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1. 发明申请

US20070244161A1 Novel mercaptophenyl naphthyl methane compounds and synthesis thereof 有权
标题翻译：新型巯基苯基萘甲烷化合物及其合成
公开(公告)号：US20070244161A1
公开(公告)日：2007-10-18
申请号：US11812251
申请日：2007-06-15
申请人： Sangita , Atul Kumar , Man Singh , Girish Jain , Puvvada Sri Ramanchandra Murthy , Suprabhat Ray
发明人： Sangita , Atul Kumar , Man Singh , Girish Jain , Puvvada Sri Ramanchandra Murthy , Suprabhat Ray
IPC分类号： A61K31/12 , A61K31/38 , A61K31/40 , A61K31/44 , A61P19/08 , A61P25/28 , A61P35/00
CPC分类号： C07D295/088 , C07C317/22 , C07C317/24 , C07C323/19 , C07C323/22 , C07C323/25
摘要： Novel mercaptophenyl naphthyl methane compounds, their pharmaceutically acceptable salts and compositions comprised thereof are useful for the prevention or treatment of various medical indications associated with estrogen dependent diseases or syndromes related to osteoporosis, bone loss, bone formation, cardiovascular disorders, neurodegenerative disorders, menopausal disorders, physiological disorders, diabetes disorders, prostatic carcinoma, cancer of breast, cancer of uterus, cancer of the cervix and cancer of the colon, threatened or habitual abortion, obesity, ovarian development or function, post-partum lactation and depression.
摘要翻译：新的巯基苯基萘基甲烷化合物，其药学上可接受的盐和组合物可用于预防或治疗与与雌激素依赖性疾病或与骨质疏松症，骨丢失，骨形成，心血管疾病，神经变性疾病，绝经障碍相关的综合征相关的各种医学适应症，生理障碍，糖尿病，前列腺癌，乳腺癌，子宫癌，宫颈癌和结肠癌，威胁或习惯性流产，肥胖，卵巢发育或功能，产后泌乳和抑郁症。

2. 发明授权

US07582653B2 Mercaptophenyl naphthyl methane compounds and synthesis thereof 有权
标题翻译：甲基邻苯基萘甲烷化合物及其合成
公开(公告)号：US07582653B2
公开(公告)日：2009-09-01
申请号：US11812251
申请日：2007-06-15
申请人： Sangita , Atul Kumar , Man Mohan Singh , Girish Kumar Jain , Puvvada Sri Ramanchandra Murthy , Suprabhat Ray
发明人： Sangita , Atul Kumar , Man Mohan Singh , Girish Kumar Jain , Puvvada Sri Ramanchandra Murthy , Suprabhat Ray
IPC分类号： A61K31/4453 , A61K31/40 , A61K31/135 , A61K31/12 , C07D295/04 , C07C317/14 , C07C321/00
CPC分类号： C07D295/088 , C07C317/22 , C07C317/24 , C07C323/19 , C07C323/22 , C07C323/25
摘要： Novel mercaptophenyl naphthyl methane compounds, their pharmaceutically acceptable salts and compositions comprised thereof are useful for the prevention or treatment of various medical indications associated with estrogen dependent diseases or syndromes related to osteoporosis, bone loss, bone formation, cardiovascular disorders, neurodegenerative disorders, menopausal disorders, physiological disorders, diabetes disorders, prostatic carcinoma, cancer of breast, cancer of uterus, cancer of the cervix and cancer of the colon, threatened or habitual abortion, obesity, ovarian development or function, post-partum lactation and depression.
摘要翻译：新的巯基苯基萘基甲烷化合物，其药学上可接受的盐和组合物可用于预防或治疗与与雌激素依赖性疾病或与骨质疏松症，骨丢失，骨形成，心血管疾病，神经变性疾病，绝经障碍相关的综合征相关的各种医学适应症，生理障碍，糖尿病，前列腺癌，乳腺癌，子宫癌，宫颈癌和结肠癌，威胁或习惯性流产，肥胖，卵巢发育或功能，产后泌乳和抑郁症。

