Novel indazole derivative

C - Chemistry – Metallurgy – 07 – D

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C07D 231/56 (2006.01) A61K 31/416 (2006.01) A61K 31/4439 (2006.01) A61P 27/06 (2006.01) A61P 43/00 (2006.01) C07D 401/04 (2006.01)

Patent

CA 2542609

To prepare a novel indazole derivative useful as a medicine and to find out a new pharmacological activity of the derivative. The compound is represented by the general formula [I] and has excellent Rho-kinase inhibitory activity. In the formula, ring X is a benzene ring or pyridine ring; R1 and R2 each is hydrogen or alkyl; R3 and R4 each is halogeno, hydrogen, OH, alkoxy, alkenyloxy, alkynyloxy, cycloalkyloxy, cycloalkenyloxy, aryloxy, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, carboxy, hydrocarbonyl, alkylcarbonyl, etc.; and R5 is halogeno, hydrogen, OH, alkoxy, aryloxy, alkyl, or aryl. These groups may be substituted.

L'invention concerne un procédé de préparation d'un nouveau dérivé d'indazole utile comme médicament, et une nouvelle application pharmacologique de ce dérivé. Le composé est représenté par la formule générale I et possède une excellente activité d'inhibition de la kinase Rho. Dans la formule, le noyau X représente un noyau benzène ou un noyau pyridine ; R?1¿ et R?2¿ représentent chacun hydrogène ou alkyle ; R?3¿ et R?4¿ représentent chacun halogéno, hydrogène, OH, alcoxy, alcényloxy, alcynyloxy, cycloalkyloxy, cycloalcényloxy, aryloxy, alkyle, alcényle, alcynyle, cycloalkyle, cycloalcényle, aryle, carboxy, hydrocarbonyle, alkylcarbonyle, etc. ; et R?5¿ représente halogéno, hydrogène, OH, alcoxy, aryloxy, alkyle ou aryle. Les groupes peuvent être substitués.

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