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公开(公告)号:US20140243290A1
公开(公告)日:2014-08-28
申请号:US14255480
申请日:2014-04-17
申请人: Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Sathesh Bhat , Jason Burch , Kaleen Konrad Childers , Bernard Cote , Maria Emilia Di Francesco , Anthony Donofrio , Kristina Dupont-Gaudet , John Michael Ellis , Christian Fischer , Jean-Francois Fournier , Jacques Yves Gauthier , Jonathan Grimm , Daniel Guay , David Joseph Guerin , Andrew M. Haidle , Solomon D. Kattar , Sandra Lee Knowles , Chaomin Li , Jongwon Lim , Michelle R. Machacek , Matthew L. Maddess , Alan B. Northrup , Brendan M. O'Boyle , Ryan D. Otte , Alessia Petrocchi , Michael H. Reutershan , Joel S. Robichaud , Eric T. Romeo , Adam J. Schell , Tony Siu , Kerrie B. Spencer , Brandon M. Taoka , B. Wesley Trotter , Hyun Chong Woo , Hua Zhou
发明人: Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Sathesh Bhat , Jason Burch , Kaleen Konrad Childers , Bernard Cote , Maria Emilia Di Francesco , Anthony Donofrio , Kristina Dupont-Gaudet , John Michael Ellis , Christian Fischer , Jean-Francois Fournier , Jacques Yves Gauthier , Jonathan Grimm , Daniel Guay , David Joseph Guerin , Andrew M. Haidle , Solomon D. Kattar , Sandra Lee Knowles , Chaomin Li , Jongwon Lim , Michelle R. Machacek , Matthew L. Maddess , Alan B. Northrup , Brendan M. O'Boyle , Ryan D. Otte , Alessia Petrocchi , Michael H. Reutershan , Joel S. Robichaud , Eric T. Romeo , Adam J. Schell , Tony Siu , Kerrie B. Spencer , Brandon M. Taoka , B. Wesley Trotter , Hyun Chong Woo , Hua Zhou
IPC分类号: C07D417/12 , C07D495/04 , C07D451/06 , C07F9/6558 , C07D471/08 , C07D487/04 , C07D471/04 , C07D417/14 , C07D491/08
CPC分类号: C07D417/12 , C07D417/14 , C07D451/06 , C07D471/04 , C07D471/08 , C07D487/04 , C07D491/08 , C07D495/04 , C07F9/65583
摘要: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
摘要翻译: 本发明提供了新颖的式(I)嘧啶胺,其是脾脏酪氨酸激酶的有效抑制剂,并且可用于治疗和预防由所述酶介导的疾病,例如哮喘,COPD和类风湿性关节炎。
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公开(公告)号:US20120277192A1
公开(公告)日:2012-11-01
申请号:US13516455
申请日:2010-12-15
申请人: Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Sathesh Bhat , Jason Burch , Kaleen Konrad Childers , Bernard Cote , Maria Emilia Di Francesco , Anthony Donofrio , Kristina Dupont-Gaudet , John Michael Ellis , Christian Fischer , Jean-Francois Fournier , Jacques Yves Gauthier , Jonathan Grimm , Daniel Guay , David Joseph Guerin , Andrew M. Haidle , Solomon Kattar , Sandra Lee Knowles , Chaomin Li , Jongwon Lim , Michelle R. Machacek , Matthew L. Maddess , Alan B. Northrup , Brendan M. O'Boyle , Ryan D. Otte , Alessia Petrocchi , Michael H. Reutershan , Joel S. Robichaud , Eric Romeo , Adam J. Schell , Tony Siu , Kerrie B. Spencer , Brandon M. Taoka , B. Wesley Trotter , Hyun Chong Woo , Hua Zhou
发明人: Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Sathesh Bhat , Jason Burch , Kaleen Konrad Childers , Bernard Cote , Maria Emilia Di Francesco , Anthony Donofrio , Kristina Dupont-Gaudet , John Michael Ellis , Christian Fischer , Jean-Francois Fournier , Jacques Yves Gauthier , Jonathan Grimm , Daniel Guay , David Joseph Guerin , Andrew M. Haidle , Solomon Kattar , Sandra Lee Knowles , Chaomin Li , Jongwon Lim , Michelle R. Machacek , Matthew L. Maddess , Alan B. Northrup , Brendan M. O'Boyle , Ryan D. Otte , Alessia Petrocchi , Michael H. Reutershan , Joel S. Robichaud , Eric Romeo , Adam J. Schell , Tony Siu , Kerrie B. Spencer , Brandon M. Taoka , B. Wesley Trotter , Hyun Chong Woo , Hua Zhou
