专利检索 ap:("Neville J. ANTHONY" OR "Brain M. ANDERSEN" OR "Alan B. NORTHRUP" OR "Kaleen K. CHILDERS" OR "Anthony FRIO" OR "Thomas A. MILLER" OR "Yuan LIU" OR "Michelle R. MACHACEK" OR "Hyun Chong WOO" OR "Kerrie B. SPENCER" OR "John Michael ELLIS" OR "Micheal D. ALTMAN" OR "Eric T. ROMEO" OR "Daniel GUAY" OR "Jonathan GRIMM" OR "Marie-Eve LEBRUN" OR "Joel S. ROBICHAUD" OR "Liping WANG" OR "Byron DUBOIS" OR "Qiaolin DENG" OR "MERICK SHARP & DOHNE CORP." OR "MERCK CANADA INC.") AND inv:"Eric T. Romeo" 第 1 页

1.

发明申请
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。

2.

发明申请
Aminopyrimidines as SYK Inhibitors 审中-公开
标题翻译：氨基嘧啶类作为SYK抑制剂

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。

3.

发明授权
Triazolyl derivatives as Syk inhibitors 有权
标题翻译：三唑基衍生物作为Syk抑制剂

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。

4.

发明申请
TRIAZOLYL DERIVATIVES AS SYK INHIBITORS 有权
标题翻译：三唑衍生物作为SYK抑制剂

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。

5.

发明申请
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：US20160326156A1

公开(公告)日：2016-11-10

申请号：US15105316

申请日：2014-12-18

申请人： Thomas A. MILLER , Alessia PETROCCHI , Eric T. ROMEO , Dilrukshi VITHARANA , Solomon D. KATTAR , Alan B. NORTHRUP , Michael D. ALTMAN , Neville J. ANTHONY , MERCK SHARP & DOHME CORP.

发明人： Thomas A. Miller , Alessia Petrocchi , Eric T. Romeo , Dilrukshi Vitharana , Solomon D. Kattar , Alan B. Northrup , Michael D. Altman , Neville J. Anthony

IPC分类号： C07D417/12 , C07D495/04 , A61K31/437 , C07D471/04 , A61K31/444 , C07D491/048 , A61K31/517 , A61K31/519

CPC分类号： C07D417/12 , A61K31/437 , A61K31/444 , A61K31/517 , A61K31/519 , C07D413/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04

摘要： The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring A, and the subscripts n1, n2, and r 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： 本发明提供了式（I）（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R 1，R 2，R 3，R 4，环A和下标n 1，n 2和r如上定义这里。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。

6.

发明申请
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：US20160311813A1

公开(公告)日：2016-10-27

申请号：US15105411

申请日：2014-12-15

申请人： Michelle R. MACHACEK , Eric T. ROMEO , Alan B. NORTHUP , Michael D. ALTMAN , MERCK SHARP & DOHME CORP.

发明人： Michelle R. Machacek , Eric T. Romeo , Alan B.. Nortrup , Michael D. Altman

IPC分类号： C07D417/12 , A61K31/5377 , A61K31/433 , A61K31/427 , A61K45/06

CPC分类号： C07D417/12 , A61K31/427 , A61K31/433 , A61K31/5377 , A61K45/06

摘要： The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R3, R5, R6, A, Cy and the subscripts r, s, and t 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).