Morpholinone and morpholine derivatives and uses thereof

Details Morpholinone and morpholine derivatives and uses thereof Morpholinone and morpholine derivatives and uses thereof

C - Chemistry, Metallurgy

07

D

C07D 265/32 (2006.01) A61K 31/5375 (2006.01) A61K 31/5377 (2006.01) C07D 413/12 (2006.01) C07D 413/14 (2006.01)

Patent

CA 2355201

This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human .alpha.1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the .alpha.1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

L'invention concerne le morpholinone et les dérivés de morpholine qui constituent des antagonistes sélectifs pour les récepteurs .alpha.¿1a? humains. Cette invention concerne aussi l'utilisation de ces composés pour baisser la pression intraoculaire, inhiber la synthèse de cholestérol, détendre les tissus des voies urinaires inférieures, traiter l'hyperplasie prostatique bénigne, l'impuissance, l'arythmie, les douleurs d'origine sympathique, la migraine et toute autre maladie où seraient utiles les antagonistes des récepteurs .alpha.¿1a? humains. L'invention concerne en outre une composition pharmaceutique comprenant une quantité thérapeutiquement efficace des composés définis plus haut et un excipient pharmaceutiquement acceptable.

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