EP0577725A4 - Targeted drug delivery via mixed phosphate derivatives - Google Patents

Targeted drug delivery via mixed phosphate derivatives

Info

Publication number
EP0577725A4
EP0577725A4 EP92909373A EP92909373A EP0577725A4 EP 0577725 A4 EP0577725 A4 EP 0577725A4 EP 92909373 A EP92909373 A EP 92909373A EP 92909373 A EP92909373 A EP 92909373A EP 0577725 A4 EP0577725 A4 EP 0577725A4
Authority
EP
European Patent Office
Prior art keywords
drug delivery
targeted drug
delivery via
phosphate derivatives
mixed phosphate
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.)
Withdrawn
Application number
EP92909373A
Other versions
EP0577725A1 (en
Inventor
Nicholas S Bodor
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.)
University of Florida
Original Assignee
University of Florida
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 University of Florida filed Critical University of Florida
Publication of EP0577725A1 publication Critical patent/EP0577725A1/en
Publication of EP0577725A4 publication Critical patent/EP0577725A4/en
Withdrawn legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • C07H19/10Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07F9/091Esters of phosphoric acids with hydroxyalkyl compounds with 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
    • C07F9/06Phosphorus compounds without P—C bonds
    • C07F9/08Esters of oxyacids of phosphorus
    • C07F9/09Esters of phosphoric acids
    • C07F9/094Esters of phosphoric acids with arylalkanols
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/5532Seven-(or more) membered rings
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/5532Seven-(or more) membered rings
    • C07F9/5535Seven-(or more) membered rings condensed with carbocyclic rings or ring systems
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/5537Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom the heteroring containing the structure -C(=O)-N-C(=O)- (both carbon atoms belong to the heteroring)
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572Five-membered rings
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572Five-membered rings
    • C07F9/5728Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • C07F9/5765Six-membered rings condensed with carbocyclic rings or carbocyclic ring systems
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • C07F9/59Hydrogenated pyridine rings
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503Five-membered rings
    • C07F9/6506Five-membered rings having the nitrogen atoms in positions 1 and 3
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503Five-membered rings
    • C07F9/6506Five-membered rings having the nitrogen atoms in positions 1 and 3
    • C07F9/65068Five-membered rings having the nitrogen atoms in positions 1 and 3 condensed with carbocyclic rings or carbocyclic ring systems
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509Six-membered rings
    • C07F9/650952Six-membered rings having the nitrogen atoms in the positions 1 and 4
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509Six-membered rings
    • C07F9/6512Six-membered rings having the nitrogen atoms in positions 1 and 3
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6536Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
    • C07F9/6544Six-membered rings
    • C07F9/6547Six-membered rings condensed with carbocyclic rings or carbocyclic ring systems
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic 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
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic 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
    • C07F9/65611Heterocyclic 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 (X = CH2, O, S, NH) optionally with an additional double bond and/or substituents, e.g. penicillins and analogs
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic 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
    • C07F9/65613Heterocyclic 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 (X = CH2, O, S, NH) optionally with an additional double bond and/or substituents, e.g. cephalosporins and analogs
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic 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
    • C07F9/65616Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16Purine radicals
    • C07H19/20Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J51/00Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J63/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/008Expansion of ring D by one atom, e.g. D homo steroids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring
    • C07J71/0026Oxygen-containing hetero ring cyclic ketals
    • C07J71/0031Oxygen-containing hetero ring cyclic ketals at positions 16, 17

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
EP92909373A 1991-03-29 1992-03-27 Targeted drug delivery via mixed phosphate derivatives Withdrawn EP0577725A4 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US67730491A 1991-03-29 1991-03-29
US677304 1991-03-29

Publications (2)

Publication Number Publication Date
EP0577725A1 EP0577725A1 (en) 1994-01-12
EP0577725A4 true EP0577725A4 (en) 1996-04-17

Family

ID=24718156

Family Applications (1)

Application Number Title Priority Date Filing Date
EP92909373A Withdrawn EP0577725A4 (en) 1991-03-29 1992-03-27 Targeted drug delivery via mixed phosphate derivatives

Country Status (4)

