Yali He

US Patent:

6569896, May 27, 2003

Filed:

Aug 23, 2001

Appl. No.:

09/935045

Inventors:

James T. Dalton - Columbus OH
Duane D. Miller - Germantown TN
Donghua Yin - Columbus OH
Yali He - Florence SC

Assignee:

The University of Tennessee Research Corporation - Knoxville TN

International Classification:

A01N 3222

US Classification:

514493, 514616, 514619, 564153, 564156, 564158

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 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.

US Patent:

6838484, Jan 4, 2005

Filed:

Oct 15, 2002

Appl. No.:

10/270232

Inventors:

Mitchell S. Steiner - Germantown TN, US
Karen A. Veverka - Cordova TN, US
James T. Dalton - Columbus OH, US
Duane D. Miller - Germantown TN, US
Yali He - Florence SC, US
Donghua Yin - St. Louis MO, US

Assignee:

University of Tennessee Research Foundation - Knoxville TN

International Classification:

A61K 3116

US Classification:

514616, 514617, 514697, 514520, 514602, 514478, 514415, 514312

Abstract:

The present invention relates to pharmaceutical compositions and formulations comprising a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia,osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; and/or e) decreasing the incidence of, halting or causing a regression of prostate cancer. The present invention provides pharmaceutical compositions comprising the selective androgen receptor modulator compounds, together with pharmaceutically acceptable excipients.

US Patent:

6995284, Feb 7, 2006

Filed:

Oct 22, 2002

Appl. No.:

10/277108

Inventors:

James T. Dalton - Columbus OH, US
Duane D. Miller - Germantown TN, US
Yali He - Florence SC, US
Donghua Yin - St. Louis MO, US

Assignee:

The University of Tennessee Research Foundation - Knoxville TN

International Classification:

C07C 233/05
C07C 231/12

US Classification:

564155, 564138, 564142, 564162, 564163, 564164, 548571

Abstract:

The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.

US Patent:

6998500, Feb 14, 2006

Filed:

Oct 16, 2002

Appl. No.:

10/270732

Inventors:

James T. Dalton - Columbus OH, US
Duane D. Miller - Germantown TN, US
Yali He - Florence SC, US
Donghua Yin - St. Louis MO, US

Assignee:

University of Tennessee Research Foundation - Knoxville TN

International Classification:

C07C 255/50
A61K 31/275

US Classification:

558417, 564153, 564157, 564175, 514522, 514524, 514616, 514617

Abstract:

This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy; and/or g) decreasing the incidence of, halting or causing a regression of prostate cancer.

US Patent:

7205437, Apr 17, 2007

Filed:

May 10, 2005

Appl. No.:

11/125159

Inventors:

James T. Dalton - Upper Arlington OH, US
Duane D. Miller - Germantown TN, US
Yali He - Germantown TN, US
Donghua Yin - Pawcatuck CT, US

Assignee:

University of Tennessee Research Foundation - Knoxville TN

International Classification:

C07C 233/05
C07C 255/00

US Classification:

564158, 564155

Abstract:

The present invention relates to androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity, which are nonsteroidal ligands for the androgen receptor. The selective androgen receptor modulators (SARM) are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas.

US Patent:

7518013, Apr 14, 2009

Filed:

Feb 14, 2006

Appl. No.:

11/353225

Inventors:

James T. Dalton - Upper Arlington OH, US
Duane D. Miller - Germantown TN, US
Yali He - Germantown TN, US
Donghua Yin - Pawcatuck CT, US

Assignee:

University of Tennessee Research Foundation - Knoxville TN

International Classification:

C07C 255/49
A61K 31/275

US Classification:

558414, 514520, 514525

Abstract:

The present invention relates to androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity, which are nonsteroidal ligands for the androgen receptor. The selective androgen receptor modulators (SARM) are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas.

US Patent:

7759520, Jul 20, 2010

Filed:

Feb 23, 2005

Appl. No.:

11/062752

Inventors:

James T. Dalton - Upper Arlington OH, US
Duane D. Miller - Germantown TN, US
Donghua Yin - Pawcatuck CT, US
Yali He - Germantown TN, US

Assignee:

University of Tennessee Research Foundation - Knoxville TN

International Classification:

C07C 233/05

US Classification:

564165, 564153, 564157, 564158, 558417

Abstract:

The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.

US Patent:

7919647, Apr 5, 2011

Filed:

Feb 16, 2006

Appl. No.:

11/355187

Inventors:

James T. Dalton - Upper Arlington OH, US
Duane D. Miller - Germantown TN, US
Yali He - Germantown TN, US
Donghua Yin - Pawcatuck CT, US

Assignee:

University of Tennessee Research Foundation - Knoxville TN

International Classification:

C07C 255/49
A61K 31/275
A61K 31/13
A01N 37/34
A01N 33/02

US Classification:

558414, 514520, 514525, 514673

Abstract:

This invention provides a class of androgen receptor targeting agents. The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM).