钯催化的羰基化反应是合成有价值分子的有效方法。然而,通过经典的低价钯催化实现具有优异产率和化学选择性、区域选择性和对映选择性的羰基化是极具挑战性的。在此,我们描述了使用高价钯催化策略并使用手性亚砜膦 (SOP) 配体的对映选择性羰基化反应。这种双氨基羰基化反应开始于氨基甲酰钯 (II) 物种的形成,它与环状二芳基碘盐进行对映选择性氧化加成,生成钯 (IV) 中间体,然后进行第二次 CO 插入和还原消除。该机制已通过实验和计算研究得到说明。
[EN] CINNOLINE DERIVATIVES AS AS BTK INHIBITORS<br/>[FR] DÉRIVÉS DE CINNOLINE EN TANT QU'EN TANT QU'INHIBITEURS DE LA BTK
申请人:TAKEDA PHARMACEUTICAL
公开号:WO2013148603A1
公开(公告)日:2013-10-03
Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined in the specification. The compounds are inhibitors of Bruton's tyrosine kinase (BTK). This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders or conditions associated with BTK.
[EN] 4,5-DIHYDRO-6H-THIENO[3,2-D]BENZAZEPINE DERIVATIVES AND THEIR USE TO TREAT RESPIRATORY SYNCYTIAL VIRUS (RSV) INFECTIONS<br/>[FR] DÉRIVÉS DE 4,5-DIHYDRO-6H-THIÉNO[3,2-D] ET LEUR UTILISATION POUR TRAITER LES INFECTIONS À VIRUS RESPIRATOIRE SYNCYTIAL (VRS)
申请人:PULMOCIDE LTD
公开号:WO2016097761A1
公开(公告)日:2016-06-23
There are provided inter alia compounds which are intended to treat or prevent respiratory syncytial virus infections and associated disease particularly infections caused by the A and B strains thereof.
其中提供了一些化合物,旨在治疗或预防呼吸道合胞病毒感染及相关疾病,特别是由其A和B亚型引起的感染。
[EN] SOMATOSTATIN MODULATORS AND USES THEREOF<br/>[FR] MODULATEURS DE SOMATOSTATINE ET LEURS UTILISATIONS
申请人:CRINETICS PHARMACEUTICALS INC
公开号:WO2019157458A1
公开(公告)日:2019-08-15
Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.
[EN] SULFONANILIDE AND BENZYLSULFONYL DERIVATIVES, AND COMPOSITIONS AND METHODS THEREOF<br/>[FR] DÉRIVÉS DE SULFONANILIDE ET BENZYLSULFONYLE, ET COMPOSITIONS ET PROCÉDÉS ASSOCIÉS
申请人:LYSOWAY THERAPEUTICS INC
公开号:WO2022076383A1
公开(公告)日:2022-04-14
The invention provides novel sulfonanilide and benzylsulfonyl derivatives, and compositions and methods of preparation and use thereof, that are useful in treating various diseases and disorders related to TRPML activities such as lysosome storage diseases, muscular dystrophy, age-related common neurodegenerative diseases, oxidative stress or reactive oxygen species (ROS) related diseases, and ageing.