| abstract |
The present invention relates to benzofuryl-oximes of formula (I) or a pharmaceutically acceptable salt or ester form thereof wherein R1 is a direct bond to A, C1-C4 alkylene, or -O-C1-C4 alkylene; R2 and R3 are, independently hydrogen, halogen, C1-C4 alkyl, C1-C3 perfluoroalkyl, -O-C1-C3 perfluoroalkyl, C1-C3 alkoxy, -OH, -NH2, -NO2, -O(CH2)p-aryl, -O(CH2)P-heteroaryl, aryl, heteroaryl, -NH(CH2)P-aryl, -NH(CH2)P-heteroaryl, -NH(CO)-aryl, NH(CO)-heteroaryl, -O(CO)-aryl, O(CO)-heteroaryl, -NH(CO)-CH=CH-aryl, or -NH(CO)-CH=CH-heteroaryl; p is an integer from 0-6; R4 is hydrogen, C1-C8 alkyl, or C3-C6 cycloalkyl; A is -COOH or an acid mimic; X is C1-C8 alkylène, C3-C6 cycloalkylene, -(CH2)mO-, or -(CH2)mNH-; m is an integer from 1-6; and R5 is hydrogen, C1-C8 alkyl, C3-C6 alkyl, C3-C6 cycloalkyl, -CH2-C3-C6 cycloalkyl, heteroaryl, -CH2-heteroaryl, aryl or benzyl; R6 and R7 are independently, hydrogen, halogen, C1-C6 alkyl, C1-C6 perfluoroalkyl, -O-C1-C6 perfluoroalkyl, C1-C6 alkoxy, _OH, -NH2, -NO2, -O(CH2)n-aryl, -O(CH2)n-heteroaryl, aryl, or heteroaryl; and n is an integer from 0-6, wherein the alkyl, cycloalkyl, aryl and heteroaryl groups are each optionally substituted by one or more substituents. The present compounds are PAI-1 inhibitors for the treatment e.g of impairment of the fibrinolytic system, thrombosis or cardiovascular diseases. |