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1. 发明授权

US5656625A Nitrogen-containing cyclohetero cycloheteroaminoaryl derivatives for CNS disorders 失效
标题翻译：用于CNS疾病的含氮环杂环芳基氨基芳基衍生物
公开(公告)号：US5656625A
公开(公告)日：1997-08-12
申请号：US442867
申请日：1995-05-17
申请人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
发明人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
IPC分类号： C07D207/14 , C07D211/56 , C07D223/12 , C07D409/06 , C07D403/04 , A61K31/55 , C07D413/04 , C07D417/04
CPC分类号： C07D409/06 , C07D207/14 , C07D211/56 , C07D223/12
摘要： Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl;wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
摘要翻译：描述某些含氮环杂环烷基氨基芳基化合物用于治疗中枢神经系统疾病如脑缺血，精神病和抽搐。特别感兴趣的化合物具有下式：其中R 1，R 4，R 5，R 6和R 7各自独立地选自氢，低级烷基，苄基和卤代低级烷基; 其中R2，R3和R8至R11各自独立地选自氢，羟基，低级烷基，苄基，苯氧基，苄氧基和卤代低级烷基; 其中n为4-6的整数; 其中m是2至4的整数; 其中A选自苯基，萘基，苯并噻吩基，苯并呋喃基和噻吩基; 其中前述A基团中的任一个可以进一步被一个或多个独立地选自氢，羟基，低级烷基，低级烷氧基，卤素，卤代低级烷基，氨基，单低级烷基氨基和二低级烷基氨基的取代基取代。或其药学上可接受的盐。

2. 发明授权

US5856318A Nitrogen-containing cyclohetero cyclo-heteroaminoaryl derivatives for CNS disorders 失效
标题翻译：用于CNS疾病的含氮环杂环芳基芳基衍生物
公开(公告)号：US5856318A
公开(公告)日：1999-01-05
申请号：US910302
申请日：1997-08-11
申请人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
发明人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
IPC分类号： C07D207/14 , C07D211/56 , C07D223/12 , C07D409/06 , A61K31/33 , A61K31/55 , C07D295/00 , C07D405/00
CPC分类号： C07D409/06 , C07D207/14 , C07D211/56 , C07D223/12
摘要： Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl;wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
摘要翻译：描述某些含氮环杂环烷基氨基芳基化合物用于治疗中枢神经系统疾病如脑缺血，精神病和抽搐。特别感兴趣的化合物具有下式：其中R 1，R 4，R 5，R 6和R 7各自独立地选自氢，低级烷基，苄基和卤代低级烷基; 其中R2，R3和R8至R11各自独立地选自氢，羟基，低级烷基，苄基，苯氧基，苄氧基和卤代低级烷基; 其中n为4-6的整数; 其中m是2至4的整数; 其中A选自苯基，萘基，苯并噻吩基，苯并呋喃基和噻吩基; 其中前述A基团中的任一个可以进一步被一个或多个独立地选自氢，羟基，低级烷基，低级烷氧基，卤素，卤代低级烷基，氨基，单低级烷基氨基和二低级烷基氨基的取代基取代。或其药学上可接受的盐。

3. 发明授权

US5679679A Aralkyl diazabicycloalkane derivatives for CNS disorders 失效
标题翻译：用于CNS病症的芳烷基二氮杂双环烷烃衍生物
公开(公告)号：US5679679A
公开(公告)日：1997-10-21
申请号：US348654
申请日：1994-12-02
申请人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
发明人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
IPC分类号： A61K31/495 , C07D471/04 , C07D487/04 , C07D31/495 , C07D31/55
CPC分类号： C07D471/04 , A61K31/495 , C07D487/04
摘要： Certain aralkyl diazabicyloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein: each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from the group consisting of hydrido, loweralkyl, benzyl and haloloweralkyl; each of R.sup.2, R.sup.3, and R.sup.8 through R.sup.11 is independently selected from the group consisting of hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; n is an integer of from three to four; m is an integer of two; A is selected from the group consisting of phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl and wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from the group consisting of hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
摘要翻译：描述了某些芳烷基二氮杂双环烷基化合物用于治疗中枢神经系统疾病如脑缺血，精神病和抽搐。特别感兴趣的化合物具有下式：其中：R 1，R 4，R 5，R 6和R 7各自独立地选自氢，低级烷基，苄基和卤代低级烷基; R 2，R 3和R 8至R 11各自独立地选自氢，羟基，低级烷基，苄基，苯氧基，苄氧基和卤代低级烷基; n是3至4的整数; m是2的整数; A选自苯基，萘基，苯并噻吩基，苯并呋喃基和噻吩基，其中任何前述A基团可以进一步被一个或多个独立地选自羟基，羟基，低级烷基，低级烷氧基，卤代，卤代低级烷基，氨基，单低级烷基氨基和二低级烷基氨基; 或其药学上可接受的盐。

