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公开(公告)号：US10738074B2
公开(公告)日：2020-08-11
申请号：US15752144
申请日：2016-08-11
申请人： Merck Sharp & Dohme Corp. , Michael D. Altman , Brian Andresen , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , Andrew Marc Haidle , Timothy J. Henderson , James P. Jewell , Min Lu , Alan B. Northrup , Ryan D. Otte , Tony Siu , Benjamin Wesley Trotter , Quang T. Truong
发明人： Michael D. Altman , Brian Andresen , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , Andrew Marc Haidle , Timothy J. Henderson , James P. Jewell , Min Lu , Alan B. Northrup , Ryan D. Otte , Tony Siu , Benjamin Wesley Trotter , Quang T. Truong
IPC分类号： A01N43/04 , A61K31/70 , C07H21/04 , C07H21/02 , A61K39/39 , C07H19/20 , C07H19/23 , C07H21/00 , A61P35/00 , A61K31/7064 , A61K31/7084 , A61K31/708 , A61K31/706 , A61K31/7076
摘要： A class of polycyclic compounds of general formula (II), of general formula (II′), or of general formula (II″), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3a, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.
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公开(公告)号：US20180051028A1
公开(公告)日：2018-02-22
申请号：US15557197
申请日：2016-03-07
申请人： JONGWON LIM , MICHAEL D. ALTMAN , JASON D. BRUBAKER , CRAIG R. GIBEAU , MERCK SHARP & DOHME CORP.
IPC分类号： C07D487/04 , A61K31/519 , A61K45/06 , A61K31/551 , C07D519/00 , A61K31/55 , A61K31/553
CPC分类号： C07D487/04 , A61K31/519 , A61K31/55 , A61K31/551 , A61K31/553 , A61K45/06 , A61P29/00 , C07D519/00
摘要： The present invention relates to pyrazolopyrimidine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
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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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![Pyrazolo[1,5-A]pyrimidines as mark inhibitors](/abs-image/US/2015/02/03/US08946237B2/abs.jpg.150x150.jpg)
公开(公告)号：US08946237B2
公开(公告)日：2015-02-03
申请号：US13521382
申请日：2011-01-11
申请人： Jongwon Lim , Brandon M. Taoka , Sandra Lee , Alan Northrup , Michael D. Altman , David L. Sloman , Matthew G. Stanton , Njamkou Noucti
发明人： Jongwon Lim , Brandon M. Taoka , Sandra Lee , Alan Northrup , Michael D. Altman , David L. Sloman , Matthew G. Stanton , Njamkou Noucti
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention encompasses pyrazolo[1,5-a]pyrimidine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.
摘要翻译： 本发明包括选择性抑制微管亲和调节激酶（MARK）的吡唑并[1,5-a]嘧啶衍生物，因此可用于治疗或预防阿尔茨海默氏病。 还包括药物组合物和使用方法。
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![Imidazo[1,2-a]pyridines and imidazo[1,2-b]pyridazines as mark inhibitors](/abs-image/US/2013/11/26/US08592425B2/abs.jpg.150x150.jpg)
6.发明授权Imidazo[1,2-a]pyridines and imidazo[1,2-b]pyridazines as mark inhibitors 有权咪唑并[1,2-a]吡啶和咪唑并[1,2-b]哒嗪作为标记抑制剂公开(公告)号：US08592425B2
公开(公告)日：2013-11-26
申请号：US13144123
申请日：2010-01-12
申请人： Michael D. Altman , Mark T. Bilodeau , Jongwon Lim , Alan Northrup , Matthew G. Stanton , Brandon M. Taoka
发明人： Michael D. Altman , Mark T. Bilodeau , Jongwon Lim , Alan Northrup , Matthew G. Stanton , Brandon M. Taoka
IPC分类号： A01N43/58 , A61K31/50 , C07D487/00
CPC分类号： A61K31/5025 , C07D471/04 , C07D487/04
摘要： The invention encompasses imidazo[1,2-a]pyridine and imidazo[1,2-b]pyridazine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.
摘要翻译： 本发明包括选择性抑制微管亲和调节激酶（MARK）的咪唑并[1,2-a]吡啶和咪唑并[1,2-b]哒嗪衍生物，因此可用于治疗或预防阿尔茨海默氏病。 还包括药物组合物和使用方法。
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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：US10329295B2
公开(公告)日：2019-06-25
申请号：US15557203
申请日：2016-03-07
申请人： MERCK SHARP & DOHME CORP. , Jongwon Lim , Michael D. Altman , Jason D. Brubaker , Craig R. Gibeau
IPC分类号： C07D487/04 , A61K31/519 , A61K31/53 , A61K45/06 , C07D403/14 , A61P29/00
摘要： The present invention relates to pyrrolotriazine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
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公开(公告)号：US20180051029A1
公开(公告)日：2018-02-22
申请号：US15557201
申请日：2016-03-07
申请人： JONGWON LIM , MICHAEL D. ALTMAN , JASON D. BRUBAKER , CRAIG R. GIBEAU , MERCK SHARP & DOHME CORP.
IPC分类号： C07D487/04 , A61K45/06 , A61K31/5025 , C07D519/00 , A61K31/551 , A61K31/55
CPC分类号： C07D487/04 , A61K31/5025 , A61K31/55 , A61K31/551 , A61K45/06 , C07D519/00
摘要： The present invention relates to pyrrolopyridazine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
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公开(公告)号：US20170275297A1
公开(公告)日：2017-09-28
申请号：US15515383
申请日：2015-09-25
申请人： Michael D. ALTMAN , Brian M. ANDRESEN , Jason D. BRUBAKER , Matthew L. CHILDERS , Anthony DONOFRIO , Thierry FISCHMANN , Craig R. GIBEAU , Solomon D. KATTAR , Charles A. LESBURG , Jongwon LIM , John K.F. MACLEAN , Umar F. MANSOOR , Alan B. NORTHRUP , John SANDERS , Graham F. SMITH , Luis TORRES
发明人： MICHAEL D. ALTMAN , BRIAN M. ANDRESEN , JASON D. BRUBAKER , MATTHEW L. CHILDERS , ANTHONY DONOFRIO , THIERRY FISCHMANN , CRAIG R. GIBEAU , SOLOMON D. KATTAR , CHARLES A. LESBURG , JONGWON LIM , JOHN K.F. MACLEAN , UMAR F. MANSOOR , ALAN B. NORTHRUP , JOHN M. SANDERS , LUIS TORRES
IPC分类号： C07D498/04 , A61K31/517 , C07D403/04 , C07D239/94 , C07D401/04 , A61K31/5377 , C07D405/14 , C07D401/14 , C07D413/04 , C07D405/04 , C07D471/04 , A61K31/5383 , C07D491/048 , C07D417/04 , C07D409/04 , A61K45/06
CPC分类号： C07D498/04 , A61K31/517 , A61K31/5377 , A61K31/5383 , A61K45/06 , A61P37/00 , C07D239/94 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D491/048 , A61K2300/00
摘要： The present invention relates to inhibitors of IRAK4 of Formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
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