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公开(公告)号：US11685761B2
公开(公告)日：2023-06-27
申请号：US16771814
申请日：2018-12-17
申请人： Merck Sharp & Dohme Corp. , Brian M. Andresen , Frank Bennett , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , Jongwon Lim , Min Lu , Benjamin Wesley Trotter , Wen-Lian Wu
发明人： Brian M. Andresen , Frank Bennett , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , Jongwon Lim , Min Lu , Benjamin Wesley Trotter , Wen-Lian Wu
IPC分类号： C07H21/00 , A61P37/04 , C07H21/02 , A61K31/7084 , C07H21/04
CPC分类号： C07H21/00 , A61K31/7084 , A61P37/04 , C07H21/02 , C07H21/04 , C07B2200/07
摘要： A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Za, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, R8a, and R9 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：US20210206796A1
公开(公告)日：2021-07-08
申请号：US16771814
申请日：2018-12-17
申请人： Brian M. ANDRESEN , Frank BENNETT , Wonsuk CHANG , Matthew Lloyd CHILDERS , Jared N. CUMMING , Jongwon LIM , Min LU , Benjamin Wesley TROTTER , Wen-Lian WU , Merck Sharp & Dohme Corp.
发明人： Brian M. Andresen , Frank Bennett , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , Jongwon Lim , Min Lu , Benjamin Wesley Trotter , Wen-Lian Wu
摘要： A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Za, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, R8a and R9 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：US20200062798A1
公开(公告)日：2020-02-27
申请号：US16611624
申请日：2018-05-07
申请人： Wen-Lian WU , Jongwon LIM , Jared N. CUMMING , Benjamin Wesley TROTTER , Wonsuk CHANG , Merck Sharp & Dohme Corp.
IPC分类号： C07H21/00
摘要： A class of polycyclic compounds 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, R8a, and R9 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：US11466047B2
公开(公告)日：2022-10-11
申请号：US16611624
申请日：2018-05-07
申请人： Merck Sharp & Dohme Corp. , Wen-Lian Wu , Jongwon Lim , Jared N. Cumming , Benjamin Wesley Trotter , Wonsuk Chang
摘要： A class of polycyclic compounds 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, R8a, and R9 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：US20180230178A1
公开(公告)日：2018-08-16
申请号：US15752144
申请日：2016-08-11
申请人： 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 , Merck Sharp & Dohme Corp.
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
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：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：US20210009608A1
公开(公告)日：2021-01-14
申请号：US17040192
申请日：2019-03-28
申请人： Michael D. ALTMAN , Brandon D. CASH , Jared N. CUMMING , Duane E. DEMONG , Andrew M. HAIDLE , James P. JEWELL , Matthew A. LARSEN , Min LU , Ryan D. OTTE , Brandon M. TAOKA , Benjamin Wesley TROTTER , Quang T, TRUONG , Merck Sharp & Dohme Corp.
发明人： Michael D. Altman , Brandon D. Cash , Jared N. Cumming , Duane E. DeMong , Andrew M. Haidle , James P. Jewell , Matthew A. Larsen , Min Lu , Ryan D. Otte , Brandon M. Taoka , Benjamin Wesley Trotter , Quang T. Truong
IPC分类号： C07D513/04 , C07D495/04 , A61P37/04
摘要： Compounds of general formula (I), and their pharmaceutically acceptable salts, wherein R1, R2, R3, R5, R6, R8, R9, A, X1, X2, and X3 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer.
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![Combinations of PD-1 antagonists and benzo [b] thiophene STING agonists for cancer treatment](/abs-image/US/2022/04/26/US11312772B2/abs.jpg.150x150.jpg)
8.发明授权公开(公告)号：US11312772B2
公开(公告)日：2022-04-26
申请号：US16635059
申请日：2018-07-30
申请人： Merck Sharp & Dohme Corp. , Saso Cemerski , Jared N. Cumming , Johnny E. Kopinja , Samanthi A. Perera , Benjamin Wesley Trotter , Archie Ngai-Chiu Tse
发明人： Saso Cemerski , Jared N. Cumming , Johnny E. Kopinja , Samanthi A. Perera , Benjamin Wesley Trotter , Archie Ngai-Chiu Tse
IPC分类号： A61P35/00 , A61K31/381 , A61K39/00 , C07K16/28
摘要： Therapeutic combinations that comprise at least one antagonist of the Programmed Death 1 receptor (PD-1) and at least one benzo[b]thiophene compound that activates the Stimulator of Interferon Genes (STING) pathway are disclosed herein. Also disclosed is the use of such therapeutic combinations for the treatment of cancers.
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9.发明申请公开(公告)号：US20190218223A1
公开(公告)日：2019-07-18
申请号：US16324596
申请日：2017-08-10
申请人： Jared N. CUMMING , Kevin D. DYKSTRA , Alan HRUZA , Derun LI , Hong LIU , Haiqun TANG , Brandon M. TAOKA , Andreas VERRAS , Shawn P. WALSH , Wen-Lian WU , Merck Sharp & Dohme Corp.
发明人： Jared N. Cumming , Kevin D. Dykstra , Alan Hruza , Derun Li , Hong Liu , Haiqun Tang , Brandon M. Taoka , Andreas Verras , Shawn P. Walsh , Wen-Lian Wu
IPC分类号： C07D487/04 , C07D519/00 , C07D471/04 , C07D498/04 , C07D513/04 , A61P3/10
CPC分类号： C07D487/04 , A61P3/10 , C07D471/04 , C07D498/04 , C07D513/04 , C07D519/00
摘要： Described herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as Cyp8b1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for diabetes and cardiovascular disease.
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10.发明申请C2-AZASPIRO IMINOTHIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 有权C2-AZASPIRO三嗪类二氧化物作为BACE抑制剂，组合物及其使用公开(公告)号：US20160016975A1
公开(公告)日：2016-01-21
申请号：US14774204
申请日：2014-03-11
申请人： Eric J. GILBERT , Jared N. CUMMING , Jack D. SCOTT , Wen-Lian WU , Duane A. BURNETT , Andrew W. STAMFORD , MERCK SHARP & DOHME CORP.
发明人： Eric J. Gilbert , Jared N. Cumming , Jack D. Scott , Wen-Lian Wu , Duane A. Burnett , Andrew W. Stamford
IPC分类号： C07D513/10
CPC分类号： C07D513/10
摘要： In its many embodiments, the present invention provides certain C2-azaspiro substituted iminothiazine dioxide compounds. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
摘要翻译： 在其许多实施方案中，本发明提供某些C2-氮杂螺环取代的亚氨基噻嗪二氧化物化合物。 本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与其相关的各种病症。 还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括用于治疗阿尔茨海默氏病的药物组合物。
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