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WO2006029081A3 - Nucleoside-lipid conjugates, their method of preparation and uses thereof - Google Patents

Nucleoside-lipid conjugates, their method of preparation and uses thereof Download PDF

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Publication number
WO2006029081A3
WO2006029081A3 PCT/US2005/031543 US2005031543W WO2006029081A3 WO 2006029081 A3 WO2006029081 A3 WO 2006029081A3 US 2005031543 W US2005031543 W US 2005031543W WO 2006029081 A3 WO2006029081 A3 WO 2006029081A3
Authority
WO
WIPO (PCT)
Prior art keywords
conjugates
nucleoside
cardiolipin
analogues
lipid conjugates
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US2005/031543
Other languages
French (fr)
Other versions
WO2006029081A2 (en
Inventor
Moghis U Ahmad
Shoukath M Ali
Abdul R Khan
Imran Ahmad
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Neopharm Inc
Original Assignee
Neopharm Inc
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 Neopharm Inc filed Critical Neopharm Inc
Publication of WO2006029081A2 publication Critical patent/WO2006029081A2/en
Anticipated expiration legal-status Critical
Publication of WO2006029081A3 publication Critical patent/WO2006029081A3/en
Ceased legal-status Critical Current

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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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/127—Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention provides methods for synthesizing nucleoside-lipid conjugates having varying fatty acid and alkyl chain lengths with or without unsaturation and their use in the treatment of cancer and viral diseases. More particularly, the invention provides methods for preparing gemcitabine-cardiolipin conjugates, and analogues thereof, cytarabine-cardiolipin conjugates, and analogues thereof. Additionally, the methods of the invention comprise administering a compound of invention as prodrug or a pharmaceutical preparation to combat mammalian diseases, preferably cancer, viral infections and bone disorders.
PCT/US2005/031543 2004-09-02 2005-09-02 Nucleoside-lipid conjugates, their method of preparation and uses thereof Ceased WO2006029081A2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US60661004P 2004-09-02 2004-09-02
US60/606,610 2004-09-02
US63232804P 2004-12-01 2004-12-01
US60/632,328 2004-12-01

Publications (2)

Publication Number Publication Date
WO2006029081A2 WO2006029081A2 (en) 2006-03-16
WO2006029081A3 true WO2006029081A3 (en) 2009-04-23

Family

ID=36036926

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2005/031543 Ceased WO2006029081A2 (en) 2004-09-02 2005-09-02 Nucleoside-lipid conjugates, their method of preparation and uses thereof

Country Status (1)

Country Link
WO (1) WO2006029081A2 (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8956613B2 (en) 2012-11-13 2015-02-17 BoYen Therapeutics, Inc. Gemcitabine prodrugs and uses thereof
US9393256B2 (en) 2011-09-16 2016-07-19 Gilead Pharmasset Llc Methods for treating HCV

