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US 5,691,356 AGranted
Disubstituted heterocyclic thrombin inhibitors
AssigneeBristol-Myers Squibb Company
InventorsJagabandhu Das, Spencer D. Kimball, Wan Fang Lau
Life of this patent
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Abstract
Disubstituted heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein G is ##STR2## wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; p is 0, 1 or 2, Q is a single bond or ##STR3## and Z, A, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 are as defined herein.
Claims11
A compound having the structure ##STR99## including all stereoisomers, wherein n is 0, 1 or 2;
- Z is NR.sup.7 or O, where R.sup.7 is H, lower alkyl, aryl or arylalkyl;
- G is an amido moiety which includes a cyclic member which is free of ##STR100## a group in the ring;
- R is hydrogen, hydroxyalkyl, hydroxyalkyl(alkyl), aminoalkyl, lower alkyl, cycloalkyl, arylalkyl, alkenyl, alkynyl, amidoalkyl, arylalkoxyalkyl or an amino acid side chain, either protected or unprotected;
- R.sup.1 is lower alkyl exclusive of methyl, cycloalkyl, aryl, or arylalkyl;
- or R.sup.1 and R.sup.2 together with the carbons to which they are attached form a cycloalkyl, aryl or heteroaryl ring;
- R.sup.2 and R.sup.3 are independently hydrogen, lower alkyl, cycloalkyl, aryl, arylalkyl, hydroxy, alkoxy, oxo, thioketal, thioalkyl, thioaryl, amino or alkylamino;
- or R.sup.2 and R.sup.3 together with the carbons to which they are attached form a cycloalkyl, aryl or heteroaryl ring;
- R.sup.4 is H, lower alkyl, arylalkyl, aryl, ##STR101## or --CO.sub.2 R.sup.5, where R.sup.5 is lower alkyl, aryl, arylalkyl, cycloheteroalkyl, heteroaryl, quinolinyl or tetrahydroquinolinyl;
- including pharmaceutically acceptable salts thereof.
6 more elements
Dependencies are inferred from the claim text.