86786-24-5Relevant articles and documents
NEW PYRROLIDINE DERIVATIVES AND THEIR USE AS ACETYL-COA CARBOXYLASE INHIBITORS
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Page/Page column 82, (2014/05/07)
The invention relates to new pyrrolidine derivatives of the formula (I) to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
New pyrrolidine derivatives, pharmaceutical compositions and uses thereof
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Paragraph 0411, (2014/04/18)
Pyrrolidine derivatives of the formula and their use as medicaments for the treatment of obesity and type 2 diabetes.
Piperazine oxadiazole inhibitors of acetyl-CoA carboxylase
Bourbeau, Matthew P.,Siegmund, Aaron,Allen, John G.,Shu, Hong,Fotsch, Christopher,Bartberger, Michael D.,Kim, Ki-Won,Komorowski, Renee,Graham, Melissa,Busby, James,Wang, Minghan,Meyer, James,Xu, Yang,Salyers, Kevin,Fielden, Mark,Véniant, Murielle M.,Gu, Wei
supporting information, p. 10132 - 10141 (2014/01/17)
Acetyl-CoA carboxylase (ACC) is a target of interest for the treatment of metabolic syndrome. Starting from a biphenyloxadiazole screening hit, a series of piperazine oxadiazole ACC inhibitors was developed. Initial pharmacokinetic liabilities of the piperazine oxadiazoles were overcome by blocking predicted sites of metabolism, resulting in compounds with suitable properties for further in vivo studies. Compound 26 was shown to inhibit malonyl-CoA production in an in vivo pharmacodynamic assay and was advanced to a long-term efficacy study. Prolonged dosing with compound 26 resulted in impaired glucose tolerance in diet-induced obese (DIO) C57BL6 mice, an unexpected finding.
Organoiron Complexes in Organic Synthesis. Part 27. Synthesis and Reactivity of Tricarbonyliron Derivatives of 1,2-Disubstituted 4-Alkoxycyclohexadienylium Cations
Pearson, Anthony J.,Perrior, Trevor R.,Griffin, David A.
, p. 625 - 631 (2007/10/02)
The synthesis, and reactions with stable enolate nucleophiles, of 1,2-disubstituted 4-alkoxycyclohexadienylium(tricarbonyl)iron complexes (3a), (3b), (3c), and (3d) is described.Only the 1,2-dimethyl-4-isopropoxycyclohexadienylium complex (3b) was found to react with nucleophiles with sufficiently high regioselectivity to allow a useful method of preparation of 3,4,4-trisubstituted cyclohexenones.