1292822-17-3Relevant academic research and scientific papers
Development of novel NK3 receptor antagonists with reduced environmental impact
Yamamoto, Koki,Okazaki, Shiho,Ohno, Hiroaki,Matsuda, Fuko,Ohkura, Satoshi,Maeda, Kei-ichiro,Fujii, Nobutaka,Oishi, Shinya
, p. 3494 - 3500 (2016)
The neurokinin B (NKB)–neurokinin-3 receptor (NK3R) signaling positively regulates the release of gonadotropin-releasing hormone (GnRH) from the hypothalamus. The NK3R-selective antagonists may suppress the reproductive functions of mammals. For developme
NOVEL COMPOUND, AGENT AND NK3 RECEPTOR ANTAGONIST
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Paragraph 0070; 0071, (2017/08/02)
PROBLEM TO BE SOLVED: To provide a NK3 receptor antagonist that inhibits the propagation of animals without adverse effect on an ecological system. SOLUTION: The present invention provides a compound represented by formula (I') (R1 is H, a hydroxy group or the like; R2 is a hydroxy group, a mercapto group or the like; R3 is a phenyl group or naphthyl group). SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
Synthesis and SAR of sulfoxide substituted carboxyquinolines as NK3 receptor antagonists
Xiong, Hui,Kang, James,Woods, James M.,McCauley Jr., John P.,Koether, Gerard M.,Albert, Jeffrey S.,Hinkley, Lindsay,Li, Yan,Gadient, Reto A.,Simpson, Thomas R.
scheme or table, p. 1896 - 1899 (2011/05/05)
The neurokinin-3 (NK3) receptor is regarded as a potential novel target for treating patients with schizophrenia. Herein we report the synthesis and SAR of a series of C3-alkylsulfoxide substituted quinolines as potent NK3 receptor antagonists. These compounds have excellent NK3 functional activity, good selectivity and drug-like properties. Several key compounds have good in vitro/in vivo DMPK characteristics, and are active in a gerbil locomotor activity model.
