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1. 发明授权

US5436240A Heterocyclic amines having central nervous system activity 失效
标题翻译：具有中枢神经系统活性的杂环胺
公开(公告)号：US5436240A
公开(公告)日：1995-07-25
申请号：US132633
申请日：1993-10-06
申请人： Malcolm W. Moon , Richard F. Heier , Jeanette K. Morris
发明人： Malcolm W. Moon , Richard F. Heier , Jeanette K. Morris
IPC分类号： C07D215/40 , C07D455/04 , C07D471/06 , C07D498/06 , C07D513/06 , A61K31/50 , A61K31/495 , C07D471/12 , C07D513/12
CPC分类号： C07D471/06 , C07D215/40 , C07D455/04 , C07D513/06
摘要： Tricyclic nitrogen containing compounds, having central nervous system activity of the following structural formula: ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1, R.sub.2, and R.sub.3 are independently hydrogen, C.sub.1-6 alkyl, alkenyl, or alkynyl, C.sub.3-10 cycloalkyl, or R.sub.1 and R.sub.2 are joined to form a C.sub.3-7 cyclic amine which can contain additional heteroatoms; X is hydrogen, C.sub.1-6 alkyl, halogen, hydroxy, alkoxy, cyano, carboxamide, carboxyl, or carboalkoxyl; A is SO.sub.2, N, CH, CH.sub.2, CHCH.sub.3, C=O, C=S, C-SCH.sub.3, C=NH, C-NH.sub.2, C-NHCH.sub.3, CNHCOOCH.sub.3, or C-NHCN. B is CH.sub.2, CH, C=O, N, NH or N-CH.sub.3 ; n is 0 or 1; and D is CH, CH.sub.2, C=O, 0, N, NH or N-CH.sub.3. These new compounds are suitable for treating schizophrenia, Parkinson's disease, anxiety, depression or as compounds for lowering blood pressure in animal or human hosts.
摘要翻译：具有以下结构式的中枢神经系统活性的三环氮类化合物：其中R 1，R 2和R 3独立地是氢，C 1-6烷基，烯基或炔基，C 3-10环烷基，或R 1和R 2连接形成可含有其它杂原子的C 3-7环胺; X是氢，C 1-6烷基，卤素，羟基，烷氧基，氰基，羧酰胺，羧基或烷氧羰基; A是SO 2，N，CH，CH 2，CHCH 3，C = O，C = S，C-SCH 3，C = NH，C-NH 2，C-NHCH 3，CNHCOOCH 3或C-NHCN。 B是CH 2，CH，C = O，N，NH或N-CH 3; n为0或1; 且D为CH，CH 2，C = O，O，N，NH或N-CH 3。这些新化合物适用于治疗精神分裂症，帕金森病，焦虑症，抑郁症或作为降低动物或人类宿主血压的化合物。

2. 发明授权

US06903090B2 Substituted azepino[4,5b]indole derivatives 失效
标题翻译：取代的azepino [4,5b]吲哚衍生物
公开(公告)号：US06903090B2
公开(公告)日：2005-06-07
申请号：US10393968
申请日：2003-03-20
申请人： Kristine E. Frank , Brad A. Acker , Michael D. Ennis , Jed F. Fisher , Jian-min Fu , William W. McWhorter, Jr. , Jeanette K. Morris , Donald Joseph Rogier , Eric Jon Jacobsen
发明人： Kristine E. Frank , Brad A. Acker , Michael D. Ennis , Jed F. Fisher , Jian-min Fu , William W. McWhorter, Jr. , Jeanette K. Morris , Donald Joseph Rogier , Eric Jon Jacobsen
IPC分类号： A61K31/55 , A61P3/04 , A61P25/00 , A61P25/02 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D487/04 , G06T3/00
CPC分类号： C07D487/04
摘要： Disclosed are compounds of Formula (I): wherein R1-R4, p and q have any of the values described in the specification, as well as pharmaceutical salts thereof, and pharmaceutical compositions containing such compounds or salts. The compounds and salts are 5-HT ligands and are useful for treating diseases, disorders, and/or conditions in a mammal wherein activity of a 5-HT receptor is implicated. The compounds and salts are particularly useful for treating diseases of the central nervous system.
摘要翻译：公开了式（I）的化合物：其中R 1 -R 4，p和q具有说明书中描述的任何值，以及其药用盐，和含有这些化合物或盐的药物组合物。化合物和盐是5-HT配体，可用于治疗其中涉及5-HT受体的活性的哺乳动物的疾病，病症和/或病症。化合物和盐特别适用于治疗中枢神经系统疾病。

