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公开(公告)号:US20170369507A1
公开(公告)日:2017-12-28
申请号:US15532549
申请日:2015-12-01
Applicant: Merck Sharp & Dohme Corp.
Inventor: Fischer Christian , Stephane L. Bogen , Matthew L. Childers , Francesc Xavier Fradera Llinas , Michael J. Ellis , Sara Esposite , Qingmei Hong , Chunhui Huang , Alexander J. Kim , John W. Lampe , Michelle R. Machacek , Daniel R. McMasters , Ryan D. Otte , Dann L. Parker, Jr. , Michael H. Reutershan , Nunzio Sciammetta , Patrick Pengcheng Shao , David L. Sloman , Feroze Ujjainwalla , Catherine White , Zhicai Wu , Yang Yu , Kake Zhao , Craig R. Gibeau
IPC: C07D498/08 , C07D471/04 , C07D498/10 , C07D471/08 , A01N43/00
CPC classification number: C07D498/08 , A01N43/00 , A61K31/551 , C07D471/04 , C07D471/08 , C07D471/14 , C07D498/04 , C07D498/10
Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
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公开(公告)号:US20180237469A1
公开(公告)日:2018-08-23
申请号:US15886578
申请日:2018-02-01
Applicant: Merck Sharp & Dohme Corp.
Inventor: Michael D. Altman , Brian Andresen , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , Andrew Marc Haidle , Timothy J. Henderson , James P. Jewell , Rui Liang , Jongwon Lim , Hong Liu , Min Lu , Alan B. Northrup , Ryan D. Otte , Tony Siu , Benjamin Wesley Trotter , Quang T. Truong , Shawn P. Walsh , Kake Zhao
IPC: C07H21/04 , C07H19/23 , C07H21/00 , C07H19/20 , A61K39/39 , C07H21/02 , A61K31/7076 , A61K31/708 , A61K31/706 , A61K31/7084 , A61K31/7064
Abstract: A class of polycyclic compounds of general formula (I), of general formula (I′), or of general formula (I″), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, 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:US20180244712A1
公开(公告)日:2018-08-30
申请号:US15886568
申请日:2018-02-01
Applicant: Merck Sharp & Dohme Corp.
Inventor: Michael D. Altman , Brian Andresen , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , Andrew Marc Haidle , Timothy J. Henderson , James P. Jewell , Rui Liang , Jongwon Lim , Hong Liu , Min Lu , Alan B. Northrup , Ryan D. Otte , Tony Siu , Benjamin Wesley Trotter , Quang T. Truong , Shawn P. Walsh , Kake Zhao
IPC: C07H21/04 , C07H21/02 , C07H21/00 , C07H19/23 , C07H19/20 , A61K39/39 , A61K31/7084 , A61K31/708 , A61K31/7076 , A61K31/7064 , A61K31/706
Abstract: A class of polycyclic compounds of general formula (I), of general formula (I′), or of general formula (I″), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, 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:US20210395255A1
公开(公告)日:2021-12-23
申请号:US17292511
申请日:2019-11-15
Applicant: Zachary G. BRILL , Amjad ALI , Jared CUMMING , Duane DEMONG , Qiaolin DENG , Thomas H. GRAHAM , Rongze KUANG , Yeon-Hee LIM , Christopher W. PLUMMER , Jenny Lorena RICO DUQUE , Huijun WANG , Yonglian ZHANG , Kake ZHAO , Merck Sharp & Dohme Corp.
Inventor: Zachary G. Brill , Amjad Ali , Jared Cumming , Duane DeMong , Qiaolin Deng , Thomas H. Graham , Rongze Kuang , Yeon-Hee Lim , Christopher W. Plummer , Jenny Lorena Rico Duque , Huijun Wang , Yonglian Zhang , Kake Zhao
IPC: C07D487/04 , C07K16/28
Abstract: In its many embodiments, the present invention provides certain substituted amino triazolopyrimidine and amino triazolopyrazine compounds of Formula (IA) and Formula (IB): or and pharmaceutically acceptable salts thereof, wherein, R1, R2, and R3 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and their use in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.
