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1.发明申请公开(公告)号：US20190100507A1
公开(公告)日：2019-04-04
申请号：US16085311
申请日：2017-03-16
Inventor： Hong LIU , Jia LI , Jiang WANG , Mingbo SU , Shuni WANG , Yubo ZHOU , Wei ZHU , Wei XU , Chunpu LI , Hualiang JIANG , Kaixian CHEN
IPC: C07D401/12 , C07D401/06 , C07D405/12 , C07D409/12 , C07D409/14 , C07D409/06 , C07D417/12 , C07D471/04 , C07D205/04 , C07D265/30 , C07D211/38 , C07D211/96 , A61P35/00
Abstract: Provided is a fluorinated cyclopropylamine compound represented by formula I, a racemate thereof, an R-isomer thereof, an S-isomer thereof, a pharmaceutical salt thereof, and a mixture thereof. Also provided are pharmaceutical compositions containing the compound, a preparation method for the compound, and uses thereof as a lysine specific demethylase 1 (LSD1) inhibitor, and in the treatment of cancers.
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公开(公告)号：US20190233456A1
公开(公告)日：2019-08-01
申请号：US16337338
申请日：2017-09-19
Inventor： Hong LIU , Jiang WANG , Shengbin ZHOU , Panfeng PENG , Yong NIAN , Shuni WANG , Shuangjie SHU , Hao SHEN , Hualiang JIANG , Kaixian CHEN
IPC: C07F15/04 , C07D207/16
CPC classification number: C07F15/045 , C07C227/34 , C07C229/34 , C07D207/16 , C07D401/04 , C07D409/12 , C07F15/04 , Y02P20/55
Abstract: Disclosed is a method for synthesizing a novel chiral ligand, a metal chelate, a variety of non-natural amino acids, Maraviroc and a key intermediate thereof. In the invention, (R)-2-methyl proline is selected and used as a starting raw material, (S)-β3-amino acid is obtained by asymmetric resolution induced by using a nickel chelate, and Maraviroc is synthesized by using (S)-3-amino-3-phenylpropionic acid as a key intermediate with a high yield and the ee value reaching 98.2% or more. The method of the present invention has widely available materials, mild synthetic process conditions, is easy to control, and produces a product of a high optical purity.
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