654682-18-5Relevant academic research and scientific papers
N-[(4,5-DIPHENYL-2-THIENYL)METHYL]AMINE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
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Page/Page column 8, (2010/11/29)
The subject of the present invention is compounds corresponding to formula (I): Wherein X, R1, R2, R3 and R4 are as described herein. The invention also relates to a method for the preparation and application of said compounds as cannabinoid CB1 receptor antagonists.
Regioselective synthesis of highly aryl-substituted pyrrole carboxylates as useful medicinal chemistry leads
Bhatt, Ulhas,Duffy, Bryan C.,Guzzo, Peter R.,Cheng, Leifeng,Elebring, Thomas
, p. 2793 - 2806 (2008/02/12)
The regioselective syntheses of two pharmaceutically relevant pyrrole scaffolds are described. A synthetic route for the preparation of differentially substituted pyrrole-3,4-dicarboxylates is presented and exemplified. This route circumvents some of the
DIPHENYLPYRIDINE DERIVATIVES, PREPARATION AND THERAPEUTIC APPLICATION THEREOF
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Page/Page column 6, (2008/06/13)
The invention relates to 5,6-diphenylpyridine-3-carboxamide derivatives of general formula (I): where: R1 represents hydrogen or a (C1-C 4)alkyl; R2 represents: a monoazo saturated heterocycle of 5 to 7 atoms, the nitrogen atom being substituted with a (C1-C4)alkanoyl; NR10R11; a nonaromatic (C3-C10) carbocycle more than tri-substituted with (C1-C4)alkyl; a nonaromatic (C11-C12) carbocycle unsubstituted or mono-or polysubstituted with (C1-C4) alkyl; a monooxygenated saturated heterocycle with 5 to 7 atoms, more than tri-substituted with (C1-C4)alkyl; or R1 and R2, together with the nitrogen atom to which the above are bonded, form a 4-disubstituted piperidin- 1-yl group; the salts, solvates and hydrates thereof. The invention further relates to a method for production and therapeutic application thereof.
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
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)
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
CHEMICAL COMPOUNDS
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Page 85, (2010/02/06)
Compounds of formula (I):wherein variable groups are as defined within; for use in the inhibition of 11betaHSD1 are described