IPC分类号: A61K31/506 , A61K31/55 , A61K31/554 , A61K31/551 , A61P35/00 , C07D417/14 , C07F9/6539 , C07D417/12 , A61P19/02 , A61P11/06 , A61K31/675 , A61K31/5377
CPC分类号: C07D417/12 , C07D417/14 , C07D451/06 , C07D471/04 , C07D471/08 , C07D487/04 , C07D491/08 , C07D495/04 , C07F9/65583
摘要: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
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公开(公告)号:US20110245205A1
公开(公告)日:2011-10-06
申请号:US12968608
申请日:2010-12-15
申请人: Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Sathesh Bhat , Jason Burch , Kaleen Konrad Childers , Bernard Cote , Maria Emilia Di Francesco , Anthony Donofrio , Kristina Dupont-Gaudet , John Michael Ellis , Christian Fischer , Jean-Francois Fournier , Jacques Yves Gauthier , Jonathan Grimm , Daniel Guay , David Joseph Guerin , Andrew M. Haidle , Solomon Kattar , Sandra Lee Knowles , Chaomin Li , Jongwon Lim , Michelle R. Machacek , Matthew L. Maddess , Alan B. Northrup , Brendan M. O'Boyle , Ryan D. Otte , Alessia Petrocchi , Michael H. Reutershan , Joel S. Robichaud , Eric Romeo , Adam J. Schell , Tony Siu , Kerrie B. Spencer , Brandon M. Taoka , B. Wesley Trotter , Hyun Chong Woo , Hua Zhou
发明人: Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Sathesh Bhat , Jason Burch , Kaleen Konrad Childers , Bernard Cote , Maria Emilia Di Francesco , Anthony Donofrio , Kristina Dupont-Gaudet , John Michael Ellis , Christian Fischer , Jean-Francois Fournier , Jacques Yves Gauthier , Jonathan Grimm , Daniel Guay , David Joseph Guerin , Andrew M. Haidle , Solomon Kattar , Sandra Lee Knowles , Chaomin Li , Jongwon Lim , Michelle R. Machacek , Matthew L. Maddess , Alan B. Northrup , Brendan M. O'Boyle , Ryan D. Otte , Alessia Petrocchi , Michael H. Reutershan , Joel S. Robichaud , Eric Romeo , Adam J. Schell , Tony Siu , Kerrie B. Spencer , Brandon M. Taoka , B. Wesley Trotter , Hyun Chong Woo , Hua Zhou
IPC分类号: A61K31/675 , C07D417/14 , A61K31/55 , C07D417/12 , A61K31/506 , C07F9/6558 , A61K31/397 , A61K31/551 , A61K31/553 , A61K31/541 , C07D413/14 , A61K31/5377 , A61P11/06 , A61P35/00 , A61P19/02
CPC分类号: C07D417/12 , C07D417/14 , C07D451/06 , C07D471/04 , C07D471/08 , C07D487/04 , C07D491/08 , C07D495/04 , C07F9/65583
摘要: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
摘要翻译: 本发明提供了新颖的式(I)嘧啶胺,其是脾脏酪氨酸激酶的有效抑制剂,并且可用于治疗和预防由所述酶介导的疾病,例如哮喘,COPD和类风湿性关节炎。
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公开(公告)号:US08551984B2
公开(公告)日:2013-10-08
申请号:US12968608
申请日:2010-12-15
申请人: Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Jason Burch , Kaleen Konrad Childers , Bernard Cote , Maria Emilia Di Francesco , Anthony Donofrio , Kristina Dupont-Gaudet , John Michael Ellis , Christian Fischer , Daniel Guay , David Joseph Guerin , Andrew M. Haidle , Solomon Kattar , Sandra Lee Knowles , Chaomin Li , Jongwon Lim , Michelle R. Machacek , Alan B. Northrup , Brendan M. O'Boyle , Ryan D. Otte , Michael H. Reutershan , Eric Romeo , Adam J. Schell , Tony Siu , Kerrie B. Spencer , Brandon M. Taoka , B. Wesley Trotter , Hua Zhou
