| abstract |
An isoquinoline derivative or a pharmaceutically acceptable salt thereof has the formula (I) wherein: one of R1 and R2 is H and the other is N=C(NH2)2 or NHC(=NH)NH2; R3 is H, halogen, alkyl optionally substituted by one or more halogen, or alkoxy optionally substituted by one or more halogen; R4, R5, R6 and R7 are each independently H, OH, halogen, alkyl optionally substituted by one or more halogen or OH, alkoxy optionally substituted by one or more halogen, CN, COalkyl optionally substituted by one or more halogen, (Cm-alkylene)CO2R8, O(Cn-alkylene)CO2R8, O(Cn-alkylene)CN, (Cn-alkylene)CN, (Cm-alkylene)CONR9R10, (Cm-alkylene)NR9COR10, O(Cn -alkylene)CONR9R10, (Cm-alkylene)NR9SO2R11, (Cm-alkylene)S(O)pR11, (Cm-alkylene)SO2NR9R10, CH=CHCOR8, CH=CHCONR9R10, CH=CHSO2R8, CH=CHSO2NR9R10, CH=CHSO2aryl or a group of formula X-aryl or X-het or, where two of R4, R5, R6 and R7 are attached to adjacent carbon atoms, they can be taken together to form an -O(Cn-alkylene)-O-moiety; R8 to R11 are as defined in the specification; X is a direct link, Cn-alkylene, O, (Cn-alkylene)O, O(Cn-alkylene), CH(OH), alkylOH, CO, S(O)p (Cm-alkylene), (Cm-alkylene)S(O)p, CH=CH, or CºC; m is from 0 to 3, n is from 1 to 3, and p is an integer from 0 to 2. A pharmaceutical composition thereof is useful as a urokinase inhibitor. |