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2906207T3 (en) 2003-05-30 2022-04-13 Gilead Pharmasset Llc Modified fluorinated nucleoside analogs
CN101023094B (en) 2004-07-21 2011-05-18 法莫赛特股份有限公司 Preparation of alkyl-substituted 2-deoxy-2-fluoro-d-ribofuranosyl pyrimidines and purines and their derivatives
PT3109244T (en) 2004-09-14 2019-06-04 Gilead Pharmasset Llc Preparation of 2'fluoro-2'-alkyl-substituted or other optionally substituted ribofuranosyl pyrimidines and purines and their derivatives
US7964580B2 (en) 2007-03-30 2011-06-21 Pharmasset, Inc. Nucleoside phosphoramidate prodrugs
US8716263B2 (en) 2008-12-23 2014-05-06 Gilead Pharmasset Llc Synthesis of purine nucleosides
TW201026716A (en) 2008-12-23 2010-07-16 Pharmasset Inc Nucleoside analogs
TW201026715A (en) 2008-12-23 2010-07-16 Pharmasset Inc Nucleoside phosphoramidates
US8618076B2 (en) 2009-05-20 2013-12-31 Gilead Pharmasset Llc Nucleoside phosphoramidates
TWI598358B (en) 2009-05-20 2017-09-11 基利法瑪席特有限責任公司 Nucleoside phosphoramidates
PT3290428T (en) 2010-03-31 2021-12-27 Gilead Pharmasset Llc Tablet comprising crystalline (s)-isopropyl 2-(((s)-(((2r,3r,4r,5r)-5-(2,4-dioxo-3,4-dihydropyrimidin-1 (2h)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoate
WO2012075140A1 (en) 2010-11-30 2012-06-07 Pharmasset, Inc. Compounds
KR20140027987A (en) * 2011-04-08 2014-03-07 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) Methods and pharmaceutical compositions for inhibiting influenza viruses replication
WO2013043529A1 (en) 2011-09-19 2013-03-28 Emory University Bone morphogenetic protein pathway activation, compositions for ossification, and methods related thereto
US8889159B2 (en) 2011-11-29 2014-11-18 Gilead Pharmasset Llc Compositions and methods for treating hepatitis C virus
CN104144682A (en) 2013-01-31 2014-11-12 吉利德法莫赛特有限责任公司 Combination formulation of two antiviral compounds
KR102239196B1 (en) 2013-08-27 2021-04-12 길리애드 파마셋 엘엘씨 Combination formulation of two antiviral compounds
US10463684B2 (en) 2014-01-29 2019-11-05 Board Of Regents, The Uneversety Of Texas System Nucleobase analogue derivatives and their applications
JP2017530976A (en) 2014-10-08 2017-10-19 エピジェネティクス・ファーマ・エルエルシー Vitamin E-Nucleoside Prodrug
US20240042044A1 (en) * 2019-09-10 2024-02-08 Virginia Commonwealth University Polymer drugs for cancer therapies
EP4248949B1 (en) 2022-03-21 2024-08-28 R.G.C.C. Holdings AG Liposomal compositions

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3564089A (en) * 1966-09-29 1971-02-16 Sandra Jean Kiddy Diagnostic reagent for syphilis
US6384019B1 (en) * 1997-01-24 2002-05-07 Norsk Hydro Asa Gemcitabine derivatives

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3564089A (en) * 1966-09-29 1971-02-16 Sandra Jean Kiddy Diagnostic reagent for syphilis
US6384019B1 (en) * 1997-01-24 2002-05-07 Norsk Hydro Asa Gemcitabine derivatives

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
EARLY ET AL.: "Lake Michigan Sponge Phosphatic Metabolite Variations with Habitat: a 31P Nuclear Magnetic Resonance Study", COMPARATIVE BIOCHEMISTRY AND PHYSIOLOGY, PART B: BIOCHEMISTRY & MOLECULAR BIOLOGY, vol. 123B, no. 4, 1999, pages 329 - 343 *
HONG ET AL.: "Nucleoside Conjugates. 15. Synthesis and Biological Activity of Anti-HIV Nucleoside Conjugates of Ether and Thioether Phospholipidsl", JOURNAL OF MEDICINAL CHEMISTRY, vol. 39, 1996, pages 1771 - 1777 *
SCHNEIDER ET AL.: "Oligonucleotides containing flexible nucleoside analogs", JOURNAL OF AMERICAN CHEMICAL SOCIETY, vol. 112, no. 1, 1990, pages 453 - 455 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9393256B2 (en) 2011-09-16 2016-07-19 Gilead Pharmasset Llc Methods for treating HCV
US8956613B2 (en) 2012-11-13 2015-02-17 BoYen Therapeutics, Inc. Gemcitabine prodrugs and uses thereof
US9540410B2 (en) 2012-11-13 2017-01-10 BoYen Therapeutics, Inc. Gemcitabine prodrugs and uses thereof
US9890189B2 (en) 2012-11-13 2018-02-13 BoYen Therapeutics, Inc. Gemcitabine prodrugs and uses thereof

Also Published As

Publication number Publication date
WO2006029081A2 (en) 2006-03-16

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