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1. 发明授权

US07157491B2 Aryl-carbaldehyde oxime derivatives and their use as estrogenic agents 失效
标题翻译：芳基甲醛肟衍生物及其作为雌激素剂的用途
公开(公告)号：US07157491B2
公开(公告)日：2007-01-02
申请号：US10845687
申请日：2004-05-13
申请人： Richard Eric Mewshaw , Stephen Todd Cohn
发明人： Richard Eric Mewshaw , Stephen Todd Cohn
IPC分类号： A61K31/15 , A61K31/343 , A61K31/381 , C07C251/48 , C07C251/66 , C07D333/54 , C07D307/79
CPC分类号： C07D333/58 , C07C251/48 , C07D307/81
摘要： This invention provides estrogen receptor modulators having the structure where R1–R5 are as defined in the specification; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有如本说明书中定义的结构的雌激素受体调节剂，其中R 1〜或其药学上可接受的盐。

2. 发明授权

US5817690A 4-aminoethoxy indolone derivatives 失效
标题翻译： 4-氨基乙氧基吲哚酮衍生物
公开(公告)号：US5817690A
公开(公告)日：1998-10-06
申请号：US909800
申请日：1997-08-12
申请人： Richard Eric Mewshaw
发明人： Richard Eric Mewshaw
IPC分类号： C07D209/34 , C07D401/12 , C07D403/12 , A61K31/40 , C07D209/12
CPC分类号： C07D401/12 , C07D209/34 , C07D403/12
摘要： A compound of the formula I: ##STR1## in which Y is hydrogen, halogen or lower alkoxy; R.sub.1 is hydrogen, lower alkyl or aryl(lower)alkyl; R.sub.2 is hydrogen, lower alkyl or --(CH.sub.2).sub.n X.sub.p Ar, where X is oxygen or carbonyl; Ar is cycloalkyl, aryl or arylaryl, oxindolyl, benzimidazolyl, indolyl, 2-oxobenzimidazolyl or 2-thioxobenzimidazolyl; or R.sub.1 and R.sub.2, taken together with the nitrogen atom to which they are attached, complete a 3,4-dihydro-1H-isoquinolinyl or 1,3-dihydro-isoindolyl; n is one of the integers 1,2,3,4,5 or 6; p is one of the integers 0 or 1; or a pharmaceutically acceptable salt thereof are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analogous drugs.
摘要翻译：式I的化合物：其中Y是氢，卤素或低级烷氧基; R1是氢，低级烷基或芳基（低级）烷基; R2是氢，低级烷基或 - （CH2）nXpAr，其中X是氧或羰基; Ar是环烷基，芳基或芳基芳基，羟基吲哚基，苯并咪唑基，吲哚基，2-氧代苯并咪唑基或2-硫代苯并咪唑基; 或R 1和R 2与它们所连接的氮原子一起形成3,4-二氢-1H-异喹啉基或1,3-二氢 - 异吲哚基; n是整数1,2,3,4,5或6之一; p是整数0或1之一; 或其药学上可接受的盐是多巴胺合成和释放的抑制剂，可用于治疗精神分裂症，帕金森病，图雷特氏综合征，酒精成瘾，可卡因成瘾和类似药物的成瘾。

3. 发明申请

US20090054454A1 BENZOFURANYL- AND BENZOTHIENYL- PIPERAZINYL QUINOLINES AND METHODS OF THEIR USE 审中-公开
标题翻译：苯并呋喃和苯并噻吩 - 哌嗪喹啉及其使用方法
公开(公告)号：US20090054454A1
公开(公告)日：2009-02-26
申请号：US11842393
申请日：2007-08-21
申请人： Aranapakam Mudumbai Venkatesan , Osvaldo Dos Santos , Magda Asselin , George Theodore Grosu , Deborah A. Evrard , Richard Eric Mewshaw , Kristin Meagher
发明人： Aranapakam Mudumbai Venkatesan , Osvaldo Dos Santos , Magda Asselin , George Theodore Grosu , Deborah A. Evrard , Richard Eric Mewshaw , Kristin Meagher
IPC分类号： A61K31/496 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/34 , A61P35/00 , C07D295/00
CPC分类号： C07D409/12 , C07D407/12
摘要： Benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such compounds are disclosed. Methods of using benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such composition in the treatment and/or prevention of serotonin-related disorders, such as depression and anxiety, are also disclosed. In addition, processes for the preparation of benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives are disclosed.
摘要翻译：公开了苯并呋喃基 - 和苯并噻吩基 - 哌嗪基喹啉衍生物和含有这些化合物的组合物。还公开了使用苯并呋喃基 - 和苯并噻吩基 - 哌嗪基喹啉衍生物的方法和含有这种组合物的组合物在治疗和/或预防5-羟色胺相关疾病如抑郁和焦虑中的方法。此外，公开了制备苯并呋喃基和苯并噻吩基 - 哌嗪基喹啉衍生物的方法。

