JP-2025515330-A5 -

Dates

Publication Date

20260508

Application Date

20230425

Description

Various changes and modifications to the disclosed embodiments will be obvious to those skilled in the art and can be made without departing from the spirit and scope thereof. Another aspect of the present invention may be as follows: [1] Compound of formula (I) or a pharmaceutically acceptable salt thereof (In the formula, R1 is a lipid moiety having at least 8 carbon atoms, and hydrogen. X1 is selected from O, NRw, S, and bond , R2a , R2b , R2c , and R2d are each independently selected from hydrogen, C1 - C4 alkyl, C1 - C4 alkoxy , C3 - C6 cycloalkyl , halo-C1 - C4 alkyl , amino - C1 - C4 alkyl, hydroxy-C1 - C4 alkyl , C1 - C4 alkoxy - C1 - C4 alkyl, halo, hydroxy, amino, C1 - C4 alkylamino , di-C1 - C4 alkylamino , and cyano; R2a and R2b , or R2b and R2c , or R2c and R2d may , together with the carbon atoms to which they are bonded, form optionally substituted 3- to 6-membered rings. X 4 is CR 4 or N, X 5 is CR 5 or N, X 6 is CR 6 or N, X 7 is CR 7 or N, R3 , R4 , R5 , R6 , and R7 are each independently selected from hydrogen, C1 - C6 alkyl , C2 -C6 alkenyl, C2 - C6 alkynyl , C1 - C6 alkoxy , C1 - C6 alkylthio, C3 - C6 cycloalkyl , halo-C1 - C6 alkyl , halo - C1 - C6 alkoxy, amino-C1 - C6 alkyl , hydroxy-C1 - C6 alkyl , C1 - C6 alkoxy -C1 - C6 alkyl , halo-hydroxy-amino, C1 - C4 alkylamino , di-C1 - C4 alkylamino , cyano, -COORx , -CON(Ry ) 2 , -SO2Rz , oligo or polyethylene glycol chain, and the group -Y- R8 ; R 4 and R5 , R5 and R6 , or R6 and R7 may , together with the carbon atoms to which they are bonded, optionally form a substituted five-membered or six-membered ring. Y is selected from -C(O)-, -C(O)O-, -C(O)NRv- , and -C(O)S-. R8 is a lipid moiety having at least 8 carbon atoms . R v , R w , R x , R y , and R z are each independently selected from hydrogen, C1 - C6 alkyl , C2 - C6 alkenyl, C2 - C6 alkynyl , C3 - C6 cycloalkyl , and halo-C1 - C6 alkyl . If R1 is hydrogen, then at least one of R3 , R4 , R5 , R6 , and R7 is a -Y -R 8 group. [2] The compound described in [1] above, or a pharmaceutically acceptable salt thereof, wherein the compound is the compound of formula (Ia): [3] The compound described in [1] or [2] above, or a pharmaceutically acceptable salt thereof, wherein R 2a , R 2b , R 2c , and R 2d are each independently selected from hydrogen, C1 - C4 alkyl, C3 - C6 cycloalkyl, C1 - C4 alkoxy C1 - C4 alkyl, and hydroxy. [4] A compound according to any one of [1] to [3] above, or a pharmaceutically acceptable salt thereof, wherein R 2a , R 2b , R 2c , and R 2d are each independently selected from hydrogen and C1 - C4 alkyl. [5] A compound according to any one of the above [1] to [4], or a pharmaceutically acceptable salt thereof, wherein R 2a , R 2b , and R 2d are hydrogen, and R 2c is selected from hydrogen and C1 - C4 alkyl . [6] The compound described in [1] or [2] above, or a pharmaceutically acceptable salt thereof, wherein R 2a and R 2d are hydrogen atoms, and R 2b and R 2c form a three-membered ring together with the carbon atoms to which they are bonded. [7] A compound according to any one of [1] to [6] above, or a pharmaceutically acceptable salt thereof, wherein R3 is selected from hydrogen and halo . [8] A compound according to any one of the above items [1] to [7], wherein R3 is hydrogen, or a pharmaceutically acceptable salt thereof. [9] A compound according to any one of [1] to [8] above, or a pharmaceutically acceptable salt thereof, wherein R 4 is selected from hydrogen and halo. [10] A compound according to any one of the above items [1] to [9], wherein R4 is hydrogen, or a pharmaceutically acceptable salt thereof. [11] A compound according to any one of the above [1] to [10], or a pharmaceutically acceptable salt thereof, wherein R 5 and R 6 are independently selected from C1-C6 alkyl, C2- C6 alkenyl, C2-C6 alkynyl , C1 - C6 alkoxy , C1 - C6 alkylthio , C3 - C6 cycloalkyl , halo - C1 - C6 alkyl , halo - C1 - C6 alkoxy , amino - C1 - C6 alkyl , hydroxy - C1 - C6 alkyl , C1 - C6 alkoxy - C1 - C6 alkyl , halo , hydroxy, amino, C1-C4 alkylamino, di-C1-C4 alkylamino, cyano, -COOR x , -CON( Ry ) 2 , and -SO2Rz . [12] A compound according to any one of [1] to [11], or a pharmaceutically acceptable salt thereof, wherein R 5 and R 6 are each independently selected from C1- C4 alkyl , C2-C4 alkenyl , C2 - C4 alkynyl , C1 - C4 alkoxy , C1 - C6 alkylthio , halo - C1 - C4 alkyl , halo - C1 - C4 alkoxy , hydroxy, halo, and C1-C4 alkylamino. [13] A compound according to any one of [1] to [12], or a pharmaceutically acceptable salt thereof, wherein R 5 and R 6 are each independently selected from C1 - C4 alkyl , C1 - C4 alkoxy , and halo. [14] A compound according to any one of the above [1] to [13], or a pharmaceutically acceptable salt thereof, wherein R 5 and R 6 are each independently selected from C1 - C4 alkoxys. [15] A compound according to any one of the above items [1] to [14], wherein R7 i