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公开(公告)号:US09586931B2
公开(公告)日:2017-03-07
申请号:US14431895
申请日:2013-09-24
申请人: Michelle R. Machacek , Eric T. Romeo , Solomon D. Kattar , Matthew Christopher , Michael D. Altman , Alan B. Northrup , John Michael Ellis , Brendan O'Boyle , Anthony Donofrio , Jonathan Grimm , Michael H. Reutershan , Kaleen Konrad Childers , Ryan D. Otte , Brandon Cash , Yves Ducharme , Andrew M. Haidle , Kerrie Spencer , Dilrukshi Vitharana , Lingyun Wu , Li Zhang , Peng Zhang , Christian Beaulieu , Daniel Guay
发明人: Michelle R. Machacek , Eric T. Romeo , Solomon D. Kattar , Matthew Christopher , Michael D. Altman , Alan B. Northrup , John Michael Ellis , Brendan O'Boyle , Anthony Donofrio , Jonathan Grimm , Michael H. Reutershan , Kaleen Konrad Childers , Ryan D. Otte , Brandon Cash , Yves Ducharme , Andrew M. Haidle , Kerrie Spencer , Dilrukshi Vitharana , Lingyun Wu , Li Zhang , Peng Zhang , Christian Beaulieu , Daniel Guay
IPC分类号: A61K9/10 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D498/04 , C07D413/14 , C07D239/42 , A61K9/00 , A61K9/20 , A61K9/48 , C07D403/12 , C07D405/12 , C07D409/12 , C07D471/04
CPC分类号: C07D401/14 , A61K9/0019 , A61K9/0073 , A61K9/0075 , A61K9/10 , A61K9/2027 , A61K9/4858 , C07D239/42 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04
摘要: Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
摘要翻译: 提供式I的三唑衍生物,其是脾脏酪氨酸激酶和药物组合物的有效抑制剂。 三唑衍生物可用于治疗和预防由所述酶介导的疾病,例如哮喘,COPD,类风湿性关节炎和癌症。
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公开(公告)号:US20150239866A1
公开(公告)日:2015-08-27
申请号:US14431895
申请日:2013-09-24
申请人: Michelle R. MACHACEK , Eric T. ROMEO , Solomon D. KATTAR , Matthew CHRISTOPHER , Michael D. ALTMAN , Alan B. NORTHRUP , John Michael ELLIS , Brendan O BOYLE , Anthony DONOFRIO , Jonathan GRIMM , Michael H. REUTERSHAN , Kaleen Konrad CHILDERS , Ryan D. OTTE , Brandon CASH , Yves DUCHARME , Andrew M. HAIDLE , Kerrie SPENCER , Dilrukshi VITHARANA , Lingyun WU , Li ZHANG , Peng ZHANG , Christian BEAULIEU , Daniel GUAY
发明人: Michelle R. Machacek , Eric T. Romeo , Solomon D. Kattar , Matthew Christopher , Michael D. Altman , Alan B. Northrup , John Michael Ellis , Brendan O'Boyle , Anthony Donofrio , Jonathan Grimm , Michael H. Reutershan , Kaleen Konrad Childers , Ryan D. Otte , Brandon Cash , Yves Ducharme , Andrew M. Haidle , Kerrie Spencer , Dilrukshi Vitharana , Lingyun Wu , Li Zhang , Peng Zhang , Christian Beaulieu , Daniel Guay
IPC分类号: C07D401/14 , C07D471/04 , C07D405/14 , C07D413/14 , C07D498/04 , C07D409/14 , C07D417/14
CPC分类号: C07D401/14 , A61K9/0019 , A61K9/0073 , A61K9/0075 , A61K9/10 , A61K9/2027 , A61K9/4858 , C07D239/42 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04
摘要: Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
摘要翻译: 提供式I的三唑衍生物,其是脾脏酪氨酸激酶和药物组合物的有效抑制剂。 三唑衍生物可用于治疗和预防由所述酶介导的疾病,例如哮喘,COPD,类风湿性关节炎和癌症。
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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:US09290490B2
公开(公告)日:2016-03-22
申请号:US14116207
申请日:2012-05-04
申请人: Michael D. Altman , Kaleen Konrad Childers , Maria Emilia Di Francesco , John Michael Ellis , Christian Fischer , Jonathan Grimm , Andrew M. Haidle , Solomon D. Kattar , Alan B. Northrup , Ryan D. Otte , Alessia Petrocchi , Adam J. Schell , Hua Zhou
发明人: Michael D. Altman , Kaleen Konrad Childers , Maria Emilia Di Francesco , John Michael Ellis , Christian Fischer , Jonathan Grimm , Andrew M. Haidle , Solomon D. Kattar , Alan B. Northrup , Ryan D. Otte , Alessia Petrocchi , Adam J. Schell , Hua Zhou
IPC分类号: C07D401/12 , A61K31/506 , C07D487/04 , C07D401/14 , C07D417/12 , C07D417/14
CPC分类号: C07D417/12 , C07D417/14
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, rheumatoid arthritis and cancer.
