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1. 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.

2. 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。

3. 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.

4. 发明申请

WO2003074471A1 HALOACETAMIDE AND AZIDE SUBSTITUTED COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：羟基乙酰胺和酰胺取代的化合物及其使用方法
公开(公告)号：WO2003074471A1
公开(公告)日：2003-09-12
申请号：PCT/US2003/003122
申请日：2003-02-24
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION , DALTON, James , MILLER, Duane, D.
发明人： DALTON, James , MILLER, Duane, D.
IPC分类号： C07C231/00
CPC分类号： A61K31/165 , A61K31/215 , A61K31/275 , A61K31/655 , C07C235/16 , C07C235/24 , C07C247/16 , C07F9/46 , C07F9/5004 , C07F9/5022 , C07F9/52
摘要： The present invention relates to a novel class of androgen receptor targeting agents (ARTA), which contain a haloacetamide or azide moiety and are alkylating agents. These agents which define a new subclass of compounds, namely selective androgen receptor modulators (SARMs) which, either alone or in 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：本发明涉及含有卤代乙酰胺或叠氮化物部分并且是烷化剂的新一类雄激素受体靶向剂（ARTA）。这些定义新化合物亚类的药剂，即选择性雄激素受体调节剂（SARM），其单独或组合物可用于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; c）治疗与男性雄激素降低相关的病症（ADIF），如性功能障碍，性欲降低，性腺机能减退，肌营养不良，骨质减少，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖，子宫内膜异位症，乳腺癌癌症，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。

5. 发明公开

EP1487780A1 HALOACETAMIDE AND AZIDE SUBSTITUTED COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：卤乙酰胺和AZIDSUBSTITUIERTE化合物和申请流程。
公开(公告)号：EP1487780A1
公开(公告)日：2004-12-22
申请号：EP03713345.1
申请日：2003-02-24
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION
发明人： DALTON, James , MILLER, Duane, D.
IPC分类号： C07C231/00 , C07C233/05 , C07C247/00 , C07C255/00 , A61K31/165 , A61K31/215 , A61K31/275 , A61K31/655
CPC分类号： A61K31/165 , A61K31/215 , A61K31/275 , A61K31/655 , C07C235/16 , C07C235/24 , C07C247/16 , C07F9/46 , C07F9/5004 , C07F9/5022 , C07F9/52
摘要： The present invention relates to a novel class of androgen receptor targeting agents (ARTA), which contain a haloacetamide or azide moiety and are alkylating agents. These agents which define a new subclass of compounds, namely selective androgen receptor modulators (SARMs) which, either alone or in 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.

6. 发明授权

EP1401801B1 SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 有权
标题翻译：作者雄GENREZEPTORS方法及其用途选择性调节剂。
公开(公告)号：EP1401801B1
公开(公告)日：2006-11-02
申请号：EP01964368.3
申请日：2001-08-23
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION
发明人： DALTON, James , MILLER, Duane, D. , YIN, Donghua , HE, Yali
IPC分类号： C07C233/15 , C07C233/33 , C07C233/48 , C07C235/26 , C07C237/14 , A01N37/18 , A01N31/16 , C07C235/24 , A61K31/167
CPC分类号： C07D215/227 , A61K31/167 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/24 , C07D209/08 , C07D271/12 , G01N33/5438 , G01N33/74
摘要： 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.

7. 发明公开

EP1401801A1 SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 有权
标题翻译：作者雄GENREZEPTORS方法及其用途选择性调节剂。
公开(公告)号：EP1401801A1
公开(公告)日：2004-03-31
申请号：EP01964368.3
申请日：2001-08-23
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION
发明人： DALTON, James , MILLER, Duane, D. , YIN, Donghua , HE, Yali
IPC分类号： C07C233/15 , C07C233/33 , C07C233/48 , C07C235/26 , C07C237/14 , A01N37/18 , A01N31/16
CPC分类号： C07D215/227 , A61K31/167 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/24 , C07D209/08 , C07D271/12 , G01N33/5438 , G01N33/74
摘要： 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.

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