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    • 1. 发明授权
    • Cyclopenta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives
    • 环戊基[b] [1,4]二氮杂[6,7,1-hi]吲哚及其衍生物
    • US07271163B2
    • 2007-09-18
    • US10898029
    • 2004-07-23
    • Annmarie L. SabbRobert L. VogelJames A. NelsonSharon J. Rosenzweig-LipsonGregory S. WelmakerJoan E. Sabalski
    • Annmarie L. SabbRobert L. VogelJames A. NelsonSharon J. Rosenzweig-LipsonGregory S. WelmakerJoan E. Sabalski
    • A61K31/55A61P25/00A61P25/24C07D243/00
    • C07D209/94A61K31/55C07D487/06
    • 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.
    • 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各自独立地为氢,1-6个碳原子的烷基,环烷基,1-6个碳原子的烷氧基,-CH 2 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,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个碳原子的氟代烷氧基 -6个碳原子,2-7个碳原子的酰基,芳基或芳酰基; R 4和R 5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,氟烷基,-CN,烷基 1-6个碳原子的磺酰胺,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个碳原子或芳酰基; R 6和R 7各自独立地为氢,C 1 -C 6烷基或环烷基; 或其药学上可接受的盐,以及含有这些化合物的药物组合物及其使用方法,包括治疗强迫症,恐慌症,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。
    • 2. 发明授权
    • 2,3,4,4A-tetrahydro-1H-pyrazino[1,2-A]quinoxalin-5(6H)one derivatives
    • 2,3,4,4-四氢-1H-吡嗪并[1,2-A]喹喔啉-5(6H)酮衍生物
    • US06372745B1
    • 2002-04-16
    • US09455220
    • 1999-12-06
    • Annmarie L. SabbGregory S. WelmakerJames A. Nelson
    • Annmarie L. SabbGregory S. WelmakerJames A. Nelson
    • A61K315025
    • C07D487/04A61K31/4985
    • 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.
    • 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。