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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Применить Всего найдено 349. Отображено 151.
13-03-2014 дата публикации

PYRAZOLO[1,5-A]PYRIMIDINES FOR ANTIVIRAL TREATMENT

Номер: US20140072554A1
Принадлежит: Gilead Sciences, Inc.

The invention provides compounds of Formula I or Formula II: 2. The method of wherein the Pneumovirinae virus infection is caused by human respiratory syncytial virus.3. The method of further comprising administering a therapeutically effective amount of at least one other therapeutic agent selected from ribavirin claim 1 , palivizumab claim 1 , motavizumab claim 1 , RSV-IGIV claim 1 , MEDI-557 claim 1 , A-60444 claim 1 , MDT-637 claim 1 , BMS-433771 claim 1 , ALN-RSV0 and ALX-0171 claim 1 , or mixtures thereof.4. The method of wherein the therapeutically effective amount is a daily dose of from 1 mg to 1 claim 1 ,000 mg administered in a single dose or multiple doses.5. The method of wherein the therapeutically effective amount is administered orally.6. The method of wherein the therapeutically effective amount is administered in an aqueous solution or suspension.7. The method of wherein the therapeutically effective amount is a daily dose of from 5 mg to 500 mg administered in a single dose or multiple doses.8. The method of wherein the therapeutically effective amount is administered orally.9. The method of wherein the therapeutically effective amount is administered in an aqueous solution or suspension.10. The method of wherein the pharmaceutically acceptable salt is a trifluoroacetic acid salt. This patent application is a continuation of U.S. patent application Ser. No. 13/905,410, filed May 30, 2013, which is a continuation of U.S. patent application Ser. No. 13/167,618, filed Jun. 23, 2011 (now U.S. Pat. No. 8,486,938), which claims the benefit of U.S. Provisional Patent Application No. 61/358,122, filed Jun. 24, 2010. These applications are incorporated herein by reference in their entireties.The invention relates generally to methods and compounds for treating Pneumovirinae virus infections, particularly methods and nucleosides for treating respiratory syncytial virus infections.Pneumovirinae viruses are negative-sense, single-stranded, RNA viruses that ...

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20-09-2011 дата публикации

Antiviral phosphonate analogs

Номер: US0008022083B2

The invention is related to phosphorus substituted compounds with antiviral activity, 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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12-01-2010 дата публикации

Therapeutic phosphonate compounds

Номер: US0007645747B2

The invention is related to phosphorus substituted therapeutic agents, compositions containing such phosphorus substituted agents, and therapeutic methods that include the administration of such phosphorus substituted agents, as well as to processes and intermediates useful for preparing such agents.

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18-11-2008 дата публикации

Anti-cancer phosphonate analogs

Номер: US0007452901B2

The invention is related to phosphorus substituted anti-cancer 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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25-05-2007 дата публикации

PHOSPHONATE ANALOGS OF HIV INHIBITOR COMPOUNDS

Номер: KR1020070053722A
Принадлежит:

The invention is related to phosphorus substituted anti-viral inhibitory 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. © KIPO & WIPO 2007 ...

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23-01-2014 дата публикации

MACROCYCLIC INHIBITORS OF FLAVIVIRIDAE VIRUSES

Номер: US20140023616A1
Принадлежит: Selcia Limited, Gilead Sciences, Inc.

Provided are compounds of Formula I: 127.-. (canceled)29. (canceled)30. The method of further comprising administering at least one additional therapeutic agent selected from the group consisting of interferons claim 28 , ribavirin or its analogs claim 28 , HCV NS3 protease inhibitors claim 28 , HCV NS5a inhibitors claim 28 , nucleoside or nucleotide inhibitors of HCV NS5B polymerase claim 28 , non-nucleoside inhibitors of HCV NS5B polymerase claim 28 , and TLR-7 agonists; or mixtures thereof.32. The method of further comprising administering at least one additional therapeutic agent selected from the group consisting of interferons claim 31 , ribavirin or its analogs claim 31 , HCV NS3 protease inhibitors claim 31 , HCV NS5a inhibitors claim 31 , nucleoside or nucleotide inhibitors of HCV NS5B polymerase claim 31 , non-nucleoside inhibitors of HCV NS5B polymerase claim 31 , and TLR-7 agonists; or mixtures thereof. The present application claims the benefit of U.S. Provisional Application No. 61/422,071, filed Dec. 10, 2010.The present application provides novel inhibitors Flaviviridae viruses, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.RNA viruses comprising the Flaviviridae family include at least three distinguishable genera including pestiviruses, flaviviruses, and hepaciviruses (Calisher, et al., J. Gen. Virol., 1993, 70, 37-43). While pestiviruses cause many economically important animal diseases such as bovine viral diarrhea virus (BVDV), classical swine fever virus (CSFV, hog cholera) and border disease of sheep (BDV), their importance in human disease is less well characterized (Moennig, V., et al., Adv. Vir. Res. 1992, 48, 53-98). Flaviviruses are responsible for important human diseases such as dengue fever and yellow fever while hepaciviruses cause hepatitis C virus infections in humans. Other important viral infections caused by the Flaviviridae family include West Nile virus (WNV) ...

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30-09-2008 дата публикации

Antiviral phosphonate analogs

Номер: US0007429565B2

The invention is related to phosphorus substituted compounds with antiviral activity, 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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02-02-2012 дата публикации

METHODS AND COMPOUNDS FOR TREATING PARAMYXOVIRIDAE VIRUS INFECTIONS

Номер: US20120027752A1
Принадлежит: Gilead Sciences, Inc.

Provided are methods for treating Paramyxoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula I: wherein the 1 position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are particularly useful for the treatment of Human parainfluenza and Human respiratory syncytial virus infections.

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22-01-2015 дата публикации

ANTIVIRAL PHOSPHONATE ANALOGS

Номер: US20150025039A1
Принадлежит:

The invention is related to phosphorus substituted compounds with antiviral activity, 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. 123-. (canceled)32. The method of claim 31 , wherein the viral infection is an HIV infection. This application claims the benefit of priority under 35 U.S.C. §119(e) to U.S. Provisional Patent Application Ser. Nos. 60/465,630, 60/465,400, 60/465,587, 60/465,463, 60/465,602, 60/465,598, 60/465,633, 60/465,550, 60/465,610, 60/465,720, 60/465,634, 60/465,537, 60/465,698, 60/465,667, 60/465,554, 60/465,553, 60/465,561, 60/465,548, 60/465,696, 60/465,347, 60/465,289, 60/465,478, 60/465,600, 60/465,591, 60/465,684, 60/465,821, 60/465,647, 60/465,742, 60/465,649, 60/465,690, 60/465,469, 60/465,408, 60/465,608, 60/465,584, 60/465,687, 60/465,759, 60/465,559, 60/465,322, 60/465,377, 60/465,844, and 60/465,544, all filed Apr. 25, 2003; and to U.S. Provisional Patent Application Ser. No. 60/490,799, filed Jul. 29, 2003; and to U.S. Provisional Patent Application Ser. Nos. 60/495,687, 60/495,490, 60/495,805, 60/495,684, 60/495,600, 60/495,342, 60/495,564, 60/495,772, 60/495,592, 60/495,453, 60/495,491, 60/495,964, 60/495,317, 60/495,696, 60/495,760, 60/495,334, 60/495,671, 60/495,349, 60/495,273, 60/495,763, 60/495,345, 60/495,602, 60/495,343, 60/495,344, 60/495,278, 60/495,277, 60/495,275, 60/495,630, 60/495,485, 60/495,430, 60/495,388, 60/495,341, 60/495,631, 60/495,633, 60/495,632, 60/495,539, 60/495,387, 60/495,392, 60/495,425, 60/495,393, and 60/495,616, all filed Aug. 15, 2003; and to U.S. Provisional Patent Application Ser. No. 60/510,245, filed Oct. 10, 2003; and to U.S. Provisional Patent Application Ser. Nos. 60/514,202, 60/513,948, and 60/514,258, all filed Oct. 24, 2003; and to U.S. Provisional Patent Application Ser. No. 60/515,266, filed Oct. 29, 2003; and to U.S. Provisional Patent ...

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23-09-2014 дата публикации

Antiviral compounds

Номер: US0008841278B2

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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16-07-2013 дата публикации

Pyrazolo[1,5-a]pyrimidines for antiviral treatment

Номер: US0008486938B2

The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

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11-10-2006 дата публикации

ANTIVIRAL PHOSPHONATE ANALOGS

Номер: KR1020060105426A
Принадлежит:

The invention is related to phosphorus substituted compounds with antiviral activity, 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. © KIPO & WIPO 2007 ...

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30-03-2006 дата публикации

ANTI-INFLAMMATORY PHOSPHONATE COMPOUNDS

Номер: KR1020060028632A
Принадлежит:

The invention is related to phosphorus substituted anti-inflammatory 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. © KIPO & WIPO 2007 ...

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07-06-2006 дата публикации

IMMUNOMODULATOR PHOSPHONATE CONJUGATES

Номер: KR1020060061292A
Принадлежит:

The invention is related to phosphonate substituted compounds having immuno-modulatory activity, 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. © KIPO & WIPO 2007 ...

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05-05-2017 дата публикации

Compuestos derivados de pirrolo1,2-f1,2,4triazina ,composición farmacéutica que los comprende y su uso en el tratamiento de una infección por virus sincicial compuestos intermediarios. pct

Номер: CL2016001120A1
Принадлежит:

LA SOLICITUD SE REFIERE A COMPUESTOS DERIVADOS DE PIRROLO1,2-F1,2,4TRIAZINA , A UNA COMPOSICIÓN FARMACÉUTICA QUE LOS COMPRENDE Y A SU USO EN EL TRATAMIENTO DE UNA INFECCIÓN POR VIRUS SINCICIAL COMPUESTOS INTERMEDIARIOS.

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15-04-2014 дата публикации

Antiviral compounds

Номер: US0008697861B2

The invention is related to phosphorus substituted anti-viral inhibitory 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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08-06-2006 дата публикации

ANTI-CANCER PHOSPHONATE ANALOGS

Номер: KR1020060061930A
Принадлежит:

The invention is related to phosphorus substituted anti-cancer 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. © KIPO & WIPO 2007 ...

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16-07-2009 дата публикации

KINASE INHIBITORY PHOSPHONATE ANALOGS

Номер: US2009181930A1
Принадлежит:

The invention is related to phosphorus substituted kinase inhibitory 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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04-12-2012 дата публикации

Nucleoside analogs for antiviral treatment

Номер: US0008324179B2

The invention provides unsaturated phosphonates of Formula I or a tautomer or pharmaceutically acceptable salt thereof, as described herein, as well as pharmaceutical compositions comprising the compounds, and therapeutic methods comprising administering the compounds. The compounds have anti-viral properties and are useful for treating viral infections (e.g. HCV) in animals (e.g. humans).

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29-09-2005 дата публикации

Antiviral phosphonate analogs

Номер: US2005215513A1
Принадлежит:

The invention is related to phosphorus substituted compounds with antiviral activity, 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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22-09-2005 дата публикации

Cellular accumulation of phosphonate analogs of HIV protease inhibitor compounds

Номер: US2005209197A1
Принадлежит:

Phosphonate substituted compounds with HIV protease inhibitory properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit HIV protease activity and/or are useful therapeutically for the treatment of AIDS and other antiviral infections, as well as in assays for the detection of HIV protease.

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05-11-2009 дата публикации

ANTIVIRAL PHOSPHONATE ANALOGS

Номер: US2009275535A1
Принадлежит:

The invention is related to phosphorus substituted compounds with antiviral activity, 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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22-09-2015 дата публикации

Antiviral phosphonate analogs

Номер: US0009139604B2

The invention is related to phosphorus substituted compounds with antiviral activity, 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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13-08-2009 дата публикации

Phosphonate Analogs of Hiv Inhibitor Compounds

Номер: US2009202470A1
Принадлежит:

The invention is related to phosphorus substituted anti-viral inhibitory 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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25-04-2007 дата публикации

NUCLEOSIDE PHOSPHONATE CONJUGATES AS ANTI HIV AGENTS

Номер: KR1020070043867A
Принадлежит:

The invention is related to phosphorus substituted anti-viral inhibitory 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. © KIPO & WIPO 2007 ...

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23-04-2015 дата публикации

METHODS AND COMPOUNDS FOR TREATING PARAMYXOVIRIDAE VIRUS INFECTIONS

Номер: US20150111839A1
Принадлежит:

Provided are methods for treating Paramyxoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula I: 4. The method of wherein Ris CN claim 1 , methyl claim 1 , ethenyl claim 1 , or ethynyl.5. The method of wherein Ris OR.6. The method of wherein Ris OH claim 1 , —OC(═O)R claim 1 , or —OC(═O)OR.7. The method of wherein Ris NRRor OR.8. The method of wherein Ris NH.9. The method of wherein Ris OH.10. The method of wherein Ris H.11. The method of wherein Ris NH.12. The method of wherein Ris H.14. The method of further comprising a pharmaceutically acceptable carrier or excipient.15. The method of further comprising administering a therapeutically effective amount of at least one other therapeutic agent or composition thereof selected from the group consisting of a corticosteroid claim 1 , an anti-inflammatory signal transduction modulator claim 1 , a β2-adrenoreceptor agonist bronchodilator claim 1 , an anticholinergic claim 1 , a mucolytic agent claim 1 , hypertonic saline and other drugs for treating Paramyxoviridae virus infections; or mixtures thereof.16. The method of wherein the at least one other thereapeutic agent is ribavirin claim 15 , palivizumab claim 15 , motavizumab claim 15 , RSV-IGIV (RespiGam®) claim 15 , MEDI-557 claim 15 , A-60444 claim 15 , MDT-637 or BMS-433771 or mixtures thereof.17. The method of wherein at least one therapeutic agent or mixtures thereof is administered by inhalation.18. The method of wherein at least one therapeutic agent or mixtures thereof is administered by nebulization.19. The method of wherein the Paramyxoviridae infection is caused by a Paramyxovirina virus.20. The method of wherein the Paramyxoviridae infection is caused by a Respirovirus virus.21. The method of wherein the Paramyxoviridae infection is caused by a type 1 or 3 Human parainfluenza virus.22. The method of wherein the Pararnyxoviridae infection is caused by a Pneumovirinae virus.23. The method of wherein the ...

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18-07-2012 дата публикации

Nucleoside phosphonate conjugates as anti HIV agents

Номер: CN0101914124B
Принадлежит:

The invention is related to phosphorus substituted anti-viral inhibitory 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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24-12-2004 дата публикации

CELLULAR ACCUMULATION OF PHOSPHONATE ANALOGS OF HIV PROTEASE INHIBITOR COMPOUNDS AND THE COMPOUNDS AS SUCH

Номер: KR20040108757A
Принадлежит:

Phosphonate substituted compounds with HIV protease inhibitory properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit HIV protease activity and/or are useful therapeutically for the treatment of AIDS and other antiviral infections, as well as in assays for the detection of HIV protease. © KIPO & WIPO 2007 ...

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15-03-2005 дата публикации

(Hetero)aryl-bicyclic heteroaryl derivatives, their preparation and their use as protease inhibitors

Номер: US0006867200B1

The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a partially unsaturated bicyclic heterocyclic ring structure, and B represents an aryl or a heteroaryl group. Preferred compounds of the present invention comprise a benzimidazole or indole nucleus. The compounds of this invention are inhibitors of serine proteases, Urokinase (uPA), Factor Xa (FXa), and/or Factor VIIa (FVIIa), and have utility as anti cancer agents and/or as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals.

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10-03-2006 дата публикации

KINASE INHIBITOR PHOSPHONATE CONJUGATES

Номер: KR1020060022647A
Принадлежит:

The invention is related to phosphorus substituted kinase inhibitory 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. © KIPO & WIPO 2007 ...

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24-11-2005 дата публикации

Kinase inhibitory phosphonate analogs

Номер: US2005261253A1
Принадлежит:

The invention is related to phosphorus substituted kinase inhibitory 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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11-12-2012 дата публикации

Antiviral compounds

Номер: US0008329926B2

The invention is related to phosphorus substituted anti-viral inhibitory 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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05-12-2018 дата публикации

METHODS FOR TREATING VIRUS INFECTIONS FILOVIRIDAE

Номер: SV2017005561A
Принадлежит:

SE PROPORCIONAN COMPUESTOS Y COMPOSICIONES FARMACÉUTICAS PARA TRATAR INFECCIONES POR EL VIRUS FILOVIRIDAE, ADMINISTRANDO RIBÓSIDOS, FOSFATOS DE RIBÓSIDOS, Y PROFÁRMACOS DE LOS MISMOS, DE FÓRMULA (IV). (VER FÓRMULA). LOS COMPUESTOS Y COMPOSICIONES PROVISTOS SON PARTICULARMENTE ÚTILES PARA EL TRATAMIENTO DE INFECCIONES POR EL VIRUS MARBURG, VIRUS DE EBOLA Y VIRUS CUEVA.

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24-01-2013 дата публикации

MACROCYCLIC INHIBITORS OF FLAVIVIRIDAE VIRUSES

Номер: US20130022573A1
Принадлежит: Selcia Limited, Gilead Sciences, Inc.

