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1. 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。

2. 发明授权

US06228880B1 4-amino-(ethylamino)-oxindole dopamine autoreceptor agonists 失效
标题翻译： 4-氨基 - （乙基氨基） - 氧吲哚多巴胺自身受体激动剂
公开(公告)号：US06228880B1
公开(公告)日：2001-05-08
申请号：US09287675
申请日：1999-04-07
申请人： James A. Nelson , Mira A. Kanzelberger , Richard E. Mewshaw
发明人： James A. Nelson , Mira A. Kanzelberger , Richard E. Mewshaw
IPC分类号： A61K31404
CPC分类号： C07D209/34
摘要： Compounds having dopaminegic activity are provided, having the formula: wherein R1 and R2 are each, independently, hydrogen, C1-10 alkyl, or (CH2)mR4, wherein R4 is phenyl or naphthyl which may be substituted by one or two substituents selected from the group consisting of C1-6 alkyl, halogen, C1-6 alkoxide and trifluoromethyl and m is 1 to 5; and R3 is hydrogen or C1-6 alkyl; or pharmaceutically acceptable salts thereof.
摘要翻译：提供了具有多巴胺活性的化合物，其具有下式：其中R 1和R 2各自独立地为氢，C 1-10烷基或（CH 2）m R 4，其中R 4为苯基或萘基，其可以被一个或两个选自由C 1-6烷基，卤素，C 1-6烷氧基和三氟甲基组成的组，m为1至5; 和R 3是氢或C 1-6烷基; 其药学上可接受的盐。

3. 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。

4. 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。

5. 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。

6. 发明授权

US5750556A 2-(aminomethyl)-3,4,7,9-tetrahydro-2H-pyrano-�2,3-E!indol-8-ones and derivatives 失效
标题翻译： -2（氨基甲基）-3,4,7,9-四氢-2H-吡喃并[2,3-E]吲哚-8-酮和衍生物
公开(公告)号：US5750556A
公开(公告)日：1998-05-12
申请号：US739917
申请日：1996-10-30
申请人： Richard E. Mewshaw , Gary P. Stack
发明人： Richard E. Mewshaw , Gary P. Stack
IPC分类号： A61K31/407 , C07D491/04 , C07D491/052 , A61K31/40 , A61K31/44 , C07D491/00
CPC分类号： C07D491/04 , A61K31/407
摘要： Compounds of Formula I are selective autoreceptor agonists useful in treating disease states involving hyperactivity of dopamine systems: ##STR1## in which X is --(CH.sub.2).sub.n --; n is 1-3; R.sub.1 is hydrogen, alkyl, hydroxyalkyl, cycloalkyl-methyl, bicyclo-alkylmethyl or --(CH.sub.2).sub.m YAr; where m is 0-4, Y is --CH.sub.2 --, and Ar is phenyl, halophenyl, alkylphenyl, dialkylphenyl or alkoxyphenyl; R.sub.2 is hydrogen or alkyl; R.sub.3 is hydrogen, halogen, alkyl, alkoxy or hydroxy; or a pharmaceutically acceptable salt thereof.
摘要翻译：式I的化合物是可用于治疗涉及多巴胺系统多动症的疾病状态的选择性自体受体激动剂：其中X是 - （CH 2）n - ; n为1-3; R1是氢，烷基，羟基烷基，环烷基 - 甲基，双环烷基甲基或 - （CH2）mYAr; 其中m为0-4，Y为-CH2-，Ar为苯基，卤代苯基，烷基苯基，二烷基苯基或烷氧基苯基; R2是氢或烷基; R3是氢，卤素，烷基，烷氧基或羟基; 或其药学上可接受的盐。

