Agent for prophylaxis and treatment of asthenopia or...

A - Human Necessities – 61 – K

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Details

A61K 31/44 (2006.01) A61K 9/08 (2006.01) A61K 31/437 (2006.01) A61K 45/00 (2006.01) A61P 27/02 (2006.01)

Patent

CA 2635412

Disclosed is a pharmaceutical composition for the prophylaxis and treatment of asthenopia or pseudomyopia, which comprises a compound having a Rho kinase inhibitory activity and a pharmaceutically acceptable carrier. The compound having the Rho kinase inhibitory activity, for example, has the following formula (I): (see formula I) wherein Ra is a group of the following formula (a), (b) or (c) : (see formula (a)) (see formula (b)) (see formula (c)) in which R is hydrogen, alkyl, phenyl or the like; R1 is hydrogen, alkyl, phenyl or the like; R2 is hydrogen or alkyl; R3 and R4 are hydrogen, alkyl or the like; A is a bond or alkylene; L is hydrogen, alkyl or the like; R5 is hydrogen, hydroxyl or the like; R b is hydrogen, alkyl or the like; and R c is optionally substituted heterocycle containing nitrogen.

Est divulguée dans l'invention une préparation pharmaceutique destinée à la prophylaxie et au traitement de l'asthénopie ou de la pseudomyopie, qui contient un composé présentant une activité inhibitrice envers la kinase Rho et un vecteur pharmaceutiquement acceptable. Le composé présentant une activité inhibitrice envers la kinase Rho, par exemple, a la formule (I) suivante : (voir formule I) où Ra est un groupe ayant la formule (a), (b) ou (c) : (voir la formule ¬a|) (voir la formule ¬b|) (voir la formule ¬c|) dans laquelle R est un hydrogène, un alkyle, un phényle ou un groupe apparenté; R1 est un hydrogène, un alkyle, un phényle ou un groupe apparenté; R2 est un hydrogène ou un alkyle; R3 et R4 sont des hydrogènes, des alkyles ou des groupes apparentés; A est une liaison ou un alcoylène; L est un hydrogène, un alkyle ou un groupe apparenté; R5 est un hydrogène, un hydroxyle ou un groupe apparenté; R b est un hydrogène, un alkyle ou un groupe apparenté; et R c est un hétérocycle facultativement substitué contenant de l'azote.

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