3. 发明授权

US5273975A Heterocyclic amines having central nervous system activity 失效
标题翻译：具有中枢神经系统活性的杂环胺
公开(公告)号：US5273975A
公开(公告)日：1993-12-28
申请号：US778204
申请日：1991-12-06
申请人： Malcolm W. Moon , Richard F. Heier , Jeanette K. Morris
发明人： Malcolm W. Moon , Richard F. Heier , Jeanette K. Morris
IPC分类号： C07D215/40 , C07D455/04 , C07D471/06 , C07D498/06 , C07D513/06 , A61K31/495 , A61K31/50 , C07D513/02
CPC分类号： C07D471/06 , C07D215/40 , C07D455/04 , C07D513/06
摘要： Tricyclic nitrogen containing compounds, having central nervous system activity of the following structural formula: ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1, R.sub.2, and R.sub.3 are independently hydrogen, C.sub.1-6 alkyl, alkenyl, or alkynyl, C.sub.3-10 cycloalkyl, or R.sub.1 and R.sub.2 are joined to form a C.sub.3-7 cyclic amine which can contain additional heteroatoms; X is hydrogen, C.sub.1-6 alkyl halogen, hydroxy, alkoxy, cyano, carboxamide, carboxyl, or carboalkoxyl; A is SO.sub.2, N, CH, CH.sub.2, CHCH.sub.3, C.dbd.O, C.dbd.S, C-SCH.sub.3, C.dbd.NH, C-NH.sub.2, C-NHCH.sub.3, C--NHCOOCH.sub.3, or C--NHCN. B is CH.sub.2, CH, C.dbd.O, N, NH or N--CH.sub.3 ; n is 0 or 1; and D is CH, CH.sub.2, C.dbd.O, O, N, NH or N--CH.sub.3. These new compounds are suitable for treating schizophrenia, Parkinson's disease, anxiety, depression or as compounds for lowering blood pressure in animal or human hosts.
摘要翻译： PCT No.PCT / US90 / 02621 Sec。 371 1991年12月6日第 102（e）1990年12月6日授权PCT 1990年5月15日提交PCT。具有以下结构式的中枢神经系统活性的三环氮化合物：其中R1，R2和R3独立地为氢，C 1-6烷基，烯基或炔基，C 3-10环烷基或R 1和R 2连接形成可含有其它杂原子的C 3-7环胺; X是氢，C 1-6烷基卤素，羟基，烷氧基，氰基，羧酰胺，羧基或烷氧羰基; A是SO 2，N，CH，CH 2，CHCH 3，C = O，C = S，C-SCH 3，C = NH，C-NH 2，C-NHCH 3，C-NHCOOCH 3或C-NHCN。 B是CH 2，CH，C = O，N，NH或N-CH 3; n为0或1; 且D为CH，CH 2，C = O，O，N，NH或N-CH 3。这些新化合物适用于治疗精神分裂症，帕金森病，焦虑症，抑郁症或作为降低动物或人类宿主血压的化合物。

