6296-28-2Relevant academic research and scientific papers
Synthesis and biological evaluation of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists
Wang, Xuekun,Zhao, Tianxiao,Yang, Baowei,Li, Zheng,Cui, Jian,Dai, Yuxuan,Qiu, Qianqian,Qiang, Hao,Huang, Wenlong,Qian, Hai
, p. 132 - 140 (2015/02/18)
Free fatty acid receptor 1 (FFA1) is a new potential drug target for the treatment of type 2 diabetes because of its role in amplifying glucose-stimulated insulin secretion in pancreatic β-cell. In the present studies, we identified phenoxyacetic acid derivative (18b) as a potent FFA1 agonist (EC50 = 62.3 nM) based on the structure of phenylpropanoic acid derivative 4p. Moreover, compound 18b could significantly improve oral glucose tolerance in ICR mice and dose-dependently reduced glucose levels in type 2 diabetic C57BL/6 mice without observation of hypoglycemic side effect. Additionally, compound 18b exhibited acceptable PK profiles. In summary, compound 18b with ideal PK profiles exhibited good activity in vitro and in vivo, and might be a promising drug candidate for the treatment of diabetes mellitus.
ARYL PYRIMIDINE DERIVATIVES, PREPARATION METHODS AND PHARMACEUTICAL USES THEREOF
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Page/Page column 8, (2011/02/15)
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof. Various substituents in the formula (I) are as defined in the specification. The present invention also relates to a pharmaceutical composition comprising the compound of formula (I), the preparation method of compound of formula (I), and the use of the compound for the preparation of a medicament for treating and/or preventing human peroxisome proliferators activated receptor δ (hPPARδ)-associated diseases and risk factors.
ARYL PYRIMIDINE DERIVATIVES, PREPARATION METHODS AND PHARMACEUTICAL USES THEREOF
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Page/Page column 12, (2010/06/11)
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof. Various substituents in the formula (I) are as defined in the specification. The present invention also relates to a pharmaceutical composition comprising the compound of formula (I), the preparation method of compound of formula (I), and the use of the compound for the preparation of a medicament for treating and/or preventing human peroxisome proliferators activated receptor δ (hPPARδ) -associated diseases and risk factors.
ANTIBACTERIAL SMALL MOLECULES AND METHODS FOR THEIR SYNTHESIS
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Page/Page column 16, (2009/10/31)
The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use.
A new supported reagent for the photochemical generation of radicals in solution
De Luca, Lidia,Giacomelli, Giampaolo,Porcu, Giancarlo,Taddei, Maurizio
, p. 855 - 857 (2007/10/03)
matrix presented A new polymer-supported radical source was developed by loading an N-hydroxy thiazole 2(3)-thione on a Wang resin. This new supported reagent can be employed for a solid-phase version of the Hunsdiecker reaction or to liberate free alkoxy radicals, in a variant of the "catch and release" technique, under very mild conditions (irradiation with a discharge lamp) and simplifying the purification procedure.
Piperazine derivatives, medicaments comprising these compounds, their use and processes for their preparation
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, (2008/06/13)
The present invention relates to piperazine derivatives of the general formula STR1 in which Ra, Y1 to Y3 and E are defined herein, tautomers thereof, stereoisomers thereof, including their mixtures, and salts thereof, and in particular physiologically tolerated salts thereof with inorganic or organic acids or bases. These compounds have valuable pharmacological properties, such as aggregation-inhibiting activity. This invention also relates to medicaments comprising these compounds and to processes for the preparation of these compounds.
NOVEL HETEROCYCLIC COMPOUNDS HAVING PLATELET AGGREGATION INHIBITORY EFFECTS
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, (2008/06/13)
Disclosed are a compound represented by the following formula (I) and pharmacologically acceptable salt and solvate thereof having inhibitory activity against platelet aggregation: ???wherein A represents the following formula (II), (III), or (IV): A phar
Pyrone derivatives as protease inhibitors and antiviral agents
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, (2008/06/13)
The present invention relates to novel tri- and tetrasubstituted pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The pyrone derivatives are useful in the development of therapies for the treatment
Piperazine derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them
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, (2008/06/13)
Piperazine derivatives useful in the treatment or prevention of inflammation, bone degradation, thrombosis and tumor metastasis. Exemplary species are: (a) ?4-trans-?3-?4-(4-Pyridyl)-piperazin-1-yl!propionyl!amino!-cyclohexanecarboxylic acid, (b) 3-?4-trans-?4-(4-Pyridyl)-piperazin-1-yl!carbonylamino!-cyclohexylpropionic acid, (c) 3-?4-trans-?4-(4-Pyridyl)-piperazin-1-yl!malonylamino!cyclohexylcarboxylic acid, (d) Methyl ?4-trans-?3-?4-(4-pyridyl)-piperazin-1-yl!-propionyl!-amino!cyclohexane carboxylate, (e) Methyl 3-?4-trans-?4-(4-pyridyl)-piperazin-1-yl!-carbonylamino!cyclohexyl propionate, (f) Methyl ?4-trans-?4-(4-pyridyl)-piperazin-1-yl!-malonylamino!-cyclohexyl carboxylate, (g) Cyclohexyl ?4-trans-??4-(4-pyridyl)-piperazin-1-yl!-acetyl!-amino!-cyclohexane carboxylate, and (h) Isobutyl ?4-trans-??4-(4-pyridyl)-piperazin-1-yl!-acetyl!-amino!-cyclohexane carboxylate.
