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US 4,880,938 AGranted
Amino acid analogs
AssigneeMerck & Co., Inc.
InventorRoger M. Freidinger
Life of this patent
Estimating the term…
Abstract
Analogs of glutamic acid and related amino acids and pharmaceutically-acceptable salts thereof which antagonize the function of cholecystokinins and gastrin disease states in animals and compositions for and methods of preventing or treating disorders of the gastrointestinal, central nervous and appetite regulatory systems of mammals, especially of humans.
Claims6
A compound of the formula:
- ##STR33## wherein:
- R.sup.1 is (CH.sub.2).sub.m --R.sup.5 or X.sup.1 --(CH.sub.2).sub.m --R.sup.6 ;
- R.sup.2 and R.sup.3 are independently selected from H;
- C.sub.1 -C.sub.8 -straight- or branched-chain-alkyl;
- C.sub.3 -C.sub.8 -cycloalkyl;
- with the proviso that R.sup.2 and R.sup.3 cannot both be H concurrently;
- R.sup.4 is OH;
- C.sub.1 -C.sub.4 -straight- or branched-chain-alkoxy;
- C.sub.3 -C.sub.6 -cycloalkoxy;
- OCH.sub.2 -phenyl;
- amino-mono- or di-C.sub.1 -C.sub.4 -straight- or branched-chain-alkyl;
- amino-mono- or di-C.sub.3 -C.sub.6 -cycloalkyl;
- or NH--CH.sub.2 -phenyl;
- R.sup.5 is ##STR34## or ##STR35## R.sup.6 is ##STR36## or ##STR37## R.sup.7 is H;
- C.sub.1 -C.sub.4 -straight- or branched-chain-alkyl;
- X.sup.1 is O or NH;
- X.sup.2 and X.sup.3 are independently H;
- OH;
- NO.sub.2 ;
- halo;
- C.sub.1 -C.sub.4 -straight- or branched-chain-alkyl;
- C.sub.1 -C.sub.4 -straight- or branched-chain-alkylthio;
- or C.sub.1 -C.sub.4 -straight- or branched-chain-akoxy;
- X.sup.4 is O or HH;
- Y is NR.sup.7 ;
- n is 1-to-3;
- m is 0-to-4;
- and
- halo is F, Cl, Br, or I;
- or pharmaceutically-acceptable salts of these compounds.
27 more elements
The compound (R)-5-(dipentylamino)-4-[(1H-indol-2-ylcarbonyl)amino]-5-oxo-pentanoic acid, or pharmaceutically acceptable salts of this compound.
Dependencies are inferred from the claim text.