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WO2002060374A3 - Benz-1,3-azole derivatives and their uses as heparanase inhibitors - Google Patents

Benz-1,3-azole derivatives and their uses as heparanase inhibitors Download PDF

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Publication number
WO2002060374A3
WO2002060374A3 PCT/IL2002/000081 IL0200081W WO02060374A3 WO 2002060374 A3 WO2002060374 A3 WO 2002060374A3 IL 0200081 W IL0200081 W IL 0200081W WO 02060374 A3 WO02060374 A3 WO 02060374A3
Authority
WO
WIPO (PCT)
Prior art keywords
benz
azole derivatives
heparanase inhibitors
heparanase
derivatives
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.)
Ceased
Application number
PCT/IL2002/000081
Other languages
French (fr)
Other versions
WO2002060374A2 (en
Inventor
Maty Ayal-Hershkovitz
Daphna Miron
Ofra Levy
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.)
Insight Strategy and Marketing Ltd
Original Assignee
Insight Strategy and Marketing Ltd
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 Insight Strategy and Marketing Ltd filed Critical Insight Strategy and Marketing Ltd
Priority to AU2002228317A priority Critical patent/AU2002228317A1/en
Publication of WO2002060374A2 publication Critical patent/WO2002060374A2/en
Publication of WO2002060374A3 publication Critical patent/WO2002060374A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/18—Benzimidazoles; Hydrogenated benzimidazoles with aryl radicals directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/28—Radicals substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/84—Naphthothiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

The invention provides benz-1,3-azole derivatives, namely benzimidazole, benzoxazole and benzthiazole derivatives as heparanase inhibitors suitable for treatment of diseases and disorders caused by or associated with heparanase catalytic activity such as cancer, inflammatory disorders and autoimmune diseases.
PCT/IL2002/000081 2001-01-29 2002-01-29 Benz-1,3-azole derivatives and their uses as heparanase inhibitors Ceased WO2002060374A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002228317A AU2002228317A1 (en) 2001-01-29 2002-01-29 Benz-1,3-azole derivatives and their uses as heparanase inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US26430601P 2001-01-29 2001-01-29
US60/264,306 2001-01-29

Publications (2)

Publication Number Publication Date
WO2002060374A2 WO2002060374A2 (en) 2002-08-08
WO2002060374A3 true WO2002060374A3 (en) 2003-02-27

Family

ID=23005454

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IL2002/000081 Ceased WO2002060374A2 (en) 2001-01-29 2002-01-29 Benz-1,3-azole derivatives and their uses as heparanase inhibitors

Country Status (2)