4. 发明授权

US06828314B2 Substituted azepino[4,5b]indoline derivatives 失效
标题翻译：取代的azepino [4,5b]二氢吲哚衍生物
公开(公告)号：US06828314B2
公开(公告)日：2004-12-07
申请号：US10394676
申请日：2003-03-20
申请人： Kristine E. Frank , Brad A. Acker , Michael D. Ennis , Jed F. Fisher , Jian-min Fu , Eric Jon Jacobsen , William W. McWhorter, Jr. , Jeanette K. Morris , Donald Joseph Rogier
发明人： Kristine E. Frank , Brad A. Acker , Michael D. Ennis , Jed F. Fisher , Jian-min Fu , Eric Jon Jacobsen , William W. McWhorter, Jr. , Jeanette K. Morris , Donald Joseph Rogier
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： The invention provides compounds of Formula (I): wherein R1-R4, p and q have any of the values described in the specification, as well as pharmaceutical salts thereof, and pharmaceutical compositions containing such compounds or salts. The compounds and salts are 5-HT ligands and are useful for treating diseases, disorders, and/or conditions in a mammal wherein activity of a 5-HT receptor is implicated. The compounds and salts are particularly useful for treating diseases of the central nervous system.
摘要翻译：本发明提供式（I）化合物：其中R 1 -R 4，p和q具有说明书中描述的任何值，以及其药用盐，以及含有这些化合物或盐的药物组合物。化合物和盐是5-HT配体，可用于治疗其中涉及5-HT受体的活性的哺乳动物的疾病，病症和/或病症。化合物和盐特别适用于治疗中枢神经系统疾病。

5. 发明授权

US06586421B2 Substituted azepino[4,5b]indoline derivatives 失效
标题翻译：取代的azepino [4,5b]二氢吲哚衍生物
公开(公告)号：US06586421B2
公开(公告)日：2003-07-01
申请号：US09957319
申请日：2001-09-20
申请人： Kristine E. Frank , Brad A. Acker , Michael D. Ennis , Jed F. Fisher , Jian-min Fu , Eric Jon Jacobsen , William W. McWhorter, Jr. , Jeanette K. Morris , Donald Joseph Rogier
发明人： Kristine E. Frank , Brad A. Acker , Michael D. Ennis , Jed F. Fisher , Jian-min Fu , Eric Jon Jacobsen , William W. McWhorter, Jr. , Jeanette K. Morris , Donald Joseph Rogier
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： The invention provides compounds of Formula (I): wherein R1-R4, p and q have any of the values described in the specification, as well as pharmaceutical salts thereof, and pharmaceutical compositions containing such compounds or salts. The compounds and salts are 5-HT ligands and are useful for treating diseases, disorders, and/or conditions in a mammal wherein activity of a 5-HT receptor is implicated. The compounds and salts are particularly useful for treating diseases of the central nervous system.
摘要翻译：本发明提供式（I）化合物：其中R1-R4，p和q具有说明书中所述的任何值，以及其药用盐，以及含有这些化合物或盐的药物组合物。化合物和盐是5-HT配体，可用于治疗其中涉及5-HT受体的活性的哺乳动物的疾病，病症和/或病症。化合物和盐特别适用于治疗中枢神经系统疾病。

6. 发明授权

US06583135B2 Substituted azepino[4,5b]indole derivatives 失效
标题翻译：取代的azepino [4,5b]吲哚衍生物
公开(公告)号：US06583135B2
公开(公告)日：2003-06-24
申请号：US09957625
申请日：2001-09-20
申请人： Kristine E. Frank , Brad A. Acker , Michael D. Ennis , Jed F. Fisher , Jian-min Fu , William W. McWhorter, Jr. , Jeanette K. Morris , Donald Joseph Rogier , Eric Jon Jacobsen
发明人： Kristine E. Frank , Brad A. Acker , Michael D. Ennis , Jed F. Fisher , Jian-min Fu , William W. McWhorter, Jr. , Jeanette K. Morris , Donald Joseph Rogier , Eric Jon Jacobsen
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： Disclosed are compounds of Formula (I): wherein R1-R4, p and q have any of the values described in the specification, as well as pharmaceutical salts thereof, and pharmaceutical compositions containing such compounds or salts. The compounds and salts are 5-HT ligands and are useful for treating diseases, disorders, and/or conditions in a mammal wherein activity of a 5-HT receptor is implicated. The compounds and salts are particularly useful for treating diseases of the central nervous system.
摘要翻译：公开了式（I）的化合物：其中R1-R4，p和q具有说明书中描述的任何值，以及其药用盐，以及含有这些化合物或盐的药物组合物。化合物和盐是5-HT配体，可用于治疗其中涉及5-HT受体的活性的哺乳动物的疾病，病症和/或病症。化合物和盐特别适用于治疗中枢神经系统疾病。

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