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公开(公告)号：US11311528B2
公开(公告)日：2022-04-26
申请号：US16980594
申请日：2019-03-15
申请人： Merck Sharp & Dohme Corp. , Michael D. Altman , Matthew L. Childers , James P. Jewell , Charles A. Lesburg , Tony Siu
IPC分类号： C07D405/10 , C07D405/14 , C07D409/04 , C07D411/04 , C07D413/04 , C07D413/14 , C07D417/14 , A61K31/4725 , A61K31/497 , A61K31/5377 , A61K31/538
摘要： The instant invention provides compounds of formula I which are STING inhibitors, and as such are useful for the treatment of STING-mediated diseases such as inflammation, asthma, COPD and cancer.
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公开(公告)号：US20210052573A1
公开(公告)日：2021-02-25
申请号：US16980594
申请日：2019-03-15
申请人： Michael D. NEEDHAM , Matthew L. CHILDERS , James P. JEWELL , Charles A. LESBURG , Tony SIU , Merck Sharp & Dohme Corp.
IPC分类号： A61K31/4725 , C07D405/10 , C07D413/14 , C07D405/14 , C07D417/14 , C07D413/04 , C07D409/04 , C07D411/04 , A61K31/5377 , A61K31/497 , A61K31/538
摘要： The instant invention provides compounds of formula I which are STING inhibitors, and as such are useful for the treatment of STING-mediated diseases such as inflammation, asthma, COPD and cancer.
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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：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：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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6.发明申请公开(公告)号：US20150299125A1
公开(公告)日：2015-10-22
申请号：US14440517
申请日：2013-11-04
申请人： Andrew M. HAIDLE , Brandon CASH , James P. JEWELL , Kerrie SPENCER , Michael D. ALTMAN , Ryan D. OTTE , Alan B. NORTHRUP , MERCK SHARP & DOHME CORP.
发明人： Andrew M. Haidle , Brandon Cash , James P. Jewell , Kerrie Spencer , Michael D. Altman , Ryan D. Otte , Alan B. Northrup
IPC分类号： C07D213/74 , C07D401/14 , C07D405/14
CPC分类号： C07D213/74 , C07D401/14 , C07D405/14 , C07D451/10 , C07H13/08
摘要： The present invention provides compounds of Formula (I), which are prodrugs of trans-4-[(1R)-(6-{[4-(difluoromethyl)pyridin-2-yl]amino}-4-methyl-2,3′-bipyridin-6′-yl)-1-hydroxyethyl]cyclohexanecarboxylic acid, a potent inhibitor of Syk. The compounds are useful in the treatment and prevention of diseases mediated by the enzyme, such as asthma, COPD, rheumatoid arthritis and cancer.
摘要翻译： 本发明提供式（I）化合物，其为反式-4 - [（1R） - （6 - {[4-（二氟甲基）吡啶-2-基]氨基} -4-甲基-2,3 “ - 联吡啶-6'-基）-1-羟乙基]环己烷羧酸，Syk的有效抑制剂。 该化合物可用于治疗和预防由酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。
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公开(公告)号：US11702430B2
公开(公告)日：2023-07-18
申请号：US17040192
申请日：2019-03-28
申请人： Merck Sharp & Dohme LLC , 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
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 , C07D277/64 , A61P37/04 , A61P35/00
CPC分类号： C07D513/04 , A61P37/04 , C07D495/04
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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8.发明授权2-Pyridyl carboxamide-containing spleen tyrosine kinase (SYK) inhibitors 有权含2-吡啶甲酰胺的脾脏酪氨酸激酶（SYK）抑制剂公开(公告)号：US09216173B2
公开(公告)日：2015-12-22
申请号：US14349551
申请日：2012-10-01
申请人： Michael D. Altman , Corey E. Bienstock , John W. Butcher , Kaleen Konrad Childers , Maria Emilia Di Francesco , Anthony Donofrio , John Michael Ellis , Christian Fischer , Andrew M. Haidle , James P. Jewell , Sandra Lee Knowles , Alan B. Northrup , Ryan D. Otte , Scott L. Peterson , Graham Frank Smith
发明人： Michael D. Altman , Corey E. Bienstock , John W. Butcher , Kaleen Konrad Childers , Maria Emilia Di Francesco , Anthony Donofrio , John Michael Ellis , Christian Fischer , Andrew M. Haidle , James P. Jewell , Sandra Lee Knowles , Alan B. Northrup , Ryan D. Otte , Scott L. Peterson , Graham Frank Smith
IPC分类号： C07D213/73 , A61K31/4439 , C07D401/14 , C07D405/14 , C07D413/14 , C07D213/81 , C07D401/12 , C07D409/14 , C07D417/14 , C07D487/04 , C07D495/04 , A61K31/444 , A61K31/496 , A61K31/5025 , A61K31/506 , A61K31/519 , A61K31/5377
CPC分类号： A61K31/4439 , A61K31/444 , A61K31/496 , A61K31/5025 , A61K31/506 , A61K31/519 , A61K31/5377 , C07D213/81 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D495/04
摘要： The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B 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) kinase.
摘要翻译： 本发明提供了具有式（I）的某些含2-吡啶甲酰胺的化合物或其药学上可接受的盐，其中A和B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）激酶介导的疾病或病症的方法。
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公开(公告)号：US10793557B2
公开(公告)日：2020-10-06
申请号：US16372103
申请日：2019-04-01
发明人： Michael D. Altman , Brandon D. Cash , Matthew Lloyd Childers , Jared N. Cumming , Duane E. DeMong , Andrew Marc Haidle , Timothy J. Henderson , James P. Jewell , Matthew A. Larsen , Jongwon Lim , Min Lu , Ryan D. Otte , Benjamin Wesley Trotter
IPC分类号： C07D409/12 , C07D417/10 , C07D498/04 , C07D495/04 , C07D277/64 , C07D417/12 , C07D333/56 , A61P35/00
摘要： Compounds of general formula (I), of general formula (II), of general formula (III), of general formula (IV), of general formula (V), of general formula (VI), and their pharmaceutically acceptable salts, wherein all variables 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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公开(公告)号：US10759825B2
公开(公告)日：2020-09-01
申请号：US15886568
申请日：2018-02-01
发明人： 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 (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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