Provided are compounds of Formula I: 3. The compound of wherein each Rand Ris H.4. The compound of wherein Ris methyl.5. The compound of wherein Ais optionally substituted (C)alkylene or optionally substituted (C)alkenylene.7. The compound of wherein Ris H.8. The compound of wherein Ais optionally substituted arylene.11. The compound of wherein each Ror Ris independently H claim 10 , optionally substituted (C-C)alkyl or halogen.12. The compound of wherein each Rand Ris H.13. The compound of wherein Ris optionally substituted (C-C)alkyl claim 2 , optionally substituted aryl claim 2 , or optionally substituted aryl(C-C)alkyl.14. The compound of wherein Ris optionally substituted (C-C)alkyl.15. The compound of wherein Ris optionally substituted aryl(C-C)alkyl.16. The compound of wherein Ris optionally substituted benzyl.18. The compound of wherein Ris OR claim 17 , CHOR claim 17 , N(R) claim 17 , NHCOR claim 17 , NHC(O)OR claim 17 , NHC(O)N(R) claim 17 , NHC(NR)R claim 17 , NHC(NR)N(R) claim 17 , C(O)N(R) claim 17 , S(O)N(R) claim 17 , NHS(O)OR claim 17 , NHS(O)Ror NHS(O)N(R).19. The compound of wherein Ris OH.21. The compound of wherein Ris O(C-C)alkyl.22. The compound of wherein Ris (C-C)alkyl.23. The compound of or a pharmaceutically acceptable salt thereof claim 2 , wherein:{'sup': 1', '1, 'Xis O or NR;'}{'sup': '1', 'sub': 1', '4', '2', '4', '2', '4, 'each Ris independently H, optionally substituted (C-C)alkyl, optionally substituted (C-C)alkenyl or optionally substituted (C-C)alkynyl;'}{'sup': 4', '7', '7', '7', '16', '16', '7', '7, 'sub': 1', '4', '2', '4', '2', '4', '2', '2', '2', '2', '2, 'each Ris independently H, optionally substituted (C-C)alkyl, optionally substituted (C-C)alkenyl, optionally substituted (C-C)alkynyl, cyano, C(O)R, C(O)OR, CON(R), S(O)R, S(O)R, S(O)ORor S(O)N(R);'}{'sup': 5', '6, 'sub': 0', '4, 'Ris aryl(C-C)alkyl, optionally substituted with one or more R;'}{'sup': 6', '4', '4', '4', '16', '16', '1', '1', '1', '1', '1', '1', '1', '1', '1 ...

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19-01-2016 дата публикации

Pyrazolo[1,5-A]pyrimidines for antiviral treatment

Номер: US0009238039B2

The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

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29-11-2018 дата публикации

COMPOUNDS OF TOLL-LIKE RECEPTOR MODULATORS

Номер: SV2017005528A
Принадлежит:

LA PRESENTE DESCRIPCION SE REFIERE EN GENERAL A COMPUESTOS MODULADORES DE RECEPTOR TIPO TOLL, TALES COMO COMPUESTOS DE DIAMINO PIRIDO [3,2 D] PIRIMIDINA Y COMPOSICIONES FARMACÉUTICAS QUE, ENTRE OTRAS COSAS, MODULAN LOS RECEPTORES TIPO TOLL (POR EJEMPLO TLR-8), Y MÉTODOS DE FABRICACIÓN Y USOS DE LOS MISMOS ...

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24-11-2011 дата публикации

ANTIVIRAL PHOSPHONATE ANALOGS

Номер: US20110288053A1
Принадлежит: Gilead Sciences, Inc.

The invention is related to phosphorus substituted compounds with antiviral activity, 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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02-08-2012 дата публикации

ANTI-RSV COMPOUNDS

Номер: US20120196846A1
Принадлежит: Gilead Sciences, Inc.

The present invention relates to anti-RSV compounds of Formula (I) and methods for use of the compounds in the treatment and prevention of RSV infection. 2. The compound of wherein A is C-Caryl claim 1 , or monocyclic 6-membered heteroaryl.3. The compound of wherein A is monocyclic 5-membered heteroaryl or bicyclic 8- to 10-membered heteroaryl.4. The compound of wherein A is a monocyclic 5-membered heteroaryl; Ris alkyl claim 1 , or aryl; Ris hydrogen claim 1 , or alkyl; Ris cycloalkyl claim 1 , or alkyl; Ris hydrogen; Ris hydrogen claim 1 , or halo.5. The compound of wherein A is thienyl or pyrazolyl group.6. The compound of wherein A is a bicyclic 8- to 10-membered heteroaryl; Ris alkyl claim 1 , or hydrogen; Ris hydrogen claim 1 , or alkyl; Ris cycloalkyl claim 1 , or alkyl; Ris hydrogen; Ris hydrogen claim 1 , or halo.7. The compound of wherein A is indolyl claim 6 , indazolyl claim 6 , or quinoxalinyl group.9. The compound of wherein X and Z are CH claim 8 , Y is N.10. The compound of wherein X claim 8 , Y and Z are CH.11. The compound of wherein X and Z are N claim 8 , Y is CH.12. The compound of wherein X and Z are CH; Y is N; Ris haloalkyl claim 8 , or heterocyclyl claim 8 , said heterocyclyl is optionally substituted by one to two substituents independently selected from the group consisting of halo claim 8 , hydroxyl claim 8 , alkoxy-alkyl- claim 8 , alkyl claim 8 , haloalkyl claim 8 , or hydroxyl-alkyl-; Ris hydrogen; Ris hydrogen claim 8 , alkyl claim 8 , heteroaryl claim 8 , heteroaryl-alkyl- claim 8 , or cycloalkyl claim 8 , said alkyl is optionally substituted by one substituent selected from the group consisting of NH—C(O)— claim 8 , halo claim 8 , hydroxyl claim 8 , NH—SO— claim 8 , alkoxy-alkyl- claim 8 , and heterocyclyl; Ris hydrogen claim 8 , or alkyl; Rand Rtaken together with the nitrogen atom to which they are attached optionally form a 3- to 7-membered ring; Ris hydrogen claim 8 , or halo; or a pharmaceutically acceptable salt thereof; or an ...

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05-06-2014 дата публикации

PYRAZOLO[1,5-A]PYRIMIDINES FOR ANTIVIRAL TREATMENT

Номер: US20140154240A1
Принадлежит: Gilead Sciences Inc

The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

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26-08-2008 дата публикации

Kinase inhibitory phosphonate analogs

Номер: US0007417055B2

The invention is related to phosphorus substituted kinase inhibitory 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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18-01-2018 дата публикации

QUINAZOLINE DERIVATIVES USED TO TREAT HIV

Номер: SV2017005471A
Принадлежит:

SE DESCRIBEN EN EL PRESENTE DOCUMENTO COMPUESTOS DE FÓRMULA (I) Y TAUTÓMEROS Y SALES FARMACÉUTICAS DE LOS MISMOS, COMPOSICIONES Y FORMULACIONES QUE CONTIENEN DICHOS COMPUESTOS, Y MÉTODOS PARA USAR Y PREPARAR DICHOS COMPUESTOS ...

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03-02-2015 дата публикации

Pyrazolo[1,5-A]pyrimidines as antiviral agents

Номер: US8946238B2
Принадлежит: GILEAD SCIENCES INC, GILEAD SCIENCES, INC.

The invention provides compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections. The compounds and compositions are useful for treating Pneumovirinae virus infection including Human respiratory syncytial virus infections.

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27-11-2012 дата публикации

Phosphonate analogs of HIV inhibitor compounds

Номер: US0008318701B2

The invention is related to phosphorus substituted anti-viral inhibitory 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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29-04-2010 дата публикации

NUCLEOSIDE ANALOGS FOR ANTIVIRAL TREATMENT

Номер: US20100104532A1
Принадлежит: GILEAD SCIENCES, INC.

The invention provides unsaturated phosphonates of Formula I or a tautomer or pharmaceutically accepatble salt thereof, as described herein, as well as pharmaceutical compositions comprising the compounds, and therapeutic methods comprising administering the compounds. The compounds have anti-viral properties and are useful for treating viral infections (e.g. HCV) in animals (e.g. humans).

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05-01-2012 дата публикации

PYRAZOLO[1,5-A]PYRIMIDINES FOR ANTIVIRAL TREATMENT

Номер: US20120003215A1
Принадлежит: Gilead Sciences, Inc.

The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

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10-09-2009 дата публикации

PHOSPHONATE COMPOUNDS HAVING IMMUNO-MODULATORY ACTIVITY

Номер: US2009227543A1
Принадлежит:

The invention is related to phosphonate substituted compounds having immuno-modulatory activity, 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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13-04-2006 дата публикации

Anti-cancer phosphonate analogs

Номер: US2006079478A1
Принадлежит:

The invention is related to phosphorus substituted anti-cancer 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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08-05-2008 дата публикации

Phosphonate inhibitors of HCV

Номер: US2008107628A1
Принадлежит:

A compound of Formula I, Formula II, Formula III, or Formula IV: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, therapeutic compositions containing such compounds, and therapeutic methods that include the administration of such compounds.

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30-11-2010 дата публикации

Phosphonate inhibitors of HCV

Номер: US0007842672B2

A compound of Formula I, Formula II, Formula III, or Formula IV: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, therapeutic compositions containing such compounds, and therapeutic methods that include the administration of such compounds.

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16-02-2006 дата публикации

Phosphonate compounds having immuno-modulatory activity

Номер: US2006035866A1
Принадлежит:

The invention is related to phosphonate substituted compounds having immuno-modulatory activity, 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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19-04-2013 дата публикации

Uso de compuestos derivados de ribosas 1 sustituidas que comprenden nucleobases de pirrolo[1,2-f][1,2,4]triazina para tratar infecciones por paramyxoviridae; compuestos derivados de ribosas 1 sustituidas que comprenden nucleobases de pirrolo[1,2-f][1,2,4]triazina; y composicion farmaceutica que los comprende.

Номер: CL2013000077A1
Принадлежит:

Uso de compuestos derivados de ribosas 1 sustituidas que comprenden nucleobases de pirrolo[1,2-f][1,2,4]triazina para tratar infecciones por paramyxoviridae; compuestos derivados de ribosas 1 sustituidas que comprenden nucleobases de pirrolo[1,2-f][1,2,4]triazina; y composición farmacéutica que los comprende.

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01-10-2009 дата публикации

ANTI-INFLAMMATORY PHOSPHONATE COMPOUNDS

Номер: US2009247488A1
Принадлежит:

The invention is related to phosphorus substituted anti-inflammatory 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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18-06-2015 дата публикации

PYRAZOLO[1,5-A]PYRIMIDINES AS ANTIVIRAL AGENTS

Номер: US20150166546A1
Принадлежит:

The invention provides compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections. The compounds and compositions are useful for treating Pneumovirinae virus infection including Human respiratory syncytial virus infections. 130-. (canceled) This application is a divisional of U.S. patent application Ser. No. 13/722,962, filed Dec. 20, 2012, which claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Application No. 61/579,625, filed Dec. 22, 2011, and U.S. Provisional Application No. 61/618,510, filed Mar. 30, 2012. The foregoing applications are incorporated herein by reference in their entireties.Pneumovirinae viruses are negative-sense, single-stranded, RNA viruses that are responsible for many prevalent human and animal diseases. The Pneumovirinae sub-family of viruses is a part of the family Paramyxoviridae and includes human respiratory syncytial virus (HRSV). Almost all children will have had an HRSV infection by their second birthday. HRSV is the major cause of lower respiratory tract infections in infancy and childhood with 0.5% to 2% of those infected requiring hospitalization. The elderly and adults with chronic heart, lung disease or those that are immunosuppressed also have a high risk for developing severe HRSV disease (http://www.cdc.gov/rsv/index.html). No vaccine to prevent HRSV infection is currently available. The monoclonal antibody palivizumab is available for immunoprophylaxis, but its use is restricted to infants at high risk, e.g., premature infants or those with either congenital heart or lung disease, and the cost for general use is often prohibitive. In addition, nucleoside analog ribavirin has been approved as the only antiviral agent to treat HRSV infections but has limited efficacy. Therefore, there is a need for anti-Pneumovirinae therapeutics.Provided herein are methods and compounds for the treatment of infections caused by the Pneumovirinae virus family.Accordingly, ...

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18-07-2018 дата публикации

METHODS FOR TREATING VIRUS INFECTIONS FILOVIRIDAE

Номер: SV2017005424A
Принадлежит:

SE PROPORCIONAN COMPUESTOS, MÉTODOS, Y COMPOSICIONES FARMACÉUTICAS PARA TRATAR INFECCIONES POR EL VIRUS FILOVIRIDAE ADMINISTRANDO RIBÓSIDOS, FOSFATOS DE RIBÓSIDO, Y PROFÁRMACOS DEL MISMO, DE FÓRMULA IV: (VER FORMULA). LOS COMPUESTOS, COMPOSICIONES, Y MÉTODOS PROVISTOS SON PARTICULARMENTE ÚTILES PARA EL TRATAMIENTO DE INFECCIONES POR EL VIRUS DE MARBURG, VIRUS DE EBOLA Y VIRUS CUEVA.

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13-01-2015 дата публикации

Macrocyclic inhibitors of flaviviridae viruses

Номер: US0008933015B2

Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.

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04-06-2015 дата публикации

METHODS AND COMPOUNDS FOR TREATING PARAMYXOVIRIDAE VIRUS INFECTIONS

Номер: US20150152116A1
Принадлежит:

Provided are methods for treating Paramyxoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula I: 124.-. (canceled)2633.-. (canceled) This application claims the benefit of U.S. Provisional Application 61/366,609 filed on Jul. 22, 2010.The invention relates generally to methods and compounds for treating Paramyxoviridae virus infections, particularly methods and nucleosides for treating respiratory syncytial virus infections and parainfluenza virus infections.Paramyxoviruses of the Paramyxoviridae family are negative-sense, single-stranded, RNA viruses that are responsible for many prevalent human and animal diseases. These viruses comprise at least two major subfamilies, Paramyxovirinae and Pneumovirinae. The subfamily Paramyxovirina includes the human parainfluenza viruses (HPIV), measles virus and mumps virus. Although, vaccines are available to prevent measles and mumps infections, these infections caused 745, 00 deaths in 2001 so additional treatments would be desireable for susceptible populations. HPIV are the second most common cause of lower respiratory tract infection in younger children and collectively cause about 75% of the cases of Croup (http://www.cdc.gov/ncidod/dvrd/revb/respiratory/hpivfeat.htm). HPIVs can cause repeated infections throughout life including upper respiratory tract illness and even serious lower respiratory tract disease (e.g., pneumonia, bronchitis, and bronchiolitis), the latter being especially of concern among the elderly, and among patients with compromised immune systems (Sable, 1995, 9, 987-1003). Currently, no vaccines are available to prevent HPIV infections. Therefore there is a need for anti-Paramyxovirina therapeutics.The subfamily Pneumovirinae includes Human respiratory syncytial virus (HRSV). Almost all children will have had an HRSV infection by their second birthday. HRSV is the major cause of lower respiratory tract infections in infancy and childhood with 0.5% ...

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21-06-2012 дата публикации

ANTIVIRAL COMPOUNDS

Номер: US20120157404A1
Принадлежит: GILEAD SCIENCES, INC.

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. 227-. (canceled)40. The method of claim 1 , further comprising administering at least one additional therapeutic agent.41. The method of claim 40 , wherein said additional therapeutic agent is selected from the group consisting of ribavirin analogs claim 40 , NS3 protease inhibitors claim 40 , NS5b polymerase inhibitors claim 40 , alpha-glucosidase 1 inhibitors claim 40 , hepatoprotectants claim 40 , non-nucleoside inhibitors of HCV claim 40 , and other drugs for treating HCV.42. The method of claim 40 , wherein said additional therapeutic agent is a nucleoside analogue.43. The method of claim 42 , wherein said nucleoside analogue is selected from ribavirin claim 42 , viramidine claim 42 , levovirin claim 42 , an L-nucleoside claim 42 , and isatoribine.44. The method of claim 39 , further comprising administering at least one additional therapeutic agent.45. The method of claim 44 , wherein said additional therapeutic agent is selected from the group consisting of ribavirin analogs claim 44 , NS3 protease inhibitors claim 44 , NS5b polymerase inhibitors claim 44 , alpha-glucosidase 1 inhibitors claim 44 , hepatoprotectants claim 44 , non-nucleoside inhibitors of HCV claim 44 , and other drugs for treating HCV.46. The method of claim 44 , wherein said additional therapeutic agent is a nucleoside analogue.47. The method of claim 46 , wherein said nucleoside analogue is selected from ribavirin claim 46 , viramidine claim 46 , levovirin claim 46 , an L-nucleoside claim 46 , and isatoribine. This application claims priority to U.S. Provisional Application Nos. 61/177,972, filed 13 May 2009; 61/224,745, filed 10 Jul. 2009; and 61/238,760, filed 1 Sep. 2009. The entire content of each of these applications is hereby incorporated ...

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07-04-2015 дата публикации

Anti-RSV compounds

Номер: US0008999969B2

The present invention relates to anti-RSV compounds of Formula (I) and methods for use of the compounds in the treatment and prevention of RSV infection.

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28-01-2010 дата публикации

ANTI-CANCER PHOSPHONATE ANALOGS

Номер: US2010022467A1
Принадлежит:

The invention is related to phosphorus substituted anti-cancer 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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14-05-2015 дата публикации

PYRROLO[1,2-f][1,2,4]TRIAZINES USEFUL FOR TREATING RESPIRATORY SYNCITIAL VIRUS INFECTIONS

Номер: US20150133395A1
Принадлежит:

Provided herein are formulations, methods and substituted tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds. 2. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein both Rand Rare H claim 1 , and Ris OH.3. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein both Rand Rare H claim 1 , Ris F.5. A compound according to claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , wherein Ris CN claim 4 , methyl claim 4 , ethyl claim 4 , ethenyl claim 4 , ethynyl claim 4 , azido claim 4 , F claim 4 , Cl claim 4 , —CHCl claim 4 , —CHF claim 4 , —CHF claim 4 , or —CF.6. A compound according to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris F.7. A compound according to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris OH.8. A compound according to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris F and Ris CN.9. A compound according to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris OH and Ris CN.10. A compound according to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris F claim 5 , and Ris methyl claim 5 , ethyl claim 5 , vinyl claim 5 , or ethynyl.11. A compound according to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris OH claim 5 , and Ris methyl claim 5 , ethyl claim 5 , vinyl claim 5 , or ethynyl.12. A compound according to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris F and Ris halomethyl.13. A compound according to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris OH and Ris halomethyl.14. A ...

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28-10-2014 дата публикации

Antiviral phosphonate analogs

Номер: US0008871785B2

The invention is related to phosphorus substituted compounds with antiviral activity, 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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20-02-2014 дата публикации

ANTIVIRAL COMPOUNDS

Номер: US20140051656A1
Принадлежит: Gilead Sciences, Inc.

