| 摘要 |
The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases. Compounds of the invention display soft drug characteristics, i.e. they are rapidly inactivated upon entry in the systemic circulation. Therefore, they allow for reduced systemic exposure to functionally active ROCK inhibitors.; |
| 主权项 |
1. A compound of Formula I or a stereoisomer, tautomer, racemic, salt, hydrate, or solvate thereof, Wherein Ar1 is selected from Ar2 represents an aryl or heteroaryl; Cy is a C3-15cycloalkyl wherein optionally one carbon atom is replaced by a nitrogen atom; X is a direct bond, —NH— or —N(C1-6alkyl)-; R1 is selected from hydrogen, halogen, C1-6 alkyl, and C1-6 alkoxyl; R2 is selected from hydrogen and C1-3 alkyl; R3 is selected from hydrogen, halogen, C1-6 alkyl, and C1-6 alkoxyl; R4 is an optionally substituted group selected from C1-20alkyl, C2-20alkenyl, C2-20alkynyl, C3-15cycloalkyl, aryl, heterocyclyl, and heteroaryl; R5 is selected from hydrogen, C1-6alkyl and NH2; R6 is selected from hydrogen, halo or C1-6alkyl; k is an integer from 0 to 3; l is an integer from 0 to 3; m is an integer from 0 to 3. |
