公开(公告)号：US10526363B2

公开(公告)日：2020-01-07

申请号：US15503776

申请日：2015-08-14

申请人： Merck Sharp & Dohme Corp. ,  Merck Sharp & Dohme Limited ,  John Simon Edwards ,  Peter Richard Mullens ,  Edward Cleator ,  Bryon L. Simmons ,  Courtney K. Maguire ,  Jeremy Peter Scott ,  Nobuyoshi Yasuda ,  Yong-Li Zhong ,  Lisa F. Frey ,  Peter G. Dormer ,  Andrew Brunskill ,  Artis Klapars ,  Pu Qian ,  Yi Zhang ,  Baoqiang Wan ,  Eric Ashley

发明人： John Simon Edwards ,  Peter Richard Mullens ,  Edward Cleator ,  Bryon L. Simmons ,  Courtney K. Maguire ,  Jeremy Peter Scott ,  Nobuyoshi Yasuda ,  Yong-Li Zhong ,  Lisa F. Frey ,  Peter G. Dormer ,  Andrew Brunskill ,  Artis Klapars ,  Pu Qian ,  Yi Zhang ,  Baoqiang Wan ,  Eric Ashley

IPC分类号： C07H19/10 ,  C07F9/58 ,  C07H19/06 ,  C07F9/24 ,  C07F9/6558

摘要： The present invention is directed to Compounds of Formula (I) and salts thereof, wherein R1, R2, R3 and R4 are defined above herein. The present invention is also directed to uses of the compounds of Formula (I) to add phosphoramidate groups onto organic alcohols.

公开(公告)号：US20170275327A1

公开(公告)日：2017-09-28

申请号：US15503776

申请日：2015-08-14

申请人： John Simon EDWARDS ,  Peter Richard MULLENS ,  Edward CLEATOR ,  Bryon L. SIMMONS ,  Courtney K. MAGUIRE ,  Jeremy Peter SCOTT ,  Nobuyoshi YASUDA ,  Yong ZHONG ,  Lisa F. FREY ,  Peter G. DORMER ,  Andrew BRUNSKILL ,  Artis KLAPARS ,  Eric ASHLEY ,  Pu QIAN ,  Yi ZHANG ,  Baoqiang WAN ,  MERCK SHARP & DOHME CORP. ,  MERCK SHARP & DOHME LIMITED

发明人： John Edwards ,  Peter Richard Mullens ,  Ed Cleator ,  Bryon L. Simmons ,  Courtney K. Maguire ,  Jeremy Peter Scott ,  Nobuyoshi Yasuda ,  Yong-Li Zhong ,  Lisa F. Frey ,  Peter G. Dormer ,  Andrew Brunskill ,  Artis Klapars ,  Puneet Qian ,  Yi Zhang ,  Baoqiang Wan

IPC分类号： C07H19/10 ,  C07F9/24 ,  C07F9/58

CPC分类号： C07H19/10 ,  C07F9/242 ,  C07F9/2458 ,  C07F9/2487 ,  C07F9/58 ,  C07F9/65586 ,  C07H19/06

摘要： The present invention is directed to Compounds of Formula (I) and salts thereof, wherein R1, R2, R3 and R4 are defined above herein. The present invention is also directed to uses of the compounds of Formula (I) to add phosphoramidate groups onto organic alcohols.

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：US08193216B2

公开(公告)日：2012-06-05

申请号：US13210908

申请日：2011-08-16

申请人： Daniel J. Kumke ,  Jerry A. Murry ,  Bryon L. Simmons ,  Feng Xu

发明人： Daniel J. Kumke ,  Jerry A. Murry ,  Bryon L. Simmons ,  Feng Xu

IPC分类号： A61K31/4355 ,  C07D498/04

CPC分类号： C07D498/04

摘要： The present invention is directed to novel polymorphic forms of the compound 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol hydrate (gaboxadol monohydrate). The invention is further concerned with pharmaceutical compositions containing the polymorphic forms as an active ingredient, methods for treatment of disorders susceptible to amelioration by GABAA receptor agonism with the polymorphic forms, and processes for the preparation of the polymorphic forms.

摘要翻译： 本发明涉及化合物4,5,6,7-四氢异恶唑并[5,4-c]吡啶-3-醇水合物（加波沙朵一水合物）的新型多晶型物。 本发明进一步涉及含有多晶型物作为活性成分的药物组合物，用多巴胺形式治疗易受GABA A受体激动作用改善的病症的方法，以及多晶型物的制备方法。

公开(公告)号：US20110301190A1

公开(公告)日：2011-12-08

申请号：US13210908

申请日：2011-08-16

申请人： Daniel J. Kumke ,  Jerry A. Murry ,  Bryon L. Simmons ,  Feng Xu

发明人： Daniel J. Kumke ,  Jerry A. Murry ,  Bryon L. Simmons ,  Feng Xu

IPC分类号： A61K31/437 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/18 ,  A61P25/20 ,  A61P27/16 ,  A61P15/00 ,  C07D498/04 ,  A61P25/16

CPC分类号： C07D498/04

摘要： The present invention is directed to novel polymorphic forms of the compound 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol hydrate (gaboxadol monohydrate). The invention is further concerned with pharmaceutical compositions containing the polymorphic forms as an active ingredient, methods for treatment of disorders susceptible to amelioration by GABAA receptor agonism with the polymorphic forms, and processes for the preparation of the polymorphic forms.

摘要翻译： 本发明涉及化合物4,5,6,7-四氢异恶唑并[5,4-c]吡啶-3-醇水合物（加波沙朵一水合物）的新型多晶型物。 本发明进一步涉及含有多晶型物作为活性成分的药物组合物，用多巴胺形式治疗易受GABA A受体激动作用改善的病症的方法，以及多晶型物的制备方法。

公开(公告)号：US08022084B2

公开(公告)日：2011-09-20

申请号：US11813796

申请日：2006-01-26

申请人： Daniel J. Kumke ,  Jerry A. Murry ,  Bryon L. Simmons ,  Feng Xu

发明人： Daniel J. Kumke ,  Jerry A. Murry ,  Bryon L. Simmons ,  Feng Xu

IPC分类号： A61K31/4355 ,  C07D498/04

CPC分类号： C07D498/04

摘要： The present invention is directed to novel polymorphic forms of the compound 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol hydrate (gaboxadol monohydrate). The invention is further concerned with pharmaceutical compositions containing the polymorphic forms as an active ingredient, methods for treatment of disorders susceptible to amelioration by GABAA receptor agonism with the polymorphic forms, and processes for the preparation of the polymorphic forms.

摘要翻译： 本发明涉及化合物4,5,6,7-四氢异恶唑并[5,4-c]吡啶-3-醇水合物（加波沙朵一水合物）的新型多晶型物。 本发明进一步涉及含有多晶型物作为活性成分的药物组合物，用多巴胺形式治疗易受GABA A受体激动作用改善的病症的方法，以及多晶型物的制备方法。