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1. 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。

2. 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.

3. 发明申请

WO2008091555A2 NUCLEAR RECEPTOR BINDING AGENTS 审中-公开
标题翻译：核受体结合剂
公开(公告)号：WO2008091555A2
公开(公告)日：2008-07-31
申请号：PCT/US2008/000736
申请日：2008-01-22
申请人： GTX, INC. , DALTON, James, T. , MILLER, Duane, D. , MOHLER, Michael, L. , WU, Zhongzhi , HONG, Seoung-Soo
发明人： DALTON, James, T. , MILLER, Duane, D. , MOHLER, Michael, L. , WU, Zhongzhi , HONG, Seoung-Soo
IPC分类号： A61K31/4709
CPC分类号： A61K31/472 , C07D217/22 , C07D217/24 , Y02A50/463
摘要： The present invention relates to a novel class of nuclear receptor binding agents (NRBAs). The NRBAs 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, inflammatory diseases, oxidative stress related disorders such as Parkinson's and stroke, neurological disorders, ophthalamic disorders, cardiovascular disease, and obesity.
摘要翻译：本发明涉及一类新型的核受体结合剂（NRBA）。 NRBA适用于预防和/或治疗多种疾病和病症，包括预防和治疗癌症，例如前列腺癌和乳腺癌，骨质疏松症，激素相关疾病，炎性疾病，氧化应激相关病症如帕金森病和中风，神经紊乱，眼科疾病，心血管疾病和肥胖。

4. 发明申请

WO2013142390A1 ALDO-KETO REDUCTASE SUBFAMILY 1C3 (AKR1C3) INHIBITORS 审中-公开
标题翻译： ALDO-KETO还原亚型1C3（AKR1C3）抑制剂
公开(公告)号：WO2013142390A1
公开(公告)日：2013-09-26
申请号：PCT/US2013/032674
申请日：2013-03-15
申请人： GTX, INC. , DALTON, James, T. , MILLER, Duane, D. , NARAYANAN, Ramesh , YEPURU, Muralimohan , COSS, Christopher, C. , MOHLER, Michael, L. , WU, Zhongzhi
发明人： DALTON, James, T. , MILLER, Duane, D. , NARAYANAN, Ramesh , YEPURU, Muralimohan , COSS, Christopher, C. , MOHLER, Michael, L. , WU, Zhongzhi
IPC分类号： C07D217/22 , C07D217/00
CPC分类号： C07C39/38 , C07D217/24
摘要： The present invention relates to a novel class of AKR1C3 inhibitors, to compositions containing them, to methods for their preparation, and to methods of use thereof. The AKR1C3 inhibitors may be useful in the treatment of, for example, prostate cancer, benign prostate hyperplasia (BPH), lung cancer, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, uterine cancer, uterine fibroids, endometriosis, myeloma and leiomyoma.
摘要翻译：本发明涉及新一类的AKR1C3抑制剂，含有它们的组合物，其制备方法及其使用方法。 AKR1C3抑制剂可用于治疗例如前列腺癌，良性前列腺增生（BPH），肺癌，痤疮，皮脂溢，多毛症，秃发，脱发，早熟性青春期，肾上腺肥大，多囊卵巢综合征，乳腺癌，子宫癌，子宫肌瘤，子宫内膜异位症，骨髓瘤和平滑肌瘤。

