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1. 发明授权

US06326381B1 Arylpiperidine and aryl-1,2,5,6-tetrahydropyidine amide derivates 失效
标题翻译：芳基哌啶和芳基-1,2,5,6-四氢吡啶酰胺衍生物
公开(公告)号：US06326381B1
公开(公告)日：2001-12-04
申请号：US09459801
申请日：1999-12-13
申请人： Michael G. Kelly , Gan Zhang , Yvette L. Palmer , Wayne E. Childers
发明人： Michael G. Kelly , Gan Zhang , Yvette L. Palmer , Wayne E. Childers
IPC分类号： C07D40106
CPC分类号： C07D401/06 , C07D211/22
摘要： Compounds of the formula wherein R1, R2, R3, R4, X and n are defined in the specification, are useful for the treatment of anxiety, depression and related CNS disorders, and other related conditions such as the treatment of alcohol and drug withdrawal, sexual dysfunction and Alzheimer's disease.
摘要翻译：化学式R 1，R 2，R 3，R 4，X和n的化合物在本说明书中定义，可用于治疗焦虑，抑郁和相关的中枢神经系统疾病以及其他相关病症，例如治疗酒精和药物戒断，性功能障碍和阿尔茨海默病。

2. 发明授权

US06503928B2 Arylpiperidine and aryl-1,2,5,6-tetrahydropyridine amide derivatives 失效
标题翻译：芳基哌啶和芳基-1,2,5,6-四氢吡啶酰胺衍生物
公开(公告)号：US06503928B2
公开(公告)日：2003-01-07
申请号：US09954784
申请日：2001-09-18
申请人： Michael G. Kelly , Gan Zhang , Yvette L. Palmer , Wayne E. Childers
发明人： Michael G. Kelly , Gan Zhang , Yvette L. Palmer , Wayne E. Childers
IPC分类号： C07D40106
CPC分类号： C07D401/06 , C07D211/22
摘要： Compounds of the formula wherein R1, R2, R3, R4, X and n are defined in the specification, are useful for the treatment of anxiety, depression and related CNS disorders, and other related conditions such as the treatment of alcohol and drug withdrawal, sexual dysfunction and Alzheimer's disease.
摘要翻译：化学式R 1，R 2，R 3，R 4，X和n的化合物在本说明书中定义，可用于治疗焦虑，抑郁和相关的中枢神经系统疾病以及其他相关病症，例如治疗酒精和药物戒断，性功能障碍和阿尔茨海默病。

3. 发明授权

US06306859B1 N-substituted imide derivatives with serotonergic activity 失效
标题翻译：具有5-羟色胺能活性的N-取代酰亚胺衍生物
公开(公告)号：US06306859B1
公开(公告)日：2001-10-23
申请号：US09516137
申请日：2000-03-01
申请人： Wayne E. Childers , Michael G. Kelly , Gan Zhang , Yvette L. Palmer , Edward J. Podlesny
发明人： Wayne E. Childers , Michael G. Kelly , Gan Zhang , Yvette L. Palmer , Edward J. Podlesny
IPC分类号： A61K31495
CPC分类号： C07D295/185 , C07D295/13 , C07D403/10
摘要： Compounds of the Formula (I) wherein R2, Y, X and n are as defined in the specification which compounds are useful in the treatment of disorders associated with serotonergic neuron-related diseases.
摘要翻译：式（I）的化合物，其中R2，Y，X和n如本说明书中所定义，该化合物可用于治疗与5-羟色胺能神经元相关疾病相关的病症。

