- Synthesis and biological evaluation of thiazole derivatives as GPR119 agonists
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A series of 4-(phenoxymethyl)thiazole derivatives was synthesized and evaluated for their GPR119 agonistic effect. Several 4-(phenoxymethyl)thiazoles with pyrrolidine-2,5-dione moieties showed potent GPR119 agonistic activities. Among them, compound 27 and 32d showed good in vitro activity with an EC50 value of 49 nM and 18 nM, respectively with improved human and rat liver microsomal stability compare with MBX-2982. Compound 27 & 32d did not exhibit significant CYP inhibition, hERG binding, and cytotoxicity. Moreover, these compounds lowered the glucose excursion in mice in an oral glucose-tolerance test.
- Kim, Hyojin,Cho, Suk Joon,Yoo, Minjin,Kang, Seung Kyu,Kim, Kwang Rok,Lee, Hwan Hee,Song, Jin Sook,Rhee, Sang Dal,Jung, Won Hoon,Ahn, Jin Hee,Jung, Jae-Kyung,Jung, Kwan-Young
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p. 5213 - 5220
(2017/11/21)
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- PREPARATION OF 5-ETHYL-2-{4-[4-(4-TETRAZOL-1-YL-PHENOXYMETHYL)-THIAZOL-2-YL]-PIPERIDIN-1-YL}-PYRIMIDINE
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Processes and intermediates for the synthesis of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine are provided.
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Page/Page column 19-20
(2011/12/14)
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- COMPOSITIONS OF 5-ETHYL-2--PYRIMIDINE
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This invention relates to the field of pharmaceutical chemistry and, more specifically, to pharmaceutical formulations as well as to intermediates used to prepare such formulations and to methods for manufacturing such formulations.
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Page/Page column 15
(2012/01/13)
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- SUBSTITUTED TETRAZOL-1-YL-PHENOXYMETHYL-THIAZOL-2-YL-PIPERIDINYL-PYRIMIDINE SALTS
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Crystalline salts of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine, compositions thereof, methods for their preparation, and methods for their use are disclosed.
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