5. 发明申请

WO2005037206A2 ANTI-CANCER COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：抗癌化合物及其使用方法
公开(公告)号：WO2005037206A2
公开(公告)日：2005-04-28
申请号：PCT/US2004/033697
申请日：2004-10-14
申请人： GTX, INC. , STEINER, Mitchell, S. , MILLER, Duane, D. , VEVERKA, Karen, A. , BARRETT, Christina , HONG, Seoung-Soo
发明人： STEINER, Mitchell, S. , MILLER, Duane, D. , VEVERKA, Karen, A. , BARRETT, Christina , HONG, Seoung-Soo
IPC分类号： A61K
CPC分类号： C07D207/448 , C07C215/76 , C07C235/16 , C07C235/24 , C07C255/60 , C07C271/24 , C07C309/87 , C07C317/46 , C07C323/60 , C07D233/74
摘要： The present invention relates to a novel class of anti-cancer compounds which selectively target androgen receptor (AR)-expressing cancer, cells, such as prostate cancer cells and breast cancer cells, These agents comprise an androgen receptor (AR) binding moiety, which selectively tar-gets the compounds to (AR)-expressing cancer cells, and a cytotoxic alkylating moiety, such as a nitrogen mustard moiety, The inherent high density expression of the androgen receptor in certain cancers, such as prostate cancer and breast cancer, is thus used as a tool to selectively increase the intracellular concentration of cytotoxic compounds, such as alkylating agents, e,g. DNA alkylating agents, by selectively targeting the agents to the AR-expressing cancer cells. These agents, either alone or in a composition, are thus useful for treating, delaying the progression of, treating the recurrence of, suppressing, inhibiting or reducing the incidence of cancers characterized by the presence of AR-expressing cells, such as prostate cancer. Accordingly, the present invention provides a) methods of selectively killing an (AR)-expressing cancer, cell; b) methods of inducing apoptosis in an (AR) expressing cancer cell; c) methods of treating a cancer characterized by the presence of AR-expressing cells in a subject; d) methods of delaying the progression of a cancer characterized by the presence of AR-expressing cells in a subject; e) methods of treating the recurrence of a cancer characterized by the presence of AR-expressing cells in a subject; f) methods of suppressing, inhibiting or reducing the incidence of a cancer characterized by the presence of'AR-expressing cells in a subject; and g) methods of treating metastasis of a cancer characterized by the presence of AR.-expressing cells in a subject; by administering to the subject or by contacting the cancer cells with a compound comprising an androgen receptor, ligand moiety and an alkylating moiety, such as the novel compounds described herein.
摘要翻译：本发明涉及选择性靶向表达雄激素受体（AR）的癌症的新类别的抗癌化合物，诸如前列腺癌细胞和乳腺癌细胞的细胞。这些试剂包含雄激素（AR） - 表达癌细胞的受体（AR）结合部分，以及细胞毒性烷化部分（例如氮芥）。在某些癌症中固有的高密度雄激素受体表达，例如作为前列腺癌和乳腺癌，因此被用作选择性增加细胞毒性化合物如烷化剂（例如细胞毒性化合物）的细胞内浓度的工具。 DNA烷化剂，通过选择性靶向试剂至表达AR的癌细胞。因此，单独或组合物中的这些药剂因此可用于治疗，延缓疾病进展，治疗复发，抑制，抑制或减少以表达AR表达细胞如前列腺癌为特征的癌症的发病率。因此，本发明提供了a）选择性杀死表达（AR）的癌症细胞的方法; b）在（AR）＆shy中诱导细胞凋亡的方法; 表达癌细胞; c）治疗以受试者中存在AR-表达细胞为特征的癌症的方法; d）延迟以受试者中存在AR-表达细胞为特征的癌症进展的方法; e）治疗以受试者中存在AR-表达细胞为特征的癌症复发的方法; f）抑制，抑制或降低特征在于受试者中存在表达AR的细胞的癌症发病率的方法; 和g）治疗特征在于受试者中存在表达AR的细胞的癌症转移的方法; 通过向受试者施用或通过使癌细胞与包含雄激素受体，配体部分和烷基化部分的化合物例如本文所述的新化合物接触来进行。

6. 发明申请

WO2008011072A2 SELECTIVE ANDROGEN RECEPTOR MODULATORS, ANALOGS AND DERIVATIVES THEREOF AND USES THEREOF 审中-公开
标题翻译：选择性雄激素受体调节剂，类似物及其衍生物及其用途
公开(公告)号：WO2008011072A2
公开(公告)日：2008-01-24
申请号：PCT/US2007/016311
申请日：2007-07-19
申请人： OSURF (OHIO STATE UNIVERSITY RESEARCH FOUNDATION) , UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION , DALTON, James, T. , MILLER, Duane, D. , RAKOV, Igor , BOHL, Casey , MOHLER, Michael, L.
发明人： DALTON, James, T. , MILLER, Duane, D. , RAKOV, Igor , BOHL, Casey , MOHLER, Michael, L.
IPC分类号： A61K31/501
CPC分类号： C07D241/04 , C07C255/54 , C07C255/58 , C07C255/60 , C07C317/46 , C07C323/60 , C07C335/18 , C07D233/86
摘要： 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.
摘要翻译：本发明提供了新化合物及其用于治疗受试者中的多种疾病或病症，包括尤其是前列腺癌，肌肉萎缩疾病和/或病症或与骨有关的疾病和/或疾病。

7. 发明申请

WO2008011073A3 SELECTIVE ANDROGEN RECEPTOR MODULATORS, ANALOGS AND DERIVATIVES THEREOF AND USES THEREOF 审中-公开
公开(公告)号：WO2008011073A3
公开(公告)日：2008-01-24
申请号：PCT/US2007/016312
申请日：2007-07-19
申请人： OSURF , UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION , DALTON, James, T. , MILLER, Duane, D. , RAKOV, Igor , BOHL, Casey , MOHLER, Michael, L.
发明人： DALTON, James, T. , MILLER, Duane, D. , RAKOV, Igor , BOHL, Casey , MOHLER, Michael, L.
IPC分类号： A61K31/44 , A61K31/47 , C07D215/02 , C07D219/04
摘要： This invention provides nuclear hormone receptor binding compounds, compositions comprising the same and methods of uses thereof in treating a variety of diseases or conditions in a subject, including, inter-alia , prostate cancer and/or diseases or disorders of bone and muscle.

8. 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。

9. 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.

10. 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。

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