4. 发明授权

US5679673A Aralkyl bridged diazabicycloalkane derivatives for CNS disorders 失效
标题翻译：用于CNS病症的芳烷基桥连二氮杂双环烷烃衍生物
公开(公告)号：US5679673A
公开(公告)日：1997-10-21
申请号：US344304
申请日：1994-11-21
申请人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
发明人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
IPC分类号： C07D453/02 , C07D487/08 , A61K31/55 , C07D471/08
CPC分类号： C07D487/08 , C07D453/02
摘要： Certain aralkyl diazabicycloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R, R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower-alkyl, benzyl, and haloloweralkyl; wherein each of R.sup.2, R.sup.3 and R.sup.10 through R.sup.13 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein each of R.sup.8 and R.sup.9 is selected from hydrido, loweralkyl, benzyl and haloloweralkyl; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothiophenyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
摘要翻译：描述了某些芳烷基二氮杂双环烷基化合物用于治疗中枢神经系统疾病如脑缺血，精神病和抽搐。特别感兴趣的化合物具有下式：其中R，R 1，R 4，R 5，R 6和R 7各自独立地选自氢，低级烷基，苄基和卤代低级烷基; 其中R2，R3和R10至R13各自独立地选自氢，羟基，低级烷基，苄基，苯氧基，苄氧基和卤代低级烷基; 其中R8和R9各自选自氢，低级烷基，苄基和卤代低级烷基; 其中m是2至4的整数; 其中A选自苯基，萘基，苯并噻吩基，苯并呋喃基和噻吩基; 其中前述A基团中的任一个可以进一步被一个或多个独立地选自氢，羟基，低级烷基，低级烷氧基，卤素，卤代低级烷基，氨基，单低级烷基氨基和二低级烷基氨基的取代基取代。或其药学上可接受的盐。

5. 发明授权

US5346908A Nitrogen-containing cyclohetero cycloheteroaminoaryl derivatives for CNS disorders 失效
标题翻译：用于CNS疾病的含氮环杂环芳基氨基芳基衍生物
公开(公告)号：US5346908A
公开(公告)日：1994-09-13
申请号：US904354
申请日：1992-06-25
申请人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
发明人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
IPC分类号： C07D207/14 , C07D211/56 , C07D223/12 , C07D409/06 , A61K31/55 , A61K31/40 , A61K31/445 , C07D211/08
CPC分类号： C07D409/06 , C07D207/14 , C07D211/56 , C07D223/12
摘要： Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl; wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
摘要翻译：描述某些含氮环杂环烷基氨基芳基化合物用于治疗中枢神经系统疾病如脑缺血，精神病和抽搐。特别感兴趣的化合物具有下式：其中R 1，R 4，R 5，R 6和R 7各自独立地选自氢，低级烷基，苄基和卤代低级烷基; 其中R2，R3和R8至R11各自独立地选自氢，羟基，低级烷基，苄基，苯氧基，苄氧基和卤代低级烷基; 其中n为4-6的整数; 其中m是2至4的整数; 其中A选自苯基，萘基，苯并噻吩基，苯并呋喃基和噻吩基; 其中前述A基团中的任一个可以进一步被一个或多个独立地选自氢，羟基，低级烷基，低级烷氧基，卤素，卤代低级烷基，氨基，单低级烷基氨基和二低级烷基氨基的取代基取代。或其药学上可接受的盐。

