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AssigneeThe University of Tennessee Research Corporation
InventorsJames T. Dalton, Duane D. Miller, Donghua Yin, Yali He
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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 non-steroidal agonist compounds. The invention further provides compositions containing the selective androgen modulator compounds or the non-steroidal agonist compounds and methods of binding an androgen receptor, modulating spermatogenesis, treating and imaging prostate cancer, and providing hormonal therapy for androgen-dependent conditions.
A composition comprising a selective androgen receptor modulator (SARM) compound having in-vivo androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor, said compound represented by the structure of formula (I):
A pharmaceutical composition comprising:
A method of binding a selective androgen receptor modulator compound to an androgen receptor, comprising the step of contacting the androgen receptor with a selective androgen receptor modulator (SARM) compound having in-vivo androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor, in an amount effective to bind the selective androgen receptor modulator compound to the androgen receptor, wherein said compound is represented by the structure of formula (I):
A method of suppressing spermatogenesis in a subject, comprising the step of contacting an androgen receptor of the subject with a selective androgen receptor modulator (SARM) compound having in-vivo androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor, in an amount effective to suppress sperm production, wherein said compound is represented by the structure of formula (I):
A method of hormone therapy comprising the step of contacting an androgen receptor of a subject with a selective androgen receptor modulator (SARM) compound having in-vivo androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor, in an amount effective bind the selective androgen receptor modulator compound to the androgen receptor and effect a change in an androgen-dependent condition, wherein said compound is represented by the structure of formula (I):
A method of treating a subject having a related hormone condition, comprising the step of contacting an androgen receptor of the subject with a selective androgen receptor modulator (SARM) compound having in-vivo androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor, in an amount effective bind the selective androgen receptor modulator compound to the androgen receptor and effect a change in an androgen-dependent condition, wherein said compound is represented by the structure of formula (I):
Dependencies are inferred from the claim text.