公开(公告)号：EP2513337A1

公开(公告)日：2012-10-24

申请号：EP10842465.6

申请日：2010-12-09

申请人： Merck Sharp & Dohme Corp.

发明人： BUTORA, Gabor ,  DAVIES, Ian, W. ,  FLANAGAN, William Michael ,  FU, Wenlang ,  KENSKI, Denise, M. ,  QI, Ning

IPC分类号： C12Q1/68 ,  C40B30/10

CPC分类号： C12N15/113 ,  C12N15/111 ,  C12N2310/14 ,  C12N2310/32 ,  C12N2310/322 ,  C12N2310/331 ,  C12N2320/11 ,  C12N2320/51

摘要： It is an object of the instant invention to provide a method for the rapid evaluation of novel sugar modifications to be used in siRNA synthesis including the rapid evaluation of chemical modification patterns within the siRNA to effectuate increased stability and ultimately increased efficacy of a siRNA therapeutic. It is a further object of the instant invention to provide novel nucleosides useful for siRNA therapy.

公开(公告)号：EP2928877A1

公开(公告)日：2015-10-14

申请号：EP13860461.6

申请日：2013-12-02

申请人： Merck Sharp & Dohme Corp.

发明人： BUTORA, Gabor

IPC分类号： C07D339/08

CPC分类号： C07H19/10 ,  A61K47/549 ,  A61P35/00 ,  C07D339/08 ,  C07D405/04 ,  C07D409/14 ,  C07D487/04 ,  C07F9/655363 ,  C07F9/65586 ,  C07F9/65616 ,  C07H19/20 ,  C07H19/207 ,  C07H21/00 ,  C07K9/001 ,  C12N15/113 ,  C12N2310/14 ,  C12N2310/351 ,  C12N2320/30

摘要： The present invention relates to disulfide masked prodrug compounds, compositions and methods that are amenable to bioactivation by a reducing agent such as glutathione. Such disulfide based compounds, compositions, and methods can be useful, for example, in providing novel prodrugs for use as therapeutics.

公开(公告)号：EP2928877B1

公开(公告)日：2020-01-22

申请号：EP13860461.6

申请日：2013-12-02

申请人： Merck Sharp & Dohme Corp.

发明人： BUTORA, Gabor

IPC分类号： C07H21/00 ,  C07H19/10 ,  A61K47/54 ,  C07K9/00 ,  A61P35/00 ,  C12N15/113 ,  C07D487/04 ,  C07D409/14 ,  C07F9/6553 ,  C07D405/04 ,  C07F9/6561 ,  C07F9/6558 ,  C07H19/20 ,  C07D339/08 ,  C07H19/207

公开(公告)号：EP2928876B1

公开(公告)日：2018-01-17

申请号：EP13859616.8

申请日：2013-12-02

申请人： Merck Sharp & Dohme Corp.

发明人： BUTORA, Gabor

IPC分类号： C07D339/08 ,  C07F9/6561

CPC分类号： C07F9/655363 ,  C07D339/08 ,  C07D407/04 ,  C07D409/12 ,  C07D409/14 ,  C07D487/04 ,  C07F9/65586 ,  C07F9/6561 ,  C07F9/65616 ,  C07F9/657127 ,  C07F9/657154 ,  C07F9/65744

摘要： Such disulfide based compounds, compositions, and methods can be useful, for example, in providing prodrugs for use as therapeutics.

公开(公告)号：EP2928876A1

公开(公告)日：2015-10-14

申请号：EP13859616.8

申请日：2013-12-02

申请人： Merck Sharp & Dohme Corp.

发明人： BUTORA, Gabor

IPC分类号： C07D339/08

CPC分类号： C07F9/655363 ,  C07D339/08 ,  C07D407/04 ,  C07D409/12 ,  C07D409/14 ,  C07D487/04 ,  C07F9/65586 ,  C07F9/6561 ,  C07F9/65616 ,  C07F9/657127 ,  C07F9/657154 ,  C07F9/65744

摘要： The present invention relates to disulfide masked prodrug compounds, compositions and methods that are amenable to bioactivation by a reducing agent such as glutathione. Such disulfide based compounds, compositions, and methods can be useful, for example, in providing novel prodrugs for use as therapeutics. The compounds feature a conformationally restricted disulfide phosphotriester moiety to mask anionic charge. The compounds include a 1,2-dithigne moiety.

公开(公告)号：EP2919792A1

公开(公告)日：2015-09-23

申请号：EP13854794.8

申请日：2013-11-14

申请人： Merck Sharp & Dohme Corp.

发明人： BENNETT, Frank ,  HUANG, Yuhua ,  WANG, Lingyan ,  BOGEN, Stephane, L. ,  KEREKES, Angela, D. ,  GIRIJAVALLABHAN, Vinay M. ,  BUTORA, Gabor ,  TRUONG, Quang ,  DAVIES, Ian ,  WEBER, Anne E.

IPC分类号： A61K31/7068 ,  C07H19/02 ,  C07H19/10

CPC分类号： C07H19/10 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61K45/06 ,  C07H19/06 ,  C07H19/067 ,  C07H19/09 ,  C07H19/11

摘要： The present invention relates to 2′-Alkynyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2, R3 and R4 are as defined herein. The present invention also relates to compositions comprising at least one 2′-Alkynyl Substituted Nucleoside Derivative, and methods of using the 2′-Alkynyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

摘要翻译： 本发明涉及式（I）的2'-炔炔基取代的核苷衍生物及其药学上可接受的盐，其中B，X，R 1，R 2，R 3和R 4如本文所定义。 本发明还涉及包含至少一种2'-炔炔基取代的核苷衍生物的组合物，以及使用2'-炔基取代的核苷衍生物治疗或预防患者HCV感染的方法。

公开(公告)号：EP1758453B1

公开(公告)日：2014-07-16

申请号：EP05785614.8

申请日：2005-06-10

申请人： Merck Sharp & Dohme Corp. ,  Isis Pharmaceuticals, Inc.

发明人： BUTORA, Gabor ,  MACCOSS, Malcolm ,  BHAT, Balkrishen ,  ELDRUP, Anne, B.

IPC分类号： C07D498/04 ,  A01N43/04 ,  A61K31/70 ,  A61P35/00 ,  C07D487/04 ,  C07D491/04

CPC分类号： C07D491/04 ,  C07D487/04 ,  C07H19/16 ,  C07H19/20