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1. 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。

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

US06291683B1 N-arloxyethyl-alkylamines for the treatment of depression 失效
标题翻译： N-芳氧基乙基 - 烷基胺用于治疗抑郁症
公开(公告)号：US06291683B1
公开(公告)日：2001-09-18
申请号：US09593267
申请日：2000-06-13
申请人： Richard E. Mewshaw , Dahui Zhou
发明人： Richard E. Mewshaw , Dahui Zhou
IPC分类号： A61K31405
CPC分类号： C07D401/12 , C07D209/14 , C07D405/12
摘要： Compounds useful for alleviating symptoms of depression are provided which have the following formula: wherein: R1 is hydrogen, lower alkyl or aryl; R2 is hydrogen, lower alkyl, phenyl or substituted phenyl; X and Y are each, independently, hydrogen, lower alkyl, lower alkoxy, or halogen, or together combine with the carbon atoms to which they are attached to complete a cyclopentyl, cyclohexyl, phenyl, pyrrolyl, pyranyl, pyridinyl, dihydrofuranyl, furanyl, dioxanyl, oxazolyl or isoxazolyl group; Z is hydrogen, halogen or lower alkoxy; with the proviso that when X, Y or Z represent lower alkoxy, they are not present at the ortho position; W is hydrogen, halogen, lower alkyl, cyano or a trifluoromethyl group; and n is 2-5; or pharmaceutically acceptable salts thereof.
摘要翻译：提供了可用于减轻抑郁症状的化合物，其具有下式：其中：R 1是氢，低级烷基或芳基; R 2是氢，低级烷基，苯基或取代的苯基; X和Y各自独立地是氢，低级烷基，低级烷氧基或卤素，或与它们所连接的碳原子一起结合形成环戊基，环己基，苯基，吡咯基，吡喃基，吡啶基，二氢呋喃基，呋喃基，二恶烷基，恶唑基或异恶唑基; Z是氢，卤素或低级烷氧基; 条件是当X，Y或Z表示低级烷氧基时，它们不存在于邻位; W是氢，卤素，低级烷基，氰基或三氟甲基; andn是2-5; 其药学上可接受的盐。

5. 发明授权

US5962465A Aminomethyl-2,3,8,9-tetrahydro-7H-1,4-dioxino-�2,3-e!-indol-8-ones and derivatives 失效
标题翻译：氨基甲基-2,3,8,9-四氢-7H-1,4-二氧杂 - [2,3-e] - 吲哚-8-酮和衍生物
公开(公告)号：US5962465A
公开(公告)日：1999-10-05
申请号：US15149
申请日：1998-01-29
申请人： Gary P. Stack , Richard E. Mewshaw , Byron A. Bravo , Young H. Kang
发明人： Gary P. Stack , Richard E. Mewshaw , Byron A. Bravo , Young H. Kang
IPC分类号： A61K31/357 , A61K31/40 , A61K31/407 , A61K31/4439 , A61P25/00 , A61P25/16 , A61P25/18 , A61P43/00 , C07D209/60 , C07D405/14 , C07D409/14 , C07D491/04 , C07D491/056 , C07D491/113 , A61K31/47
CPC分类号： C07D491/04
摘要： The compounds of formula I: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, phenyl or benzyl; or R.sup.1 and R.sup.2, taken together, are benzylidene optionally substituted with R.sup.3 as defined below or alkylidene, or R.sup.1 and R.sup.2, taken together with the carbon to which they are attached, form a carbonyl moiety or a cycloalkyl group; R.sup.3 is hydrogen, hydroxy, halo, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, aralkoxy, alkanoyloxy, amino, mono- or di-alkylamino, alkanamido or alkanesulfonamido; R.sup.4 is hydrogen or alkyl; m is an integer 0, 1 or 2; n is an integer from 0 to 6, inclusive; Z is hydrogen, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, polycyclo-alkyl, phenyl optionally substituted with R.sup.3 as defined above, phenoxy optionally substituted with R.sup.3 as defined above, naphthyl optionally substituted with R.sup.3 as defined above or naphthyloxy optionally substituted with R.sup.3 as defined above, heteroaryl or heteroaryloxy, in which the heterocyclic ring of the heteroaryl or heteroaryloxy group is selected from thiophene, furan, pyridine, pyrazine, pyrimidine, indole, indazole, imidazole, chroman, coumarin, carbostyril, quinoline, benzisoxazole, benzoxazole, pyrazole, pyrrole, thiazole, oxazole, or isoxazole and the heterocyclic ring is optionally substituted by R.sup.3 as defined above; or a pharmaceutically acceptable salt thereof, are useful in treating disorders of the dopaminergic system.
摘要翻译：式I的化合物：其中R 1和R 2独立地是氢，烷基，苯基或苄基; 或者R 1和R 2一起是可以被如下定义的R 3取代的亚苄基或亚烷基，或者R 1和R 2与它们所连接的碳一起形成羰基部分或环烷基; R 3是氢，羟基，卤素，三氟甲基，三氟甲氧基，烷基，烷氧基，芳烷氧基，烷酰氧基，氨基，单 - 或二 - 烷基氨基，烷酰氨基或烷磺酰氨基; R4是氢或烷基; m是整数0,1或2; n为0〜6的整数，包括0和6; Z是氢，羟基，烷基，烯基，炔基，烷氧基，环烷基，多环烷基，任选被如上所定义的R 3取代的苯基，任选被如上所定义的R 3取代的苯氧基，任选被如上定义的R 3取代的萘基，其中杂芳基或杂芳氧基的杂环选自噻吩，呋喃，吡啶，吡嗪，嘧啶，吲哚，吲唑，咪唑，苯并二氢吡喃，香豆素，喹诺酮，喹啉，苯并异恶唑，苯并恶唑，吡唑，吡咯，噻唑，恶唑或异恶唑，杂环任选被如上定义的R 3取代; 或其药学上可接受的盐可用于治疗多巴胺能系统的病症。

