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1. 发明授权

US6110956A N-aryloxyethylamine derivatives for the treatment of depression 失效
标题翻译： N-芳氧基乙胺衍生物用于治疗抑郁症
公开(公告)号：US6110956A
公开(公告)日：2000-08-29
申请号：US287416
申请日：1999-04-07
申请人： Richard E. Mewshaw , Dahui Zhou , Ping Zhou
发明人： Richard E. Mewshaw , Dahui Zhou , Ping Zhou
IPC分类号： A61P25/24 , C07D209/14 , C07D403/12 , C07D405/12 , A61K31/404 , A61K31/4045 , C07D209/04 , C07D403/08
CPC分类号： C07D403/12 , C07D209/14 , C07D405/12
摘要： Compounds effective in treating disorders of the serotonin-affected neurological systems are provided, such compounds having the following formula: ##STR1## wherein: R.sub.1 and R.sub.2 are each, independently, hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy, MeSO.sub.2, or together can form a 5-7 membered carbocyclic or heterocyclic ring;R.sub.3 is alkoxy, halogen, hydrogen or carbamoyl;R.sub.4 is hydrogen, hydroxy, lower alkyl, or lower alkoxy;R.sub.5 is hydrogen, lower alkyl, or halogen;R.sub.6 is hydrogen, lower alkyl, or phenyl;R.sub.7 is hydrogen, lower alkyl, lower alkoxy, halogen, CN, CF.sub.3, or hydroxy; andX is (CH.sub.2).sub.n,wherein n is 0 to 3; or pharmaceutically acceptable salts thereof.
摘要翻译：提供了有效治疗受5-羟色胺影响的神经系统疾病的化合物，具有下式的化合物：其中：R 1和R 2各自独立地为氢，卤素，CF 3，低级烷基，低级烷氧基，MeSO 2或一起可形成 5-7元碳环或杂环; R3是烷氧基，卤素，氢或氨基甲酰基; R4是氢，羟基，低级烷基或低级烷氧基; R5是氢，低级烷基或卤素; R6是氢，低级烷基或苯基; R7是氢，低级烷基，低级烷氧基，卤素，CN，CF3或羟基; X为（CH 2）n，n为0〜3; 或其药学上可接受的盐。

2. 发明授权

US06489342B2 Aryloxy piperidinyl indoles for treating depression 失效
标题翻译：芳氧基哌啶基吲哚用于治疗抑郁症
公开(公告)号：US06489342B2
公开(公告)日：2002-12-03
申请号：US10002340
申请日：2001-11-15
申请人： Richard E. Mewshaw , Dahui Zhou , Ping Zhou
发明人： Richard E. Mewshaw , Dahui Zhou , Ping Zhou
IPC分类号： A61K31454
CPC分类号： C07D401/14
摘要： This invention provides aryloxy indole derivatives which are useful for the treatment of diseases affected by disorders of the serotonin-affected neurological systems, such as depression and anxiety, the compounds having the formula: wherein R1 is H or alkyl; R2, R3, and R4 are H, alkyl, or halogen; X is H, halogen, CN, or C1-C6 alkoxy; Z is (CH2)n or carbonyl; n is 1 or 2; and the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了芳氧基吲哚衍生物，其可用于治疗受血清素受影响的神经系统疾病如抑郁和焦虑影响的疾病，具有下式的化合物：其中R1是H或烷基; R2，R3和R4是H，烷基或卤素; X是H，卤素，CN或C 1 -C 6烷氧基; Z是（CH 2）n或羰基; n为1或2; 虚线表示可选的双键; 或其药学上可接受的盐。

3. 发明授权

US06313126B1 Arylpiperazinyl-cyclohexyl indole derivatives for the treatment of depression 失效
标题翻译：用于治疗抑郁症的芳基哌嗪基 - 环己基吲哚衍生物
公开(公告)号：US06313126B1
公开(公告)日：2001-11-06
申请号：US09476254
申请日：1999-12-30
申请人： Richard E. Mewshaw , Ping Zhou , Dahui Zhou , Kristin L. Meagher , Magda Asselin , Deborah A. Evrard , Adam M. Gilbert
发明人： Richard E. Mewshaw , Ping Zhou , Dahui Zhou , Kristin L. Meagher , Magda Asselin , Deborah A. Evrard , Adam M. Gilbert
IPC分类号： A61K31496
CPC分类号： C07D401/08 , C07D209/14 , C07D209/34 , C07D401/12 , C07D403/12 , C07D405/12 , C07D471/04
摘要： Compounds are provided which are useful for the treatment of serotonin-affected neurological disorders which comprise Wherein: R1, R2 and R3 are each, independently, hydrogen, halogen, CF3, alkyl, alkoxy, MeSO2, or together can form a 5-7 membered carbocyclic or heterocyclic ring; R4 is hydrogen, halogen, or alkyl; R5 is hydrogen, alkyl, alkylaryl, or aryl; R6 is hydrogen, halogen, CF3, CN, carbamide, or alkoxy; X1, X2 and X3 are each carbon or one of X1, X2 or X3 may be nitrogen; Y is carbon or nitrogen; and Z is carbon or nitrogen; or pharmaceutically acceptable salts thereof.
摘要翻译：提供了可用于治疗受5-羟色胺影响的神经系统疾病的化合物，其包括：R 1，R 2和R 3各自独立地为氢，卤素，CF 3，烷基，烷氧基，MeSO 2或一起可以形成5-7元碳环或杂环; R 4为氢，卤素或烷基; R 5为氢，烷基，烷基芳基或芳基; R 6为氢，卤素，CF 3，CN，脲或烷氧基; X 1，X 2和X 3为碳或 X1，X2或X3可以是氮; Y是碳或氮; Z为碳或氮; 其药学上可接受的盐。

