One-pot synthesis of sulfonamides from methyl sulfinates using ultrasound
摘要:
Room temperature ultrasonic irradiation of neat mixtures of methyl sulfinates and primary or secondary amines (1.5 equiv) produced sulfinamides, which on m-CPBA oxidation (in dichloromethane) were converted into the corresponding sulfonamides. The two steps can be accomplished in one pot, in good overall yields, when using secondary amines, but primary amines give better sulfonamide yields when the peracid oxidation is effected on the purified sulfinamide. This constitutes a mild, efficient, and potentially scalable route to sulfonamides, which obviates the use of water sensitive, often lachrymatory sulfonyl chlorides and large reagent excesses. (C) 2011 Elsevier Ltd. All rights reserved.
PYRROLOPYRAZINE-SPIROCYCLIC PIPERIDINE AMIDES AS MODULATORS OF ION CHANNELS
申请人:Hadida Ruah Sara Sabina
公开号:US20120196869A1
公开(公告)日:2012-08-02
The invention relates to pyrrolopyrazine-spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
METHODS AND INTERMEDIATES FOR PREPARING PHARMACEUTICAL AGENTS
申请人:Polniaszek Richard
公开号:US20100256366A1
公开(公告)日:2010-10-07
The invention provides methods and intermediates that are useful for preparing a compound of formula I:
and salts thereof.
本发明提供了用于制备公式I化合物的有用方法和中间体:
及其盐类。
[EN] COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY<br/>[FR] COMPOSÉS ET COMPOSITIONS POUR TRAITER DES ÉTATS ASSOCIÉS À UNE ACTIVITÉ DE STING
申请人:IFM DUE INC
公开号:WO2020252240A1
公开(公告)日:2020-12-17
This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
[EN] AMINO - PYRIMIDINE COMPOUNDS AS INHIBITORS OF TBKL AND/OR IKK EPSILON<br/>[FR] COMPOSÉS D'AMINO-PYRIMIDINE EN TANT QU'INHIBITEURS DE TBKL ET OU D'IKK EPSILON
申请人:MYREXIS INC
公开号:WO2011046970A1
公开(公告)日:2011-04-21
The invention relates to certain amino-pyrimidine compounds which inhibit TBK1 and/or IKK epsilon and which may therefore find application in treating inflammation, cancer, septic shock and/or Primary open Angle Glaucoma (POAG).
HETEROCYCLIC MODULATORS OF HIF ACTIVITY FOR TREATMENT OF DISEASE
申请人:Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer Center
公开号:US20140057914A1
公开(公告)日:2014-02-27
The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.