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1. 发明授权

US06620838B1 Benzopyrazone compounds, compositions thereof, and methods of treatment therewith 失效
标题翻译：苯并吡唑酮化合物，其组合物及其处理方法
公开(公告)号：US06620838B1
公开(公告)日：2003-09-16
申请号：US10125965
申请日：2002-04-19
申请人： Jeffrey A. McKie , Shripad S. Bhagwat , Johanne Renaud , Martin Missbach
发明人： Jeffrey A. McKie , Shripad S. Bhagwat , Johanne Renaud , Martin Missbach
IPC分类号： A61K314025
CPC分类号： C07D311/16
摘要： Benzopyranone compounds having the following structure: wherein R1, X, Y and n are as defined here, are disclosed. The compounds of formula (I), wherein R1 is H, can be prepared by demethylation of the corresponding phenolic methyl ether. The compounds are useful for treating a bone-resorbing disease, cancer, arthritis or an estrogen-related condition such as breast cancer, osteoporosis and endometriosis.
摘要翻译：公开了具有以下结构的苯并吡喃酮化合物：其中R1，X，Y和n如本文所定义。其中R 1为H的式（I）化合物可通过相应的酚甲醚的去甲基化制备。该化合物可用于治疗骨吸收性疾病，癌症，关节炎或雌激素相关病症如乳腺癌，骨质疏松症和子宫内膜异位症。

2. 发明授权

US07247646B2 Benzopyranone compounds, compositions thereof, and methods of treatment therewith 失效
标题翻译：苯并吡喃酮化合物，其组合物及其处理方法
公开(公告)号：US07247646B2
公开(公告)日：2007-07-24
申请号：US10942519
申请日：2004-09-15
申请人： Jeffrey A. McKie , Shripad S. Bhagwat , Johanne Renaud , Martin Missbach
发明人： Jeffrey A. McKie , Shripad S. Bhagwat , Johanne Renaud , Martin Missbach
IPC分类号： C07D405/12 , A61K31/4025 , A61K31/453
CPC分类号： C07D311/16 , C07D311/14
摘要： Benzopyranone Compounds having the following structure: wherein R1, R2, X, Y and n are as defined herein, are disclosed. The Benzopyranone Compounds are useful for treating or preventing a bone-resorbing disease, a neoplastic disease, arthritis, a disease exacerbated by the presence of estrogen or a disease improved by the presence of estrogen, comprising administering an effective amount of a Benzopyranone Compound to a patient in need of the treating or preventing; activating the function of estrogen receptor (“ER”) in a bone cell; inhibiting the function of ER in a cancer cell; inhibiting the expression of interleukin-6 (“IL-6”) in a cell; and inhibiting the growth of a neoplastic cell, comprising contacting the cell with an effective amount of a Benzopyranone Compound.
摘要翻译：苯并吡喃酮具有以下结构的化合物：其中R 1，R 2，X，Y和n如本文所定义。苯并吡喃酮化合物可用于治疗或预防骨吸收疾病，肿瘤性疾病，关节炎，由雌激素的存在或由雌激素的存在而改善的疾病而加重的疾病，包括将有效量的苯并吡喃酮化合物给予需要治疗或预防的患者; 激活骨细胞中雌激素受体（“ER”）的功能; 抑制ER在癌细胞中的功能; 抑制细胞中白细胞介素-6（“IL-6”）的表达; 并抑制肿瘤细胞的生长，包括使细胞与有效量的苯并吡喃酮化合物接触。

3. 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。

4. 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。

5. 发明授权

US06291456B1 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：US06291456B1
公开(公告)日：2001-09-18
申请号：US09492939
申请日：2000-01-27
申请人： Bernd M. Stein , David Wesley Anderson , Leah M. Gayo-Fung , May S. Sutherland , 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 , May S. Sutherland , 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。

