Discovery and initial structure–Activity relationships of trisubstituted ureas as thrombin receptor (PAR-1) antagonists
摘要:
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. (C) 2001 Elsevier Science Ltd. All rights reserved.
[EN] SUBSTITUTED BENZAMIDES AND METHODS OF USE THEREOF<br/>[FR] BENZAMIDES SUBSTITUÉS ET LEURS MÉTHODES D'UTILISATION
申请人:GENENTECH INC
公开号:WO2015078374A1
公开(公告)日:2015-06-04
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.
Phenylethanolamine derivatives and acid addition salts thereof for
申请人:American Cyanamid Company
公开号:US04404222A1
公开(公告)日:1983-09-13
There is provided a method for enhancing the growth rate of meat-producing animals and/or improving the efficiency of feed utilization thereby, which involves, orally or parenterally, administering to said animals a growth-enhancing amount of a phenylethane compound or the acid addition salt thereof.
Phenylethanolamine derivatives and acid addition salts thereof for the
申请人:American Cyanamid Company
公开号:US04407819A1
公开(公告)日:1983-10-04
There is provided a method for increasing lean meat deposition and/or improving lean meat to fat ratio in poultry, domestic pets, sheep, swine, rabbits, goats and cattle by administering, orally or parenterally, to said animals an effective amount of a phenylethane derivative or acid salt thereof.
Phenylethane derivatives and acid addition salts thereof for increasing
申请人:American Cyanamid Company
公开号:US04522822A1
公开(公告)日:1985-06-11
There is provided a method for increasing lean meat deposition and/or improving lean meat to fat ratio in poultry, domestic pets, sheep, swine, rabbits, goats and cattle by administering, orally or parenterally, to said animals an effective amount of a phenylethane derivative or acid salt thereof.
The invention provides compounds having the general formula I:
and pharmaceutically acceptable salts thereof, wherein the variables R
A
, R
AA
, subscript n, ring A, X
2
, L, subscript m, X
1
, R
1
, R
2
, R
3
, R
4
, R
5
, and R
N
have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compactions.