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US 5,312,936 AGranted
Angiotensin II antagonists
AssigneeEli Lilly and Company
InventorsSherryl L. Lifer, Winston S. Marshall, Fariborz Mohamadi, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, Celia A. Whitesitt
Life of this patent
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Abstract
This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their use for antagonizing angiotensin II receptors in mammals.
Claims10
A compound of the formula ##STR11## or a pharmaceutically acceptable salt or solvate thereof where G is ##STR12## Ar is ##STR13## each of A.sub.1, A.sub.2, and A.sub.3 is independently N or CH;
- X is --CO--, --CONH--, --NHCO--, --Ch.sub.2 CONH--, --O--, --NH--, --CH.sub.2 --or a bond;
- each R.sub.1 is independently --(CH.sub.2).sub.n R.sub.3 ;
- R.sub.2 is C.sub.4 -C.sub.7 straight chain alkyl;
- each R.sub.3 is independently --OH, --COOH, or 5-tetrazolyl;
- each n is independently 0, 1, 2, 3, or 4,
- R.sub.4 is H, OH, halo, nitro, methyl, amino, acetamido, or methanesulfonamido;
- Q is a bond or --O--;
- and
- W is H, methyl, ethyl, or hydroxy,
- provided that A.sub.2 is not N when A.sub.1 and A.sub.3 are each CH and R.sub.1 is --COOOH or 5-tetrazolyl;
- provided that if G is not imidazolyl or tetrazolyl, at least one R.sub.3 is 5-tetrazolyl.
8 more elements
A compound of the formula ##STR14## where G is ##STR15## Ar' is ##STR16## each of A.sub.1, A.sub.2, and A.sub.3 is independently N or CH;
- X is --CO--, --CONH--, --NHCO--, --CH.sub.2 CONH--, --O--, --NH--, --CH.sub.2 -- or a bond;
- each R.sub.1 ' is independently --(CH.sub.2).sub.n R.sub.3 ';
- R.sub.2 is C.sub.4 -C.sub.7 straight chain alkyl;
- each R.sub.3 ' is independently --OH, --COOH, 5-tetrazolyl, --COO(C.sub.1 -C.sub.4 alkyl), or --CN;
- each n is independently 0, 1, 2, 3, or 4;
- R.sub.4 is H, OH, halo, nitro, methyl, amino, acetamido, or methanesulfonamide;
- Q is a bond or --O--;
- W is H, methyl, ethyl, or hydroxy;
- provided at least one R.sub.3 ' is --COO(C.sub.1 -C.sub.4 alkyl) or --CN;
- provided that G is imidazolyl or tetrazolyl.
7 more elements
Dependencies are inferred from the claim text.