C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/12 (2006.01) A61K 31/497 (2006.01) A61P 35/00 (2006.01) C07D 401/14 (2006.01) C07D 403/12 (2006.01) C07D 403/14 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01) C07D 413/14 (2006.01) C07D 417/14 (2006.01)
Patent
CA 2738980
The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain pyrazin- 2 - yl -pyridin- 2 -yl -amine and pyrazine - 2 - yl -pyrimidin- 4 - yl -amine compounds of formula (I), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1 ) kinase function The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1. that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or 11 inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionisi.pi.q radiation. wherein: -X= is independently -CR A5 or -N=; and the rest of the substituents are as specified in the claims.
La présente invention concerne d'une manière générale le domaine des composés thérapeutiques, et, plus spécifiquement, certains composés biarylamines (appelés ci-après composés BAA) et, notamment, certains composés pyrazin-2-yl-pyridin-2-yl-amine et pyrazine-2-yl-pyrimidin-4-yl-amine, qui, entre autres, inhibent la fonction kinase de la Checkpoint Kinase 1 (CHK1). La présente invention porte également sur des compositions pharmaceutiques comprenant de tels composés, et sur l'utilisation de tels composés et de telles compositions, à la fois in vitro et in vivo, pour inhiber la fonction kinase CHK1, et dans le traitement de maladie et d'états qui sont médiés par CHK1, qui sont améliorés par l'inhibition de la fonction kinase CHK1, entre autres, comprenant des états prolifératifs tels que le cancer, entre autres, facultativement en combinaison avec un autre agent, par exemple (a) un inhibiteur de l'ADN topoisomérase I ou II, (b) un agent d'endommagement de l'ADN ; (c) un antimétabolite ou inhibiteur de TS ; (d) un agent ciblé micro tubulaire ; et (e) un rayonnement ionisant.
Addison Glynn Jonathan
Cherry Michael
Cheung Kwai Ming
Collins Ian
Klair Sukhbinder Singh
Cancer Research Technology Limited
Kirby Eades Gale Baker
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