专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2007062230A3 NUCLEAR RECEPTOR BINDING AGENTS 审中-公开
公开(公告)号：WO2007062230A3
公开(公告)日：2007-05-31
申请号：PCT/US2006/045451
申请日：2006-11-28
申请人： GTX, INC. , DALTON, James, T. , BARRETT, Christina , HE, Yali , HONG, Seoung-Soo , MILLER, Duane, D. , MOHLER, Michael, L. , NARAYANAN, Ramesh , WU, Zhongzhi
发明人： DALTON, James, T. , BARRETT, Christina , HE, Yali , HONG, Seoung-Soo , MILLER, Duane, D. , MOHLER, Michael, L. , NARAYANAN, Ramesh , WU, Zhongzhi
IPC分类号： C07C233/65 , A61K31/165
摘要： The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.

2. 发明申请

WO2008130571A1 NUCLEAR RECEPTOR BINDING AGENTS 审中-公开
标题翻译：核受体结合剂
公开(公告)号：WO2008130571A1
公开(公告)日：2008-10-30
申请号：PCT/US2008/004908
申请日：2008-04-16
申请人： GTX, INC. , DALTON, James, T. , BARRETT, Christina , MILLER, Duane, D. , HONG, Seoung-soo , HE, Yali , MOHLER, Michael, L. , NARAYANAN, Ramesh , WU, Zhongzhi
发明人： DALTON, James, T. , BARRETT, Christina , MILLER, Duane, D. , HONG, Seoung-soo , HE, Yali , MOHLER, Michael, L. , NARAYANAN, Ramesh , WU, Zhongzhi
IPC分类号： C07C327/00
CPC分类号： A61K31/138 , A61K31/40 , A61K31/445 , A61K31/55 , C07D221/12
摘要： The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.
摘要翻译：本发明涉及新型选择性雌激素受体调节剂（SERM）。 SERM化合物可用于预防和/或治疗各种疾病和病症，包括预防和治疗诸如前列腺和乳腺癌，骨质疏松症，激素相关疾病，潮热或血管舒缩症状，神经系统疾病，心血管疾病和肥胖。

3. 发明申请

WO2005113565A2 METABOLITES OF SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：选择性受体调节剂的代谢物及其使用方法
公开(公告)号：WO2005113565A2
公开(公告)日：2005-12-01
申请号：PCT/US2005/017588
申请日：2005-03-19
申请人： UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION , DALTON, James, T. , MILLER, Duane, D. , YIN, Donghua , HE, Yali
发明人： DALTON, James, T. , MILLER, Duane, D. , YIN, Donghua , HE, Yali
IPC分类号： C07F7/22
CPC分类号： A61K31/166 , A61K31/7036 , C07C235/24 , C07H15/18 , C07H15/203
摘要： This invention provides metabolites of a class of androgen receptor targeting agents (ARTA). The SARM compounds and their metabolites, 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; g) decreasing the incidence of, halting or causing a regression of prostate cancer; and/or h) inducing apoptosis in a cancer cell.
摘要翻译：本发明提供一类雄激素受体靶向剂（ARTA）的代谢物。 SARM化合物及其代谢物，单独或作为组合物，可用于a）男性避孕; b）治疗各种激素相关病症，例如与老年雄性雄激素降低有关的病症（ADAM），如疲劳，抑郁，性欲降低，性功能障碍，勃起功能障碍，性腺机能减退，骨质疏松症，脱发，贫血，肥胖，肌营养不良，骨质减少，骨质疏松症，良性前列腺增生，情绪和认知和前列腺癌的改变; （ADIF），性功能障碍，性欲降低，性腺机能减退，肌肉减少症，骨质减少症，骨质疏松症，认知改变，情绪，抑郁症，贫血，脱发，肥胖，子宫内膜异位症，乳腺癌，子宫癌和卵巢癌; d）治疗和/或预防急性和/或慢性肌肉消瘦病症; e）预防和/或治疗干眼症状; f）口服雄激素替代疗法; g）降低前列腺癌的发生率，停止或导致消退; 和/或h）诱导癌细胞中的细胞凋亡。