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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03-01-2012 дата публикации

Antiviral compounds

Номер: US0008088368B2

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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18-10-2012 дата публикации

ANTIVIRAL COMPOUNDS

Номер: US20120264711A1
Принадлежит: GILEAD SCIENCES, INC.

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. 127-. (canceled)29. The compound of claim 28 , wherein Lis a thienothiophene ring structure.32. A pharmaceutical composition comprising the compound as described in or a pharmaceutically acceptable salt claim 28 , or prodrug thereof; and at least one pharmaceutically acceptable carrier.33. The pharmaceutical composition of claim 28 , further comprising at least one additional therapeutic agent.34. The pharmaceutical composition of claim 33 , wherein said additional therapeutic agent is selected from the group consisting of ribavirin analogs claim 33 , NS3 protease inhibitors claim 33 , NS5b polymerase inhibitors claim 33 , alpha-glucosidase 1 inhibitors claim 33 , hepatoprotectants claim 33 , non-nucleoside inhibitors of HCV claim 33 , and other drugs for treating HCV.35. The pharmaceutical composition according to claim 34 , further comprising a nucleoside analogue.36. The pharmaceutical composition according to claim 35 , wherein said nucleoside analogue is selected from ribavirin claim 35 , viramidine claim 35 , levovirin claim 35 , an L-nucleoside claim 35 , and isatoribine.3736. A method for treating or preventing an HCV infection in a subject claims 28 , which comprises administering to the subject a compound of -.39. A pharmaceutical composition comprising the compound as described in or a pharmaceutically acceptable salt claim 38 , or prodrug thereof; and at least one pharmaceutically acceptable carrier.40. The pharmaceutical composition of claim 38 , further comprising at least one additional therapeutic agent.41. The pharmaceutical composition of claim 40 , wherein said additional therapeutic agent is selected from the group consisting of ribavirin analogs claim 40 , NS3 protease inhibitors claim 40 , NS5b polymerase ...

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15-12-2010 дата публикации

Nucleoside phosphonate conjugates as anti HIV agents

Номер: CN0101914124A
Принадлежит:

The invention is related to phosphorus substituted anti-viral inhibitory 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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11-04-2013 дата публикации

Phosphonate analogs of hiv inhibitor compounds

Номер: US20130090299A1
Принадлежит: Gilead Sciences Inc

The invention is related to phosphorus substituted anti-viral inhibitory 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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11-04-2013 дата публикации

ANTIVIRAL COMPOUNDS

Номер: US20130090302A1
Принадлежит: Gilead Sciences, Inc.

The invention is related to phosphorus substituted anti-viral inhibitory 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. 1103-. (canceled) This application claims priority to U.S. Application No. 60/591,811, filed Jul. 27, 2004, the disclosures of which are incorporated by reference in their entirety. In particular, the figures described on pages 161 to 184 are incorporated as Figures herein.The invention relates generally to compounds with HIV inhibitory activity.Improving the delivery of drugs and other agents to target cells and tissues has been the focus of considerable research for many years. Though many attempts have been made to develop effective methods for importing biologically active molecules into cells, both in vivo and in vitro, none has proved to be entirely satisfactory. Optimizing the association of the inhibitory drug with its intracellular target, while minimizing intercellular redistribution of the drug, e.g., to neighboring cells, is often difficult or inefficient.Most agents currently administered to a patient parenterally are not targeted, resulting in systemic delivery of the agent to cells and tissues of the body where it is unnecessary, and often undesirable. This may result in adverse drug side effects, and often limits the dose of a drug (e.g., glucocorticoids and other anti-inflammatory drugs) that can be administered. By comparison, although oral administration of drugs is generally recognized as a convenient and economical method of administration, oral administration can result in either (a) uptake of the drug through the cellular and tissue barriers, e.g., blood/brain, epithelial, cell membrane, resulting in undesirable systemic distribution, or (b) temporary residence of the drug within the gastrointestinal tract. Accordingly, a major goal has been to develop methods for ...

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27-06-2013 дата публикации

PYRAZOLO[1,5-A]PYRIMIDINES AS ANTIVIRAL AGENTS

Номер: US20130164280A1
Принадлежит: Gilead Sciences, Inc.

The invention provides compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections. The compounds and compositions are useful for treating Pneumovirinae virus infection including Human respiratory syncytial virus infections. 2. The compound of wherein each Ris H.3. The compound of wherein n is 3.4. The compound of wherein each Ris H.5. The compound of wherein A is —(CH)—.7. The compound of wherein Ar is phenyl claim 1 , pyridyl claim 1 , 1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthyl claim 1 , indazolyl claim 1 , 1 claim 1 ,6-naphthyridyl claim 1 , 2 claim 1 ,3 claim 1 ,-dihydroindanyl claim 1 , quinolyl claim 1 , indolyl claim 1 , 4H-benzo][d][1 claim 1 ,3]dioxanyl claim 1 , pyrazolo[1 claim 1 ,5-a]pyridinyl claim 1 , imidazo[1 claim 1 ,2-a]pyridinyl claim 1 , 1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydroquinolyl claim 1 , benzo[d][1 claim 1 ,3]dioxolyl claim 1 , quinoxalyl claim 1 , isoquinolyl claim 1 , naphthyl claim 1 , thiophenyl claim 1 , pyrazolyl claim 1 , 4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydrobenzothiophenyl or pyrazolo[3 claim 1 ,4 claim 1 ,b]pyridinyl claim 1 , wherein any phenyl claim 1 , pyridyl claim 1 , 1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthyl claim 1 , indazolyl claim 1 , 1 claim 1 ,6-naphthyridyl claim 1 , 2 claim 1 ,3 claim 1 ,-dihydroindanyl claim 1 , quinolyl claim 1 , indolyl claim 1 , 4H-benzo][d][1 claim 1 ,3]dioxanyl claim 1 , pyrazolo[1 claim 1 ,5-a]pyridinyl claim 1 , imidazo[1 claim 1 ,2-a]pyridinyl claim 1 , 1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydroquinolyl claim 1 , benzo[d][1 claim 1 ,3]dioxolyl claim 1 , quinoxalyl claim 1 , isoquinolyl claim 1 , naphthyl claim 1 , thiophenyl claim 1 , pyrazolyl claim 1 , 4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydrobenzothiophenyl or pyrazolo[3 claim 1 ,4 claim 1 ,b]pyridinyl of Ar is optionally substituted with 1 to 5 R.8. The compound of wherein each Ris independently OR claim 1 , CN claim 1 , S(O)R claim 1 , ...

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28-11-2013 дата публикации

ANTIVIRAL PHOSPHONATE ANALOGS

Номер: US20130316969A1
Принадлежит: Gilead Sciences, Inc.

The invention is related to phosphorus substituted compounds with antiviral activity, 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. 2. The conjugate of wherein C-Csubstituted alkyl claim 1 , C-Csubstituted alkenyl claim 1 , C-Csubstituted alkynyl claim 1 , C-Csubstituted aryl claim 1 , and C-Csubstituted heterocycle are independently substituted with one or more substituents selected from F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , OH claim 1 , —NH claim 1 , —NH claim 1 , —NHR claim 1 , —NR claim 1 , —NR claim 1 , C-Calkylhalide claim 1 , carboxylate claim 1 , sulfate claim 1 , sulfamate claim 1 , sulfonate claim 1 , 5-7 membered ring sultam claim 1 , C-Calkylsulfonate claim 1 , C-Calkylamino claim 1 , 4-dialkylaminopyridinium claim 1 , C-Calkylhydroxyl claim 1 , C-Calkylthiol claim 1 , —SOR claim 1 , —SOAr claim 1 , —SOAr claim 1 , —SAr claim 1 , —SONR claim 1 , —SOR claim 1 , —COR claim 1 , —C(═O)NR claim 1 , 5-7 membered ring lactam claim 1 , 5-7 membered ring lactone claim 1 , —CN claim 1 , —N claim 1 , —NO claim 1 , C-Calkoxy claim 1 , C-Ctrifluoroalkyl claim 1 , C-Calkyl claim 1 , C-Ccarbocycle claim 1 , C-Caryl claim 1 , C-Cheterocycle claim 1 , polyethyleneoxy claim 1 , phosphonate claim 1 , phosphate claim 1 , and a prodrug moiety.3. The conjugate of wherein protecting group is selected from a carboxyl ester claim 1 , a carboxamide claim 1 , an aryl ether claim 1 , an alkyl ether claim 1 , a trialkylsilyl ether claim 1 , a sulfonic acid ester claim 1 , a carbonate claim 1 , and a carbamate.5. The conjugate of wherein X is O and each Ris H.14. The conjugate of wherein Z is H.15. The conjugate of wherein B is adenine.18. The conjugate of wherein Yis O.19. The conjugate of wherein Yis N(CH).21. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a conjugate as described in ...

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12-01-2017 дата публикации

PYRROLO[1,2-f][1,2,4]TRIAZINES USEFUL FOR TREATING RESPIRATORY SYNCITIAL VIRUS INFECTIONS

Номер: US20170008897A1
Принадлежит:

Provided herein are formulations, methods and substituted tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds. 13-. (canceled)514-. (canceled)16. A compound according to claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Rand Rare each C-Calkyl.17. A compound according to claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Rand Rare each selected from C-Calkyl.18. A compound according to claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Rand Rare each selected from C-Calkyl.1920-. (canceled)2225-. (canceled)26. A method of treating Pneumovirinae virus infection in a human claim 4 , the method comprising administering to the human a therapeutically effective amount of a compound of claim 4 , or a pharmaceutically acceptable salt thereof.27. The method of wherein the Pneumovirinae virus infection in a human is a human respiratory syncytial virus infection.28. A pharmaceutical formulation comprising a pharmaceutically effective amount of a compound of claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , and a pharmaceutically acceptable carrier or excipient.2930-. (canceled) This application claims the benefit of and priority to U.S. Provisional Application Ser. No. 61/902,544, filed Nov. 11, 2013, the disclosure of which is hereby incorporated by reference in its entirety.Provided herein are substituted tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds, methods and pharmaceutical formulations for treating Pneumovirinae virus infections, particularly including respiratory syncytial virus infections, as well as methods and intermediates useful for preparing the compounds.Pneumovirinae viruses are negative-sense, single-stranded, ...

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18-01-2018 дата публикации

PYRROLO[1,2-f][1,2,4]TRIAZINES USEFUL FOR TREATING RESPIRATORY SYNCITIAL VIRUS INFECTIONS

Номер: US20180016280A1
Принадлежит:

Provided herein are formulations, methods and substituted tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds. 23-. (canceled)5. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris CN claim 1 , —CHCl claim 1 , —CHF claim 1 , —CHF claim 1 , or —CF.6. A compound according to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris CN claim 5 , —CHCl claim 5 , or —CHF.78-. (canceled)9. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris CN.10. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris C-Chaloalkyl.11. (canceled)12. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris CN or halomethyl.13. (canceled)14. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H.18. A compound according to claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Ris C-Calkyl.19. (canceled)2124-. (canceled)26. A method of treating Pneumovirinae virus infection in a human in need thereof claim 1 , the method comprising administering to the human a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.27. The method of wherein the Pneumovirinae virus infection in the human is a human respiratory syncytial virus infection.28. A pharmaceutical formulation comprising a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier or excipient.2930-. (canceled)31. A method of treating Pneumovirinae virus infection in a ...

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16-01-2020 дата публикации

TOLL LIKE RECEPTOR MODULATOR COMPOUNDS

Номер: US20200017451A1
Принадлежит:

This application relates generally to toll like receptor modulator compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR8), and methods of making and using them. 2. (canceled)3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —H or Calkyl.4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris methyl.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Calkyl.610.-. (canceled)11. The compound of claim 1 , wherein Rand Rare taken together to form tetrahydropyridinyl optionally substituted with —C(O)Rwherein Ris Calkyl optionally substituted with —CN or —NH; Chaloalkyl; tetrahydropyranyl; thienyl optionally substituted with 1 to 3 Calkyl; thiazolyl; imidazolyl optionally substituted with 1 to 3 Calkyl; oxazolyl; isoxazolyl optionally substituted with 1 to 3 Calkyl; thiadiazolyl; pyrazinyl; or quinolinyl.12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': '1', 'sub': '1-4', 'Ris —H or Calkyl;'}{'sup': '2', 'sub': '3-6', 'Ris Calkyl; and'}{'sup': 3', '4, 'Rand Rare taken together to form 5 to 6 membered heterocyclyl having 1 to 3 heteroatoms selected from oxygen, nitrogen, and sulfur, wherein{'sub': '1-4', 'the 5 to 6 membered heterocyclyl is optionally substituted with 1 to 3 —C(O)Calkyl.'}15. (canceled)16. The compound of claim 12 , or a pharmaceutically acceptable salt thereof claim 12 , wherein Rand Rare taken together to form tetrahydropyridinyl optionally substituted with 1 to 3 C(O)Calkyl.17. (canceled)18. (canceled)21. A pharmaceutical composition comprises a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable excipient.22. The pharmaceutical composition of claim 21 , further comprising one or more additional therapeutic agents.2326.-. (canceled)27. A method of treating or ...

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21-01-2021 дата публикации

PROCESSES FOR PREPARING TOLL-LIKE RECEPTOR MODULATOR COMPOUNDS

Номер: US20210017170A1
Принадлежит:

The present disclosure provides methods for preparing (R)-2-((2-amino-7-fluoropyrido[3,2-d]pyrimidin-4-yl)amino)-2-methylhexan-1-ol or a salt thereof and related key intermediates. 3. The method of claim 1 , wherein the salt of the compound having the Formula PG-NHC(═NH)NHis a hemisulfate claim 1 , a sulfate claim 1 , a chloride claim 1 , a bromide claim 1 , a carbonate claim 1 , a nitrate claim 1 , or an acetate salt.4. The method of claim 1 , wherein PG is 2 claim 1 ,4-dimethoxybenzyl.5. The method of claim 2 , wherein the first transition-metal catalyst comprises a copper metal claim 2 , a copper oxide claim 2 , a copper (I) salt claim 2 , a copper (II) salt claim 2 , or combinations thereof.6. The method of claim 2 , wherein the first transition-metal catalyst is Cu(I) iodide claim 2 , Cu(I) bromide claim 2 , Cu(I) chloride claim 2 , Cu(I) acetate claim 2 , Cu(I) carbonate claim 2 , Cu(I) nitrate claim 2 , Cu(I) sulfate claim 2 , Cu(I) phosphate claim 2 , Cu(I) 3-methylsalicylate claim 2 , Cu(I) thiophene-2-carboxylate claim 2 , Cu(I) oxide claim 2 , Cu(II) iodide claim 2 , Cu(II) bromide claim 2 , Cu(II) chloride claim 2 , Cu(II) acetate claim 2 , Cu(II) carbonate claim 2 , Cu(II) nitrate claim 2 , Cu(II) sulfate claim 2 , Cu(II) pyrophosphate claim 2 , Cu(II) phosphate claim 2 , Cu(II) tartrate claim 2 , Cu(II) oxide claim 2 , or combinations thereof.7. The method of claim 2 , wherein the first transition-metal catalyst comprises Cu(II) acetate.8. The method of claim 1 , wherein the first base is lithium carbonate claim 1 , sodium carbonate claim 1 , potassium carbonate claim 1 , cesium carbonate claim 1 , lithium bicarbonate claim 1 , sodium bicarbonate claim 1 , potassium bicarbonate claim 1 , sodium phosphate tribasic claim 1 , potassium phosphate tribasic claim 1 , potassium acetate claim 1 , potassium trimethylacetate claim 1 , tetrabutylphosphonium malonate claim 1 , 1 claim 1 ,8-diazabicyclo[5.4.0]undec-7-ene claim 1 , 1 claim 1 ,5-diazabicyclo[4.3.0] ...

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28-01-2016 дата публикации

THIENO[3,2-d]PYRIMIDINE, FURO[3,2-d]PYRIMIDINE, AND PYRROLO[3,2-D]PYRIMIDINES USEFUL FOR TREATING RESPIRATORY SYNCITIAL VIRUS INFECTIONS

Номер: US20160024107A1
Принадлежит:

Provided herein are formulations, methods and substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds. 2. A compound of wherein X is S claim 1 , or a pharmaceutically acceptable salt thereof.3. A compound of claim 1 , wherein Ris selected from the group of CN claim 1 , OR claim 1 , C-Calkyl claim 1 , C-Calkenyl claim 1 , C-Calkynyl claim 1 , —CH—O—C-Calkyl claim 1 , —CH—S—C-Calkyl claim 1 , C-Ccycloalkyl claim 1 , azido claim 1 , halogen claim 1 , C-Cchloroalkyl claim 1 , C-Cbromoalkyl claim 1 , and C-Cfluoroalkyl; or a pharmaceutically acceptable salt thereof.4. A compound of claim 1 , wherein Ris selected from the group of H claim 1 , CH claim 1 , F claim 1 , Cl claim 1 , and NH; Ris selected from the group of OH claim 1 , F claim 1 , Cl claim 1 , N claim 1 , NH claim 1 , and CN; and Ris selected from the group of CN claim 1 , N claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , vinyl claim 1 , propenyl claim 1 , ethynyl claim 1 , CHF claim 1 , CHF claim 1 , CHCl claim 1 , CHSMe claim 1 , and CHOMe; or a pharmaceutically acceptable salt thereof.8. A compound of wherein X is S claim 7 , or a pharmaceutically acceptable salt thereof.10. A compound of claim 9 , or a pharmaceutically acceptable salt thereof claim 9 , wherein Ris H.11. A compound of claim 9 , or a pharmaceutically acceptable salt thereof claim 9 , wherein Ris F12. A compound of claim 9 , or a pharmaceutically acceptable salt thereof claim 9 , wherein Ris F.13. A compound of claim 9 , or a pharmaceutically acceptable salt thereof claim 9 , wherein Ris Cl.14. A compound of claim 9 , or a pharmaceutically acceptable salt thereof claim 9 , wherein Ris N.15. A compound of claim 9 , or a ...

