Transition-metal-free synthesis of primary to tertiary carboxamides: A quick access to prodrug-pyrazinecarboxamide
摘要:
One-pot expedient and direct carbamoylation of heterocyclics is described. The transformation is realized via direct dehydrogenative aminocarbonylation of heterocyclic compounds under transition-metal-free conditions. This method is regioselective and the protocol is proved to be scalable on a gram scale. Further, the therapeutically useful antitubercular agent pyrazinecarboxamide is successfully synthesized by employing this protocol. (C) 2017 Elsevier Ltd. All rights reserved.
Compounds of formula (I) are disclosed. Compounds according to the and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
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。
[EN] 1H-BENZ IMIDAZOLE-5-CARBOXAMIDES AS ANTI-INFLAMMATORY AGENTS<br/>[FR] 1H-BENZIMIDAZOLE-5-CARBOXAMIDES COMME AGENTS ANTI-INFLAMMATOIRES
申请人:BOEHRINGER INGELHEIM INT
公开号:WO2010034796A1
公开(公告)日:2010-04-01
There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.
BENZAMIDE FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
申请人:Priestley Eldon Scott
公开号:US20100227894A1
公开(公告)日:2010-09-09
The present invention provides novel benzamide derivatives of Formula (I):
or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, W, Y, Z, R
8
, and R
9
are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
Novel N-formyl hydroxylamine compounds, compositions and methods of use
申请人:——
公开号:US20030045479A1
公开(公告)日:2003-03-06
N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl]-(carbonylamino-aryl or -heteroaryl)-azacyclo
4-7
alkanes or thiazacyclo
4-7
alkanes or imidazacyclo
4-7
alkanes have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by peptidyl deformylase inhibitors such as treatment of bacterial infections.