3. 发明授权

US07250446B2 Mercaptophenyl naphthyl methane compounds and synthesis thereof 有权
标题翻译：甲基邻苯基萘甲烷化合物及其合成
公开(公告)号：US07250446B2
公开(公告)日：2007-07-31
申请号：US10809845
申请日：2004-03-26
申请人： Sangita , Atul Kumar , Man Mohan Singh , Girish Kumar Jain , Puvvada Sri Ramanchandra Murthy , Suprabhat Ray
发明人： Sangita , Atul Kumar , Man Mohan Singh , Girish Kumar Jain , Puvvada Sri Ramanchandra Murthy , Suprabhat Ray
IPC分类号： A61K31/18 , C07C313/00 , C07C315/00
CPC分类号： C07D295/088 , C07C317/22 , C07C317/24 , C07C323/19 , C07C323/22 , C07C323/25
摘要： Novel mercaptophenyl naphthyl methane compounds, their pharmaceutically acceptable salts and compositions comprised thereof are useful for the prevention or treatment of various medical indications associated with estrogen dependent diseases or syndromes related to osteoporosis, bone loss, bone formation, cardiovascular disorders, neurodegenerative disorders, menopausal disorders, physiological disorders, diabetes disorders, prostatic carcinoma, cancer of breast, cancer of uterus, cancer of the cervix and cancer of the colon, threatened or habitual abortion, obesity, ovarian development or function, post-partum lactation and depression.
摘要翻译：新的巯基苯基萘基甲烷化合物，其药学上可接受的盐和组合物可用于预防或治疗与与雌激素依赖性疾病或与骨质疏松症，骨丢失，骨形成，心血管疾病，神经变性疾病，绝经障碍相关的综合征相关的各种医学适应症，生理障碍，糖尿病，前列腺癌，乳腺癌，子宫癌，宫颈癌和结肠癌，威胁或习惯性流产，肥胖，卵巢发育或功能，产后泌乳和抑郁症。

4. 发明申请

US20050070597A1 (3R, 4R)-trans-3, 4-diarylchroman derivatives and a method for the prevention and/or treatment of estrogen dependent diseases 失效
标题翻译：（3R，4R） - 反-3,4-二芳基苯并二氢吡喃衍生物和预防和/或治疗雌激素依赖性疾病的方法
公开(公告)号：US20050070597A1
公开(公告)日：2005-03-31
申请号：US10677116
申请日：2003-09-30
申请人： Sangita , Atul Kumar , Man Singh , Suprabhat Ray , Girish Jain
发明人： Sangita , Atul Kumar , Man Singh , Suprabhat Ray , Girish Jain
IPC分类号： C07D311/58 , A61K31/541 , A61K31/353 , A61K31/452 , A61K31/496 , A61K31/5377 , C07D45/02
CPC分类号： C07D311/58
摘要： The present invention relates to compounds of the formula I in which substituents R2 and R3 are arranged in trans-configuration: wherein: R1 is H or C1-C6 alkyl; C3-C7 cycloalkyl; R2 is phenyl, optionally substituted with 1 to 5 substituents independently selected from the group comprising OH, C1-C6-alkyl, halogen, nitro, cyano, SH, SR4, trihalo-C1-C6-alkyl, C1-C6-alkoxy and phenyl, wherein R4 is C1-C6 alkyl; R3 is phenyl substituted with OR5 wherein R5 has the formula (II), (III) or (IV) wherein Y is chosen from NHR4, NR42, NHCOR4, NHSO2R4, CONHR4, CONR4, CONR42, COOH, COOR4, SO2R4, SOR4, SONHR4, SONR42, a C3-C7 heterocyclic ring, saturated or unsaturated, containing one or two heteroatoms independently selected from the group consisting of O, S and N, optionally being substituted with 1 to 3 substituents independently selected from the group comprising H, OH, halogen, nitro, cyano, SH, SR4, trihalo-C1-C6-alkyl, C1-C6-alkyl and C1-C6-alkoxy, preferably NHR4, NR24, or a nitrogen heterocycle, wherein R4 is as defined above, and the esters, ethers, and salts of the compounds of formula I, optionally along pharmaceutically acceptable excipients, a process for the preparation of the same, and a method of preventing and/or treating estrogen-related disease conditions in a subject using compounds of formula 1, or its salts, optionally along with pharmaceutically acceptable excipients.
摘要翻译：本发明涉及式I化合物，其中取代基R 2和R 3以反式构型排列：其中：R 1是H或C 1 -C 6烷基; C3-C7环烷基; R 2是苯基，任选地被1至5个独立地选自OH，C 1 -C 6 - 烷基，卤素，硝基，氰基，SH，SR 4， - 3卤代-C 1 -C 6烷基，C 1 C 1-6 - 烷氧基和苯基，其中R 4是C 1 -C 6烷基; R 3是被OR 5取代的苯基，其中R 5具有式（II），（III）或（IV），其中Y选自NHR 4，NR 4，NHCOR 4 >，NHSO 2 R 4，CONHR 4，CONR 4，CONR 4，COOH，COOR 4，SO 2 R 4，SOR 4，SONHR 4，SONR 4 饱和或不饱和的C3-C7杂环，其含有一个或两个独立地选自O，S和N的杂原子，任选被1至3个独立地选自H，OH，卤素，硝基，氰基，SH，SR 4，三卤代-C 1 -C 6烷基，C 1 -C 6烷基和C 1 -C 6烷氧基，优选NH 4，NR 2 4或氮杂环， 4>如上所定义，并且式I化合物的酯，醚和盐，任选地沿着药学上可接受的赋形剂，其制备方法，以及预防和/或治疗雌激素相关疾病的方法使用式1化合物的受试者的条件，或其盐，任选地与药物 lly可接受的赋形剂。

