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1. 发明授权

US5990144A 4-aminoalkoxy-1,3-dihydrobenzoimidazol-2-one dopamine autoreceptor agonists 失效
标题翻译： 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
申请人： Richard Eric Mewshaw , James Albert Nelson , Uresh Shantilal Shah
发明人： Richard Eric Mewshaw , James Albert Nelson , Uresh Shantilal Shah
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。

2. 发明授权

US5922715A 5-aminoalkoxy-1, 4-dihydroquinoxaline-2, 3-diones 失效
标题翻译： 5-氨基烷氧基-1,4-二氢喹喔啉-2,3-二酮
公开(公告)号：US5922715A
公开(公告)日：1999-07-13
申请号：US025018
申请日：1998-02-17
申请人： James Albert Nelson , Uresh Shantilal Shah , Richard Eric Mewshaw
发明人： James Albert Nelson , Uresh Shantilal Shah , Richard Eric Mewshaw
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。

3. 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。

4. 发明授权

US6103744A 4-aminoalkoxy-1,3-dihydrobenzoimidazol-2-one dopamine autoreceptor agonists 失效
标题翻译： 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
申请人： Richard Eric Mewshaw , James Albert Nelson , Uresh Shantilal Shah
发明人： Richard Eric Mewshaw , James Albert Nelson , Uresh Shantilal Shah
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。

5. 发明授权

US6127380A 4-aminoalkoxy-1H-benzoimidazoles 失效
标题翻译： 4-氨基烷氧基-1H-苯并咪唑
公开(公告)号：US6127380A
公开(公告)日：2000-10-03
申请号：US24845
申请日：1998-02-17
申请人： James Albert Nelson , Richard Eric Mewshaw
发明人： James Albert Nelson , Richard Eric Mewshaw
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。

6. 发明授权

US06777407B2 Cyclopenta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives 失效
标题翻译：环戊基[b] [1,4]二氮杂[6,7,1-hi]吲哚及其衍生物
公开(公告)号：US06777407B2
公开(公告)日：2004-08-17
申请号：US10016331
申请日：2001-11-02
申请人： Annmarie Louise Sabb , Robert Lewis Vogel , James Albert Nelson , Sharon Joy Rosenzweig-Lipson , Gregory Scott Welmaker , Joan Eileen Sabalski
发明人： Annmarie Louise Sabb , Robert Lewis Vogel , James Albert Nelson , Sharon Joy Rosenzweig-Lipson , Gregory Scott Welmaker , Joan Eileen Sabalski
IPC分类号： A61K3155
CPC分类号： C07D209/94 , A61K31/55 , C07D487/06
摘要： This invention provides compounds of the formulae: wherein: R1 is hydrogen, —C(O)CH3 or alkyl of 1-6 carbon atoms; R2 and R3 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl, alkoxy of 1-6 carbon atoms, —CH2OH, fluoroalkyl, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, aryl, or aroyl; R4 and R5 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, fluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R6 and R7 are each independently hydrogen, C1-C6 alkyl or cycloalkyl; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions containing these compounds and methods for their use, including treatment of obsessive-compulsive disorder, panic disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.
摘要翻译：本发明提供下式的化合物：其中：R 1是氢，-C（O）CH 3或1-6个碳原子的烷基; R 2和R 3各自独立地是氢，1-6个碳原子的烷基，环烷基，烷氧基 1-6个碳原子的-CH 2 OH，氟代烷基，1-6个碳原子的烷基磺酰胺，1-6个碳原子的烷基酰胺，1-6个碳原子的烷基氨基，每个烷基部分1-6个碳原子的二烷基氨基，1-6个碳原子的氟烷氧基，2-7个碳原子的酰基，芳基或芳酰基; R4和R5各自独立地是氢，1-6个碳原子的烷基，1-6个碳原子的烷氧基，卤素，氟烷基，-CN，1-6个碳原子的烷基磺酰胺，1-6个碳原子的烷基酰胺，1-6个碳原子的烷基氨基，每个烷基部分1-6个碳原子的二烷基氨基，1-6个碳的氟烷氧基原子，2-7个碳原子的酰基或芳酰基; R6和R7各自独立地为氢，C1-C6烷基或环烷基;或其药学上可接受的盐，以及药物组合物conta 包括治疗强迫症，惊恐障碍，抑郁症，焦虑症，广泛性焦虑症，精神分裂症，偏头痛，睡眠障碍，进食障碍，肥胖，癫痫和脊髓损伤的这些化合物和方法。

