On August 19, 2010, Bollu, Venkataiah; Boren, Brant Clayton; Dalgard, Jackline Eve; Flatt, Brenton T.; Haq, Nadia; Hudson, Sarah; Mohan, Raju; Morrissey, Michael; Pratt, Benjamin; Wang, Tie-Lin published a patent.Electric Literature of 86239-00-1 The title of the patent was Triazole and imidazole derivatives for use as TGR5 agonists in the treatment of diabetes and obesity and their preparation. And the patent contained the following:
The present invention comprises TGR5 agonists of structural formula I, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprises composition comprising the compounds, N-oxides, and/or pharmaceutically acceptable salts thereof. The invention also comprises use of the compounds and compositions for treating diseases in which TGR5 is a mediator or is implicated. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases in which TGR5 is a mediator or is implicated. Compounds of formula I wherein X is N, CPh, CR4, etc.; R1 is Ph, C5-6 cycloalkyl, CH2phenyl, etc.; R2 is [CR2]pY[CR2]q-R6; p and q are independently 0 and 1; each R is independently H, C1-3 alkyl, halo, OH and CH2OH; Y is a bond, S, SO2, CHOH, O, etc.; R6 is C6-10 aryl, NH-Ph, cycloalkyl, etc.; R2 is R4 is H, C1-3 alkyl, and halo; R5 is CH2phenyl, CH2naphthalenyl, CH2-heteroaryl, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by S-alkylation of 5-(2-(3,4-dimethoxyphenyl)propan-2-yl)-1-(4-fluorophenyl)-1H-imidazole-2(3H)-thine with 2-chloro-4-fluorobenzyl bromide. All the invention compounds were evaluated for their TGR5 agonistic activity (some data given). The experimental process involved the reaction of Ethyl 3-fluoro-4-methylbenzoate(cas: 86239-00-1).Electric Literature of 86239-00-1
The Article related to imidazole triazole preparation tgr5 agonist treatment diabetes obesity, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Electric Literature of 86239-00-1
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