Cyclic amino acid derivatives

Details Cyclic amino acid derivatives Cyclic amino acid derivatives

C - Chemistry, Metallurgy

07

K

C07K 5/065 (2006.01) A61K 31/215 (2006.01) A61K 31/33 (2006.01) A61K 38/05 (2006.01) C07C 323/40 (2006.01) C07C 327/34 (2006.01) C07D 209/20 (2006.01) C07D 213/55 (2006.01) C07D 213/79 (2006.01) C07D 295/15 (2006.01) C07D 333/38 (2006.01) C07D 401/12 (2006.01) C07K 5/078 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2135711

CYCLIC AMINO ACID DERIVATIVES Abstract of the Disclosure Disclosed are the compounds of formula I Image (I) wherein R represents hydrogen, lower alkyl, carbocyclic or heterocyclic aryl-lower alkyl or cycloalkyl-lower alkyl; R1 represents hydrogen, lower alkyl, cycloalkyl, carbocyclic aryl or heterocyclic aryl, or biaryl; R3 represents hydrogen or acyl; R4 represents hydrogen, lower alkyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, biaryl or biaryl-lower alkyl; R5 represents hydrogen or lower alkyl; or R4 and R5 together with the carbon atom to which they are attached represent cycloalkylidene or benzo-fused cycloalkylidene; A together with the carbon atom to which it is attached represents 3 to 10 membered cycloalkylidene or 5 to 10 membered cycloalkenylidene radical which may be substituted by lower alkyl or aryl-lower alkyl or may be fused to a saturated or unsaturated carbocyclic 5-7-membered ring; or A together with the carbon to which it is attached represents 5 or 6 membered oxacycloalkylidene, thiacycloalkylidene or azacycloalkylidene optionally substituted by lower alkyl or aryl-lower alkyl; or A together with the carbon atom to which it is attached represents 2,2-norbornylidene; m is 0, 1, 2 or 3; and COOR2 represents carboxyl or carboxyl derivatized in form of a pharmaceutically acceptable ester; disulfide derivatives derived from said compounds wherein R3 is hydrogen; and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for preparation of said compounds; intermediates; and methods of treating disorders in mammals which are responsive to ACE and NEP inhibition by administration of said compounds to mammals in need of such treatment.

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