Country Link
AU (1) AU2002228317A1 (en)
WO (1) WO2002060374A2 (en)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60329513D1 (en) * 2002-07-30 2009-11-12 Banyu Pharma Co Ltd ANTAGONIST OF MELANINE CONCENTRATING HORMONE RECEPTOR, CONTAINING A BENZIMIDAZOLE DERIVATIVE AS AN ACTIVE SUBSTANCE
US20050260126A1 (en) * 2002-08-30 2005-11-24 Yukitsuka Kudo Diagnostic probes and remedies for diseases with accumulation of prion protein, and stains for prion protein
WO2004046122A2 (en) * 2002-11-16 2004-06-03 Oxford Glycosciences (Uk) Ltd Benzoxazole, benzthiazole and benzimidazole acid derivatives and their use as heparanase inhibitors
GB0226822D0 (en) * 2002-11-16 2002-12-24 Oxford Glycosciences Uk Ltd Novel compounds
US7829552B2 (en) 2003-11-19 2010-11-09 Metabasis Therapeutics, Inc. Phosphorus-containing thyromimetics
WO2006128058A2 (en) 2005-05-26 2006-11-30 Metabasis Therapeutics, Inc. Thyromimetics for the treatment of fatty liver diseases
CA2573185A1 (en) 2004-07-14 2006-02-23 Ptc Therapeutics, Inc. Methods for treating hepatitis c
US7772271B2 (en) 2004-07-14 2010-08-10 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7868037B2 (en) 2004-07-14 2011-01-11 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7781478B2 (en) 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
MX2007000762A (en) 2004-07-22 2007-04-02 Ptc Therapeutics Inc Thienopyridines for treating hepatitis c.
CA2666840C (en) * 2006-10-20 2015-07-14 The Australian National University Inhibition of degradation of extracellular matrix
US7906655B2 (en) * 2008-08-07 2011-03-15 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
GB0821913D0 (en) * 2008-12-02 2009-01-07 Price & Co Antibacterial compounds
CN101735152A (en) * 2009-12-18 2010-06-16 长沙理工大学 2,2'-(1,4-phenylene)bi(benzimidazole-5-carboxylic acid) and preparation method thereof
US8686048B2 (en) * 2010-05-06 2014-04-01 Rhizen Pharmaceuticals Sa Immunomodulator and anti-inflammatory compounds
JP5845502B2 (en) 2010-06-01 2016-01-20 サミット セラピューティクス ピーエルシー Compounds for treating Clostridium difficile-related diseases
US11202789B2 (en) 2016-11-21 2021-12-21 Viking Therapeutics, Inc. Method of treating glycogen storage disease
US11787783B2 (en) 2016-12-13 2023-10-17 Beta Therapeutics Pty Ltd Heparanase inhibitors and use thereof
CN110291073A (en) 2016-12-13 2019-09-27 贝塔医疗私人有限公司 Heparanase inhibitors and application thereof
EP3381907A1 (en) 2017-03-27 2018-10-03 Leadiant Biosciences SA Symmetrical 2-aminophenyl-benzazolyl-5-acetate compounds and their use as anti-heparanase
EP3381906A1 (en) * 2017-03-27 2018-10-03 Leadiant Biosciences SA Compounds for use as heparanase inhibitors
CN110996966A (en) 2017-06-05 2020-04-10 维京治疗公司 Composition for treating fibrosis
CN112135832A (en) 2018-03-22 2020-12-25 维京治疗公司 Crystalline forms of a compound and methods of making crystalline forms of a compound
US12102646B2 (en) 2018-12-05 2024-10-01 Viking Therapeutics, Inc. Compositions for the treatment of fibrosis and inflammation

Citations (3)

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US5932600A (en) * 1997-03-14 1999-08-03 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme
US6153631A (en) * 1996-10-23 2000-11-28 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
WO2001027088A1 (en) * 1999-10-12 2001-04-19 Japan Tobacco Inc. Lpl potentiators

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6153631A (en) * 1996-10-23 2000-11-28 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US5932600A (en) * 1997-03-14 1999-08-03 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme
WO2001027088A1 (en) * 1999-10-12 2001-04-19 Japan Tobacco Inc. Lpl potentiators

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
DATABASE CAPLUS [online] (COLUMBUS, OH, USA); CHAUHAN ET AL.: "Synthesis of 2,5(6)-disubstituted benzimidazoles, 2-substituted 5-(4-substituted phenyl) - 1,3,4-thiadiazoles and imidazothioxanthene and their antifilarial activity, section B: organic chemistry including medicinal chemistry", XP002958527, accession no. ACS Database accession no. 1987:477754 *
DATABASE CAPLUS [online] (COLUMBUS, OH, USA); MIKROYANNIDIS ET AL.: "Heat-resistance mixture resin vbased on addition-type bismidobenzimidazoles", XP002958526, accession no. ACS Database accession no. 1991:123605 *
EUROPEAN POLYMER J., vol. 27, no. 2, 1991, pages 199 - 203 *
INDIAN JOURNAL OF CHEMISTRY, vol. 25B, no. 11, 1986, pages 1146 - 1149 *

Also Published As

Publication number Publication date
AU2002228317A1 (en) 2002-08-12
WO2002060374A2 (en) 2002-08-08

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