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1. 发明授权

US06372739B1 Compounds and methods for modulation of estrogen receptors 失效
标题翻译：用于调节雌激素受体的化合物和方法
公开(公告)号：US06372739B1
公开(公告)日：2002-04-16
申请号：US09897048
申请日：2001-07-02
申请人： Bernd M. Stein , David Wesley Anderson , Leah M. Gayo-Fung , Mary Doubleday , Graziella I. Shevlin , Adam Kois , Sak Khammungkhune , Ravi Kumar Jalluri , Shripad S. Bhagwat , Jeffrey A. McKie
发明人： Bernd M. Stein , David Wesley Anderson , Leah M. Gayo-Fung , Mary Doubleday , Graziella I. Shevlin , Adam Kois , Sak Khammungkhune , Ravi Kumar Jalluri , Shripad S. Bhagwat , Jeffrey A. McKie
IPC分类号： A61K315377
CPC分类号： C07D311/16 , C07D311/18 , C07D405/12
摘要： Compounds that modulate gene expression through the estrogen receptor (ER) are disclosed having the following structure, as well as pharmaceutical compositions containing the same: wherein R1, R2, R3, n and p are as defined here. Methods are also disclosed for modulating ER in cells and/or tissues expressing the same, such as bone, breast, prostate, uterus, CNS or the cardiovascular system. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, and adverse reproductive effects associated with exposure to environmental chemicals or natural hormonal imbalances.
摘要翻译：公开了通过雌激素受体（ER）调节基因表达的化合物以及含有以下结构的药物组合物：其中R1，R2，R3，n和p如本文所定义。还公开了用于在表达其的细胞和/或组织中调节ER的方法，例如骨，乳腺，前列腺，子宫，CNS或心血管系统。还公开了治疗雌激素相关病症的方法，包括诸如乳腺癌，骨质疏松症，子宫内膜异位症，心血管疾病，高胆固醇血症，前列腺肥大，前列腺癌，肥胖症，潮热，皮肤效应，情绪波动，记忆丧失和不良与暴露于环境化学品或天然荷尔蒙失衡相关的生殖影响。

2. 发明授权

US07351729B2 JNK inhibitors for use in combination therapy for treating or managing proliferative disorders and cancers 失效
标题翻译：用于联合治疗用于治疗或控制增殖性疾病和癌症的JNK抑制剂
公开(公告)号：US07351729B2
公开(公告)日：2008-04-01
申请号：US10384440
申请日：2003-03-07
申请人： Bernd M. Stein , John K. Westwick , Bruce W. Ennis
发明人： Bernd M. Stein , John K. Westwick , Bruce W. Ennis
IPC分类号： A61K31/41 , A61K31/47 , A61K31/44 , A61K31/535
CPC分类号： A61K31/704 , A61K31/337 , A61K31/416 , A61K31/4196 , A61K31/454 , A61K31/4745 , A61K31/505 , A61K31/513 , A61K31/675 , A61K33/24 , A61K45/06 , A61K2300/00
摘要： The present invention relates to methods and compositions designed for the treatment, management or prevention of cancer. The methods of the invention comprise the administration of an effective amount of one or more inhibitors of JNK in combination with the administration of an effective amount of one or more other agents useful for cancer therapy. The invention also provides pharmaceutical compositions comprising one or more inhibitors of JNK in combination with one or more other agents useful for cancer therapy. In particular, the invention is directed to methods of treatment and prevention of cancer by the administration of an effective amount of one or more inhibitors of JNK in combination with standard and experimental chemotherapies, hormonal therapies, bone marrow transplants, stem cell replacement therapies, biological therapies/immunotherapies and/or radiation therapies for treatment or prevention of cancer. Also included are methods of treatment of cancer by the administration of one or more inhibitors of JNK in combination with surgery, alone or in further combination with standard and experimental chemotherapies, hormonal therapies, bone marrow transplants, stem cell replacement therapies, biological therapies/immunotherapies and/or radiation therapies.
摘要翻译：本发明涉及设计用于治疗，管理或预防癌症的方法和组合物。本发明的方法包括施用有效量的一种或多种JNK抑制剂与施用有效量的一种或多种其它可用于癌症治疗的试剂的组合。本发明还提供包含一种或多种JNK抑制剂与一种或多种其它可用于癌症治疗的试剂组合的药物组合物。特别地，本发明涉及通过给予有效量的一种或多种JNK抑制剂与标准和实验化学疗法，激素疗法，骨髓移植物，干细胞替代疗法，生物学方法，治疗和预防癌症的方法用于治疗或预防癌症的治疗/免疫治疗和/或放射疗法。还包括通过单独或与标准和实验化学疗法，激素治疗，骨髓移植，干细胞替代疗法，生物疗法/免疫疗法单独或进一步组合的一种或多种JNK抑制剂的给药来治疗癌症的方法和/或放射疗法。

