84452-98-2Relevant academic research and scientific papers
SSAO INHIBITOR
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Paragraph 0427; 0428; 0429; 0451; 0452; 0453, (2020/04/02)
The present invention provides an SSAO inhibitor and an application thereof in preparing a drug for treating a disease related to SSAO. In particular, the present invention provides a compound shown in formula (IV) and a pharmaceutically acceptable salt thereof.
Discovery of SHR1653, a Highly Potent and Selective OTR Antagonist with Improved Blood-Brain Barrier Penetration
Li, Xin,Zhang, Zhigao,Chen, Yang,Wan, Hong,Sun, Jiakang,Wang, Bin,Feng, Bingqiang,Hu, Bing,Shi, Xingxing,Feng, Jun,Zhang, Lei,He, Feng,Bai, Chang,Zhang, Lianshan,Tao, Weikang
supporting information, p. 996 - 1001 (2019/06/21)
The oxytocin receptor (OTR) plays a major role in the control of male sexual responses. Antagonists of the OTR have been reported to inhibit ejaculation in animal models and serve as a potential treatment for premature ejaculation (PE). Herein, we describe a novel scaffold featuring an aryl substituted 3-azabicyclo [3.1.0] hexane structure. The lead compound, SHR1653, was shown to be a highly potent OTR antagonist, which exhibited excellent selectivity over V1AR, V1BR, and V2R. This novel molecule was shown to have a favorable pharmacokinetic profile across species, as well as robust in vivo efficacy in a rat uterine contraction model. Interestingly, SHR1653 exhibited excellent blood-brain barrier penetration, which might be beneficial for the treatment of CNS-related PE.
Efficient synthesis of tri- and difluoroacetyl hydrazides as useful building blocks for non-symmetrically substituted, fluoroalkylated 1,3,4-oxadiazoles
Mlostoń, Grzegorz,Obijalska, Emilia,?urawik, Alicja,Heimgartner, Heinz
, p. 133 - 139 (2016/07/06)
[Figure not available: see fulltext.] A convenient and efficient approach to 2-arylamino-5-fluoroalkyl-1,3,4-oxadiazoles has been established via heterocyclization of tri- and difluoroacetylated thiosemicarbazides using dicyclohexylcarbodiimide. A heteroc
Process for the production of pyrazoles
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Page/Page column 9; 15-16, (2009/01/24)
The present invention relates to novel processes for the production of compounds of formula I
Chemical compounds
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Page/Page column 48, (2008/06/13)
Compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
