Heteroaromatic and thioheteroaromatic substituted sulfonamide thrombin inhibitors
AssigneeBristol-Myers Squibb Company
InventorRaj N. Misra
Life of this patent
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Abstract
Sulfonamide thrombin inhibitors are provided which have the structure ##STR1## including all stereoisomers thereof, wherein X is S or --CH.sub.2 --; m is 0, 1 or 2 when X is --S-- or m is 0 when X is --CH.sub.2 --; n is 1, 2 or 3; R.sup.1 and R.sup.2 are independently H, lower alkyl, cyclo-alkyl, aryl, heteroaryl or heteroarylalkyl, or R.sup.1 and R.sup.2 can be taken together with the N atom to which they are attached to form a 5- to 8-membered ring which may optionally contain an additional N, O or S atom in the ring; R.sup.3 is heteroaryl; and R.sup.4 is alkyl, cycloalkyl, aryl, heteroaryl, quinolinyl or tetrahydroquinolinyl, and pharmaceutically acceptable salts thereof.
Claims15
A compound of the structure ##STR39## including all stereoisomers thereof, wherein
- X is --S--;
- m is 0, 1 or 2;
- n is 1, 2 or 3;
- R.sup.1 and R.sup.2 may be the same or different and are independently hydrogen, lower alkyl, cycloalkyl, aryl, heteroaryl, or heteroarylalkyl, or R.sup.1 and R.sup.2 can be taken together with the nitrogen atom to which they are attached to form a 5- to 8-membered N-containing heterocyclic ring, which may optionally contain an additional N, O or S atom in the ring, which may be unsubstituted or substituted on the N-atom or a carbon atom with lower alkyl, carboxy, amido, carboalkoxy, aryl, cycloalkyl, hydroxy, alkoxy, amino, alkylamino or dialkylamino;
- R.sup.3 is heteroaryl;
- R.sup.4 is aryl, quinolinyl, or tetrahydroquinolinyl;
- wherein the term "heteroaryl" by itself or as part of another group refers to a 5- or 6 -membered monocyclic aromatic ring which includes 1 or 2 hetero atoms which are nitrogen, oxygen or sulfur any of which may optionally include 1 or 2 substituents which is halogen, lower alkyl, lower alkoxy, cyano, hydroxy, carboxy, amido, carboalkoxy, aryl, cycloalkyl, alkylthio, alkylsulfinyl, alkylsulfonyl, arylthio, arylsulfinyl, arylsulfonyl, amino, lower alkylamino and/or di-lower alkylamino;
- and pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.