6. 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。

7. 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。

8. 发明授权

US06331562B1 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：US06331562B1
公开(公告)日：2001-12-18
申请号：US09611156
申请日：2000-07-06
申请人： Shripad S. Bhagwat , Jeffrey A. McKie , Sak Khammungkhune
发明人： Shripad S. Bhagwat , Jeffrey A. McKie , Sak Khammungkhune
IPC分类号： A61K3137
CPC分类号： C07D405/12 , C07D311/16 , C07D311/18
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. In a specific embodiment, the compounds are selective modulators for Er-&bgr; over ER-&agr;. Methods are also disclosed for modulating ER-&bgr; in cells and/or tissues expressing the same, including cells and/or tissues 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。在具体的实施方案中，化合物是Er-β在ER-α上的选择性调节剂。还公开了用于调节表达其的细胞和/或组织中的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

US07129242B2 Anilinopyrimidine derivatives as JNK pathway inhibitors and compositions and methods related thereto 失效
标题翻译：苯丙嘧啶衍生物作为JNK途径抑制剂及其组合物和方法
公开(公告)号：US07129242B2
公开(公告)日：2006-10-31
申请号：US10004645
申请日：2001-12-04
申请人： Yoshitaka Satoh , Shripad S. Bhagwat
发明人： Yoshitaka Satoh , Shripad S. Bhagwat
IPC分类号： A61K31/50 , A61K31/497
CPC分类号： C07D239/42 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D487/08 , C07D491/10 , A61K2300/00
摘要： Compounds having activity as inhibitors of the JNK pathway are disclosed. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 through R6 are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to inhibition of the JNK pathway. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.
摘要翻译：公开了具有JNK途径抑制剂活性的化合物。本发明的化合物是具有以下结构的苯胺基嘧啶衍生物：其中R 1至R 6如本文所定义。这些化合物可用于治疗对抑制JNK通路有反应的广泛的条件。因此，还公开了治疗这些病症的方法，以及含有一种或多种上述化合物的化合物的药物组合物。

10. 发明授权

US06897231B2 Indazole derivatives as JNK inhibitors and compositions and methods related thereto 失效
标题翻译：作为JNK抑制剂的吲唑衍生物及其相关的组合物和方法
公开(公告)号：US06897231B2
公开(公告)日：2005-05-24
申请号：US09910950
申请日：2001-07-23
申请人： Shripad S. Bhagwat , Yoshitaka Satoh , Steven T. Sakata , Chris A. Buhr , Ronald Albers , John Sapienza , Veronique Plantevin , Qi Chao , Kiran Sahasrabudhe , Rachel Ferri
发明人： Shripad S. Bhagwat , Yoshitaka Satoh , Steven T. Sakata , Chris A. Buhr , Ronald Albers , John Sapienza , Veronique Plantevin , Qi Chao , Kiran Sahasrabudhe , Rachel Ferri
IPC分类号： A61K31/41 , A61K31/416 , A61K31/4178 , A61K31/4184 , A61K31/4196 , A61K31/42 , A61K31/4245 , A61K31/427 , A61K31/4409 , A61K31/4439 , A61K31/4453 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/12 , A61P17/02 , A61P17/08 , A61P19/02 , A61P19/06 , A61P19/08 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/28 , A61P27/08 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/02 , A61P37/06 , C07D231/56 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/12
CPC分类号： C07D403/12 , C07D231/56 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/12
摘要： Compounds having activity as selective inhibitors of JNK are disclosed. The compounds of this invention are indazole derivatives having the following structure: wherein R1, R2 and A are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to JNK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.
摘要翻译：公开了具有活性作为JNK的选择性抑制剂的化合物。本发明的化合物是具有以下结构的吲唑衍生物：其中R 1，R 2和A如本文所定义。这些化合物可用于治疗对JNK抑制作用有响应的广泛范围的病症。因此，还公开了治疗这些病症的方法，以及含有一种或多种上述化合物的化合物的药物组合物。

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