公开(公告)号：US06503900B2

公开(公告)日：2003-01-07

申请号：US10017738

申请日：2001-11-02

申请人： Annmarie Louise Sabb ,  Gregory Scott Welmaker ,  Robert Lewis Vogel ,  Joan Eileen Sabalski

发明人： Annmarie Louise Sabb ,  Gregory Scott Welmaker ,  Robert Lewis Vogel ,  Joan Eileen Sabalski

IPC分类号： A61K3155

CPC分类号： C07D487/06

摘要： This invention provides [1,4]diazepino[6,7,1-jk]carbazole compounds of the formula: wherein: R1 and R2 are H, alkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, phenoyl or thiophenoyl; R3, R4, R5 and R6 are H, alkyl, cycloalkyl, alkoxy or cycloalkoxy; R7 is H or alkyl; R8 is H or alkyl; and the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof, as well as methods and pharmaceutical compositions utilizing them for the treatment or prevention of disorders such as obsessive-compulsive disorder, depression, anxiety, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.

摘要翻译： 本发明提供下式的[1,4]二氮杂[6,7,1-jk]咔唑化合物：其中：R1和R2是H，烷基，烷氧基，卤素，氟化烷基，-CN，-NH-SO2-烷基 ，-SO 2 -NH-烷基，烷基酰胺，氨基，烷基氨基，二烷基氨基，氟化烷氧基，酰基，苯甲酰基或噻吩甲酰基; R3，R4，R5和R6是H，烷基，环烷基，烷氧基或环烷氧基; R7是H或烷基; R8是H或烷基; 虚线表示可选的双键; 或其药学上可接受的盐，以及利用它们用于治疗或预防诸如强迫症，抑郁症，焦虑症，精神分裂症，偏头痛，睡眠障碍，进食障碍，肥胖，癫痫和脊髓障碍的疾病的方法和药物组合物 线损伤。

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：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：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：US06414144B1

公开(公告)日：2002-07-02

申请号：US10016435

申请日：2001-11-02

申请人： Gregory Scott Welmaker ,  Joan Eileen Sabalski

发明人： Gregory Scott Welmaker ,  Joan Eileen Sabalski

IPC分类号： C07D24300

CPC分类号： C07D487/06

摘要： The present invention provides processes for the preparation of 1, 2, 3, 4, 8, 9, 10, 10a-octahydro-7bH-cyclopenta[b][1, 4]diazepino[6, 7, 1-hi]indole derivatives of the general formula: wherein: R is H, alkyl, acyl, or aroyl; R1, R2, R4 and R5 are H, OH, alkyl, cycloalkyl, alkoxy s, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino s, dialkylamino, fluorinated alkoxy, acyl, aryl, or aroyl; R3 is H, alkyl, cycloalkyl, alkoxy, fluorinated alkyl, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, aryl, or aroyl; or a pharmaceutically acceptable salt thereof, which are useful in the treatment of central nervous system disorders.

摘要翻译： 本发明提供制备1,2,3,4,8,9,10,10a-八氢-7H-环戊二烯并[b] [1,4]二氮杂[6,7，1-hi]吲哚衍生物的方法 其中：R是H，烷基，酰基或芳酰基; R1，R2，R4和R5是H，OH，烷基，环烷基，烷氧基，卤素，氟化烷基，-CN，-NH-SO2-烷基，-SO2-NH-烷基，烷基酰胺，氨基，烷基氨基，二烷基氨基 ，氟化烷氧基，酰基，芳基或芳酰基; R 3是H，烷基，环烷基，烷氧基，氟化烷基，-NH-SO 2 - 烷基，-SO 2 -NH-烷基，烷基酰胺，氨基，烷基氨基，二烷基氨基，氟化烷氧基，酰基，芳基或芳酰基。 或其药学上可接受的盐，其可用于治疗中枢神经系统疾病。