PYRIDINYL-PYRIMIDINE DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATING AGENTS
申请人:Eriksen Birgitte L.
公开号:US20110144140A1
公开(公告)日:2011-06-16
This invention relates to novel pyridinyl-pyrimidine derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.
Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors
作者:F. Gellibert、M.-H. Fouchet、V.-L. Nguyen、R. Wang、G. Krysa、A.-C. de Gouville、S. Huet、N. Dodic
DOI:10.1016/j.bmcl.2009.02.087
日期:2009.4
Starting from quinazoline 3a, we designed potent and selective ALK5 inhibitors over p38MAP kinase from a rational drug design approach based on co-crystal structures in the human ALK5 kinase domain. The quinazoline 3d exhibited also in vivo activity in an acute rat model of DMN-induced liver fibrosis when administered orally at 5 mg/kg (bid). (c) 2009 Elsevier Ltd. All rights reserved.
[EN] PYRIDINYL-PYRIMIDINE DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATING AGENTS<br/>[FR] DÉRIVÉS DE PYRIDINYL-PYRIMIDINE UTILES COMME AGENTS MODULATEURS DES CANAUX POTASSIQUES
申请人:NEUROSEARCH AS
公开号:WO2008028935A2
公开(公告)日:2008-03-13
[EN] This invention relates to novel pyridinyl-pyrimidine derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels. [FR] La présente invention concerne de nouveaux dérivés de pyridinyl-pyrimidine et leur utilisation comme agents modulateurs des canaux potassiques. L'invention concerne également des compositions pharmaceutiques utiles pour le traitement ou l'atténuation de maladies ou de troubles associés à l'activité des canaux potassiques.
The present invention provides compounds of formula (I) wherein D1, D2, D3, G1, G2, G3, Y3, Y4, Y6, p and X are as defined in the claims. The invention further relates to compositions which comprise these compounds and to their in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.