4. 发明授权

US06518272B2 Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents 失效
标题翻译：环烷基取代的芳基哌嗪，哌啶和四氢吡啶作为血清素能药
公开(公告)号：US06518272B2
公开(公告)日：2003-02-11
申请号：US10107866
申请日：2002-03-27
申请人： Wayne E. Childers , Michael G. Kelly , Yvette L. Palmer , Edward J. Podlesny
发明人： Wayne E. Childers , Michael G. Kelly , Yvette L. Palmer , Edward J. Podlesny
IPC分类号： A61K3150
CPC分类号： C07D239/42 , C07D209/08 , C07D211/22 , C07D213/74 , C07D217/22 , C07D277/82 , C07D295/125 , C07D295/13 , C07D319/20
摘要： This invention relates to compounds which have activity as 5-HT1A agonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer, having the formula wherein: X is a moiety selected from the group of: n is selected from the integers 1 through 5; R1 is optionally substituted aryl or mono or bicyclic heteroaryl, with a proviso that heteroaryl is not thiadiazole; R2 is H or alkyl; R3 is H, COR5, COOR5, and CONR5R6; R4 is H, alkyl, alkenyl, alkynyl, aryl, mono or bicyclic heteroaryl, aralkyl, and mono or bicyclic heteroaralkyl, wherein the aryl or heteroaryl groups are optionally substituted; R5 and R6 are H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, adamantyl, and noradamantyl or R5 and R6 taken together may form a 5-7 membered azacyclic ring, optionally containing an additional heteroatom selected from O, S, or NR4; when R5 or R6 are chosen from cycloalkyl or cycloalkenyl, the cyclic group may optionally be substituted at the 1-position with a C1-C3 alkyl group; or an optical isomer; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及具有作为5-HT 1A激动剂和拮抗剂的活性的化合物，其可用于治疗具有下列基团的焦虑，抑郁，认知缺陷和前列腺癌：X是选自以下的部分：n是从整数1到5中选择; R 1是任选取代的芳基或单或双环杂芳基，条件是杂芳基不是噻二唑; R2是H或烷基; R3是H，COR5，COOR5和CONR5R6; R 4是H，烷基，烯基，炔基，芳基，单或双环杂芳基，芳烷基和单或双环杂芳烷基，其中芳基或杂芳基任选被取代; R5和R6是H，烷基，烯基，炔基，环烷基，环烯基，金刚烷基和去月桂烷基或R5和R6一起可以形成5-7元的氮杂环，任选地含有选自O，S或NR4的另外的杂原子; 当R5或R6选自环烷基或环烯基时，环状基团可以任选在1-位被C1-C3烷基取代;或光学异构体; 或其药学上可接受的盐。

5. 发明授权

US06376494B1 Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents 失效
标题翻译：环烷基取代的芳基哌嗪，哌啶和四氢吡啶作为血清素能药
公开(公告)号：US06376494B1
公开(公告)日：2002-04-23
申请号：US09723478
申请日：2000-11-28
申请人： Wayne E. Childers , Michael G. Kelly , Yvette L. Palmer , Edward J. Podlesny
发明人： Wayne E. Childers , Michael G. Kelly , Yvette L. Palmer , Edward J. Podlesny
IPC分类号： A61K31496
CPC分类号： C07D239/42 , C07D209/08 , C07D211/22 , C07D213/74 , C07D217/22 , C07D277/82 , C07D295/125 , C07D295/13 , C07D319/20
摘要： This invention relates to compounds which have activity as 5-HT1A agonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer, having the formula wherein: X is a moiety selected from the group of: n is selected from the integers 1 through 5; R1 is optionally substituted aryl or mono or bicyclic heteroaryl, with a proviso that heteroaryl is not thiadiazole; R2 is H or alkyl; R3 is H, COR5, COOR5, and CONR5R6; R4 is H, alkyl, alkenyl, alkynyl, aryl, mono or bicyclic heteroaryl, aralkyl, and mono or bicyclic heteroaralkyl, wherein the aryl or heteroaryl groups are optionally substituted; R5 and R6 are H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, adamantyl, and noradamantyl or R5 and R6 taken together may form a 5-7 membered azacyclic ring, optionally containing an additional heteroatom selected from O, S, or NR4; when R5 or R6 are chosen from cycloalkyl or cycloalkenyl, the cyclic group may optionally be substituted at the 1-position with a C1-C3 alkyl group; or an optical isomer; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及具有作为5-HT 1A激动剂和拮抗剂的活性的化合物，其可用于治疗具有下列基团的焦虑，抑郁，认知缺陷和前列腺癌：X是选自以下的部分：n是从整数1到5中选择; R1是任选取代的芳基或单或双环杂芳基，条件是杂芳基不是噻二唑; R2是H或烷基; R3是H，COR5，COOR5和CONR5R6; R 4是H，烷基，烯基，炔基，芳基，单或双环杂芳基，芳烷基和单或双环杂芳烷基，其中芳基或杂芳基任选被取代; R5和R6是H，烷基，烯基，炔基，环烷基，环烯基，金刚烷基和去月桂烷基或R5和R6一起可以形成5-7元的氮杂环，任选地含有选自O，S或NR4的另外的杂原子; 当R5或R6选自环烷基或环烯基时，环状基团可以任选在1-位被C1-C3烷基取代;或光学异构体; 或其药学上可接受的盐。

