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Nitrosated and nitrosylated phosphodiestrase inhibitor compounds, compositions and their uses

a technology of nitrosylated phosphodiestrase inhibitors and compositions, applied in the field of pharmaceuticals, can solve the problems of unexplored effects of modified phosphodiesterase inhibitors directly or indirectly linked with nitric oxide adducts

Inactive Publication Date: 2001-06-19
NITROMED
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the effects of modified phosphodiesterase inhibitors which are directly or indirectly linked with a nitric oxide adduct have not been investigated.
Such toxicities and adverse effects include hypotension, syncope, as well as priapism.

Method used

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  • Nitrosated and nitrosylated phosphodiestrase inhibitor compounds, compositions and their uses
  • Nitrosated and nitrosylated phosphodiestrase inhibitor compounds, compositions and their uses
  • Nitrosated and nitrosylated phosphodiestrase inhibitor compounds, compositions and their uses

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Embodiment Construction

The following definitions may be used throughout the specification.

The term "lower alkyl" as used herein refers to branched or straight chain alkyl groups comprising one to ten carbon atoms, including methyl, ethyl, propyl, isopropyl, n-butyl, t-butyl, neopentyl and the like.

The term "alkoxy" as used herein refers to R.sub.50 O-- wherein R.sub.50 is a lower alkyl group as defined herein. "Alkoxy groups" include, for example, methoxy, ethoxy, t-butoxy and the like.

The term "alkoxyalkyl" as used herein refers to an alkoxy group as previously defined appended to an alkyl group as previously defined. Examples of alkoxyalkyl include, but are not limited to, methoxymethyl, methoxyethyl, isopropoxymethyl and the like.

The term "hydroxy" as used herein refers to --OH.

The term "hydroxyalkyl" as used herein refers to a hydroxy group as previously defined appended to a lower alkyl group as previously defined.

The term "alkenyl" as used herein refers to a branched or straight chain C.sub.2 -C.sub...

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Abstract

Disclosed are nitrosated and / or nitrosylated phosphodiesterase inhibitors having the formula NOn-PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides a composition comprising a therapeutically effective amount of an phosphodiesterase inhibitor (PDE inhibitor), which can optionally be substituted with at least one NO or NO2 moiety, and one to ten fold molar excess of a compound that donates, transfers or releases nitrogen monoxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO-), or as the neutral species, nitric oxide (NO.) or which stimulates endogenous EDRF production. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides methods for treating sexual dysfunctions in males and females.

Description

FIELD OF THE INVENTIONThis invention generally relates to pharmaceuticals and more specifically to methods and compositions for treating sexual dysfunctions in males and females.BACKGROUND OF THE INVENTIONAdequate sexual function is a complex interaction of hormonal events and psychosocial relationships. There are four stages to sexual response as described in the International Journal of Gynecology & Obstetrics, 51(3):265-277 (1995). The first stage of sexual response is desire. The second stage of sexual response is arousal. Both physical and emotional stimulation may lead to breast and genital vasodilation and clitoral engorgement (vasocongestion). In the female, dilation and engorgement of the blood vessels in the labia and tissue surrounding the vagina produce the "orgasmic platform," an area at the distal third of the vagina where blood becomes sequestered. Localized perivaginal swelling and vaginal lubrication make up the changes in this stage of sexual response. Subsequently...

Claims

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Application Information

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Patent Type & Authority Patents(United States)
IPC IPC(8): A61K31/4164A61K31/444A61K31/4188A61K31/4015A61K31/4427A61K31/501A61K31/4738A61K31/519A61K31/4745A61K31/4985A61K31/52A61K31/522C07D403/10C07D207/00C07D237/04C07D207/12C07D237/00C07D215/00C07D403/04C07D215/227C07D403/00C07D213/89C07D213/00C07D279/00C07D279/04C07D401/06C07D401/10C07D471/00C07D401/00C07D401/02C07D487/14C07D401/04C07D471/04C07D473/00C07D487/04C07D487/00C07D471/14C07D473/30
CPCC07D405/14C07D487/04
Inventor GARVEY, DAVID S.SAENZ DE TEJADA, INIGO
Owner NITROMED
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