Treating smooth muscle hyperactivity with (r)-oxybutynin and...

A - Human Necessities – 61 – K

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A61K 31/216 (2006.01) A01N 37/10 (2006.01) A61K 31/21 (2006.01)

Patent

CA 2378754

The optically pure R(-)-isomer of oxybutynin and the optically pure R(-)- isomer of desethyl-oxybutynin, which are substantially free of the corresponding S(+)-isomers, are potent anticholinergic spasmolytics, useful for relief of symptoms associated with urinary bladder smooth muscle hyperactivity, such as Urinary Incontinence and gastrointestinal smooth muscle hyperactivity, such as Irritable Bowel Syndrome. Methods are disclosed utilizing the optically pure R(-)-isomers of oxybutynin and desethyloxybutynin for treating cholinergically mediated smooth muscle hyperactivity while minimizing the side effects associated with administration of racemic oxybutynin or racemic desethyloxybutynin.

Selon l'invention, l'isomère R(-) optiquement pur d'oxybutynine et l'isomère R(-) optiquement pur de déséthyloxybutynine, essentiellement libres des isomères S(+) correspondants, sont des agents spasmolytiques anticholinergiques servant au traitement de symptômes associés à une hyperactivité de muscles lisses de la vessie urinaire, tels que l'incontinence urinaire, et à une hyperactivité de muscles lisses gastro-intestinaux tels que le syndrome du côlon irritable. L'invention concerne des procédés faisant intervenir les isomères R(-) optiquement pur d'oxybutynine et de déséthyloxybutynine pour le traitement de l'hyperactivité de muscles lisses induite de manière cholinergique, les effets secondaires associés à l'administration d'oxybutynine racémique et de déséthyloxybuthynine racémique étant minimisés.

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