Mercaptoacyl aminolactam endopeptidase inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 223/12 (2006.01) A61K 31/40 (2006.01) A61K 31/44 (2006.01) A61K 31/55 (2006.01) C07D 207/273 (2006.01) C07D 211/76 (2006.01) C07D 401/02 (2006.01) C07D 403/02 (2006.01) C07D 405/02 (2006.01)

Patent

CA 2077746

2077746 9113870 PCTABS00007 Mercaptoacyl aminolactam inhibitors of endopeptidases of formula (I), wherein Y is -(CHR5)n(CR3R4)- or -(CR3R4)pX(CR3R4)q-, wherein two substituents selected from the group consisting of R3, R4 and R5, can form a benzene, cyclopentane or cyclohexane ring; X is -O-, -S-, -SO- or -SO2-; Q is hydrogen or R6CO-; m is 1 or 2; n is 1, 2, 3 or 4; p is 1 or 2; q is 2 or 3; R1 is lower alkyl, aryl or heteroaryl; R2 is hydrogen, lower alkyl, hydroxylower alkyl, lower alkoxylower alkyl, aryllower alkyl or heteroaryllower alkyl; R3 and R4 are independently hydrogen, lower alkyl, aryllower alkyl or heteroaryllower alkyl; R5 is hydrogen, lower alkyl, aryllower alkyl, heteroaryllower alkyl, hydroxy, lower alkoxy, mercapto, or lower alkylthio; and R6 is lower alkyl, aryl or heteroaryl, use of the compounds, alone or in combination with an ACE inhibitor or an ANF, in the treatment of cardiovascular disorders such as hypertension, congestive heart failure, edema and renal insufficiency, use of the compounds in the treatment of nephrotoxicity and pain conditions, and pharmaceutical compositions containing said compounds are disclosed.

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