JP-2022507514-A5 -

Dates

Publication Date

20221209

Application Date

20191115

Description

The following is one embodiment of the present invention.(1) Equation I:A compound having the structure, or a pharmaceutically acceptable salt thereof.[In the formula,R1ishydrogen, halogen, optionally substituted C1-4alkyl, optionally substituted C2-4alkenyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, CN, OR1a , SR 1a , NR 1a R 1b , N(R 1a )C(O)R 1a , or C(O)N(R 1a )(R 1b ). L1 is bonded, and sometimes substituted, C1-5 alkyl , C(O), O, C(O)N(R4 ) (C(R4 ) 2 ) m , (C(R4 ) 2 ) m C (O)N(R4 ) , N(R4) , S(O) 2 N(R4 ) , N(R4 ) S(O) 2 , S(O) 2 , cycloalkyl or heterocyclyl. is pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, triazinyl, or Furthermore, any of the pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, and triazinyl may optionally be substituted with one or more substituents selected from halogens, optionally substituted C1-3 alkyls, and N(R3 ) 2 . X is independently selected from CH and N in each occurrence. L2 is optionally substituted C1-5 alkyl, C(O)N(R4 ) (C(R4 ) 2 ) m , (C(R4 ) 2 ) m C ( O )N( R4 ), C(O) heterocyclyl, heterocyclyl-C(O), N(R4 ) , S(O) 2 N(R4 ) , N(R4 ) S(O) 2 , S(O) 2 , or heterocyclyl, and each of the heterocyclyls is optionally substituted with one or more optionally substituted aryl, optionally substituted C1-4 alkyl, or halogen . is aryl or heteroaryl, If R2 is present, in each case it is independently a optionally substituted C1-6 alkyl , optionally substituted cycloalkyl, CN, NR1aR1b , C (O)N( R1a )(R1b ) , N(R1a ) C(O)R1a , halogen, or CF3 . Each of R1a and R1b is , in each case independently, hydrogen, optionally substituted C1-4 alkyl , optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl, or optionally substituted heterocycline, or R1a and R1b together with the N to which they are bound to form optionally substituted heterocycline. R3 is , in each case independently, a C1-4 alkyl group that is hydrogen or optionally substituted . R 4 is independently in each case hydrogen, optionally substituted C1-4 alkyl , optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl, or optionally substituted heterocycline, and m is 0, 1, 2, or 3, and q is 0, 1, 2, or 3. (2) The compound described in (1), wherein L2 is a C1-5 alkyl group which may be substituted . (3) The compound described in (1), wherein L2 is a substituted C1-5 alkyl group. (4) The compound described in (1), wherein L2 is a hydroxysubstituted C1-5 alkyl group. (5) The compound described in (1), wherein L2 is a methoxy -substituted C1-5 alkyl group. (6) The compound described in (1), wherein L2 is a heterocycline in which it may be substituted. (7) The compound described in (1), wherein L2 is an unsubstituted heterocycline. (8) The compound described in (7), wherein L2 is oxazolinyl . (9) The compound described in (7), wherein L2 is imidazolinyl . (10) The compound described in (1), wherein L2 is a substituted heterocyclyl . (11) The compound described in (1), wherein L2 is an aryl-substituted heterocycline . (12) The compound described in (1), wherein L2 is oxazolinyl . ( 13) The compound described in (1), wherein L2 is C (O)N(R4 ) (C(R4R4 ) ) m . (14) The compound described in (13), wherein m is 1 or 2. (15) The compound according to (13), wherein each case of R 4 is independently hydrogen or C 1-4 alkyl, and m is 0, 1, or 2. (16) A compound according to any of (1) to (15), wherein L1 is a bond. (17) The compound described in (1), wherein L2 is a C(O) heterocyclyl . (18) The compound of formula I is, formula Ia': A compound having the structure of (1), or a pharmaceutically acceptable salt thereof. [In the formula, R1 is a heterocycline that may be substituted, an aryl that may be substituted, or a heteroaryl that may be substituted. is pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, triazinyl, or Furthermore, any of the pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, and triazinyl may optionally be substituted with one or more substituents selected from halogens, optionally substituted C1-3 alkyls, and N(R3 ) 2 . L2 is optionally substituted C1-5 alkyl, C(O)N(R4 ) (C(R4 ) 2 ) m , (C(R4 ) 2 ) m C ( O )N( R4 ), C(O) heterocyclyl, heterocyclyl-C(O), N(R4 ) , S(O) 2 N(R4 ) , N(R4 ) S(O) 2 , S(O) 2 , or heterocyclyl, and each of the heterocyclyls is optionally substituted with one or more optionally substituted aryl, optionally substituted C1-4 alkyl, or halogen . is aryl or heteroaryl, If R2 is present , in each case independently it is optionally substituted C1-6 alkyl , alkoxy, optionally substituted cycloalkyl, CN, NR1aR1b , C( O )N(R1a ) (R1b ) , N(R1a ) C(O)R1a , halogen, or CF3 . Each of R1a and R1b is , in each case independently, hydrogen, optionally substituted C1-4 alkyl , optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl, or optionally substituted heterocycline, or R1a and R1b together with the N to which they are bound to