Pharmaceutical composition of male sexual dysfunction

A drug, selective technology, applied in the prevention and/or treatment of male sexual dysfunction, ejaculation disorders, ejaculation disorders, which can solve the problems of not very effective, high and high dropout rates

Inactive Publication Date: 2009-06-17
埃克切西斯有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Behavior therapy is another control tool, but none are very effective and have high drop-out and relapse rates

Method used

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  • Pharmaceutical composition of male sexual dysfunction
  • Pharmaceutical composition of male sexual dysfunction
  • Pharmaceutical composition of male sexual dysfunction

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0660] Example 1. In the presence of a selective oxytocin receptor antagonist (L-368,899) ejaculation delay

[0661] The oxytocin receptor antagonist L-368,899 significantly delayed parachloramphetamine (PCA)-induced ejaculation in anesthetized rats (0.1-10 mg / kg sc) at oxytocin-selective doses. At 5.4±1.5nM (0.9xKi OT, see figure 1At free plasma concentrations of ), ejaculation was delayed by 140% (near maximal effect) - assuming that any activity at this dose was due to oxytocin receptor antagonism.

[0662] Erectile mechanisms were largely unaffected by oxytocin receptor blockade - the cup of the penis and expansion were similar between the control and oxytocin antagonist groups (see Table 1 below). Administer 1 mg / kg -1 After sc doses of L-368,899 (a dose that significantly delayed ejaculation) - 95% of PCA-induced erections resulted in cupping of the penis compared to 94% of the vehicle control group, and 61% of PCA-induced erections resulted in penis spreading, wh...

Embodiment 2

[0667] Example 2. Selective oxytocin antagonist (L-368,899) on the seminal vesicles of anesthetized rats effects of stress

[0668] L-368,899 can significantly reduce the increase in seminal vesicle pressure stimulated by splanchnic nerve in anesthetized rats (1-3 mg / kg iv). Contraction of the seminal vesicles is necessary for ejaculation, and delivery of semen into the prostatic portion of the urethra is thought to trigger ejaculation. Oxytocin has a direct contractile effect on mammalian seminal vesicles and may additionally have a neuromodulatory effect affecting sympathetic innervation in ejaculation. In this study, seminal vesicle contraction was reduced by 41% following 1 mg / kg bolus injection (see figure 2 ). Preliminary studies indicated that the achieved free plasma L-368,899 concentration after 1.0 mg / kg iv injection was approximately 60 nM - based on literature PK and protein plasma binding.

[0669] The data show that oxytocin is released during visceral ne...

Embodiment 3

[0670] Example 3. Selective Oxytocin Antagonist (L-368,899) Effects on Rat Mating Behavior for the influence

[0671] At doses up to 10 mg / kg sc, L-368,899 had no effect on the mating behavior of sexually experienced rats. Mating behavior in rodents is characterized by a series of upper body movements, with and without vaginal penetration (50-80% of the upper body results in penetration [vaginal penetration]) and ejaculation occurs after 6 to 12 thrusts. Each thrust lasts several seconds - it is not possible to quantify the length of penetration, ie the time in the vagina. The effect of L-368,899 was assessed on a number of mating parameters (see above). We focused on coitus efficiency as a measure to profile vaginal penetration.

[0672] L-368,899 had no effect on mating efficiency at any dose tested (0.05-10 mg / kg sc, see Table 2 below). Preliminary pharmacokinetic studies have shown that free plasma concentrations of 4.5 nM and 40 nM are expected to be achieved 30 mi...

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Abstract

A composition comprising a selective oxytocin antagonist for treating and / or preventing male ejaculatory disorders; the selective oxytocin antagonist can optionally be mixed with a pharmaceutically acceptable carrier, diluent or excipient.

Description

【Field of Invention】 [0001] The present invention relates to compounds and medicaments useful in the treatment or prevention of male sexual dysfunction, in particular ejaculatory disorders, such as premature ejaculation. [0002] The invention also relates to a method of preventing and / or treating male sexual dysfunction, especially ejaculation disorders, such as premature ejaculation. [0003] The present invention also relates to an assay for screening compounds useful in the treatment of male sexual dysfunction, particularly ejaculatory disorders such as premature ejaculation. [Background of the invention] [0004] male sexual dysfunction [0005] Sexual dysfunction (SD) is a distinct clinical problem that can affect both men and women. The etiology of SD can be organic or psychiatric, with the organic aspect of SD generally being caused by underlying vascular disease, such as those associated with hypertension or diabetes, by prescribed medications, and / or by psychiatr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D295/26A61K31/495A61P15/00A61K45/06A01K67/027A61K38/095A61K45/00A61P43/00C07D295/22C07K14/72
CPCA61K31/495C07D295/26A61K45/06A61P15/00A61P15/10A61P43/00A61K31/4965
Inventor A·M·奈勒R·J·拉塞尔S·D·A·斯特里特邓剑华P·H·范德格拉夫C·P·威曼
Owner 埃克切西斯有限公司
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