6. 发明授权

US06310064B1 Aralkyl diazabicycloalkane derivatives for CNS disorders 失效
标题翻译：用于CNS病症的芳烷基二氮杂双环烷烃衍生物
公开(公告)号：US06310064B1
公开(公告)日：2001-10-30
申请号：US09347659
申请日：1999-07-06
申请人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
发明人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
IPC分类号： C07D47104
CPC分类号： C07D471/04 , A61K31/495 , C07D487/04
摘要： Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis, and convulsions. For example, compounds of interest are of the formula:
摘要翻译：公开了某些芳烷基二氮杂双环烷基化合物用于治疗中枢神经系统疾病，例如脑缺血，精神病和抽搐。例如，感兴趣的化合物具有下式：

7. 发明授权

US5958920A Aralkyl diazabicycloalkane derivatives for CNS disorders 失效
标题翻译：用于CNS病症的芳烷基二氮杂双环烷烃衍生物
公开(公告)号：US5958920A
公开(公告)日：1999-09-28
申请号：US954284
申请日：1997-10-20
申请人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
发明人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
IPC分类号： A61K31/495 , C07D471/04 , C07D487/04 , C07D31/495 , C07D31/55
CPC分类号： C07D471/04 , A61K31/495 , C07D487/04
摘要： Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein m is three or four; wherein z is selected from the group consisting of ##STR2## wherein when Z is ##STR3## n and p are integers of from one to four, with a sum of four or five, and when Z is ##STR4## n and p are integers of from one to three, with a sum of three or four; wherein A is selected from the group consisting of aryl, heteroaryl, aryloxy, heteroaryloxy, aralkoxy, heteroaralkoxy, arylamino, heteroarylamino, aralkylamino, heteroaralkylamino, arylthio, heteroarylthio, aralkylthio, and heteroaralkylthio; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from the group consisting of hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, aralkyl, aryl, alkoxy, aryloxy, aralkoxy, alkoxyalkyl, halo, haloalkyl, hydroxyalkyl, cyano, amino, monoalkylamino, dialkylamino, carboxy, carboxyalkyl, alkanoyl, alkenyl and alkynyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：公开了某些芳烷基二氮杂双环烷基化合物用于治疗中枢神经系统疾病，如脑缺血，精神病和抽搐。特别感兴趣的化合物具有下式：其中m为三或四; 其中z选自其中当Z为n且p为1至4的整数时，其总数为4或5，当Z为n且p为1至3的整数时，其总和为三或四; 其中A选自芳基，杂芳基，芳氧基，杂芳氧基，芳烷氧基，杂芳烷氧基，芳基氨基，杂芳基氨基，芳烷基氨基，杂芳烷基氨基，芳硫基，杂芳硫基，芳烷硫基和杂芳烷硫基。其中前述A基团中的任一个可以进一步被一个或多个独立地选自羟基，羟基，烷基，环烷基，环烷基烷基，芳烷基，芳基，烷氧基，芳氧基，芳烷氧基，烷氧基烷基，卤素，卤代烷基，，氰基，氨基，单烷基氨基，二烷基氨基，羧基，羧基烷基，烷酰基，烯基和炔基; 或其药学上可接受的盐。

8. 发明授权

US06656930B2 Aralkyl diazabicycloalkane derivatives for CNS disorders 失效
标题翻译：用于CNS病症的芳烷基二氮杂双环烷烃衍生物
公开(公告)号：US06656930B2
公开(公告)日：2003-12-02
申请号：US09946284
申请日：2001-09-04
申请人： Wayne D Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
发明人： Wayne D Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
IPC分类号： C07D48704
CPC分类号： C07D471/04 , A61K31/495 , C07D487/04
摘要： Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis, and convulsions. For example, compounds of interest are of the formula:
摘要翻译：公开了某些芳烷基二氮杂双环烷基化合物用于治疗中枢神经系统疾病，例如脑缺血，精神病和抽搐。例如，感兴趣的化合物具有下式：

