Pharmaceutically active sulfonyl hydrazide derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 417/14 (2006.01) A61K 31/44 (2006.01) A61K 31/4436 (2006.01) A61K 31/4439 (2006.01) C07D 213/74 (2006.01) C07D 409/12 (2006.01) C07D 409/14 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2385001

The present invention is related to sulfonyl hydrazide derivatives for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonyl hydrazide derivatives. Said sulfonyl hydrazide derivatives are efficient modulators of the JNK pathway, they are in particular efficient inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonyl hydrazide derivatives as well as to methods of their preparation. In Formula (I) Ar1 and Ar2 are independently from each other an unsubstituted or substituted aryl or heteroaryl group, X1 and X2 are independently from each other O or S; R1, R2, R3 are independently from each other hydrogen or a C1-C6-alkyl substituent or R1 forms a substituted or unsubstituted 5-6-membered saturated or unsaturated ring with Ar1; or R2 and R3 form a substituted or unsubstituted 5-6-membered saturated or unsaturated ring; n is an integer from 0 to 5; G is selected from a group comprising or consisting of an unsubstituted or substituted 4-8 membered heterocycle containing at least one heteroatom, or G is a substituted or unsubstituted C1-C6-alkyl group.

La présente invention concerne des dérivés de sulfonyl hydrazide utilisés comme composés actifs au plan pharmaceutique, ainsi que des formulations pharmaceutiques renfermant lesdits dérivés. Ces dérivés sont des modulateurs efficaces de la voie JNK ainsi que des inhibiteurs particulièrement efficaces de JNK 2 et 3. De plus, cette invention concerne de nouveaux dérivés de sulfonyl hydrazide ainsi que des procédés de préparation de ces dérivés. Dans cette formule, Ar?1¿ et Ar?2¿ sont indépendamment l'un de l'autre un groupe aryle ou hétéroaryle non substitué ou substitué, X?1¿ et X?2¿ sont indépendamment l'un de l'autre O ou S; R?1¿, R?2¿, R?3¿ sont indépendamment les uns des autres hydrogène ou un substituant alkyle en C¿1?-C¿6? ou R?1¿ forme avec Ar?1¿ un noyau saturé ou insaturé à cinq ou six éléments, substitué ou non ; ou R?2¿ et R?3¿ forment un noyau saturé ou non saturé à 5 à 6 éléments, substitué ou non; n est un entier compris entre 0 et 5; G est pris dans le groupe comprenant ou composé d'un hétérocycle à 4-8 éléments, non substitué ou substitué, renfermant au moins un hétéroatome, ou G est un groupe alkyle en C¿1?-C¿6? substitué ou non.

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