4. 发明申请

WO2004035736A2 HALOGENATED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：卤化选择性雄激素受体调节剂及其使用方法
公开(公告)号：WO2004035736A2
公开(公告)日：2004-04-29
申请号：PCT/US2003/032507
申请日：2003-10-14
申请人： UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION , DALTON, James, T. , MILLER, Duane, D. , YIN, Donghua , HE, Yali , STEINER, Mitchell, S. , VEVERKA, Karen, A.
发明人： DALTON, James, T. , MILLER, Duane, D. , YIN, Donghua , HE, Yali , STEINER, Mitchell, S. , VEVERKA, Karen, A.
IPC分类号： C12N
CPC分类号： C07D215/227 , A61K31/165 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/16 , C07C235/24 , C07C255/60 , C07C335/18 , C07D209/08 , C07D271/12
摘要： 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; g) decreasing the incidence of, halting or causing a regression of prostate cancer; and/or h) inducing apoptosis in a cancer cell.
摘要翻译：本发明提供了一类雄激素受体靶向剂（ARTA）。代理商定义了一类新的化合物，它们是选择性雄激素受体调节剂（SARM）。已经发现几种SARM化合物具有雄激素受体的非甾体配体的意想不到的雄激素和合成代谢活性。已经发现其他SARM化合物对雄激素受体的非甾体配体具有出乎意料的抗雄激素活性。 SARM化合物单独或作为组合物可用于a）男性避孕; b）治疗多种激素相关病症，例如与衰老男性（ADAM）中的雄激素降低相关的病症，例如疲劳，抑郁症，性欲减退，性功能障碍，勃起功能障碍，性腺机能减退，骨质疏松症，脱发，贫血，肥胖症，肌肉减少症，骨质减少症，骨质疏松症，良性前列腺增生症，情绪和认知改变以及前列腺癌; c）治疗与女性雄激素降低（ADIF）有关的病症，例如性功能障碍，性欲减退，性腺功能减退症，肌肉减少症，骨质减少症，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖症，子宫内膜异位症，乳房癌症，子宫癌和卵巢癌; d）治疗和/或预防急性和/或慢性肌肉萎缩症状; e）预防和/或治疗干眼症; f）口服雄激素替代疗法; g）降低前列腺癌的发病率，停止或导致其消退; 和/或h）诱导癌细胞凋亡。

5. 发明申请

WO2003074449A3 MULTI-SUBSTITUED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2003074449A3
公开(公告)日：2003-09-12
申请号：PCT/US2003/003123
申请日：2003-02-24
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION , DALTON, James, T. , MILLER, Duane, D. , HE, Yali , YIN, Donghua , STEINER, Mitchell, S. , VEVERKA, Karen, A.
发明人： DALTON, James, T. , MILLER, Duane, D. , HE, Yali , YIN, Donghua , STEINER, Mitchell, S. , VEVERKA, Karen, A.
IPC分类号： A61K31/655
摘要： This invention provides 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.

6. 发明申请

WO2003074449A2 MULTI-SUBSTITUED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：多取代的选择性雄激素受体调节剂及其使用方法
公开(公告)号：WO2003074449A2
公开(公告)日：2003-09-12
申请号：PCT/US2003/003123
申请日：2003-02-24
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION , DALTON, James, T. , MILLER, Duane, D. , HE, Yali , YIN, Donghua , STEINER, Mitchell, S. , VEVERKA, Karen, A.
发明人： DALTON, James, T. , MILLER, Duane, D. , HE, Yali , YIN, Donghua , STEINER, Mitchell, S. , VEVERKA, Karen, A.
IPC分类号： C07C
CPC分类号： C07C235/24
摘要： This invention provides 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.
摘要翻译：本发明提供了雄激素受体靶向剂（ARTA）。代理商定义了一类新的化合物，它们是选择性雄激素受体调节剂（SARM）。已经发现几种SARM化合物具有雄激素受体的非甾体配体的意想不到的雄激素和合成代谢活性。已经发现其他SARM化合物对雄激素受体的非甾体配体具有出乎意料的抗雄激素活性。 SARM化合物单独或作为组合物可用于a）男性避孕; b）治疗多种激素相关病症，例如与衰老男性（ADAM）中的雄激素降低相关的病症，例如疲劳，抑郁症，性欲减退，性功能障碍，勃起功能障碍，性腺机能减退，骨质疏松症，脱发，贫血，肥胖症，肌肉减少症，骨质减少症，骨质疏松症，良性前列腺增生症，情绪和认知改变以及前列腺癌; c）治疗与女性雄激素降低（ADIF）有关的病症，例如性功能障碍，性欲减退，性腺功能减退症，肌肉减少症，骨质减少症，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖症，子宫内膜异位症，乳房癌症，子宫癌和卵巢癌; d）治疗和/或预防急性和/或慢性肌肉萎缩症状; e）预防和/或治疗干眼症; f）口服雄激素替代疗法; 和/或g）降低前列腺癌的发病率，停止或导致其消退。

7. 发明申请

WO2003074450A3 RADIOLABELED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND THEIR USE IN PROSTATE CANCER IMAGING AND THERAPY 审中-公开
公开(公告)号：WO2003074450A3
公开(公告)日：2003-09-12
申请号：PCT/US2003/003124
申请日：2003-02-24
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION , DALTON, James , MILLER, Duane, D. , YIN, Donghua , HE, Yali
发明人： DALTON, James , MILLER, Duane, D. , YIN, Donghua , HE, Yali
IPC分类号： A61K31/40
摘要： Provided is a class of radiolabeled androgen receptor targeting agents (ARTA), useful for prostate cancer imaging and n treating or preventing prostate cancer. The agents define a new subclass of radiolabeled compounds, which are selective androgen receptor modulators (SARM), which demonstrate antiandrogenic activity of a nonsteroidal ligand for the androgen receptor, and/or which bind irreversibly to the androgen receptor. The present invention further provides methods for a) imaging of cancer in a subject, b) imaging an androgen receptor-containing tissue in a subject, c) in-vivo imaging in a subject, d) treating a subject suffering from prostate cancer, e) delaying the progression of prostate cancer in a subject suffering from prostate cancer, f) preventing the recurrence of prostate cancer in a subject suffering from prostate cancer, and g) treating the recurrence of prostate cancer in a subject suffering from prostate cancer, which comprise using the radiolabeled compounds of the present invention. The present invention further provides a method of producing the radiolabeled SARM compounds, and precursor compounds useful in the preparation of the radiolabeled SARM compounds.

