WO2009064174A1 - Forme polymorphe du ténofovir disoproxil fumarate, son procédé de préparation et son utilisation - Google Patents

Forme polymorphe du ténofovir disoproxil fumarate, son procédé de préparation et son utilisation Download PDF

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Publication number
WO2009064174A1
WO2009064174A1 PCT/NL2008/000250 NL2008000250W WO2009064174A1 WO 2009064174 A1 WO2009064174 A1 WO 2009064174A1 NL 2008000250 W NL2008000250 W NL 2008000250W WO 2009064174 A1 WO2009064174 A1 WO 2009064174A1
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WO
WIPO (PCT)
Prior art keywords
degrees
ult
tenofovir
theta
preferable
Prior art date
Application number
PCT/NL2008/000250
Other languages
English (en)
Inventor
Evanthia Dova
Original Assignee
Ultimorphix Technologies B.V.
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
Application filed by Ultimorphix Technologies B.V. filed Critical Ultimorphix Technologies B.V.
Publication of WO2009064174A1 publication Critical patent/WO2009064174A1/fr

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    • 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 System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne une nouvelle forme cristalline du ténofovir disoproxil fumarate (ténofovir DF), appelée forme ULT-3, des procédés pour la préparer et son utilisation dans des applications pharmaceutiques, en particulier dans des médicaments anti-VIH. La forme cristalline du ténofovir DF peut être utilisée en combinaison avec d'autres médicaments anti-VIH tels que l'éfavirenz et l'emtricitabine.
PCT/NL2008/000250 2007-11-14 2008-11-11 Forme polymorphe du ténofovir disoproxil fumarate, son procédé de préparation et son utilisation WO2009064174A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US98795107P 2007-11-14 2007-11-14
US60/987,951 2007-11-14

Publications (1)

Publication Number Publication Date
WO2009064174A1 true WO2009064174A1 (fr) 2009-05-22

Family

ID=40090465

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/NL2008/000250 WO2009064174A1 (fr) 2007-11-14 2008-11-11 Forme polymorphe du ténofovir disoproxil fumarate, son procédé de préparation et son utilisation

Country Status (1)

Country Link
WO (1) WO2009064174A1 (fr)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012027972A1 (fr) * 2010-08-30 2012-03-08 杭州和素化学技术有限公司 FORME CRISTALLINE α DU TÉNOFOVIR DISOPROXIL FUMARATE, PROCÉDÉ POUR LA PRÉPARER ET SON UTILISATION
CN104288118A (zh) * 2014-07-08 2015-01-21 南京卡文迪许生物工程技术有限公司 富马酸替诺福韦二吡呋酯片剂及其制备方法
WO2015051875A1 (fr) 2013-10-09 2015-04-16 Zentiva, K.S. Sel dihydrogénophosphate de ténofovir disoproxil
US9908908B2 (en) 2012-08-30 2018-03-06 Jiangsu Hansoh Pharmaceutical Co., Ltd. Tenofovir prodrug and pharmaceutical uses thereof

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998004569A1 (fr) * 1996-07-26 1998-02-05 Gilead Sciences, Inc. Analogues de nucleotides
WO2007013085A1 (fr) * 2005-07-26 2007-02-01 Hetero Drugs Limited Procede innovant pour analogues acycliques de nucleotide phosphonate
WO2007013086A1 (fr) * 2005-07-26 2007-02-01 Hetero Drugs Limited Nouveaux polymorphes de tenofovir disoproxil fumarate
CN101066980A (zh) * 2007-05-08 2007-11-07 黑龙江加州国际投资咨询有限公司 富马酸泰诺福韦酯新晶型及其药用制剂
WO2008007392A2 (fr) * 2006-07-12 2008-01-17 Matrix Laboratories Limited Procédé amélioré destiné à préparer du ténofovir
WO2008140302A1 (fr) * 2007-05-14 2008-11-20 Ultimorphix Technologies B.V. Formes polymorphes de ténofovir disoproxil fumarate

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998004569A1 (fr) * 1996-07-26 1998-02-05 Gilead Sciences, Inc. Analogues de nucleotides
WO2007013085A1 (fr) * 2005-07-26 2007-02-01 Hetero Drugs Limited Procede innovant pour analogues acycliques de nucleotide phosphonate
WO2007013086A1 (fr) * 2005-07-26 2007-02-01 Hetero Drugs Limited Nouveaux polymorphes de tenofovir disoproxil fumarate
WO2008007392A2 (fr) * 2006-07-12 2008-01-17 Matrix Laboratories Limited Procédé amélioré destiné à préparer du ténofovir
CN101066980A (zh) * 2007-05-08 2007-11-07 黑龙江加州国际投资咨询有限公司 富马酸泰诺福韦酯新晶型及其药用制剂
WO2008140302A1 (fr) * 2007-05-14 2008-11-20 Ultimorphix Technologies B.V. Formes polymorphes de ténofovir disoproxil fumarate

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
CENTER FOR DRUG EVALUATION AND RESEARCH: "Application Number: 21-356", 2001, XP002507928, Retrieved from the Internet <URL:http://www.fda.gov/cder/foi/nda/2001/21-356_Viread_chemr.pdf> [retrieved on 20081212] *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012027972A1 (fr) * 2010-08-30 2012-03-08 杭州和素化学技术有限公司 FORME CRISTALLINE α DU TÉNOFOVIR DISOPROXIL FUMARATE, PROCÉDÉ POUR LA PRÉPARER ET SON UTILISATION
US9908908B2 (en) 2012-08-30 2018-03-06 Jiangsu Hansoh Pharmaceutical Co., Ltd. Tenofovir prodrug and pharmaceutical uses thereof
WO2015051875A1 (fr) 2013-10-09 2015-04-16 Zentiva, K.S. Sel dihydrogénophosphate de ténofovir disoproxil
CN104288118A (zh) * 2014-07-08 2015-01-21 南京卡文迪许生物工程技术有限公司 富马酸替诺福韦二吡呋酯片剂及其制备方法

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