Carboxyalkyl dipeptide inhibitors of endopeptidases

C - Chemistry – Metallurgy – 07 – K

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C07K 5/02 (2006.01) A61K 31/40 (2006.01) A61K 38/04 (2006.01) A61K 38/05 (2006.01) C07K 5/06 (2006.01) C07K 5/065 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2069312

2069312 9105796 PCTABS00005 Carboxyalkyl dipeptide inhibitors of endopeptidases of formula (I) or pharmaceutically acceptable salt thereof, wherein R1 is H, alkyl, arylalkyl or aryl; R2 is H, alkyl, alkenyl or alkynyl, 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 hydroxy, alkoxy, or R5; 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 pain conditions, and pharmaceutical compositions containing said compounds are disclosed.

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