1059705-62-2Relevant articles and documents
Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors
Zhao, Bin,Li, Yixuan,Xu, Pan,Dai, Yang,Luo, Cheng,Sun, Yiming,Ai, Jing,Geng, Meiyu,Duan, Wenhu
supporting information, p. 629 - 634 (2016/07/06)
Fibroblast growth factor receptors (FGFRs) are important targets for cancer therapy. Herein, we describe the design, synthesis, and biological evaluation of a novel series of 1H-pyrazolo[3,4-b]pyridine derivatives as potent and selective FGFR kinase inhibitors. On the basis of its excellent in vitro potency and favorable pharmacokinetic properties, compound 7n was selected for in vivo evaluation and showed significant antitumor activity in a FGFR1-driven H1581 xenograft model. These results indicated that 7n would be a promising candidate for further drug development.
Preparation of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives as novel arginine vasopressin V2 receptor agonists
Tsukamoto, Issei,Koshio, Hiroyuki,Akamatsu, Seijiro,Kuramochi, Takahiro,Saitoh, Chikashi,Yatsu, Takeyuki,Yanai-Inamura, Hiroko,Kitada, Chika,Yamamoto, Eisaku,Sakamoto, Shuichi,Tsukamoto, Shin-ichi
experimental part, p. 9524 - 9535 (2009/04/05)
The present work describes the discovery of novel series of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene)acetamide derivatives as arginine vasopressin (AVP) V2 receptor agonists. By replacing the amide juncture in YM-35278 with a direct ring connection gave compound 10a, which acts as a V2 receptor agonist. These studies provided the potent, orally active non-peptidic V2 receptor agonists 10a and 10j.
SUBSTITUTED PHENYL-PIPERAZINE COMPOUNDS, THEIR PREPARATION AND USE IN MEDICAMENTS
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Page/Page column 98, (2008/06/13)
The present invention relates to substituted phenyl-piperazine compounds of general formula (I), a process for their preparation, medicaments comprising said substituted phenyl-piperazine compounds as well as the use of said substituted phenyl-piperazine compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.