| 主权项 |
1. A method of treating a fibrotic condition, comprising administering a therapeutically effective amount of a compound having the structure of Formula (III): or a pharmaceutically acceptable salt thereof to a subject in need thereof, wherein R1 is selected from the group consisting of halogen, —CN, —C(O)R8, —SO2R16, C1-6 alkyl optionally substituted with one or more R4, C2-6 alkenyl optionally substituted with one or more R4, C2-6 alkynyl optionally substituted with one or more R4, C6-10 aryl optionally substituted with one or more R4, 5-10 membered heteroaryl optionally substituted with one or more R4, C3-10 carbocyclyl optionally substituted with one or more R4, and 3-10 membered heterocyclyl optionally substituted with one or more R4; R2 is selected from the group consisting of halogen, —CN, —OR5, —SR5, —NR6R7, and —C(O)R8; R3 is selected from the group consisting of hydrogen, —(CH2)n—(C6-10 aryl), —(CH2)n-(5-10 membered heteroaryl), —(CH2)n—(C3-10 carbocyclyl), and —(CH2)n-(3-10 membered heterocyclyl), each optionally substituted with one or more R9; each R4 is independently selected from the group consisting of halogen, —CN, —OH, —C(O)R8, —SO2R16, optionally substituted C1-6 alkyl, optionally substituted C2-6 alkenyl, optionally substituted C2-6 alkynyl, optionally substituted C1-6 alkoxy, optionally substituted C6-10 aryl optionally substituted with one or more R11, C7-14 aralkyl optionally substituted with one or more R11, 5-10 membered heteroaryl optionally substituted with one or more R11, or independently two geminal R4 together are oxo; each R5 is independently selected from the group consisting of hydrogen, optionally substituted C1-6 alkyl, optionally substituted C2-6 alkenyl, optionally substituted C2-6 alkynyl, optionally substituted C2-8 alkoxyalkyl, C6-10 aryl optionally substituted with one or more R11, C7-14 aralkyl optionally substituted with one or more R11, and —(CH2)n-(3-10 membered heterocyclyl) optionally substituted with one or more R10; R6 is selected from the group consisting of hydrogen, optionally substituted C1-6 alkyl, optionally substituted C2-6 alkenyl, optionally substituted C2-6 alkynyl, C6-10 aryl optionally substituted with one or more R11, C7-14 aralkyl optionally substituted with one or more R11, (5-10 membered heteroaryl)alkyl optionally substituted with one or more R11, —C(O)R8, and —C(O)OR5; R7 is selected from the group consisting of hydrogen, optionally substituted C1-6 alkyl, optionally substituted C2-6 alkenyl, optionally substituted C2-6 alkynyl, C6-10 aryl optionally substituted with one or more R11, C7-14 aralkyl optionally substituted with one or more R11, (5-10 membered heteroaryl)alkyl optionally substituted with one or more R11, —C(O)R8, and —C(O)OR5; or R6 and R7 together with the nitrogen to which they are attached form a 3-10 membered heterocyclyl optionally substituted with one or more R10; each R8 is independently selected from the group consisting of hydrogen, optionally substituted C1-6 alkyl, optionally substituted C2-6 alkenyl, optionally substituted C2-6 alkynyl, C6-10 aryl optionally substituted with one or more R11, C7-14 aralkyl optionally substituted with one or more R11, —NR12R13, and —OR5; each R9 is independently selected from the group consisting of hydroxy, halogen, optionally substituted C1-6 alkyl, optionally substituted C2-6 alkenyl, optionally substituted C2-6 alkynyl, optionally substituted C1-6 alkylthio, optionally substituted C2-8 alkoxyalkyl, optionally substituted C3-10 carbocyclyl, optionally substituted C6-10 aryl, —OR5, —NR14R15, —C(O)R8, —SO2R16, —CN, and —NO2; each R10 is independently selected from the group consisting of optionally substituted C1-6 alkyl, optionally substituted C2-6 alkenyl, and optionally substituted C2-6 alkynyl, or independently two geminal R10 together are oxo; each R11 is independently selected from the group consisting of halogen, —CN, optionally substituted C1-6 alkyl, optionally substituted C2-6 alkenyl, optionally substituted C2-6 alkynyl, —O—(CH2)n—C1-8alkoxy, —C(O)R8, and optionally substituted C1-6 alkoxy; each R12 is independently selected from the group consisting of hydrogen, optionally substituted C1-6 alkyl, optionally substituted C2-6 alkenyl, optionally substituted C2-6 alkynyl, C6-10 aryl optionally substituted with one or more R11, and C7-14 aralkyl optionally substituted with one or more R11; each R13 is independently selected from the group consisting of hydrogen, optionally substituted C1-6 alkyl, optionally substituted C2-6 alkenyl, optionally substituted C2-6 alkynyl, C6-10 aryl optionally substituted with one or more R11, and C7-14 aralkyl optionally substituted with one or more R11; R14 is selected from the group consisting of hydrogen, optionally substituted C1-6 alkyl, optionally substituted C6-10 aryl, and —C(O)R8; R15 is selected from the group consisting of hydrogen, optionally substituted C1-6 alkyl, optionally substituted C6-10 aryl, and —C(O)R8; each R16 is independently selected from the group consisting of optionally substituted C1-6 alkyl, optionally substituted C2-6 alkenyl, optionally substituted C2-6 alkynyl, C6-10 aryl optionally substituted with one or more R11, C7-14 aralkyl optionally substituted with one or more R11, —NR12R13, and —OR5; Z is selected from oxygen and sulfur; each n is independently an integer from 0 to 4; and the bonds represented by a solid and dashed line are independently selected from the group consisting of a single bond and a double bond, provided that when R3 is H, then R1 is selected from C6-10 aryl optionally substituted with one or more R4, or 5-10 membered heteroaryl optionally substituted with one or more R4; when R2 is —NH-(2-fluoro-4-bromo-phenyl), and R1 is C(O)OH, then R3 is not —CH2-phenyl; when R2 is methoxy, R1 is 4-methoxyphenyl, and Z is O, then R3 is not —(CH2)-2-fluro-4-chloro-phenyl; when R3 is a phenyl; R2 is OR5 or NR6R7; then R1 is not triazolyl; when R3 is 4-methyl phenyl, R2 is morpholinyl, and Z is O; then R1 is not methyl; and when R3 is 4-methyl phenyl, R2 is —N(CH3)2, Z is O; then R1 is not methyl. |