4. 发明授权

US06465482B2 Arylpiperazinyl-cyclohexyl indole derivatives for the treatment of depression 失效
标题翻译：用于治疗抑郁症的芳基哌嗪基 - 环己基吲哚衍生物
公开(公告)号：US06465482B2
公开(公告)日：2002-10-15
申请号：US09969910
申请日：2001-10-03
申请人： Richard E. Mewshaw , Ping Zhou , Dahui Zhou , Kristin L. Meagher , Magda Asselin , Deborah A. Evrard , Adam M. Gilbert
发明人： Richard E. Mewshaw , Ping Zhou , Dahui Zhou , Kristin L. Meagher , Magda Asselin , Deborah A. Evrard , Adam M. Gilbert
IPC分类号： A61K31454
CPC分类号： C07D401/08 , C07D209/14 , C07D209/34 , C07D401/12 , C07D403/12 , C07D405/12 , C07D471/04
摘要： Compounds are provided which are useful for the treatment of serotonin-affected neurological disorders which comprise Wherein: R1, R2 and R3 are each, independently, hydrogen, halogen, CF3, alkyl, alkoxy, MeSO2, or together can form a 5-7 membered carbocyclic or heterocyclic ring; R4 is hydrogen, halogen, or alkyl; R5 is hydrogen, alkyl, alkylaryl, or aryl; R6 is hydrogen, halogen, CF3, CN, carbamide, or alkoxy; X1, X2 and X3 are each carbon or one of X1, X2 or X3 may be nitrogen; Y is carbon or nitrogen; and Z is carbon or nitrogen; or pharmaceutically acceptable salts thereof.
摘要翻译：提供了可用于治疗受5-羟色胺影响的神经系统疾病的化合物，其包括：R 1，R 2和R 3各自独立地为氢，卤素，CF 3，烷基，烷氧基，MeSO 2或一起可以形成5-7元碳环或杂环; R 4为氢，卤素或烷基; R 5为氢，烷基，烷基芳基或芳基; R 6为氢，卤素，CF 3，CN，脲或烷氧基; X 1，X 2和X 3为碳或 X1，X2或X3可以是氮; Y是碳或氮; Z为碳或氮; 其药学上可接受的盐。

5. 发明授权

US6162803A Indol-3-yl-cyclohexyl amine derivatives for the treatment of depression 失效
标题翻译：吲哚-3-基 - 环己基胺衍生物用于治疗抑郁症
公开(公告)号：US6162803A
公开(公告)日：2000-12-19
申请号：US287676
申请日：1999-04-07
申请人： Richard E. Mewshaw , Ping Zhou
发明人： Richard E. Mewshaw , Ping Zhou
IPC分类号： C07D413/12 , A61K31/536 , A61K31/4985 , C07D215/12 , C07D241/38 , C07D413/08
CPC分类号： C07D413/12
摘要： Compounds effective in treating disorders of the serotonin-affected neurological symptoms are provided, such compounds having the following formula: ##STR1## wherein: R.sub.1 and R.sub.5 are each, independently, hydrogen, halogen, lower alkoxy, lower alkyl, cyano, or trifluoromethyl;R.sub.2 and R.sub.4 are each, independently, hydrogen, lower alkyl, phenyl, or substituted phenyl;R.sub.3 is hydrogen or lower alkyl; andX and Y are each, independently, O, NR.sub.6, or CH.sub.2, whereinR.sub.6 is hydrogen, lower alkyl, phenyl, or substituted phenyl; or pharmaceutically acceptable salts thereof.
摘要翻译：提供了有效治疗血清素受影响的神经症状的疾病的化合物，具有下式的化合物：其中：R 1和R 5各自独立地为氢，卤素，低级烷氧基，低级烷基，氰基或三氟甲基; R2和R4各自独立地为氢，低级烷基，苯基或取代的苯基; R3是氢或低级烷基; 并且X和Y各自独立地是O，NR 6或CH 2，其中R 6是氢，低级烷基，苯基或取代的苯基; 或其药学上可接受的盐。

