Cytoskeletal active rho kinase inhibitor compounds,...

C - Chemistry – Metallurgy – 07 – D

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C07D 401/12 (2006.01) A61K 31/454 (2006.01) A61K 31/4725 (2006.01) C07D 401/14 (2006.01)

Patent

CA 2672825

The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions.

L'invention concerne des composés actifs cytosquelettiques synthétiques qui sont des inhibiteurs de protéine kinase associée à RHO. La présente invention concerne également des compositions pharmaceutiques comprenant de tels composés et un véhicule pharmaceutiquement acceptable. L'invention concerne en outre un procédé de prévention et de traitement de maladies ou affections associées à une réorganisation cytosquelettique. Dans un mode de réalisation, le procédé traite l'augmentation de la pression intraoculaire, telle qu'un glaucome chronique primaire. Le procédé comprend l'administration à un sujet d'une quantité thérapeutiquement efficace d'un composé actif cytosquelettique représenté par la formule I ou la formule II, la quantité étant efficace pour influencer les interactions avec l'actomyosine, par exemple en conduisant à une relaxation cellulaire et à des modifications des adhérences cellule-substrat.

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