146256-98-6Relevant articles and documents
(S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements and Structural and Biological Investigation
Brogi, Simone,Brindisi, Margherita,Butini, Stefania,Kshirsagar, Giridhar U.,Maramai, Samuele,Chemi, Giulia,Gemma, Sandra,Campiani, Giuseppe,Novellino, Ettore,Fiorenzani, Paolo,Pinassi, Jessica,Aloisi, Anna Maria,Gynther, Mikko,Venskutonyte, Raminta,Han, Liwei,Frydenvang, Karla,Kastrup, Jette Sandholm,Pickering, Darryl S.
supporting information, p. 2124 - 2130 (2018/03/21)
Starting from 1-4 and 7 structural templates, analogues based on bioisosteric replacements (5a-c vs 1, 2 and 6 vs 7) were synthesized for completing the SAR analysis. Interesting binding properties at GluA2, GluK1, and GluK3 receptors were discovered. The requirements for GluK3 interaction were elucidated by determining the X-ray structures of the GluK3-LBD with 2 and 5c and by computational studies. Antinociceptive potential was demonstrated for GluK1 partial agonist 3 and antagonist 7 (2 mg/kg ip).
Preparation method for omarigliptin midbody
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Paragraph 0030-0032, (2017/07/19)
The invention provides an efficient and simple preparation method for omarigliptin midbody pyrrole and [3,4-c] pyrazol-5(2H,4H,6H)-carboxylic acid tert-butyl ester, wherein the total recovery ratio is close to 50%. The preparation method is easy to operate, the recovery ratio is higher, three produced wastes are less, and the method is suitable for industrialized production.
ANTI-ANGIOGENESIS COMPOUND, INTERMEDIATE AND USE THEREOF
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, (2016/11/02)
Disclosed are an anti-abnormal proliferation of angiogenesis compound represented by formula I, use and intermediate thereof. The compound has good effect against abnormal proliferation of angiogenesis, and the activity of the compound is produced by inhibiting VEGFR2. The compound can be used for treating diseases, such as wet macular degeneration, inflammation, malignant tumor and the like, caused by abnormity of angiogenesis and protein kinases such as VEGFR2, FGFR2 and the like.