EA201071170A1 - Аналоги 1' - замещённого карба-нуклеозида для противовирусного лечения - Google Patents
Аналоги 1' - замещённого карба-нуклеозида для противовирусного леченияInfo
- Publication number
- EA201071170A1 EA201071170A1 EA201071170A EA201071170A EA201071170A1 EA 201071170 A1 EA201071170 A1 EA 201071170A1 EA 201071170 A EA201071170 A EA 201071170A EA 201071170 A EA201071170 A EA 201071170A EA 201071170 A1 EA201071170 A1 EA 201071170A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- nucleoside
- analogues
- triazinyl
- substituted carbon
- virus treatment
- Prior art date
Links
- 239000002777 nucleoside Substances 0.000 title abstract 4
- 230000002155 anti-virotic effect Effects 0.000 title 1
- -1 [1,2,4] triazinyl- Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000005176 Hepatitis C Diseases 0.000 abstract 1
- 229910019142 PO4 Inorganic materials 0.000 abstract 1
- 208000036142 Viral infection Diseases 0.000 abstract 1
- 208000015181 infectious disease Diseases 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 150000003833 nucleoside derivatives Chemical class 0.000 abstract 1
- 235000021317 phosphate Nutrition 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 230000009385 viral infection Effects 0.000 abstract 1
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- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/23—Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups C07H19/14 - C07H19/22
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- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/12—Ketones
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
- C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
- C07F9/6574—Esters of oxyacids of phosphorus
- C07F9/65744—Esters of oxyacids of phosphorus condensed with carbocyclic or heterocyclic rings or ring systems
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- C07H5/04—Compounds containing saccharide radicals in which the hetero bonds to oxygen have been replaced by the same number of hetero bonds to halogen, nitrogen, sulfur, selenium, or tellurium to nitrogen
- C07H5/06—Aminosugars
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Virology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Gastroenterology & Hepatology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Saccharide Compounds (AREA)
Abstract
В изобретении предложены пирроло[1,2-f][1,2,4]триазинил-, имидазо[1,5-f][1,2,4]триазинил-, имидазо[1,2-f][1,2,4]триазинил- и [1,2,4]триазоло[4,3-f][1,2,4]триазинилнуклеозиды, а также нуклеозид фосфаты и пролекарства указанных соединений, причем положение 1' сахара в составе нуклеозида является замещенным. Предложенные соединения, композиции и способы подходят для лечения вирусных инфекций, вызываемых, в частности инфекций, вызываемых вирусом гепатита С.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US4726308P | 2008-04-23 | 2008-04-23 | |
US13944908P | 2008-12-19 | 2008-12-19 | |
PCT/US2009/041447 WO2009132135A1 (en) | 2008-04-23 | 2009-04-22 | 1' -substituted carba-nucleoside analogs for antiviral treatment |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201071170A1 true EA201071170A1 (ru) | 2011-08-30 |
EA020659B1 EA020659B1 (ru) | 2014-12-30 |
Family
ID=40887058
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201071128A EA019883B1 (ru) | 2008-04-23 | 2009-04-22 | Карбануклеозидные аналоги для противовирусной терапии |
