WO2010142761A1 - Succinate de ténofovir disoproxil - Google Patents

Succinate de ténofovir disoproxil Download PDF

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Publication number
WO2010142761A1
WO2010142761A1 PCT/EP2010/058146 EP2010058146W WO2010142761A1 WO 2010142761 A1 WO2010142761 A1 WO 2010142761A1 EP 2010058146 W EP2010058146 W EP 2010058146W WO 2010142761 A1 WO2010142761 A1 WO 2010142761A1
Authority
WO
WIPO (PCT)
Prior art keywords
succinate
tenofovir disoproxil
tenofovir
degrees
disoproxil
Prior art date
Application number
PCT/EP2010/058146
Other languages
English (en)
Inventor
Evanthia Dova
Samir Kulkarni
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.
Priority to EP10724845A priority Critical patent/EP2440560A1/fr
Publication of WO2010142761A1 publication Critical patent/WO2010142761A1/fr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/536—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
    • 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
    • A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • A61K31/685—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/10—Succinic acid
    • 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

Landscapes

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

Abstract

La présente invention a pour objet un succinate de Ténofovir disoproxil, des procédés pour sa préparation et son utilisation dans des applications pharmaceutiques, en particulier dans des médicaments anti-VIH. Le succinate de Ténofovir disoproxil peut être utilisé en combinaison avec d'autres médicaments anti-VIH tels que l'Efavirenz et l'Emtricitabine. La présente invention concerne aussi des procédés pour le traitement du VIH au moyen de médicaments à base de succinate de Ténofovir disoproxil tels que l'Efavirenz et l'Emtricitabine.
PCT/EP2010/058146 2009-06-10 2010-06-10 Succinate de ténofovir disoproxil WO2010142761A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP10724845A EP2440560A1 (fr) 2009-06-10 2010-06-10 Succinate de ténofovir disoproxil

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US18573509P 2009-06-10 2009-06-10
US61/185,735 2009-06-10

Publications (1)

Publication Number Publication Date
WO2010142761A1 true WO2010142761A1 (fr) 2010-12-16

Family

ID=42648080

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2010/058146 WO2010142761A1 (fr) 2009-06-10 2010-06-10 Succinate de ténofovir disoproxil

Country Status (2)

Country Link
EP (1) EP2440560A1 (fr)
WO (1) WO2010142761A1 (fr)

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110009368A1 (en) * 2007-12-12 2011-01-13 Ultimorphix Technologies B.V. Solid forms of tenofovir disoproxil
WO2015051875A1 (fr) 2013-10-09 2015-04-16 Zentiva, K.S. Sel dihydrogénophosphate de ténofovir disoproxil
KR20160003532A (ko) 2014-07-01 2016-01-11 한미약품 주식회사 테노포비어 디소프록실 인산염과, 비금속염 붕해제 및 비금속염 활택제를 포함하는 약학 조성물
US9908908B2 (en) 2012-08-30 2018-03-06 Jiangsu Hansoh Pharmaceutical Co., Ltd. Tenofovir prodrug and pharmaceutical uses thereof
US20220016140A1 (en) * 2006-02-03 2022-01-20 The United States Of America, As Represented By The Secretary, Department Of Health And Human Servic Inhibition of hiv infection through chemoprophylaxis
US11337989B2 (en) 2013-12-19 2022-05-24 Evofem, Inc. Compositions and methods for inhibiting inflammation and diseases using an alginic acid-based antimicrobial compound
US11419835B2 (en) 2016-10-04 2022-08-23 Evofem, Inc. Method of treatment and prevention of bacterial vaginosis
US11439610B2 (en) 2012-06-13 2022-09-13 Evofem, Inc. Compositions and methods for enhancing the efficacy of contraceptive microbicides

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6043230A (en) * 1996-07-26 2000-03-28 Gilead Sciences, Inc. Antiviral phosphonomethoxy nucleotide analogs having increased oral bioavailability
WO2007013086A1 (fr) * 2005-07-26 2007-02-01 Hetero Drugs Limited Nouveaux polymorphes de tenofovir disoproxil fumarate
WO2009074351A2 (fr) * 2007-12-12 2009-06-18 Ultimorphix Technologies B.V. Formes solides de ténofovir disoproxil

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6043230A (en) * 1996-07-26 2000-03-28 Gilead Sciences, Inc. Antiviral phosphonomethoxy nucleotide analogs having increased oral bioavailability
WO2007013086A1 (fr) * 2005-07-26 2007-02-01 Hetero Drugs Limited Nouveaux polymorphes de tenofovir disoproxil fumarate
WO2009074351A2 (fr) * 2007-12-12 2009-06-18 Ultimorphix Technologies B.V. Formes solides de ténofovir disoproxil

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20220016140A1 (en) * 2006-02-03 2022-01-20 The United States Of America, As Represented By The Secretary, Department Of Health And Human Servic Inhibition of hiv infection through chemoprophylaxis
US20110009368A1 (en) * 2007-12-12 2011-01-13 Ultimorphix Technologies B.V. Solid forms of tenofovir disoproxil
US11439610B2 (en) 2012-06-13 2022-09-13 Evofem, Inc. Compositions and methods for enhancing the efficacy of contraceptive microbicides
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
US11337989B2 (en) 2013-12-19 2022-05-24 Evofem, Inc. Compositions and methods for inhibiting inflammation and diseases using an alginic acid-based antimicrobial compound
KR20160003532A (ko) 2014-07-01 2016-01-11 한미약품 주식회사 테노포비어 디소프록실 인산염과, 비금속염 붕해제 및 비금속염 활택제를 포함하는 약학 조성물
US11419835B2 (en) 2016-10-04 2022-08-23 Evofem, Inc. Method of treatment and prevention of bacterial vaginosis

Also Published As

Publication number Publication date
EP2440560A1 (fr) 2012-04-18

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