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AU2001290841A1 - Water soluble rapamycin esters - Google Patents

Water soluble rapamycin esters

Info

Publication number
AU2001290841A1
AU2001290841A1 AU2001290841A AU9084101A AU2001290841A1 AU 2001290841 A1 AU2001290841 A1 AU 2001290841A1 AU 2001290841 A AU2001290841 A AU 2001290841A AU 9084101 A AU9084101 A AU 9084101A AU 2001290841 A1 AU2001290841 A1 AU 2001290841A1
Authority
AU
Australia
Prior art keywords
water soluble
soluble rapamycin
rapamycin esters
esters
hydroxyesters
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.)
Abandoned
Application number
AU2001290841A
Inventor
Mahdi Bakir Fawzi
Tianmin Zhu
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.)
Wyeth LLC
Original Assignee
American Home Products Corp
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 American Home Products Corp filed Critical American Home Products Corp
Publication of AU2001290841A1 publication Critical patent/AU2001290841A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18Bridged systems
    • 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
    • A61K47/56Medicinal 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59Medicinal 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60Medicinal 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Saccharide Compounds (AREA)

Abstract

This invention provide pegylated hydroxyesters of rapamycin which are useful in inducing immunosuppression and in the treatment of transplantation rejection, autoimmune diseases, solid tumors, fungal infections, and vascular disease.
AU2001290841A 2000-09-19 2001-09-13 Water soluble rapamycin esters Abandoned AU2001290841A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US23377600P 2000-09-19 2000-09-19
US60/233,776 2000-09-19
PCT/US2001/028575 WO2002024706A2 (en) 2000-09-19 2001-09-13 Water soluble rapamycin esters

Publications (1)

Publication Number Publication Date
AU2001290841A1 true AU2001290841A1 (en) 2002-04-02

Family

ID=22878646

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2001290841A Abandoned AU2001290841A1 (en) 2000-09-19 2001-09-13 Water soluble rapamycin esters

Country Status (13)

Country Link
US (1) US6432973B1 (en)
EP (1) EP1319008B1 (en)
JP (1) JP2004509898A (en)
CN (1) CN1222529C (en)
AT (1) ATE411321T1 (en)
AU (1) AU2001290841A1 (en)
BR (1) BR0113975A (en)
CA (1) CA2421485A1 (en)
DE (1) DE60136200D1 (en)
DK (1) DK1319008T3 (en)
ES (1) ES2313983T3 (en)
MX (1) MXPA03002258A (en)
WO (1) WO2002024706A2 (en)

