- SUBSTITUTED BENZAMIDES AND METHODS OF USE THEREOF
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The invention provides compounds having the general formula I, and pharmaceutically acceptable salts thereof, wherein the variables RA, RAA, subscript n, ring A, X2, L, subscript m, X1, R1, R2, R3, R4, R5, and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
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Page/Page column 220
(2015/06/11)
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- Discovery and initial structure-activity relationships of trisubstituted ureas as thrombin receptor (PAR-1) antagonists
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Thrombin is the most potent agonist of platelet activation, and its effects are predominantly mediated by platelet thrombin receptors. Therefore, antagonists of the thrombin receptor have potential utility for the treatment of thrombotic disorders. Screening of combinatorial libraries revealed 2 to be a potent antagonist of the thrombin receptor. Modifications of this structure produced 11k, which inhibits thrombin receptor stimulated secretion and aggregation of platelets.
- Barrow, James C,Nantermet, Philippe G,Selnick, Harold G,Glass, Kristen L,Ngo, Phung L,Young, Mary Beth,Pellicore, Janetta M,Breslin, Michael J,Hutchinson, John H,Freidinger, Roger M,Condra, Cindra,Karczewski, Jerzy,Bednar, Rodney A,Gaul, Stanley L,Stern, Andrew,Gould, Robert,Connolly, Thomas M
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p. 2691 - 2696
(2007/10/03)
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