Gem-disubstituted amino acid derivatives

Details Gem-disubstituted amino acid derivatives Gem-disubstituted amino acid derivatives

1994-06-22

1996-04-16

Richter, Johann

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

548495, 549 76, 558254, 560 16, 562426, A61K 3805, C07C32706, C07C32341

Patent

active

055082661

ABSTRACT:
Disclosed are the compounds of formula I ##STR1## wherein R represents hydrogen, lower alkyl, carbocyclic or heterocyclic aryl-lower alkyl or cycloalkyl-lower alkyl;
R.sub.1 represents hydrogen, lower alkyl, cycloalkyl, carbocyclic aryl or heterocyclic aryl, or biaryl;
R.sub.3 represents hydrogen or acyl;
R.sub.4 represents hydrogen, lower alkyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, biaryl or biaryl-lower alkyl;
R.sub.5 represents hydrogen or lower alkyl; or R.sub.4 and R.sub.5 together with the carbon atom to which they are attached represent cycloalylidene or benzo-fused cycloalkylidene;
R.sub.6 represents lower alkyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, biaryl or biaryl-lower alkyl;
R.sub.7 represents lower alkyl, carbocyclic or heterocyclic aryl-lower alkyl, cycloalkyl-lower alkyl or biaryl-lower alkyl;
m is 0, 1, 2 or 3; and
COOR.sub.2 represents carboxyl or carboxyl derivatized in form of a pharmaceutically acceptable ester;
disulfide derivatives derived from said compounds wherein R.sub.3 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.

REFERENCES:
patent: 4613587 (1986-09-01), Kessler et al.
patent: 4684660 (1987-08-01), Ondetti et al.
Yukio, S. et al. Chem. Abstr. 1979, 90(15), 116647; Bioinorg Chem. 1978, 9(6), 521-528.
Holden, H. M. et al. J. Biol. Chem. 1988, 263(7), 3256-3260.
Kortylewicz, Z. P. et al. J. Med. Chem. 1990, 33, 263-273.

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