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公开(公告)号：US11053243B2
公开(公告)日：2021-07-06
申请号：US16829878
申请日：2020-03-25
发明人： Craig A. Coburn , Steven W. Ludmerer , Kun Liu , Hao Wu , Richard Soil , Bin Zhong , Jian Zhu
IPC分类号： C07D471/04 , C07D407/14 , C07D487/04 , C07D401/14 , C07D403/14 , C07D403/12 , C07D413/14 , C07D405/14 , C07D405/12 , C07D417/14 , C07D409/14 , A61K31/4985 , A61K31/4439 , A61K31/4184 , A61K31/423 , A61K31/4025 , A61K31/519 , A61K31/404 , A61K31/506 , A61K31/5377 , A61K31/427 , A61K31/4245 , A61K31/475 , A61K31/536 , A61K31/4178 , A61K31/517 , A61K31/5386 , A61K31/553 , A61K31/437
摘要： The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
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2.发明授权Sulfonamide derivatives and methods of use thereof for improving the pharmacokinetics of a drug 有权磺酰胺衍生物及其用于改善药物的药代动力学的方法公开(公告)号：US09556202B2
公开(公告)日：2017-01-31
申请号：US14410846
申请日：2013-06-25
发明人： Craig A. Coburn , Milana Maletic , Richard Soll , Chunsing Li , Yunfu Luo , Zhiqi Qi
IPC分类号： C07D498/04 , C07D417/10 , C07D417/12 , C07D417/14 , C07D487/04 , C07D401/14 , A61K31/496 , A61K31/4545 , A61K31/4985 , A61K31/4402 , A61K31/513 , A61K31/5377 , A61K31/5383 , C07D471/10 , C07D471/04 , A61K38/05 , C07D403/14 , C07D491/04 , A61K45/06
CPC分类号： C07D498/04 , A61K31/4402 , A61K31/496 , A61K31/4985 , A61K31/513 , A61K31/5377 , A61K31/5383 , A61K38/05 , A61K45/06 , C07D401/14 , C07D403/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D491/04
摘要： The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.
摘要翻译： 本发明涉及式（I）的磺酰胺衍生物及其药学上可接受的盐，其中A，W，X，R 1，R 2，R 3，R 4和R 5如本文所定义。 本发明还涉及包含至少一种磺酰胺衍生物的组合物，以及使用磺酰胺衍生物来改善药物的药代动力学的方法。
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3.发明申请IMIDAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG 有权咪唑衍生物及其用于改善药物药物动力学的方法公开(公告)号：US20160108048A1
公开(公告)日：2016-04-21
申请号：US14895406
申请日：2014-06-02
申请人： Craig A. COBURN , Milana MALETIC , Yunfu LUO , Zhiqi QI , Chunsing LI , Tingting YU , Richard SOLL , MERCK SHARP & DOHME CORP.
发明人： Craig A. Coburn , Milana Maletic , Yunfu Luo , Zhiqi Qi , Chunsing Li , Tingting Yu , Richard Soll
IPC分类号： C07D487/04 , A61K31/4545 , C07D498/04 , A61K31/5383 , A61K31/4985 , A61K45/06 , A61K31/496 , A61K31/551 , C07D405/14 , C07D401/06 , C07D413/14 , C07D401/14 , A61K31/454
CPC分类号： C07D487/04 , A61K31/4375 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/4985 , A61K31/513 , A61K31/5365 , A61K31/5383 , A61K31/55 , A61K31/551 , A61K45/06 , C07D401/06 , C07D401/14 , C07D405/14 , C07D413/14 , C07D471/04 , C07D498/04 , A61K2300/00
摘要： The present invention relates to Imidazole Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein A, B, Y, R1 and R2 are as defined herein. The present invention also relates to compositions comprising at least one Imidazole Derivative, and methods of using the Imidazole Derivatives for inhibiting CYP450 3A. Inhibition of CYP450 3A can be used to improve the pharmacokinetics of a drug that is metabolized by CYP450 3A4.
