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Selective androgen receptor modulators, analogs and derivatives thereof and uses thereof

A compound, unsaturated technology, applied in organic chemistry and other directions, can solve problems such as non-ideal

Inactive Publication Date: 2009-08-26
THE OHIO STATE UNIV RES FOUND +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0028] While there are many treatments and treatments for these conditions, none are ideal

Method used

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  • Selective androgen receptor modulators, analogs and derivatives thereof and uses thereof
  • Selective androgen receptor modulators, analogs and derivatives thereof and uses thereof
  • Selective androgen receptor modulators, analogs and derivatives thereof and uses thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0914] The preparation of pharmaceutical compositions containing the active ingredients is well understood in the art, for example by mixing, granulating or tabletting. The active therapeutic ingredient is often mixed with excipients which are pharmaceutically acceptable and compatible with the active ingredient. For oral administration, the compounds according to the invention or their physiologically tolerated derivatives such as salts, esters, N-oxides etc. are mixed with additives customary for this purpose such as carriers, stabilizers or inert diluents and reacted in a conventional manner. Conversion into a form suitable for administration, such as tablets, coated tablets, hard or soft capsules, aqueous, alcoholic or oily solutions. For parenteral administration, the compounds of the present invention or their physiologically tolerated derivatives such as salts, esters, N-oxides, etc. are converted into solutions, suspensions or emulsions (if necessary, with conventional...

Embodiment 15

[1097] Example 15 shows that compounds of formula (I) are anabolic, but minimally androgenic, and that such compounds may therefore be useful in the treatment of patient populations for whom androgens were contraindicated in the past. Compounds of formula (I) have been shown to promote muscle growth irrespective of the presence or absence of testosterone while exerting an antiproliferative effect on the prostate, thus, in one embodiment, the methods of the invention are used to restore loss in individuals suffering from sarcopenia or cachexia of muscle mass.

[1098] In one embodiment, the compounds described herein alter leptin levels in a subject. In another embodiment, the compounds described herein lower the levels of leptin. In another embodiment, the compounds described herein increase leptin levels in a subject. Leptin is known to have an effect on appetite, weight loss in obese mice and thus has been associated with obesity.

[1099] In one embodiment, the compounds...

Embodiment 1

[1176] I

[1177] Synthesis of Compound XIII

[1178] 2-Substituted acrylic acid (compound 46) was reacted with 4-cyano-3-trifluoromethylaniline followed by epoxidation. Opening of the epoxide with p-CN-phenol in the presence of potassium carbonate yields compound XIII as Figure 1B shown in .

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Abstract

This invention provides new compounds and uses thereof in treating a variety of diseases or conditions in a subject, including,inter alia, prostate cancer, muscle wasting diseases and / or disorders or a bone-related diseases and / or disorders.

Description

[0001] Cross reference to related applications [0002] This application claims the benefit of US Provisional Patent Application 60 / 831880, filed July 19, 2006, and US Provisional Patent Application 60 / 831988, filed July 19, 2006; both of which are hereby incorporated by reference in their entirety. field of invention [0003] The present invention provides nuclear hormone receptor binding compounds, compositions comprising them and methods of their use in the treatment of various diseases or conditions in an individual including, inter alia, prostate cancer, muscular dystrophy and diseases related thereto or disorders, and / or bone-related diseases or disorders. Background of the invention [0004] The nuclear hormone receptor superfamily is the largest class of transcription factors involved in a wide range of physiological processes. The 48 members of this family fall into three classes, class 1 includes androgens (AR), estrogens (ER-α and ER-β), glucocorticoids (GR), pro...

Claims

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Application Information

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IPC IPC(8): C07C255/00C07D207/00
CPCC07C255/58C07D233/86C07C255/00C07D401/06C07D263/44C07D241/04C07C323/60C07D213/57C07C317/46C07D307/20C07C255/60C07C255/54C07C335/18C07D207/416
Inventor J·T·多尔顿D·D·米勒I·拉科夫C·博尔M·L·莫勒
Owner THE OHIO STATE UNIV RES FOUND
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