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公开(公告)号:US20110082107A1
公开(公告)日:2011-04-07
申请号:US12898279
申请日:2010-10-05
申请人: Martin Henriksson , Evert Homan , Lars Johansson , Jerk Vallgarda , Meredith Williams , Eric A. Bercot , Christopher H. Fotsch , Aiwen Li , Guolin Cai , Randall W. Hungate , Chester Chenguang Yuan , Christopher Tegley , David J.St. Jean, JR. , Nianhe Han , Qi Huang , Qingyian Liu , Michael D. Bartberger , George A. Moniz , Matthew J. Frizzle
发明人: Martin Henriksson , Evert Homan , Lars Johansson , Jerk Vallgarda , Meredith Williams , Eric A. Bercot , Christopher H. Fotsch , Aiwen Li , Guolin Cai , Randall W. Hungate , Chester Chenguang Yuan , Christopher Tegley , David J.St. Jean, JR. , Nianhe Han , Qi Huang , Qingyian Liu , Michael D. Bartberger , George A. Moniz , Matthew J. Frizzle
IPC分类号: A61K31/695 , C07D277/54 , A61K31/426 , C07D413/06 , A61K31/5377 , C07D277/60 , A61K31/428 , C07D417/06 , C07D417/12 , A61K31/55 , A61K31/4439 , C07D413/14 , A61K31/454 , C07D497/10 , A61K31/438 , C07F7/18 , A61P3/00 , A61P25/28 , A61P35/00
CPC分类号: C07D417/06 , C07D263/34 , C07D263/48 , C07D275/03 , C07D277/42 , C07D277/54 , C07D277/60 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D513/10 , C07F7/1804
摘要: The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.
摘要翻译: 本发明涉及具有式(I),(II),(III)或(IV)的化合物:其中R1,R2,R3,R4,R5,R6,R7,X和Z如本文所定义, 涉及包含该化合物的药物组合物,以及该化合物用于治疗与人类11-羟基类固醇脱氢酶1型酶相关的病症的用途和用于制备作用于人类11- 羟类固醇脱氢酶1型酶。
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公开(公告)号:US07807700B2
公开(公告)日:2010-10-05
申请号:US11819607
申请日:2007-06-28
申请人: Martin Henriksson , Evert Homan , Lars Johansson , Jerk Vallgarda , Meredith Williams , Eric Bercot , Christopher H. Fotsch , Aiwen Li , Guolin Cai , Randall W. Hungate , Chester Chenguang Yuan , Christopher Tegley , David J. St. Jean, Jr. , Nianhe Han , Qi Huang , Qingyian Liu , Michael D. Bartberger , George A. Moniz , Matthew J. Frizzle
发明人: Martin Henriksson , Evert Homan , Lars Johansson , Jerk Vallgarda , Meredith Williams , Eric Bercot , Christopher H. Fotsch , Aiwen Li , Guolin Cai , Randall W. Hungate , Chester Chenguang Yuan , Christopher Tegley , David J. St. Jean, Jr. , Nianhe Han , Qi Huang , Qingyian Liu , Michael D. Bartberger , George A. Moniz , Matthew J. Frizzle
IPC分类号: A61K31/427 , C07D277/14 , C07D277/18
CPC分类号: C07D417/06 , C07D263/34 , C07D263/48 , C07D275/03 , C07D277/42 , C07D277/54 , C07D277/60 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D513/10 , C07F7/1804
摘要: The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.
摘要翻译: 本发明涉及具有式(I),(II),(III)或(IV)的化合物:其中R1,R2,R3,R4,R5,R6,R7,X和Z如本文所定义, 涉及包含该化合物的药物组合物,以及该化合物用于治疗与人类11-羟基类固醇脱氢酶1型酶相关的病症的用途和用于制备作用于人类11- 羟类固醇脱氢酶1型酶。
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公开(公告)号:US07642267B2
公开(公告)日:2010-01-05
申请号:US11942480
申请日:2007-11-19
申请人: Guiying Li , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu , George P. Luke , Scott Mitchell , Martin Patrick Allen , Spiros Liras
发明人: Guiying Li , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu , George P. Luke , Scott Mitchell , Martin Patrick Allen , Spiros Liras
IPC分类号: C07D471/04 , A61K31/437
CPC分类号: C07D401/04 , C07D233/20 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10
摘要: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I. The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.
