链霉菌属 通过使用2-甲基-1-吡咯啉(2-MPN)筛选,发现GF3587和3546是具有高R-和S-选择性的亚胺还原菌株。他们的全细胞催化剂产生91 mMR -2-甲基吡咯烷(R -2-MP)含99.2%ee和27.5 mM S -2-MP(92.3%ee),由2-MPN转化为91-92%,葡萄糖, 分别。
The present invention provides compounds of formula (I*):
their use as H
3
inhibitors, processes for their preparation, and pharmaceutical compositions thereof.
本发明提供了式(I*)的化合物:它们作为H3抑制剂的用途,其制备方法以及药物组合物。
PHENYLQUINAZOLINE DERIVATIVES
申请人:Eggenweiler Hans-Michael
公开号:US20130178443A1
公开(公告)日:2013-07-11
Novel quinazolinamide derivatives of the formula (I), in which R1-R43 and X have the meanings indicated in claim
1
, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
[EN] SUBSTITUTED IMIDAZOPYRIDINES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS<br/>[FR] IMIDAZOPYRIDINES SUBSTITUÉES, LEUR PRÉPARATION ET LEUR UTILISATION COMME MÉDICAMENTS
申请人:NEOMED INST
公开号:WO2017066876A1
公开(公告)日:2017-04-27
This application relates to substituted imidazopyridines, compositions comprising them and their uses in the treatment of diseases and conditions in which inhibition of a bromodomain is indicated. For example, the application relates to substituted imidazopyridines and to their use as bromodomain inhibitors. The present application is also related to the treatment or prevention of proliferative disorders, auto-immune disorders, inflammatory disorders, dermal disorders, and neoplasms, including tumors and/or cancers.
Discovery of an MLLT1/3 YEATS Domain Chemical Probe
作者:Moses Moustakim、Thomas Christott、Octovia P. Monteiro、James Bennett、Charline Giroud、Jennifer Ward、Catherine M. Rogers、Paul Smith、Ioanna Panagakou、Laura Díaz-Sáez、Suet Ling Felce、Vicki Gamble、Carina Gileadi、Nadia Halidi、David Heidenreich、Apirat Chaikuad、Stefan Knapp、Kilian V. M. Huber、Gillian Farnie、Jag Heer、Nenad Manevski、Gennady Poda、Rima Al-awar、Darren J. Dixon、Paul E. Brennan、Oleg Fedorov
DOI:10.1002/anie.201810617
日期:2018.12.10
YEATS domain (YD) containing proteins are an emerging class of epigenetic targets in drug discovery. Dysregulation of these modified lysine-binding proteins has been linked to the onset and progression of cancers. We herein report the discovery and characterisation of the first small-molecule chemical probe, SGC-iMLLT, for the YD of MLLT1 (ENL/YEATS1) and MLLT3 (AF9/YEATS3). SGC-iMLLT is a potent and
[EN] COMPOUNDS AND THEIR METHODS OF USE<br/>[FR] COMPOSÉS ET LEURS MÉTHODES D'UTILISATION
申请人:PRAXIS PREC MEDICINES INC
公开号:WO2018148745A1
公开(公告)日:2018-08-16
The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including Dravet syndrome or epilepsy are also provided herein.