3. 发明授权

US06436923B1 Compounds and methods for modulation of estrogen receptors 失效
标题翻译：用于调节雌激素受体的化合物和方法
公开(公告)号：US06436923B1
公开(公告)日：2002-08-20
申请号：US09527750
申请日：2000-03-17
申请人： Shripad S. Bhagwat , Leah M. Gayo-Fung , Bernd M. Stein , Qi Chao , Anthony R. Gangloff , Jeffrey A. McKie , Kenneth D. Rice
发明人： Shripad S. Bhagwat , Leah M. Gayo-Fung , Bernd M. Stein , Qi Chao , Anthony R. Gangloff , Jeffrey A. McKie , Kenneth D. Rice
IPC分类号： C07D21718
CPC分类号： C07D223/16 , C07D209/44 , C07D217/04 , C07D217/16 , C07D217/18 , C07D217/20 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04
摘要： Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-&bgr;. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.
摘要翻译：公开了调节雌激素受体（ER）的化合物以及含有它们的药物组合物。在一个具体的实施方案中，化合物是针对ER-α的ER-β的选择性调节剂。公开了用于在表达其的细胞和/或组织中调节ER-β的方法，包括优先表达ER-β的细胞和/或组织。更一般地，还公开了治疗雌激素相关病症的方法，包括诸如乳腺癌，睾丸癌，骨质疏松症，子宫内膜异位症，心血管疾病，高胆固醇血症，前列腺肥大，前列腺癌，肥胖症，潮热，皮肤效应，情绪波动，记忆丧失，尿失禁，脱发，白内障，天然荷尔蒙失衡，以及与暴露于环境化学品相关的不良生殖影响。

4. 发明授权

US07589119B2 Methods for treating or preventing metastatic cancer using benzopyranone compounds 失效
标题翻译：使用苯并吡喃酮化合物治疗或预防转移性癌症的方法
公开(公告)号：US07589119B2
公开(公告)日：2009-09-15
申请号：US12072011
申请日：2008-02-22
申请人： Glenn Friedman , Jeffrey McKie , Jonathan Wright , Sophie Perrin-Ninkovic , Bernd M. Stein
发明人： Glenn Friedman , Jeffrey McKie , Jonathan Wright , Sophie Perrin-Ninkovic , Bernd M. Stein
IPC分类号： A61K31/4025 , C07D405/12
CPC分类号： C07D311/16 , A61K31/40
摘要： This invention relates to Benzopyranone Compounds, compositions comprising a Benzopyranone Compound and methods for treating or preventing cancer or inhibiting the growth of a cancer cell or neoplastic cell comprising administering an effective amount of a Benzopyranone Compound. The Benzopyranone Compounds have the formula: or a pharmaceutically acceptable salt thereof, wherein R1 is halogen, trifluoromethyl or C1-6 alkyl.
摘要翻译：本发明涉及苯并吡喃酮化合物，包含苯并吡喃酮化合物的组合物和用于治疗或预防癌症或抑制癌细胞或肿瘤细胞生长的方法，包括给予有效量的苯并吡喃酮化合物。苯并吡喃酮化合物具有下式：或其药学上可接受的盐，其中R 1是卤素，三氟甲基或C 1-6烷基。

5. 发明申请

US20080146648A1 Methods for treating or preventing metastatic cancer using benzopyranone compounds 失效
标题翻译：使用苯并吡喃酮化合物治疗或预防转移性癌症的方法
公开(公告)号：US20080146648A1
公开(公告)日：2008-06-19
申请号：US12072011
申请日：2008-02-22
申请人： Glenn Friedman , Jeffrey McKie , Jonathan Wright , Sophie Perrin-Ninkovic , Bernd M. Stein
发明人： Glenn Friedman , Jeffrey McKie , Jonathan Wright , Sophie Perrin-Ninkovic , Bernd M. Stein
IPC分类号： A61K31/40 , A61P35/00
CPC分类号： C07D311/16 , A61K31/40
摘要： This invention relates to Benzopyranone Compounds, compositions comprising a Benzopyranone Compound and methods for treating or preventing cancer or inhibiting the growth of a cancer cell or neoplastic cell comprising administering an effective amount of a Benzopyranone Compound. The Benzopyranone Compounds have the formula: or a pharmaceutically acceptable salt thereof, wherein R1 is halogen, trifluoromethyl or C1-6 alkyl.
摘要翻译：本发明涉及苯并吡喃酮化合物，包含苯并吡喃酮化合物的组合物和用于治疗或预防癌症或抑制癌细胞或肿瘤细胞生长的方法，包括给予有效量的苯并吡喃酮化合物。苯并吡喃酮化合物具有下式：或其药学上可接受的盐，其中R 1是卤素，三氟甲基或C 1-6烷基。

