WO2000004868A3 - Libraries of polyhydroxamates and their analogs - Google Patents

Libraries of polyhydroxamates and their analogs Download PDF

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Publication number
WO2000004868A3
WO2000004868A3 PCT/US1999/016848 US9916848W WO0004868A3 WO 2000004868 A3 WO2000004868 A3 WO 2000004868A3 US 9916848 W US9916848 W US 9916848W WO 0004868 A3 WO0004868 A3 WO 0004868A3
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WIPO (PCT)
Prior art keywords
polyhydroxamate
matrix
analog
polyhydroxamates
bound
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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.)
Ceased
Application number
PCT/US1999/016848
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French (fr)
Other versions
WO2000004868A2 (en
Inventor
Garland R Marshall
Leonard O Rosik
Otto F Schall
Urszula J Slomczynska
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METAPHORE Inc
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METAPHORE Inc
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Publication date
Application filed by METAPHORE Inc filed Critical METAPHORE Inc
Priority to JP2000560861A priority Critical patent/JP2002521319A/en
Priority to EP99937465A priority patent/EP1098659A4/en
Priority to AU52295/99A priority patent/AU5229599A/en
Priority to CA002337756A priority patent/CA2337756A1/en
Publication of WO2000004868A2 publication Critical patent/WO2000004868A2/en
Publication of WO2000004868A3 publication Critical patent/WO2000004868A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C259/00Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
    • C07C259/04Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
    • C07C259/06Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/06Antiabortive agents; Labour repressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P39/00General protective or antinoxious agents
    • A61P39/02Antidotes
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/11Compounds covalently bound to a solid support
    • CCHEMISTRY; METALLURGY
    • C40COMBINATORIAL TECHNOLOGY
    • C40BCOMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B40/00Libraries per se, e.g. arrays, mixtures
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pregnancy & Childbirth (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Psychology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Toxicology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Compositions Of Macromolecular Compounds (AREA)

Abstract

A method of synthesizing desired polyhydroxamates and polyhydroxamate analogs is provided. The method comprises linking a first component of the desired polyhydroxamate or polyhydroxamate analog to a support matrix under conditions effective to form a first matrix-bound intermediate of said desired polyhydroxamate or analog, extending said first matrix-bound intermediate using reagents and reaction conditions effective to form one or more additional matrix-bound intermediates of said desired polyhydroxamate or analog, thereby forming a matrix-bound precursor of the desired polyhydroxamate or polyhydroxamate analog. Protective groups used during synthesis of the precursor are removed and the matrix-bound precursor is cleared from the support matrix, thereby synthesizing the desired polyhydroxamate or polyhydroxamate analog. Methods of making, screening and selecting libraries of candidate polyhydroxamates, the libraries and polyhydroxamates, polyhydroxamate analogs, their intermediates, and methods for using such compounds and their compositions are also disclosed.
PCT/US1999/016848 1998-07-23 1999-07-23 Libraries of polyhydroxamates and their analogs Ceased WO2000004868A2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
JP2000560861A JP2002521319A (en) 1998-07-23 1999-07-23 Library of polyhydroxamates and their analogs
EP99937465A EP1098659A4 (en) 1998-07-23 1999-07-23 Libraries of polyhydroxamates and their analogs
AU52295/99A AU5229599A (en) 1998-07-23 1999-07-23 Libraries of polyhydroxamates and their analogs
CA002337756A CA2337756A1 (en) 1998-07-23 1999-07-23 Libraries of polyhydroxamates and their analogs

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US9388398P 1998-07-23 1998-07-23
US60/093,883 1998-07-23

Publications (2)

Publication Number Publication Date
WO2000004868A2 WO2000004868A2 (en) 2000-02-03
WO2000004868A3 true WO2000004868A3 (en) 2000-05-04

Family

ID=22241527

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1999/016848 Ceased WO2000004868A2 (en) 1998-07-23 1999-07-23 Libraries of polyhydroxamates and their analogs

Country Status (5)

Country Link
EP (1) EP1098659A4 (en)
JP (1) JP2002521319A (en)
AU (1) AU5229599A (en)
CA (1) CA2337756A1 (en)
WO (1) WO2000004868A2 (en)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6916799B2 (en) 1997-11-03 2005-07-12 Duke University Substituted porphyrins
US7470677B2 (en) 1993-10-15 2008-12-30 Aeolus Pharmaceuticals, Inc. Oxidant scavengers
US7485721B2 (en) 2002-06-07 2009-02-03 Duke University Substituted porphyrins