摘要翻译： 本发明涉及式（I）的咪唑衍生物及其药学上可接受的盐，其中A，B，Y，R 1和R 2如本文所定义。 本发明还涉及包含至少一种咪唑衍生物的组合物，以及使用咪唑衍生物抑制CYP450A 3A的方法。 CYP450 3A的抑制可用于改善由CYP450 3A4代谢的药物的药代动力学。
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4.发明授权公开(公告)号：US10738062B2
公开(公告)日：2020-08-11
申请号：US16326043
申请日：2017-08-14
发明人： Wensheng Yu , Joseph A. Kozlowski , Ling Tong , Craig A. Coburn , Bin Hu , Bin Zhong , Jinglai Hao , Dahai Wang
IPC分类号： C07D498/04 , A61K45/06 , A61K31/496 , A61K31/5365 , A61P31/14
摘要： The present invention relates to novel Chromane-Substituted Tetracyclic Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, A′, R2 R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising a Chromane-Substituted Tetracyclic Compound, and methods of using the Chromane-Substituted Tetracyclic Compounds for treating or preventing HCV infection in a patient.
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公开(公告)号：US20170008906A1
公开(公告)日：2017-01-12
申请号：US15272669
申请日：2016-09-22
发明人： Craig A. Coburn , Steven W. Ludmerer , Kun Liu , Hao Wu , Richard Soll , Bin Zhong , Jian Zhu
IPC分类号： C07D498/04 , A61K31/4178 , A61K31/553 , A61K45/06 , A61K31/5365
CPC分类号： C07D498/04 , A61K31/4025 , A61K31/404 , A61K31/4178 , A61K31/4184 , A61K31/423 , A61K31/437 , A61K31/4439 , A61K31/4985 , A61K31/506 , A61K31/5365 , A61K31/5377 , A61K31/5383 , A61K31/553 , A61K38/05 , A61K38/06 , A61K45/06 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D498/10 , C07K5/06 , C07K5/08
摘要： The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
摘要翻译： 本发明涉及可用作丙型肝炎病毒（HCV）NS5A抑制剂，这种化合物的合成以及这些化合物用于抑制HCV NS5A活性用于治疗或预防HCV感染的用途的式（I）化合物和 抑制基于细胞的系统中的HCV病毒复制和/或病毒生产。
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公开(公告)号：US20140371138A1
公开(公告)日：2014-12-18
申请号：US14473117
申请日：2014-08-29
发明人： Craig A. Coburn , John A. McCauley , Steven W. Ludmerer , Kun Liu , Joseph P. Vacca , Hao Wu , Bin Hu , Richard Soll , Fei Sun , Xinghai Wang , Man Yan , Chengren Zhang , Mingwei Zheng , Bin Zhong , Jian Zhu
IPC分类号： C07K5/08 , A61K38/05 , A61K38/06 , C07D471/04 , A61K31/437 , C07K5/06 , A61K45/06
CPC分类号： C07D498/04 , A61K31/4025 , A61K31/404 , A61K31/4178 , A61K31/4184 , A61K31/423 , A61K31/437 , A61K31/4439 , A61K31/4985 , A61K31/506 , A61K31/5365 , A61K31/5377 , A61K31/5383 , A61K31/553 , A61K38/05 , A61K38/06 , A61K45/06 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D498/10 , C07K5/06 , C07K5/08
摘要： The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
摘要翻译： 本发明涉及可用作丙型肝炎病毒（HCV）NS5A抑制剂，这种化合物的合成以及这些化合物用于抑制HCV NS5A活性用于治疗或预防HCV感染的用途的式（I）化合物和 抑制基于细胞的系统中的HCV病毒复制和/或病毒生产。
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公开(公告)号：US20220356182A1
公开(公告)日：2022-11-10
申请号：US17324799
申请日：2021-05-19
发明人： Craig A. Coburn , Steven W. Ludmerer , Kun Liu , Hao Wu , Richard Soll , Bin Zhong , Jian Zhu
