic domain. Over the past several decades, RAS family protein-SOS1 protein interactions have been increasingly recognized. Recently, research has also been conducted on screening and identifying small molecular weight inhibitors of SOS1—that is, compounds that bind to SOS1 and inhibit protein-protein interactions with RAS family proteins—by combining rational design and screening platforms. For example, WO2021105960A1 describes various fused-ring SOS1 inhibitors. While several SOS1 small molecule inhibitors have been disclosed, none of the SOS1 inhibitors currently under development have reached the market. Therefore, developing new compounds with better efficacy and pharmacokinetic properties that have commercial potential remains an urgent task. (Definition of terms) The terms "optional,""atwill,""atwill," or "may be at will" mean that the event or situation described thereafter may occur, but is not necessarily guaranteed to occur, and the description includes both cases where the event or situation occurs and cases where it does not. Unless otherwise specified, the term "alkyl group" refers to a monovalent saturated aliphatic hydrocarbon functional group, either linear or branched, that generally comprises 1 to 20 carbon atoms, preferably 1 to 10 carbon atoms (i.e., C1-10 alkyl), more preferably 1 to 8 carbon atoms (i.e., C1-8 alkyl), and more preferably 1 to 6 carbon atoms (i.e., C1-6 alkyl). For example, " C1-6 alkyl group" refers to a functional group that is an alkyl group and has 1 to 6 carbon atoms on its carbon chain (specifically, 1, 2, 3, 4, 5, or 6). Non-limiting examples of alkyl groups include, but are not limited to, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, tert-butyl, sec-butyl, n-pentyl, neopentyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl, 2,2-dimethylpropyl, 1-ethylpropyl, 2-methylbutyl, 3-methylbutyl, n-hexyl, n-heptyl, and n-octyl groups. Unless otherwise specified, the term "alkenyl group" refers to a monovalent unsaturated aliphatic hydrocarbon functional group, either linear or branched, having at least one double bond, generally comprising 2 to 20 carbon atoms, preferably 2 to 10 carbon atoms (i.e., a C2-10 a