发明人: Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Jason Burch , Kaleen Konrad Childers , Bernard Cote , Maria Emilia Di Francesco , Anthony Donofrio , Kristina Dupont-Gaudet , John Michael Ellis , Christian Fischer , Daniel Guay , David Joseph Guerin , Andrew M. Haidle , Solomon Kattar , Sandra Lee Knowles , Chaomin Li , Jongwon Lim , Michelle R. Machacek , Alan B. Northrup , Brendan M. O'Boyle , Ryan D. Otte , Michael H. Reutershan , Eric Romeo , Adam J. Schell , Tony Siu , Kerrie B. Spencer , Brandon M. Taoka , B. Wesley Trotter , Hua Zhou
IPC分类号: C07D417/12 , A61K31/497
CPC分类号: C07D417/12 , C07D417/14 , C07D451/06 , C07D471/04 , C07D471/08 , C07D487/04 , C07D491/08 , C07D495/04 , C07F9/65583
摘要: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
摘要翻译: 本发明提供了新颖的式(I)嘧啶胺,其是脾脏酪氨酸激酶的有效抑制剂,并且可用于治疗和预防由所述酶介导的疾病,例如哮喘,COPD和类风湿性关节炎。
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公开(公告)号:US08735417B2
公开(公告)日:2014-05-27
申请号:US13515941
申请日:2010-12-16
申请人: Michael D. Altman , Kenneth L. Arrington , Jason Burch , Bernard Cote , Jean-Francois Fournier , Jacques Yves Gauthier , Solomon Kattar , Sandra Lee Knowles , Jongwon Lim , Michelle R. Machacek , Alan B. Northrup , Michael H. Reutershan , Joel S. Robichaud , Adam J. Schell , Kerrie B. Spencer
发明人: Michael D. Altman , Kenneth L. Arrington , Jason Burch , Bernard Cote , Jean-Francois Fournier , Jacques Yves Gauthier , Solomon Kattar , Sandra Lee Knowles , Jongwon Lim , Michelle R. Machacek , Alan B. Northrup , Michael H. Reutershan , Joel S. Robichaud , Adam J. Schell , Kerrie B. Spencer
IPC分类号: A61K31/506 , C07D417/02
CPC分类号: C07D417/12 , C07D417/14 , C07D471/10 , C07D487/04 , C07D491/10
摘要: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
摘要翻译: 本发明提供了新颖的式(I)嘧啶胺,其是脾脏酪氨酸激酶的有效抑制剂,并且可用于治疗和预防由所述酶介导的疾病,例如哮喘,COPD和类风湿性关节炎。
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公开(公告)号:US20120309735A1
公开(公告)日:2012-12-06
申请号:US13515941
申请日:2010-12-16
申请人: Michael D. Altman , Kenneth L. Arrington , Jason Burch , Bernard Cote , Jean-Francois Fournier , Jacques Yves Gauthier , Solomon Kattar , Sandra Lee Knowles , Jongwon Lim , Michelle R. Machacek , Alan B. Northrup , Michael H. Reutershan , Joel S. Robichaud , Adam J. Schell , Kerrie B. Spencer
发明人: Michael D. Altman , Kenneth L. Arrington , Jason Burch , Bernard Cote , Jean-Francois Fournier , Jacques Yves Gauthier , Solomon Kattar , Sandra Lee Knowles , Jongwon Lim , Michelle R. Machacek , Alan B. Northrup , Michael H. Reutershan , Joel S. Robichaud , Adam J. Schell , Kerrie B. Spencer
IPC分类号: A61K31/506 , C07D417/12 , C07D417/14 , C07D471/04 , A61P19/02 , A61K31/551 , A61P11/06 , A61P11/00 , A61P29/00 , C07D471/10 , A61K31/5377
CPC分类号: C07D417/12 , C07D417/14 , C07D471/10 , C07D487/04 , C07D491/10
摘要: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
摘要翻译: 本发明提供了新颖的式(I)嘧啶胺,其是脾脏酪氨酸激酶的有效抑制剂,并且可用于治疗和预防由所述酶介导的疾病,例如哮喘,COPD和类风湿性关节炎。
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公开(公告)号:US06399636B2
公开(公告)日:2002-06-04
申请号:US09810119
申请日:2001-03-16
申请人: Richard Freisen , Yves Ducharme , Bernard Cote , Marc Blouin , Evelyn Martins , Daniel Guay , Pierre Hamel , Mario Girard , Richard Frenette , Sebastien Laliberte
发明人: Richard Freisen , Yves Ducharme , Bernard Cote , Marc Blouin , Evelyn Martins , Daniel Guay , Pierre Hamel , Mario Girard , Richard Frenette , Sebastien Laliberte
IPC分类号: A61K314439
CPC分类号: C07D417/06
摘要: Novel ethanes substituted with i) a phenyl, ii) a thiazole, and iii) a pyridyl moiety are PDE4 inhibitors.
