Substituted 4-anilino-7-phenyl-3-quinolinecarbonitriles as Src kinase inhibitors
摘要:
A series of substituted 4-anilino-7-phenyl-3-quinolinecarbonitriles has been prepared as Src kinase inhibitors. Optimal activity is observed with compounds that have basic amines attached via the para position of the 7-phenyl ring, and a hydrogen atom at the C-6 position. The best compounds are low nanomolar inhibitors of Src kinase, and have potent activity against Src-transformed fibroblast cells. (C) 2002 Elsevier Science Ltd. All rights reserved.
3-cyanoquinolines, 3-cyano-1,6-naphthyridines, and 3-cyano-1,7-naphthyridines as protein kinase inhibitors
申请人:American Home Products Corporation
公开号:US20020026052A1
公开(公告)日:2002-02-28
This invention provides compounds of Formula (I), having the structure
1
where T, Z, X, A, R
1
, R
2a
, R
2b
, R
2c
, R
3
, R
4
, and n are defined herein, or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of osteoporosis and polycystic kidney disease.
Pyridine derivatives and pharmaceutical compositions containing them
申请人:AstraZeneca AB
公开号:US06300352B1
公开(公告)日:2001-10-09
The invention relates to novel pyridyl derivatives, their use as medicaments, pharmaceutical formulations containing them and methods for their preparation.
Chemoselective α-Sulfidation of Amides Using Sulfoxide Reagents
作者:Mario Leypold、Kyan A. D’Angelo、Mohammad Movassaghi
DOI:10.1021/acs.orglett.0c03160
日期:2020.11.20
The direct α-sulfidation of tertiary amidesusing sulfoxide reagents under electrophilic amide activation conditions is described. Employing convenient and readily available reagents, selective functionalization takes place to generate isolable sulfonium ions en route to α-sulfide amides. Mechanistic studies identified activated sulfoxides as promoters of the desired transformation and enabled the
[EN] MITOGEN ACTIVATED PROTEIN KINASE-ACTIVATED PROTEIN KINASE-2 INHIBITING COMPOUNDS<br/>[FR] COMPOSES INHIBANT LA PROTEINE KINASE-2 ACTIVEE PAR LA PROTEINE KINASE ACTIVEE PAR DES AGENTS MITOGENES
申请人:PHARMACIA CORP
公开号:WO2004058762A1
公开(公告)日:2004-07-15
Compounds are described which inhibit mitogen activated protein kinase-activated protein kinase-2 (MK-2). Methods of using such compounds for the inhibition of MK-2, and for the prevention or treatment of a disease or disorder that is mediated by TNFα, are described, where the method involves administering to the subject an MK-2 inhibiting compound of the present invention. Therapeutic compositions, pharmaceutical compositions and kits which contain the present MK-2 inhibiting compounds are also described.
[EN] 3-CYANOQUINOLINES,3-CYANO-1,6-NAPHTHYRIDINES, AND 3-CYANO-1,7-NAPHTHYRIDINES AS PROTEIN KINASE INHIBITORS<br/>[FR] 3-CYANOQUINOLINES,3-CYANO-1,6-NAPHTHYRIDINES ET 3-CYANO-1,7-NAPHTHYRIDINES UTILISEES COMME INHIBITEURS DE PROTEINEKINASE
申请人:AMERICAN HOME PROD
公开号:WO2001072711A1
公开(公告)日:2001-10-04
Compounds of Formula (I), having the structure or a pharmaceutically salt thereof are useful as antineoplastic agents and in the treatment of osteoporosis and polycystic kidney disease.