BR112016013714A8 - compostos cristalinos de análogos de sofosbuvir antivirais, uso dos mesmos e composição farmacêutica - Google Patents

compostos cristalinos de análogos de sofosbuvir antivirais, uso dos mesmos e composição farmacêutica Download PDF

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BR112016013714A8
BR112016013714A8 BR112016013714A BR112016013714A BR112016013714A8 BR 112016013714 A8 BR112016013714 A8 BR 112016013714A8 BR 112016013714 A BR112016013714 A BR 112016013714A BR 112016013714 A BR112016013714 A BR 112016013714A BR 112016013714 A8 BR112016013714 A8 BR 112016013714A8
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sofosbuvir
antiviral
analogs
pharmaceutical composition
crystalline compounds
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BR112016013714A
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English (en)
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BR112016013714A2 (pt
Inventor
Shi Bing
Wang Fang
Jung Hyuk-Jun
Dashner Kathleen
Jean Casteel Melissa
Sik Seo Mun
Zia Vahid
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Gilead Pharmasset Llc
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Application filed by Gilead Pharmasset Llc filed Critical Gilead Pharmasset Llc
Publication of BR112016013714A2 publication Critical patent/BR112016013714A2/pt
Publication of BR112016013714A8 publication Critical patent/BR112016013714A8/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A61K31/7072Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • C07H19/10Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
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  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

as formas sólidas cristalinas do composto anti-hcv 2-((s)-(((2r,3r,4r,5r)-5-(2,4-dioxo-3,4-di-hidropirimidin-1(2h)-il)-4-fluoro-3-hidróxi-4-metiltetraidrofuran-2-il)metóxi)(fenóxi)fosforilamino)propanoato de (s)-isopropila (composto i) são descritas. são também fornecidos, os processos de preparação e os métodos de uso das formas cristalinas.
BR112016013714A 2013-12-23 2014-12-08 compostos cristalinos de análogos de sofosbuvir antivirais, uso dos mesmos e composição farmacêutica BR112016013714A8 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361920371P 2013-12-23 2013-12-23
PCT/US2014/069123 WO2015099989A1 (en) 2013-12-23 2014-12-08 Crystalline forms of antiviral sofosbuvir analogues

Publications (2)

Publication Number Publication Date
BR112016013714A2 BR112016013714A2 (pt) 2017-08-08
BR112016013714A8 true BR112016013714A8 (pt) 2020-05-26

Family

ID=52146765

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112016013714A BR112016013714A8 (pt) 2013-12-23 2014-12-08 compostos cristalinos de análogos de sofosbuvir antivirais, uso dos mesmos e composição farmacêutica

Country Status (27)

