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公开(公告)号：US5972958A
公开(公告)日：1999-10-26
申请号：US25011
申请日：1998-02-17
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。
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2.发明授权4-aminoalkoxy-1,3-dihydrobenzoimidazol-2-one dopamine autoreceptor agonists 失效4-氨基烷氧基-1,3-二氢苯并咪唑-2-酮多巴胺自身受体激动剂
公开(公告)号：US5990144A
公开(公告)日：1999-11-23
申请号：US025083
申请日：1998-02-17
IPC分类号： C07D235/26 , C07D401/12 , C07D409/12 , A61K31/415 , C07D405/12
CPC分类号： C07D401/12 , C07D235/26 , C07D409/12
摘要： Disclosed are compounds of the formula ##STR1## wherein: R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.2 is selected from hydrogen, straight-chain and branched C.sub.1 -C.sub.10 alkyl, 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 alkoxy and trifluoromethyl;or NR.sup.1 R.sup.2 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;R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;Y is hydrogen, C.sub.1 -C.sub.6 alkyl, and C.sub.1 -C.sub.6 alkoxy;or a pharmaceutically acceptable salt thereof, which are dopamine autoreceptor agonists and as such are useful in the treatment of schizophrenia, Parkinson's disease, Tourette's syndrome, alcohol addiction and drug addiction.
摘要翻译： 公开了下式的化合物其中：R 1是氢或C 1 -C 6烷基; R 2选自氢，直链和支链C 1 -C 10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C 1 -C 6 烷基，卤素，C 1 -C 6烷氧基和三氟甲基; 或NR 1 R 2是1,2,3,4-四氢喹啉-1-基或1,2,3,4四氢异喹啉-2-基; m为1-5; n为1或2; R3是氢或C1-C6烷基; Y是氢，C 1 -C 6烷基和C 1 -C 6烷氧基; 或其药学上可接受的盐，其是多巴胺自身受体激动剂，因此可用于治疗精神分裂症，帕金森病，图雷特综合征，酒精成瘾和药物成瘾。
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公开(公告)号：US5922715A
公开(公告)日：1999-07-13
申请号：US025018
申请日：1998-02-17
IPC分类号： C07D241/44 , A61K31/495
CPC分类号： C07D241/44
摘要： This invention relates to compounds of Formula I ##STR1## wherein: R.sup.1 and R.sup.2 are independently selected from hydrogen, straight-chain and branched alkyl group having up to 10 carbon atoms or --(CH.sub.2).sub.m Ar where Ar is phenyl, naphthyl or thienyl, 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 and trifluoromethyl;or NR.sup.1 R.sup.2 is 1, 2, 3, 4-tetrahydroquinolin-1-yl or 1, 2, 3, 4-tetrahydroisoquinoline-2-yl;m is 1-5;n is 1 or 2;Y is hydrogen, C.sub.1 -C.sub.6 alkyl, and C.sub.1 -C.sub.6 alkoxy;or the pharmaceutically acceptable salts thereof, which are dopamine D.sub.2 agonists and therefore useful in the treatment of psychoses and Parkinson's disease.
摘要翻译： 本发明涉及式I化合物，其中：R 1和R 2独立地选自具有至多10个碳原子的氢，直链和支链烷基或 - （CH 2）mAr，其中Ar是苯基，萘基或噻吩基， 一个或两个独立地选自C 1 -C 6烷基，卤素，C 1 -C 6醇盐和三氟甲基的取代基; 或NR 1 R 2为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是氢，C 1 -C 6烷基和C 1 -C 6烷氧基; 或其药学上可接受的盐，其是多巴胺D2激动剂，因此可用于治疗精神病和帕金森病。
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4.发明授权4-aminoalkoxy-1,3-dihydrobenzoimidazol-2-one dopamine autoreceptor agonists 失效4-氨基烷氧基-1,3-二氢苯并咪唑-2-酮多巴胺自身受体激动剂
公开(公告)号：US6103744A
公开(公告)日：2000-08-15
申请号：US394448
申请日：1999-09-10
IPC分类号： C07D235/26 , C07D401/12 , C07D409/12 , A61K31/415 , A61K31/34 , A61K31/38 , A61K31/44
CPC分类号： C07D401/12 , C07D235/26 , C07D409/12
摘要： Disclosed are compounds of the formula ##STR1## wherein: R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.2 is selected from hydrogen, straight-chain and branched C.sub.1 -C.sub.10 alkyl, 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 and trifluoromethyl;or NR.sup.1 R.sup.2 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;R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;Y is halogen, C.sub.1 -C.sub.6 alkyl, and C.sub.1 -C.sub.6 alkoxy;or a pharmaceutically acceptable salt thereof, which are dopamine autoreceptor agonists and as such are useful in the treatment of schizophrenia, Parkinson's disease, Tourette's syndrome, alcohol addiction and drug addiction.
