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WO2002060867A3 - Carbazole derivatives and their uses as heparanase inhibitors - Google Patents

Carbazole derivatives and their uses as heparanase inhibitors Download PDF

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Publication number
WO2002060867A3
WO2002060867A3 PCT/IL2002/000079 IL0200079W WO02060867A3 WO 2002060867 A3 WO2002060867 A3 WO 2002060867A3 IL 0200079 W IL0200079 W IL 0200079W WO 02060867 A3 WO02060867 A3 WO 02060867A3
Authority
WO
WIPO (PCT)
Prior art keywords
substituted
carbazole derivatives
heparanase inhibitors
group
heparanase
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/IL2002/000079
Other languages
French (fr)
Other versions
WO2002060867A2 (en
Inventor
Maty Ayal-Hershkovitz
Daphna Miron
Avi Koller
Neta Ilan
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 AU2002228316A priority Critical patent/AU2002228316A1/en
Publication of WO2002060867A2 publication Critical patent/WO2002060867A2/en
Anticipated expiration legal-status Critical
Publication of WO2002060867A3 publication Critical patent/WO2002060867A3/en
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • C07D209/88—Carbazoles; Hydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system

Landscapes

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

Abstract

Carbazole derivatives having at the 9-position a 3-(substituted)amino-2-hydroxypropyl group and fluorene derivatives having at the 9-position a =N-NH-R4 group, wherein R4 is a (substituted) carboxamido, (substituted) thiocarboxamido or (substituted) hydrazido group, are provided as heparanase inhibitors suitable for the treatment of diseases and disorders caused by or associated with heparanase catalytic activity such as cancer, inflammatory disorders and autoimmune diseases.
PCT/IL2002/000079 2001-01-29 2002-01-29 Carbazole derivatives and their uses as heparanase inhibitors Ceased WO2002060867A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002228316A AU2002228316A1 (en) 2001-01-29 2002-01-29 Carbazole derivatives and their uses as heparanase inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US26430401P 2001-01-29 2001-01-29
US60/264,304 2001-01-29

Publications (2)

Publication Number Publication Date
WO2002060867A2 WO2002060867A2 (en) 2002-08-08
WO2002060867A3 true WO2002060867A3 (en) 2004-03-18

Family

ID=23005445

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IL2002/000079 Ceased WO2002060867A2 (en) 2001-01-29 2002-01-29 Carbazole derivatives and their uses as heparanase inhibitors

Country Status (2)

Country Link
AU (1) AU2002228316A1 (en)
WO (1) WO2002060867A2 (en)

Families Citing this family (41)

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GB0220214D0 (en) * 2002-08-30 2002-10-09 Novo Pharmaceuticals De Ltd Compounds and their use
CN100532374C (en) 2002-10-23 2009-08-26 格兰马克药品有限公司 Novel tricyclic compounds useful in the treatment of inflammatory and allergic disorders: processes for their preparation and pharmaceutical compositions containing them
EA010634B1 (en) * 2003-04-11 2008-10-30 Гленмарк Фармасьютикалс С.А. Novel heterocyclic compounds useful for thr treatment of inflammatory and allergic disorders:process for their preparation and pharmaceutical compositions containing them
EP1713501B1 (en) * 2004-01-29 2008-01-16 Cellzome Ag Treatment of neurodegenerative diseases by the use of gpr49
AU2005211255A1 (en) * 2004-02-06 2005-08-18 Insight Biopharmaceuticals Ltd Heparanase inhibitors and uses thereof
GB0412553D0 (en) 2004-06-04 2004-07-07 Univ Aberdeen Therapeutic agents for the treatment of bone conditions
CA2570884C (en) * 2004-06-16 2016-04-19 Jack Arbiser Carbazole formulations for the treatment of psoriasis and angiogenesis
MX2007004400A (en) 2004-10-13 2007-06-19 Glenmark Pharmaceuticals Sa Process for the preparation of n-(3, 5-dichloropyrid-4-yl)-4 oromethoxy-8-methanesulfonamido-dibenzo [b, d] diflufuran-1-carboxamide.
ES2417491T3 (en) 2004-12-17 2013-08-08 Glenmark Pharmaceuticals S.A. Novel heterocyclic compounds useful for the treatment of inflammatory and allergic disorders
AP2334A (en) 2004-12-17 2011-12-06 Glenmark Pharmaceuticals Sa Novel heterocyclic compounds useful for the treatment of inflamatory and allergic disorders.
WO2006133353A2 (en) 2005-06-08 2006-12-14 The University Of North Carolina At Chapel Hill Methods of facilitating neural cell survival using non-peptide and peptide bdnf neurotrophin mimetics
JP5404406B2 (en) * 2006-10-20 2014-01-29 ジ オーストラリアン ナショナル ユニバーシティ Inhibition of extracellular matrix degradation
GB0705400D0 (en) 2007-03-21 2007-05-02 Univ Aberdeen Therapeutic compounds andm their use
AU2009282451B2 (en) 2008-08-15 2014-02-13 Georgetown University Fluorescent regulators of RASSF1A expression and human cancer cell proliferation
GB0817207D0 (en) 2008-09-19 2008-10-29 Pimco 2664 Ltd therapeutic apsac compounds and their use
GB0817208D0 (en) 2008-09-19 2008-10-29 Pimco 2664 Ltd Therapeutic apsap compounds and their use
US8362277B2 (en) 2009-01-09 2013-01-29 Board Of Regents Of The University Of Texas System Pro-neurogenic compounds
US8604074B2 (en) 2009-01-09 2013-12-10 Board Of Regents Of The University Of Texas System Pro-neurogenic compounds
US9962368B2 (en) * 2009-01-09 2018-05-08 Board Of Regents Of The University Of Texas System Pro-neurogenic compounds
US9162980B2 (en) 2009-01-09 2015-10-20 Board Of Regents Of The University Of Texas System Anti-depression compounds
EP2590647B1 (en) 2010-07-07 2017-11-08 Board of Regents of the University of Texas System Pro-neurogenic compounds
US9701676B2 (en) 2012-08-24 2017-07-11 Board Of Regents Of The University Of Texas System Pro-neurogenic compounds
WO2014031125A1 (en) * 2012-08-24 2014-02-27 Board Of Regents Of The University Of Texas System Pro-neurogenic compounds
EP2943480B1 (en) 2013-01-10 2019-01-30 Merck Patent GmbH Piperidinylcarbazole as antimalarial
US9828332B2 (en) 2013-03-15 2017-11-28 PharmatorophiX, Inc. Non-peptide BDNF neurotrophin mimetics
BR112015022832A2 (en) 2013-03-15 2017-07-18 Pharmatrophix Inc non-peptide bdnf neurotrophin mimetics
GB201311361D0 (en) 2013-06-26 2013-08-14 Pimco 2664 Ltd Compounds and their therapeutic use
US9353078B2 (en) * 2013-10-01 2016-05-31 New York University Amino, amido and heterocyclic compounds as modulators of rage activity and uses thereof
EP3068388A4 (en) 2013-11-11 2017-04-12 Board of Regents of the University of Texas System Neuroprotective compounds and use thereof
WO2015070237A1 (en) 2013-11-11 2015-05-14 Board Of Regents Of The University Of Texas System Neuroprotective chemicals and methods for identifying and using same
EP3164397B1 (en) 2014-07-04 2018-12-19 Merck Patent GmbH Azepanyl-derivatives and pharmaceutical compositions comprising the same with antiparasitic activity
EP3188738A4 (en) * 2014-09-02 2018-01-24 The Children's Hospital of Philadelphia Compositions and methods for the inhibition of chondrogenesis
ES2899852T3 (en) 2014-12-17 2022-03-15 Pimco 2664 Ltd N-(4-hydroxy-4-methyl-cyclohexyl)-4-phenyl-benzenesulfonamide and N-(-4-hydroxy-4-methyl-cyclohexyl)-4-(2-pyridyl)-benzenesulfonamide compounds and their therapeutic use
KR101652305B1 (en) * 2015-02-02 2016-08-30 충남대학교산학협력단 Composition containing the carbazole urea derivative for preventing or treating vascular disease
DK3307323T3 (en) * 2015-06-15 2022-08-15 Raziel Therapeutics Ltd Carbazole derivatives for the treatment of fibrotic diseases and related symptoms, and conditions thereof
US11053255B2 (en) 2015-06-22 2021-07-06 Georgetown University Synthesis of mahanine and related compounds
JP2020503377A (en) * 2016-12-13 2020-01-30 ベータ セラピューティクス プロプライアタリー リミティド Heparanase inhibitors and uses thereof
US11787783B2 (en) 2016-12-13 2023-10-17 Beta Therapeutics Pty Ltd Heparanase inhibitors and use thereof
EP3381906A1 (en) 2017-03-27 2018-10-03 Leadiant Biosciences SA Compounds for use as heparanase inhibitors
CN111217741B (en) * 2019-03-01 2022-03-15 广东省中医院（广州中医药大学第二附属医院、广州中医药大学第二临床医学院、广东省中医药科学院） Fluorine-substituted monocarbazole derivatives, preparation method and application thereof
CN117486782A (en) * 2023-12-29 2024-02-02 中国医学科学院药用植物研究所 N-substituted carbazole derivative and preparation method and application thereof

Citations (2)

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US5407940A (en) * 1992-10-02 1995-04-18 Adir Et Compagnie New ellipticine compounds
US5679694A (en) * 1992-07-20 1997-10-21 The Wellcome Foundation Ltd. Tetracyclic compounds, intermediates for their preparation and their use as antitumor agents

Patent Citations (2)

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US5679694A (en) * 1992-07-20 1997-10-21 The Wellcome Foundation Ltd. Tetracyclic compounds, intermediates for their preparation and their use as antitumor agents
US5407940A (en) * 1992-10-02 1995-04-18 Adir Et Compagnie New ellipticine compounds

Also Published As

Publication number Publication date
AU2002228316A1 (en) 2002-08-12
WO2002060867A2 (en) 2002-08-08

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