📜(-)-(S)-N-(5-氨基-2-甲基-3-苯基-L,2-二氢吡啶并[3,4-B]吡嗪-7-基)氨基甲酸乙酯 反应生成(-)-(S)-N-(5-氨基-2-甲基-3-苯基-L,2-二氢吡啶并[3,4-B]吡嗪-7-基)氨基甲酸乙酯2-羟基乙基磺酸盐 参考文献:Journal Of Labelled Compounds And Radiopharmaceuticals 1994,34,11-16 标题:Journal Of Labelled Compounds And Radiopharmaceuticals 1994,34,11-16
专利号:US-8598153-B2 优先权日:2006-09-22 标题 :Method of treatment using fatty acid synthesis inhibitors 发明人:SINGH SHEO B; TOTA MICHAEL R; WANG JUN 权利人:SINGH SHEO B; TOTA MICHAEL R; WANG JUN; MERCK SHARP & DOHME 摘要:The present invention relates to natural products that possess fatty acid synthesis inhibitor activity and can be used to treat and prevent diseases such as obesity, cancer, diabetes, fungal infections, Mycobacterium tuberculosis infections, malarial infections and other apicomplexan protozoal diseases.
专利号:US-10793557-B2 优先权日:2018-04-03 标题 :Sting agonist compounds 发明人:ALTMAN MICHAEL D; CASH BRANDON D; CHILDERS MATTHEW LLOYD; CUMMING JARED N; DEMONG DUANE E; HAIDLE ANDREW MARC; HENDERSON TIMOTHY J; JEWELL JAMES P; LARSEN MATTHEW A; LIM JONGWON; LU MIN; OTTE RYAN D; TROTTER BENJAMIN WESLEY 权利人:MERCK SHARP & DOHME 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.
专利号:US-2011104052-A1 优先权日:2007-12-03 标 题 :Methods of synthesis and use of chemospheres 发明人:BARNETT BRADLEY POWERS; GESCHWIND JEFFREY 权利人:UNIV JOHNS HOPKINS 摘要:The present invention provides, in general, compositions comprising a hydrogel and an agent, for example a therapeutic agent or an imaging agent, for locoregional delivery. In certain preferred embodiments of the invention, the hydrogel compositions are detectable by Magnetic Responance and CT Scan and are used for locoregional delivery of therapeutic agents, for example chemotherapeutic agents. The invention also features polymer matrix compositions comprising nanoparticles that can be loaded after polymerization with bioactive agents, for example a diagnostic agent or therapeutic agent.
专利号:US-11702430-B2 优先权日:2018-04-03 标 题:Aza-benzothiophene compounds as STING agonists 发明人:ALTMAN MICHAEL D; CASH BRANDON D; CUMMING JARED N; DEMONG DUANE E; HAIDLE ANDREW M; JEWELL JAMES P; LARSEN MATTHEW A; LU MIN; OTTE RYAN D; TAOKA BRANDON M; TROTTER BENJAMIN WESLEY; TRUONG QUANG T 权利人:MERCK SHARP & DOHME LLC; ALTMAN MICHAEL D; CASH BRANDON D; CUMMING JARED N; DEMONG DUANE E; HAIDLE ANDREW M; JEWELL JAMES P; LARSEN MATTHEW A; LU MIN; OTTE RYAN D; TAOKA BRANDON M; TROTTER BENJAMIN WESLEY; TRUONG QUANG T 摘要:Compounds of general formula (I), and their pharmaceutically acceptable salts, wherein R 1 , R 2 , R 3 , R 5 , R 6 , R 8 , R 9 , A, X 1 , X 2 , and X 3 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.
专利号:US-11685761-B2 优先权日:2017-12-20 标 题:Cyclic di-nucleotide compounds as sting agonists 发明人:ANDRESEN BRIAN M; BENNETT FRANK; CHANG WONSUK; CHILDERS MATTHEW LLOYD; CUMMING JARED N; LIM JONGWON; LU MIN; TROTTER BENJAMIN WESLEY; WU WEN-LIAN 权利人:MERCK SHARP & DOHME; ANDRESEN BRIAN M; BENNETT FRANK; CHANG WONSUK; CHILDERS MATTHEW LLOYD; CUMMING JARED N; LIM JONGWON; LU MIN; TROTTER BENJAMIN WESLEY; WU WEN LIAN; MERCK SHARP & DOHME LLC 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.
专利号:US-10766919-B2 优先权日:2015-08-13 标 题 :Cyclic di-nucleotide compounds as sting agonists 发明人:ALTMAN MICHAEL D; ANDRESEN BRIAN; CHANG WONSUK; CHILDERS MATTHEW LLOYD; CUMMING JARED N; HAIDLE ANDREW MARC; HENDERSON TIMOTHY J; JEWELL JAMES P; LIANG RUI; LIM JONGWON; LIU HONG; LU MIN; NORTHRUP ALAN B; OTTE RYAN D; SIU TONY; TROTTER BENJAMIN WESLEY; TRUONG QUANG T; WALSH SHAWN P; ZHAO KAKE 权利人:MERCK SHARP & DOHME 摘要:A class of polycyclic compounds of general formula (I), of general formula (I′), or of general formula (I″), wherein Base 1 , Base 2 , Y, Y a , X a , X a1 , X b , X b1 , X c , X c1 , X d , X d1 , R 1 , R 1a , R 2 , R 2a , R 3 , R 4 , R 4a , R 5 , R 6 , R 6a , R 7 , R 7a , R 8 , and R 8a 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.
1: Kunschner LJ, Fine H, Hess K, Jaeckle K, Kyritsis AP, Yung WK. CI-980 for the treatment of recurrent or progressive malignant gliomas: national central nervous system consortium phase I-II evaluation of CI-980. Cancer Invest. 2002;20(7-8):948-54. . A phase II study of CI-980 in previously untreated extensive small cell lung cancer: an Ohio State University phase II research consortium study. Cancer Invest. 2002;20(2):192-8. 15: Barbier P, Peyrot V, Dumortier C, D'Hoore A, Rener GA, Engelborghs Y. Kinetics of association and dissociation of two enantiomers, NSC 613863 (R)-(+) and NSC 613862 (S)-(-) (CI 980), to tubulin. Biochemistry. 1996 Feb 13;35(6):2008-15.
合成参考文献
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