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PE20160750A1 - Formas cristalinas de los analogos de sofosbuvir antivirales - Google Patents

Formas cristalinas de los analogos de sofosbuvir antivirales

Info

Publication number
PE20160750A1
PE20160750A1 PE2016000813A PE2016000813A PE20160750A1 PE 20160750 A1 PE20160750 A1 PE 20160750A1 PE 2016000813 A PE2016000813 A PE 2016000813A PE 2016000813 A PE2016000813 A PE 2016000813A PE 20160750 A1 PE20160750 A1 PE 20160750A1
Authority
PE
Peru
Prior art keywords
crystalline forms
sofosbuvir
theta
compound
treatment
Prior art date
Application number
PE2016000813A
Other languages
English (en)
Inventor
Mun Sik Seo
Vahid Zia
Fang Wang
Melissa Jean Casteel
Hyuk-Jun Jung
Kathleen Dashner
Bing Shi
Original Assignee
Gilead Pharmasset Llc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
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=PE20160750(A1) "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 PE20160750A1 publication Critical patent/PE20160750A1/es

Links

Classifications

    • 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

Landscapes

  • 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 invencion se refiere a formas 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 de metilo (Compuesto I) caracterizado por un espectro XRPD que comprende picos a 8,6; 9,2; 12,6; 13,5; 14,2; 15,6; 16,0; 17,1; 17,3; 17,5; 18,1; 19,8 y 25,6 °2(theta)+/-0.2°2(theta). Tambien se refiere a una composicion farmaceutica y un metodo de tratamiento. Dichas formas cristalinas son agentes eficaces anti-VHC, siendo utiles en el tratamiento de la hepatitis causada por el virus de la hepatitis C
PE2016000813A 2013-12-23 2014-12-08 Formas cristalinas de los analogos de sofosbuvir antivirales PE20160750A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361920371P 2013-12-23 2013-12-23

Publications (1)

Publication Number Publication Date
PE20160750A1 true PE20160750A1 (es) 2016-07-27

Family

ID=52146765

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016000813A PE20160750A1 (es) 2013-12-23 2014-12-08 Formas cristalinas de los analogos de sofosbuvir antivirales

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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Publication number Priority date Publication date Assignee Title
PL2604620T5 (pl) 2003-05-30 2024-10-14 Gilead Pharmasset Llc Zmodyfikowane fluorowane analogi nukleozydu
US10214553B2 (en) 2014-06-13 2019-02-26 Teva Pharmaceuticals International Gmbh Solid state forms of sofosbuvir
WO2016023906A1 (en) * 2014-08-13 2016-02-18 Sandoz Ag A crystalline form of sofosbuvir
US20190022116A1 (en) 2014-12-26 2019-01-24 Emory University N4-Hydroxycytidine and Derivatives and Anti-Viral Uses Related Thereto
WO2016156512A1 (en) * 2015-04-01 2016-10-06 Sandoz Ag A process for preparing a crystalline form of sofosbuvir
WO2017023714A1 (en) * 2015-08-04 2017-02-09 Merck Sharp & Dohme Corp. Fixed-dose combinations of antiviral compounds
WO2017023716A1 (en) * 2015-08-04 2017-02-09 Merck Sharp & Dohme Corp. Fixed-dose combinations of antiviral compounds
WO2017023715A1 (en) * 2015-08-04 2017-02-09 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
AU2017314148A1 (en) 2016-08-19 2019-02-28 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
CN109952307B (zh) * 2016-12-22 2022-03-25 四川科伦博泰生物医药股份有限公司 4’-硫代-2’-氟代核苷磷酰胺化合物的固体形式及其制备方法和用途
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
WO2019025600A1 (en) 2017-08-03 2019-02-07 Sandoz Ag SOFOSBUVIR HYDRATE
DK3706762T3 (da) 2017-12-07 2024-12-16 Univ Emory N4-hydroxycytidin og derivater og antivirale anvendelser relateret dertil
IL317123A (en) 2018-08-27 2025-01-01 Regeneron Pharma Using Raman Spectroscopy for Downstream Purification
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)
EP4355319A4 (en) 2021-06-17 2025-01-22 ATEA Pharmaceuticals, Inc. BENEFICIAL ANTI-HCV COMBINATION THERAPY

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Also Published As

Publication number Publication date
AU2014370299A1 (en) 2016-06-23
PH12019500372A1 (en) 2020-03-02
CR20160288A (es) 2016-08-31
PH12016501203B1 (en) 2016-08-15
TW201609785A (zh) 2016-03-16
CN105873593A (zh) 2016-08-17
CL2016001509A1 (es) 2016-12-02
US20150175646A1 (en) 2015-06-25
MD20160087A2 (ro) 2016-12-31
ZA201604345B (en) 2017-11-29
AR098929A1 (es) 2016-06-22
DOP2016000141A (es) 2016-07-15
EP3086795A1 (en) 2016-11-02
AP2016009254A0 (en) 2016-06-30
HK1222334A1 (zh) 2017-06-30
BR112016013714A2 (pt) 2017-08-08
EA201691029A1 (ru) 2017-01-30
BR112016013714A8 (pt) 2020-05-26
SG11201604818SA (en) 2016-07-28
WO2015099989A1 (en) 2015-07-02
AU2014370299B2 (en) 2017-11-30
KR20160099710A (ko) 2016-08-22
UY35917A (es) 2015-05-29
MY178102A (en) 2020-10-02
CA2934799A1 (en) 2015-07-02
JP2017503015A (ja) 2017-01-26
MX2019005253A (es) 2019-08-05
CU20160096A7 (es) 2016-11-29
US9340568B2 (en) 2016-05-17
PH12016501203A1 (en) 2016-08-15
IL246066A0 (en) 2016-07-31
MX2016008453A (es) 2016-10-14

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