6. 发明授权

US07049330B2 Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents 失效
标题翻译：环烷基取代的芳基哌嗪，哌啶和四氢吡啶作为血清素能药
公开(公告)号：US07049330B2
公开(公告)日：2006-05-23
申请号：US10340087
申请日：2003-01-10
申请人： Wayne E. Childers , Michael G. Kelly , Yvette L. Palmer , Edward J. Podlesny
发明人： Wayne E. Childers , Michael G. Kelly , Yvette L. Palmer , Edward J. Podlesny
IPC分类号： A61K31/445 , C07D211/26
CPC分类号： C07D239/42 , C07D209/08 , C07D211/22 , C07D213/74 , C07D217/22 , C07D277/82 , C07D295/125 , C07D295/13 , C07D319/20
摘要： This invention relates to compounds which have activity as 5-HT1A agonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer, having the formula wherein: X is a moiety selected from the group of: n is selected from the integers 1 through 5; R1 is optionally substituted aryl or mono or bicyclic heteroaryl, with a proviso that heteroaryl is not thiadiazole; R2 is H or alkyl; R3 is H, COR5, COOR5, and CONR5R6; R4 is H, alkyl, alkenyl, alkynyl, aryl, mono or bicyclic heteroaryl, aralkyl, and mono or bicyclic heteroaralkyl, wherein the aryl or heteroaryl groups are optionally substituted; R5 and R6 are H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, adamantyl, and noradamantyl or R5 and R6 taken together may form a 5–7 membered azacyclic ring, optionally containing an additional heteroatom selected from O, S, or NR4; when R5 or R6 are chosen from cycloalkyl or cycloalkenyl, the cyclic group may optionally be substituted at the 1-position with a C1–C3 alkyl group; or an optical isomer; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及具有下式的化合物，其具有作为5-HT 1A激动剂和拮抗剂的活性，其可用于治疗焦虑，抑郁，认知缺陷和前列腺癌，其中：X为选自以下的基团：n选自整数1至5; R 1是任选取代的芳基或单或双环杂芳基，条件是杂芳基不是噻二唑; R 2是H或烷基; R 3是H，COR 5，COOR 5和CONR 5 R 6 O / >; R 4是H，烷基，烯基，炔基，芳基，单或双环杂芳基，芳烷基和单或双环杂芳烷基，其中芳基或杂芳基任选被取代; R 5和R 6是H，烷基，烯基，炔基，环烷基，环烯基，金刚烷基和去月桂外基或R 5和R 共同组合可以形成5-7元的氮杂环，任选地含有选自O，S或NR 4的另外的杂原子。当R 5或R 6选自环烷基或环烯基时，环状基团可以任选地在1位被C 1〜 -C 3烷基; 或光学异构体; 或其药学上可接受的盐。

