1-benzylpyrazole derivatives, preparation thereof and...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 231/12 (2006.01) A61K 31/4155 (2006.01) A61P 1/00 (2006.01) A61P 9/00 (2006.01) A61P 13/12 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) A61P 37/00 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01)

Patent

CA 2689116

The invention relates to compounds of the formula (I) in which: Y is a group selected from N(R7)CO-, -N(R7)CO-N(R7)-, -OCO-, -N(R7)S(O)n-; R1 is a hydrogen atom or a (C1-C4)alkyl group; R6 is a group selected from a (C1-C6)alkyl group, phenyl, benzyl or benzohydryl, a heterocyclic radical, a carbocyclic radical, a C3-C7)cycloalkylmethyl group; said salts being in state of a base or addition salts to an acid. The invention also relates to methods for preparing compounds of the formula (I) and to the use thereof as CB2 receptor antagonists that can cross the intestinal barrier for the treatment for autoimmune disorders, pain, gastrointestinal disorders, cardiovascular disorders and cancer.

La présente invention a pour objet des composés répondant à la formule (I): dans laquelle: - Y représente un groupement choisi parmi : -N(R7)C0-, -N(R7)CO-N(R7)-, -OCO-, N(R7)S(0)n - Rl représente un atome d'hydrogène ou un groupe (C1-C4)alkyle; - R6 représente un groupe choisi parmi: un groupe (C1 -C6)alkyle; un phényle; un benzyle ou benzhydryle; un radical hétérocyclique; un radical carbocyclique; un groupe (C3-C7)cycloalkylméthyle; à l'état de base ou de sels d'addition à un acide ainsi qu'à l'état d'hydrate ou de solvats. La présente invention concerne également les procédés de préparation et l'utilisation des composés de formule (I) comme antagonistes de récepteurs CB2 présentant un bon passage de la barrière intestinale pour le traitement des troubles auto-immunes, de la douleur, des troubles gastro-intestinaux, des troubles cardiovasculaires et du cancer.

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