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02-02-2017 дата публикации

ANTIVIRAL COMPOUNDS

Номер: US20170029408A1
Принадлежит:

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. 15. The compound of wherein each Xis absent.20. A pharmaceutical composition comprising the compound as described in or a pharmaceutically acceptable salt claim 1 , or prodrug thereof; and at least one pharmaceutically acceptable carrier.21. The pharmaceutical composition according to for use in treating disorders associated with HCV.22. The pharmaceutical composition of claim 20 , further comprising at least one additional therapeutic agent.23. The pharmaceutical composition of claim 22 , wherein said additional therapeutic agent is selected from the group consisting of interferons claim 22 , ribavirin analogs claim 22 , NS3 protease inhibitors claim 22 , NS5b polymerase inhibitors claim 22 , alpha-glucosidase 1 inhibitors claim 22 , hepatoprotectants claim 22 , non-nucleoside inhibitors of HCV claim 22 , and other drugs for treating HCV.24. The pharmaceutical composition according to claim 20 , further comprising a nucleoside analogue.25. The pharmaceutical composition according to claim 24 , further comprising an interferon or pegylated interferon.26. The pharmaceutical composition according to claim 25 , wherein said nucleoside analogue is selected from ribavirin claim 25 , viramidine claim 25 , levovirin claim 25 , a L-nucleoside claim 25 , and isatoribine and said interferon is α-interferon or pegylated interferon.27. A method of treating disorders associated with hepatitis C claim 1 , said method comprising administering to an individual a pharmaceutical composition which comprises a therapeutically effective amount of the compound as described in or a pharmaceutically acceptable salt claim 1 , or prodrug thereof. This application claims priority to U.S. Provisional Application No. 61/177,972, filed 13 May 2009; 61/224, ...

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25-02-2021 дата публикации

METHODS FOR TREATING FILOVIRIDAE VIRUS INFECTIONS

Номер: US20210052613A1
Принадлежит:

Provided are compounds, methods, and pharmaceutical compositions for treating Filoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula IV: 124-. (canceled)27. The pharmaceutical composition of claim 26 , comprising at least one other therapeutic agent.28. The pharmaceutical composition of claim 27 , wherein the at least one other therapeutic agent is selected from the group consisting of parenteral fluids claim 27 , antibiotics claim 27 , antifungals claim 27 , fever and pain medication claim 27 , antiemetics claim 27 , antidiarrheal agents claim 27 , vitamin and mineral supplements claim 27 , anti-inflammatory agents claim 27 , and anti-malarial agents; or mixtures thereof.29. The pharmaceutical composition of claim 27 , wherein the at least one other therapeutic agent is selected from the group consisting of ribavirin claim 27 , palivizumab claim 27 , motavizumab claim 27 , RSV-IGIV claim 27 , MEDI-557 claim 27 , A-60444 claim 27 , MDT-637 claim 27 , BMS-433771 claim 27 , amiodarone claim 27 , dronedarone claim 27 , verapamil claim 27 , Ebola Convalescent Plasma (ECP) claim 27 , TKM-100201 claim 27 , (2S claim 27 ,3S claim 27 ,4R claim 27 ,5R)-2-(4-amino-5H-pyrrolo[3 claim 27 ,2-d]pyrimidin-7-yl)-5-(hydroxymethyl)pyrrolidine-3 claim 27 ,4-diol claim 27 , favipiravir claim 27 , T-705 monophosphate claim 27 , T-705 diphosphate claim 27 , T-705 triphosphate claim 27 , 1-N claim 27 ,7-N-bis[3-(dimethylamino)propyl]-3 claim 27 ,9-dimethylquinolino[8 claim 27 ,7-h]quinolone-1 claim 27 ,7-diamine claim 27 , JK-05 claim 27 , TKM-Ebola claim 27 , ZMapp claim 27 , rNAPc2 claim 27 , VRC-EBOADC076-00-VP claim 27 , OS-2966 claim 27 , MVA-BN filo claim 27 , brincidofovir claim 27 , Vaxart adenovirus vector 5-based ebola vaccine claim 27 , Ad26-ZEBOV claim 27 , FiloVax vaccine claim 27 , GOVX-E301 claim 27 , GOVX-E302 claim 27 , ebola virus entry inhibitors (NPC1 inhibitors) claim 27 , and rVSV-EBOV; or mixtures thereof.31. ...

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25-02-2016 дата публикации

2'-CHLORO AMINOPYRIMIDINONE AND PYRIMIDINE DIONE NUCLEOSIDES

Номер: US20160052953A1
Принадлежит:

Provided herein are formulations, methods and substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds. 4. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein R is hydrogen.5. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein wherein Ris selected from the group of CN claim 1 , unsubstituted C-Calkyl claim 1 , C-Calkyl substituted with 1 claim 1 , 2 claim 1 , or 3 halogens selected from F and Cl claim 1 , C-Calkyl substituted with 1 substituent selected from —S—CHand —O—CH claim 1 , C-Calkenyl claim 1 , C-Calkynyl claim 1 , unsubstituted C-Ccycloalkyl claim 1 , C-Ccycloalkyl substituted by 1 claim 1 , 2 claim 1 , or 3 substituents selected from F and CH;6. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen.7. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris F.8. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare both hydrogen.9. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein R claim 1 , R claim 1 , and R are each hydrogen.10. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris F and Rand R are each hydrogen.11. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group of H and F; Ris selected from the group of CN claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , vinyl claim 1 , propenyl claim 1 , ethynyl claim 1 , CHF claim 1 , CHF claim 1 , CHCl claim 1 , CHSMe claim 1 , —CHOMe claim 1 , ...

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10-03-2022 дата публикации

TOLL LIKE RECEPTOR MODULATOR COMPOUNDS

Номер: US20220073473A1
Принадлежит:

This application relates generally to toll like receptor modulator compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR8), and methods of making and using them. 2. (canceled)3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —H or Calkyl.4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris methyl.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Calkyl.6. (canceled)7. (canceled)8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare taken together to form a 6-membered cycloalkyl.9. (canceled)10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare taken together to form pyrazinyl claim 1 ,{'sub': '1-2', '#text': 'pyridinyl or thienyl optionally substituted with 1 to 3 Calkyl.'}11. (canceled)12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': '1', 'sub': '1-4', '#text': 'Ris —H or Calkyl;'}{'sup': '2', 'sub': '3-6', '#text': 'Ris Calkyl; and'}{'sup': ['3', '4'], 'sub': '5-6', 'claim-text': [{'sup': '6', '#text': '5 to 6 membered heteroaryl is optionally substituted with 1 to 3 R; and'}, {'sup': '6', 'sub': ['1-4', '1-4'], '#text': 'each Ris independently halogen, —OH, Calkyl, or Calkoxy.'}], '#text': 'Rand Rare taken together to form Ccycloalkyl, or 5 to 6 membered heteroaryl having 1 to 3 heteroatoms selected from oxygen, nitrogen, and sulfur, wherein:'}16. (canceled)17. (canceled)18. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare taken together to form pyrazinyl claim 1 , thienyl or pyridinyl.21. A pharmaceutical composition comprises a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable excipient.22. The pharmaceutical ...

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21-02-2019 дата публикации

METHODS AND COMPOUNDS FOR TREATING PARAMYXOVIRIDAE VIRUS INFECTIONS

Номер: US20190055251A1
Принадлежит:

Provided are methods for treating Paramyxoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula I: 1. (canceled)314.-. (canceled)15. The method of further comprising administering a therapeutically effective amount of at least one other therapeutic agent or composition thereof selected from the group consisting of a corticosteroid claim 2 , an anti-inflammatory signal transduction modulator claim 2 , a β2-adrenoreceptor agonist bronchodilator claim 2 , an anticholinergic claim 2 , a mucolytic agent claim 2 , hypertonic saline and other drugs for treating Paramyxoviridae virus infections; or mixtures thereof.16. The method of wherein the at least one other therapeutic agent is ribavirin claim 15 , palivizumab claim 15 , motavizumab claim 15 , RSV-IGIV (RespiGam®) claim 15 , MEDI-557 claim 15 , A-60444 claim 15 , MDT-637 or BMS-433771 or mixtures thereof.1720.-. (canceled)21. The method of wherein the Paramyxoviridae infection is caused by a type 1 or 3 Human parainfluenza virus.22. The method of wherein the Paramyxoviridae infection is caused by a Pneumovirinae virus.23. The method of wherein the Paramyxoviridae infection is caused by a Human respiratory syncytial virus.2430.-. (canceled)32. The pharmaceutical composition of further comprising administering a therapeutically effective amount of at least one other therapeutic agent or composition thereof selected from the group consisting of a corticosteroid claim 31 , an anti-inflammatory signal transduction modulator claim 31 , a β2-adrenoreceptor agonist bronchodilator claim 31 , an anticholinergic claim 31 , a mucolytic agent claim 31 , hypertonic saline and other drugs for treating Paramyxoviridae virus infections; or mixtures thereof.33. The pharmaceutical composition of wherein the at least one other therapeutic agent is ribavirin claim 32 , palivizumab claim 32 , motavizumab claim 32 , RSV-IGIV (RespiGam®) claim 32 , MEDI-557 claim 32 , A-60444 claim 32 , MDT ...

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21-02-2019 дата публикации

PYRROLO[1,2-f][1,2,4]TRIAZINES USEFUL FOR TREATING RESPIRATORY SYNCITIAL VIRUS INFECTIONS

Номер: US20190055253A1
Принадлежит:

Provided herein are formulations, methods and substituted tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds. 130-. (canceled)35. A pharmaceutical composition comprising the compound or the pharmaceutically acceptable salt of .36. A pharmaceutical composition comprising the compound or the pharmaceutically acceptable salt of .37. A pharmaceutical composition comprising the compound of .38. A pharmaceutical composition comprising the compound of .39. A method of treating a Pneumovirinae virus infection in a human claim 31 , the method comprising administering to the human a therapeutically effective amount of the compound or the pharmaceutically acceptable salt of .40. The method of claim 39 , wherein the Pneumovirinae virus infection in the human is a human respiratory syncytial virus infection.41. A method of treating a Pneumovirinae virus infection in a human claim 32 , the method comprising administering to the human a therapeutically effective amount of the compound or the pharmaceutically acceptable salt of .42. The method of claim 41 , wherein the Pneumovirinae virus infection in the human is a human respiratory syncytial virus infection.43. A method of treating a Pneumovirinae virus infection in a human claim 33 , the method comprising administering to the human a therapeutically effective amount of the compound of .44. The method of claim 43 , wherein the Pneumovirinae virus infection in the human is a human respiratory syncytial virus infection.45. A method of treating a Pneumovirinae virus infection in a human claim 34 , the method comprising administering to the human a therapeutically effective amount of the compound of .46. The method of claim 45 , wherein the Pneumovirinae virus infection in the human is a human ...

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04-03-2021 дата публикации

METHODS AND COMPOUNDS FOR TREATING PARAMYXOVIRIDAE VIRUS INFECTIONS

Номер: US20210061806A1
Принадлежит:

Provided are methods for treating Paramyxoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula I: 125.-. (canceled)27. The method of wherein each R claim 26 , R claim 26 , and Ris H and Ris OR.28. The method of wherein Ris CN claim 26 , methyl claim 26 , ethenyl claim 26 , or ethynyl.29. The method of wherein Ris NHand Ris H.31. The method of claim 26 , further comprising administering a pharmaceutically acceptable carrier.32. The method of further comprising administering a therapeutically effective amount of at least one other therapeutic agent selected from the group consisting of a corticosteroid claim 31 , an anti-inflammatory signal transduction modulator claim 31 , β2-adrenoreceptor agonist bronchodilator claim 31 , an anticholinergic claim 31 , a mucolytic agent claim 31 , hypertonic saline and other drugs for treating Paramyxoviridae virus infections; or mixtures thereof.33. The method of wherein the at least one other therapeutic agent is ribavirin claim 32 , palivizumab claim 32 , motavizumab claim 32 , RSV-IGIV (RespiGam®) claim 32 , MEDI-557 claim 32 , A-60444 claim 32 , MDT-637 or BMS-433771 or mixtures thereof.34. The method of claim 26 , wherein the Paramyxoviridae infection is a Paramyxovirina infection.35. The method of claim 34 , wherein the Paramyxovirina infection is a human parainfluenza virus infection.36. The method of claim 26 , wherein the Paramyxoviridae infection is a Pneumovirinae infection.37. The method of claim 36 , wherein the Pneumovirinae infection is a human respiratory syncytial virus infection. This Application is a Continuation of U.S. patent application Ser. No. 16/042,085, filed on Jul. 23, 2018, which is a Divisional of U.S. patent application Ser. No. 14/613,719, filed on Feb. 4, 2015, now U.S. Pat. No. 10,065,958, issued on Sep. 4, 2018, which is a Continuation of U.S. patent application Ser. No. 13/189,373, filed on Jul. 22, 2011, abandoned, which claims the benefit of ...

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17-03-2022 дата публикации

COMPOUNDS AND METHODS FOR TREATMENT OF VIRAL INFECTIONS

Номер: US20220081462A1
Принадлежит:

Compounds and methods of using said compounds, singly or in combination with additional agents, and salts, crystalline forms, pharmaceutical compositions of said compounds for the treatment of viral infections are disclosed. 139-. (canceled)41. (canceled)42. (canceled)43. The crystalline form of claim 40 , wherein the XRPD pattern further comprises one of the degree 2θ-reflections (+/−0.2 degrees 2θ) at 15.4° claim 40 , 16.9° claim 40 , and 28.1°.44. The crystalline form of claim 40 , wherein the XRPD pattern comprises degree 2θ-reflections (+/−0.2 degrees 2θ) at 8.5° claim 40 , 15.4° claim 40 , 16.9° claim 40 , 22.1° claim 40 , 23.8° and 28.1°45. (canceled)46. (canceled)47. The crystalline form of claim 40 , wherein the XRPD pattern comprises degree 2θ-reflections (+/−0.2 degrees 2θ) at 8.5° claim 40 , 10.5° claim 40 , 15.4° claim 40 , 16.9° claim 40 , 17.5° claim 40 , 22.1° claim 40 , 23.8° claim 40 , 27.5° claim 40 , and 28.1°.48. The crystalline form of claim 40 , wherein the XRPD pattern is substantially as shown in .49. The crystalline form of claim 40 , wherein the crystalline form is characterized by a differential scanning calorimetry (DSC) pattern substantially as set forth in .50. The crystalline form of claim 40 , wherein the crystalline form is characterized by a thermogravimetric analysis (TGA) pattern substantially as set forth in .52. (canceled)53. (canceled)54. The crystalline form of claim 51 , wherein the XRPD pattern further comprises one of the degree 2θ-reflections (+/−0.2 degrees 2θ) at 18.4° claim 51 , 20.8° claim 51 , and 23.3°.55. The crystalline form of claim 51 , wherein the XRPD pattern comprises degree 2θ-reflections (+/−0.2 degrees 2θ) at 6.4° claim 51 , 13.7° claim 51 , 16.3° claim 51 , 18.4° claim 51 , 20.8° claim 51 , and 23.3°.56. The crystalline form of claim 55 , wherein the XRPD pattern further comprises a degree 2θ-reflection at 25.4°.57. The crystalline form of claim 51 , wherein the XRPD pattern is substantially as shown in . ...

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08-03-2018 дата публикации

TOLL LIKE RECEPTOR MODULATOR COMPOUNDS

Номер: US20180065938A1
Принадлежит:

This application relates generally to toll like receptor modulator compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR8), and methods of making and using them. 2. The compound of wherein Q is CH or CR.3. The compound of wherein Ris —H or Calkyl.4. The compound of claim 1 , wherein Ris methyl.5. The compound of claim 1 , wherein Ris Calkyl.6. The compound of claim 1 , wherein Ris Calkoxy optionally substituted with 1 R.7. The compound of claim 1 , wherein each Ris independently OR claim 1 , morpholino claim 1 , phenyl claim 1 , pyridinyl claim 1 , pyrazolyl claim 1 , or pyridazinyl claim 1 , wherein each morpholino claim 1 , phenyl claim 1 , pyridinyl claim 1 , pyrazolyl claim 1 , and pyridazinyl are independently optionally substituted with —OCH claim 1 , Calkyl claim 1 , chloro claim 1 , or fluoro; wherein Ris —CH claim 1 , —CHCF claim 1 , or quinolinyl optionally substituted with —OCH claim 1 , Calkyl claim 1 , chloro claim 1 , or fluoro.8. The compound of claim 1 , wherein Rand Rare taken together to form a 6-membered cycloalkyl.9. The compound of claim 1 , wherein Rand Rare taken together to form phenyl optionally substituted with 1 to 3 chloro claim 1 , fluoro claim 1 , bromo claim 1 , —CN claim 1 , Calkyl optionally substituted with —OH claim 1 , Calkoxy claim 1 , —C(O)Calkyl claim 1 , —C(O)OCalkyl claim 1 , pyrazolyl optionally substituted with 1 to 3 Calkyl; or imidazolyl optionally substituted with 1 to 3 Calkyl.10. The compound of claim 1 , wherein Rand Rare taken together to form pyrazinyl claim 1 , pyridinyl or thienyl optionally substituted with 1 to 3 Calkyl.11. The compound of claim 1 , wherein Rand Rare taken together to form tetrahydropyridinyl optionally substituted with —C(O)Rwherein Ris Calkyl optionally substituted with —CN or —NH claim 1 , Chaloalkyl claim 1 , cyclopropyl claim 1 , cyclobutyl claim 1 , tetrahydropyranyl claim 1 , thienyl optionally substituted with 1 to 3 Calkyl; thiazolyl ...

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16-03-2017 дата публикации

Methods for treating arenaviridae and coronaviridae virus infections

Номер: US20170071964A1
Принадлежит: Gilead Sciences Inc

Provided are methods for treating Arenaviridae and Coronaviridae virus infections by administering nucleosides and prodrugs thereof, of Formula I: wherein the 1′ position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are particularly useful for the treatment of Lassa virus and Junin virus infections.

