公开(公告)号：US10513534B2

公开(公告)日：2019-12-24

申请号：US14047862

申请日：2013-10-07

申请人： IDENIX PHARMACEUTICALS LLC ,  Centre National De La Recherche Scientifique ,  UNIVERSITE DE MONTPELLIER

发明人： Gilles Gosselin ,  Christophe Claude Parsy ,  Francois-Rene Alexandre ,  Houcine Rahali ,  Jean-Francois Griffon ,  Dominique Surleraux ,  Cyril B. Dousson ,  Claire Pierra ,  Adel M. Moussa ,  Benjamin Alexander Mayes ,  Alistair James Stewart

IPC分类号： C07H19/06 ,  C07H19/073 ,  C07H19/10 ,  C07H19/11 ,  C07H19/16 ,  C07H19/173 ,  C07H19/20 ,  C07H19/213 ,  A61K31/7072 ,  A61K45/06 ,  A61K38/21 ,  A61K31/7076 ,  C07H19/14 ,  A61K31/7064 ,  C07H19/12 ,  A61K31/706 ,  A61K31/7068 ,  A61K31/708 ,  A61K31/403 ,  A61K31/497 ,  A61K31/7105 ,  C07H19/23

摘要： Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2′-chloro nucleosides according to Formula 2001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein B, Z and PD are as described herein.

公开(公告)号：US10251903B2

公开(公告)日：2019-04-09

申请号：US15519846

申请日：2015-10-20

申请人： MERCK SHARP & DOHME CORP. ,  IDENIX Pharmaceuticals LLC ,  Bryon L. Simmons ,  Kevin R. Campos ,  Artis Klapars ,  Alistair J. Stewart ,  Benjamin A. Mayes ,  Peter E. Maligres ,  Alan Hyde ,  Steven Mark Silverman ,  Yong-Li Zhong ,  Adel M. Moussa ,  Kenneth Baker ,  Kara Van Valkenburg

发明人： Bryon L. Simmons ,  Kevin R. Campos ,  Artis Klapars ,  Alistair J. Stewart ,  Benjamin A. Mayes ,  Peter E. Maligres ,  Alan Hyde ,  Steven Mark Silverman ,  Yong-Li Zhong ,  Adel M. Moussa ,  Kenneth Baker ,  Kara Van Valkenburg

IPC分类号： C07H19/10 ,  A61K31/7052 ,  C07H1/00 ,  C08K3/08

摘要： The present invention is directed to a process for making Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).

公开(公告)号：US10717758B2

公开(公告)日：2020-07-21

申请号：US15981813

申请日：2018-05-16

申请人： IDENIX PHARMACEUTICALS LLC

发明人： Benjamin Alexander Mayes ,  Adel M. Moussa ,  Alistair James Stewart ,  David Dukhan

IPC分类号： C07H19/20 ,  A61K31/403 ,  C07H19/10 ,  A61K31/7072 ,  A61K45/06 ,  A61K31/7076 ,  A61K31/708 ,  A61K31/4709 ,  A61K31/497 ,  A61K38/21 ,  A61K38/55 ,  C07H19/16 ,  A61K31/7056

摘要： Provided herein are compounds, compositions and methods for the treatment of liver disease and conditions, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.

公开(公告)号：US10238680B2

公开(公告)日：2019-03-26

申请号：US14954815

申请日：2015-11-30

申请人： IDENIX PHARMACEUTICALS LLC ,  CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE ,  UNIVERSITE DE MONTPELLIER

发明人： Benjamin Alexander Mayes ,  Adel M. Moussa ,  Cyril B. Dousson ,  Gilles Gosselin ,  Claire Pierra ,  David Dukhan

IPC分类号： C07H19/10 ,  A61K31/7068 ,  A61K31/7072 ,  A61K45/06 ,  A61K9/00

摘要： Provided herein are compounds, compositions, and methods for the treatment of viral infections, for example, Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are D-amino acid phosphoramidate halogeno pyrimidine nucleoside analog compounds which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human. In certain embodiments, the compounds are of Formula I: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form, or polymorphic form thereof, wherein: PD, X, R1, R2, RA, and RB are as described herein.

公开(公告)号：US20170066795A1

公开(公告)日：2017-03-09

申请号：US15123124

申请日：2015-03-05

申请人： IDENIX PHARMACEUTICALS LLC ,  Merck Sharp & Dohme Corp.

发明人： John Zoltan Sulliva-Bolyai ,  Benjamin Alexander Mayes ,  Douglas Lytle Mayers ,  Xiao-Jian Zhou ,  Adel M. Moussa ,  Alistair James Stewart ,  Sindhura Ganga ,  Clinton Scott Shultz ,  Alfred Lee

IPC分类号： C07H19/10 ,  A61K9/48 ,  A61K31/7072 ,  A61K9/20

CPC分类号： C07H19/10 ,  A61K9/20 ,  A61K9/2018 ,  A61K9/2077 ,  A61K9/48 ,  A61K9/4858 ,  A61K31/7072 ,  C07B2200/13

摘要： Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are solid forms of Compound I: (Compound I)

摘要翻译： 本文提供了用于治疗黄病毒科感染（包括HCV感染）的化合物，组合物和方法。 在某些实施方案中，公开了核苷衍生物的化合物和组合物，其可以单独施用或与其它抗病毒剂组合施用。 在某些实施方案中，化合物是化合物I的固体形式：（化合物I）

