Glutamate as an Efficient Amine Donor for the Synthesis of Chiral β‐ and γ‐Amino Acids Using Transaminase
作者:Geon‐Hee Kim、Hyunwoo Jeon、Taresh P. Khobragade、Mahesh D. Patil、Sihyong Sung、Sanghan Yoon、Yumi Won、Sharad Sarak、Hyungdon Yun
DOI:10.1002/cctc.201802048
日期:2019.3.6
A recyclable glutamate amine donor system employing transaminase (TA), glutamate dehydrogenase (GluDH) and mutant formate dehydrogenase (FDHm) was developed, wherein amine donor Glu was regenerated using GluDH and thereby circumvented the inhibition of TA by α‐ketoglutarate. Various enantiopure β‐, γ‐aminoacids, and amines were successfully synthesized with high conversions and excellent enantiomeric
In particular, the present invention is concerned with compounds of the general formula (I)
wherein X, Y and R
1
to R
10
are as described herein. The compounds are V1a receptor antagonists. The invention also relates to the manufacture of compounds of formula I, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases.
Isoindolinone inhibitors of the MDM2-p53 interaction having anticancer activity
申请人:ASTEX THERAPEUTICS LIMITED
公开号:US10544132B2
公开(公告)日:2020-01-28
The invention provides a compound of formula (I):
or tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims.
Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds.