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公开(公告)号:US20200323894A1
公开(公告)日:2020-10-15
申请号:US16306424
申请日:2017-06-01
IPC分类号: A61K31/7072 , A61K31/4178 , A61K31/4985 , A61K47/32 , A61K47/38
摘要: Disclosed are pharmaceutical compositions comprising three antiviral compounds. In particular, the pharmaceutical compositions comprise an effective amount of velpatasvir, an effective amount of sofosbuvir, and an effective amount of voxilaprevir. Also disclosed are methods of use for the pharmaceutical composition.
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公开(公告)号:US09884873B2
公开(公告)日:2018-02-06
申请号:US15459785
申请日:2017-03-15
IPC分类号: C07D491/052
CPC分类号: C07D491/052 , C07B2200/13
摘要: Crystalline solid forms of methyl {(2S)-1-[(2S,5S)-2-(9-{2-[(2S,4S)-1-{(2R)-2-[(methoxycarbonyl)amino]-2-phenylacetyl}-4-(methoxymethyl)pyrrolidin-2-yl]-1H-imidazol-5-yl}-1,11-dihydroisochromeno[4′,3′:6,7]naphtho[1,2-d]imidazol-2-yl)-5-methylpyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl}carbamate (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using these crystalline forms.
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公开(公告)号:US09845299B2
公开(公告)日:2017-12-19
申请号:US15454561
申请日:2017-03-09
发明人: Rongmin Chen , Yuanqiang Li , Jianqiang Zhao , Jianbing Zheng , Guoliang Zhu
IPC分类号: C07D263/26
CPC分类号: C07D263/26 , C07D307/33 , C07D413/06 , Y02P20/55
摘要: A novel process for the preparation of a fluorolactone derivative of the formula and of its acylated derivative of formula wherein R1 stands for a hydroxy protecting group is described. The acylated fluor lactones of formula V, particularly the benzoyl derivative with R1=benzyl are important precursors for the synthesis of prodrug compounds which have the potential to be potent inhibitors of the Hepatitis C Virus (HCV) NS5B polymerase.
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公开(公告)号:US09630972B2
公开(公告)日:2017-04-25
申请号:US14733101
申请日:2015-06-08
IPC分类号: C07D491/052
CPC分类号: C07D491/052 , C07B2200/13
摘要: Crystalline solid forms of methyl {(2S)-1-[(2S,5S)-2-(9-{2-[(2S,4S)-1-{(2R)-2-[(methoxycarbonyl)amino]-2-phenylacetyl}-4-(methoxymethyl)pyrrolidin-2-yl]-1H-imidazol-5-yl}-1,11-dihydroisochromeno[4′,3′:6,7]naphtho[1,2-d]imidazol-2-yl)-5-methylpyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl}carbamate (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using these crystalline forms.
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公开(公告)号:US09549941B2
公开(公告)日:2017-01-24
申请号:US14538736
申请日:2014-11-11
发明人: Darryl G. Cleary , Charles J. Reynolds , Miriam Michelle Berrey , Robert G. Hindes , William T. Symonds , Adrian S. Ray , Hongmei Mo , Christy M. Hebner , Reza Oliyai , Vahid Zia , Dimitrios Stefanidis , Rowchanak Pakdaman , Melissa Jean Casteel
IPC分类号: A61K31/685 , A61K31/7056 , A61K31/7068 , A61K31/4196 , A61K31/7072 , A61K9/20 , A61K31/513 , A61K31/664 , A61K31/675
CPC分类号: A61K31/7072 , A61K9/2009 , A61K9/2013 , A61K9/2054 , A61K31/4196 , A61K31/513 , A61K31/664 , A61K31/675 , A61K31/685 , A61K31/7056 , A61K31/7068 , A61K2300/00
摘要: Disclosed herein are a composition and unit dosage form for the treatment of hepatitis C virus (HCV) infection comprising GS-7977 and at least one pharmaceutically acceptable excipient, as well as methods for making said composition and unit dosage form. Also disclosed herein is a method of treating a subject, preferably a human, infected with hepatitis C virus, said method comprising administering to the subject for a time period an effective amount of GS-7977 and an effective amount of ribavirin. In one aspect, the method comprises administering to the subject an interferon-free treatment regimen comprising an effective amount of GS-7977 and an effective amount of ribavirin. In a particular aspect, the method is sufficient to produce an undetectable amount of HCV RNA in the subject for at least 12 weeks after the end of the time period.
