PHENETHYLAMIDE DERIVATIVES AND THEIR HETEROCYCLIC ANALOGUES
申请人:Aissaoui Hamed
公开号:US20110212968A1
公开(公告)日:2011-09-01
The invention relates to novel phenethylamide derivatives and their wherein A, B, R
1
, R
2
and R
3
are as described in the application, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
The present invention relates to novel compounds and method for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (II) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R8, R9, R10, R12, Z, Y and m are as defined herein.
本发明涉及新型化合物和去泛素化酶(DUB)抑制剂的制造方法。特别是,本发明涉及泛素 C 端水解酶 30(USP30)的抑制。本发明还涉及 DUB 抑制剂在治疗线粒体功能障碍和癌症方面的用途。本发明的化合物包括具有式(II)的化合物或其药学上可接受的盐,其中R1、R2、R3、R4、R5、R8、R9、R10、R12、Z、Y和m如本文所定义。
Synthesis of 4-Aryl and Unsymmetrical 4,6-Diarylpyrimidines by the Suzuki-Miyaura Cross-Coupling Reaction
作者:Victor Snieckus、Gerald J. Tanoury、Sahaj Gupta、Jennifer A. Melanson、M Selim Hossain、Louis Vaillancourt、William A. Nugent
DOI:10.3987/com-18-13956
日期:——
A two-step procedure for the synthesis of 4-arylpyrimidines from inexpensive 4,6-dichloropyrimidine via a Suzuki-Miyaura/hydrodechlorination reaction sequence is described. The reaction resulted in the predominant formation of mono-arylated product. The cross-coupling of 4-chloro-6-substituted pyrimidines with various aryl/heteroarylboronic acids also furnished 4,6-disubstituted pyrimidines in acceptable yields.
1-CYANO-PYRROLIDINE COMPOUNDS AS USP30 INHIBITORS
申请人:Mission Therapeutics Limited
公开号:EP3277677B9
公开(公告)日:2021-07-14
BARAM, S. G.;SHKURKO, O. P.;MAMAEV, V. P., IZV. CO AN CCCP. CEP. XIM. N., 1983, N 4/2, 111-117