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15-03-2018 дата публикации

THIENO[3,2-d]PYRIMIDINE, FURO[3,2-d]PYRIMIDINE, AND PYRROLO[3,2-D]PYRIMIDINES USEFUL FOR TREATING RESPIRATORY SYNCITIAL VIRUS INFECTIONS

Номер: US20180072755A1
Принадлежит:

Provided herein are formulations, methods and substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds. 15-. (canceled)717-. (canceled)21. A compound of claim 6 , or a pharmaceutically acceptable salt thereof claim 6 , wherein Ris F or OH.2328-. (canceled)31. A pharmaceutical composition comprising a compound of claim 6 , or a pharmaceutically acceptable salt thereof claim 6 , and a pharmaceutically acceptable carrier or excipient.32. A pharmaceutical composition comprising a compound of claim 22 , or a pharmaceutically acceptable salt thereof claim 22 , and a pharmaceutically acceptable carrier or excipient.33. A pharmaceutical composition comprising a compound of claim 29 , or a pharmaceutically acceptable salt thereof claim 29 , and a pharmaceutically acceptable carrier or excipient.34. A pharmaceutical composition comprising a compound of claim 30 , or a pharmaceutically acceptable salt thereof claim 30 , and a pharmaceutically acceptable carrier or excipient.35. A method of treating Pneumovirinae virus infection in a human in need thereof claim 6 , the method comprising administering to the human in need thereof a therapeutically effective amount of a compound of claim 6 , or a pharmaceutically acceptable salt thereof.36. The method of claim 35 , wherein the Pneumovirinae virus infection is a respiratory syncytial virus infection.37. A method of treating Pneumovirinae virus infection in a human in need thereof claim 22 , the method comprising administering to the human in need thereof a therapeutically effective amount of a compound of claim 22 , or a pharmaceutically acceptable salt thereof.38. The method of claim 37 , wherein the Pneumovirinae virus infection ...

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29-03-2018 дата публикации

TOLL LIKE RECEPTOR MODULATOR COMPOUNDS

Номер: US20180086755A1
Принадлежит:

This application relates generally to toll like receptor modulator compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR8), and methods of making and using them. 10. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable excipient.11. The pharmaceutical composition of claim 10 , further comprising one or more additional therapeutic agents.12. The pharmaceutical composition of claim 11 , wherein one or more additional agents are selected from the group consisting of HBV DNA polymerase inhibitors claim 11 , toll-like receptor 7 modulators claim 11 , toll-like receptor 8 modulators claim 11 , toll-like receptor 7 and 8 modulators claim 11 , toll-like receptor 3 modulators claim 11 , interferon alpha ligands claim 11 , HBsAg inhibitors claim 11 , compounds targeting HbcAg claim 11 , cyclophilin inhibitors claim 11 , HBV therapeutic vaccines claim 11 , HBV prophylactic vaccines claim 11 , HBV viral entry inhibitors claim 11 , NTCP inhibitors claim 11 , antisense oligonucleotide targeting viral mRNA claim 11 , short interfering RNAs (siRNA) claim 11 , hepatitis B virus E antigen inhibitors claim 11 , HBx inhibitors claim 11 , cccDNA inhibitors claim 11 , HBV antibodies including HBV antibodies targeting the surface antigens of the hepatitis B virus claim 11 , thymosin agonists claim 11 , cytokines claim 11 , nucleoprotein inhibitors (HBV core or capsid protein inhibitors) claim 11 , stimulators of retinoic acid-inducible gene 1 claim 11 , stimulators of NOD2 claim 11 , recombinant thymosin alpha-1 and hepatitis B virus replication inhibitors claim 11 , hepatitis B surface antigen (HBsAg) secretion or assembly inhibitors claim 11 , IDO inhibitors claim 11 , and combinations thereof.13. The pharmaceutical composition of claim 11 , wherein one or more additional therapeutic agents are selected from the group consisting of ...

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29-03-2018 дата публикации

Phosphonate analogs of HIV inhibitor compounds

Номер: US20180086784A1
Принадлежит:

The invention is related to phosphorus substituted anti-viral inhibitory 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. 1104.-. (canceled) This non-provisional application claims the benefit of Provisional Application No. 60/591,811, filed Jul. 27, 2004, and all of which are incorporated herein by reference.The invention relates generally to compounds with antiviral activity and more specifically with anti-HIV properties.AIDS is a major public health problem worldwide. Although drugs targeting HIV viruses are in wide use and have shown effectiveness, toxicity and development of resistant strains have limited their usefulness. Assay methods capable of determining the presence, absence or amounts of HIV viruses are of practical utility in the search for inhibitors as well as for diagnosing the presence of HIV.Human immunodeficiency virus (HIV) infection and related disease is a major public health problem worldwide. The retrovirus human immunodeficiency virus type 1 (HIV-1), a member of the primate lentivirus family (DeClercq E (1994) 724:438-456; Barre-Sinoussi F (1996) 348:31-35), is generally accepted to be the causative agent of acquired immunodeficiency syndrome (AIDS) Tarrago et al. 1994, 8:497-503). AIDS is the result of repeated replication of HIV-1 and a decrease in immune capacity, most prominently a fall in the number of CD4+ lymphocytes. The mature virus has a single stranded RNA genome that encodes 15 proteins (Frankel et al. (1998) 67:1-25; Katz et al. (1994) 63:133-173), including three key enzymes: (i) protease (Prt) (von der Helm K (1996) 377:765-774); (ii) reverse transcriptase (RT) (Hottiger et al. (1996) -377:97-120), an enzyme unique to retroviruses; and (iii) integrase (Asante et al. (1999) 52:351-369; Wlodawer A (1999) 52:335-350; Esposito et al. (1999) 52:319-333). Protease is responsible ...

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30-03-2017 дата публикации

ANTIVIRAL COMPOUNDS

Номер: US20170088576A1
Принадлежит:

The invention is related to phosphorus substituted anti-viral inhibitory 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. 1103-. (canceled)105. The compound of claim 104 , wherein Ris H claim 104 , methyl claim 104 , or ethyl.106. The compound of claim 104 , wherein Ris methyl or ethyl.107. The compound of claim 104 , wherein Ris methyl.108. The compound of claim 104 , wherein Ris ethyl claim 104 , n-propyl claim 104 , isopropyl claim 104 , n-butyl claim 104 , isobutyl claim 104 , or n-pentyl.109. The compound of claim 104 , wherein Ris ethyl claim 104 , n-propyl claim 104 , n-butyl claim 104 , or n-pentyl.110. The compound of claim 104 , wherein Ris ethyl.113. A pharmaceutical composition comprising a compound of claim 104 , or a pharmaceutically acceptable salt thereof claim 104 , and one or more pharmaceutically acceptable excipients or carriers. This application claims priority to U.S. Application No. 60/591,811, filed Jul. 27, 2004, the disclosures of which are incorporated by reference in their entirety. In particular, the figures described on pages 161 to 184 are incorporated as Figures herein.The invention relates generally to compounds with HIV inhibitory activity.Improving the delivery of drugs and other agents to target cells and tissues has been the focus of considerable research for many years. Though many attempts have been made to develop effective methods for importing biologically active molecules into cells, both in vivo and in vitro, none has proved to be entirely satisfactory. Optimizing the association of the inhibitory drug with its intracellular target, while minimizing intercellular redistribution of the drug, e.g., to neighboring cells, is often difficult or inefficient.Most agents currently administered to a patient parenterally are not targeted, resulting in systemic delivery of the ...

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19-03-2020 дата публикации

2'-CHLORO AMINOPYRIMIDINONE AND PYRIMIDINE DIONE NUCLEOSIDES

Номер: US20200087337A1
Принадлежит:

Provided herein are formulations, methods and substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds. 4. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein R is hydrogen.5. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein wherein Ris selected from the group of CN claim 1 , unsubstituted C-Calkyl claim 1 , C-Calkyl substituted with 1 claim 1 , 2 claim 1 , or 3 halogens selected from F and Cl claim 1 , C-Calkyl substituted with 1 substituent selected from —S—CHand —O—CH claim 1 , C-Calkenyl claim 1 , C-Calkynyl claim 1 , unsubstituted C-Ccycloalkyl claim 1 , C-Ccycloalkyl substituted by 1 claim 1 , 2 claim 1 , or 3 substituents selected from F and CH;6. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen.7. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris F.8. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare both hydrogen.9. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein R claim 1 , R claim 1 , and R are each hydrogen.10. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris F and Rand R are each hydrogen.11. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group of H and F; Ris selected from the group of CN claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , vinyl claim 1 , propenyl claim 1 , ethynyl claim 1 , CHF claim 1 , CHF claim 1 , CHCl claim 1 , CHSMe claim 1 , —CHOMe claim 1 , ...

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05-05-2016 дата публикации

METHODS FOR TREATING FILOVIRIDAE VIRUS INFECTIONS

Номер: US20160122374A1
Принадлежит:

Provided are compounds, methods, and pharmaceutical compositions for treating Filoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula IV: 2. The method of wherein Ris H.8. The method of further comprising a pharmaceutically acceptable carrier or excipient.9. The method of further comprising administering a therapeutically effective amount of at least one other therapeutic agent or composition thereof selected from the group consisting of a corticosteroid claim 1 , an anti-inflammatory signal transduction modulator claim 1 , a β2-adrenoreceptor agonist bronchodilator claim 1 , an anticholinergic claim 1 , a mucolytic agent claim 1 , hypertonic saline and other drugs for treating Filoviridae virus infections; or mixtures thereof.10. The method of wherein the at least one other therapeutic agent is ribavirin claim 9 , palivizumab claim 9 , motavizumab claim 9 , RSV-IGIV (RespiGam®) claim 9 , MEDI-557 claim 9 , A-60444 claim 9 , MDT-637 claim 9 , BMS-433771 claim 9 , amiodarone claim 9 , dronedarone claim 9 , verapamil claim 9 , Ebola Convalescent Plasma (ECP) claim 9 , TKM-100201 claim 9 , BCX4430 ((2S claim 9 ,3S claim 9 ,4R claim 9 ,5R)-2-(4-amino-5H-pyrrolo[3 claim 9 ,2-d]pyrimidin-7-yl)-5-(hydroxymethyl)pyrrolidine-3 claim 9 ,4-diol) claim 9 , favipiravir (also known as T-705 or Avigan) claim 9 ,T-705 monophosphate claim 9 , T-705 diphosphate claim 9 , T-705 triphosphate claim 9 , FGI-106 (1-N claim 9 ,7-N-bis[3-(dimethylamino)propyl]-3 claim 9 ,9-dimethylquinolino[8 claim 9 ,7-h]quinolone-1 claim 9 ,7-diamine) claim 9 , JK-05 claim 9 , TKM-Ebola claim 9 , ZMapp claim 9 , rNAPc2 claim 9 , VRC-EBOADC076-00-VP claim 9 , OS-2966 claim 9 , MVA-BN filo claim 9 , brincidofovir claim 9 , Vaxart adenovirus vector 5-based ebola vaccine claim 9 , Ad26-ZEBOV claim 9 , FiloVax vaccine claim 9 , GOVX-E301 claim 9 , GOVX-E302 claim 9 , ebola virus entry inhibitors (NPC1 inhibitors) claim 9 , or rVSV-EBOV or mixtures thereof. ...

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12-05-2016 дата публикации

PYRAZOLO[1,5-A]PYRIMIDINES FOR ANTIVIRAL TREATMENT

Номер: US20160130275A1
Принадлежит:

The invention provides compounds of Formula I or Formula II: 2. The compound of which is a compound of Formula I.3. The compound of wherein each Ris H.5. The compound of which is a compound of Formula VII.6. The compound of wherein Ris H.7. The compound of wherein Ris H claim 1 , halogen or (C-C)alkyl.8. The compound of wherein n is 3 or 4.9. The compound of wherein each Ris independently H or optionally substituted (C-C)alkyl claim 1 , or four Ron adjacent carbon atoms claim 1 , when taken together claim 1 , may form an optionally substituted Caryl ring.11. The compound of wherein A is —(CH)—.12. The compound of wherein X is —CR(NRC(O)OR)— claim 1 , —CR(NRR)— claim 1 , —CR(NRS(O)R)— or X is absent.13. The compound of wherein X is absent.14. The compound of wherein Ris H claim 1 , OR claim 1 , NRR claim 1 , CN claim 1 , (C-C)alkyl claim 1 , C-Caryl claim 1 , C-Cheterocyclyl or (C-C)cycloalkyl claim 1 , wherein any (C-C)alkyl claim 1 , C-Caryl claim 1 , C-Cheterocyclyl or (C-C)cycloalkyl of Ris optionally substituted with one or more oxo claim 1 , halogen claim 1 , hydroxy claim 1 , NH claim 1 , CN claim 1 , N claim 1 , N(R) claim 1 , NHR claim 1 , SH claim 1 , SR claim 1 , S(O)R claim 1 , OR claim 1 , (C-C)alkyl claim 1 , (C-C)haloalkyl claim 1 , —C(O)R claim 1 , —C(O)H claim 1 , —C(═O)OR claim 1 , —C(═O)OH claim 1 , —C(═O)N(R) claim 1 , —C(═O)NHR claim 1 , —C(═O)NH claim 1 , NHS(O)R claim 1 , NRS(O)R claim 1 , NHC(O)R claim 1 , NRC(O)R claim 1 , NHC(O)OR claim 1 , NRC(O)OR claim 1 , NRC(O)NHR claim 1 , NRC(O)N(R) claim 1 , NRC(O)NH claim 1 , NHC(O)NHR claim 1 , NHC(O)N(R) claim 1 , NHC(O)NH claim 1 , ═NH claim 1 , ═NOH claim 1 , ═NOR claim 1 , NRS(O)NHR claim 1 , NRS(O)N(R) claim 1 , NRS(O)NH claim 1 , NHS(O)NHR claim 1 , NHS(O)N(R) claim 1 , NHS(O)NH claim 1 , —OC(═O)R claim 1 , —OP(O)(OH)or R.15. The compound of wherein Ris H or C-Cheterocyclyl claim 1 , wherein any C-Cheterocyclyl of Ris optionally substituted with or more oxo claim 1 , halogen claim 1 , hydroxy ...

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09-05-2019 дата публикации

Quinazoline Compounds

Номер: US20190134035A1
Принадлежит:

Described herein are compounds of Formula (I) and tautomers and pharmaceutical salts thereof, compositions and formulations containing such compounds, and methods of using and making such compounds. 135-. (canceled)37. (canceled)38. A pharmaceutical composition comprising a compound of claim 36 , or a tautomer or a pharmaceutically acceptable salt thereof claim 36 , and a pharmaceutically acceptable carrier.39. The pharmaceutical composition of claim 38 , further comprising one claim 38 , two claim 38 , three claim 38 , or four additional therapeutic agents.40. The pharmaceutical composition of claim 39 , wherein the therapeutic agent is independently selected from the group consisting of HIV protease inhibiting compounds claim 39 , HIV non-nucleoside inhibitors of reverse transcriptase claim 39 , HIV nucleoside inhibitors of reverse transcriptase claim 39 , HIV nucleotide inhibitors of reverse transcriptase claim 39 , HIV integrase inhibitors claim 39 , gp41 inhibitors claim 39 , CXCR4 inhibitors claim 39 , gp120 inhibitors claim 39 , CCR5 inhibitors claim 39 , capsid polymerization inhibitors claim 39 , and other drugs for treating HIV claim 39 , and combinations thereof.4143-. (canceled)44. A method for treating an HIV infection in a subject comprising administering to the subject a compound of claim 36 , or a tautomer or a pharmaceutically acceptable salt thereof.45. A method for treating an HIV infection in a subject comprising administering to the subject in need thereof a compound of claim 36 , or a tautomer or a pharmaceutically acceptable salt thereof claim 36 , in combination with a therapeutically effective amount of one or more additional therapeutic agents selected from the group consisting of HIV protease inhibiting compounds claim 36 , HIV non-nucleoside inhibitors of reverse transcriptase claim 36 , HIV nucleoside inhibitors of reverse transcriptase claim 36 , HIV nucleotide inhibitors of reverse transcriptase claim 36 , HIV integrase inhibitors ...

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04-09-2014 дата публикации

ANTIVIRAL COMPOUNDS

Номер: US20140249074A1
Принадлежит: GILEAD PHARMASSET LLC

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. 127.-. (canceled)29. The composition of claim 28 , wherein the NS3 protease inhibitor is boceprevir.30. The composition of claim 28 , wherein the NS3 protease inhibitor is telaprevir.31. The composition of claim 28 , wherein the NS3 protease inhibitor is TMC435350.32. The composition of claim 28 , wherein the NS3 protease inhibitor is BI-1335.33. The composition of claim 28 , wherein the NS3 protease inhibitor is BI-1230.34. The composition of claim 28 , wherein the NS3 protease inhibitor is MK-7009.35. The composition of claim 28 , wherein the NS3 protease inhibitor is VBY-376.36. The composition of claim 28 , wherein the NS3 protease inhibitor is ITMN-191.38. The method of claim 37 , wherein the NS3 protease inhibitor is boceprevir.39. The method of claim 37 , wherein the NS3 protease inhibitor is telaprevir.40. The method of claim 37 , wherein the NS3 protease inhibitor is TMC435350.41. The method of claim 37 , wherein the NS3 protease inhibitor is BI-1335.42. The method of claim 37 , wherein the NS3 protease inhibitor is BI-1230.43. The method of claim 37 , wherein the NS3 protease inhibitor is MK-7009.44. The method of claim 37 , wherein the NS3 protease inhibitor is VBY-376.45. The method of claim 37 , wherein the NS3 protease inhibitor is ITMN-191.46. The method of claim 37 , wherein the human is treated for 12 weeks or less.47. The method of claim 37 , wherein the human is treated for 8 weeks or less.48. The method of claim 37 , wherein the human is treated for 6 weeks or less.49. The method of claim 37 , wherein the human is treated for 4 weeks or less.50. The method of claim 37 , wherein the human is treated for 2 weeks or less. This application claims priority to U.S. Provisional Application Nos. 61/177,972, filed ...

