AZETIDINE COMPOUNDS AS GRP119 MODULATORS FOR THE TREATMENT OF DIABETES, OBESITY, DYSLIPIDEMIA AND RELATED DISORDERS
申请人:SANOFI
公开号:US20180237419A1
公开(公告)日:2018-08-23
The present disclosure relates to azetidine compounds. The azetidine compounds are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The present disclosure furthermore relates to the use of azetidine compounds as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
The present invention provides a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes and the like, and having superior efficacy.
The present invention relates to a compound represented by the formula (I):
wherein each symbol is as defined in the specification, or a salt thereof.
The present invention provides a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes and the like, and having superior efficacy.
The present invention relates to a compound represented by the formula (I):
wherein each symbol is as defined in the specification, or a salt thereof.
Discovery of Oxazolobenzimidazoles as Positive Allosteric Modulators for the mGluR2 Receptor
作者:Robert M. Garbaccio、Edward J. Brnardic、Mark E. Fraley、George D. Hartman、Pete H. Hutson、Julie A. O'Brien、Brian C. Magliaro、Jason M. Uslaner、Sarah L. Huszar、Kerry L. Fillgrove、James H. Small、Cuyue Tang、Yuhsin Kuo、Marlene A. Jacobson
DOI:10.1021/ml100115a
日期:2010.11.11
Novel oxazolobenzimidazoles are described as potent and selective positive allosteric modulators of the metabotropic glutamate receptor 2. The discovery of this class and optimization of its physicial and pharmacokinetic properties led to the identification of potent and orally bioavailable compounds (20 and 21) as advanced leads. Compound 20 (TBPCOB) was shown to have robust activity in a PCP-induced hyperlocomotion model in rat, an assay responsive to clinical antipsychotic treatments for schizophrenia.