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US 5,703,125 AGranted
Substituted .beta.-amino acid derivatives useful as platelet aggregation inhibitors
AssigneesG. D. Searle & Co., Monsanto Company
InventorsPhilippe R. Bovy, Joseph G. Rico, Thomas E. Rogers, Foe S. Tjoeng, Jeffery A. Zablocki
Life of this patent
Estimating the term…
Abstract
The invention relates to platelet aggregation inhibitors which are substituted beta amino acid derivatives of the formula: ##STR1## wherein Z, A, Z', Z", W, q, R.sup.1 and R.sup.2 are as defined in the specification.
Claims10
A substituted .beta. amino acid derivative or a pharmaceutically acceptable salt thereof having the formula:
- ##STR97## wherein R.sup.1 is selected from the group consisting of hydrogen, lower alkyl radicals, lower alkenyl radicals, aromatic hydrocarbon radicals, alicyclic hydrocarbon radicals, benzyl radicals, phenethyl radicals, wherein said radicals are optionally substituted with halogen, lower alkoxy, hydroxy and lower alkyl;
- R.sup.2 is an aromatic hydrocarbon radical, wherein said radical is optionally substituted with hydroxy, lower alkoxy, lower alkyl, halogen, nitro, cyano, azido, ureido, ureylene, carboxyl or carbonyl derivatives, trifluoromethyl, acyloxy, alkylthio, arylthio, alkylsulfinyl, arylsulfinyl, alkylsulfonyl, arylsulfonyl, amino, alkylamino, trialkylsilyl, aminosulfonyl, dialkylamino, alkanoylamino, aroylamino, phenyl, naphthyl, or lower alkynyl which are optionally substituted with one or more of the following:
- halogen, nitro, lower alkoxy, lower alkyl, trialkylsilyl, azide and phenyl;
- A is selected from the group consisting of ethylene, lower alkenylene radicals, lower alkynylene radicals, and divalent alicyclic radicals, wherein said radicals are optionally substituted with hydroxyl, lower alkoxy, lower alkyl, halogen, alkoxycarbonylalkyl, amino, alkylamino, dialkylamino, acylamino, alkylthio, sulfonyl, and aromatic hydrocarbons which are optionally substituted with halogen, nitro, lower alkoxy and lower alkyl;
- W is selected from the group consisting of hydrogen, lower alkyl radicals, lower alkenyl radicals, lower alkynyl radicals, alicyclic hydrocarbon radicals and aromatic hydrocarbon radicals, wherein said radicals are optionally substituted with hydroxyl, lower alkoxy, lower alkyl, halogen, nitro, amino, acyloxy, phenyl and naphthyl which may be optionally substituted with halogen, nitro, lower alkoxy, and lower alkyl;
- Z, Z', Z" are independently selected from the group consisting of hydrogen, lower alkyl radicals, halogen, alkoxy, cyano, sulfonyl, carboxyl, alkoxycarbonyl, and hydroxyl radicals;
- q is an integer from 0 to about 6;
- and
- with the proviso that when A is trimethylene and q is 0 then R.sub.2 is not a phenyl radical.
6 more elements
A substituted .beta. amino acid derivative which is
- t-Butyl .beta.-2-4-(aminoiminomethyl)phenyl!amino!carbonyl!cyclopropyl!carbo nyl!amino!phenylpropanoate.
Dependencies are inferred from the claim text.