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公开(公告)号:US10766919B2
公开(公告)日:2020-09-08
申请号:US15886578
申请日:2018-02-01
Applicant: Merck Sharp & Dohme Corp.
Inventor: Michael D. Altman , Brian Andresen , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , Andrew Marc Haidle , Timothy J. Henderson , James P. Jewell , Rui Liang , Jongwon Lim , Hong Liu , Min Lu , Alan B. Northrup , Ryan D. Otte , Tony Siu , Benjamin Wesley Trotter , Quang T. Truong , Shawn P. Walsh , Kake Zhao
IPC: 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
Abstract: A class of polycyclic compounds of general formula (I), of general formula (I′), or of general formula (I″), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, 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:US20170044206A1
公开(公告)日:2017-02-16
申请号:US15234182
申请日:2016-08-11
Applicant: Merck Sharp & Dohme Corp.
Inventor: Michael D. Altman , Brian Michael Andresen , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , Andrew Marc Haidle , Timothy J. Henderson , James P. Jewell , Rui Liang , Jongwon Lim , Hong Liu , Min Lu , Alan B. Northrup , Ryan D. Otte , Tony Siu , Benjamin Wesley Trotter , Quang T. Truong , Shawn P. Walsh , Kake Zhao
CPC classification number: C07H21/04 , A61K31/706 , A61K31/7064 , A61K31/7076 , A61K31/708 , A61K31/7084 , A61K39/39 , A61P35/00 , C07H19/20 , C07H19/23 , C07H21/00 , C07H21/02
Abstract: A class of polycyclic compounds of general formula (I), of general formula (I′), or of general formula (I″), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, 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.
Abstract translation: 一类通式(I),通式(I')或通式(I“)的多环化合物,其中基团1,碱基2,Y,亚氨基,Xa,Xa1,Xb,Xb1,Xc,Xc1, Xd,Xd1,R1,R1a,R2,R2a,R3,R4,R4a,R5,R6,R6a,R7,R7a,R8和R8a在本文中定义,其可用作I型干扰素生产的电感器, 提供了STING活性剂,还提供了合成和使用化合物的方法。
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公开(公告)号:US10759825B2
公开(公告)日:2020-09-01
申请号:US15886568
申请日:2018-02-01
Applicant: Merck Sharp & Dohme Corp.
Inventor: Michael D. Altman , Brian Andresen , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , James P. Jewell , Jongwon Lim , Alan B. Northrup , Ryan D. Otte , Benjamin Wesley Trotter , Quang T. Truong , Shawn P. Walsh , Kake Zhao
IPC: 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
Abstract: A class of polycyclic compounds of general formula (I), of general formula (I′), or of general formula (I″), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, 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:US20140357632A1
公开(公告)日:2014-12-04
申请号:US14239452
申请日:2012-08-13
Applicant: MERCK SHARP & DOHME CORP.
Inventor: Rajan Anand , Vincent J. Colandrea , Maud Reiter , Petr Vachal , Aaron Zwicker , Jonathan E. Wilson , Fengqi Zhang , Kake Zhao
IPC: C07D409/06 , A61K31/498 , C07D401/04 , C07D403/04 , A61K45/06 , C07D401/06 , C07D405/04 , A61K31/5377 , C07D405/06 , C07D241/42 , A61K31/506
CPC classification number: C07D409/06 , A61K31/498 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D241/42 , C07D401/04 , C07D401/06 , C07D403/04 , C07D405/04 , C07D405/06
Abstract: Compounds having the structure of Formula Ia, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
Abstract translation: 具有式Ia结构的化合物,包括化合物的药学上可接受的盐,是CETP抑制剂,可用于培养HDL-胆固醇,降低LDL-胆固醇,以及用于治疗或预防动脉粥样硬化。
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