Pharmaceutically active diketopiperazines

Details Pharmaceutically active diketopiperazines Pharmaceutically active diketopiperazines

C - Chemistry, Metallurgy

07

D

C07D 241/18 (2006.01) A61K 31/495 (2006.01) C07D 241/02 (2006.01)

Patent

CA 2141938

A diketopiperazine of formula (A) wherein each of R1 to R10, which may be the same or different, is independently se- lected from hydrogen, C1-C6 alkyl unsubstituted or substituted by one or more hydrogen atoms, C1-C6 alkoxy, C1-C6 al- kylthio, halogen, hydroxy, nitro, optionally substituted phenyl, -cyano, -CH2COOH, -CH2OH, -CO2R11, -NHCOR11, -NHSO2R13, -SO2R13, -CON(R11R12), -SOR13, -SO2N(R11R12), -N(R11R12), -O(CH2)nN(R11R12), -O(CH2)nCO2R11, -OCOR11, -CH2OCOR11, -CH2NHCOR11, -CH2NHCOOR13, -CH2SR11, -CH2SCOR11, -CH2S(O)mR13 wherein m is 1 or 2, -CH2NHCO(CH2)nCO2R11, -N(R11)COR12, -NHCOCF3, -NHCO(CH2)nCO2R11, -NHCO(CH2)nOCOR11 and -NHCO(CH2)nOR11 wherein n is 0 or is an integer of from 1 to 6, each of R11 and R12 is independently H or C1-C6 alkyl and R13 is C1-C6 alkyl; or any of R1 and R2, R2 and R3, R3 and R4 and R4 and R5, or R6 and R7, R7 and R8, R8 and R9 and R9 and R10, form together with the carbon atoms to which they are attached a benzene ring which is optionally substituted; and pharmaceutically acceptable salts and esters thereof; are inhibitors of the plasminogen activator inhibitor.

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