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1. 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。

2. 发明授权

US07425558B2 Serotonergic agents for treating sexual dysfunction 失效
标题翻译：用于治疗性功能障碍的5-羟色胺能药物
公开(公告)号：US07425558B2
公开(公告)日：2008-09-16
申请号：US11506514
申请日：2006-08-18
申请人： Stacey J. Sukoff Rizzo , Sharon Joy Rosenzweig-Lipson , Wayne Everett Childers , Michael Kelly , Lee Erwin Schechter
发明人： Stacey J. Sukoff Rizzo , Sharon Joy Rosenzweig-Lipson , Wayne Everett Childers , Michael Kelly , Lee Erwin Schechter
IPC分类号： A61K31/496
CPC分类号： A61K31/137 , A61K31/165 , A61K31/445 , A61K31/496 , A61K31/515 , A61K31/519 , A61K31/5415 , A61K31/55 , A61K31/551
摘要： Methods and compositions are provided for treating sexual dysfunction, e.g., sexual dysfunction associated with drug treatment, using 5-HT1A receptor antagonists.
摘要翻译：提供了使用5-HT 1A受体拮抗剂治疗性功能障碍（例如与药物治疗相关的性功能障碍）的方法和组合物。

3. 发明授权

US07816362B2 Serotonergic agents 失效
标题翻译：血清素能药
公开(公告)号：US07816362B2
公开(公告)日：2010-10-19
申请号：US12435862
申请日：2009-05-05
申请人： Wayne Everett Childers , Michael Kelly , Sharon Joy Rosenzweig-Lipson
发明人： Wayne Everett Childers , Michael Kelly , Sharon Joy Rosenzweig-Lipson
IPC分类号： A61K31/496
CPC分类号： A61K31/496
摘要： Novel piperazine derivatives are provided having the formula wherein R1 is cyano, nitro, trifluoromethyl or halogen, or pharmaceutically acceptable acid addition salts thereof, which are useful as 5-HT1A receptor antagonists.
摘要翻译：提供具有下式的新型哌嗪衍生物其中R 1是氰基，硝基，三氟甲基或卤素，或其药学上可接受的酸加成盐，其可用作5-HT 1A受体拮抗剂。

4. 发明申请

US20080161260A1 Methods for Detecting and Quantifying Cell Proliferation In Vivo 审中-公开
标题翻译：检测和定量细胞增殖的方法
公开(公告)号：US20080161260A1
公开(公告)日：2008-07-03
申请号：US11844909
申请日：2007-08-24
申请人： Zia Rahman , Jessica Eden Malberg , Robert Hamlink Ring , Sharon Joy Rosenzweig-Lipson , Lee E. Schechter
发明人： Zia Rahman , Jessica Eden Malberg , Robert Hamlink Ring , Sharon Joy Rosenzweig-Lipson , Lee E. Schechter
IPC分类号： A61K31/70 , C12Q1/68 , A61P43/00
CPC分类号： C12Q1/6804 , C07K16/44 , C07K2317/55
摘要： The invention provides a rapid, sensitive method for detecting and quantifying in vivo cell proliferation in a mammal.
摘要翻译：本发明提供了用于检测和定量哺乳动物体内细胞增殖的快速，灵敏的方法。

5. 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。

6. 发明授权

US06589986B2 Methods of treating anxiety disorders 失效
标题翻译：治疗焦虑症的方法
公开(公告)号：US06589986B2
公开(公告)日：2003-07-08
申请号：US10022579
申请日：2001-12-17
申请人： Mark R. Bowlby , Sharon Joy Rosenzweig-Lipson
发明人： Mark R. Bowlby , Sharon Joy Rosenzweig-Lipson
IPC分类号： A01N4710
CPC分类号： A61K31/18 , A61K31/167 , A61K31/17 , A61K31/27 , A61K31/325 , Y10S514/903
摘要： This invention provides methods for treating, preventing or inhibiting anxiety, anxiety-related conditions and phobias in a mammal using compounds of the formula: wherein: R1 is H, alkyl, alkanoyl or the radical Ar; R2 is H or alkyl; R3 is alkoxy, NH2, alkylamino, dialkylamino, amino substituted by the radical Ar, alkyl, alkenyl, alkynyl, or the radicals Ar or ArO—; R4 is H, alkyl or the radical Ar; R5 is H or alkyl or the radical Ar; or a pharmaceutically acceptable salt or ester form thereof; Ar is an optionally substituted phenyl radical; and n is 0 or 1, or a pharmaceutically acceptable salt or ester form thereof, with the methods particularly including the use of N-[2-amino-4-(4-fluorobenzylamino)-phenyl]carbamic acid ethyl ester, also known as retigabine.
摘要翻译：本发明提供了使用下式化合物治疗，预防或抑制哺乳动物焦虑，焦虑相关病症和恐惧症的方法：其中：R1是H，烷基，烷酰基或基团Ar; R2是H或烷基; R 3是烷氧基，NH 2，烷基氨基，二烷基氨基，被基团Ar，烷基，烯基，炔基或基团Ar或ArO-取代的氨基; R4是H，烷基或基团Ar; R5是H或烷基或基团Ar; 或其药学上可接受的盐或酯形式; Ar是任选取代的苯基; 并且n为0或1，或其药学上可接受的盐或酯形式，其中所述方法特别包括使用N- [2-氨基-4-（4-氟苄基氨基） - 苯基]氨基甲酸乙酯，也称为瑞替加滨

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