摘要翻译: 本发明涉及苯并咪唑,吡啶基咪唑和相关的双环杂芳基化合物,所有这些可以由式I描述。本发明特别涉及以高选择性和高亲和力结合GABA A受体的苯并二氮杂位点的化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物在治疗某些中枢神经系统(CNS)疾病中的用途。 公开了制备式I化合物的新方法。 本发明还涉及式I的苯并咪唑,吡啶基咪唑和相关的双环杂芳基化合物与一种或多种其它CNS剂的组合用于增强其它CNS剂的作用。 此外,本发明涉及使用这些化合物作为组织切片中GABA A受体定位的探针。
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公开(公告)号:US20080045503A1
公开(公告)日:2008-02-21
申请号:US11819607
申请日:2007-06-28
申请人: Martin Henriksson , Evert Homan , Lars Johansson , Jerk Vallgarda , Meredith Williams , Eric Bercot , Christopher Fotsch , Aiwen Li , Guolin Cai , Randall Hungate , Chester Yuan , Christopher Tegley , David St. Jean , Nianhe Han , Qi Huang , Qingyian Liu , Michael Bartberger , George Moniz , Matthew Frizzle
发明人: Martin Henriksson , Evert Homan , Lars Johansson , Jerk Vallgarda , Meredith Williams , Eric Bercot , Christopher Fotsch , Aiwen Li , Guolin Cai , Randall Hungate , Chester Yuan , Christopher Tegley , David St. Jean , Nianhe Han , Qi Huang , Qingyian Liu , Michael Bartberger , George Moniz , Matthew Frizzle
IPC分类号: C07D277/34 , A61K31/421 , A61K31/426 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K31/55 , A61P25/00 , C07D277/62 , C12N9/99 , C07D417/00 , C07D413/00 , C07D401/00 , A61P3/00 , A61P37/00 , A61P9/00 , C07D211/06 , C07D221/20 , C07D263/36 , C07D263/52
CPC分类号: C07D417/06 , C07D263/34 , C07D263/48 , C07D275/03 , C07D277/42 , C07D277/54 , C07D277/60 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D513/10 , C07F7/1804
摘要: The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.
摘要翻译: 本发明涉及具有式(I),(II),(III)或(IV)的化合物:其中R 1,R 2,R 2, 3,R 4,R 5,R 6,R 7,X和Z分别为 以及包含该化合物的药物组合物的使用方法,以及该化合物用于治疗与人类11-β-羟基类固醇脱氢酶1型酶相关的病症和用于制备作用于人的药物的方法 11-β-羟基类固醇脱氢酶1型酶。
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公开(公告)号:US07300945B2
公开(公告)日:2007-11-27
申请号:US11179458
申请日:2005-07-12
申请人: Guiying Li , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu , George P. Luke , Scott Mitchell , Martin Patrick Allen , Spiros Liras
发明人: Guiying Li , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu , George P. Luke , Scott Mitchell , Martin Patrick Allen , Spiros Liras
IPC分类号: C07D471/04 , A61K31/437
CPC分类号: C07D401/04 , C07D233/20 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10
摘要: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed.This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.
摘要翻译: 本发明涉及苯并咪唑,吡啶基咪唑和相关双环杂芳基化合物,所有这些可以由式I描述。本发明特别涉及以高选择性和高亲和力结合GABA A的苯并二氮杂部位的化合物, / SUB>受体。 本发明还涉及包含这些化合物的药物组合物以及这些化合物在治疗某些中枢神经系统(CNS)疾病中的用途。 公开了制备式I化合物的新方法。 本发明还涉及式I的苯并咪唑,吡啶基咪唑和相关的双环杂芳基化合物与一种或多种其它CNS剂的组合用于增强其它CNS剂的作用。 此外,本发明涉及使用这些化合物作为组织切片中GABA A A受体定位的探针。
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公开(公告)号:US20060100213A1
公开(公告)日:2006-05-11
申请号:US11247046
申请日:2005-10-11
申请人: Toshihiro Aya , Guolin Cai , Jian Chen , Derin D'Amico , Thomas Nguyen , Wenyuan Qian
发明人: Toshihiro Aya , Guolin Cai , Jian Chen , Derin D'Amico , Thomas Nguyen , Wenyuan Qian
IPC分类号: A61K31/497 , C07D405/14
CPC分类号: C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D471/04
摘要: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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公开(公告)号:US20060025425A1
公开(公告)日:2006-02-02
申请号:US11179458
申请日:2005-07-12
申请人: Guiying Li , Pamela Albaugh , Kevin Currie , Guolin Cai , Linda Gustavson , Kyungae Lee , Alan Hutchison , George Maynard , Jun Yuan , Ling Xie , Manuka Ghosh , Nian Liu , George Luke , Scott Mitchell , Martin Allen , Spiros Liras
发明人: Guiying Li , Pamela Albaugh , Kevin Currie , Guolin Cai , Linda Gustavson , Kyungae Lee , Alan Hutchison , George Maynard , Jun Yuan , Ling Xie , Manuka Ghosh , Nian Liu , George Luke , Scott Mitchell , Martin Allen , Spiros Liras
IPC分类号: A61K31/506 , A61K31/4745 , A61K31/427 , A61K31/4184 , C07D471/02 , C07D403/02 , C07D417/02 , C07D413/02
CPC分类号: C07D401/04 , C07D233/20 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10
摘要: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.
