Selective androgen receptor modulator and method for using thereof

An androgen receptor, selective technology, used in pharmaceutical formulations, organic active ingredients, medical preparations containing active ingredients, etc., can solve the problems of individual health hazards, poor behavioral status, and weakened physical conditions.

Active Publication Date: 2013-03-20
UNIV OF TENNESSEE RES FOUND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, changes that occur during muscle wasting can result in a weakened physical condition that is detrimental to the individual's health, leading to increased susceptibility to infection and poor performance status

Method used

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  • Selective androgen receptor modulator and method for using thereof
  • Selective androgen receptor modulator and method for using thereof
  • Selective androgen receptor modulator and method for using thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0232] Effect of selective androgen receptor modulator (SARM) compound III on the differentiation of progenitor cells into osteoblasts and The role of bone cells

[0233] Materials and methods

[0234] chemical

[0235] Compound III, THT and PTH were prepared at concentrations ranging from 1 nM to 1 μM.

[0236] animal

[0237] Four-month-old female rats were euthanized, and the femurs of the animals were excised. Any muscle and connective tissue on the femur was removed and stored on ice in minimal essential medium (MEM) containing penicillin, streptomycin, and amphotericin B until cell culture.

[0238] Bone Marrow Cell Culture

[0239]All cell culture materials were purchased from Invitrogen (Carlsbad, CA). Femurs were first washed in 70% ethanol and washed three times with 5 ml each of penicillin and streptomycin. Both ends of the femur were snapped off and the bone marrow cells were flushed with 15 ml of MEM containing penicillin, streptomycin and amphotericin...

Embodiment 2

[0249] Bone effects of SARMs alone and in combination with the antiresorptive agent alendronate

[0250] Materials and methods

[0251] Sixty female, nonpregnant, intact 23-week-old Sprague-Dawley rats were obtained from Charles River Laboratories (Wilmington, MA). 2–3 animals were housed per cage and adapted to a 12-h light / dark cycle. Food (7012C LM-485 mouse / rat sterile diet, Harlan Teklad, Madison, WI) and water were freely available. The animal protocol for this study was reviewed and approved by the Institutional Animal Care and Use Committee of Tennessee State University.

[0252] Sham surgery or ovariectomy was performed on day 0. The study consisted of the following six treatment groups: (1) intact + vehicle, (2) intact + compound III, (3) OVX + vehicle, (4) OVX + compound III, (5) OVX + alendronate, ( 6) OVX + alendronate + compound III. The DMSO:PEG300(10:90) vehicle group was given daily dosage (200L) by gavage from day 1. Animals were sacrificed on day 4...

Embodiment 3

[0261] Androgenic & anabolic activity in intact and ORX rats

[0262] Materials and methods

[0263] Male Spargue-Dawley rats weighing approximately 200 g were purchased from Harlan Bioproducts for Science (Indianapolis, IN). Animals were maintained on a 12 hour light / dark cycle and had free access to food (7012C LM-485 mouse / rat sterile diet, Harlan Teklad, Madison, WI) and water. Animal protocols were reviewed and approved by the Institutional Animal Care and Use Committee of Tennessee State University. Compound III was evaluated for its anabolic and androgenic activity in intact animals and additionally for dose response in acute orchiectomy (ORX) animals. The regenerative effects of compound III in chronic (9 day) ORX rats were also evaluated.

[0264]The compounds were weighed and dissolved in 10% DMSO (Fisher) diluted with PEG 300 (Acros Organics, NJ) for preparation of appropriate dosage concentrations. 2-3 animals were housed in each cage. Intact and ORX anima...

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Abstract

The invention relates to a selective androgen receptor modulator and a method for using thereof. Specifically, the invention provides a SARM compound and application of treating various diseases or illnesses in individuals. The diseases or illnesses especially comprise muscle marasmus diseases or illnesses or bone related diseases or illnesses.

Description

[0001] This application is a divisional application of the Chinese patent application 200580018468.2 with the title of "selective androgen receptor modulator and method of use thereof" submitted on June 7, 2005. Background technique [0002] The androgen receptor ("AR") is a ligand-activated transcriptional regulatory protein that mediates the induction of male sexual development and function through its endogenous androgenic activity. Androgens are often called male sex hormones. Androgens are steroids that are produced in the body by the testes and adrenal cortex, or can be synthesized in the laboratory. Androgenic steroids play an important role in many physiological processes, including the development and maintenance of male sexual characteristics such as muscle and bone mass, prostate growth, spermatogenesis, and male hair distribution (Matsumoto, Endocnnol. Met. Clin. N. Am. 23: 857-75(1994)). Endogenous steroid androgens include testosterone and dihydrotestosterone (...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C255/60A61K31/663A61K31/277A61P19/10A61P19/08A61P21/00A61P3/04A61P3/10A61P5/28
Inventor 詹姆斯·T.·多尔顿杜安·D.·米勒卡伦·A.·韦韦尔卡J·金
Owner UNIV OF TENNESSEE RES FOUND
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