公开(公告)号：US09192621B2

公开(公告)日：2015-11-24

申请号：US14038617

申请日：2013-09-26

申请人： IDENIX PHARMACEUTICALS LLC

发明人： Benjamin Alexander Mayes ,  Adel M. Moussa

IPC分类号： C07H19/10 ,  C07H19/20 ,  A61K31/7076 ,  C07H17/02 ,  A61K45/06 ,  C07H19/16 ,  A61K31/403 ,  A61K31/497 ,  A61K31/7056 ,  A61K31/708 ,  A61K38/21

CPC分类号： A61K31/7076 ,  A61K31/403 ,  A61K31/497 ,  A61K31/7056 ,  A61K31/708 ,  A61K38/212 ,  A61K45/06 ,  C07H17/02 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20 ,  A61K2300/00

摘要： Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, provided herein are compounds according to Formula 1001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein Base, Y, Z, A, RC and RD are as described herein.

摘要翻译： 本文提供了用于治疗黄病毒科感染（包括HCV感染）的化合物，组合物和方法。 在某些实施方案中，公开了核苷衍生物的化合物和组合物，其可以单独施用或与其它抗病毒剂组合施用。 在某些实施方案中，本文提供了根据式1001的化合物：或其药学上可接受的盐，溶剂化物，立体异构体形式，互变异构形式或其多晶型物，其中碱，Y，Z，A，RC和RD如本文所述。

公开(公告)号：US20170066779A1

公开(公告)日：2017-03-09

申请号：US15123170

申请日：2015-03-04

申请人： IDENIX Pharmaceuticals LLC

发明人： Adel M. Moussa ,  Benjamin Alexander Mayes ,  Alistair James Stewart

IPC分类号： C07D495/04 ,  A61K31/4184 ,  A61K45/06

CPC分类号： C07D495/04 ,  A61K31/4184 ,  A61K45/06 ,  C07B2200/13

摘要： Provided herein are crystalline and salt forms of methyl N-{(1R)-2-[(2S)-2-{5-[4-(6-{2-[(2S)-1-{(2S)-2-[(methoxycarbonyl)amino]-3-methylbutanoyl} pyrrolidin-2-yl]-3H-benzimidazol-5-yl}thieno[3,2-b]thiophen-3-yl)phenyl]-1H-imidazol-2-yl}pyrrolidin-1-yl]-2-oxo-1-phenylethyl} carbamate, a Flaviviridae, including hepatitis C, virus inhibitor, pharmaceutical compositions comprising the compound, and processes of preparation thereof. Also provided are methods of its use for the treatment of a Flaviviridae, including HCV, infection in a subject in need thereof.

摘要翻译： 本文提供的是N - {（1R）-2 - [（2S）-2- {5- [4-（6- {2 - [（2S）-1 - {（2S）-2 - [（甲氧基羰基）氨基] -3-甲基丁酰基}吡咯烷-2-基] -3H-苯并咪唑-5-基}噻吩并[3,2-b]噻吩-3-基）苯基〕-1H-咪唑-2-基） 吡咯烷-1-基] -2-氧代-1-苯基乙基}氨基甲酸酯，黄病毒科，包括丙型肝炎病毒抑制剂，包含该化合物的药物组合物及其制备方法。 还提供了其用于治疗有需要的受试者中的黄病毒科（包括HCV）感染的方法。

公开(公告)号：US20160271162A1

公开(公告)日：2016-09-22

申请号：US15033725

申请日：2014-10-30

申请人： IDENIX PHARMACEUTICALS, LLC

发明人： Adel M. Moussa ,  Benjamin Alexander Mayes ,  Alistair James Stewart

IPC分类号： A61K31/7076 ,  A61K45/06 ,  A61K9/00 ,  C07H19/207

CPC分类号： A61K31/7076 ,  A61K9/0053 ,  A61K45/06 ,  C07H19/207

摘要： Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are D-alanine phosphoramidate pronucleotides of 2′-methyl 2′-fluoro guanosine nucleoside which display remarkable efficacy and bioavailability for the treatment of for example, HCV infection in a human. In certain embodiments, the compounds are of Formula I or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof; where W and R are as described herein.

公开(公告)号：US10723754B2

公开(公告)日：2020-07-28

申请号：US14059233

申请日：2013-10-21

申请人： IDENIX PHARMACEUTICALS LLC

发明人： Benjamin Alexander Mayes ,  Adel M. Moussa ,  Alistair James Stewart

IPC分类号： C07H19/10 ,  C07H19/24 ,  C07H19/20 ,  A61K31/7076 ,  A61K45/06 ,  C07H19/207 ,  C07H19/11 ,  C07H19/213

摘要： Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2′,4′-bridged nucleosides which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human. In certain embodiments, the 2′,4′-bridged nucleosides are of Formula 3001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, where PD, B, W, X, RA, RB, RC and RD are as described herein.

公开(公告)号：US20180162898A1

公开(公告)日：2018-06-14

申请号：US15104706

申请日：2014-12-17

申请人： IDENIX PHARMACEUTICALS LLC

发明人： David Dukhan ,  Cyril B. Dousson ,  Adel M. Moussa ,  Benjamin Alexander Mayes ,  James Alistair Stewart

IPC分类号： C07H19/207 ,  C07H19/10 ,  A61P31/14

CPC分类号： C07H19/207 ,  A61P31/14 ,  C07H19/06 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20

摘要： Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 4′-OR nucleosides of Formula I: or a pharmaceutically acceptable salt thereof, wherein Base, PD, R, Z1, Z2, Z3, and Z4 are as defined herein.