Treating obesity with selective androgen receptor modulators

A technology of androgen receptor and obesity, which is applied in the fields of suppression, treatment, prevention, suppression or reduction of obesity, and can solve problems such as unclear molecular mechanisms

Inactive Publication Date: 2006-01-25
GTX INCORPORATED
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although there is evidence that body weight is physiologically regulated, the molecular mechanisms remain unclear

Method used

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  • Treating obesity with selective androgen receptor modulators
  • Treating obesity with selective androgen receptor modulators
  • Treating obesity with selective androgen receptor modulators

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0272] Effects of Compound VI and Compound VII on Organ Weights and Leptin Levels

[0273]

[0274] In a recent pharmacological study, applicants identified two SARMs (compounds VI and VII) with high androgen receptor (AR) binding affinity in vitro and androgenic and anabolic activity in vivo. Since compounds VI and VII exhibit tissue-selective anabolic activity, the effects of these compounds on target organ weight and leptin levels were tested in intact male rats following short- and long-term drug treatment, target organ weight and leptin levels A hallmark of anabolic action and has been linked to obesity.

[0275] method:

[0276] Immature male Sprague-Dawley rats (body weight 195-205 g) were used in this study. Animals were divided into groups of 15 animals (5 animals per time point) and received the following treatments: (1) vehicle control, (2) testosterone propionate dissolved in vehicle solution at a dose of 500 μg / day, (3) compound VI dissolved in the vehicle...

Embodiment 2

[0284] Effect of Compound VI on Lean Mass and Percent Body Fat

[0285] method:

[0286] 230 female Sprague-Dawley rats (23 weeks old) were used in these studies.

[0287] Animals were randomized (ten per group) into the respective treatment groups listed in Table 2 below. Animals in groups 6 to 23 were ovariectomized on day 0 of the experiment.

[0288] Dosing of Compound VI, bicalutamide (anti-androgen) and / or DHT was initiated on Day 0 or Day 90 and the target compound was given by daily subcutaneous injection (0.20 mL) and continued until Day 120 or Day 90 of the study. 210 days. Drug solutions were prepared daily by dissolving in DMSO and diluting with PEG 300. The percentage of DMSO determined by solubility based test compound was the same in all vehicles (17.6%).

[0289] As shown in Table 2, whole body DEXA images were acquired up to 120 days or 210 days after ovariectomy. Lean body mass (LBM), fat mass (FM) and total body mass (TBM) were determined at each tim...

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PUM

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Abstract

This invention relates to the prevention and treatment of obesity. More particularly, this invention relates to a method of: a) treating, preventing, suppressing, inhibiting, or reducing obesity; b) promoting, increasing or facilitating weight loss; c) decreasing, suppressing, inhibiting or reducing appetite; d) altering the body composition, e) altering lean body mass or fat free body mass, f) converting fat to lean muscle; g) treating, preventing, suppressing, inhibiting, or reducing an obesity-associated metabolic disorder, for example hypertension, osteoarthritis, Type II diabetes mellitus, increased blood pressure, stroke, or heart disease; h) decreasing, suppressing, inhibiting or reducing adipogenesis; i) altering stem cell differentiation; and / or j) altering the level of leptin; comprising administering a therapeutically effective amount of a selective androgen receptor modulator and / or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, crystal, or any combination thereof, as described herein.

Description

technical field [0001] The present invention relates to the prevention and treatment of obesity. More specifically, the present invention relates to a) treating, preventing, suppressing, suppressing or reducing obesity; b) promoting, increasing or assisting in weight loss; c) reducing, suppressing, suppressing or reducing appetite; d) altering body composition; e) Altering lean or fat-free body mass; f) converting fat into lean muscle; g) treating, preventing, suppressing, inhibiting or alleviating obesity-related metabolic diseases such as hypertension, osteoarthritis, type II diabetes, increased blood pressure, Stroke or heart disease; h) reducing, suppressing, inhibiting or reducing adipogenesis; i) altering stem cell differentiation; and / or j) methods of altering leptin levels comprising administering a therapeutically effective amount of a selective androgen receptor modulator And / or its analogs, derivatives, isomers, metabolites, pharmaceutically acceptable salts, drugs...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/165A61K31/405A61K31/4706A61K31/675
CPCA61K31/165A61P1/16A61P19/02A61P3/04A61P3/06A61P43/00A61P5/26A61P5/28A61P9/04A61P9/10A61P9/12A61P3/10
Inventor 詹姆斯·T.·多尔顿杜安·D.·米勒米切尔·S.·斯坦纳卡伦·A.·韦韦尔卡
Owner GTX INCORPORATED
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