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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：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：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：US11542505B1
公开(公告)日：2023-01-03
申请号：US17047271
申请日：2019-04-15
申请人： Merck Sharp & Dohme Corp. , Craig A. Parish , Hongwu Wang , Wonsuk Chang , Quang T. Truong , Tony Siu , Anne Mai Wassermann
发明人： Craig A. Parish , Hongwu Wang , Wonsuk Chang , Quang T. Truong , Tony Siu , Anne Mai Wassermann
IPC分类号： C12N15/113 , C07H21/02
摘要： This invention provides compositions, compounds, and uses thereof, wherein said compounds comprise a single strand oligonucleotide that may form a short oligonucleotide hairpin or stem loop molecule with self complementary base pairing of less than 12 base pairs that bind to RIG-I and activate the RIG-I pathway.
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![Benzo[b]thiophene compounds as sting agonists](/abs-image/US/2019/09/17/US10414747B2/abs.jpg.150x150.jpg)
公开(公告)号：US10414747B2
公开(公告)日：2019-09-17
申请号：US15722093
申请日：2017-10-02
发明人： Michael D. Altman , Brandon D. Cash , Wonsuk Chang , Jared N. Cumming , Andrew M. Haidle , Timothy J. Henderson , James P. Jewell , Matthew A. Larsen , Rui Liang , Jongwon Lim , Min Lu , Ryan D. Otte , Tony Siu , Benjamin Wesley Trotter , Sriram Tyagarajan
IPC分类号： C07D333/60 , C07D333/62 , C07D409/12 , C07D498/04
摘要： Compounds of general formula (Ia), compounds of general formula (Ia′), compounds of general formula (Ib), compounds of general formula (Ib′), compounds of general formula (I), compounds of general formula (I′), and their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, R6, R8, R9, 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 processes for the synthesis and use of compounds of the disclosure.
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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
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 , 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分类号： C07H21/04 , C07H21/02 , C07H21/00 , C07H19/23 , C07H19/20 , A61K39/39 , A61K31/7084 , A61K31/708 , A61K31/7076 , A61K31/7064 , A61K31/706
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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![BENZO[b]THIOPHENE COMPOUNDS AS STING AGONISTS](/abs-image/US/2018/04/05/US20180093964A1/abs.jpg.150x150.jpg)
公开(公告)号：US20180093964A1
公开(公告)日：2018-04-05
申请号：US15722093
申请日：2017-10-02
发明人： Michael D. Altman , Brandon D. Cash , Wonsuk Chang , Jared N. Cumming , Andrew M. Haidle , Timothy J. Henderson , James P. Jewell , Matthew A. Larsen , Rui Liang , Jongwon Lim , Min Lu , Ryan D. Otte , Tony Siu , Benjamin Wesley Trotter , Sriram Tyagarajan
IPC分类号： C07D333/60 , C07D333/62 , C07D409/12 , C07D498/04
CPC分类号： C07D333/60 , C07D333/62 , C07D409/12 , C07D498/04
摘要： Compounds of general formula (Ia), compounds of general formula (Ia′), compounds of general formula (Ib), compounds of general formula (Ib′), compounds of general formula (I), compounds of general formula (I′), and their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, R6, R8, R9, 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 processes for the synthesis and use of compounds of the disclosure.
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公开(公告)号：US10246457B2
公开(公告)日：2019-04-02
申请号：US15564352
申请日：2016-04-04
发明人： Tony Siu , Michael D. Altman , Brian M. Andresen , Jian Liu , Joseph Kozlowski , Sobhana Babu Boga , Younong Yu , Rajan Anand , Jiaqiang Cai , Dahai Wang , Shilan Liu
IPC分类号： C07D471/04 , C07D401/14 , C07D405/14 , C07D401/10 , C07D403/04 , C07D403/10 , C07D403/14 , C07D409/14 , A61P19/02 , A61K45/06 , C07D231/56 , C07D413/14
摘要： The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R7, R8 and R9 are as herein described. The present invention also provides pharmaceutical compositions comprising these compounds and methods for their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated disorders.
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公开(公告)号：US20150191461A1
公开(公告)日：2015-07-09
申请号：US14409133
申请日：2013-06-18
发明人： Michelle R. Machacek , Michael D. Altman , Eric T. Romeo , Dilrukshi Vitharana , Brandon Cash , Tony Siu , Matthew Christopher , Solomon D. Kattar , Andrew M. Haidle , Kaleen Konrad Childers , Matthew L. Maddess , Michael H. Reutershan , Yves Ducharme , David J. Guerin , Kerrie Spencer , Christian Beaulieu , Vouy Linh Truong , Daniel Guay , Alan B. Northrup , Brandon M. Taoka , Jongwon Lim , Christian Fischer , John W. Butcher , Ryan D. Otte , Binyuan Sun , John Michael Ellis
IPC分类号： C07D471/04 , C07D401/14 , C07D413/14 , C07D409/14 , C07D403/14 , C07D403/12
CPC分类号： C07D471/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention provides novel pyrazole derivatives 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, rheumatoid arthritis, and cancer.
摘要翻译： 本发明提供了式I的新型吡唑衍生物，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，类风湿性关节炎和癌症。
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