Novel indole and benzothiazole derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 403/12 (2006.01) A61K 31/40 (2006.01) A61K 31/415 (2006.01) A61K 31/42 (2006.01) A61K 31/425 (2006.01) C07D 277/62 (2006.01) C07D 403/14 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2246813

This invention is directed to novel indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Cette invention concerne de nouveaux composés d'indole et de benzothiazole présentant une sélectivité vis à vis de récepteurs alpha 2 humains clonés. Cette invention concerne également des utilisations de ces composés pour toutes les indications dans lesquelles l'utilisation d'un agoniste alpha 2 peut être appropriée. Spécifiquement, cela inclut l'utilisation desdits composés en tant qu'agents analgésiques, sédatifs et anesthésiques. De plus, l'invention a trait à l'utilisation de ces composés pour réduire la pression intra-oculaire, la presbytie, pour le traitement de la migraine, de l'hypertension, du sevrage alcoolique, de la toxicomanie, de la polyarthrite rhumatoïde, des douleurs ischémiques, de la spasticité, de la diarrhée, la décongestion nasale, de l'incontinence urinaire, et a trait à l'utilisation de ces composés en tant que stimulateurs de la cognition et d'agents de vasoconstriction oculaire. En outre, l'invention concerne une composition pharmaceutique contenant une dose thérapeutique efficace des composés ci-dessus définis et un excipient pharmaceutique acceptable.

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