Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-02-14
1997-09-16
Davis, Zinna Northington
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514365, 514367, 514419, 514438, 546236, 546335, 548180, 548204, 548495, 548496, 549 76, 549 77, C07D21302, A61K 3144
Patent
active
056681585
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 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
COOR.sub.2 represents carboxyl or carboxyl derivatized in form of a pharmaceutically acceptable ester.
REFERENCES:
patent: 4093739 (1978-06-01), Martin
patent: 4132803 (1979-01-01), Martin
patent: 5208236 (1993-05-01), Neustadt
J. Med. Chem. 1985, 28, 910-914, Martin et al.
Davis Zinna Northington
Gruenfeld Norbert
Novartis Corporation
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