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1. 发明授权

US5597826A Compositions containing sertraline and a 5-HT.sub.1D receptor agonist or antagonist 失效
标题翻译：含有舍曲林和5-HT1D受体激动剂或拮抗剂的组合物
公开(公告)号：US5597826A
公开(公告)日：1997-01-28
申请号：US306230
申请日：1994-09-14
申请人： Harry R. Howard , John E. Macor , Bertrand L. Chenard , Jeffrey S. Sprouse , David W. Schulz
发明人： Harry R. Howard , John E. Macor , Bertrand L. Chenard , Jeffrey S. Sprouse , David W. Schulz
IPC分类号： C07D295/12 , A61K31/40 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/505 , A61K45/06 , A61P1/00 , A61P3/04 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D207/09 , C07D211/08 , C07D235/06 , C07D239/26 , C07D401/10 , C07D471/04 , A01N43/60
CPC分类号： A61K45/06 , Y10S514/811
摘要： The present invention relates to novel compositions containing the serotonin selective re-uptake inhibitor (SSRI), preferably (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine, and an agonist or antagonist of the serotonin 1 (5-HT.sub.1) receptor and to the use of such compositions for treating or preventing a condition selected from mood disorders, including depression, seasonal affective disorders and dysthmia, anxiety disorders including generalized anxiety disorder and panic disorder; agoraphobia, avoidant personality disorder; social phobia; obsessive compulsive disorder; post-traumatic stress disorder; memory disorders including dementia, amnestic disorders and age-associated memory impairment; disorders of eating behavior, including anorexia nervosa and bulimia nervosa; obesity; cluster headache; migraine; pain; Alzheimer's disease; chronic paroxysmal hemicrania; headache associated with vascular disorders; Parkinson's disease, including dementia in Parkinson's disease, neuroleptic-induced parkinsonism and tardive dyskinesias; endocrine disorders such as hyperprolactinaemia; vasospasm (particularly in the cerebral vasculature); hypertension; disorders in the gastrointestinal tract where changes in motility and secretion are involved; sexual dysfunction, including premature ejaculation; and chemical dependencies.
摘要翻译：本发明涉及含有5-羟色胺选择性再摄取抑制剂（SSRI），优选（1S-顺式）-4-（3,4-二氯苯基）-1,2,3,4-四氢-N-甲基 - 以及5-羟色胺1（5-HT1）受体的激动剂或拮抗剂，以及这些组合物用于治疗或预防选自情绪障碍，包括抑郁症，季节性情感障碍和心律不适的病症的用途，焦虑症包括广泛性焦虑症和恐慌症; 广场恐惧症，避孕人格障碍; 社交恐惧症强迫症创伤后应激障碍; 记忆障碍包括痴呆，遗忘性障碍和年龄相关记忆障碍; 饮食行为障碍，包括神经性厌食症和神经性贪食症; 肥胖; 簇头痛; 偏头痛疼痛; 阿尔茨海默氏病; 慢性阵发性黑血病与血管疾病相关的头痛; 帕金森病，包括帕金森病中的痴呆，精神安定药物引起的帕金森综合征和迟发性运动障碍; 内分泌紊乱如高泌乳素血症; 血管痉挛（特别是脑血管系统）; 高血压; 涉及运动和分泌变化的胃肠道疾病; 性功能障碍，包括早泄; 和化学依赖性。

