通过醇与芳基卤的交叉偶联形成芳基-烷基醚键代表了对经典S N 2 方法的有用的战略偏离。过去几年出现了许多依赖钯基、铜基和镍基催化系统的策略。在此,我们公开了一种镍催化电化学驱动方案,以一种操作简单的方式在广泛的底物范围内实现这种有用的转化。这种电化学方法不需要强碱、昂贵的外源过渡金属催化剂(例如铱、钌),并且可以轻松地在批量或流动设置中扩大规模。有趣的是,与机械相关的光化学变体相比,电子醚化表现出增强的底物范围,因为它耐受醇亲核试剂中的叔胺官能团。
[EN] PYRIDINEDIONE CARBOXAMIDE INHIBITORS OF ENDOTHELIAL LIPASE<br/>[FR] INHIBITEURS PYRIDINEDIONE CARBOXAMIDE DE LIPASE ENDOTHÉLIALE
申请人:BRISTOL MYERS SQUIBB CO
公开号:WO2013048930A1
公开(公告)日:2013-04-04
The present invention provides compounds of Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
COMBINATION OF A MUSCARINIC RECEPTOR ANTAGONIST AND A BETA-2-ADRENOCEPTOR AGONIST
申请人:Harry Finch
公开号:US20110046191A1
公开(公告)日:2011-02-24
The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is a selected muscarinic receptor antagonist selected, and a second active ingredient which is a β
2
-adrenoceptor agonist, of use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease and asthma.
Compounds of formula (I) are useful in the treatment of diseases where enhanced M3 receptor activation is implicated, such as respiratory tract diseases:
式(I)的化合物在治疗呼吸道疾病等需要增强M3受体激活的疾病中很有用。
ARGINASE INHIBITORS AND METHODS OF USE
申请人:THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
公开号:US20160194340A1
公开(公告)日:2016-07-07
The present invention is directed to arginase inhibitor compounds of formula IA or formula IB:
or a pharmaceutically acceptable salt thereof, compositions containing these compounds, and methods of their use for the treatment and diagnosis of conditions characterized by upregulation of arginase, abnormally high arginase activity, or by abnormally low nitric oxide synthase activity.
SUBSTITUTED BENZOFURAN, BENZOTHIOPHENE AND INDOLE MCL-1 INHIBITORS
申请人:VANDERBILT UNIVERSITY
公开号:US20150336925A1
公开(公告)日:2015-11-26
The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.