DIARYLTRIAZOLMETHYLAMINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
The invention concerns compounds of formula (I): Wherein X, R1, R2, R3 and R4 are as described herein. The invention also concerns a method for preparing same and the therapeutic use thereof.
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Page/Page column 5
(2009/01/20)
Bioisosteric replacements of the pyrazole moiety of rimonabant: Synthesis, biological properties, and molecular modeling investigations of thiazoles, triazoles, and imidazoles as potent and selective CB1 cannabinoid receptor antagonists
Series of thiazoles, triazoles, and imidazoles were designed as bioisosteres, based on the 1,5-diarylpyrazole motif that is present in the potent CB1 receptor antagonist rimonabant (SR141716A, 1). A number of target compounds was synthesized an
Lange, Jos H. M.,Van Stuivenberg, Herman H.,Coolen, Hein K. A. C.,Adolfs, Tiny J. P.,McCreary, Andrew C.,Keizer, Hiskias G.,Wals, Henri C.,Veerman, Willem,Borst, Alice J. M.,De Looff, Wouter,Verveer, Peter C.,Kruse, Chris G.
p. 1823 - 1838
(2007/10/03)
Potent imidazole and triazole CB1 receptor antagonists related to SR141716
Diarylimidazolecarboxamides and diaryltriazolecarboxamides related to SR141716 were synthesized and tested for binding to the human CB1 receptor. Suitably substituted imidazoles are comparably potent to the clinical candidate, whereas the analo
Dyck, Brian,Goodfellow, Val S.,Phillips, Teresa,Grey, Jonathan,Haddach, Mustapha,Rowbottom, Martin,Naeve, Gregory S.,Brown, Brock,Saunders, John
p. 1151 - 1154
(2007/10/03)
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