DE69637381T2 - Prodrugs von pharmazeutika mit erhöhter bioverfügbarheit - Google Patents

Prodrugs von pharmazeutika mit erhöhter bioverfügbarheit Download PDF

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Publication number
DE69637381T2
DE69637381T2 DE69637381T DE69637381T DE69637381T2 DE 69637381 T2 DE69637381 T2 DE 69637381T2 DE 69637381 T DE69637381 T DE 69637381T DE 69637381 T DE69637381 T DE 69637381T DE 69637381 T2 DE69637381 T2 DE 69637381T2
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DE
Germany
Prior art keywords
octadecyl
group
pfa
mixture
mmol
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 - Lifetime
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DE69637381T
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German (de)
English (en)
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DE69637381D1 (de
Inventor
Karl Y. Del Mar Hostetler
Ganesh D. San Diego KINI
James R. San Diego BEADLE
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Individual
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Publication of DE69637381D1 publication Critical patent/DE69637381D1/de
Application granted granted Critical
Publication of DE69637381T2 publication Critical patent/DE69637381T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/127Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
    • A61K9/1271Non-conventional liposomes, e.g. PEGylated liposomes or liposomes coated or grafted with polymers
    • A61K9/1272Non-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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/06Phosphorus compounds without P—C bonds
    • C07F9/08Esters of oxyacids of phosphorus
    • C07F9/09Esters of phosphoric acids
    • C07F9/098Esters of polyphosphoric acids or anhydrides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/06Phosphorus compounds without P—C bonds
    • C07F9/08Esters of oxyacids of phosphorus
    • C07F9/09Esters of phosphoric acids
    • C07F9/10Phosphatides, e.g. lecithin
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40Esters thereof
    • C07F9/4003Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4006Esters of acyclic acids which can have further substituents on alkyl
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40Esters thereof
    • C07F9/4003Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4062Esters of acids containing the structure -C(=X)-P(=X)(XR)2 or NC-P(=X)(XR)2, (X = O, S, Se)
    • C07F9/4065Esters 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)
DE69637381T 1995-06-07 1996-06-07 Prodrugs von pharmazeutika mit erhöhter bioverfügbarheit Expired - Lifetime DE69637381T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US487081 1983-04-27
US08/487,081 US7517858B1 (en) 1995-06-07 1995-06-07 Prodrugs of pharmaceuticals with improved bioavailability
PCT/US1996/010054 WO1996039831A1 (en) 1995-06-07 1996-06-07 Prodrugs of pharmaceuticals with improved bioavailability

Publications (2)

Publication Number Publication Date
DE69637381D1 DE69637381D1 (de) 2008-02-07
DE69637381T2 true DE69637381T2 (de) 2008-12-11

Family

ID=23934330

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69637381T Expired - Lifetime DE69637381T2 (de) 1995-06-07 1996-06-07 Prodrugs von pharmazeutika mit erhöhter bioverfügbarheit

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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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
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ES3015457T3 (en) 2020-08-24 2025-05-05 Gilead Sciences Inc Phospholipid compounds and uses thereof
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Also Published As

Publication number Publication date
DE69637381D1 (de) 2008-02-07
CA2223989C (en) 2010-11-23
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
AU711774B2 (en) 1999-10-21

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