Country Link
EP (1) EP0577725A4 (en)
JP (1) JPH06510020A (en)
CA (1) CA2108041A1 (en)
WO (1) WO1992017185A1 (en)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL105244A (en) * 1993-03-31 2003-07-31 Dpharm Ltd Prodrugs with enhanced penetration into cells
US20100173864A1 (en) 2004-03-29 2010-07-08 Cheng Jin Q Compositions including triciribine and one or more platinum compounds and methods of use thereof
US20100009928A1 (en) 2004-03-29 2010-01-14 Cheng Jin Q Compositions including triciribine and taxanes and methods of use thereof
ES2629682T3 (en) 2004-03-29 2017-08-14 University Of South Florida Effective treatment of tumors and cancer with triciribin phosphate
US20100009929A1 (en) 2004-03-29 2010-01-14 Cheng Jin Q Compositions including triciribine and bortezomib and derivatives thereof and methods of use thereof
US20100028339A1 (en) 2004-03-29 2010-02-04 Cheng Jin Q Compositions including triciribine and trastuzumab and methods of use thereof
US20110008327A1 (en) 2004-03-29 2011-01-13 Cheng Jin Q Compositions including triciribine and epidermal growth factor receptor inhibitor compounds or salts thereof and methods of use thereof
JP3849124B1 (en) 2004-12-03 2006-11-22 グリーンアーム株式会社 Method for continuously regenerating asphalt mixture layer on pavement on road and self-propelled vehicle system therefor
CN108026136A (en) 2015-08-06 2018-05-11 奇默里克斯公司 Pyrrolopyrimidine nucleosides as useful antivirotic and the like
CN106365998A (en) * 2016-08-19 2017-02-01 陕西思尔生物科技有限公司 Preparation method of iodomethyl pivalate
US11111264B2 (en) 2017-09-21 2021-09-07 Chimerix, Inc. Morphic forms of 4-amino-7-(3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-2-methyl-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide and uses thereof

Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0112130A1 (en) * 1982-12-09 1984-06-27 Teva Pharmaceutical Industries Limited Ethoxycarbonyloxy ethyl esters of non-steroidal anti-inflammatory carboxylic acids, their preparation and use
EP0202703A1 (en) * 1985-05-15 1986-11-26 N.V. Gantax Pharmaceutica Pharmaceutical compositions of the prodrug type, a process for the preparation thereof, a process for the preparation of them as prodrug functioning compounds and compounds obtained therein
EP0271983A1 (en) * 1986-10-31 1988-06-22 Pfizer Inc. Transdermal flux enhancing compositions
EP0291873A2 (en) * 1987-05-22 1988-11-23 Hoechst Aktiengesellschaft Method to determine the anti-aggregatory activity of vasoactive substances, especially phosphodiesterase and/or cyclooxygenase inhibitors
EP0331382A2 (en) * 1988-02-29 1989-09-06 Pfizer Inc. Transdermal flux enhancing compositions
EP0335164A2 (en) * 1988-03-31 1989-10-04 Merckle GmbH Ester derivatives of neopentanol, process for their preparation and their use as medicines
WO1990008155A1 (en) * 1989-01-23 1990-07-26 Board Of Regents, The University Of Texas System Biologically reversible phosphate and phosphonate protective groups
EP0407815A2 (en) * 1989-07-10 1991-01-16 Eisai Co., Ltd. Polyprenyl compound composition for soft capsules
EP0452908A2 (en) * 1990-04-19 1991-10-23 Abbott Laboratories Lipoxygenase-inhibiting compounds derived from non-steroidal antiinflammatory carboxylic acids
WO1992000988A1 (en) * 1990-07-13 1992-01-23 Bodor Nicholas S Targeted drug delivery via phosphonate derivatives
EP0481214A1 (en) * 1990-09-14 1992-04-22 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Prodrugs of phosphonates
EP0486045A2 (en) * 1990-11-15 1992-05-20 MEDICEChem.-Pharm. Fabrik Pütter GmbH & Co. KG S(+)-Phenyl-alkanoic acids and alpha-amino acid containing complexes
EP0486046A2 (en) * 1990-11-15 1992-05-20 MEDICEChem.-Pharm. Fabrik Pütter GmbH & Co. KG S(+)-Phenyl-alkanoic acids and aminosugar containing complexes