Country Link
US (1) US9340568B2 (pt)
EP (1) EP3086795A1 (pt)
JP (1) JP2017503015A (pt)
KR (1) KR20160099710A (pt)
CN (1) CN105873593A (pt)
AP (1) AP2016009254A0 (pt)
AR (1) AR098929A1 (pt)
AU (1) AU2014370299B2 (pt)
BR (1) BR112016013714A8 (pt)
CA (1) CA2934799A1 (pt)
CL (1) CL2016001509A1 (pt)
CR (1) CR20160288A (pt)
CU (1) CU20160096A7 (pt)
DO (1) DOP2016000141A (pt)
EA (1) EA201691029A1 (pt)
HK (1) HK1222334A1 (pt)
IL (1) IL246066A0 (pt)
MD (1) MD20160087A2 (pt)
MX (2) MX2016008453A (pt)
MY (1) MY178102A (pt)
PE (1) PE20160750A1 (pt)
PH (2) PH12019500372A1 (pt)
SG (1) SG11201604818SA (pt)
TW (1) TW201609785A (pt)
UY (1) UY35917A (pt)
WO (1) WO2015099989A1 (pt)
ZA (1) ZA201604345B (pt)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100503628C (zh) 2003-05-30 2009-06-24 法莫赛特股份有限公司 修饰的氟化核苷类似物
EP3154526B1 (en) 2014-06-13 2019-03-06 ratiopharm GmbH Solid state forms of sofosbuvir
WO2016023906A1 (en) * 2014-08-13 2016-02-18 Sandoz Ag A crystalline form of sofosbuvir
KR20230130175A (ko) 2014-12-26 2023-09-11 에모리 유니버시티 N4-하이드록시시티딘, 이와 관련된 유도체 및 이의 항 바이러스적 용도
WO2016156512A1 (en) * 2015-04-01 2016-10-06 Sandoz Ag A process for preparing a crystalline form of sofosbuvir
US20180228828A1 (en) * 2015-08-04 2018-08-16 Merck Sharp & Dohme Corp. Fixed-dose combinations of antiviral compounds
US20180228827A1 (en) * 2015-08-04 2018-08-16 Merck Sharp & Dohme Corp. Fixed-dose combinations of antiviral compounds
US20180228826A1 (en) * 2015-08-04 2018-08-16 Merck Sharp & Dohme Corp. Fixed-dose combinations of antiviral compounds
WO2017029408A1 (en) * 2015-08-20 2017-02-23 Ratiopharm Gmbh Solid state forms of sofosbuvir
EP3430023A1 (en) 2016-03-17 2019-01-23 Mylan Laboratories, Limited Polymorphic forms of sofosbuvir
CZ2016257A3 (cs) 2016-05-05 2017-11-15 Zentiva, K.S. Amorfní forma sofosbuviru, způsob její přípravy a její stabilizace
BR102017011025A2 (pt) 2016-06-02 2017-12-19 Gilead Pharmasset Llc Formulation of combination of three antiviral compounds
US20190185507A1 (en) 2016-08-19 2019-06-20 Sandoz Ag Sofosbuvir Derivatives for the Treatment of Hepatitis C
CN108084237A (zh) * 2016-11-23 2018-05-29 广东东阳光药业有限公司 索非布韦的一水合物及其制备方法
EA201990780A1 (ru) * 2016-12-22 2019-11-29 Твердая форма соединения 4'-тио-2'-фторнуклеозид фосфамида и способ его получения и применения
RU2656228C9 (ru) * 2017-06-13 2019-04-16 Олег Ростиславович Михайлов Слабозакристаллизованная β-модификация (S)-изопропил 2-((S)-(((2R,3R,4R,5R)-5-(2,4-диоксо-3,4-дигидропиримидин-(2Н)-ил)-4-фтор-3-гидрокси-4-метилтетрагидрофуран-2-ил)метокси)-(фенокси)фосфориламино)пропаноата, способ её получения и фармацевтическая композиция на её основе
EP3661944A1 (en) 2017-08-03 2020-06-10 Sandoz AG Sofosbuvir hydrate
AU2018378832B9 (en) 2017-12-07 2021-05-27 Emory University N4-hydroxycytidine and derivatives and anti-viral uses related thereto
CN109517018B (zh) * 2018-12-29 2021-05-04 石药集团中奇制药技术(石家庄)有限公司 一种索磷布韦新晶型及其制备方法
RU2745293C1 (ru) * 2019-12-26 2021-03-23 Общество С Ограниченной Ответственностью "Технология Лекарств" Способ получения кристаллической формы 8 софосбувира (варианты)

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US7964580B2 (en) * 2007-03-30 2011-06-21 Pharmasset, Inc. Nucleoside phosphoramidate prodrugs
EP2857394A1 (en) 2009-05-13 2015-04-08 Gilead Pharmasset LLC Antiviral compounds
TWI576352B (zh) * 2009-05-20 2017-04-01 基利法瑪席特有限責任公司 核苷磷醯胺
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HUE026235T2 (en) * 2010-03-31 2016-06-28 Gilead Pharmasset Llc Crystalline (S) -isopropyl 2 - (((S) - (((2R, 3R, 4R, 5R) -5- (2,4-dioxo-3,4-dihydropyrimidin-1 (2H) -IL) - 4-Fluoro-3-hydroxy-4-methyltetrahydrofuran-2-IL) methoxy) (phenoxy) phosphoryl) amino) propanoate
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Also Published As

Publication number Publication date
BR112016013714A2 (pt) 2017-08-08
UY35917A (es) 2015-05-29
AU2014370299B2 (en) 2017-11-30
AU2014370299A1 (en) 2016-06-23
ZA201604345B (en) 2017-11-29
PE20160750A1 (es) 2016-07-27
SG11201604818SA (en) 2016-07-28
TW201609785A (zh) 2016-03-16
CL2016001509A1 (es) 2016-12-02
KR20160099710A (ko) 2016-08-22
CA2934799A1 (en) 2015-07-02
PH12016501203A1 (en) 2016-08-15
JP2017503015A (ja) 2017-01-26
AP2016009254A0 (en) 2016-06-30
MY178102A (en) 2020-10-02
CN105873593A (zh) 2016-08-17
PH12019500372A1 (en) 2020-03-02
EP3086795A1 (en) 2016-11-02
EA201691029A1 (ru) 2017-01-30
WO2015099989A1 (en) 2015-07-02
PH12016501203B1 (en) 2016-08-15
CR20160288A (es) 2016-08-31
DOP2016000141A (es) 2016-07-15
HK1222334A1 (zh) 2017-06-30
US20150175646A1 (en) 2015-06-25
US9340568B2 (en) 2016-05-17
MD20160087A2 (ro) 2016-12-31
CU20160096A7 (es) 2016-11-29
MX2019005253A (es) 2019-08-05
IL246066A0 (en) 2016-07-31
AR098929A1 (es) 2016-06-22
MX2016008453A (es) 2016-10-14

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