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51. 发明授权

US06514976B2 Arylpiperazines having activity at the serotonin 1A receptor 失效
标题翻译：具有5-羟色胺1A受体活性的芳基哌嗪
公开(公告)号：US06514976B2
公开(公告)日：2003-02-04
申请号：US10136101
申请日：2002-04-30
申请人： Daniel Timothy Kohlman , Yao-Chang Xu
发明人： Daniel Timothy Kohlman , Yao-Chang Xu
IPC分类号： A61K31495
CPC分类号： C07D295/088 , A61K31/495 , A61K31/496 , C07C45/004 , C07C45/29 , C07C45/40 , C07C45/515 , C07C45/59 , C07C45/68 , C07C49/563 , C07C49/577 , C07C49/583 , C07C49/86 , C07D213/74 , C07D295/104 , C07D295/108
摘要： Described herein is a compound of the formula wherein Ar′ is a mono or bicyclic aromatic or heteroaromatic radical substituted with one to three substituents selected from the group consisting of hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; R1 is hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio; R2 is phenyl, naphthyl or (C3-C12)cycloalkyl substituted with one or two substituents selected from the group consisting of hydrogen (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; R3 is selected from the group consisting of hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; X is —(C═O)—; or a pharmaceutically acceptable salt racemate, optical isomer or solvate thereof.
摘要翻译：本文描述的是一种化合物，其中Ar'是被一个或三个选自氢，（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷氧基，）（C 2 -C 6）烷基卤代，（C 3 -C 8）环烷基，（C 3 -C 8）环烯基或卤素; R 1是氢，（C 1 -C 6）烷基，（C1-C6）烷氧基，（C1-C6）烷硫基; R2是苯基，萘基或被一个或两个选自氢（C1-C6）烷基，（C1- C6烷氧基，（C1-C6）烷硫基，（C2-C6）烯基，（C2-C6）炔基，（C1-C6）烷基卤，（C3-C8）环烷基，（C3-C8）环烯基或卤素; R3是选自氢，（C1-C6）烷基，（C1-C6）烷氧基，（C1-C6）烷硫基，（C2-C6）烯基，（C2-C6）炔基，（C1-C6）烷基卤素，（C 3 -C 8）环烷基，（C 3 -C 8）环烯基或卤素; X是 - （C = O） - ;或其药学上可接受的外消旋盐，旋光异构体或溶剂化物。

52. 发明授权

US06355674B1 Aminotetralins as 5-HT1D &agr; Agonists 失效
标题翻译：氨基丝氨酸作为5-HT1Dα激动剂
公开(公告)号：US06355674B1
公开(公告)日：2002-03-12
申请号：US09403854
申请日：2000-05-02
申请人： John M Schaus , Clint D Walker , Yao-Chang Xu
发明人： John M Schaus , Clint D Walker , Yao-Chang Xu
IPC分类号： C07C21142
CPC分类号： C07D307/14 , C07C211/42 , C07C215/42 , C07C217/52 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07D309/04
摘要： A class of novel aminotetralins is disclosed useful as 5-HT1D&agr; agonists.
摘要翻译：一类新的氨基喋呤被公开用作5-HT1Dα激动剂

53. 发明授权

US06353008B1 Pyrrolidine and pyrroline derivatives having effects on serotonin related systems 失效
标题翻译：吡咯烷和吡咯啉衍生物对5-羟色胺相关系统有影响
公开(公告)号：US06353008B1
公开(公告)日：2002-03-05
申请号：US09701361
申请日：2000-11-28
申请人： Larry Wayne Hertel , Yao-Chang Xu
发明人： Larry Wayne Hertel , Yao-Chang Xu
IPC分类号： A61K3144
CPC分类号： C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： The present invention provides the compounds of the following formula (I): and a method for inhibiting the reuptake of seretonin, antagonizing the 5-HT1A receptor and antagonizing the 5-HT2A receptor which comprises administering to a subject in need of such treatment an effective amount of formula (I).
摘要翻译：本发明提供了下述式（I）的化合物和抑制依那普利钠的再摄取，拮抗5-HT 1A受体和拮抗5-HT 2A受体的方法，其包括向需要这种治疗的受试者施用有效的式（I）的量。

54. 发明授权

US5846982A Inhibition of serotonin reuptake 失效
公开(公告)号：US5846982A
公开(公告)日：1998-12-08
申请号：US862208
申请日：1997-05-22
申请人： James E. Audia , Daniel J. Koch , Thomas E. Mabry , Jeffrey S. Nissen , Vincent P. Rocco , Yao-Chang Xu
发明人： James E. Audia , Daniel J. Koch , Thomas E. Mabry , Jeffrey S. Nissen , Vincent P. Rocco , Yao-Chang Xu
IPC分类号： A61K31/00 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61P25/04 , A61P43/00 , C07D211/68 , C07D333/58 , C07D401/04 , C07D401/14 , C07D409/04 , C07D409/14 , C07D417/14 , A61K31/43
CPC分类号： C07D401/04 , C07D401/14 , C07D409/04 , C07D409/14 , C07D417/14
摘要： This invention provides compounds and a method for the inhibition of serotonin reuptake in mammals.

55. 发明授权

US5814653A Pharmaceutical method using 6-substituted-1, 2, 3, 4-tetrahydro-9H-carbazoles and 7-substituted-10H -cyclohepta (7, 6-B) indoles 失效
标题翻译：使用6-取代-1,2,3,4-四氢-9H-咔唑和7-取代-10H-环庚三烯（7,6-B）吲哚的药物方法
公开(公告)号：US5814653A
公开(公告)日：1998-09-29
申请号：US992320
申请日：1997-12-17
申请人： Michael Edward Flaugh , Anton Daniel Kiefer, Jr. , Clint Duane Walker , Yao-Chang Xu
发明人： Michael Edward Flaugh , Anton Daniel Kiefer, Jr. , Clint Duane Walker , Yao-Chang Xu
IPC分类号： C07D209/88 , C07D209/94 , A61K31/40
CPC分类号： C07D209/94 , C07D209/88
摘要： This invention provides novel 6-substituted-1,2,3,4-tetrahydro-9H-carbazoles and 7-substituted-10H-cyclohepta�7,6-b!indoles. These compounds are 5-HT.sub.1F agonists which are useful for the treatment of migraine and associated disorders.
摘要翻译：本发明提供新的6-取代-1,2,3,4-四氢-9H-咔唑和7-取代-10H-环庚三烯并[7,6-b]吲哚。这些化合物是可用于治疗偏头痛和相关疾病的5-HT1F激动剂。

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