7. 发明授权

US07098338B2 2,3,4,4a-tetrahydro-1H-pyrazino(1,2-a) quinoxalin-5(6H)one derivatives 失效
标题翻译： 2,3,4,4-四氢-1H-吡嗪并（1,2-a）喹喔啉-5（6H）酮衍生物
公开(公告)号：US07098338B2
公开(公告)日：2006-08-29
申请号：US10724844
申请日：2003-12-01
申请人： Annmarie Louise Sabb , Gregory Scott Welmaker , James Albert Nelson
发明人： Annmarie Louise Sabb , Gregory Scott Welmaker , James Albert Nelson
IPC分类号： C07D487/00 , A61K31/495
CPC分类号： C07D487/04 , A61K31/4985
摘要： This invention provides compounds of formula I, wherein R is hydrogen or alkyl of 1–6 carbon atoms; R′ is hydrogen, alkyl of 1–6 carbon atoms, acyl of 2–7 carbon atoms, or aroyl; R1, R2, R3, and R4 are each, independently, hydrogen, alkyl of 1–6 carbon atoms, alkoxy of 1–6 carbon atoms, halogen, trifluoroalkyl, or trifluoroalkoxy of 1–6 carbon atoms; X is CR5R6 or a carbonyl group; R5 and R6 are each, independently, hydrogen or alkyl of 1–6 carbon atoms; or a pharmaceutically acceptable salt thereof, with the proviso that at least two of R1, R2, R3, or R4 are not hydrogen; which are 5HT2C receptor agonists useful for the treatment of disorders involving the central nervous system such as obsessive-compulsive disorder, depression, anxiety, schizophrenia, migraine, sleep disorders, eating disorders, obesity, type II diabetes, and epilepsy.
摘要翻译：本发明提供式I化合物，其中R是氢或1-6个碳原子的烷基; R'是氢，1-6个碳原子的烷基，2-7个碳原子的酰基或芳酰基; R 1，R 2，R 3和R 4各自独立地为氢，烷基为1 -6个碳原子，1-6个碳原子的烷氧基，1-6个碳原子的卤素，三氟烷基或三氟烷氧基; X是CR 5 R 6或羰基; R 5和R 6各自独立地为氢或1-6个碳原子的烷基; 或其药学上可接受的盐，条件是R 1，R 2，R 3或R 3中的至少两个， 4不是氢; 其是可用于治疗涉及中枢神经系统的障碍（例如强迫症，抑郁症，焦虑症，精神分裂症，偏头痛，睡眠障碍，进食障碍，肥胖症，II型糖尿病）的5HT 2C受体激动剂，和癫痫。

8. 发明授权

US06706714B2 2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5(6H)one derivatives 失效
标题翻译： 2,3,4,4a-四氢-1H-吡嗪并[1,2-a]喹喔啉-5（6H）一种衍生物
公开(公告)号：US06706714B2
公开(公告)日：2004-03-16
申请号：US10244773
申请日：2002-09-16
申请人： Annmarie Louise Sabb , Gregory Scott Welmaker , James Albert Nelson
发明人： Annmarie Louise Sabb , Gregory Scott Welmaker , James Albert Nelson
IPC分类号： A61K31495
CPC分类号： C07D487/04 , A61K31/4985
摘要： This invention provides compounds of formula I, R is hydrogen or alkyl of 1-6 carbon atoms; R′ is hydrogen, alkyl of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R1, R2, R3, and R4 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, trifluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, trifluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; X is CR5R6 or a carbonyl group; R5 and R6 are each, independently, hydrogen or alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof, with the proviso that at least one of R1, R2, R3, or R4 are not hydrogen; which are 5HT2C receptor agonists useful for the treatment of disorders involving the central nervous system such as obsessive-compulsive disorder, depression, anxiety, schizophrenia, migraine, sleep disorders, eating disorders, obesity, type II diabetes, and epilepsy.
摘要翻译：本发明提供式I化合物，R是氢或1-6个碳原子的烷基; R'是氢，1-6个碳原子的烷基，2-7个碳原子的酰基或芳酰基; R1，R2，R3，和R 4各自独立地为氢，1-6个碳原子的烷基，1-6个碳原子的烷氧基，卤素，三氟烷基，-CN，1-6个碳原子的烷基磺酰胺，1-6个碳原子的烷基酰胺，氨基，1-6个碳原子的烷基氨基，每个烷基部分1-6个碳原子的二烷基氨基，1-6个碳原子的三氟烷氧基，2-7个碳原子的酰基或芳酰基; X是CR5R6或羰基; R5和 R6各自独立地为氢或1-6个碳原子的烷基;或其药学上可接受的盐，条件是R 1，R 2，R 3或R 4中的至少一个不是氢;它们是5HT 2C受体激动剂，其可用于治疗涉及中枢神经系统的障碍，如强迫症，抑郁症，焦虑症，精神分裂症，偏头痛，睡眠障碍，进食障碍，obesit y，II型糖尿病和癫痫。