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4816570A (en) * 1982-11-30 1989-03-28 The Board Of Regents Of The University Of Texas System Biologically reversible phosphate and phosphonate protective groups
CA1330794C (en) * 1987-03-27 1994-07-19 Phillip Frost Anti-viral compounds, dosage forms and methods
US4837311A (en) * 1987-06-22 1989-06-06 Hoffman-La Roche Inc. Anti-retroviral compounds
EP0375183A1 (en) * 1988-12-05 1990-06-27 Schering Corporation Antiviral dimers and trimers

Patent Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0112130A1 (en) * 1982-12-09 1984-06-27 Teva Pharmaceutical Industries Limited Ethoxycarbonyloxy ethyl esters of non-steroidal anti-inflammatory carboxylic acids, their preparation and use
EP0202703A1 (en) * 1985-05-15 1986-11-26 N.V. Gantax Pharmaceutica Pharmaceutical compositions of the prodrug type, a process for the preparation thereof, a process for the preparation of them as prodrug functioning compounds and compounds obtained therein
EP0271983A1 (en) * 1986-10-31 1988-06-22 Pfizer Inc. Transdermal flux enhancing compositions
EP0291873A2 (en) * 1987-05-22 1988-11-23 Hoechst Aktiengesellschaft Method to determine the anti-aggregatory activity of vasoactive substances, especially phosphodiesterase and/or cyclooxygenase inhibitors
EP0331382A2 (en) * 1988-02-29 1989-09-06 Pfizer Inc. Transdermal flux enhancing compositions
EP0335164A2 (en) * 1988-03-31 1989-10-04 Merckle GmbH Ester derivatives of neopentanol, process for their preparation and their use as medicines
WO1990008155A1 (en) * 1989-01-23 1990-07-26 Board Of Regents, The University Of Texas System Biologically reversible phosphate and phosphonate protective groups
EP0407815A2 (en) * 1989-07-10 1991-01-16 Eisai Co., Ltd. Polyprenyl compound composition for soft capsules
EP0452908A2 (en) * 1990-04-19 1991-10-23 Abbott Laboratories Lipoxygenase-inhibiting compounds derived from non-steroidal antiinflammatory carboxylic acids
WO1992000988A1 (en) * 1990-07-13 1992-01-23 Bodor Nicholas S Targeted drug delivery via phosphonate derivatives
EP0481214A1 (en) * 1990-09-14 1992-04-22 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Prodrugs of phosphonates
EP0486045A2 (en) * 1990-11-15 1992-05-20 MEDICEChem.-Pharm. Fabrik Pütter GmbH & Co. KG S(+)-Phenyl-alkanoic acids and alpha-amino acid containing complexes
EP0486046A2 (en) * 1990-11-15 1992-05-20 MEDICEChem.-Pharm. Fabrik Pütter GmbH & Co. KG S(+)-Phenyl-alkanoic acids and aminosugar containing complexes

Non-Patent Citations (13)

