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。

公开(公告)号：US5811428A

公开(公告)日：1998-09-22

申请号：US581473

申请日：1995-12-18

申请人： Mark J. Suto ,  Mark E. Goldman ,  Leah M. Gayo ,  Lynn J. Ransone-Fong ,  Moorthy S. S. Palanki ,  Robert W. Sullivan

发明人： Mark J. Suto ,  Mark E. Goldman ,  Leah M. Gayo ,  Lynn J. Ransone-Fong ,  Moorthy S. S. Palanki ,  Robert W. Sullivan

IPC分类号： C07D239/28 ,  C07D239/30 ,  C07D239/34 ,  C07D239/42 ,  C07D241/24 ,  A61K31/505 ,  C07D239/36

CPC分类号： C07D239/28 ,  C07D239/30 ,  C07D239/34 ,  C07D239/42 ,  C07D241/24

摘要： Compounds having utility as antinflammatory agents in general and, more specifically, for the prevention and/or treatment of immunoinflammatory and autoimmune diseases are disclosed. The compounds are pyrimidine- or pyrazine-containing compounds and, in one embodiment, are carboxyamides of the same. Methods are also disclosed for preventing and/or treating inflammatory conditions by administering to an animal in need thereof an effective amount of a compound of this invention, preferably in the form of a pharmaceutical composition.

摘要翻译： 公开了一般具有用作抗炎剂的化合物，更具体地，用于预防和/或治疗免疫炎症和自身免疫疾病的化合物。 这些化合物是含嘧啶或吡嗪的化合物，在一个实施方案中是它们的羧酰胺。 还公开了通过向有需要的动物施用有效量的本发明化合物，优选以药物组合物的形式，来预防和/或治疗炎性病症的方法。

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。

公开(公告)号：US5935966A

公开(公告)日：1999-08-10

申请号：US807677

申请日：1997-02-27

申请人： Mark J. Suto ,  Leah M. Gayo ,  Moorthy S. S. Palanki ,  Lynn J. Ransone-Fong

发明人： Mark J. Suto ,  Leah M. Gayo ,  Moorthy S. S. Palanki ,  Lynn J. Ransone-Fong

IPC分类号： C07D239/28 ,  C07D239/30 ,  C07D239/34 ,  C07D239/42 ,  C07D241/24 ,  C07D401/04 ,  C07D403/12 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D239/02 ,  A01N43/54

CPC分类号： C07D239/42 ,  C07D239/28 ,  C07D239/30 ,  C07D239/34 ,  C07D241/24 ,  C07D401/04 ,  C07D403/12 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

摘要： Compounds having utility as anti-inflammatory agents in general and, more specifically, for the prevention and/or treatment of immunoinflammatory and autoimmune diseases are disclosed. The compounds are pyrimidine-containing compounds and, in one embodiment, are esters of the same. Methods are also disclosed for preventing and/or treating inflammatory conditions by administering to an animal in need thereof an effective amount of a compound of this invention, preferably in the form of a pharmaceutical composition.

摘要翻译： 一般具有用作抗炎剂的化合物，更具体地，用于预防和/或治疗免疫炎症和自身免疫疾病的化合物被公开。 化合物是含嘧啶的化合物，并且在一个实施方案中是它们的酯。 还公开了通过向有需要的动物施用有效量的本发明化合物，优选以药物组合物的形式，来预防和/或治疗炎性病症的方法。

公开(公告)号：US5932618A

公开(公告)日：1999-08-03

申请号：US740711

申请日：1996-11-04

申请人： Carla M. Suto ,  Jun Wu ,  Leah M. Gayo

发明人： Carla M. Suto ,  Jun Wu ,  Leah M. Gayo

IPC分类号： A61K31/167 ,  A61K31/19

CPC分类号： A61K31/167

摘要： Compounds having utility as anti-viral agents in general and, more specifically, to methods for treating a viral condition in an animal are disclosed. The compounds are naphthalene derivatives, and are preferably administered to the patient in the form of a pharmaceutical composition. Viruses treatable by the methods of this invention include viruses of the herpes virus family, such as cytomegalovirus, herpes simplex virus and human lymphotrophic herpes virus.

摘要翻译： 公开了一般用作抗病毒剂的化合物，更具体地，涉及用于治疗动物中的病毒病症的方法。 化合物是萘衍生物，优选以药物组合物的形式施用于患者。 可通过本发明的方法治疗的病毒包括疱疹病毒家族的病毒，例如巨细胞病毒，单纯疱疹病毒和人类淋巴细胞性疱疹病毒。

公开(公告)号：US5852028A

公开(公告)日：1998-12-22

申请号：US574406

申请日：1995-12-18

申请人： Mark J. Suto ,  Leah M. Gayo ,  Moorthy S. S. Palanki ,  Lynn J. Ransone-Fong

发明人： Mark J. Suto ,  Leah M. Gayo ,  Moorthy S. S. Palanki ,  Lynn J. Ransone-Fong

IPC分类号： C07D239/42 ,  C07D403/12 ,  C07D239/24 ,  A61K31/505

CPC分类号： C07D239/42 ,  C07D403/12

摘要： Compounds having utility as anti-inflammatory agents in general and, more specifically, for the prevention and/or treatment of immunoinflammatory and autoimmune diseases are disclosed. The compounds are pyrimidine-containing compounds and, in one embodiment, are esters of the same. Methods are also disclosed for preventing and/or treating inflammatory conditions by administering to an animal in need thereof an effective amount of a compound of this invention, preferably in the form of a pharmaceutical composition.

公开(公告)号：US06686351B2

公开(公告)日：2004-02-03

申请号：US10085999

申请日：2002-02-27

申请人： Shripad S. Bhagwat ,  Leah M. Gayo-Fung ,  Qi Chao

发明人： Shripad S. Bhagwat ,  Leah M. Gayo-Fung ,  Qi Chao

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中的细胞和/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。

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。