9. 发明授权

US06784172B2 Processes for preparation of cyclopenta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives 失效
标题翻译：制备环戊二烯并[b] [1,4]二氮杂[6,7,1-hi]吲哚及其衍生物的方法
公开(公告)号：US06784172B2
公开(公告)日：2004-08-31
申请号：US10016420
申请日：2001-11-02
申请人： Annmarie Louise Sabb , Robert Lewis Vogel , Madelene Miyoko Antane , Panolil Raveendranath , Sreenivasulu Megati , Michael David Smith , James Albert Nelson
发明人： Annmarie Louise Sabb , Robert Lewis Vogel , Madelene Miyoko Antane , Panolil Raveendranath , Sreenivasulu Megati , Michael David Smith , James Albert Nelson
IPC分类号： A61K3155
CPC分类号： C07D487/06
摘要： This invention provides processes for synthesizing compounds of formula I: wherein R is H or alkyl; R1, R2 are H, alkyl, alkoxy, halogen, fluorinated alkyl, —CN, alkyl sulfonamide, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, or aroyl; R3 and R4 are H, alkyl or cycloalkyl; the dashed line indicates an optional double bond; as well as intermediates and pharmaceutically acceptable salts thereof.
摘要翻译：本发明提供了合成式I化合物的方法：其中R是H或烷基; R1，R2是H，烷基，烷氧基，卤素，氟化烷基，-CN，烷基磺酰胺，烷基酰胺，氨基，烷基氨基，二烷基氨基，氟化烷氧基，酰基或芳酰基。 R3和R4是H，烷基或环烷基; 虚线表示可选的双键; 以及其中间体和药学上可接受的盐。

10. 发明授权

US06476032B2 2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5(6H)one derivatives 失效
标题翻译： 2,3,4,4a-四氢-1H-吡嗪并[1,2-a]喹喔啉-5（6H）一种衍生物
公开(公告)号：US06476032B2
公开(公告)日：2002-11-05
申请号：US09891593
申请日：2001-06-26
申请人： Sharon Joy Rosenzweig-Lipson , Annmarie Louise Sabb , Gregory Scott Welmaker , James Albert Nelson
发明人： Sharon Joy Rosenzweig-Lipson , Annmarie Louise Sabb , Gregory Scott Welmaker , James Albert Nelson
IPC分类号： A61K314985
CPC分类号： C07D487/04 , A61K31/4985
摘要： This invention provides compounds of formula I, wherein R is hydrogen or alkyl of 1-6 carbon atoms; R′ is hydrogen, alkyl of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R1, R2, R3, and R4 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, trifluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, trifluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; X is CR5R6 or a carbonyl group; R5 and R6 are each, independently, hydrogen or alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof, with the proviso that at least one of R1, R2, R3, or R4 are not hydrogen; which are 5HT2C receptor agonists useful for the treatment of disorders involving the central nervous system such as obsessive-compulsive disorder, depression, anxiety, schizophrenia, migraine, sleep disorders, eating disorders, obesity, type II diabetes, and epilepsy.
摘要翻译：本发明提供了式I化合物，其中R是氢或1-6个碳原子的烷基; R'是氢，1-6个碳原子的烷基，2-7个碳原子的酰基或芳酰基; R1，R2，R3，和R 4各自独立地为氢，1-6个碳原子的烷基，1-6个碳原子的烷氧基，卤素，三氟烷基，-CN，1-6个碳原子的烷基磺酰胺，1-6个碳原子的烷基酰胺，氨基，1-6个碳原子的烷基氨基，每个烷基部分1-6个碳原子的二烷基氨基，1-6个碳原子的三氟烷氧基，2-7个碳原子的酰基或芳酰基; X是CR5R6或羰基; R5和 R6各自独立地为氢或1-6个碳原子的烷基;或其药学上可接受的盐，条件是R 1，R 2，R 3或R 4中的至少一个不是氢;它们是5HT 2C受体激动剂，其可用于治疗涉及中枢神经系统的障碍，例如强迫症，抑郁症，焦虑症，精神分裂症，偏头痛，睡眠障碍，进食障碍，肥胖，II型糖尿病和癫痫。

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