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Selective androgen receptor modulators and methods of use thereof

An androgen receptor and selective technology, applied in diseases, drug combinations, metabolic diseases, etc., can solve problems such as vulnerability, weakened physical condition, and poor behavioral status

Inactive Publication Date: 2007-10-31
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 sarcoid wasting can result in a weakened physical condition that is detrimental to the individual's health, leading to increased susceptibility to infection, poor performance status, and vulnerability to injury

Method used

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  • Selective androgen receptor modulators and methods of use thereof
  • Selective androgen receptor modulators and methods of use thereof
  • Selective androgen receptor modulators and methods of use thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0289] The preparation of pharmaceutical compositions containing active ingredients is well known in the art, for example by mixing, granulating or tabletting techniques. The active therapeutic ingredient is often mixed with excipients which are pharmaceutically acceptable and compatible with the active ingredient. For oral administration, the SARM drug or its physiologically tolerable derivatives such as salts, esters, N-oxides, etc. are mixed with additives customary for oral administration such as excipients, stabilizers or inert diluents , and converted into dosage forms suitable for administration such as tablets, coated tablets, hard or soft gelatin capsules, water, alcohol or oil solutions by conventional methods. For parenteral administration, the SARM drug or its physiologically tolerable derivatives, such as salts, esters, N-oxides, etc., can be converted together with substances customary and suitable here, such as solubilizers, etc. as a solution, suspension or em...

Embodiment 1

[0297] Androgenic and anabolic activities of compounds 1-4

[0298] The binding affinities of selected SARM compounds whose B rings were Fylated, Clyd, Bryd, or Iylated were determined and are shown in Table 1:

[0299] Table 1

[0300]

[0301]

[0302] experimental method

[0303] Animals. Immature male Sprague-Dawley rats, weighing 90-100 g, were purchased from Harlan Biosciences (Indianapolis, IN). Animals were maintained on a 12-hour light-dark cycle with ad libitum access to food and water. The animal experiment protocol was reviewed and approved by the Institutional Laboratory Animal Care and Use Committee.

[0304] Study Design. Rats were randomly assigned to treatment groups. One day before starting drug treatment, animals were individually removed from cages, weighed, and anesthetized with ip ketamine / xylazine (87 / 13 mg / kg; approximately 1 mL / kg). When moderately anesthetized (ie, unresponsive to toe pinch), animals were earmarked for easy identification. ...

Embodiment 2

[0312] Androgenic and anabolic activity of compound 5

[0313] The binding affinities of selected compounds 5 are shown in Table 2.

[0314] Table 2

[0315]

[0316] After 14 days of administration, the androgenic and anabolic activity of Compound 5 in the castrated rat model were detected according to the method described in Example 1 above.

[0317] As shown in Table 3 and Figure 2, compound 5 exhibited tissue-selective pharmacological effects in castrated male rats, and in anabolic tissues (i.e. levator ani) compared to androgenic tissues (i.e. prostate and capsule) has higher efficacy. The compound showed little pharmacological activity in the prostate (8.7 ± 1.39% intact at a dose of 1.0 mg / day) and capsules (10.7 ± 0.91% intact at a dose of 1.0 mg / day), which It was shown to act as only a weak partial agonist in these tissues. Importantly, Compound 5 exhibited potent anabolic activity at a dose of 1.0 mg / day, restoring the levator ani muscle to 75.2 ± 9.51% of th...

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PUM

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Abstract

This invention provides a novel selective androgen receptor targeting agents compound and / or other analogue, isomer, metabolite, derivative, pharmaceutical acceptable salts, medicine, polycrystal product, crystal, impurity, N-oxide, hydrate or their optional combination for using in the preparation of the medicine for the treatment of conditions associated with Androgen Decline in Female (ADIF).

Description

[0001] This application is a divisional application of the Chinese invention patent application No. 200380106307.X filed on October 14, 2003 with the title of "aromatic ring selective androgen receptor modulator and method for its use". technical field [0002] The present invention relates to a new class of androgen receptor targeting agents (ARTAs), which are selective androgen receptor modulators (SARMs). These SARM compounds are useful in a) male contraception; b) in the treatment of various hormone-related conditions such as those associated with decreased androgen in aging males (ADAM) such as fatigue, depression, decreased libido, sexual dysfunction, erectile function disorders, hypogonadism, osteoporosis, alopecia, anemia, obesity, senile muscular atrophy, osteopenia, osteoporosis, benign prostatic hyperplasia, mood and cognitive changes, and prostate cancer; c) treatment and androgen reduction in women (ADIF) related conditions such as sexual dysfunction, decreased li...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/165A61K31/275C07C233/05C07C255/50A61P15/08A61P19/10A61P25/24A61P35/02A61K31/404A61K31/4706A61K31/661C07C235/16C07C235/24C07C255/60C07C335/18C07D209/08C07D215/22C07D215/227C07D271/12
CPCC07D271/12C07C255/60C07C235/24A61K31/165A61K31/661C07C235/16C07D209/08C07C335/18C07D215/227A61K31/404A61K31/4706A61P13/08A61P15/00A61P15/08A61P15/16A61P17/14A61P19/00A61P19/08A61P19/10A61P21/06A61P25/22A61P25/24A61P27/02A61P3/04A61P35/00A61P35/02A61P43/00A61P5/26A61P5/28A61P7/06C07C235/38C07C233/07
Inventor 詹姆斯·T.·多尔顿杜安·D.·米勒尹东华何亚利米切尔·S.·斯坦纳卡伦·A.·韦韦尔卡
Owner UNIV OF TENNESSEE RES FOUND
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