Aryl–indolyl maleimides as inhibitors of CaMKIIδ. Part 1: SAR of the aryl region
摘要:
A family of aryl-substituted maleimides was prepared and studied for their activity against calmodulin dependant kinase. Inhibitory activities against the enzyme ranged from 34 nM to > 20 mu M and were dependant upon both the nature of the aryl group and the hydrogen bond donating potential of the maleimide ring. Key interactions with the kinase ATP site and hinge region were found to be consistent with homology modeling predictions. (C) 2008 Elsevier Ltd. All rights reserved.
伯酰胺的制备是有机化学中的一个重要反应。报道的这种转化方法包括 a) 酸与氨的直接反应;b) 相应酸酐或酯的氨解和 c) 酰氯与气态或氨水的反应。除非酯具有良好的离去基团,否则酯的氨解通常是缓慢的反应。* Litjens 及其同事开发了脂肪酶催化的羧酸与铵盐作为氨源的酰胺化反应。尽管此过程温和且具有选择性,但耗时(17 天)。3 羧酸与氨的直接酰胺化需要苛刻的条件(20O0,7 bar 和无水氨)。微波加热及其在有机合成中的应用受到广泛关注,近期综述如下:我们在此报告了在微波辐射下从甲酰胺中的羧酸铵盐制备伯酰胺的直接和快速方法。据我们所知,这是利用微波技术快速合成伯酰胺的第一份报告。
[EN] CANNABIGEROL DERIVATIVES AND USE THEREOF AS CANNABINOID RECEPTOR MODULATORS<br/>[FR] DÉRIVÉS DE CANNABIGÉROL ET LEUR UTILISATION EN TANT QUE MODULATEURS DES RÉCEPTEURS CANNABINOÏDES
申请人:CANOPY GROWTH CORP
公开号:WO2021102567A1
公开(公告)日:2021-06-03
The synthesis of a range of pentylbezene- 1,3-diol compounds of formula I is disclosed. These compounds bind to cannabinoid 1 and 2 receptors (CB1 and CB2), and are thus presumed to be useful in modulating the activity of such receptors. Accordingly, the use of such synthetic cannabinoids in the treatment of various disorders mediated by CB1 and CB2 is contemplated.
[EN] PYRROLOPYRAZINE KINASE INHIBITORS<br/>[FR] INHIBITEURS DE PYRROLOPYRAZINE KINASE
申请人:HOFFMANN LA ROCHE
公开号:WO2013030138A1
公开(公告)日:2013-03-07
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
AMIDES BY MICROWAVE-ASSISTED DEHYDRATION OF AMMONIUM SALTS OF CARBOXYLIC ACIDS
作者:Yanqing Peng、Gonghua Song
DOI:10.1080/00304940209355747
日期:2002.2
mild and selective, is time-consuming (17 days).3 Direct amidation of carboxylic acids with ammonia requires drastic conditions (20O0,7 bar, and anhydrous ammonia). Microwave heating and its applications in organicsynthesis have received extensive attention and has been reviewed recently: We report herein a direct and rapid procedure for the preparation of primary amides from ammonium salts of carboxylic
伯酰胺的制备是有机化学中的一个重要反应。报道的这种转化方法包括 a) 酸与氨的直接反应;b) 相应酸酐或酯的氨解和 c) 酰氯与气态或氨水的反应。除非酯具有良好的离去基团,否则酯的氨解通常是缓慢的反应。* Litjens 及其同事开发了脂肪酶催化的羧酸与铵盐作为氨源的酰胺化反应。尽管此过程温和且具有选择性,但耗时(17 天)。3 羧酸与氨的直接酰胺化需要苛刻的条件(20O0,7 bar 和无水氨)。微波加热及其在有机合成中的应用受到广泛关注,近期综述如下:我们在此报告了在微波辐射下从甲酰胺中的羧酸铵盐制备伯酰胺的直接和快速方法。据我们所知,这是利用微波技术快速合成伯酰胺的第一份报告。
[EN] MACROLIDE ANTIBIOTICS<br/>[FR] ANTIBIOTIQUES A BASE DE MACROLIDES
申请人:GLAXO GROUP LTD
公开号:WO2002050091A1
公开(公告)日:2002-06-27
The present invention relates to 11,12 η lactone ketolides of formula (I) wherein R, R?1, R2, R3¿ are as defined herein and pharmaceutically acceptable salts and solvates thereof, to process for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.