| 摘要 |
The present invention provides novel chemical compounds characterized as Rho kinase (ROCK) inhibitors, methods for their discovery, and their therapeutic, research, and diagnostic use. In particular, the present invention provides 1,4-benzodiazepine-2,5-dione compounds and related compounds having ROCK inhibitory activity, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with ROCK activity. |
| 主权项 |
1. A compound defined by a formula selected from the group consisting of:or a pharmaceutically acceptable salt thereof;
wherein R1 is selected from the group consisting of: hydrogen, alkyl, wherein R1′ is selected from the group consisting of wherein R2 is H; wherein R3 is selected from the group consisting of H; alkyl; substituted alkyl; and OH; wherein R4 is N; wherein R5 is selected from the group consisting of H, alkyl, substituted alkyl, mono-substituted aryl, di-substituted aryl, and tri-substituted aryl; wherein R6 is N; wherein R7, R8, R9, and R10 are independently absent or selected from the group consisting of, H, halogen, and wherein R11, R12, R13, and R14, are H; wherein R15, R16, R17, and R18 are independently selected from the group consisting of C and N; wherein R21, R22, R23, and R24 are independently absent or selected from the group consisting of, H, halogen, and,wherein no more than two of R21, R22, R23, and R24 can be hydrogen; and
wherein R25, R26, R27, and R28, are independently selected from the group consisting of hydrogen, alkyl, fluoroalkyl,aminoalkyl,wherein no more than three of R25, R26, R27, and R28 can be hydrogen;
wherein the stereochemical configuration at a stereocenter in said compound is R, S, or a mixture thereof. |