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21-05-2020 дата публикации

2'-CHLORO AMINOPYRIMIDINONE AND PYRIMIDINE DIONE NUCLEOSIDES

Номер: US20200157137A1
Принадлежит:

Provided herein are formulations, methods and substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds. 4. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein R is hydrogen.5. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein wherein Ris selected from the group of CN claim 1 , unsubstituted C-Calkyl claim 1 , C-Calkyl substituted with 1 claim 1 , 2 claim 1 , or 3 halogens selected from F and Cl claim 1 , C-Calkyl substituted with 1 substituent selected from —S—CHand —O—CH claim 1 , C-Calkenyl claim 1 , C-Calkynyl claim 1 , unsubstituted C-Ccycloalkyl claim 1 , C-Ccycloalkyl substituted by 1 claim 1 , 2 claim 1 , or 3 substituents selected from F and CH;6. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen.7. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris F.8. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare both hydrogen.9. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein R claim 1 , R claim 1 , and R are each hydrogen.10. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris F and Rand R are each hydrogen.11. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group of H and F; Ris selected from the group of CN claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , vinyl claim 1 , propenyl claim 1 , ethynyl claim 1 , CHF claim 1 , CHF claim 1 , CHCl claim 1 , CHSMe claim 1 , —CHOMe claim 1 , ...

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06-07-2017 дата публикации

PYRAZOLO[1,5-A]PYRIMIDINES FOR ANTIVIRAL TREATMENT

Номер: US20170190708A1
Принадлежит:

The invention provides compounds of Formula I or Formula II: 138-. (canceled) This application is a continuation of U.S. patent application Ser. No. 13/167,618, filed Jun. 23, 2011, which claims the benefit of priority of U.S. Provisional Application No. 61/358,122, filed Jun. 24, 2010. These applications are incorporated herein by reference in their entireties.The invention relates generally to methods and compounds for treating Pneumovirinae virus infections, particularly methods and nucleosides for treating respiratory syncytial virus infections.Pneumovirinae viruses are negative-sense, single-stranded, RNA viruses that are responsible for many prevalent human and animal diseases. The Pneumovirinae sub-family of viruses is a part of the family Paramyxoviridae and includes human respiratory syncytial virus (HRSV). Almost all children will have had an HRSV infection by their second birthday. HRSV is the major cause of lower respiratory tract infections in infancy and childhood with 0.5% to 2% of those infected requiring hospitalization. The elderly and adults with chronic heart, lung disease or those that are immunosuppressed also have a high risk for developing severe HRSV disease (http://www.cdc.gov/rsv/index.html). No vaccine to prevent HRSV infection is currently available. The monoclonal antibody palivizumab is available for immunoprophylaxis, but its use is restricted to infants at high risk, e.g., premature infants or those with either congenital heart or lung disease, and the cost for general use is often prohibitive. In addition, nucleoside analog ribavirin has been approved as the only antiviral agent to treat HRSV infections but has limited efficacy. Therefore, there is a need for anti-Pneumovirinae therapeutics.Certain racemic phenyl(2-(pyrazolo[1,5-a]pyrimidin-2-yl)piperidin-1-yl)methanone compounds are offered for sale by Asinex Corporation (101 N. Chestnet St., Winston-Salem, N.C. 27101) but the utility of these compounds for treating Pneumovirinae ...

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06-07-2017 дата публикации

MACROCYCLIC INHIBITORS OF FLAVIVIRIDAE VIRUSES

Номер: US20170190737A1
Принадлежит:

Provided are compounds of Formula I: 2. The compound of claim 1 , wherein Ais ethenylene claim 1 , propenylene claim 1 , butenylene claim 1 , ethylene claim 1 , propylene claim 1 , butylene claim 1 , oxypropylene claim 1 , oxypropenylene claim 1 , pyrazolylene claim 1 , phenylene claim 1 , pyridylene or pyrimidinylene.3. The compound of claim 1 , wherein Ais isoquinolinylene claim 1 , phenylene or halophenylene.4. The compound of claim 1 , wherein Xis —O— or —NH—; one of Rand Ris H and the other is methyl; Ris iso-propyl; Ris methyl and Ris H or methyl.5. The compound of claim 1 , wherein Ris H or methyl; Ris H; Ris H claim 1 , —OH claim 1 , methoxy claim 1 , trifluoroethoxy; and Ris H.7. The compound of claim 1 , wherein Ais heteroarylene; Ais (C-C)alkylene claim 1 , (C-C)alkenylene claim 1 , (C-C)alkynylene claim 1 , wherein Ais optionally substituted with one or more (C-C)alkyl; Ris H or methyl; and Ris H claim 1 , —OH or (C-C)alkoxy.8. (canceled)9. The compound of claim 1 , wherein Ais arylene;{'sup': 1', '1', '3a', '4a, 'sub': 2', '5', '2', '5', '2', '5', '2', '5', '2', '4', '1', '4', '1', '4', '1', '4, 'and Ais (C-C)alkylene, (C-C)alkenylene, (C-C)alkynylene, —O—(C-C)alkylene, —O—(C-C)alkenylene, wherein Ais optionally substituted with one or more (C-C)alkyl; Ris H or methyl; and Ris H, —OH, (C-C)alkoxy or halo(C-C)alkoxy.'}11. The compound of claim 1 , wherein Ais arylene; and Ais pyrazolylene claim 1 , phenylene or pyridylene.12. (canceled)13. The compound of claim 1 , wherein Ais halophenylene; and Ais —O—(C-C)alkylene or —O—(C-C)alkenylene.14. (canceled)17. A pharmaceutical composition comprising a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt claim 1 , isotope claim 1 , stereoisomer claim 1 , mixture of stereoisomers claim 1 , tautomer claim 1 , ester or prodrug thereof and a pharmaceutically acceptable excipient.18. The pharmaceutical composition of claim 17 , further comprising at least one additional ...

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25-09-2014 дата публикации

ANTIVIRAL COMPOUNDS

Номер: US20140288294A1
Принадлежит: Gilead Sciences, Inc.

The invention is related to phosphorus substituted anti-viral inhibitory 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. 1103-. (canceled) This application claims priority to U.S. Application No. 60/591,811, filed Jul. 27, 2004, the disclosures of which are incorporated by reference in their entirety. In particular, the figures described on pages 161 to 184 are incorporated as Figures herein.The invention relates generally to compounds with HIV inhibitory activity.Improving the delivery of drugs and other agents to target cells and tissues has been the focus of considerable research for many years. Though many attempts have been made to develop effective methods for importing biologically active molecules into cells, both in vivo and in vitro, none has proved to be entirely satisfactory. Optimizing the association of the inhibitory drug with its intracellular target, while minimizing intercellular redistribution of the drug, e.g., to neighboring cells, is often difficult or inefficient.Most agents currently administered to a patient parenterally are not targeted, resulting in systemic delivery of the agent to cells and tissues of the body where it is unnecessary, and often undesirable. This may result in adverse drug side effects, and often limits the dose of a drug (e.g., glucocorticoids and other anti-inflammatory drugs) that can be administered. By comparison, although oral administration of drugs is generally recognized as a convenient and economical method of administration, oral administration can result in either (a) uptake of the drug through the cellular and tissue barriers, e.g., blood/brain, epithelial, cell membrane, resulting in undesirable systemic distribution, or (b) temporary residence of the drug within the gastrointestinal tract. Accordingly, a major goal has been to develop methods for ...

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27-06-2019 дата публикации

THIENO[3,2-d]PYRIMIDINE, FURO[3,2-d]PYRIMIDINE, AND PYRROLO[3,2-D]PYRIMIDINES USEFUL FOR TREATING RESPIRATORY SYNCITIAL VIRUS INFECTIONS

Номер: US20190194223A1
Принадлежит:

Provided herein are formulations, methods and substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds. 14-. (canceled)6. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris Cl.7. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris NH.8. (canceled)9. The compound of claim 5 , or the pharmaceutical acceptable salt thereof wherein Ris H.10. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris H.11. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris F.12. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris F.13. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris Cl.14. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris N.15. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris selected from the group consisting of CN and N.16. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris selected from the group consisting of methyl claim 5 , ethyl claim 5 , and propyl.17. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris selected from the group consisting of CHF claim 5 , CHF claim 5 , and CHCl.23. A method of treating a Pneumoviridae virus infection in a human in need thereof claim 5 , the method comprising administering to the human a therapeutically effective amount of the compound of claim 5 , or the pharmaceutically acceptable salt thereof. ...

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27-07-2017 дата публикации

PHOSPHONATE ANALOGS OF HIV INHIBITOR COMPOUNDS

Номер: US20170210770A1
Принадлежит:

The invention is related to phosphorus substituted anti-viral inhibitory 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. 158-. (canceled)60. The method of claim 59 , wherein the conversion of compound 8 to compound 11 further comprises pyridine and triethylamine.61. The method of claim 60 , wherein the conversion of compound 8 to compound 11 further comprises a mixture of 2 claim 60 ,2′dithiodipyridine claim 60 , triphenylphosphine and pyridine.63. The method of claim 62 , wherein the conversion of compound 7 to compound 8 further comprises bromotrimethylsilane and dimethylformamide.64. The method of claim 63 , wherein the conversion of compound 7 to compound 8 further comprises NaHCO.66. A compound which is compound XXX claim 59 , or a pharmaceutically acceptable salt thereof claim 59 , prepared by the method of .67. A compound which is compound XXX claim 65 , or a pharmaceutically acceptable salt thereof claim 65 , prepared by the method of . This non-provisional application claims the benefit of Provisional Application No. 60/591,811, filed Jul. 27, 2004, and all of which are incorporated herein by reference.The invention relates generally to compounds with antiviral activity and more specifically with anti-HIV properties.AIDS is a major public health problem worldwide. Although drugs targeting HIV viruses are in wide use and have shown effectiveness, toxicity and development of resistant strains have limited their usefulness. Assay methods capable of determining the presence, absence or amounts of HIV viruses are of practical utility in the search for inhibitors as well as for diagnosing the presence of HIV.Human immunodeficiency virus (HIV) infection and related disease is a major public health problem worldwide. The retrovirus human immunodeficiency virus type 1 (HIV-1), a member of the primate lentivirus ...

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04-07-2019 дата публикации

2'-CHLORO AMINOPYRIMIDINONE AND PYRIMIDINE DIONE NUCLEOSIDES

Номер: US20190202852A1
Принадлежит:

Provided herein are formulations, methods and substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds. 221-. (canceled) This application claims the benefit of U.S. Provisional Application No. 62/040,349, filed on Aug. 21, 2014, which is hereby incorporated by reference in its entirety.Provided herein are substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds, methods and pharmaceutical formulations for treating Pneumovirinae virus infections, particularly including respiratory syncytial virus infections, and methods and intermediates useful for preparing the compounds.Pneumovirinae viruses are negative-sense, single-stranded, RNA viruses that are responsible for many prevalent human and animal diseases. The Pneumovirinae sub-family of viruses is a part of the family Paramyxoviridae and includes human respiratory syncytial virus (HRSV). Almost all children will have had an HRSV infection by their second birthday. HRSV is the major cause of lower respiratory tract infections in infancy and childhood with 0.5% to 2% of those infected requiring hospitalization. The elderly and adults with chronic heart, lung disease or those that are immunosuppressed also have a high risk for developing severe HRSV disease (http://www.cdc.gov/rsv/index.html). No vaccine to prevent HRSV infection is currently available. The monoclonal antibody palivizumab is available for immunoprophylaxis, but its use is restricted to infants at high risk, e.g., premature infants or those with either congenital heart or lung disease, and the cost for general use is often prohibitive. In addition, nucleoside analog ribavirin has been approved as the only antiviral agent to treat HRSV infections but has limited efficacy. Therefore, there is a ...

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18-08-2016 дата публикации

Pyrazolo[1,5-a]pyrimidines as antiviral agents

Номер: US20160235748A1
Принадлежит: Gilead Sciences Inc

The invention provides compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections. The compounds and compositions are useful for treating Pneumovirinae virus infection including Human respiratory syncytial virus infections.

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18-08-2016 дата публикации

Isoquinoline Compounds

Номер: US20160237062A1
Принадлежит: Gilead Sciences Inc

Described herein are compounds of Formula (I) and tautomers and pharmaceutical salts thereof, compositions and formulations containing such compounds, and methods of using and making such compounds.

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01-09-2016 дата публикации

QUINAZOLINE COMPOUNDS

Номер: US20160250215A1
Принадлежит:

Described herein are compounds of Formula (I) and tautomers and pharmaceutical salts thereof, compositions and formulations containing such compounds, and methods of using and making such compounds. 2. The compound of claim 1 , or a tautomer or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —H claim 1 , —CN claim 1 , —OR claim 1 , or Calkyl.3. The compound of claim 1 , or a tautomer or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —CN.4. (canceled)6. (canceled)7. The compound of claim 1 , or a tautomer or a pharmaceutically acceptable salt thereof claim 1 , wherein X claim 1 , X claim 1 , and Xare each CH.8. The compound of claim 1 , or a tautomer or a pharmaceutically acceptable salt thereof claim 1 , wherein Xis N; Xis CH; and Xis CH.9. The compound of claim 1 , or a tautomer or a pharmaceutically acceptable salt thereof claim 1 , wherein X claim 1 , X claim 1 , and Xare C(R); each Rare independently selected from —H claim 1 , —CN claim 1 , —OR claim 1 , halogen claim 1 , and Calkyl; and Ris selected from —H claim 1 , —CN claim 1 , —OR claim 1 , halogen claim 1 , and Calkyl.10. (canceled)11. The compound of claim 1 , or a tautomer or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —H claim 1 , —OR claim 1 , —NRR claim 1 , —NHC(O)NRR claim 1 , Calkyl claim 1 , or Cheteroalkyl.12. (canceled)13. The compound of claim 1 , or a tautomer or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —NHor —OH.1418-. (canceled)19. The compound of claim 1 , or a tautomer or a pharmaceutically acceptable salt thereof claim 1 , wherein two of R claim 1 , R claim 1 , and Rare —H and one of R claim 1 , R claim 1 , and Ris —H claim 1 , —OR claim 1 , halogen claim 1 , —NO claim 1 , —CN claim 1 , —NRR claim 1 , —NHC(O)NRR claim 1 , or Calkyl.2021-. (canceled)22. The compound of claim 1 , or a tautomer or a pharmaceutically acceptable salt thereof claim 1 , wherein R claim 1 , R claim 1 , and Rare —H.23. The compound of ...

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01-09-2016 дата публикации

FUSED PYRIMIDINE COMPOUNDS

Номер: US20160251347A1
Принадлежит:

Described herein are compounds of Formula (I) and tautomers and pharmaceutical salts thereof, compositions and formulations containing such compounds, and methods of using and making such compounds. 2. The compound of claim 1 , or a tautomer or pharmaceutically acceptable salt thereof claim 1 , wherein Ris —H claim 1 , —NRR claim 1 , or —OH.3. The compound of claim 1 , or a tautomer or pharmaceutically acceptable salt thereof claim 1 , wherein Ris —NHor —OH.4. The compound of claim 1 , or a tautomer or pharmaceutically acceptable salt thereof claim 1 , wherein each Ris independently —H claim 1 , —OR claim 1 , halogen claim 1 , —NRR claim 1 , —C(O)OR claim 1 , or —C(O)NRR.5. The compound of claim 1 , or a tautomer or pharmaceutically acceptable salt thereof claim 1 , wherein each Ris independently —H claim 1 , C(O)OR claim 1 , or —C(O)NRR.6. The compound of claim 1 , or a tautomer or pharmaceutically acceptable salt thereof claim 1 , wherein each Ris —H.7. The compound of claim 1 , or a tautomer or pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare each independently halogen claim 1 , —O—Calkyl claim 1 , or Calkyl optionally substituted with 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 Rgroups claim 1 , which may be the same or different.8. The compound of claim 1 , or a tautomer or pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare each independently Calkyl.9. The compound of claim 1 , or a tautomer or pharmaceutically acceptable salt thereof claim 1 , wherein Ris —H claim 1 , —CN claim 1 , —O—Calkyl claim 1 , —Chaloalkyl claim 1 , or halogen.11. The compound of claim 1 , or a tautomer or pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare —CH.12. The compound of claim 1 , or a tautomer or pharmaceutically acceptable salt thereof claim 1 , wherein Ris —NH.13. The compound of claim 1 , or a tautomer or pharmaceutically acceptable salt thereof claim 1 , wherein Ris —H claim 1 , —CN claim 1 , —O—Calkyl claim 1 , —CF ...

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01-10-2015 дата публикации

MACROCYCLIC INHIBITORS OF FLAVIVIRIDAE VIRUSES

Номер: US20150274774A1
Принадлежит:

Provided are compounds of Formula I: 2. The method according to claim 1 , wherein Ais ethenylene claim 1 , propenylene claim 1 , butenylene claim 1 , ethylene claim 1 , propylene claim 1 , butylene claim 1 , oxypropylene claim 1 , oxypropenylene claim 1 , pyrazolylene claim 1 , phenylene or pyrimidinylene.3. The method according to claim 1 , wherein Ais isoquinolinylene claim 1 , phenylene or halophenylene.4. The method according to claim 1 , wherein Xis —O— or —NH—; one of Rand Ris H and the other is methyl; Ris iso-propyl; Ris methyl and Ris H or methyl.5. The method according to claim 1 , wherein Ris H or methyl; Ris H; Ris H claim 1 , —OH claim 1 , methoxy claim 1 , trifluoroethoxy; and Ris H.7. The method according to claim 6 , wherein Ais heteroarylene; Ais (C-C)alkylene claim 6 , (C-C)alkenylene claim 6 , (C-C)alkynylene claim 6 , wherein Ais optionally substituted with one or more (C-C)alkyl; Ris H or (C-C)alkyl; and Ris H claim 6 , —OH or (C-C)alkoxy.9. The method according to claim 6 , wherein Ais arylene; and Ais (C-C)alkylene claim 6 , (C-C)alkenylene claim 6 , (C-C)alkynylene claim 6 , —O—(C-C)alkylene claim 6 , —O—(C-C)alkenylene claim 6 , wherein Ais optionally substituted with one or more (C-C)alkyl; Ris H or (C-C)alkyl; and Ris H claim 6 , —OH claim 6 , C)alkoxy or halo(C-C)alkoxy.11. The method of claim 6 , wherein Ais arylene; and Ais pyrazolylene claim 6 , phenylene or pyrimidinylene.13. The method according to claim 1 , wherein Ais haloarylene; and Ais —O—(C-C)alkylene or —O—(C-C)alkenylene.17. (canceled)18. (canceled)19. (canceled)20. (canceled)21. The method of claim 1 , wherein the viral infection is caused by a Hepatitis C virus.22. The method of claim 1 , wherein the viral infection causes a disease selected from the group consisting of dengue fever claim 1 , yellow fever claim 1 , hepatitis C claim 1 , Japanese encephalitis claim 1 , Kyasanur forest disease claim 1 , Murray valley encephalitis claim 1 , St. Louis encephalitis claim 1 , ...

