Imidazole and benzimidazole caspase inhibitors and uses thereof

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

IPC codes

C07D 233/90 (2006.01) A61K 31/4164 (2006.01) A61P 29/00 (2006.01) C07D 235/24 (2006.01) C07D 471/04 (2006.01) C07D 473/00 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)

Type

Patent

Patent number

CA 2429630

Description

This invention provides caspase inhibitors having the formula (I): wherein R1 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R2 and R3 are each independently selected from hydrogen or an optionally substituted C1-C6 aliphatic group; and R4 and R5 are each independently selected from hydrogen, an optionally substituted C1-C6 aliphatic group, or R4 and R5 taken together with the ring to which they are attached form an optionally substituted bicyclic ring. The caspase inhibitors are useful for treating a number of diseases such as cancer, acute inflammatory and autoimmune disorders, ischemic diseases and certain neurodegenerative disorders.

L'invention concerne des inhibiteurs de caspase de formule (I): dans laquelle R?1¿ désigne CO¿2?H, CH¿2?CO¿2?H, ou des esters, des amides ou des isostères de ceux-ci; R?2¿ et R?3¿ sont chacun sélectionné de manière indépendante à partir de l'hydrogène ou d'un groupe aliphatique éventuellement substitué en C¿1?-C¿6?; et R?4¿ et R?5¿ sont chacun sélectionné de manière indépendante à partir de l'hydrogène, d'un groupe aliphatique éventuellement substitué en C1-C6, ou R?4¿ et R?5¿, pris conjointement avec le noyau auquel ils sont rattachés, forment un noyau bicyclique éventuellement substitué. Les inhibiteurs de caspase sont utiles pour le traitement d'un certain nombre de maladies, telles que le cancer, des troubles inflammatoires et auto-immunitaires aigus, des maladies ischémiques et certains troubles neurodégénératifs.

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