Thienopyrazole derivative having pde7 inhibitory activity

C - Chemistry – Metallurgy – 07 – D

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C07D 495/04 (2006.01) A61K 31/4162 (2006.01) A61K 31/4166 (2006.01) A61K 31/4188 (2006.01) A61K 31/422 (2006.01) A61K 31/427 (2006.01) A61K 31/433 (2006.01) A61K 31/438 (2006.01) A61K 31/4439 (2006.01) A61K 31/454 (2006.01) A61K 31/496 (2006.01) A61K 31/5377 (2006.01) A61K 31/551 (2006.01) A61P 1/00 (2006.01) A61P 1/04 (2006.01) A61P 1/16 (2006.01) A61P 1/18 (2006.01) A61P 9/10 (2006.01) A61P 11/00 (2006.01) A61P 11/06 (2006.01) A61P 17/00 (2006.01) A61P 17/06 (2006.01) A61P 19/00 (2006.01) A61P 25/00 (2006

Patent

CA 2569530

A thienopyrazole derivative represented by the following formula (I): [wherein preferably, R1 is cyclohexyl, cycloheptyl, or tetrahydropyranyl; R2 is methyl; R3 is hydrogen; and R4 is -CONR5R6 (wherein either of R5 and R6 is hydrogen)]. It has selective inhibitory activity against PDE7 and thus heightens the intracellular cAMP level to inhibit the activation of T cells. The derivative is hence useful in the prevention and treatment of various allergic diseases and inflammatory/immunologic diseases.

Dérivé de thiénopyrazole représenté par la formule (I) suivante : [dans laquelle de préférence, R1 est un cyclohexyle, un cycloheptyle ou un tétrahydropyranyle ; R2 est un méthyle ; R3 est un hydrogène ; et R4 est -CONR5R6 (où l'un ou l'autre de R5 et R6 est un hydrogène)]. Il possède une activité d'inhibition sélective vis-à-vis de la PDE7 et donc élève le niveau d'AMPc intracellulaire pour inhiber l'activation de cellules T. Le dérivé est donc utile dans la prévention et le traitement de différentes maladies allergiques et maladies inflammatoires/immunologiques.

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