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。

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。

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。

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。

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。

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。

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。

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。

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。

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。