Selective androgen receptor modulators and methods of use thereof

An androgen receptor, selective technology, applied in the direction of plant growth regulators, botany equipment and methods, applications, etc., can solve the problem of non-steroidal androgen reports and other issues

Inactive Publication Date: 2004-01-28
UNIV OF TENNESSEE RES FOUND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although non-steroidal antiandrogens are clinically used in hormone-dependent prostate cancer, no non-steroidal androgens have been reported

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

Embodiment 2

[0163] Non-steroidal ligands with androgenic and anabolic activity

[0164] The in vivo efficacy and acute toxicity of four new non-steroidal androgens (compounds IV, V, VI and VII) were examined in rats. In vitro experiments confirmed that these compounds bind the androgen receptor with high affinity. The structures and names of the four compounds are as follows:

[0165] GTx-014 R=F

[0166] GTx-015 R=COCH 3

[0167] GTx-016 R=COC 2 h 5

[0168] GTx-017 R=NHCOCH 3 experiment method

[0169] material.according to Figure 9 The shown route synthesizes compound GTx-014 (compound IV), GTx-015 (compound V), GTx-016 (compound VI) and GTx-007 (compound VII, wherein R is NHCOCH 3) and the R-isomer of GTx-014. Testosterone propionate (TP), polyethylene glycol 300 (PEG300, reagent grade) and neutral buffered formalin (10% w / v) were purchased from Sigma Chemical Company (St Louis, MO). Alzet osmotic pum...

Embodiment 4

[0186] HPLC analysis of GTx-007

[0187]A reverse-phase high-pressure liquid chromatography (HPLC) assay was developed to quantify GTx-007 concentrations in canine plasma. Canine blood samples were obtained by venipuncture and centrifuged at 1000g for 15 minutes. Samples were stored frozen at -20°C until analysis. Each sample was thawed quickly, and an aliquot (0.5 ml) was taken to elute the peak together with the internal standard (2 μl 200 μg / ml CM-II-87 aqueous solution). Aliquots of 1 ml of acetonitrile were added to the samples to precipitate plasma proteins. After vortexing the samples, centrifuge at 1000g for 15 minutes. Gently pour the supernatant into a glass extraction tube and add 7.5 ml of ethyl acetate. The extraction mixture was left at room temperature for 20 minutes, during which time it was vortexed several times. Then, the samples were centrifuged at 1000 g for 10 min, and the organic phase was removed and loaded into conical bottom glas...

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Abstract

This invention provides a novel class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds which are tissue-selective androgen receptor modulators (SARM), which are useful for oral testosterone replacement therapy, male contraception, maintaining sexual desire in women, treating prostate cancer and imaging prostate cancer. These agents have an unexpected in-vivo activity for an androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. These agents may be active alone or in combination with progestins or estrogens. The invention further provides a novel class of nonsteroidal agonist compounds and methods of binding an androgen receptor, modulating spermatogenesis, treating and imaging prostate cancer, and providing hormonal therapy for androgen-dependent conditions.

Description

technical field [0001] The present invention relates to a new class of tissue selective androgen receptor targeting agents (ARTAs) which exhibit androgenic and anabolic activity of non-steroidal ligands of the androgen receptor. Targeted Agents Definition Those are a new subclass of compounds that are Tissue Selective Androgen Receptor Modulators (SARMs) that are useful in androgen therapies such as oral testosterone replacement therapy, male contraception, maintenance of libido in women, treatment of prostate cancer and imaging of prostate cancer it works. These agents are also administered to subjects for the treatment of sarcopenia, loss of libido, osteoporosis, erythropoiesis, and fertility. Targeting agents can be used alone or in combination with progesterone or estrogen. Background technique [0002] The androgen receptor ("AR") is a ligand-activated transcriptional regulatory protein that mediates male sexual development and function through its endogenous androgen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P5/28A61K31/167A61K31/404A61K31/4706A61K31/661A61P7/06A61P13/08A61P15/00A61P15/08A61P15/16A61P19/10A61P35/00C07C235/24C07D209/08C07D215/22C07D215/227C07D271/12G01N33/543G01N33/74
CPCG01N33/74G01N33/5438C07D271/12C07C235/24A61K31/661A61K31/167C07D209/08C07D215/227A61K31/404A61K31/4706A61P13/08A61P15/00A61P15/08A61P15/16A61P17/14A61P19/10A61P35/00A61P43/00A61P5/26A61P5/28A61P7/06
Inventor 詹姆斯·多尔顿杜安·D·米勒尹东华何雅丽
Owner UNIV OF TENNESSEE RES FOUND
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