CU20160096A7 - Formas sólidas cristalinas 7 y 8 de (s)-isopropil 2-((s)-(((2r,3r,4r,5r)-5-(2,4-dioxo-3,4-dihidropirimidin-1(2h)-il)-4-fluoro-3-hidroxi-4-metiltetrahidrofuran-2-il)metoxi)(fenoxi)fosforilamino)propanoato de metilo (sofosbuvir) - Google Patents

Formas sólidas cristalinas 7 y 8 de (s)-isopropil 2-((s)-(((2r,3r,4r,5r)-5-(2,4-dioxo-3,4-dihidropirimidin-1(2h)-il)-4-fluoro-3-hidroxi-4-metiltetrahidrofuran-2-il)metoxi)(fenoxi)fosforilamino)propanoato de metilo (sofosbuvir)

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Publication number
CU20160096A7
CU20160096A7 CUP2016000096A CU20160096A CU20160096A7 CU 20160096 A7 CU20160096 A7 CU 20160096A7 CU P2016000096 A CUP2016000096 A CU P2016000096A CU 20160096 A CU20160096 A CU 20160096A CU 20160096 A7 CU20160096 A7 CU 20160096A7
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CU
Cuba
Prior art keywords
dioxo
fluoro
solid forms
phosphorilamine
methylethydrrofuran
Prior art date
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CUP2016000096A
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English (en)
Inventor
Melissa Jean Casteel
Kathleen Dashner
Fang Wang
Vahid Zia
Hyuk-Jun Jung
Mun Sik Seo
Bing Shi
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Gilead Pharmasset Llc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=52146765&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CU20160096(A7) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Gilead Pharmasset Llc filed Critical Gilead Pharmasset Llc
Publication of CU20160096A7 publication Critical patent/CU20160096A7/es

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds 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
    • A61K31/7064—Compounds 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds 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
    • A61K31/7064—Compounds 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
    • A61K31/7068—Compounds 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds 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
    • A61K31/7064—Compounds 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
    • A61K31/7068—Compounds 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
    • A61K31/7072—Compounds 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic 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
    • C07F9/65586—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline 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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invención pertenece al sector de la industria farmacéutica, especialmente al desarollo de formas sólidas cristalinas del compuesto (S)-isopropil 2-((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihidropirimidin-1(2H)-il)-4-fluoro-3-hidroxi-4-metiltetrahidrofuran-2-il)metoxi)(fenoxi)fosforilamino)propanoato (Compuesto I) las cuales son útiles para limitar el establecimiento y la progresión de la infección por VHC. ESPACIO PARA FÓRMULA También se proporcionan procesos de fabricación y métodos de uso de las formas cristalinas, útiles en el tratamiento de VHC.
CUP2016000096A 2013-12-23 2016-06-22 Formas sólidas cristalinas 7 y 8 de (s)-isopropil 2-((s)-(((2r,3r,4r,5r)-5-(2,4-dioxo-3,4-dihidropirimidin-1(2h)-il)-4-fluoro-3-hidroxi-4-metiltetrahidrofuran-2-il)metoxi)(fenoxi)fosforilamino)propanoato de metilo (sofosbuvir) CU20160096A7 (es)

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 (1)

Publication Number Publication Date
CU20160096A7 true CU20160096A7 (es) 2016-11-29

Family

ID=52146765

Family Applications (1)

Application Number Title Priority Date Filing Date
CUP2016000096A CU20160096A7 (es) 2013-12-23 2016-06-22 Formas sólidas cristalinas 7 y 8 de (s)-isopropil 2-((s)-(((2r,3r,4r,5r)-5-(2,4-dioxo-3,4-dihidropirimidin-1(2h)-il)-4-fluoro-3-hidroxi-4-metiltetrahidrofuran-2-il)metoxi)(fenoxi)fosforilamino)propanoato de metilo (sofosbuvir)

Country Status (27)

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

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US7429572B2 (en) 2003-05-30 2008-09-30 Pharmasset, Inc. Modified fluorinated nucleoside analogues
CA2988393C (en) 2014-06-13 2023-08-22 Ratiopharm Gmbh Solid state forms of sofosbuvir
WO2016023906A1 (en) * 2014-08-13 2016-02-18 Sandoz Ag A crystalline form of sofosbuvir
HRP20211456T1 (hr) 2014-12-26 2021-12-24 Emory University Protuvirusni derivati n4-hidroksicitidina
WO2016156512A1 (en) * 2015-04-01 2016-10-06 Sandoz Ag A process for preparing a crystalline form of sofosbuvir
WO2017023716A1 (en) * 2015-08-04 2017-02-09 Merck Sharp & Dohme Corp. Fixed-dose combinations of antiviral compounds
WO2017023714A1 (en) * 2015-08-04 2017-02-09 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
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
CN109843900A (zh) 2016-08-19 2019-06-04 桑多斯股份公司 治疗丙型肝炎的索非布韦衍生物
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
CA3041420A1 (en) * 2016-12-22 2018-06-28 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Solid form of 4'-thio-2'-fluoronucleoside phosphamide compound and preparation method therefor and use thereof
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
KR102248165B1 (ko) 2017-12-07 2021-05-06 에모리 유니버시티 N4-하이드록시사이티딘 및 유도체 및 이와 관련된 항-바이러스 용도
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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Also Published As

Publication number Publication date
CA2934799A1 (en) 2015-07-02
BR112016013714A2 (pt) 2017-08-08
MX2016008453A (es) 2016-10-14
UY35917A (es) 2015-05-29
AR098929A1 (es) 2016-06-22
MD20160087A2 (ro) 2016-12-31
KR20160099710A (ko) 2016-08-22
EP3086795A1 (en) 2016-11-02
TW201609785A (zh) 2016-03-16
HK1222334A1 (zh) 2017-06-30
US20150175646A1 (en) 2015-06-25
IL246066A0 (en) 2016-07-31
AU2014370299A1 (en) 2016-06-23
JP2017503015A (ja) 2017-01-26
CR20160288A (es) 2016-08-31
AP2016009254A0 (en) 2016-06-30
EA201691029A1 (ru) 2017-01-30
PH12016501203B1 (en) 2016-08-15
BR112016013714A8 (pt) 2020-05-26
CL2016001509A1 (es) 2016-12-02
SG11201604818SA (en) 2016-07-28
MY178102A (en) 2020-10-02
WO2015099989A1 (en) 2015-07-02
MX2019005253A (es) 2019-08-05
US9340568B2 (en) 2016-05-17
PH12019500372A1 (en) 2020-03-02
ZA201604345B (en) 2017-11-29
AU2014370299B2 (en) 2017-11-30
CN105873593A (zh) 2016-08-17
PE20160750A1 (es) 2016-07-27
PH12016501203A1 (en) 2016-08-15
DOP2016000141A (es) 2016-07-15

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