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22-08-2019 дата публикации

METHODS FOR TREATING ARENAVIRIDAE AND CORONAVIRIDAE VIRUS INFECTIONS

Номер: US20190255085A1
Принадлежит:

Provided are methods for treating Arenaviridae and Coronaviridae virus infections by administering nucleosides and prodrugs thereof, of Formula I: 139.-. (canceled)41. (canceled)43. (canceled)4950.-. (canceled)53. The method of wherein Ris C-Calkyl.54. The method of wherein Ris C-Calkyl.5558.-. (canceled)63. The method of further comprising a pharmaceutically acceptable carrier or excipient.64. The method of further comprising administering a therapeutically effective amount of at least one other therapeutic agent or composition thereof selected from the group consisting of a corticosteroid claim 40 , an anti-inflammatory signal transduction modulator claim 40 , a β2-adrenoreceptor agonist bronchodilator claim 40 , an anticholinergic claim 40 , a mucolytic agent claim 40 , hypertonic saline and other drugs for treating a Coronaviridae virus infection; or mixtures thereof.65. The method of wherein the Coronaviridae infection is caused by a Coronaviridae virus.66. The method of wherein the Coronaviridae infection is caused by a Coronaviridae virus selected from SARS claim 40 , MERS claim 40 , 229E claim 40 , NL63 claim 40 , OC43 claim 40 , and HKU1.6774.-. (canceled) This patent application is a Continuation of U.S. patent application Ser. No. 15/267,433, filed on Sep. 16, 2016, which claims the benefit under 35 U.S.C. § 119(e) of U.S. Provisional Patent Application No. 62/219,302, filed Sep. 16, 2015 and U.S. Provisional Application No. 62/239,696, filed Oct. 9, 2015. The foregoing applications are incorporated herein by reference in their entireties.The content of the following submission on ASCII text file is incorporated herein by reference in its entirety: a computer readable form (CRF) of the Sequence Listing (file name: 1137P2C_2016-11-28_Sequence_Listing.txt, date recorded: Nov. 29, 2016, size: 1 KB).The invention relates generally to methods and compounds for treating Arenaviridae virus infections, particularly methods and nucleosides and prodrugs thereof for ...

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05-10-2017 дата публикации

TOLL LIKE RECEPTOR MODULATOR COMPOUNDS

Номер: US20170281627A1
Принадлежит:

The present disclosure relates generally to toll like receptor modulator compounds, such as diamino pyrido[3,2 D] pyrimidine compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR-8), and methods of making and using them. 1102-. (canceled)104. The method of claim 103 , further comprising administering one or more additional therapeutic agents.105. The method of claim 103 , further comprising administering tenofovir alafenamide claim 103 , tenofovir alafenamide fumarate claim 103 , or tenofovir alafenamide hemifumarate.107. The method of claim 106 , further comprising administering one or more additional therapeutic agents.108. The method of claim 106 , further comprising administering tenofovir alafenamide claim 106 , tenofovir alafenamide fumarate claim 106 , or tenofovir alafenamide hemifumarate.110. The method of claim 109 , further comprising administering one or more additional therapeutic agents.111. The method of claim 109 , further comprising administering tenofovir alafenamide claim 109 , tenofovir alafenamide fumarate claim 109 , or tenofovir alafenamide hemifumarate.113. The method of claim 112 , further comprising administering one or more additional therapeutic agents.114. The method of claim 112 , further comprising administering tenofovir alafenamide claim 112 , tenofovir alafenamide fumarate claim 112 , or tenofovir alafenamide hemifumarate. This application claims priority to U.S. Provisional Application No. 62/128,397, filed Mar. 4, 2015, and 62/250,403, filed Nov. 3, 2015, both of which are incorporated herein in their entireties for all purposes.This application relates generally to toll like receptor modulator compounds, including diamino pyrido[3,2 D] pyrimidine compounds, and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR-8), and methods of making and using them.The toll-like receptor (TLR) family plays a fundamental role in pathogen recognition ...

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06-10-2016 дата публикации

TOLL LIKE RECEPTOR MODULATOR COMPOUNDS

Номер: US20160289229A1
Принадлежит:

The present disclosure relates generally to toll like receptor modulator compounds, such as diamino pyrido[3,2 D]pyrimidine compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR-8), and methods of making and using them. 1102-. (canceled)105. A pharmaceutical composition comprising the compound or a pharmaceutically acceptable salt thereof claim 103 , and a pharmaceutically acceptable excipient.106. A pharmaceutical composition comprising the compound of claim 104 , and a pharmaceutically acceptable excipient.109. A pharmaceutical composition comprising the compound or a pharmaceutically acceptable salt thereof claim 107 , and a pharmaceutically acceptable excipient.110. A pharmaceutical composition comprising the compound of claim 108 , and a pharmaceutically acceptable excipient.113. A pharmaceutical composition comprising the compound of or a pharmaceutically acceptable salt thereof claim 111 , and a pharmaceutically acceptable excipient.114. A pharmaceutical composition comprising the compound of claim 112 , and a pharmaceutically acceptable excipient.117. A pharmaceutical composition comprising the compound of or a pharmaceutically acceptable salt thereof claim 115 , and a pharmaceutically acceptable excipient.118. A pharmaceutical composition comprising the compound of claim 116 , and a pharmaceutically acceptable excipient. This application claims priority to U.S. Provisional Application No. 62/128,397, filed Mar. 4, 2015, and 62/250,403, filed Nov. 3, 2015, both of which are incorporated herein in their entireties for all purposes.This application relates generally to toll like receptor modulator compounds, including diamino pyrido[3,2 D]pyrimidine compounds, and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR-8), and methods of making and using them.The toll-like receptor (TLR) family plays a fundamental role in pathogen recognition and activation of innate ...

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12-09-2019 дата публикации

Methods for treating filoviridae virus infections

Номер: US20190275063A1
Принадлежит: Gilead Sciences Inc

The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.

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19-09-2019 дата публикации

TOLL LIKE RECEPTOR MODULATOR COMPOUNDS

Номер: US20190282576A1
Принадлежит:

The present disclosure relates generally to toll like receptor modulator compounds, such as diamino pyrido[3,2 D] pyrimidine compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR-8), and methods of making and using them. 1102.-. (canceled)104. The compound of claim 103 , or a pharmaceutically acceptable salt thereof claim 103 , wherein:{'sup': '1', 'sub': 1-3', '1-3, 'Ris selected from the group consisting of hydrogen, halogen, and Calkyl, wherein Calkyl is optionally substituted with 1 to 5 halogen groups;'}{'sup': 2', 'a, 'sub': 1-3', '1-3, 'Ris selected from the group consisting of hydrogen, halogen, Calkyl, CN and OR, wherein Calkyl is optionally substituted with 1 to 5 halogen groups; and'}{'sup': '3', 'sub': '1-3', 'Ris selected from the group consisting of hydrogen, halogen, and Calkyl.'}105. The compound of claim 103 , or a pharmaceutically acceptable salt thereof claim 103 , wherein:{'sup': '1', 'sub': '3', 'Ris selected from the group consisting of hydrogen, methyl, fluoro, chloro, and CF;'}{'sup': '2', 'sub': '3', 'Ris selected from the group consisting of hydrogen, methyl, ethyl, fluoro, chloro, bromo, CF, CN, OH, OMe, and OEt; and'}{'sup': '3', 'Ris selected from the group consisting of hydrogen, methyl, fluoro, and chloro.'}106. The compound of claim 103 , or a pharmaceutically acceptable salt thereof claim 103 , wherein:{'sup': '1', 'Ris hydrogen;'}{'sup': '2', 'Ris selected from the group consisting of hydrogen and fluoro; and'}{'sup': '3', 'Ris selected from the group consisting of hydrogen and methyl.'}107. The compound of claim 103 , or a pharmaceutically acceptable salt thereof claim 103 , wherein Ris methyl.108. The compound of claim 103 , or a pharmaceutically acceptable salt thereof claim 103 , wherein Ris hydrogen.109. The compound of claim 103 , or a pharmaceutically acceptable salt thereof claim 103 , wherein{'sup': a', 'b, 'sub': 1-3', '1-3, 'each Rand Ris independently selected from ...

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18-10-2018 дата публикации

PYRAZOLO[1,5-A]PYRIMIDINES FOR ANTIVIRAL TREATMENT

Номер: US20180298011A1
Принадлежит:

The invention provides compounds of Formula I or Formula II: 138-. (canceled)41. A method of treating a Pneumovirinae virus infection in a mammal in need thereof comprising administering to the mammal a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt or ester thereof.42. A method of treating a Pneumovirinae virus infection in a mammal in need thereof comprising administering to the mammal a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt or ester thereof.43. The method of wherein the Pneumovirinae virus infection is caused by a respiratory syncytial virus.44. The method of wherein the Pneumovirinae virus infection is caused by a respiratory syncytial virus.45. The method of further comprising administering a therapeutically effective amount of at least one other therapeutic agent or composition thereof selected from the group consisting of ribavirin claim 41 , palivizumab claim 41 , motavizumab claim 41 , RSV-IGIV MEDI-557 claim 41 , A-60444 claim 41 , MDT-637 claim 41 , BMS-433771 claim 41 , ALN-RSV0 and ALX-0171 or mixtures thereof.46. The method of further comprising administering a therapeutically effective amount of at least one other therapeutic agent or composition thereof selected from the group consisting of ribavirin claim 42 , palivizumab claim 42 , motavizumab claim 42 , RSV-IGIV MEDI-557 claim 42 , A-60444 claim 42 , MDT-637 claim 42 , BMS-433771 claim 42 , ALN-RSV0 and ALX-0171 or mixtures thereof. This patent application claims the benefit of priority of U.S. application Ser. No. 61/358,122, filed Jun. 24, 2010.The invention relates generally to methods and compounds for treating Pneumovirinae virus infections, particularly methods and nucleosides for treating respiratory syncytial virus infections.Pneumovirinae viruses are negative-sense, single-stranded, RNA viruses that are responsible for many prevalent human and animal diseases. The Pneumovirinae sub-family of viruses ...

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01-11-2018 дата публикации

METHODS FOR TREATING FILOVIRIDAE VIRUS INFECTIONS

Номер: US20180311263A1
Принадлежит:

Provided are compounds, methods, and pharmaceutical compositions for treating Filoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula IV: 2. The method of wherein{'sup': 'e1', 'sub': 1', '6, 'Ris H, C-Calkyl or benzyl; and'}{'sup': 'e2', 'sub': 1', '6, 'Ris H or C-Calkyl.'}5. (canceled)7. (canceled)8. The method of further comprising a pharmaceutically acceptable carrier or excipient.9. The method of further comprising administering a therapeutically effective amount of at least one other therapeutic agent or composition thereof selected from the group consisting of a corticosteroid claim 1 , an anti-inflammatory signal transduction modulator claim 1 , a β2-adrenoreceptor agonist bronchodilator claim 1 , an anticholinergic claim 1 , a mucolytic agent claim 1 , hypertonic saline and other drugs for treating Filoviridae virus infections; or mixtures thereof.10. (canceled)11. The method of wherein the Filoviridae infection is caused by a Filoviridae virus.12. The method of wherein the Filoviridae infection is caused by an ebolavirus.13. The method of wherein the Filoviridae infection is caused by Bundibugyo ebolavirus claim 1 , Reston ebolavirus claim 1 , Sudan ebolavirus claim 1 , Tai Forest ebolavirus claim 1 , or Zaire ebolavirus.14. The method of wherein the Filoviridae infection is caused by a Marburg virus.15. The method of wherein a Filoviridae polymerase is inhibited.17. (canceled)18. (canceled)19. The method of claim 16 , wherein the Filoviridae infection is caused by a Filoviridae virus.20. The method of claim 16 , wherein the Filoviridae infection is caused by an ebolavirus.21. The method of claim 16 , wherein the Filoviridae infection is caused by a Marburg virus.22. (canceled)23. (canceled)24. (canceled)26. The pharmaceutical composition of claim 25 , wherein{'sup': 'e1', 'Ris H, methyl, or benzyl; and'}{'sup': 'e2', 'Ris H or methyl.'}27. The pharmaceutical composition of claim 25 , wherein{'sup': 'e1 ...

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16-11-2017 дата публикации

2'-CHLORO AMINOPYRIMIDINONE AND PYRIMIDINE DIONE NUCLEOSIDES

Номер: US20170327526A1
Принадлежит:

Provided herein are formulations, methods and substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds. 1. (canceled)34-. (canceled)5. The method of claim 2 , wherein Ris selected from the group of CN claim 2 , unsubstituted C-Calkyl claim 2 , C-Calkyl substituted with 1 claim 2 , 2 claim 2 , or 3 halogens selected from F and Cl claim 2 , C-Calkyl substituted with 1 substituent selected from —S—CHand —O—CH claim 2 , C-Calkenyl claim 2 , C-Calkynyl claim 2 , unsubstituted C-Ccycloalkyl claim 2 , C-Ccycloalkyl substituted by 1 claim 2 , 2 claim 2 , or 3 substituents selected from F and CH;6. The method of claim 2 , wherein Ris hydrogen.7. The method of claim 2 , wherein Ris F.8. (canceled)9. The method of claim 2 , wherein R claim 2 , R claim 2 , and R are each hydrogen.10. The method of claim 2 , wherein Ris F and Rand Rare each hydrogen.11. The method of claim 2 , wherein Ris CN claim 2 , methyl claim 2 , ethyl claim 2 , propyl claim 2 , vinyl claim 2 , propenyl claim 2 , ethynyl claim 2 , CHF claim 2 , CHF claim 2 , CHCl claim 2 , CHSMe claim 2 , —CHOMe claim 2 , or cyclopropyl.1215-. (canceled)1921-. (canceled) This application claims the benefit of U.S. Provisional Application No. 62/040,349, filed on Aug. 21, 2014, which is hereby incorporated by reference in its entirety.Provided herein are substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds, methods and pharmaceutical formulations for treating Pneumovirinae virus infections, particularly including respiratory syncytial virus infections, and methods and intermediates useful for preparing the compounds.Pneumovirinae viruses are negative-sense, single-stranded, RNA viruses that are responsible for many prevalent human and animal diseases. The ...

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17-10-2019 дата публикации

PHOSPHONATE ANALOGS OF HIV INHIBITOR COMPOUNDS

Номер: US20190315785A1
Принадлежит:

The invention is related to phosphorus substituted anti-viral inhibitory 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. 158-. (canceled)60. The metabolic product of which is substantially isolated.61. A method of preparing the in vivo metabolic product of comprising contacting the compound of Formula MBF-I with a mammal for a period of time sufficient to yield the in vivo metabolic product.62. The method of wherein the mammal is a rat claim 61 , mouse claim 61 , guinea pig claim 61 , monkey claim 61 , or human.63. The method of wherein the compound of Formula MBF-I is orally administered to the mammal.64. The method of wherein the compound of Formula MBF-I is radiolabeled.65. The method of wherein the radiolabel comprises Cor H.66. A method of determining the optimal therapeutic dose of the compound of Formula MBF-I in a mammal comprising measuring the quantity of the in vivo metabolic product of produced upon contacting the mammal with a radiolabeled the compound of Formula MBF-I and correlating the measured quantity of the in vivo metabolic product with therapeutic effectiveness of the compound of Formula MBF-I.68. A pharmaceutical composition comprising the prodrug of claim 67 , or a pharmaceutically acceptable salt thereof claim 67 , and at least one pharmaceutically acceptable carrier or excipient.69. A method of improving the pharmacokinetics of a drug claim 67 , comprising administering to a patient treated with said drug claim 67 , a therapeutically effective amount of the prodrug of claim 67 , or a pharmaceutically acceptable salt thereof.71. A pharmaceutical composition comprising the solvate of claim 70 , or a pharmaceutically acceptable salt thereof claim 70 , and at least one pharmaceutically acceptable carrier or excipient.72. A method of improving the pharmacokinetics of a drug claim 70 , ...

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29-11-2018 дата публикации

2'-CHLORO AMINOPYRIMIDINONE AND PYRIMIDINE DIONE NUCLEOSIDES

Номер: US20180340004A1
Принадлежит:

Provided herein are formulations, methods and substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds. 4. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen.5. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group of CN claim 1 , unsubstituted C-Calkyl claim 1 , C-Calkyl substituted with 1 claim 1 , 2 claim 1 , or 3 halogens selected from F and Cl claim 1 , C-Calkyl substituted with 1 substituent selected from —S—CHand —O—CH claim 1 , C-Calkenyl claim 1 , C-Calkynyl claim 1 , unsubstituted C-Ccycloalkyl claim 1 , C-Ccycloalkyl substituted by 1 claim 1 , 2 claim 1 , or 3 substituents selected from F and CH;6. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen.7. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris F.8. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare both hydrogen.9. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein R claim 1 , R claim 1 , and Rare each hydrogen.10. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris F and Rand Rare each hydrogen.11. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group of H and F; Ris selected from the group of CN claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , vinyl claim 1 , propenyl claim 1 , ethynyl claim 1 , CHF claim 1 , CHF claim 1 , CHCl claim 1 , CHSMe claim 1 , —CHOMe claim 1 , and ...