EA201071170A EA020659B1 (ru) | 2008-04-23 | 2009-04-22 | 1'-замещённые карбануклеозидные аналоги для противовирусной терапии |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201071128A EA019883B1 (ru) | 2008-04-23 | 2009-04-22 | Карбануклеозидные аналоги для противовирусной терапии |
Country Status (33)
Country | Link |
---|---|
US (5) | US8012941B2 (ru) |
EP (3) | EP2268642B1 (ru) |
JP (4) | JP5425187B2 (ru) |
KR (3) | KR101681559B1 (ru) |
CN (3) | CN104262345B (ru) |
AP (2) | AP3076A (ru) |
AR (1) | AR071395A1 (ru) |
AU (2) | AU2009240630B2 (ru) |
BR (2) | BRPI0910455B8 (ru) |
CA (2) | CA2722177C (ru) |
CO (2) | CO6321235A2 (ru) |
CY (4) | CY1113647T1 (ru) |
DK (3) | DK2937350T3 (ru) |
EA (2) | EA019883B1 (ru) |
EC (2) | ECSP10010609A (ru) |
ES (3) | ES2398684T3 (ru) |
HK (3) | HK1152709A1 (ru) |
HR (3) | HRP20130048T1 (ru) |
HU (3) | HUE038946T2 (ru) |
IL (2) | IL208515A (ru) |
LT (2) | LT2937350T (ru) |
LU (1) | LUC00193I2 (ru) |
ME (1) | ME03089B (ru) |
MX (2) | MX2010011661A (ru) |
NO (1) | NO2937350T3 (ru) |
NZ (2) | NZ588670A (ru) |
PL (3) | PL2280973T3 (ru) |
PT (3) | PT2280973E (ru) |
RS (2) | RS57092B1 (ru) |
SI (3) | SI2937350T1 (ru) |
TW (2) | TW201334784A (ru) |
WO (2) | WO2009132123A1 (ru) |
ZA (2) | ZA201007713B (ru) |
Cited By (8)
Publication number | Priority date | Publication date | Assignee | Title |
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US8853171B2 (en) | 2008-04-23 | 2014-10-07 | Gilead Sciences, Inc. | 1′-substituted carba-nucleoside analogs for antiviral treatment |
US9090642B2 (en) | 2010-07-19 | 2015-07-28 | Gilead Sciences, Inc. | Methods for the preparation of diasteromerically pure phosphoramidate prodrugs |
US9724360B2 (en) | 2014-10-29 | 2017-08-08 | Gilead Sciences, Inc. | Methods for treating Filoviridae virus infections |
US10065958B2 (en) | 2010-07-22 | 2018-09-04 | Gilead Sciences, Inc. | Methods and compounds for treating Paramyxoviridae virus infections |
US10251904B2 (en) | 2015-09-16 | 2019-04-09 | Gilead Sciences, Inc. | Methods for treating arenaviridae and coronaviridae virus infections |
US10675296B2 (en) | 2017-07-11 | 2020-06-09 | Gilead Sciences, Inc. | Compositions comprising an RNA polymerase inhibitor and cyclodextrin for treating viral infections |
US10836787B2 (en) | 2017-05-01 | 2020-11-17 | Gilead Sciences, Inc. | Crystalline forms of (S)-2-ethylbutyl 2-(((S)-(((2R,3S,4R,5R)-5- (4-aminopyrrolo[2,1-f] [1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2-yl)methoxy)(phenoxy) phosphoryl)amino)propanoate |
US10988498B2 (en) | 2009-09-21 | 2021-04-27 | Gilead Sciences, Inc. | Processes and intermediates for the preparation of 1′-substituted carba-nucleoside analogs |
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MY164523A (en) | 2000-05-23 | 2017-12-29 | Univ Degli Studi Cagliari | Methods and compositions for treating hepatitis c virus |
AP1727A (en) | 2000-05-26 | 2007-03-06 | Idenix Cayman Ltd | Methods and compositions for treating flaviviruses and pestiviruses. |
DK1576138T3 (en) | 2002-11-15 | 2017-05-01 | Idenix Pharmaceuticals Llc | 2'-METHYL NUCLEOSIDES IN COMBINATION WITH INTERFERON AND FLAVIVIRIDAE MUTATION |
US8173621B2 (en) | 2008-06-11 | 2012-05-08 | Gilead Pharmasset Llc | Nucleoside cyclicphosphates |
WO2010002877A2 (en) * | 2008-07-03 | 2010-01-07 | Biota Scientific Management | Bycyclic nucleosides and nucleotides as therapeutic agents |
PT2818469T (pt) | 2008-12-09 | 2017-05-05 | Gilead Sciences Inc | Intermediários para a preparação de moduladores de recetores do tipo toll |