IPC分类号： C07D471/04 , C07D407/14 , A61K31/4985 , A61K31/4439 , A61K31/4184 , A61K31/423 , A61K31/4025 , A61K31/519 , A61K31/404 , A61K31/506 , A61K31/5377 , A61K31/427 , A61K31/4245 , A61K31/475 , A61K31/536 , A61K31/4178 , A61K31/517 , A61K31/5386 , A61K31/553 , C07D487/04 , C07D401/14 , C07D403/14 , C07D403/12 , C07D413/14 , C07D405/14 , C07D405/12 , C07D417/14 , C07D409/14 , A61K31/437
摘要： The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
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公开(公告)号：US09975888B2
公开(公告)日：2018-05-22
申请号：US15036274
申请日：2014-11-07
发明人： Craig A. Coburn , Milana M. Maletic , Yunfu Luo , Zhiqi Qi , Chun Sing Li , Tingting Yu
IPC分类号： C07D417/14 , C07D417/12 , C07D487/04 , C07D401/12 , C07D405/14 , C07D403/10 , C07D401/14 , A61K45/06 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/4985 , C07D409/14 , C07D471/04 , A61K31/4178 , A61K31/5377
CPC分类号： C07D417/14 , A61K31/4178 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/4985 , A61K31/5377 , A61K45/06 , C07D401/12 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/14 , C07D417/12 , C07D471/04 , C07D487/04 , A61K2300/00
摘要： The present invention relates to aryl linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhibiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.
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9.发明授权Spiropyrrolidine beta-secretase inhibitors for the treatment of alzheimer's disease 有权用于治疗阿尔茨海默氏病的Spiropyrrolidineβ-分泌酶抑制剂公开(公告)号：US09505739B2
公开(公告)日：2016-11-29
申请号：US14518825
申请日：2014-10-20
发明人： Shawn J. Stachel , Craig A. Coburn , Thomas G. Steele , Hao Wu
IPC分类号： A61K31/55 , C07D513/20 , A61K31/438 , A61K31/445 , A61P25/28 , C07D405/14 , C07D413/14 , C07D401/06 , C07D209/96 , C07D471/10 , C07D471/20 , C07D491/10 , C07D491/20 , C07D495/10 , C07D513/10 , C07D491/107
CPC分类号： C07D401/06 , C07D209/96 , C07D471/10 , C07D471/20 , C07D491/10 , C07D491/107 , C07D491/20 , C07D495/10 , C07D513/10 , C07D513/20
摘要： The present invention is directed to spiropyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
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公开(公告)号：US09090661B2
公开(公告)日：2015-07-28
申请号：US14473117
申请日：2014-08-29
发明人： Craig A. Coburn , John A. McCauley , Steven W. Ludmerer , Kun Liu , Joseph P. Vacca , Hao Wu , Bin Hu , Richard Soll , Fei Sun , Xinghai Wang , Man Yan , Chengren Zhang , Mingwei Zheng , Bin Zhong , Jian Zhu
IPC分类号： A61K31/4178 , C07D405/14 , C07K5/08 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D498/04 , C07D498/10 , A61K31/437 , A61K38/05 , A61K38/06 , A61K45/06 , C07K5/06
CPC分类号： C07D498/04 , A61K31/4025 , A61K31/404 , A61K31/4178 , A61K31/4184 , A61K31/423 , A61K31/437 , A61K31/4439 , A61K31/4985 , A61K31/506 , A61K31/5365 , A61K31/5377 , A61K31/5383 , A61K31/553 , A61K38/05 , A61K38/06 , A61K45/06 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D498/10 , C07K5/06 , C07K5/08
摘要： The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
摘要翻译： 本发明涉及可用作丙型肝炎病毒（HCV）NS5A抑制剂，这种化合物的合成以及这些化合物用于抑制HCV NS5A活性用于治疗或预防HCV感染的用途的式（I）化合物和 抑制基于细胞的系统中的HCV病毒复制和/或病毒生产。
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