Synthesis of primary amides by aminocarbonylation of aryl/hetero halides using non-gaseous NH3 and CO sources
摘要:
A practically simple method for the synthesis of primary amides via the palladium-catalysed aminocarbonylation of aromatic halides by using solid sources of gaseous ammonia and carbon monoxide is described. The system tolerated a wide variety of hindered and functionalized aryl/hetero halides and afforded good to excellent yields (69-94%) of the amide. Pharmacologically active Exalamide and Pyrazinecarboxamide were synthesised in high yields to demonstrate the effectiveness of this method. (C) 2015 Elsevier Ltd. All rights reserved.
[EN] SOMATOSTATIN MODULATORS AND USES THEREOF<br/>[FR] MODULATEURS DE LA SOMATOSTATINE ET UTILISATIONS DE CES DERNIERS
申请人:CRINETICS PHARMACEUTICALS INC
公开号:WO2019023278A1
公开(公告)日:2019-01-31
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.
Provided herein are compounds that are useful in the treatment of pain in a subject.
提供在本文件中的化合物可用于治疗主体的疼痛。
Novel Heterocyclic Compounds and Uses Thereof
申请人:Huang Zilin
公开号:US20130210818A1
公开(公告)日:2013-08-15
New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
The invention is related to compounds of Formula (I), (II), or (III):
or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
Heterocyclic compounds as ligands of the GABAA receptor
申请人:——
公开号:US20030105081A1
公开(公告)日:2003-06-05
Disclosed are heterocyclic compounds of the formula
1
and the pharmaceutically acceptable salts thereof wherein the variables A, V, Y, J, E, X, T, G, Q, W, Z, b, n and m are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABA
A
brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABA
A
brain receptor.
揭示了具有以下公式的杂环化合物及其药用可接受的盐,其中变量A、V、Y、J、E、X、T、G、Q、W、Z、b、n和m在此处被定义。这些化合物是GABA
A
脑受体的高度选择性激动剂、拮抗剂或逆激动剂,或者是GABA
A
脑受体的激动剂、拮抗剂或逆激动剂的前药。