* Cited by examiner, † Cited by third party
Title
BALDESSARINI R.J. ET AL: "Hydrolysis of diester prodrugs of apomorphine", BIOCHEM.PHARMACOL., 1977, VOL. 26, NO. 19, PAGE(S) 1749-1756 *
BENNETT D.B. ET AL: "Biodegradable polymeric prodrugs of naltrexone", J. CONTROL. RELEASE, 1991, VOL. 16, NO. 1-2, PAGE(S) 43-52 *
FARQUHAR D ET AL: "Biologically reversible phosphate-protective groups", J. PHARM. SCI., 1983, VOL. 72, NO. 3, PAGE(S) 324-5 *
FREED, JEROME J. ET AL: "Evidence for acyloxymethyl esters of pyrimidine 5'-deoxyribonucleotides as extracellular sources of active 5'-deoxyribonucleotides in cultured cells", BIOCHEM. PHARMACOL., 1989, VOL.38, NO. 19, 3193-8 *
LAZAR S. ET AL: "Synthesis and biological activity of the phosphate and sulfate esters of naloxone and naltrexone", EUR. J. MED. CHEM., 1994, VOL. 29, NO. 1, PAGE(S) 45-53, FR *
SASTRY J K ET AL: "Membrane-permeable dideoxyuridine 5'-monophosphate analog inhibits human immunodeficiency virus infection", MOL. PHARMACOL. 1992, VOL. 41, NO. 3, PAGES 441-445 *
See also references of WO9217185A1 *
SRIVASTVA D N ET AL: "Mass spectral characterization of acyloxymethyl phosphates", J. CHEM. TECHNOL. BIOTECHNOL., 1990, VOL. 47, NO. 3, PAGE(S) 235-43 *
SRIVASTVA, DEVENDRA N. ET AL: "Bioreversible phosphate protective groups: synthesis and stability of model acyloxymethyl phosphates", BIOORG. CHEM., vol. 12, no. 2, pages 118 - 129 *
SRIVASTVA, DEVENDRA N. ET AL: "Mass spectral characterization of acyloxymethyl phosphates", J. CHEM. TECHNOL. BIOTECHNOL., 1990, VOL. 47, NO. 3, 235-43 *
STARRETT, JOHN E., JR. ET AL: "Synthesis and in vitro evaluation of a phosphonate prodrug: bis(pivaloyloxymethyl)-9-(2-phosphonylmethoxyethyl)adenine", ANTIVIRAL RES., 1992, VOL. 19, NO. 3, PAGES 267-73 *
STELLA V.J. ET AL: "Prodrugs. Do they have advantages in clinical practice?", DRUGS, 1985, VOL. 29, NO. 5, PAGE(S) 455-473 *
THOMSON W ET AL: "Synthesis and bioactivation of bis(aroyloxymethyl) and mono(aroyloxymethyl) esters of benzylphosphonate and phosphonoacetate", J. CHEM. SOC., PERKIN TRANS. 1, 1993, NO. 19, PAGE(S) 2303-8 *

Also Published As

Publication number Publication date
WO1992017185A1 (en) 1992-10-15
JPH06510020A (en) 1994-11-10
CA2108041A1 (en) 1992-09-30
AU1674892A (en) 1992-11-02
EP0577725A1 (en) 1994-01-12
AU668506B2 (en) 1996-05-09

Similar Documents

Publication Publication Date Title
EP0647133A4 (en) Compositions and methods for enhanced drug delivery.
EP0707471A4 (en) Novel therapeutic drug delivery systems
GB8712176D0 (en) Drug delivery system
AU4989993A (en) Drug delivery system
AU8538991A (en) Delivery device for atomized medicaments
GB9200417D0 (en) Cytotoxic drug therapy
IL109661A0 (en) Drug delivery device
EP0431080A4 (en) Compositions and methods for drug delivery and chromatography
IL102777A0 (en) Pharmaceutical combination formulation
IL86802A0 (en) Drug delivery devices
EP0491812A4 (en) Drug delivery compositions
HK1020523A1 (en) Uniform drug delivery therapy
EP0577725A4 (en) Targeted drug delivery via mixed phosphate derivatives
EP0448091A3 (en) Pharmaceutical composition containing slightly water-soluble drug
IL106578A (en) Pharmaceutical compositions for drug targeting
AU660290B2 (en) Multiple drug delivery system
GB9014871D0 (en) Drug delivery system for administering growth factor
ZA927506B (en) New drug formulation.
GB9325330D0 (en) Fluorocyclodextrin drug delivery system
GB9404293D0 (en) Drug delivery system
GB9216061D0 (en) Pharmaceutical combination formulation
GB2292887B (en) Drug delivery system
AU4292993A (en) Improved delivery formulation for lipophilic drugs
EP0408019A3 (en) Pharmaceutical active derivative delivery systems
IE893139L (en) Controlled drug delivery

Legal Events

Date Code Title Description
PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

Free format text: ORIGINAL CODE: 0009012

17P Request for examination filed

Effective date: 19931014

AK Designated contracting states

Kind code of ref document: A1

Designated state(s): AT BE CH DE DK ES FR GB GR IT LI LU MC NL SE

A4 Supplementary search report drawn up and despatched

Effective date: 19960304

AK Designated contracting states

Kind code of ref document: A4

Designated state(s): AT BE CH DE DK ES FR GB GR IT LI LU MC NL SE

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: THE APPLICATION IS DEEMED TO BE WITHDRAWN

18D Application deemed to be withdrawn

Effective date: 19981002