CA2748016A1 (en) | 2008-12-23 | 2010-07-01 | Pharmasset, Inc. | Synthesis of purine nucleosides |
EP2376514A2 (en) | 2008-12-23 | 2011-10-19 | Pharmasset, Inc. | Nucleoside analogs |
MX2011006891A (es) | 2008-12-23 | 2011-10-06 | Pharmasset Inc | Fosforamidatos de nucleosidos. |
US8618076B2 (en) | 2009-05-20 | 2013-12-31 | Gilead Pharmasset Llc | Nucleoside phosphoramidates |
TWI576352B (zh) | 2009-05-20 | 2017-04-01 | 基利法瑪席特有限責任公司 | 核苷磷醯胺 |
US8455451B2 (en) | 2009-09-21 | 2013-06-04 | Gilead Sciences, Inc. | 2'-fluoro substituted carba-nucleoside analogs for antiviral treatment |
US7973013B2 (en) | 2009-09-21 | 2011-07-05 | Gilead Sciences, Inc. | 2'-fluoro substituted carba-nucleoside analogs for antiviral treatment |
BR122021021135B1 (pt) * | 2009-09-21 | 2022-08-30 | Gilead Sciences, Inc | Compostos análogos de 2-flúor substituído carba-nucleosídeo, composição farmacêutica e uso dos compostos análogos de 2´-flúoro substituído carbonucleosídeo |
CN102596961B (zh) | 2009-10-30 | 2015-12-02 | 詹森药业有限公司 | 咪唑并[1,2-b]哒嗪衍生物及其作为PDE10抑制剂的用途 |
AR080754A1 (es) | 2010-03-09 | 2012-05-09 | Janssen Pharmaceutica Nv | Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10 |
PT2609923T (pt) * | 2010-03-31 | 2017-08-30 | Gilead Pharmasset Llc | Processo para a cristalização de 2-(((s)- (perfluorofenoxi)(fenoxi)fosforil)amino)propanoato de (s)-isopropilo |
TW201201815A (en) * | 2010-05-28 | 2012-01-16 | Gilead Sciences Inc | 1'-substituted-carba-nucleoside prodrugs for antiviral treatment |
TW201305185A (zh) * | 2010-09-13 | 2013-02-01 | Gilead Sciences Inc | 用於抗病毒治療之2’-氟取代之碳-核苷類似物 |
KR101879887B1 (ko) * | 2010-09-20 | 2018-07-18 | 길리애드 사이언시즈, 인코포레이티드 | 항바이러스 치료용 2'-플루오로 치환된 카바-누클레오시드 유사체 |
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EP3042910B1 (en) | 2010-11-30 | 2019-01-09 | Gilead Pharmasset LLC | 2'-spiro-nucleosides for use in the therapy of hepatitis c |
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EP2691409B1 (en) | 2011-03-31 | 2018-02-21 | Idenix Pharmaceuticals LLC. | Compounds and pharmaceutical compositions for the treatment of viral infections |
US8877744B2 (en) * | 2011-04-04 | 2014-11-04 | Hoffmann-La Roche Inc. | 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors |
JP2014511875A (ja) * | 2011-04-13 | 2014-05-19 | メルク・シャープ・アンド・ドーム・コーポレーション | 2’−シアノ置換ヌクレオシド誘導体およびウイルス疾患の治療のためのその使用方法 |
US9156872B2 (en) | 2011-04-13 | 2015-10-13 | Merck Sharp & Dohme Corp. | 2′-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases |
JP2014515023A (ja) * | 2011-04-13 | 2014-06-26 | メルク・シャープ・アンド・ドーム・コーポレーション | 2’−置換ヌクレオシド誘導体およびウイルス疾患の処置のためのその使用方法 |
MX344600B (es) | 2011-06-27 | 2016-12-20 | Janssen Pharmaceutica Nv | Derivados de 1-aril-4-metil-[1,2,4]triazolo[4,3-a]quinoxalina. |
WO2013009737A1 (en) | 2011-07-13 | 2013-01-17 | Merck Sharp & Dohme Corp. | 5'-substituted nucleoside analogs and methods of use thereof for the treatment of viral diseases |
EP2731434A4 (en) | 2011-07-13 | 2014-12-31 | Merck Sharp & Dohme | 5'-SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHOD FOR THEIR USE FOR THE TREATMENT OF VIRUS DISEASES |
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EP2755983B1 (en) | 2011-09-12 | 2017-03-15 | Idenix Pharmaceuticals LLC. | Substituted carbonyloxymethylphosphoramidate compounds and pharmaceutical compositions for the treatment of viral infections |
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