AU711774B2 - Prodrugs of pharmaceuticals with improved bioavailability - Google Patents

Prodrugs of pharmaceuticals with improved bioavailability Download PDF

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Publication number
AU711774B2
AU711774B2 AU61717/96A AU6171796A AU711774B2 AU 711774 B2 AU711774 B2 AU 711774B2 AU 61717/96 A AU61717/96 A AU 61717/96A AU 6171796 A AU6171796 A AU 6171796A AU 711774 B2 AU711774 B2 AU 711774B2
Authority
AU
Australia
Prior art keywords
compound according
group
alkyl
acyl
octadecyl
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.)
Expired
Application number
AU61717/96A
Other languages
English (en)
Other versions
AU6171796A (en
Inventor
James R Beadle
Karl Y. Hostetler
Ganesh D. Kini
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.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of AU6171796A publication Critical patent/AU6171796A/en
Assigned to HOSTETLER, KARL Y. reassignment HOSTETLER, KARL Y. Alteration of Name(s) of Applicant(s) under S113 Assignors: REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE
Application granted granted Critical
Publication of AU711774B2 publication Critical patent/AU711774B2/en
Anticipated expiration legal-status Critical
Expired legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • 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
    • A61K9/1271—Non-conventional liposomes, e.g. PEGylated liposomes or liposomes coated or grafted with polymers
    • A61K9/1272—Non-conventional liposomes, e.g. PEGylated liposomes or liposomes coated or grafted with polymers comprising non-phosphatidyl surfactants as bilayer-forming substances, e.g. cationic lipids or non-phosphatidyl liposomes coated or grafted with polymers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/08—Esters of oxyacids of phosphorus
    • C07F9/09—Esters of phosphoric acids
    • C07F9/098—Esters of polyphosphoric acids or anhydrides
    • 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
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/08—Esters of oxyacids of phosphorus
    • C07F9/09—Esters of phosphoric acids
    • C07F9/10—Phosphatides, e.g. lecithin
    • 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
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4006—Esters of acyclic acids which can have further substituents on alkyl
    • 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
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4062—Esters of acids containing the structure -C(=X)-P(=X)(XR)2 or NC-P(=X)(XR)2, (X = O, S, Se)
    • C07F9/4065—Esters of acids containing the structure -C(=X)-P(=X)(XR)2, (X = O, S, Se)

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Dispersion Chemistry (AREA)
  • Biophysics (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AU61717/96A 1995-06-07 1996-06-07 Prodrugs of pharmaceuticals with improved bioavailability Expired AU711774B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US08/487,081 US7517858B1 (en) 1995-06-07 1995-06-07 Prodrugs of pharmaceuticals with improved bioavailability
US08/487081 1995-06-07
PCT/US1996/010054 WO1996039831A1 (en) 1995-06-07 1996-06-07 Prodrugs of pharmaceuticals with improved bioavailability

Publications (2)

Publication Number Publication Date
AU6171796A AU6171796A (en) 1996-12-30
AU711774B2 true AU711774B2 (en) 1999-10-21

Family

ID=23934330

Family Applications (1)

Application Number Title Priority Date Filing Date
AU61717/96A Expired AU711774B2 (en) 1995-06-07 1996-06-07 Prodrugs of pharmaceuticals with improved bioavailability

Country Status (9)

Country Link
US (1) US7517858B1 (2)
EP (1) EP0837630B1 (2)
JP (1) JP4301571B2 (2)
AT (1) ATE382051T1 (2)
AU (1) AU711774B2 (2)
CA (1) CA2223989C (2)
DE (1) DE69637381T2 (2)
ES (1) ES2299178T3 (2)
WO (1) WO1996039831A1 (2)