4. 发明授权

US07279600B2 Hydroxy-biphenyl-carbaldehyde oxime derivatives and their use as estrogenic agents 失效
标题翻译：羟基联苯甲醛肟衍生物及其作为雌激素剂的用途
公开(公告)号：US07279600B2
公开(公告)日：2007-10-09
申请号：US10835228
申请日：2004-04-29
申请人： Richard Eric Mewshaw , Cuijian Yang
发明人： Richard Eric Mewshaw , Cuijian Yang
IPC分类号： C07C251/24
CPC分类号： C07C251/48
摘要： This invention provides estrogen receptor modulators having the structure: wherein R1 to R6 and R8 are as defined in the specification; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了具有以下结构的雌激素受体调节剂：其中R 1至R 6和R 8均如说明书中所定义; 或其药学上可接受的盐。

5. 发明授权

US07276603B2 Benzofuranyl-and benzothienyl-piperazinyl quinolines and methods of their use 失效
标题翻译：苯并呋喃基 - 和苯并噻吩基 - 哌嗪基喹啉及其使用方法
公开(公告)号：US07276603B2
公开(公告)日：2007-10-02
申请号：US10835185
申请日：2004-04-29
申请人： Aranapakam Mudumbai Venkatesan , Osvaldo Dos Santos , Magda Asselin , George Theodore Grosu , Deborah A. Evrard , Richard Eric Mewshaw , Kristin Meagher
发明人： Aranapakam Mudumbai Venkatesan , Osvaldo Dos Santos , Magda Asselin , George Theodore Grosu , Deborah A. Evrard , Richard Eric Mewshaw , Kristin Meagher
IPC分类号： C07D405/12 , C07D409/12 , A61K31/496
CPC分类号： C07D405/12 , C07D409/12
摘要： Benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such compounds are disclosed. Methods of using benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such composition in the treatment and/or prevention of serotonin-related disorders, such as depression and anxiety, are also disclosed. In addition, processes for the preparation of benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives are disclosed. Benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives of Formula I are disclosed:
摘要翻译：公开了苯并呋喃基 - 和苯并噻吩基 - 哌嗪基喹啉衍生物和含有这些化合物的组合物。还公开了使用苯并呋喃基 - 和苯并噻吩基 - 哌嗪基喹啉衍生物的方法和含有这种组合物的组合物在治疗和/或预防5-羟色胺相关疾病如抑郁和焦虑中的方法。此外，公开了制备苯并呋喃基和苯并噻吩基 - 哌嗪基喹啉衍生物的方法。公开了式I的苯并呋喃基 - 和苯并噻吩基 - 哌嗪基喹啉衍生物：

6. 发明授权

US07250440B2 (Hydroxyphenyl)-1H-indole-3-carbaldehyde oxime derivatives as estrogenic agents 失效
标题翻译：（羟基苯基）-1H-吲哚-3-甲醛肟衍生物作为雌激素剂
公开(公告)号：US07250440B2
公开(公告)日：2007-07-31
申请号：US10914747
申请日：2004-08-09
申请人： Richard Eric Mewshaw , Stephen Marc Bowen , Eric Steven Manas
发明人： Richard Eric Mewshaw , Stephen Marc Bowen , Eric Steven Manas
IPC分类号： A61K31/404 , A61K31/405 , A61K31/255 , C07D209/80 , C07D209/58 , C07D209/14 , C07D209/34
CPC分类号： C07D209/14 , C07D209/88
摘要： This invention provides estrogen receptor modulators of formula I, having the structure where R1, R2, R3, and R4 are as defined in the specification, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供式I的雌激素受体调节剂，其具有R 1，R 2，R 3和R 4的结构本说明书中定义，或其药学上可接受的盐。

7. 发明授权

US5972958A 4-aminoalkoxy-1,3-dihydro-benzoimidazol-2-thiones 失效
标题翻译： 4-氨基烷氧基-1,3-二氢 - 苯并咪唑-2-硫酮
公开(公告)号：US5972958A
公开(公告)日：1999-10-26
申请号：US25011
申请日：1998-02-17
申请人： James Albert Nelson , Richard Eric Mewshaw , Uresh Shantilal Shah
发明人： James Albert Nelson , Richard Eric Mewshaw , Uresh Shantilal Shah
IPC分类号： C07D235/28 , C07D401/12 , C07D409/12 , A61K31/415 , A61K31/47
CPC分类号： C07D401/12 , C07D235/28 , C07D409/12
摘要： This invention relates to a novel series of compounds having potency at the dopamine D.sub.2 receptor which are illustrated by the following Formula I: ##STR1## wherein: R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.3 is selected from hydrogen, straight-chain and branched alkyl group having up to 10 carbon atoms, cyclohexylmethyl or --CH.sub.2).sub.m Ar where Ar is phenyl, naphthyl, thienyl, furanyl or pyridinyl, each optionally substituted by one or two substituents selected independently from C.sub.1 -C.sub.6 alkyl, halogen, C.sub.1 -C.sub.6 alkoxide, trifluoromethyl, 4-fluorobutyrophenone;or NR.sup.2 R.sup.3 is 1, 2, 3, 4-tetrahydroquinolin-1-yl or 1, 2, 3, 4-tetrahydroisoquinolin-2-yl;m is 1-5;n is 1 or 2;Y is halogen, C.sub.1 -C.sub.6 alkyl, and C.sub.1 -C.sub.6 alkoxy; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及一种在多巴胺D2受体上具有效力的新一系列化合物，其由下式I表示：其中：R1是氢或C1-C6烷基; R2是氢或C1-C6烷基; R 3选自具有至多10个碳原子的氢，直链和支链烷基，环己基甲基或-CH 2）mAr，其中Ar是苯基，萘基，噻吩基，呋喃基或吡啶基，各自任选被一个或两个独立地选自 C1-C6烷基，卤素，C1-C6醇盐，三氟甲基，4-氟代丁酰苯; 或NR 2 R 3是1,2,3,4-四氢喹啉-1-基或1,2,3,4,5-四氢异喹啉-2-基; m为1-5; n为1或2; Y是卤素，C 1 -C 6烷基和C 1 -C 6烷氧基; 或其药学上可接受的盐。

