67048-76-4Relevant academic research and scientific papers
Discovery of an Isothiazole-Based Phenylpropanoic Acid GPR120 Agonist as a Development Candidate for Type 2 Diabetes
Zhang, Xuqing,Cai, Chaozhong,Sui, Zhihua,Macielag, Mark,Wang, Yuanping,Yan, Wen,Suckow, Arthur,Hua, Hong,Bell, Austin,Haug, Peter,Clapper, Wilma,Jenkinson, Celia,Gunnet, Joseph,Leonard, James,Murray, William V.
, p. 947 - 952 (2017/09/22)
We have discovered a novel series of isothiazole-based phenylpropanoic acids as GPR120 agonists. Extensive structure-activity relationship studies led to the discovery of a potent GPR120 agonist 4x, which displayed good EC50 values in both calcium and β-arrestin assays. It also presented good pharmaceutical properties and a favorable PK profile. Moreover, it demonstrated in vivo antidiabetic activity in C57BL/6 DIO mice. Studies in WT and knockout DIO mice showed that it improved glucose handling during an OGTT via GPR120. Overall, 4x possessed promising antidiabetic effect and good safety profile to be a development candidate.
Isothiazole derivatives as GPR120 agonists for the treatment of type II diabetes
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, (2015/07/07)
Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, G, and Q are defined herein.
ISOTHIAZOLE DERIVATIVES AS GPR120 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES
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, (2015/11/02)
Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, G, and Q are defined herein.
GPR120 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES
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, (2014/09/30)
Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, G, and Q are defined herein; and wherein R11, R21, R41, RB1 and G1, are defined herein.
ISOTHIAZOLE AND PYRAZOLE DERIVATIVES FOR USE AS PLANT GROWTH REGULATORS
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Page/Page column 49, (2010/08/05)
The present invention relates to isothiazole and pyrazole compounds of formula (I) having plant growth regulating properties, to agricultural compositions comprising them, and to the use of said compounds for regulating plant growth.
ISOTHIAZOLE AND PYRAZOLE DERIVATIVES AS FUNGICIDES
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Page/Page column 48, (2009/03/07)
The present invention relates to compounds of Formula (I) wherein R1, R2, R3 or R4 are as defined in claim 1 or a salt or N-oxide thereof and their use in methods for the control and/or prevention of fungal infe
3-Aryl-4-isothiazolecarboxylic acid and 3-aryl-4-isoxazolecarboxylic acid derivatives and their use as herbicides
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, (2008/06/13)
Carboxylic acid derivatives having the formula STR1 have been found to be effective herbicides. They are especially effective when applied as a pre-emergent herbicide.
