cas 387350-92-7, 1-(Cloromethyl)-4,5-dihydro-1H-imidazole hydrochloride | Articles data ｜lookchem

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387350-92-7

Articles about 387350-92-7Total 3 be found

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A urea-biphenyl compound and its composition and use thereof
The invention relates to biphenyl derivatives as well as a preparation method and a pharmaceutical composition and application thereof on medicines. And particularly, the invention relates to novel urea-substituted biphenyl derivatives as well as a pharma
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Paragraph 0155; 0156

(2017/08/25)

Optimization of a novel series of potent and orally bioavailable GPR119 agonists
We describe the discovery and optimization of a novel series of furo[3,2-d]pyrimidines as G protein-coupled receptor 119 agonists. Agonistic activity of 4 (EC50?=?129?nM) was improved by replacing the intramolecular hydrogen bond between the fluorine atom and the aniline hydrogen in the head moiety with a covalent C-C bond to enhance conformational restriction, which consequently gave a lead compound 12 (EC50?=?53?nM). Optimized compound 26, which was identified by the further optimization of 12, exhibited potent activity (EC50?=?42?nM) with improved clearance in liver microsomes and induced a 33% reduction in blood glucose area under the curve at a dose of 10?mg/kg in an oral glucose tolerance test in C57BL/6N mice.
Koshizawa, Tomoaki,Morimoto, Toshiharu,Watanabe, Gen,Watanabe, Toshiaki,Yamasaki, Nao,Sawada, Yoshikazu,Fukuda, Tomoaki,Okuda, Ayumu,Shibuya, Kimiyuki,Ohgiya, Tadaaki
p. 3249 - 3253
(2017/07/07)

BICYCLIC GPR119 MODULATORS
The present invention relates to compounds of Formula (I) that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of GPR119 receptor activity. The invention also relates to the process for preparation of the compounds, pharmaceutical compositions thereof. The invention further relates to methods o f treating, preventing and/or managing diseases, disorders syndromes or conditions associated with the modulation of GPR119 receptor by using either alone or in combinations of Formula (I)
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Page/Page column 38

(2012/06/15)

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Chemical Properties

Melting Point: 129-131 °C
Boiling Point: 418.8 °C at 760 mmHg
Flash Point:207.1 °C
Density: 1.261 g/cm³
Storage Temp.:Refrigerated.
PKA: 1.33±0.20(Predicted)
PSA: 54.55000
LogP: 2.27690

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