6. 发明授权

US5684039A 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：US5684039A
公开(公告)日：1997-11-04
申请号：US684610
申请日：1996-07-19
申请人： Richard E. Mewshaw
发明人： Richard E. Mewshaw
IPC分类号： A61K31/353 , C07D311/58 , A61K31/35
CPC分类号： C07D311/58 , A61K31/353
摘要： Compounds of the formula: ##STR1## in which R is a straight or branched chain alkyl group of 1 to 6 carbon atoms, hydroxyalkyl of 1 to 6 carbon atoms or a cycloalkyl group of 3 to 8 carbon atoms; 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：其中R是1至6个碳原子的直链或支链烷基，1至6个碳原子的羟基烷基或3至8个碳原子的环烷基的下式的化合物：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，图雷特氏综合征，酒精成瘾，可卡因成瘾和对药物的成瘾。

7. 发明授权

US5401769A Dibenzofuranyl N-alkyl carbamates 失效
标题翻译：二苯并呋喃基N-烷基氨基甲酸酯
公开(公告)号：US5401769A
公开(公告)日：1995-03-28
申请号：US190402
申请日：1994-02-02
申请人： Thomas J. Commons , Richard E. Mewshaw , Donald P. Strike
发明人： Thomas J. Commons , Richard E. Mewshaw , Donald P. Strike
IPC分类号： C07D307/91 , A61K31/34
CPC分类号： C07D307/91
摘要： A compound of formula A: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, fluorine, chlorine, bromine, iodine, trifluoromethyl, cyano, nitro, alkyl, alkoxy, --CO.sub.2 H, alkylcarbonyl, alkylcarbonyloxy, alkoxycarbonyl, alkoxycarbonyloxy, mono or dialkylaminocarbonyl, or mono or dialkylaminocarbonyloxy; R.sup.3 is hydrogen or alkyl; R.sup.4 is alkyl, cycloalkylalkyl or phenylalkyl or substituted phenylalkyl, and the substituent on the benzene ring is alkyl, alkoxy, halo, nitro, cyano, trifluoromethyl or phenyl, are anti-cholesterolemic agents.
摘要翻译：式A的化合物：其中R 1和R 2独立地是氢，氟，氯，溴，碘，三氟甲基，氰基，硝基，烷基，烷氧基，-CO 2 H，烷基羰基，烷基羰基氧基，烷氧基羰基，或二烷基氨基羰基，或单或二烷基氨基羰基氧基; R3是氢或烷基; R4是烷基，环烷基烷基或苯基烷基或取代的苯基烷基，苯环上的取代基是烷基，烷氧基，卤素，硝基，氰基，三氟甲基或苯基，是抗胆固醇血症药。

8. 发明授权

US5250537A 5,6,7,8,9,10-hexahydro-7 ,10-iminocyclohept[b]indole,-6,7,8,9,10-hexahydro-7,11-imino-5H-cyclooct[ b]indole and substituted derivatives 失效
标题翻译： 5,6,7,8,9,10-六氢-7,10-亚氨基环辛烯，-6,7,8,9,10-六氢-7,11-亚氨基-5H-环辛烷并取代的衍生物
公开(公告)号：US5250537A
公开(公告)日：1993-10-05
申请号：US850761
申请日：1992-03-13
申请人： Richard E. Mewshaw , Carl Kaiser , Mary E. Abreu
发明人： Richard E. Mewshaw , Carl Kaiser , Mary E. Abreu
IPC分类号： C07D471/18 , A61K31/435 , C07D471/20
CPC分类号： C07D471/18
摘要： 5,6,7,8,9,10-Hexahydro-7,10-iminocyclohept[b]indole, 6,7,8,9,10,11-hexahydro-7,11-imino-5H-cyclooct[b]indole and substituted derivatives are effective in the treatment of psychoses with limited liability to produce concomitant adverse extrapyramidal symptoms. These compounds are also useful for treating other central nervous system and cardiovascular disorders.
摘要翻译： 5,6,7,8,9,10-六氢-7,10-亚氨基环庚三烯并[b]吲哚，6,7,8,9,10,11-六氢-7,11-亚氨基-5H-环辛[b] 吲哚和取代的衍生物在治疗精神病方面是有效的，有限责任以产生伴随的锥体外系症状。这些化合物也可用于治疗其他中枢神经系统和心血管疾病。

9. 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。

10. 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。

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