摘要翻译： 公开了下式的化合物其中：R 1是氢或C 1 -C 6烷基; R 2选自氢，直链和支链C 1 -C 10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C 1 -C 6 烷基，卤素，C 1 -C 6醇盐和三氟甲基; 或NR 1 R 2是1,2,3,4-四氢喹啉-1-基或1,2,3,4四氢异喹啉-2-基; m为1-5; n为1或2; R3是氢或C1-C6烷基; 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，其是多巴胺自身受体激动剂，因此可用于治疗精神分裂症，帕金森病，图雷特综合征，酒精成瘾和药物成瘾。
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公开(公告)号：US6127380A
公开(公告)日：2000-10-03
申请号：US24845
申请日：1998-02-17
IPC分类号： C07D235/06 , C07D235/08 , C07D235/10 , C07D401/12 , C07D409/12 , C07D235/02 , A61K31/415 , A61K31/47 , C07D401/02
CPC分类号： C07D235/06 , C07D235/08 , C07D235/10 , C07D401/12 , C07D409/12
摘要： This invention relates to D.sub.2 dopaminergic compounds of the formula ##STR1## wherein: R.sup.1 is hydrogen, trifluoromethyl, pentafluoroethyl, heptafluoropropyl, straight-chain or branched alkyl group having up to 6 carbons or benzyl optionally substituted by one to three substituents selected from halogen, amino, nitro, hydroxy, and C.sub.1 -C.sub.6 alkoxy;R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.3 is hydrogen, straight-chain or branched alkyl group having up to 10 carbon atoms, cyclohexylmethyl, --(CH.sub.2).sub.m Ar where Ar is phenyl, naphthalenyl, thienyl, furanyl, or pyridinyl, each optionally substituted by one to two substituents selected from halogen, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl and C.sub.1 -C.sub.6 alkyl, and m is 1-3or NR.sup.2 R.sup.3 is 1,2,3,4-tetrahydroquinolin-1-yl or 1,2,3,4-tetrahydroisoquinolin-2-yl;Y is hydrogen, halogen, lower alkyl, amino, or lower alkoxy;n is 1-5:or a pharmaceutically acceptable salt thereof. These D.sub.2 dopaminergic compounds are useful in the treatment of schizophrenia, Parkinson's disease, Tourette's syndrome, and drug or alcohol addiction.
摘要翻译： 本发明涉及下式的D2多巴胺能化合物，其中：R1是氢，三氟甲基，五氟乙基，七氟丙基，具有至多6个碳的直链或支链烷基或任选被一至三个选自卤素，氨基，硝基的取代基取代的苄基 ，羟基和C 1 -C 6烷氧基; R2是氢或C1-C6烷基; R 3是氢，具有至多10个碳原子的直链或支链烷基，环己基甲基， - （CH 2）mAr，其中Ar是苯基，萘基，噻吩基，呋喃基或吡啶基，各自任选被一至两个选自卤素 ，C 1 -C 6烷氧基，三氟甲基和C 1 -C 6烷基，m为1-3或NR 2 R 3为1,2,3,4-四氢喹啉-1-基或1,2,3,4-四氢异喹啉-2-基; Y是氢，卤素，低级烷基，氨基或低级烷氧基; n为1-5：或其药学上可接受的盐。 这些D2多巴胺能化合物可用于治疗精神分裂症，帕金森病，Tourette综合征和药物或酒精成瘾。
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6.发明授权公开(公告)号：US07157491B2
公开(公告)日：2007-01-02
申请号：US10845687
申请日：2004-05-13
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。
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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。
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公开(公告)号：US5872144A
公开(公告)日：1999-02-16
申请号：US024600
申请日：1998-02-17
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。
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公开(公告)号：US5760070A
公开(公告)日：1998-06-02
申请号：US909799
申请日：1997-08-12
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。
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10.发明申请BENZOFURANYL- AND BENZOTHIENYL- PIPERAZINYL QUINOLINES AND METHODS OF THEIR USE 审中-公开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。
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