9. 发明授权

US5571832A Nitrogen-containing cyclohetero alkylamino aryl derivatives for CNS disorders 失效
标题翻译：用于CNS障碍的含氮环杂烷基氨基芳基衍生物
公开(公告)号：US5571832A
公开(公告)日：1996-11-05
申请号：US261796
申请日：1994-06-20
申请人： Brian R. de Costa , Wayne D. Bowen , Xiao-Shu He , Lilian Radesca , Kenner C. Rice
发明人： Brian R. de Costa , Wayne D. Bowen , Xiao-Shu He , Lilian Radesca , Kenner C. Rice
IPC分类号： C07D207/09 , C07D211/22 , C07D211/26 , C07D211/42 , C07D211/56 , C07D211/60 , A61K31/40 , C07D207/08 , C07D207/12 , C07D207/46
CPC分类号： C07D211/22 , C07D207/09 , C07D211/26 , C07D211/42 , C07D211/56 , C07D211/60
摘要： Compounds comprising a pyrrolidinyl ring are disclosed for use in the treatment of cerebral ischemia.
摘要翻译：公开了包含吡咯烷基环的化合物用于治疗脑缺血。

10. 发明授权

US5739158A Nitrogen-containing cyclohetero cycloalkylaminoaryl derivatives for CNS disorders 失效
标题翻译：用于CNS疾病的含氮环杂环烷基氨基芳基衍生物
公开(公告)号：US5739158A
公开(公告)日：1998-04-14
申请号：US877190
申请日：1992-07-01
申请人： Brian R. de Costa , Kenner C. Rice , Nancy M. Gray , Patricia C. Contreras , Arthur E. Jacobson , Andrew Thurkauf , Lilian A. Radesca , Wayne D. Bowen , J. Michael Walker
发明人： Brian R. de Costa , Kenner C. Rice , Nancy M. Gray , Patricia C. Contreras , Arthur E. Jacobson , Andrew Thurkauf , Lilian A. Radesca , Wayne D. Bowen , J. Michael Walker
IPC分类号： A61K31/40 , A61K31/4025 , A61P25/00 , C07D295/12 , C07D295/135 , C07D405/12 , C07D295/073
CPC分类号： C07D295/135
摘要： Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychotic disorders, convulsions and parkinsonism. Compounds of particular interest are of the formula ##STR1## wherein R.sup.1 is selected from hydrido, loweralkyl, cycloalkylalkyl of four to six carbon atoms and loweralkenylloweralkyl; wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and loweralkyl; wherein each of R.sup.4 through R.sup.7, R.sup.10 and R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is a number selected from four through six; wherein p is a number selected from zero through four; wherein q is a number selected from three through five; wherein A is selected from phenyl, naphthyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
摘要翻译： PCT No.PCT / US91 / 00688 Sec。 371日期：1992年7月1日 102（e）日期1992年7月1日PCT 1991年1月31日PCT PCT。 WO91 / 12247 PCT出版物日期1991年8月22日描述了含氮环杂环烷基氨基芳基化合物用于治疗中枢神经系统疾病如脑缺血，精神障碍，抽搐和帕金森综合征。特别感兴趣的化合物具有式为四氟化烷基，四至六个碳原子的环烷基烷基和低级链烯基低级烷基; 其中R2和R3各自独立地选自氢和低级烷基; 其中R 4至R 7，R 10和R 11各自独立地选自氢，羟基，低级烷基，苄基，苯氧基，苄氧基和卤代低级烷基; 其中n是选自四至六的数字; 其中p是选自零至四的数字; 其中q是选自三至五的数; 其中A选自苯基，萘基和噻吩基; 其中前述A基团中的任一个可以进一步被一个或多个独立地选自氢，羟基，低级烷基，低级烷氧基，卤素，卤代低级烷基，氨基，单低级烷基氨基和二低级烷基氨基的取代基取代。或其药学上可接受的盐。

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