Biomimetic synthetic studies on lactonamycin: an expedient synthesis of dihydroxy-isoindolinone-carboxylates
摘要:
The synthesis of dihydroxy-isoindolinone-carboxylates from a dioxinone keto-ester and N-protected sarcosine without the use of phenolic protection is described. Base-induced aromatization of the dioxinone diketo-ester followed by lactamization furnished the desired dihydroxy-isoindolinone moiety, which could be used as an EF-ring precursor toward the synthesis of lactonamycin. (C) 2011 Elsevier Ltd. All rights reserved.
A method for the synthesis of sulfonyl chlorides and bromides from the corresponding sulfonate salts is described. The method gives good yields of the acid halides under very mild conditions, and is compatible with both acid and base sensitive functionalities.
[EN] THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS<br/>[FR] DÉRIVÉS DE THIÉNO-PYRIDINE UTILISÉS COMME INHIBITEURS DE MEK
申请人:UCB PHARMA SA
公开号:WO2009153554A1
公开(公告)日:2009-12-23
A series of thieno[2,3-6]pyridine derivatives, attached at the 2-position to a substituted anilino moiety, which are substituted in the 3-position by a carbonyl group linked to a pyrrolidin-1-yl ring which in turn forms part of a heteroatom-containing fused bicyclic ring system, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.
Macrocyclic anilinopyrimidines with substituted sulphoximine as selective inhibitors of cell cycle kinases
申请人:Lucking Ulrich
公开号:US20070191393A1
公开(公告)日:2007-08-16
The invention relates to macrocyclic anilinopyrimidines with substituted sulphoximine of the general formula I, processes for their preparation, and their use as medicaments.
这项发明涉及一般式I的带有取代磺酰羟肟的大环苯胺嘧啶类化合物,以及它们的制备方法和作为药物的用途。
BCL-XL Inhibitory Compounds and Antibody Drug Conjugates Including the Same
申请人:Ackler Scott L.
公开号:US20160158377A1
公开(公告)日:2016-06-09
Small molecule Bcl-xL inhibitors and Antibody Drug Conjugates (ADCs) comprising small molecule Bcl-xL inhibitors are disclosed herein. The Bcl-xL inhibitors and ADCs of the disclosure are useful for, among other things, inhibiting anti-apoptotic Bcl-xL proteins as a therapeutic approach towards the treatment of diseases that involve a dysregulated apoptosis pathway.
Synthesis of Oxindoles through the Gold-Catalyzed Oxidation of<i>N</i>-Arylynamides
作者:Liu-Qing Yang、Kai-Bing Wang、Chuan-Ying Li
DOI:10.1002/ejoc.201300162
日期:2013.5
α-Oxo gold carbenoids generated by the oxidation of N-arylynamides can be trapped intramolecularly at the ortho position of the aryl ring to give functionalized oxindoles under mild reaction conditions. PyridineN-oxide works as the oxidant, ligand, and base in this transformation.
Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
申请人:Mueller Georg Stephan
公开号:US20050256099A1
公开(公告)日:2005-11-17
The present invention relates to the CGRP antagonists of general formula
wherein A, X, Q and R
1
to R
3
are defined as in claim
1,
the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, mixtures and salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, their use and processes for preparing them.