Carboxyalkylcarbonyl aminoacid endopeptidase inhibitors

Details Carboxyalkylcarbonyl aminoacid endopeptidase inhibitors Carboxyalkylcarbonyl aminoacid endopeptidase inhibitors

C - Chemistry, Metallurgy

07

C

C07C 323/59 (2006.01) A61K 31/195 (2006.01) A61K 31/215 (2006.01) A61K 31/395 (2006.01) C07C 233/63 (2006.01) C07C 235/40 (2006.01) C07D 207/337 (2006.01) C07D 213/55 (2006.01) C07D 307/54 (2006.01) C07D 333/24 (2006.01)

Patent

CA 2069112

2069112 9107386 PCTABS00005 Carboxyalkylcarbonyl aminoacid inhibitors of endopeptidases of formula (I), or pharmaceutically acceptable salt thereof, wherein R1 is H, alkyl, arylalkyl, aryl or aryloxyalkyl; R2 is alkyl, alkenyl, alkynyl, alkoxy or alkylthio, wherein the alkyl portion is substituted with 0-3 substituents independently selected from the group consisting of hydroxy, alkoxy, alkoxyalkoxy, alkylthio, aryl, alkoxyalkylthio, arylalkoxy and arylalkylthio; R3 and R4 are independently alkyl or arylalkyl; or R3 and R4 together with the carbon to which they are attached form an optionally substituted 5-, 6- or 7-membered ring wherein said ring comprises 0 to 1 heteroatoms selected from the group consisting of sulfur and oxygen; R5 is H, alkyl, alkoxyalkyl, alkylthioalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, arylalkoxyalkyl or arylalkylthioalkyl; R6 is H, hydroxy, alkoxy, alkyl, arylalkoxy, alkoxyalkyl, alkylthioalkyl, arylalkoxyalkyl, arylalkylthioalkyl, aryl or heteroaryl; R7 is hydroxy, alkoxy, aryloxy, arylalkoxy, amino, alkylamino or dialkylamino; m is 0 or 1; and n is 0, 1, 2 or 3, 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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