5. 发明授权

US07427686B2 (3R, 4R)-trans-3, 4-diarylchroman derivatives and a method for the prevention and/or treatment of estrogen dependent diseases 失效
公开(公告)号：US07427686B2
公开(公告)日：2008-09-23
申请号：US10677116
申请日：2003-09-30
申请人： Sangita , Atul Kumar , Man Mohan Singh , Suprabhat Ray , Girish Kumar Jain
发明人： Sangita , Atul Kumar , Man Mohan Singh , Suprabhat Ray , Girish Kumar Jain
IPC分类号： C07D311/00
CPC分类号： C07D311/58
摘要： The present invention relates to compounds of the formula I in which substituents R2 and R3 are arranged in trans-configuration: wherein: R1 is H or C1-C6 alkyl; C3-C7 cycloalkyl; R2 is phenyl, optionally substituted with 1 to 5 substituents independently selected from the group comprising OH, C1-C6-alkyl, halogen, nitro, cyano, SH, SR4, trihalo-C1-C6-alkyl, C1-C6-alkoxy and phenyl, wherein R4 is C1-C6 alkyl; R3 is phenyl substituted with OR5 wherein R5 has the formula (II), (III) or (IV) wherein Y is chosen from NHR4, NR42, NHCOR4, NHSO2R4, CONHR4, CONR4, CONR42, COOH, COOR4, SO2R4, SOR4, SONHR4, SONR42, a C3-C7 heterocyclic ring, saturated or unsaturated, containing one or two heteroatoms independently selected from the group consisting of O, S and N, optionally being substituted with 1 to 3 substituents independently selected from the group comprising H, OH, halogen, nitro, cyano, SH, SR4, trihalo-C1-C6-alkyl, C1-C6-alkyl and C1-C6-alkoxy, preferably NHR4, NR24, or a nitrogen heterocycle, wherein R4 is as defined above, and the esters, ethers, and salts of the compounds of formula I, optionally along pharmaceutically acceptable excipients, a process for the preparation of the same, and a method of preventing and/or treating estrogen-related disease conditions in a subject using compounds of formula 1, or its salts, optionally along with pharmaceutically acceptable excipients.

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