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

Links

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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Biophysics (AREA)
  • Dispersion Chemistry (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (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 (cg-RX-API-DMAC7.html)
EP (1) EP0837630B1 (cg-RX-API-DMAC7.html)
JP (1) JP4301571B2 (cg-RX-API-DMAC7.html)
AT (1) ATE382051T1 (cg-RX-API-DMAC7.html)
AU (1) AU711774B2 (cg-RX-API-DMAC7.html)
CA (1) CA2223989C (cg-RX-API-DMAC7.html)
DE (1) DE69637381T2 (cg-RX-API-DMAC7.html)
ES (1) ES2299178T3 (cg-RX-API-DMAC7.html)
WO (1) WO1996039831A1 (cg-RX-API-DMAC7.html)

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SE9603726D0 (sv) * 1996-10-11 1996-10-11 Astra Ab Novel compounds
WO1999039740A2 (en) * 1998-02-03 1999-08-12 Inex Pharmaceuticals Corporation Sensitizing cells to compounds using lipid-mediated gene and compound delivery
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
CN1414857A (zh) * 1999-12-29 2003-04-30 加利福尼亚大学董事会 耐药性人类免疫缺陷性病毒感染的治疗
EP1460082A1 (en) * 2003-03-19 2004-09-22 Heidelberg Pharma Holding GmbH Phospholipid esters of clofarabine derivatives
EP1838283B1 (en) * 2004-11-03 2008-12-31 Liplasome Pharma A/S Lipid-based drug delivery systems containing unnatural phospholipase a2 degradable lipid derivatives and the therapeutic uses thereof
EP1812012A4 (en) 2004-11-15 2010-02-17 Ceptyr Inc PROTEIN TYROSINE PHOSPHATASE INHIBITOR AND METHOD FOR THEIR USE
ES2401285T3 (es) 2004-12-16 2013-04-18 The Regents Of The University Of California Fármacos con el pulmón como diana
JP2009530318A (ja) * 2006-03-23 2009-08-27 リプラサム ファーマ アー／エス 加水分解時に分子内環化反応を行うホスホリパーゼａ２分解性脂質を含む脂質ベース薬剤送達系
EP2012799B1 (en) * 2006-05-03 2016-08-24 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
CN102137676A (zh) * 2007-12-27 2011-07-27 伊皮芬尼生物科学公司 抗病毒化合物
EP2278963A4 (en) * 2008-01-16 2014-09-17 Anwar Rayan TAXOL DERIVATIVES AND CLOSELY RELATED COMPOUNDS
EP2147910A1 (en) * 2008-07-15 2010-01-27 Pronova BioPharma Norge AS Novel lipid compounds
AU2010244136B2 (en) 2009-05-08 2016-05-12 Pronova Biopharma Norge As Polyunsaturated fatty acids for the treatment of diseases related to cardiovascular, metabolic and inflammatory disease areas
US8884027B2 (en) 2010-10-22 2014-11-11 University Of Rochester Melampomagnolide B derivatives as antileukemic and cytotoxic agents
NZ610705A (en) 2010-11-05 2014-10-31 Pronova Biopharma Norge As Methods of treatment using lipid compounds
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.
US9629860B2 (en) 2013-03-15 2017-04-25 The Regents Of The University Of California Acyclic nucleoside phosphonate diesters
BR112016020233B1 (pt) 2014-03-14 2022-07-19 Alltech Inc. Composições de compostos seleno orgânicos e seus usos
WO2016044281A1 (en) 2014-09-15 2016-03-24 The Regents Of The University Of California Nucleotide analogs
CA2968790A1 (en) 2014-11-26 2016-06-02 Vascular Biogenics Ltd. Oxidized lipids and treatment or prevention of fibrosis
US9771385B2 (en) 2014-11-26 2017-09-26 Vascular Biogenics Ltd. Oxidized lipids
EP4667053A2 (en) 2015-03-06 2025-12-24 ATEA Pharmaceuticals, Inc. Beta-d-2'-deoxy-2'alpha-fluoro-2'-beta-c-substituted-2-modified-n6-substituted purine nucleotides for hcv treatment
BR112017023164A2 (en) 2015-04-28 2018-07-24 Pronova Biopharma Norge As and method of preventing and / or treating non-alcoholic steatohepatitis in an individual in need thereof
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
SMT202200072T1 (it) 2016-09-07 2022-03-21 Atea Pharmaceuticals Inc Nucleotidi purinici 2'-sostituiti-n6-sostituiti per il trattamento dei virus rna
SG11202005007VA (en) 2017-12-06 2020-06-29 Basf As Fatty acid derivatives for treating non-alcoholic steatohepatitis
JP7610208B2 (ja) * 2019-03-22 2025-01-08 インテグレイテッド ナノセラピューティクス インコーポレイテッド 足場部分から調製した脂質結合体
US12049474B2 (en) 2019-08-22 2024-07-30 Emory University Nucleoside prodrugs and uses related thereto
WO2021173713A1 (en) 2020-02-27 2021-09-02 Atea Pharmaceuticals, Inc. Highly active compounds against covid-19
US10874687B1 (en) 2020-02-27 2020-12-29 Atea Pharmaceuticals, Inc. Highly active compounds against COVID-19
ES3015457T3 (en) 2020-08-24 2025-05-05 Gilead Sciences Inc Phospholipid compounds and uses thereof
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
AU2023310177A1 (en) 2022-07-21 2025-03-06 Antiva Biosciences, Inc. Compositions and dosage forms for treatment of hpv infection and hpv-induced neoplasia

Citations (2)

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Publication number Priority date Publication date Assignee Title
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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Patent Citations (2)

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

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