Barbituric acid analogs as therapeutic agents

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 487/04 (2006.01) A61K 31/505 (2006.01) A61K 31/515 (2006.01) A61K 31/519 (2006.01) A61K 31/52 (2006.01) A61K 31/522 (2006.01) A61K 31/525 (2006.01) A61P 35/00 (2006.01) C07D 239/62 (2006.01) C07D 239/66 (2006.01) C07D 403/06 (2006.01) C07D 405/06 (2006.01) C07D 409/06 (2006.01) C07D 409/14 (2006.01) C07D 473/06 (2006.01) C07D 473/08 (2006.01) C07D 475/14 (2006.01)

Patent

CA 2410311

This invention pertains to active barbituric acid analogs which inhibit HIF-1 activity (e.g., the interaction between HIF-1.alpha. and p300) and thereby inhibit angiogenesis, tumorigenesis, and proliferative conditions, such as cancer. 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 HIF-1 activity, and to inhibit angiogenesis, tumorigenesis, and proliferative conditions, such as cancer.

La présente invention concerne des analogues actifs de l'acide barbiturique qui inhibent l'activité de HIF-1 (par exemple, l'interaction entre HIF-1.alpha. et p300) et, ce faisant, inhibent l'angiogenèse, la tumorigenèse et les états prolifératifs tels que le cancer. L'invention se rapporte également à des compositions pharmaceutiques renfermant les composés précités, et à l'utilisation de ces composés et compositions, tant in vitro que in vivo, pour inhiber l'activité de HIF-1 et pour inhiber l'angiogenèse, la tumorigenèse et les états prolifératifs tels que le cancer.

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