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15-12-2016 дата публикации

METHODS FOR TREATING FILOVIRIDAE VIRUS INFECTIONS

Номер: US20160361330A1
Принадлежит:

Provided are compounds, methods, and pharmaceutical compositions for treating Filoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula IV: 2. The method of wherein Ris H.8. The method of further comprising a pharmaceutically acceptable carrier or excipient.9. The method of further comprising administering a therapeutically effective amount of at least one other therapeutic agent or composition thereof selected from the group consisting of a corticosteroid claim 1 , an anti-inflammatory signal transduction modulator claim 1 , a β2-adrenoreceptor agonist bronchodilator claim 1 , an anticholinergic claim 1 , a mucolytic agent claim 1 , hypertonic saline and other drugs for treating Filoviridae virus infections; or mixtures thereof.10. The method of wherein the at least one other therapeutic agent is ribavirin claim 9 , palivizumab claim 9 , motavizumab claim 9 , RSV-IGIV (RespiGam®) claim 9 , MEDI-557 claim 9 , A-60444 claim 9 , MDT-637 claim 9 , BMS-433771 claim 9 , amiodarone claim 9 , dronedarone claim 9 , verapamil claim 9 , Ebola Convalescent Plasma (ECP) claim 9 , TKM-100201 claim 9 , BCX4430 ((2S claim 9 ,3S claim 9 ,4R claim 9 ,5R)-2-(4-amino-5H-pyrrolo[3 claim 9 ,2-d]pyrimidin-7-yl)-5-(hydroxymethyl)pyrrolidine-3 claim 9 ,4-diol) claim 9 , favipiravir (also known as T-705 or Avigan) claim 9 , T-705 monophosphate claim 9 , T-705 diphosphate claim 9 , T-705 triphosphate claim 9 , FGI-106 (1-N claim 9 ,7-N-bis[3-(dimethylamino)propyl]-3 claim 9 ,9-dimethylquinolino[8 claim 9 ,7-h]quinolone-1 claim 9 ,7-diamine) claim 9 , JK-05 claim 9 , TKM-Ebola claim 9 , ZMapp claim 9 , rNAPc2 claim 9 , VRC-EBOADC076-00-VP claim 9 , OS-2966 claim 9 , MVA-BN filo claim 9 , brincidofovir claim 9 , Vaxart adenovirus vector 5-based ebola vaccine claim 9 , Ad26-ZEBOV claim 9 , FiloVax vaccine claim 9 , GOVX-E301 claim 9 , GOVX-E302 claim 9 , ebola virus entry inhibitors (NPC1 inhibitors) claim 9 , or rVSV-EBOV or mixtures thereof. ...

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14-12-2017 дата публикации

Quinazoline Compounds

Номер: US20170354656A1
Принадлежит:

Described herein are compounds of Formula (I) and tautomers and pharmaceutical salts thereof, compositions and formulations containing such compounds, and methods of using and making such compounds. 135-. (canceled)37. (canceled)38. A pharmaceutical composition comprising a compound of claim 36 , or a tautomer or a pharmaceutically acceptable salt thereof claim 36 , and a pharmaceutically acceptable carrier.39. The pharmaceutical composition of claim 38 , further comprising one claim 38 , two claim 38 , three claim 38 , or four additional therapeutic agents.40. The pharmaceutical composition of claim 39 , wherein the therapeutic agent is independently selected from the group consisting of HIV protease inhibiting compounds claim 39 , HIV non-nucleoside inhibitors of reverse transcriptase claim 39 , HIV nucleoside inhibitors of reverse transcriptase claim 39 , HIV nucleotide inhibitors of reverse transcriptase claim 39 , HIV integrase inhibitors claim 39 , gp41 inhibitors claim 39 , CXCR4 inhibitors claim 39 , gp120 inhibitors claim 39 , CCR5 inhibitors claim 39 , capsid polymerization inhibitors claim 39 , and other drugs for treating HIV claim 39 , and combinations thereof.4143-. (canceled)44. A method for treating an HIV infection in a subject comprising administering to the subject a compound of claim 36 , or a tautomer or a pharmaceutically acceptable salt thereof.45. A method for treating an HIV infection in a subject comprising administering to the subject in need thereof a compound of claim 36 , or a tautomer or a pharmaceutically acceptable salt thereof claim 36 , in combination with a therapeutically effective amount of one or more additional therapeutic agents selected from the group consisting of HIV protease inhibiting compounds claim 36 , HIV non-nucleoside inhibitors of reverse transcriptase claim 36 , HIV nucleoside inhibitors of reverse transcriptase claim 36 , HIV nucleotide inhibitors of reverse transcriptase claim 36 , HIV integrase inhibitors ...

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14-11-2019 дата публикации

PHOSPHONATE ANALOGS OF HIV INHIBITOR COMPOUNDS

Номер: US20190345190A1
Принадлежит:

The invention is related to phosphorus substituted anti-viral inhibitory 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. 1103-. (canceled)105. The metabolic product of which is substantially isolated.106. A method of preparing the in vivo metabolic product of comprising contacting the compound of Formula A with a mammal for a period of time sufficient to yield the in vivo metabolic product.107. The method of wherein the compound of Formula A is radiolabeled.108. The method of wherein the radiolabel comprises Cor H.109. A method of determining the optimal therapeutic dose of the compound of Formula A in a mammal comprising measuring the quantity of the in vivo metabolic product of produced upon contacting the mammal with a radiolabeled the compound of Formula A and correlating the measured quantity of the in vivo metabolic product with therapeutic effectiveness of the compound of Formula A.111. A pharmaceutical composition comprising the prodrug of claim 110 , or a pharmaceutically acceptable salt thereof claim 110 , and at least one pharmaceutically acceptable carrier or excipient.112. A method of improving the pharmacokinetics of a drug claim 110 , comprising administering to a patient treated with said drug claim 110 , a therapeutically effective amount of the prodrug of claim 110 , or a pharmaceutically acceptable salt thereof114. A pharmaceutical composition comprising the solvate of claim 113 , or a pharmaceutically acceptable salt thereof claim 113 , and at least one pharmaceutically acceptable carrier or excipient.115. A method of improving the pharmacokinetics of a drug claim 113 , comprising administering to a patient treated with said drug claim 113 , a therapeutically effective amount of the solvate of claim 113 , or a pharmaceutically acceptable salt thereof. This application claims priority to U.S. ...

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21-12-2017 дата публикации

PYRAZOLO[1,5-A]PYRIMIDINES FOR ANTIVIRAL TREATMENT

Номер: US20170362244A1
Принадлежит:

The invention provides compounds of Formula I or Formula II: 138.-. (canceled)41. The process of claim 40 , wherein the reacting step is performed in a solvent comprising triethylamine and methanol.42. The process of claim 40 , comprising heating the reaction to about 75° C.43. The process of claim 40 , wherein the pharmaceutically acceptable salt is trifluoroacetic acid salt.45. The process of wherein the pharmaceutically acceptable salt is trifluoroacetic acid salt.46. The process of wherein the contacting step is performed in a solvent comprising trifluoroacetic acid and dichloromethane.47. The process of wherein the contacting step comprises stirring overnight.50. The process of wherein the contacting step is performed in a solution claim 49 , the solution comprising a solvent and a reagent.55. The process of wherein the reacting step is heated to 100° C. This patent application claims the benefit of priority of U.S. application Ser. No. 61/358122, filed Jun. 24, 2010.The invention relates generally to methods and compounds for treating Pneumovirinae virus infections, particularly methods and nucleosides for treating respiratory syncytial virus infections.Pneumovirinae viruses are negative-sense, single-stranded, RNA viruses that are responsible for many prevalent human and animal diseases. The Pneumovirinae sub-family of viruses is a part of the family Paramyxoviridae and includes human respiratory syncytial virus (HRSV). Almost all children will have had an HRSV infection by their second birthday. HRSV is the major cause of lower respiratory tract infections in infancy and childhood with 0.5% to 2% of those infected requiring hospitalization. The elderly and adults with chronic heart, lung disease or those that are immunosuppressed also have a high risk for developing severe HRSV disease (http://www.cdc.gov/rsv/index.html). No vaccine to prevent HRSV infection is currently available. The monoclonal antibody palivizumab is available for immunoprophylaxis, but ...

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12-11-2020 дата публикации

METHODS FOR TREATING ARENAVIRIDAE AND CORONAVIRIDAE VIRUS INFECTIONS

Номер: US20200352967A1
Принадлежит:

Provided are methods for treating Arenaviridae and Coronaviridae virus infections by administering nucleosides and prodrugs thereof, of Formula I: 174-. (canceled)77. The method of claim 75 , further comprising administering a pharmaceutically acceptable carrier or excipient.78. The method of claim 75 , further comprising administering a therapeutically effective amount of at least one other therapeutic agent.79. The method of claim 78 , wherein the at least one other therapeutic agent is selected from the group consisting of a corticosteroid claim 78 , an anti-inflammatory signal transduction modulator claim 78 , a β2-adrenoreceptor agonist bronchodilator claim 78 , an anticholinergic claim 78 , a mucolytic agent claim 78 , hypertonic saline claim 78 , and other drugs for treating a Coronaviridae virus infection; or mixtures thereof.80. The method of claim 75 , wherein the Coronaviridae infection is caused by a Coronaviridae virus selected from the group consisting of SARS claim 75 , MERS claim 75 , 229E claim 75 , NL63 claim 75 , OC43 claim 75 , and HKUL.81. The method of claim 75 , wherein the Coronaviridae infection is caused by a SARS virus.82. The method of claim 75 , wherein the Coronaviridae infection is caused by a MERS virus.83. The method of claim 75 , wherein the compound claim 75 , or a pharmaceutically acceptable salt thereof claim 75 , is administered by oral claim 75 , rectal claim 75 , nasal claim 75 , pulmonary claim 75 , topical claim 75 , vaginal claim 75 , or parenteral administration.84. The method of claim 83 , wherein the compound claim 83 , or a pharmaceutically acceptable salt thereof claim 83 , is administered by parenteral administration.85. The method of claim 75 , wherein the compound claim 75 , or a pharmaceutically acceptable salt thereof claim 75 , is administered by subcutaneous claim 75 , intramuscular claim 75 , intravenous claim 75 , intradermal claim 75 , intrathecal claim 75 , or epidural administration.86. The method of claim ...

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19-11-2020 дата публикации

Quinazoline Compounds

Номер: US20200360383A1
Принадлежит:

Described herein are compounds of Formula (I) and tautomers and pharmaceutical salts thereof, compositions and formulations containing such compounds, and methods of using and making such compounds. 24-. (canceled)6. (canceled)7. The pharmaceutical composition of claim 1 , wherein X claim 1 , X claim 1 , and Xare each CH.8. (canceled)9. The pharmaceutical composition of claim 1 , wherein X claim 1 , X claim 1 , and Xare C(R); each Rindependently selected from —H claim 1 , —CN claim 1 , —OR claim 1 , halogen claim 1 , and Calkyl; and Ris selected from —H claim 1 , —CN claim 1 , —OR claim 1 , halogen claim 1 , and Calkyl.10. (canceled)11. The pharmaceutical composition of claim 1 , wherein Ris —H claim 1 , —OR claim 1 , —NRR claim 1 , —NHC(O)NRR claim 1 , Calkyl claim 1 , or Cheteroalkyl.12. (canceled)13. The pharmaceutical composition of claim 1 , wherein Ris —NHor —OH.1418-. (canceled)19. The pharmaceutical composition of wherein Ris —H claim 1 , and Ris —H claim 1 , —OR claim 1 , halogen claim 1 , —NO claim 1 , —CN claim 1 , —NRR claim 1 , —NHC(O)NRR claim 1 , or Calkyl.20. (canceled)21. (canceled)22. The pharmaceutical composition of claim 1 , wherein R claim 1 , R claim 1 , and Rare —H.23. The pharmaceutical composition of claim 1 , wherein Ris Calkyl.24. The pharmaceutical composition of claim 1 , wherein Ris Calkyl.25. (canceled)26. (canceled)27. The pharmaceutical composition of claim 1 , wherein Rand Rare Calkyl.28. The pharmaceutical composition of claim 1 , wherein Rand Rare methyl.29. The pharmaceutical composition of claim 1 , wherein Ris —H or Calkyl.30. The pharmaceutical composition of claim 1 , wherein Ris —H or Calkyl.3133-. (canceled)35. (canceled)3743-. (canceled)4551-. (canceled)52. The pharmaceutical composition of claim 1 , wherein one of the additional therapeutic agents is selected from tenofovir alafenamide claim 1 , tenofovir alafenamide fumarate claim 1 , and tenofovir alafenamide hemifumarate.53. The method of claim 44 , wherein one of the ...

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10-11-2022 дата публикации

ANTIVIRAL COMPOUNDS

Номер: US20220356196A1
Принадлежит:

The present disclosure provides compounds for treating a variety of diseases, such as respiratory syncytial virus (RSV), HRV, hMPV, ebola, Zika, West Nile, Dengue, and HCV. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 1', '2', '1A', '1A', '1', '2, 'Rand Rare each independently H or —C(O)R, wherein Ris methyl, ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl, sec-butyl or t-butyl, wherein at least one of Rand Ris H;'}{'sup': 1', '2, 'sub': '2', 'or Rand Rare combined to form —C(O)—, —C(Me)- or —CH(OEt)-.'}3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 1', '2', '1A', '1A', '1', '2, 'Rand Rare each independently H or —C(O)R, wherein Ris ethyl, iso-propyl or t-butyl, wherein at least one of Rand Ris H;'}{'sup': 1', '2, 'sub': '2', 'or Rand Rare combined to form —C(O)—, —C(Me)- or —CH(OEt)-.'}4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': '3', 'sub': '2', 'Ris NH.'}5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': '4A', 'Ris O.'}6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 1', '2', '1A', '1A', '1', '2, 'Rand Rare each independently H or —C(O)R, wherein Ris ethyl, iso-propyl or t-butyl, wherein at least one of Rand Ris H;'}{'sup': 1', '2, 'sub': '2', 'or Rand Rare combined to form —C(O)—, —C(Me)- or —CH(OEt)-;'}{'sup': '3', 'sub': '2', 'Ris NH; and'}{'sup': '4A', 'Ris O.'}19. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 4G', '4G1', '4G1, 'sub': 2', '2', '2', '3', '3', '2', '2, 'Ris methyl, ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl, sec-butyl, t-butyl, n-pentane, neopentane, n-hexane, 2,2-dimethylbutyl, 3,3-dimethylbutyl, 2-ethyl-butyl, heptane, octane, nonane, decane, undecane, dodecane, pentadecane, hexadecane, or octadecane, each optionally substituted ...

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17-11-2022 дата публикации

Prodrugs of 4'-c-substituted-2-halo-2'-deoxyadenosine nucleosides and methods of making and using the same

Номер: US20220363708A1
Принадлежит: Gilead Sciences Inc

The present disclosure provides prodrugs of 4′-C-substituted-2-halo-2′-deoxyadenoside nucleosides, and compositions, methods, and kits thereof. Such compounds can be useful for treating viral infections including, but not limited to, human immunodeficiency virus.

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02-09-2014 дата публикации

Antiviral compounds

Номер: US8822430B2
Принадлежит: GILEAD PHARMASSET LLC

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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29-05-2018 дата публикации

Antiviral compounds

Номер: US9981955B2
Принадлежит: GILEAD PHARMASSET LLC

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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06-12-2016 дата публикации

Antiviral compounds

Номер: US9511056B2
Принадлежит: GILEAD PHARMASSET LLC

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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19-08-2014 дата публикации

Pyrazolo[1,5-A]pyrimidines for antiviral treatment

Номер: US8809330B2
Принадлежит: Gilead Sciences Inc

The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

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01-05-2018 дата публикации

Pyrazolo[1,5-A]pyrimidines for antiviral treatment

Номер: US9957275B2
Принадлежит: Gilead Sciences Inc

The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

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26-10-2017 дата публикации

Methods for treating zika virus infections

Номер: WO2017184670A2
Принадлежит: Gilead Sciences, Inc.

Provided are methods for treating Zika virus infections by administering a compound of Formula I, Formula II, Formula III, or Formula IV, or combinations thereof.

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19-05-2021 дата публикации

Derivatives of 4,6-diamino-pyrido [3,2-d] pyrimidine as modulators of Toll-like receptors

Номер: ES2826748T3
Принадлежит: Gilead Sciences Inc

Un compuesto, que es **(Ver fórmula)** o una sal farmacéuticamente aceptable del mismo. A compound, which is ** (See formula) ** or a pharmaceutically acceptable salt thereof.

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09-12-2010 дата публикации

Antiviral compounds

Номер: US20100310512A1
Принадлежит: Gilead Sciences Inc

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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30-09-2015 дата публикации

Pyrazolo [1,5-a] pyrimidines as antiviral agents

Номер: AP3417A
Принадлежит: Gilead Sciences Inc

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24-08-2011 дата публикации

Antiviral phosphonate analogs

Номер: EP2359833A1
Принадлежит: Gilead Sciences Inc

The invention is related to phosphorus substituted compounds with antiviral activity, 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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08-08-2017 дата публикации

Methods for treating Filoviridae virus infections

Номер: US9724360B2
Принадлежит: Gilead Sciences Inc

Provided are compounds, methods, and pharmaceutical compositions for treating Filoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula IV: The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.

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04-09-2018 дата публикации

Methods and compounds for treating Paramyxoviridae virus infections

Номер: US10065958B2
Принадлежит: Gilead Sciences Inc

Provided are methods for treating Paramyxoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula I: wherein the 1′ position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are particularly useful for the treatment of Human parainfluenza and Human respiratory syncytial virus infections.

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09-04-2019 дата публикации

Methods for treating arenaviridae and coronaviridae virus infections

Номер: US10251904B2
Принадлежит: Gilead Sciences Inc

Provided are methods for treating Arenaviridae and Coronaviridae virus infections by administering nucleosides and prodrugs thereof, of Formula I: wherein the 1′ position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are particularly useful for the treatment of Lassa virus and Junin virus infections.

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13-01-2005 дата публикации

Therapeutic phosphonate compounds

Номер: WO2005002626A2
Принадлежит: Gilead Sciences, Inc.

The invention is related to phosphorus substituted therapeutic agents, compositions containing such phosphorus substituted agents, and therapeutic methods that include the administration of such phosphorus substituted agents, as well as to processes and intermediates useful for preparing such agents.

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