Heteroaromatic amine thrombin inhibitors

Details Heteroaromatic amine thrombin inhibitors Heteroaromatic amine thrombin inhibitors

1993-06-14

1994-12-06

Richter, Johann

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514252, 514253, 514255, 514269, 514275, 514318, 514321, 514323, 514326, 544338, 544331, 544332, 544336, 544408, 544409, 546193, 546194, 546198, 546200, 546205, 546209, 546210, 546211, A61K 31445, A61K 31415, A61K 3142, C07D21514

Patent

active

053710916

ABSTRACT:
Sulfonamide thrombin inhibitors are provided which have the structure ##STR1## including all stereoisomers thereof, wherein n is 1, 2 or 3; m is 0, 1 or 2; R.sup.1 and R.sup.2 are independently H, lower alkyl, cycloalkyl, aryl, heteroaryl or heteroaryl-alkyl, or R.sup.1 and R.sup.2 can be taken together with the N atom to which they are attached to form a 4- to 8-membered ring; R.sup.3 is monocyclic heteroaryl; and R.sup.4 is alkyl, cycloalkyl, aryl, heteroaryl, quinolinyl or tetrahydroquinolinyl, and pharmaceutically acceptable salts thereof.

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Angliker, Herbert et al, "Pseudoarginine: synthesis and properties of derivatives of .delta.-(1-imidazolyl) norvaline" Biochem. J. (1990) 266, 829-834.
Hijikata-Okunomiya, Akiko et al, "A Strategy for a Rational Approach to Designing Synthetic Selective Inhibitors" Seminars in Thrombosis and Hemostasis-vol. 18, No. 1, 1992.

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