摘要翻译: 本发明提供了式I的新型嘧啶胺,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,类风湿性关节炎和癌症。
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公开(公告)号:US20140148474A1
公开(公告)日:2014-05-29
申请号:US14116207
申请日:2012-05-04
申请人: Michael D. Altman , Kaleen Konrad Childers , Maria Emilia Di Francesco , John Michael Ellis , Christian Fischer , Jonathan Grimm , Andrew M. Haidle , Solomon D. Kattar , Alan B. Northrup , Ryan D. Otte , Alessia Petrocchi , Adam J. Schell , Hua Zhou
发明人: Michael D. Altman , Kaleen Konrad Childers , Maria Emilia Di Francesco , John Michael Ellis , Christian Fischer , Jonathan Grimm , Andrew M. Haidle , Solomon D. Kattar , Alan B. Northrup , Ryan D. Otte , Alessia Petrocchi , Adam J. Schell , Hua Zhou
IPC分类号: C07D417/12 , C07D417/14
CPC分类号: C07D417/12 , C07D417/14
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, rheumatoid arthritis and cancer.
摘要翻译: 本发明提供了式I的新型嘧啶胺,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,类风湿性关节炎和癌症。
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8.THIAZOLE-SUBSTITUTED AMINOHETEROARYLS AS SPLEEN TYROSINE KINASE INHIBITORS 有权
标题翻译: 噻唑替代氨基酸作为分离型酪氨酸激酶抑制剂公开(公告)号:US20160060255A1
公开(公告)日:2016-03-03
申请号:US14786464
申请日:2014-04-22
申请人: Neville J. ANTHONY , Brain M. ANDERSEN , Alan B. NORTHRUP , Kaleen K. CHILDERS , Anthony FRIO , Thomas A. MILLER , Yuan LIU , Michelle R. MACHACEK , Hyun Chong WOO , Kerrie B. SPENCER , John Michael ELLIS , Micheal D. ALTMAN , Eric T. ROMEO , Daniel GUAY , Jonathan GRIMM , Marie-Eve LEBRUN , Joel S. ROBICHAUD , Liping WANG , Byron DUBOIS , Qiaolin DENG , MERICK SHARP & DOHNE CORP. , MERCK CANADA INC.
发明人: Neville J. Anthony , Brian M. Andresen , Alan B. Northrup , Kaleen K. Childers , Anthony Donofrio , Thomas A. Miller , Yuan Liu , Michelle R. Machacek , Hyun Chong Woo , Kerrie B. Spencer , John Michael Ellis , Michael D. Altman , Eric T. Romeo , Daniel Guay , Jonathan Grimm , Marie-Eve Lebrun , Joel S. Robichaud , Liping Wang , Byron DuBois , Qiaolin Deng
IPC分类号: C07D417/14 , A61K31/53 , A61K31/4439 , A61K31/501 , A61K31/506 , A61K31/497
CPC分类号: C07D417/14 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/53 , C07D417/12
摘要: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, and R4 are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
摘要翻译: 本发明提供式(I)的某些噻唑取代的氨基杂芳基化合物或其药学上可接受的盐,其中X 1,X 2,X 3,X 4,Y 1,Y 2,Y 3,Y 4和R 4如本文所定义。 本发明还提供包含这些化合物的药物组合物,以及使用该化合物治疗由脾脏酪氨酸激酶(Syk)介导的疾病或病症的方法。
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公开(公告)号:US20090062297A1
公开(公告)日:2009-03-05
申请号:US12087623
申请日:2007-01-08
IPC分类号: A61K31/496 , C07D333/24 , A61K31/381 , A61K31/422 , C07D413/12 , C07D333/70
CPC分类号: C07D333/70 , C07D333/20 , C07D413/12
摘要: The present invention relates to a novel class of hydroxyalkylarylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.
摘要翻译: 本发明涉及一类新的羟烷基芳基酰胺衍生物。 本发明化合物可用于治疗癌症。 氟化芳基酰胺衍生物还可以抑制组蛋白脱乙酰酶,并且适用于选择性诱导终末分化,并阻止肿瘤细胞的细胞生长和/或凋亡,从而抑制这些细胞的增殖。 因此,本发明的化合物可用于治疗具有以肿瘤细胞增殖为特征的肿瘤的患者。 本发明的化合物还可用于预防和治疗TRX介导的疾病,例如自身免疫性,过敏性和炎性疾病,以及预防和/或治疗中枢神经系统(CNS)的疾病,例如 神经退行性疾病 本发明进一步提供包含异羟肟酸衍生物和这些药物组合物的安全投药方案的药物组合物,它们易于遵循,并且其在体内导致治疗有效量的异羟肟酸衍生物。
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公开(公告)号:US08868596B2
公开(公告)日:2014-10-21
申请号:US13451827
申请日:2012-04-20
IPC分类号: G06F17/30
CPC分类号: G06Q30/0631 , G06F17/30867
摘要: A system for generating one or more recommended items for a user receives a target items set for the user which includes two or more target items. The system then queries a database of a plurality of related items sets using the target items set, where each related items set comprises a plurality of related items. In response to the querying, the system retrieves one or more similar items sets from the plurality of related item sets, each similar items set being similar to the target items set. The system then performs a union of the similar items sets to generate the recommended items.
摘要翻译: 用于为用户生成一个或多个推荐项目的系统接收包括两个或多个目标项目的用户的目标项集合。 然后,系统使用目标项集合查询多个相关项目集合的数据库,其中每个相关项集合包括多个相关项目。 响应于查询,系统从多个相关项目集中检索一个或多个类似的项目集合,每个相似项目集合与目标项集合相似。 然后,系统执行类似项目集合的并集以生成推荐项目。
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