2. 发明授权

US5436246A Serotonin receptor agents 失效
标题翻译：血清素受体剂
公开(公告)号：US5436246A
公开(公告)日：1995-07-25
申请号：US119791
申请日：1993-09-15
申请人： Ronald C. Bernotas , Jeffrey S. Sprouse , Hsien C. Cheng
发明人： Ronald C. Bernotas , Jeffrey S. Sprouse , Hsien C. Cheng
IPC分类号： C07D333/54 , A61K31/495 , A61K31/496 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D333/56 , C07D333/58 , C07D333/60 , C07D333/64 , C07D333/66 , C07D333/68 , C07D333/70 , C07D409/06
CPC分类号： C07D409/06 , C07D333/56 , C07D333/58 , C07D333/60 , C07D333/70
摘要： The present invention is directed to a new class of 2-optionally substituted-4-piperazine-benzothiophene derivatives of the formula ##STR1## in which Y is represented by hydrogen or C.sub.1-3 alkyl; R is represented by a substituent selected from the group consisting of hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, --CF.sub.3, --OCF.sub.3, and --OH; R.sub.1 is represented by hydrogen, cycloalkyl, C.sub.1-6 alkyl, phenyl optionally substituted, phenylalkyl, or phenylamidoalkyl; X is represented by hydrogen, --(CH.sub.2).sub.n X.sub.1, CH=CHX.sub.1 or CHX.sub.2 --(CH.sub.2).sub.q --CH.sub.3 ; n is an integer from 0-2; q is either the integer 0 or 1; X.sub.1 is represented by --OH--,--OR.sub.2, --NR.sub.2 R.sub.3, --CO.sub.2 R.sub.2, --CONR.sub.2 R.sub.3, --CN, or --COR.sub.2 ; R.sub.2 and R.sub.3 are each independently represented by hydrogen, C.sub.1-4 alkyl, phenyl optionally substituted, phenylalkyl, or R.sub.2 and R.sub.3 together form a (CH.sub.2).sub.m cycloalkyl, where m=2- 6; X.sub.2 is --OR.sub.4 or --NR.sub.4 R.sub.5 in which R.sub.4 and R.sub.5 are each independently hydrogen or C.sub.1-4 alkyl; and the pharmaceutically acceptable addition salts thereof; with the proviso that when n is O or X is --CH=CHX.sub.1, then X.sub.1 is not OH, OR.sub.2, or NR.sub.2 R.sub.3 ; that are serotonin 5HT.sub.1A and 5HT.sub.1D receptor agents.
摘要翻译：本发明涉及一类新的式（I）的2-任选取代的-4-哌嗪 - 苯并噻吩衍生物，其中Y由氢或C 1-3烷基表示; R由选自氢，C 1-4烷基，C 1-4烷氧基，卤素，-CF 3，-OCF 3和-OH的取代基表示; R 1由氢，环烷基，C 1-6烷基，任选取代的苯基，苯基烷基或苯基氨基烷基表示; X由氢表示， - （CH 2）n X 1，CH = CHX 1或CHX 2 - （CH 2）q -CH 3; n是0-2的整数; q是整数0或1; X1由-OH - ， - OR2，-NR2R3，-CO2R2，-CONR2R3，-CN或-COR2表示; R 2和R 3各自独立地由氢，C 1-4烷基，任选取代的苯基，苯基烷基或R 2和R 3一起形成（CH 2）m环烷基，其中m = 2-6; X 2是-OR 4或-NR 4 R 5，其中R 4和R 5各自独立地是氢或C 1-4烷基; 及其药学上可接受的加成盐; 条件是当n是O或X是-CH = CHX1时，则X1不是OH，OR2或NR2R3; 即5-羟色胺5HT1A和5HT1D受体剂。

3. 发明授权

US5387604A 1,4 benzodioxin derivatives and their use as serotonin 5HT.sub.1A agonists 失效
标题翻译： 1,4-苯并二恶英衍生物及其作为5-羟色胺5HT1A激动剂的用途
公开(公告)号：US5387604A
公开(公告)日：1995-02-07
申请号：US962434
申请日：1992-10-16
申请人： Ian A. McDonald , Ronald C. Bernotas , Mark W. Dudley , Jeffrey S. Sprouse
发明人： Ian A. McDonald , Ronald C. Bernotas , Mark W. Dudley , Jeffrey S. Sprouse
IPC分类号： A61K31/335 , A61K31/357 , A61K31/40 , A61K31/403 , A61K31/404 , A61P9/12 , A61P25/04 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D209/14 , C07D209/46 , C07D319/20
CPC分类号： C07D209/14 , C07D209/46 , C07D319/20
摘要： The present invention is directed to a new class of serotonin 5HT.sub.1A agonists.
摘要翻译：本发明涉及一类新的5-羟色胺5HT1A激动剂。

4. 发明授权

US5189179A Serotonin 5HT.sub.1A agonists 失效
标题翻译： SEROTONIN 5HT1A AGONISTS
公开(公告)号：US5189179A
公开(公告)日：1993-02-23
申请号：US735700
申请日：1991-07-30
申请人： Ian A. McDonald , Ronald C. Bernotas , Mark W. Dudley , Jeffrey S. Sprouse
发明人： Ian A. McDonald , Ronald C. Bernotas , Mark W. Dudley , Jeffrey S. Sprouse
IPC分类号： A61K31/335 , A61K31/357 , A61K31/40 , A61K31/403 , A61K31/404 , A61P9/12 , A61P25/04 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D209/14 , C07D209/46 , C07D319/20
CPC分类号： C07D209/14 , C07D209/46 , C07D319/20
摘要： The present invention is directed to a new class of serotonin 5HT.sub.1A agonists.

5. 发明授权

US5559143A Serotonin 5HT.sub.1A agonistic method 失效
标题翻译： 5-羟色胺5HT1A激动剂法
公开(公告)号：US5559143A
公开(公告)日：1996-09-24
申请号：US319916
申请日：1994-10-07
申请人： Ian A. McDonald , Ronald C. Bernotas , Mark W. Dudley , Jeffrey S. Sprouse
发明人： Ian A. McDonald , Ronald C. Bernotas , Mark W. Dudley , Jeffrey S. Sprouse
IPC分类号： A61K31/335 , A61K31/357 , A61K31/40 , A61K31/403 , A61K31/404 , A61P9/12 , A61P25/04 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D209/14 , C07D209/46 , C07D319/20 , A61K31/405
CPC分类号： C07D209/14 , C07D209/46 , C07D319/20
摘要： The present invention is directed to a new class of serotonin 5HT.sub.1A agonists.
摘要翻译：本发明涉及一类新的5-羟色胺5HT1A激动剂。

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