6. 发明授权

US07091235B2 Benzopyranone compounds, compositions thereof, and methods for treating or preventing cancer 失效
标题翻译：苯并吡喃酮化合物，其组合物，以及治疗或预防癌症的方法
公开(公告)号：US07091235B2
公开(公告)日：2006-08-15
申请号：US10685722
申请日：2003-10-14
申请人： Glenn Friedman , Jeffrey McKie , Jonathan Wright , Sophie Perrin-Ninkovic , Bernd M. Stein
发明人： Glenn Friedman , Jeffrey McKie , Jonathan Wright , Sophie Perrin-Ninkovic , Bernd M. Stein
IPC分类号： A61K31/4025 , C07D405/10
CPC分类号： C07D311/16 , A61K31/40
摘要： This invention relates to Benzopyranone Compounds, compositions comprising a Benzopyranone Compound and methods for treating or preventing cancer or inhibiting the growth of a cancer cell or neoplastic cell comprising administering an effective amount of a Benzopyranone Compound. The Benzopyranone Compounds have the formula: or a pharmaceutically acceptable salt thereof, wherein R1 is halogen, trifluoromethyl or C1-6 alkyl.
摘要翻译：本发明涉及苯并吡喃酮化合物，包含苯并吡喃酮化合物的组合物和用于治疗或预防癌症或抑制癌细胞或肿瘤细胞生长的方法，包括给予有效量的苯并吡喃酮化合物。苯并吡喃酮化合物具有下式：或其药学上可接受的盐，其中R 1是卤素，三氟甲基或C 1-6烷基。

7. 发明授权

US06593322B1 Compounds and methods for modulation of estrogen receptors 失效
标题翻译：用于调节雌激素受体的化合物和方法
公开(公告)号：US06593322B1
公开(公告)日：2003-07-15
申请号：US09668893
申请日：2000-09-21
申请人： Shripad S. Bhagwat , Leah Marie Gayo-Fung , Bernd M. Stein , Qi Chao , Anthony R. Gangloff , Jeffrey A. McKie , Kenneth D. Rice
发明人： Shripad S. Bhagwat , Leah Marie Gayo-Fung , Bernd M. Stein , Qi Chao , Anthony R. Gangloff , Jeffrey A. McKie , Kenneth D. Rice
IPC分类号： C07D21718
CPC分类号： C07D223/16 , C07D209/44 , C07D217/04 , C07D217/16 , C07D217/18 , C07D217/20 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/04 , C07D405/12 , C07D413/10 , C07D417/12
摘要： Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially ER-&bgr;. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natureal hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.
摘要翻译：公开了调节雌激素受体（ER）的化合物以及含有它们的药物组合物。在一个具体实施方案中，化合物对ER-β对ER-α是选择性的。公开了用于在表达其中的细胞和/或组织中调节ER-β的方法，包括优先ER-β的细胞和/或组织。还公开了治疗雌激素相关病症的方法，包括诸如乳腺癌，睾丸癌，骨质疏松症，子宫内膜异位症，心血管疾病，高胆固醇血症，前列腺肥大，前列腺癌，肥胖症，潮热，皮肤效应，情绪波动，记忆丧失，尿失禁，脱发，白内障，自然激素失衡和与暴露于环境化学物质相关的不良生殖影响。