7. 发明授权

US06239134B1 Diazole derivatives as serotonergic agents 失效
标题翻译：二唑衍生物作为血清素能药剂
公开(公告)号：US06239134B1
公开(公告)日：2001-05-29
申请号：US09515049
申请日：2000-02-25
申请人： Annmarie L. Sabb , Robert L. Vogel , Michael G. Kelly , Yvette L. Palmer , Wayne E. Childers
发明人： Annmarie L. Sabb , Robert L. Vogel , Michael G. Kelly , Yvette L. Palmer , Wayne E. Childers
IPC分类号： A61K31496
CPC分类号： C07D285/10 , C07D417/12
摘要： The present invention provides compounds of the general formula (1): wherein: two atoms of X, Y, or Z are nitrogen and the third atom is sulfur or oxygen; R is H, halogen, OH, SH, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, phenoxy, thiophenoxy, phenyl or substituted phenyl; A is C, CH, or N; R1 is aryl, heteroaryl, or cycloalkyl groups, optionally substituted by from 1 to 3 substituents selected from C1-C6 alkyl, C1-C6 alkoxy; CF3, Cl, Br, F, CN, or CO2CH3; R2is H or alkyl R3 is C1-C6 alkyl, optionally substituted aryl, optionally substituted 5- or 6-membered heteroaryl, C3 to C8 cycloalkyl optionally substituted by C1-C6 alkyl, or a 3 to 8-membered heterocyclic ring containing one or more heteroatoms selected from O, S or N; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods of treating central nervous system disorders using these compounds.
摘要翻译：本发明提供通式（1）的化合物：其中X，Y或Z的两个原子是氮，第三个原子是硫或氧; R是H，卤素，OH，SH，C 1 -C 6烷基， C 1 -C 6烷氧基，C 1 -C 6硫代烷基，苯氧基，硫代苯氧基，苯基或取代的苯基; A是C，CH或N; R 1是芳基，杂芳基或环烷基，任选地被1至3个选自C1- C6烷基，C1-C6烷氧基; CF 3，Cl，Br，F，CN或CO 2 CH 3; R 2为H或烷基R 3为C 1 -C 6烷基，任选取代的芳基，任选取代的5或6元杂芳基，任选被C 1 -C 6烷基取代的C 3至C 8环烷基，含有一个或多个选自O，S或N的杂原子的3至8元杂环; 或其药学上可接受的盐，以及使用这些化合物治疗中枢神经系统疾病的药物组合物和方法。

8. 发明授权

US07179813B2 Bicyclic indolyl derivatives and methods for their use as serotonergic agents 失效
标题翻译：双环吲哚基衍生物及其用作5-羟色胺能药剂的方法
公开(公告)号：US07179813B2
公开(公告)日：2007-02-20
申请号：US10864698
申请日：2004-06-09
申请人： Michael G. Kelly , Wayne E. Childers , Boyd L. Harrison , Gan Zhang , Byron A. Bravo , Lee E. Schechter
发明人： Michael G. Kelly , Wayne E. Childers , Boyd L. Harrison , Gan Zhang , Byron A. Bravo , Lee E. Schechter
IPC分类号： A61K31/496 , C07D401/14
CPC分类号： C07D401/12
摘要： Bicyclic indolyl derivatives and compositions containing such compounds are disclosed. Methods of using the bicyclic indolyl derivatives and compositions containing such composition as serotonergic agents, such as in the treatment of depression and anxiety, are also disclosed. In addition, processes for the preparation of bicyclic indolyl derivatives are disclosed.
摘要翻译：公开了双环吲哚基衍生物和含有这些化合物的组合物。还公开了使用双环吲哚基衍生物的方法和含有这样的组合物的组合物作为血清素能剂，例如治疗抑郁症和焦虑症的方法。此外，公开了制备双环吲哚基衍生物的方法。

9. 发明申请

US20090215794A1 SEROTONERGIC AGENTS 失效
标题翻译： SEROTONERGIC代理
公开(公告)号：US20090215794A1
公开(公告)日：2009-08-27
申请号：US12435862
申请日：2009-05-05
申请人： Wayne E. Childers , Michael G. Kelly , Sharon J. Rosenzweig-Lipson
发明人： Wayne E. Childers , Michael G. Kelly , Sharon J. 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。

10. 发明授权

US06469007B2 Serotonergic agents 失效
标题翻译：血清素能药物
公开(公告)号：US06469007B2
公开(公告)日：2002-10-22
申请号：US10010575
申请日：2001-11-13
申请人： Wayne E. Childers , Michael G. Kelly , Sharon J. Rosenzweig-Lipson
发明人： Wayne E. Childers , Michael G. Kelly , Sharon J. Rosenzweig-Lipson
IPC分类号： A61K31496
CPC分类号： C07D405/12
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：提供了新颖的哌嗪衍生物，其具有R 1为氰基，硝基，三氟甲基或卤素的化学式，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。

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