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SE9603726D0 (sv) * 1996-10-11 1996-10-11 Astra Ab Novel compounds
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US6410328B1 (en) * 1998-02-03 2002-06-25 Protiva Biotherapeutics Inc. Sensitizing cells to compounds using lipid-mediated gene and compound delivery
IL131887A0 (en) * 1999-09-14 2001-03-19 Dpharm Ltd Phospholipid prodrugs of anti-proliferative drugs
CA2395430A1 (en) * 1999-12-29 2001-07-05 The Regents Of The University Of California Treatment of drug-resistant human immunodeficiency virus infection
EP1460082A1 (en) * 2003-03-19 2004-09-22 Heidelberg Pharma Holding GmbH Phospholipid esters of clofarabine derivatives
ATE418966T1 (de) * 2004-11-03 2009-01-15 Liplasome Pharma As Arzneimittelabgabesysteme auf lipidbasis mit unnatürlichen phospholipase-a2-abbaubaren lipid- derivaten und ihre therapeutische verwendung
AU2005306612B2 (en) 2004-11-15 2010-12-16 Ceptyr, Inc. Protein tyrosine phosphatase inhibitors and methods of use thereof
ES2401285T3 (es) * 2004-12-16 2013-04-18 The Regents Of The University Of California Fármacos con el pulmón como diana
CA2647779A1 (en) * 2006-03-23 2007-09-27 Liplasome Pharma A/S Lipid based drug delivery systems comprising phospholipase a2 degradable lipids that perform an intramolecular cyclization reaction upon hydrolysis
WO2007130783A2 (en) * 2006-05-03 2007-11-15 Chimerix, Inc. Metabolically stable alkoxyalkyl esters of antiviral or antiproliferative phosphonates, nucleoside phosphonates and nucleoside phosphates
WO2009061208A1 (en) * 2007-11-09 2009-05-14 Pronova Biopharma Norge As Lipid compounds for use in cosmetic products, as food supplement or as a medicament
EP2070938A1 (en) * 2007-12-13 2009-06-17 Heidelberg Pharma AG Clofarabine dietherphospholipid derivatives
EP2234623A4 (en) * 2007-12-27 2012-03-28 Epiphany Biosciences ANTIVIRAL CONNECTIONS
WO2009090614A2 (en) * 2008-01-16 2009-07-23 Anwar Rayan Derivatives of taxol and closely related compounds
EP2147910A1 (en) * 2008-07-15 2010-01-27 Pronova BioPharma Norge AS Novel lipid compounds
BRPI1015120B8 (pt) 2009-05-08 2022-02-15 Basf As Composto lipídico alfa-substituídos, derivados de ácidos graxos beta-oxo poli-insaturados, composição farmacêutica e lipídica e métodos para produzir composto lipídico e ácido 2-((5z,8z,11z,14z,17z)-icosa-5,8,11,14,17-pentaeniloxi)butanóico
US8884027B2 (en) 2010-10-22 2014-11-11 University Of Rochester Melampomagnolide B derivatives as antileukemic and cytotoxic agents
ES2618604T3 (es) 2010-11-05 2017-06-21 Pronova Biopharma Norge As Métodos de tratamiento usando compuestos lipídicos
MX377728B (es) 2013-02-28 2025-03-11 Pronova Biopharma Norge As Composición que comprende un compuesto lípido, un triglicerido y un tensioactivo, y métodos de uso de la misma.
SG10201800188SA (en) 2013-03-15 2018-02-27 Univ California Acyclic nucleoside phosphonate diesters
DK3116511T3 (da) 2014-03-14 2020-11-23 Alltech Inc Sammensætninger af selenoorganiske forbindelser og fremgangsmåder til anvendelse deraf
CN111808136B (zh) 2014-09-15 2024-06-11 加利福尼亚大学董事会 核苷酸类似物
EP3223824B1 (en) 2014-11-26 2021-01-06 Vascular Biogenics Ltd. Oxidized lipids and treatment or prevention of fibrosis
US9771385B2 (en) 2014-11-26 2017-09-26 Vascular Biogenics Ltd. Oxidized lipids
CA3182565A1 (en) 2015-03-06 2016-09-15 Atea Pharmaceuticals, Inc. .beta.-d-2'-deoxy-2'-.alpha.-fluoro-2'-.beta.-c-substituted-2-modified-n6-substituted purine nucleotides for hcv treatment
ES2980790T3 (es) 2015-04-28 2024-10-03 Basf As Acidos grasos estructuralmente mejorados que contienen azufre para su uso en el tratamiento de la esteatohepatitis no alcohólica
WO2017048252A1 (en) 2015-09-15 2017-03-23 Alltech, Inc. Compositions of selenoorganic compounds and methods of use thereof
EP3350191B9 (en) 2015-09-15 2021-12-22 The Regents of the University of California Nucleotide analogs
WO2018013937A1 (en) 2016-07-14 2018-01-18 Atea Pharmaceuticals, Inc. Beta-d-2'-deoxy-2'-alpha-fluoro-2'-beta-c-substituted-4'-fluoro-n6-substituted-6-amino-2-substituted purine nucleotides for the treatment of hepatitis c virus infection
WO2018048937A1 (en) 2016-09-07 2018-03-15 Atea Pharmaceuticals, Inc. 2'-substituted-n6-substituted purine nucleotides for rna virus treatment
IL308604B2 (en) 2017-12-06 2025-08-01 Basf As Fatty acid derivatives for treating non-alcoholic steatohepatitis
US20220226480A1 (en) * 2019-03-22 2022-07-21 Integrated Nanotherapeutics Inc. Lipid conjugate prepared from scaffold moiety
WO2021035214A1 (en) 2019-08-22 2021-02-25 Emory University Nucleoside prodrugs and uses related thereto
US10874687B1 (en) 2020-02-27 2020-12-29 Atea Pharmaceuticals, Inc. Highly active compounds against COVID-19
WO2021173713A1 (en) 2020-02-27 2021-09-02 Atea Pharmaceuticals, Inc. Highly active compounds against covid-19
IL300412A (en) 2020-08-24 2023-04-01 Gilead Sciences Inc Phospholipid compounds and their uses
TW202344257A (zh) 2020-10-16 2023-11-16 美商基利科學股份有限公司 磷脂化合物及其用途
KR20250052378A (ko) 2022-07-21 2025-04-18 안티바 바이오사이언시즈, 인크. Hpv 감염 및 hpv-유도 신생물의 치료를 위한 조성물 및 투여 형태

Citations (2)

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US5194654A (en) * 1989-11-22 1993-03-16 Vical, Inc. Lipid derivatives of phosphonoacids for liposomal incorporation and method of use
US5411947A (en) * 1989-06-28 1995-05-02 Vestar, Inc. Method of converting a drug to an orally available form by covalently bonding a lipid to the drug

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US5411947A (en) * 1989-06-28 1995-05-02 Vestar, Inc. Method of converting a drug to an orally available form by covalently bonding a lipid to the drug
US5194654A (en) * 1989-11-22 1993-03-16 Vical, Inc. Lipid derivatives of phosphonoacids for liposomal incorporation and method of use

Also Published As

Publication number Publication date
EP0837630A4 (en) 1998-11-25
ES2299178T3 (es) 2008-05-16
DE69637381T2 (de) 2008-12-11
EP0837630A1 (en) 1998-04-29
JPH11512078A (ja) 1999-10-19
CA2223989C (en) 2010-11-23
AU6171796A (en) 1996-12-30
EP0837630B1 (en) 2007-12-26
DE69637381D1 (de) 2008-02-07
JP4301571B2 (ja) 2009-07-22
CA2223989A1 (en) 1996-12-19
ATE382051T1 (de) 2008-01-15
WO1996039831A1 (en) 1996-12-19
US7517858B1 (en) 2009-04-14

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