8. 发明授权

US07435729B2 Compounds and methods for modulation of estrogen receptors 失效
标题翻译：用于调节雌激素受体的化合物和方法
公开(公告)号：US07435729B2
公开(公告)日：2008-10-14
申请号：US10731666
申请日：2003-12-08
申请人： Leah Marie Gayo-Fung , Bernd M. Stein
发明人： Leah Marie Gayo-Fung , Bernd M. Stein
IPC分类号： A01N43/00 , A01N43/42 , A01N43/40 , A61K31/505
CPC分类号： C07D223/16 , C07D209/44 , C07D217/04 , C07D217/16 , C07D217/18 , C07D217/20 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04
摘要： Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-β over ER-α. Methods are disclosed for modulating ER-β in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-β. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.
摘要翻译：公开了调节雌激素受体（ER）的化合物以及含有它们的药物组合物。在一个具体的实施方案中，化合物是针对ER-α的ER-β的选择性调节剂。公开了用于在表达其的细胞和/或组织中调节ER-β的方法，包括优先表达ER-β的细胞和/或组织。更一般地，还公开了治疗雌激素相关病症的方法，包括诸如乳腺癌，睾丸癌，骨质疏松症，子宫内膜异位症，心血管疾病，高胆固醇血症，前列腺肥大，前列腺癌，肥胖症，潮热，皮肤效应，情绪波动，记忆丧失，尿失禁，脱发，白内障，天然荷尔蒙失衡，以及与暴露于环境化学品相关的不良生殖影响。

9. 发明授权

US07358274B2 Methods for treating or preventing cancer using Benzopyranone Compounds 失效
标题翻译：使用苯并吡喃酮化合物治疗或预防癌症的方法
公开(公告)号：US07358274B2
公开(公告)日：2008-04-15
申请号：US11431056
申请日：2006-05-09
申请人： Glenn Friedman , Jeffrey McKie , Jonathan Wright , Sophie Perrin-Ninkovic , Bernd M. Stein
发明人： Glenn Friedman , Jeffrey McKie , Jonathan Wright , Sophie Perrin-Ninkovic , Bernd M. Stein
IPC分类号： A61K31/4025 , C07D405/12
CPC分类号： C07D311/16 , A61K31/40
摘要： This invention relates to Benzopyranone Compounds, compositions comprising a Benzopyranone Compound and methods for treating or preventing cancer or inhibiting the growth of a cancer cell or neoplastic cell comprising administering an effective amount of a Benzopyranone Compound. The Benzopyranone Compounds have the formula: or a pharmaceutically acceptable salt thereof, wherein R1 is halogen, trifluoromethyl or C1-6 alkyl.
摘要翻译：本发明涉及苯并吡喃酮化合物，包含苯并吡喃酮化合物的组合物和用于治疗或预防癌症或抑制癌细胞或肿瘤细胞生长的方法，包括给予有效量的苯并吡喃酮化合物。苯并吡喃酮化合物具有下式：或其药学上可接受的盐，其中R 1是卤素，三氟甲基或C 1-6烷基。

10. 发明授权

US07279489B2 Compounds and methods for modulation of estrogen receptors 失效
标题翻译：用于调节雌激素受体的化合物和方法
公开(公告)号：US07279489B2
公开(公告)日：2007-10-09
申请号：US10434341
申请日：2003-05-07
申请人： Shripad S. Bhagwat , Leah Marie Gayo-Fung , Bernd M. Stein , Qi Chao , Anthony R. Gangloff , Jeffrey A. McKie , Kenneth D. Rice
发明人： Shripad S. Bhagwat , Leah Marie Gayo-Fung , Bernd M. Stein , Qi Chao , Anthony R. Gangloff , Jeffrey A. McKie , Kenneth D. Rice
IPC分类号： A61P35/00 , A61K31/47 , C07D217/00
CPC分类号： C07D223/16 , C07D209/44 , C07D217/04 , C07D217/16 , C07D217/18 , C07D217/20 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/04 , C07D405/12 , C07D413/10 , C07D417/12
摘要： Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective for ER-β over ER-α. Methods are disclosed for modulating ER-β in cell and/or tissues expressing the same, including cells and/or tissue that preferentially ER-β. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natureal hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.
摘要翻译：公开了调节雌激素受体（ER）的化合物以及含有它们的药物组合物。在一个具体实施方案中，化合物对ER-β对ER-α是选择性的。公开了用于在表达其中的细胞和/或组织中调节ER-β的方法，包括优先ER-β的细胞和/或组织。还公开了治疗雌激素相关病症的方法，包括诸如乳腺癌，睾丸癌，骨质疏松症，子宫内膜异位症，心血管疾病，高胆固醇血症，前列腺肥大，前列腺癌，肥胖症，潮热，皮肤效应，情绪波动，记忆丧失，尿失禁，脱发，白内障，自然激素失衡和与暴露于环境化学物质相关的不良生殖影响。

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