6. 发明授权

US06610712B2 Aryloxy piperidinyl derivatives for the treatment of depression 失效
标题翻译：芳氧基哌啶衍生物用于治疗抑郁症
公开(公告)号：US06610712B2
公开(公告)日：2003-08-26
申请号：US10000642
申请日：2001-11-15
申请人： Richard E. Mewshaw , Dahui Zhou , Ping Zhou
发明人： Richard E. Mewshaw , Dahui Zhou , Ping Zhou
IPC分类号： C07D40104
CPC分类号： C07D401/06 , C07D405/14
摘要： This invention provides compounds useful in treating serotonin-related central nervous system disorders, including anxiety, generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, sleep disorders, sexual dysfunction, alcohol and drug addiction, Alzheimer's disease, Parkinson's disease, obesity and migraine, the compounds having the general formula: wherein: R1 and R2 may each be H or an alkyl or alkoxy group; or R1 and R2 may be concatenated to form a bicyclic ring system with the phenyl ring to which they are bound; X is selected from hydrogen, halogen, cyano, C1-C6 alkoxy; Z is (CH2)n or carbonyl; n is 0, 1 or 2; the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了可用于治疗血清素相关的中枢神经系统疾病的化合物，包括焦虑，广泛性焦虑症，恐慌症，强迫症，睡眠障碍，性功能障碍，酒精和药物成瘾，阿尔茨海默病，帕金森病，肥胖症和偏头痛具有以下通式的化合物：其中：R 1和R 2可以各自为H或烷基或烷氧基; 或者R 1和R 2可以连接形成与它们所结合的苯环的双环系统; X选自氢，卤素，氰基，C 1 -C 6烷氧基; Z是（CH 2）n或羰基; n为0,1或2; 虚线表示可选的双键; 或其药学上可接受的盐。

7. 发明授权

US06313114B1 3,4-Dihydro-2H-benzo[1,4]oxazinyl-methyl)-[3-(1H-indol-3yl)-alkyl]- amines 失效
标题翻译： 3,4-二氢-2H-苯并[1,4]恶嗪基 - 甲基） - [3-（1H-吲哚基） - 烷基] - 胺
公开(公告)号：US06313114B1
公开(公告)日：2001-11-06
申请号：US09475940
申请日：1999-12-30
申请人： Richard E. Mewshaw , Dahui Zhou , Ping Zhou
发明人： Richard E. Mewshaw , Dahui Zhou , Ping Zhou
IPC分类号： C07D41312
CPC分类号： C07D413/12
摘要： Compounds are provided which have the following formula: wherein: R is hydrogen, alkyl of 1 to 6 carbon atoms, phenyl, or substituted phenyl; X and Y are each, independently, hydrogen, halogen, cyano, or alkoxy of 1 to 6 carbon atoms; and m is 1 to 5; or a pharmaceutically acceptable salt thereof.
摘要翻译：提供具有下式的化合物：其中：R是氢，1至6个碳原子的烷基，苯基或取代的苯基; X和Y各自独立地是氢，卤素，氰基或1-6个碳的烷氧基原子 andm是1到5; 或其药学上可接受的盐。