摘要翻译: 本发明涉及苯并咪唑,吡啶基咪唑和相关双环杂芳基化合物,所有这些可以由式I描述。本发明特别涉及以高选择性和高亲和力结合GABA A的苯并二氮杂部位的化合物, / SUB>受体。 本发明还涉及包含这些化合物的药物组合物以及这些化合物在治疗某些中枢神经系统(CNS)疾病中的用途。 公开了制备式I化合物的新方法。 本发明还涉及式I的苯并咪唑,吡啶基咪唑和相关的双环杂芳基化合物与一种或多种其它CNS剂的组合用于增强其它CNS剂的作用。 此外,本发明涉及使用这些化合物作为组织切片中GABA A A受体定位的探针。
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公开(公告)号:US20060025400A1
公开(公告)日:2006-02-02
申请号:US11182216
申请日:2005-07-15
申请人: Benny Askew , Toshihiro Aya , Kaustav Biswas , Guolin Cai , Jian Chen , Nianhe Han , Qingyian Liu , Thomas Nguyen , Nobuko Nishimura , Rana Nomak , Tanya Peterkin , Wenyuan Qian , Kevin Yang , Chester Yuan , Jiawang Zhu , Derin D' Amico , Jason Human , Qi Huang
发明人: Benny Askew , Toshihiro Aya , Kaustav Biswas , Guolin Cai , Jian Chen , Nianhe Han , Qingyian Liu , Thomas Nguyen , Nobuko Nishimura , Rana Nomak , Tanya Peterkin , Wenyuan Qian , Kevin Yang , Chester Yuan , Jiawang Zhu , Derin D' Amico , Jason Human , Qi Huang
IPC分类号: A61K31/55 , A61K31/497 , C07D403/02
CPC分类号: C07D221/10 , C07D221/08 , C07D239/74 , C07D241/08 , C07D243/08 , C07D249/08 , C07D295/135 , C07D311/96 , C07D335/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D417/12 , C07D491/04
摘要: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译: 所选化合物对于治疗疼痛和疾病如炎症介导的疾病是有效的。 本发明包括新的化合物,类似物,前药和其药学上可接受的衍生物,用于预防和治疗疾病和其它疾病或涉及疼痛,炎症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。
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公开(公告)号:US20050154008A1
公开(公告)日:2005-07-14
申请号:US11003195
申请日:2004-12-03
申请人: Guolin Cai , Pamela Albaugh , Jun Yuan
发明人: Guolin Cai , Pamela Albaugh , Jun Yuan
IPC分类号: A61P25/22 , A61P25/24 , A61P25/28 , C07D215/22 , C07D215/233 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/04 , C07D495/04 , C07D471/02 , A61K31/47 , A61K31/4745
CPC分类号: C07D215/233 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/04 , C07D495/04
摘要: Disclosed are compounds of the formula: wherein X, Q, W and are as defined herein. These compounds are agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
摘要翻译: 公开了下式的化合物:其中X,Q,W和如本文所定义。 这些化合物是用于GABA A A受体的激动剂,拮抗剂或反向激动剂或GABA A A受体的激动剂,拮抗剂或反向激动剂的前体药物,因此可用于诊断和 治疗焦虑,抑郁症,唐氏综合征,睡眠和癫痫发作障碍,用苯二氮卓类药物服用过量,并增加记忆力。 还提供药物组合物,包括包装的药物组合物。 本发明的化合物也可用作组织样品中GABA A A受体定位的探针。
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公开(公告)号:US20050153960A1
公开(公告)日:2005-07-14
申请号:US10996035
申请日:2004-11-22
申请人: Daniel Elbaum , Benny Askew , Shon Booker , Julie Germain , Gregory Habgood , Michael Handley , Tae-Seong Kim , Aiwen Li , Nobuko Nishimura , Vinod Patel , Chester Yuan , Joseph Kim , Guolin Cai , Guoqing Chen , Michael Croghan , Lucian Di Pietro , Celia Dominguez , Qi Huang , Leon Smith , Andrew Tasker , Ning Xi , Shimin Xu
发明人: Daniel Elbaum , Benny Askew , Shon Booker , Julie Germain , Gregory Habgood , Michael Handley , Tae-Seong Kim , Aiwen Li , Nobuko Nishimura , Vinod Patel , Chester Yuan , Joseph Kim , Guolin Cai , Guoqing Chen , Michael Croghan , Lucian Di Pietro , Celia Dominguez , Qi Huang , Leon Smith , Andrew Tasker , Ning Xi , Shimin Xu
IPC分类号: A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/498 , A61K31/501 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/538 , A61P1/04 , A61P3/00 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P15/00 , A61P15/08 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/00 , A61P19/02 , A61P21/00 , A61P25/28 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/12 , A61P31/18 , A61P31/22 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/02 , A61P37/04 , A61P37/08 , A61P43/00 , C07D213/81 , C07D213/82 , C07D237/04 , C07D237/24 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , A61K31/4545 , C07D413/02 , C07D41/02
CPC分类号: C07D213/81 , C04B35/632 , C07D213/82 , C07D237/04 , C07D237/24 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
摘要: Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译: 所选化合物对于预防和治疗诸如血管生成介导的疾病等疾病是有效的。 本发明包括新型化合物,类似物,前药及其药学上可接受的衍生物,用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。
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