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE312103T1 (en) 1999-01-25 2005-12-15 Nat Jewish Med & Res Center SUBSTITUTED PORPHYRINS AND THEIR THERAPEUTIC USES
AU4338502A (en) * 2000-10-23 2002-06-24 Genetics Inst Acid-labile isotope-coded extractant (alice) and its use in quantitative mass spectrometric analysis of protein mixtures
EP1439842A4 (en) 2001-06-01 2009-09-02 Nat Jewish Med & Res Center OXIDIZING SENSORS FOR THE TREATMENT OF DIABETES OR FOR USE IN TRANSPLANTATION OR INDUCING IMMUNE TOLERANCE
US20040236519A1 (en) * 2001-06-08 2004-11-25 Marshall Garland R. Libraries of confomationally constrained peptides, chiral azacrowns, and peptidomimetics and methods of making the same
CN102105146A (en) 2008-05-23 2011-06-22 国立犹太保健医院 Methods for treating injury associated with exposure to an alkylating species
US9334716B2 (en) 2012-04-12 2016-05-10 Halliburton Energy Services, Inc. Treatment fluids comprising a hydroxypyridinecarboxylic acid and methods for use thereof
EP3131585B1 (en) * 2014-03-19 2020-07-15 Universität Zürich Multidentate bifunctional chelating agents for radionuclide complexation in diagnostics and therapy
KR102727918B1 (en) * 2018-04-10 2024-11-11 사노피-아벤티스 도이칠란트 게엠베하 Synthesis of lixisenatide using capping
CN110270133A (en) * 2019-07-30 2019-09-24 深圳市百迈生命科学有限公司 A kind of integral post plate preparation method and application based on PE sieve plate conjugation chemistry group

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4987253A (en) * 1988-09-19 1991-01-22 University Of Florida Method for the synthesis of desferrioxamine B and analogs thereof
WO1996026223A1 (en) * 1995-02-24 1996-08-29 British Biotech Pharmaceuticals Limited Synthesis of hydroxamic acid derivatives

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5322961A (en) * 1992-12-09 1994-06-21 University Of Florida Analogs of desferrioxamine B and method for synthesis thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4987253A (en) * 1988-09-19 1991-01-22 University Of Florida Method for the synthesis of desferrioxamine B and analogs thereof
WO1996026223A1 (en) * 1995-02-24 1996-08-29 British Biotech Pharmaceuticals Limited Synthesis of hydroxamic acid derivatives

Non-Patent Citations (8)

* Cited by examiner, † Cited by third party
Title
BERGERON ET AL.: "Structural Alterations in Desferrioxamine Compatible with Iron Clearance in Animals", J. MED. CHEM.,, vol. 35, no. 25, 1992, pages 4739 - 4744, XP002925124 *
BERGERON ET AL.: "Synthesis and Biological Evaluation of Hydroxamate-Based Iron Chelators", J. MED. CHEM.,, vol. 34, no. 11, 1991, pages 3182 - 3187, XP002925122 *
DIONIS ET AL.: "Synthesis and Analytical Characterization of a Major Desferrioxamine B Metabolite", J. ORG. CHEM.,, vol. 54, no. 23, 1989, pages 5623 - 5627, XP002925123 *
FURKA ET AL.: "General Method for Rapid Synthesis of Multicomponent Mixtures", INT. J. PEPTIDE PROTEIN RES.,, vol. 37, 1991, pages 487 - 493, XP002925121 *
GOLEBIOASKI ET AL.: "Solid Supported Synthesis of Hydroxamic Acids", TET. LETT.,, vol. 39, no. 21, 21 May 1998 (1998-05-21), pages 3397 - 3400, XP002925120 *
GORDON ET AL.: "Applications of Combinatorial Technologies to Drug Discovery. 2. Combinatorial Organic Synthesis, Library Screening Strategies and Future Directions", J. MED. CHEM.,, vol. 37, no. 10, 13 May 1994 (1994-05-13), pages 1385 - 1401, XP002925118 *
NGU ET AL.: "A New and Efficient Solid Phase Synthesis of Hydroxamic Acids", J. ORG. CHEM.,, vol. 62, no. 21, 17 October 1997 (1997-10-17), pages 7088 - 7089, XP002925119 *
See also references of EP1098659A4 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7470677B2 (en) 1993-10-15 2008-12-30 Aeolus Pharmaceuticals, Inc. Oxidant scavengers
US6916799B2 (en) 1997-11-03 2005-07-12 Duke University Substituted porphyrins
US7485721B2 (en) 2002-06-07 2009-02-03 Duke University Substituted porphyrins

Also Published As

Publication number Publication date
EP1098659A2 (en) 2001-05-16
WO2000004868A2 (en) 2000-02-03
CA2337756A1 (en) 2000-02-03
JP2002521319A (en) 2002-07-16
EP1098659A4 (en) 2004-11-24
AU5229599A (en) 2000-02-14

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