8. 发明授权

US06245799B1 [(Indol-3-yl)-cycloalkyl]-3-substituted azetidines for the treatment of central nervous system disorders 失效
标题翻译： [（吲哚-3-基） - 环烷基] -3-取代的氮杂环丁烷，用于治疗中枢神经系统疾病
公开(公告)号：US06245799B1
公开(公告)日：2001-06-12
申请号：US09707146
申请日：2000-11-06
申请人： Magda Asselin , John W. Ellingboe , Richard E. Mewshaw
发明人： Magda Asselin , John W. Ellingboe , Richard E. Mewshaw
IPC分类号： A61K31404
CPC分类号： C07D403/08
摘要： This invention provides novel compounds and pharmaceutical compositions and methods of using the compounds in the treatment of central nervous system disorders, such as anxiety and depression, the compounds having the formula I: wherein: X is N—R, O, S(O)m; m is 0 to 2; n is 0 to 4; Ar is an aryl group of 6 to 12 carbon atoms optionally substituted with 1 to 3 R3 groups, or a heteroaryl group of 4 to 10 carbon atoms optionally substituted with 1 to 3 R3 groups; R and R2 are independently H, straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, alkoxycarbonyl of 1 to 6 carbon atoms, alkylcarbonyl of 1 to 6 carbon atoms, aminocarbonyl, or alkylaminocarbonyl of 1 to 4 carbon atoms; R1 and R3 are independently H, straight chain alkyl of 1 to 4 carbon atoms, branched alkyl of 3 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, halo, alkoxy group of 1 to 4 carbon atoms, haloalkyl of 1 to 4 carbon atoms, OH, nitro, amino, sulfonyl, CN, carboxy, alkoxycarbonyl of 1 to 4 carbon atoms, alkylcarbonyl of 1 to 4 carbon atoms, aminocarbonyl, or alkylaminocarbonyl of 1 to 4 carbon atoms; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了新的化合物和药物组合物和使用该化合物治疗中枢神经系统疾病如焦虑和抑郁的方法，具有式I的化合物：其中：X是N-R，O，S（O）m; m为0〜2; n为0〜4; Ar是任选被1至3个R 3基团取代的6至12个碳原子的芳基或任选被1至3个R 3基团取代的4至10个碳原子的杂芳基; R 2和R 2独立地是H，直链烷基 1至6个碳原子，3至6个碳原子的支链烷基，3至6个碳原子的环烷基，1至6个碳原子的烷氧基羰基，1至6个碳原子的烷基羰基，氨基羰基或1至4个碳原子的烷基氨基羰基; R 1和R 3独立地为H，1至4个碳原子的直链烷基，3至6个碳原子的支链烷基，3至8个碳原子的环烷基，卤素，1至4个碳原子的烷氧基，1至4个卤代烷基碳原子，OH，硝基，氨基，磺酰基，CN，羧基，1至4个碳原子的烷氧基羰基，1至4个碳原子的烷基羰基，氨基羰基或1至4个碳原子的烷基氨基羰基;或其药学上可接受的盐。

9. 发明授权

US06200994B1 1,4-Disubstituted cyclohexane derivatives for the treatment of depression 失效
标题翻译： 1,4-二取代的环己烷衍生物用于治疗抑郁症
公开(公告)号：US06200994B1
公开(公告)日：2001-03-13
申请号：US09475384
申请日：1999-12-30
申请人： Richard E. Mewshaw , Reinhardt B. Baudy
发明人： Richard E. Mewshaw , Reinhardt B. Baudy
IPC分类号： C07D40108
CPC分类号： C07D409/12 , C07D409/14
摘要： Compounds useful for the treatment of disorders of the serotonin-affected neurological systems are provided which have the following formula: wherein: X is carbon or nitrogen; R1 and R2 are each, independently, hydrogen, halogen, CF3, alkyl, alkoxy, or MeSO24; R3 is hydrogen, halogen, or alkyl; R4 is hydrogen, alkyl, alkylaryl, or aryl; and R5 is hydrogen, halogen, CF3, CN, carbamide, or alkoxy; or pharmaceutically acceptable salts thereof.
摘要翻译：提供了可用于治疗受5-羟色胺影响的神经系统疾病的化合物，其具有下式：其中：X是碳或氮; R 1和R 2各自独立地是氢，卤素，CF 3，烷基，烷氧基或MeSO 24 ; R 3是氢，卤素或烷基; R 4是氢，烷基，烷基芳基或芳基; 和R 5是氢，卤素，CF 3，CN，脲基或烷氧基; 其药学上可接受的盐。

10. 发明授权

US6150533A N-aryloxyethyl-indoly-alkylamines for the treatment of depression 失效
标题翻译：用于治疗抑郁症的N-芳氧基乙基 - 吲哚烷基胺
公开(公告)号：US6150533A
公开(公告)日：2000-11-21
申请号：US287832
申请日：1999-04-07
申请人： Richard E. Mewshaw , James A. Nelson
发明人： Richard E. Mewshaw , James A. Nelson
IPC分类号： C07D209/34 , C07D403/12 , C07D235/04 , A61K31/404 , A61K31/4184 , C07D209/48 , C07D235/22 , A61N25/24
CPC分类号： C07D403/12 , C07D209/34
摘要： Compounds effective in treating disorders of the serotonin-affected neurological systems are provided, such compounds having the following formula: ##STR1## wherein: R.sub.1 is hydrogen, lower alkyl, phenyl, or substituted phenyl;X and Y together complete a lactam, imidazole, imidazolone, or thioimidazolone ring;Z is hydrogen, halogen, or lower alkoxy;W is hydrogen, halogen, lower alkoxy, lower alkyl, cyano, or a trifluoromethyl group;and n=2 to 5; or pharmaceutically acceptable salts thereof.
摘要翻译：提供了有效治疗血清素受影响的神经系统疾病的化合物，这些化合物具有下式：其中：R 1是氢，低级烷基，苯基或取代的苯基; X和Y一起完成内酰胺，咪唑，咪唑啉酮或硫代咪唑啉酮环; Z是氢，卤素或低级烷氧基; W是氢，卤素，低级烷氧基，低级烷基，氰基或三氟甲基; n = 2〜5; 或其药学上可接受的盐。

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