8. 发明授权

US5872144A 4-aminoethoxyindazole derivatives 失效
标题翻译： 4-氨基乙氧基吲唑衍生物
公开(公告)号：US5872144A
公开(公告)日：1999-02-16
申请号：US024600
申请日：1998-02-17
申请人： Richard Eric Mewshaw , Anthonie Johan Verwijs
发明人： Richard Eric Mewshaw , Anthonie Johan Verwijs
IPC分类号： C07D231/56 , C07D409/12 , A61K31/415
CPC分类号： C07D231/56 , C07D409/12
摘要： This invention relates to dopamine D.sub.2 agonists of the formula ##STR1## wherein: Y is hydrogen, halogen, or C.sub.1 -C.sub.6 alkoxy;R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;X is methylene, oxygen or carbonyl;Ar is phenyl or thienyl, each optionally substituted with 1-2 groups independently selected from C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkyl, halogen, trifluoromethyl and phenyl;n=1-4,or pharmaceutically acceptable salts thereof. Dopamine D.sub.2 agonists are useful in the treatment of schizophrenia, Tourette's syndrome, drug and alcohol addiction, and also useful in the treatment of Parkinson's disease.
摘要翻译：本发明涉及下式的多巴胺D2激动剂：其中：Y是氢，卤素或C 1 -C 6烷氧基; R1是氢或C1-C6烷基; X是亚甲基，氧或羰基; Ar是苯基或噻吩基，各自任选被1-2个独立地选自C 1 -C 6烷氧基，C 1 -C 6烷基，卤素，三氟甲基和苯基的基团取代; n = 1-4，或其药学上可接受的盐。多巴胺D2激动剂可用于治疗精神分裂症，Tourette综合征，药物和酒精成瘾，也可用于治疗帕金森病。

9. 发明授权

US5760070A 4-Aminoethoxy indolone derivatives 失效
标题翻译： 4-氨基乙氧基吲哚酮衍生物
公开(公告)号：US5760070A
公开(公告)日：1998-06-02
申请号：US909799
申请日：1997-08-12
申请人： Richard Eric Mewshaw , Michael Byron Webb
发明人： Richard Eric Mewshaw , Michael Byron Webb
IPC分类号： C07D409/12 , A61K31/40
CPC分类号： C07D409/12
摘要： A compound of the formula I: ##STR1## in which Y is hydrogen, halogen or alkoxy; R is hydrogen or alkylthio; R.sub.1 is hydrogen or alkyl; X is hydrogen, halogen, alkoxy, alkyl or phenyl; n is one of the integers 1, 2, 3 or 4; or a pharmaceutically acceptable salt thereof are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analogous drugs.
摘要翻译：式I的化合物：其中Y是氢，卤素或烷氧基; R是氢或烷硫基; R1是氢或烷基; X是氢，卤素，烷氧基，烷基或苯基; n是整数1,2,3或4之一; 或其药学上可接受的盐是多巴胺合成和释放的抑制剂，可用于治疗精神分裂症，帕金森病，图雷特综合征，酒精成瘾，可卡因成瘾和类似药物的成瘾。

10. 发明授权

US07671084B2 Dibenzo chromene derivatives and their use as ERβ selective ligands 失效
标题翻译：二苯并噻吩衍生物及其用作ER＆bgr; 选择性配体
公开(公告)号：US07671084B2
公开(公告)日：2010-03-02
申请号：US11591042
申请日：2006-10-31
申请人： Richard Eric Mewshaw , Richard James Edsall, Jr.
发明人： Richard Eric Mewshaw , Richard James Edsall, Jr.
IPC分类号： A61K31/352
CPC分类号： C07D311/78 , C07D311/92
摘要： This invention provides estrogen receptor modulators of formula I having the structure where R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the specification and the use of such compounds as estrogenic agents.
摘要翻译：本发明提供式I的雌激素受体调节剂，其具有如本说明书中所定义的R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8的结构，以及这些化合物如雌激素剂的用途。

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