摘要翻译: 本文公开了用于治疗包含GS-7977和至少一种药学上可接受的赋形剂的丙型肝炎病毒(HCV)感染的组合物和单位剂型,以及制备所述组合物和单位剂型的方法。 本文还公开了一种治疗感染丙型肝炎病毒的受试者,优选人的方法,所述方法包括给予受试者一段时间有效量的GS-7977和有效量的利巴韦林。 在一个方面,所述方法包括向受试者施用包含有效量的GS-7977和有效量的利巴韦林的无干扰素治疗方案。 在特定方面,所述方法足以在所述受试者中在所述时间段结束后至少12周产生不可检测量的HCV RNA。
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公开(公告)号:US09511056B2
公开(公告)日:2016-12-06
申请号:US14280478
申请日:2014-05-16
发明人: Elizabeth M. Bacon , Eda Canales , Aesop Cho , Jeromy J. Cottell , Manoj C. Desai , Michael Graupe , Hongyan Guo , Randall L. Halcomb , Darryl Kato , Choung U. Kim , Thorsten A. Kirschberg , Evan S. Krygowski , Scott E. Lazerwith , John O. Link , Hongtao Liu , Qi Liu , Richard L. Mackman , Michael L. Mitchell , Jay P. Parrish , Hyung-Jung Pyun , Joseph H. Saugier , Scott D. Schroeder , Jianyu Sun , James G. Taylor , James D. Trenkle , Winston C. Tse , Randall W. Vivian , William J. Watkins , Lianhong Xu
IPC分类号: C07D403/04 , C07D403/14 , C07D471/08 , A61K45/06 , A61K31/4184 , C07F5/02
CPC分类号: C07D403/14 , A61K31/4025 , A61K31/4178 , A61K31/4184 , A61K31/427 , A61K31/435 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/519 , A61K31/5377 , A61K31/5415 , A61K31/55 , A61K45/06 , A61P31/12 , C07D207/16 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D491/113 , C07D495/04 , C07F5/025
摘要: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
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公开(公告)号:US09409891B2
公开(公告)日:2016-08-09
申请号:US14313877
申请日:2014-06-24
发明人: Ahmad Hashash , Scott Wolckenhauer , Bing Shi
IPC分类号: A61K31/381 , A61K31/4184 , A61K31/7056 , A61K31/7072 , A61K45/06 , C07D407/04 , C07D409/12 , C07D471/08
CPC分类号: C07D409/12 , A61K31/381 , A61K31/4184 , A61K31/7056 , A61K31/7072 , A61K45/06 , C07D407/04 , C07D471/08
摘要: Crystalline solid forms and the amorphous form of the anti-HCV compound 5-(3,3-dimethylbutyn-1-yl)-3-[(cis-4-hydroxy-4-{[(3S)-tetrahydrofuran-3-yloxy]methyl}cyclohexyl){[(1R)-4-methylcyclohex-3-en-1-yl]carbonyl}amino]thiophene-2-carboxylic acid (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.
摘要翻译: 结晶固体形式和无定形形式的抗HCV化合物5-(3,3-二甲基丁炔-1-基)-3 - [(顺式-4-羟基-4 - {[(3S) - 四氢呋喃-3-基氧基 ]甲基}环己基){[(1R)-4-甲基环己-3-烯-1-基]羰基}氨基]噻吩-2-羧酸(化合物I),并以固体状态表征:还提供了方法 的制造方法和使用结晶形式的方法。
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公开(公告)号:US09296777B2
公开(公告)日:2016-03-29
申请号:US14265840
申请日:2014-04-30
发明人: Michael Joseph Sofia , Jinfa Du
IPC分类号: C07H19/06 , C07H19/14 , C07H19/16 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076
CPC分类号: C07H19/06 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , C07H19/073 , C07H19/14 , C07H19/16 , C07H19/173
摘要: Embodiments of the invention are to compounds, methods, and compositions for use in the treatment of viral infections. More specifically embodiments of the invention are 2′,4′-substituted nucleoside compounds useful for the treatment of viral infections, such as HIV, HCV, and HBV infections.
摘要翻译: 本发明的实施方案是用于治疗病毒感染的化合物,方法和组合物。 更具体地,本发明的实施方案是用于治疗病毒感染的2',4'-取代的核苷化合物,例如HIV,HCV和HBV感染。
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公开(公告)号:US09221833B2
公开(公告)日:2015-12-29
申请号:US14696233
申请日:2015-04-24
发明人: Elizabeth M. Bacon , Jeromy J. Cottell , Ashley Anne Katana , Darryl Kato , Evan S. Krygowski , John O. Link , James Taylor , Chinh Viet Tran , Teresa Alejandra Trejo Martin , Zheng-Yu Yang , Sheila Zipfel
IPC分类号: C07D491/052
CPC分类号: C07D491/052 , A61K31/4188 , A61K31/7056 , A61K31/7064 , A61K31/7072 , A61K38/06 , A61K38/07 , A61K38/21 , A61K45/06 , A61K47/60 , C07D405/12 , C07F5/025 , Y10S514/894 , A61K2300/00
摘要: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
摘要翻译: 本公开涉及抗病毒化合物,含有这些化合物的组合物和包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。
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公开(公告)号:US09056860B2
公开(公告)日:2015-06-16
申请号:US13800202
申请日:2013-03-13
发明人: Robert William Scott , Justin Philip Vitale , Kenneth Stanley Matthews , Martin Gerald Teresk , Alexandra Formella , Jared Wayne Evans
IPC分类号: C07D403/14 , C07D403/04
CPC分类号: C07D403/14 , C07D403/04 , Y02P20/55
摘要: The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula I.
摘要翻译: 本公开提供了制备式I化合物的方法:其可用作抗病毒剂。 本公开还提供了作为式I化合物的合成中间体的化合物。
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