8. 发明申请

WO2003074450A2 RADIOLABELED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND THEIR USE IN PROSTATE CANCER IMAGING AND THERAPY 审中-公开
标题翻译：放射性选择性原癌基因调节因子及其在前列腺癌成像和治疗中的应用
公开(公告)号：WO2003074450A2
公开(公告)日：2003-09-12
申请号：PCT/US2003/003124
申请日：2003-02-24
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION , DALTON, James , MILLER, Duane, D. , YIN, Donghua , HE, Yali
发明人： DALTON, James , MILLER, Duane, D. , YIN, Donghua , HE, Yali
IPC分类号： C07C
CPC分类号： A61K51/04 , A61K51/0402 , A61K51/0406 , A61K51/0446 , A61K51/0455 , A61K51/0459
摘要： Provided is a class of radiolabeled androgen receptor targeting agents (ARTA), useful for prostate cancer imaging and n treating or preventing prostate cancer. The agents define a new subclass of radiolabeled compounds, which are selective androgen receptor modulators (SARM), which demonstrate antiandrogenic activity of a nonsteroidal ligand for the androgen receptor, and/or which bind irreversibly to the androgen receptor. The present invention further provides methods for a) imaging of cancer in a subject, b) imaging an androgen receptor-containing tissue in a subject, c) in-vivo imaging in a subject, d) treating a subject suffering from prostate cancer, e) delaying the progression of prostate cancer in a subject suffering from prostate cancer, f) preventing the recurrence of prostate cancer in a subject suffering from prostate cancer, and g) treating the recurrence of prostate cancer in a subject suffering from prostate cancer, which comprise using the radiolabeled compounds of the present invention. The present invention further provides a method of producing the radiolabeled SARM compounds, and precursor compounds useful in the preparation of the radiolabeled SARM compounds.
摘要翻译：提供了一类用于前列腺癌成像和治疗或预防前列腺癌的放射性标记的雄激素受体靶向剂（ARTA）。这些试剂定义了一种放射性标记化合物的新亚类，它们是选择性雄激素受体调节剂（SARM），其表现出非甾类配体对雄激素受体的抗雄激素活性和/或不依赖于雄激素受体的结合。本发明进一步提供a）用于a）成像受试者中的癌症的方法，b）使受试者中含有雄激素受体的组织成像，c）受试者体内成像，d）治疗患有前列腺癌的受试者，e ）延迟患有前列腺癌的受试者的前列腺癌的进展，f）预防患有前列腺癌的受试者中前列腺癌的复发，以及g）治疗患有前列腺癌的受试者中前列腺癌的复发，其包括使用本发明的放射性标记的化合物。本发明还提供了一种制备放射性标记的SARM化合物的方法，以及可用于制备放射性标记的SARM化合物的前体化合物。

9. 发明申请

WO2003074473A3 IRREVERSIBLE SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2003074473A3
公开(公告)日：2003-09-12
申请号：PCT/US2003/003121
申请日：2003-02-24
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION , DALTON, James , MILLER, Duane, D. , CHUNG, Kiwon , HE, Yali , STEINER, Mitchell, S. , VEVERKA, Karen, A.
发明人： DALTON, James , MILLER, Duane, D. , CHUNG, Kiwon , HE, Yali , STEINER, Mitchell, S. , VEVERKA, Karen, A.
IPC分类号： C07C233/05
摘要： In one embodiment, 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). The SARM compounds have unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. In one embodiment, the SARM compounds bind irreversibly to the androgen receptor. In another embodiment, the SARM compounds are androgen receptor antagonists which bind irreversibly to the androgen receptor. In another embodiment, the SARM compounds are alkylating agents. 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; g) decreasing the incidence of, halting or causing a regression of prostate cancer; and/or h) inducing apoptosis in a cancer cell.

10. 发明申请

WO2019222556A1 SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2019222556A1
公开(公告)日：2019-11-21
申请号：PCT/US2019/032751
申请日：2019-05-16
申请人： GTX, INC. , UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
发明人： NARAYANAN, Ramesh , MILLER, Duane, D. , PONNUSAMY, Thamarai , HWANG, Dong-Jin , HE, Yali
IPC分类号： A61K31/277 , A61K31/167 , A61K31/404 , A61P35/00 , A61P35/04
摘要： This invention is directed to selective androgen receptor degrader (SARD) compounds including heterocyclic rings and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedys disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式