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公开(公告)号:US06200993B1
公开(公告)日:2001-03-13
申请号:US09551040
申请日:2000-04-17
申请人: Bernard Cote , Richard Friesen , Richard Frenette , Mario Girard , Yves Girard , Cedrickx Godbout , Daniel Guay , Pierre Hamel , Marc Blouin , Yves Ducharme , Sylvie Prescott
发明人: Bernard Cote , Richard Friesen , Richard Frenette , Mario Girard , Yves Girard , Cedrickx Godbout , Daniel Guay , Pierre Hamel , Marc Blouin , Yves Ducharme , Sylvie Prescott
IPC分类号: A61K3144
CPC分类号: C07D213/74 , C07D213/76 , C07D213/79 , C07D213/89 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要: The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3′,5′-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE 4). or a pharmaceutically acceptable salt or hydrate thereof. The invention also encompasses pharmaceutical compositions and methods for treatment.
摘要翻译: 本发明包括通过通过抑制磷酸二酯酶IV(PDE 4)提高环腺苷-3',5'-单磷酸(cAMP)的水平,可用于治疗包括哮喘在内的疾病的新颖化合物。 其药学上可接受的盐或水合物。本发明还包括药物组合物和治疗方法。
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公开(公告)号:US08486975B2
公开(公告)日:2013-07-16
申请号:US13073631
申请日:2011-03-28
申请人: Jason Burch , Bernard Cote
发明人: Jason Burch , Bernard Cote
IPC分类号: A61K31/4439 , C07D401/06
CPC分类号: C07D401/06 , A61K31/4439 , A61K45/06
摘要: Heteroaromatic compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译: 式I的杂芳族化合物是HIV逆转录酶抑制剂,其中R 1,R 2,R 3,R 4和R 5在本文中定义。 式I化合物及其药学上可接受的盐可用于抑制HIV逆转录酶,预防和治疗HIV感染以及预防,延缓发病或进展以及AIDS治疗。 化合物及其盐可以用作药物组合物中的成分,任选与其它抗病毒剂,免疫调节剂,抗生素或疫苗组合使用。
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公开(公告)号:US20060040981A1
公开(公告)日:2006-02-23
申请号:US10536250
申请日:2003-11-19
申请人: Daniel Dube , Michel Gallant , Patrick Lacombe , Yves Girard , Dwight Macdonald , Richard Friesen , Yves Ducharme , Bernard Cote , Marc Blouin , Evelyn Martins , Daniel Guay , Pierre Hamel , Mario Girard , Richard Frenette , Sebastien Laliberte , Annette Robichaud , Anthony Mastracchio , Helene Perrier
发明人: Daniel Dube , Michel Gallant , Patrick Lacombe , Yves Girard , Dwight Macdonald , Richard Friesen , Yves Ducharme , Bernard Cote , Marc Blouin , Evelyn Martins , Daniel Guay , Pierre Hamel , Mario Girard , Richard Frenette , Sebastien Laliberte , Annette Robichaud , Anthony Mastracchio , Helene Perrier
IPC分类号: A61K31/4709 , A61K31/47
CPC分类号: A61K31/4709 , A61K31/277 , A61K31/4375 , A61K31/44 , A61K31/47
摘要: The present invention is directed to a method of enhancing cognition in a healthy subject comprising administering a safe cognition enhancing amount of a phosphodiesterase-4 inhibitor. In particular, this invention is directed to a method of enhancing memory, learning, retention, recall, awareness and judgement in health subjects comprising administering a safe and effective amount of a phosphodiesterase-4 inhibitor.
摘要翻译: 本发明涉及增强健康受试者的认知的方法,其包括施用安全认知增加量的磷酸二酯酶-4抑制剂。 特别地,本发明涉及增加健康受试者的记忆,学习,保留,召回,意识和判断的方法,包括施用安全有效量的磷酸二酯酶-4抑制剂。
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