STREET, Ian Philip;SLEEBS, Brad Edmund; Jonathan Bayldon;BAELL, Jonathan Bayldon;BAELL
发明人:
BAELL, Jonathan Bayldon,STREET, Ian Philip,SLEEBS, Brad Edmund
申请号：
GBGB2012/000280
公开号：
WO2012/131297A1
申请日:
2012.03.27
申请国别(地区):
GB
年份:
2012
代理人:
摘要：
The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain fused triaryl amine compounds of the following formula (for convenience, collectively referred to herein as "FTA compounds"), which, inter alia, inhibit LIM kinase (LIMK) activity. 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 LIMK activity, and in the treatment of diseases and conditions that are mediated by LIMK, that are ameliorated by the inhibition of LIMK activity, etc., including proliferative conditions such as cancer (e.g., breast cancer, prostate cancer, melanoma, glioma, etc.), as well as vasodilation (including, e.g., hypertension, angina, cerebral vasospasm, and ischemia following subarachnoid hemorrhage), neurodegenerative disorders, atherosclerosis, fibrosis, and inflammatory diseases (including, e.g., Crohn's disease and chronic obstructive pulmonary disease (COPD)), and glaucoma (also known as ocular hypertension).La présente invention concerne généralement le domaine de composés thérapeutiques, et plus spécifiquement certains composés de triarylamine condensés de la formule suivante (par souci de commodité, collectivement appelés « composés FTA »), qui, entre autres, inhibent l'activité LIM kinase (LIMK). La présente invention concerne en outre des compositions pharmaceutiques comprenant de tels composés, et l'utilisation de tels composés et compositions, in vitro et in vivo, pour inhiber l'activité LIMK, et dans le traitement de maladies et affections qui sont médiées par LIMK, qui sont améliorées par l'inhibition de l'activité LIMK, etc., comprenant des affections prolifératives telles que le cancer (par exemple, le cancer du sein, le cancer de la prostate, le mélanome, le gliome, etc.), ainsi que la vasodilatation (comprenant, par exemple, l'hypertension, l'angor, un angiospasme cérébral, et une ischémi