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WO2003097647A1 (en) * 2002-05-15 2003-11-27 Endocyte, Inc. Vitamin-mitomycin conjugates
ATE385795T1 (en) * 2002-07-30 2008-03-15 Wyeth Corp PARENTERAL FORMULATIONS CONTAINING A RAPAMYCIN HYDROXYESTER
US7169594B2 (en) * 2002-08-12 2007-01-30 Regents Of The University Of Michigan Diagnosis and treatment of diseases arising from defects in the tuberous sclerosis pathway
AU2004210136C1 (en) 2003-01-27 2010-10-07 Endocyte, Inc. Vitamin receptor binding drug delivery conjugates
JP2006524289A (en) * 2003-04-23 2006-10-26 ワイス・ホールディングズ・コーポレイション PEG-Wortmannin conjugate
AR046194A1 (en) 2003-11-04 2005-11-30 Mayo Foundation TREATMENT METHOD OF MANTO CELL LYMPHOMA
WO2005053744A1 (en) * 2003-11-26 2005-06-16 Entelos, Inc. TREATMENT OF RHEUMATOID ARTHRITIS WITH HYPOXIA-INDUCIBLE FACTOR 1α ANTAGONISTS
AR047988A1 (en) * 2004-03-11 2006-03-15 Wyeth Corp ANTI -OPLASTIC COMBINATIONS OF CCI-779 AND RITUXIMAB
JP4224115B2 (en) 2004-04-14 2009-02-12 ワイス Regiospecific synthesis of rapamycin 42-ester derivatives
JP2007534337A (en) * 2004-04-27 2007-11-29 ワイス Labeling rapamycin with a rapamycin-specific methylase
US8288557B2 (en) 2004-07-23 2012-10-16 Endocyte, Inc. Bivalent linkers and conjugates thereof
EP1856131A1 (en) * 2005-03-07 2007-11-21 Wyeth Oxepane isomer of 42-o-(2-hydroxy)ethyl-rapamycin
CN101175757B (en) * 2005-03-16 2012-11-14 恩多塞特公司 Synthesis and purification of pteroic acid and conjugates thereof
EP1948240A2 (en) * 2005-08-19 2008-07-30 Endocyte, Inc. Ligand conjugates of vinca alkaloids, analogs and derivatives
BRPI0615354A2 (en) * 2005-08-19 2011-05-17 Endocyte Inc receptor binding drug release conjugate, pharmaceutical composition comprising it, as well as its use
PE20071041A1 (en) 2005-12-07 2007-12-07 Wyeth Corp PURIFIED CRYSTAL FORM OF CCI-779 AND PROCESS FOR THE PREPARATION OF THE SAME
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US20080207671A1 (en) * 2006-07-31 2008-08-28 The Regents Of The University Of Michigan Diagnosis and treatment of diseases arising from defects in the tuberous sclerosis pathway
TW200824713A (en) 2006-10-18 2008-06-16 Wyeth Corp Processes for the synthesis of individual isomers of mono-PEG CCI-779
US8425459B2 (en) 2006-11-20 2013-04-23 Lutonix, Inc. Medical device rapid drug releasing coatings comprising a therapeutic agent and a contrast agent
US8414910B2 (en) 2006-11-20 2013-04-09 Lutonix, Inc. Drug releasing coatings for medical devices
US20080175887A1 (en) 2006-11-20 2008-07-24 Lixiao Wang Treatment of Asthma and Chronic Obstructive Pulmonary Disease With Anti-proliferate and Anti-inflammatory Drugs
US20080276935A1 (en) 2006-11-20 2008-11-13 Lixiao Wang Treatment of asthma and chronic obstructive pulmonary disease with anti-proliferate and anti-inflammatory drugs
US9737640B2 (en) 2006-11-20 2017-08-22 Lutonix, Inc. Drug releasing coatings for medical devices
US8998846B2 (en) 2006-11-20 2015-04-07 Lutonix, Inc. Drug releasing coatings for balloon catheters
US8414526B2 (en) 2006-11-20 2013-04-09 Lutonix, Inc. Medical device rapid drug releasing coatings comprising oils, fatty acids, and/or lipids
US8414525B2 (en) 2006-11-20 2013-04-09 Lutonix, Inc. Drug releasing coatings for medical devices
US9700704B2 (en) 2006-11-20 2017-07-11 Lutonix, Inc. Drug releasing coatings for balloon catheters
US20080188461A1 (en) * 2007-02-01 2008-08-07 Regents Of The University Of Michigan Compositions and methods for detecting, preventing and treating seizures and seizure related disorders
US20100104626A1 (en) * 2007-02-16 2010-04-29 Endocyte, Inc. Methods and compositions for treating and diagnosing kidney disease
NZ580132A (en) * 2007-03-14 2012-11-30 Endocyte Inc Binding ligand linked drug delivery conjugates of tubulysins to vitamins
RU2523909C2 (en) 2007-06-25 2014-07-27 Эндосайт, Инк. Conjugates, containing hydrophilic spacers of linkers
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
EP2209374B1 (en) 2007-10-25 2014-12-03 Endocyte, Inc. Tubulysins and processes for preparing
WO2010024898A2 (en) 2008-08-29 2010-03-04 Lutonix, Inc. Methods and apparatuses for coating balloon catheters
CN101676291B (en) * 2008-09-18 2012-05-09 上海海和药物研究开发有限公司 Rapamycin carbonate analog, pharmaceutical composition thereof, and preparation method and uses thereof
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US20140080175A1 (en) 2012-03-29 2014-03-20 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
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CN107949566B (en) 2016-05-10 2021-09-28 浙江海正药业股份有限公司 Water-soluble rapamycin derivatives
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Also Published As

Publication number Publication date
US20020055518A1 (en) 2002-05-09
JP2004509898A (en) 2004-04-02
CN1222529C (en) 2005-10-12
ATE411321T1 (en) 2008-10-15
ES2313983T3 (en) 2009-03-16
EP1319008A2 (en) 2003-06-18
CN1460108A (en) 2003-12-03
US6432973B1 (en) 2002-08-13
DK1319008T3 (en) 2009-02-09
MXPA03002258A (en) 2003-06-24
BR0113975A (en) 2003-07-29
EP1319008B1 (en) 2008-10-15
CA2421485A1 (en) 2002-03-28
WO2002024706A2 (en) 2002-03-28
DE60136200D1 (en) 2008-11-27
WO2002024706A3 (en) 2002-10-10

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