7. 发明授权

US5541199A Chroman-2-ylmethylamino derivatives 失效
标题翻译：色满-2-基甲基氨基衍生物
公开(公告)号：US5541199A
公开(公告)日：1996-07-30
申请号：US460168
申请日：1995-06-02
申请人： Richard E. Mewshaw
发明人： Richard E. Mewshaw
IPC分类号： C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D493/02 , C07D498/02
CPC分类号： C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12
摘要： Compounds of the formula: ##STR1## in which n is one of the integers 1, 2, 3,or 4; m is one of the integers 0 or 1; R is ##STR2## or a pharmaceutically acceptable salt thereof, are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.
摘要翻译：下式的化合物：其中n是整数1,2,3或4之一; m是整数0或1之一; R是或其药学上可接受的盐，是多巴胺合成和释放的抑制剂，可用于治疗精神分裂症，帕金森病，图雷特综合征，酒精成瘾，可卡因成瘾和成瘾到药物。

8. 发明授权

US4709025A Beta-lactams substituted at C-4 with substituted aminooxymethyl 失效
标题翻译：在C-4被取代的氨氧基甲基取代的β-内酰胺
公开(公告)号：US4709025A
公开(公告)日：1987-11-24
申请号：US4529
申请日：1987-01-20
申请人： Richard E. Mewshaw , Thomas J. Commons
发明人： Richard E. Mewshaw , Thomas J. Commons
IPC分类号： C07D417/12 , A61K31/425 , A61K31/55 , C07D417/14
CPC分类号： C07D417/12
摘要： This invention provides novel antibacterial beta-lactams of the formula: ##STR1## in which R is alkyl of 1 to 6 carbon atoms, carboxyalkyl of 2 to 6 carbon atoms or alkoxycarbonylalkyl wherein the alkyl and alkoxy moieties contain, independently, 1 to 6 carbon atoms;R.sup.1 is alkylideneamino of 2 to 6 carbon atoms, alkanoylamino of 2 to 6 carbon atoms, carboxyalkylideneamino of 2 to 6 carbon atoms, alkylsulfonylamino of 1 to 6 carbon atoms, alkoxycarbonylalkylsulfonylamino of 3 to 13 carbon atoms, or N,N-cyclodialkanoylamino of 4 to 6 carbon atoms;or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供新的抗菌β-内酰胺，其结构式为：其中R是1至6个碳原子的烷基，2至6个碳原子的羧基烷基或烷氧基羰基，其中烷基和烷氧基部分独立地包含1至6个碳原子 R 1是2至6个碳原子的亚烷基氨基，2至6个碳原子的烷酰基氨基，2至6个碳原子的羧基亚烷基氨基，1至6个碳原子的烷基磺酰基氨基，3至13个碳原子的烷氧基羰基烷基磺酰基氨基，或4个N，N-二环烷酰基氨基至6个碳原子; 或其药学上可接受的盐。

9. 发明授权

US06559169B2 Antidepressant azaheterocyclymethyl derivatives of 2,3-dihydro-1,4-benzodioxan 失效
标题翻译： 2,3-二氢-1,4-苯并二恶烷的抗抑郁药氮杂杂环甲基衍生物
公开(公告)号：US06559169B2
公开(公告)日：2003-05-06
申请号：US10128447
申请日：2002-04-23
申请人： George E. M. Husbands , Gary P. Stack , Richard E. Mewshaw , Ian A. Cliffe
发明人： George E. M. Husbands , Gary P. Stack , Richard E. Mewshaw , Ian A. Cliffe
IPC分类号： C07D40104
CPC分类号： C07D405/14 , C07D471/04
摘要： Compounds of the formula useful for the treatment of depression and other conditions such as obsessive compulsive disorder, panic attacks, generalized anxiety disorder, sexual dysfunction, eating disorders, addictive disorders caused by ethanol or cocaine abuse and related illnesses.
摘要翻译：用于治疗抑郁症和强迫症，恐慌发作，广泛性焦虑症，性功能障碍，饮食失调，乙醇或可卡因滥用引起的成瘾性疾病和相关疾病的其他疾病的组合物。

10. 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。

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