AU2001292231B2 - Derivatives of partially desulphated glycogaminoglycans as heparanase inhibitors, endowed with antiangiogenic activity and devoid of anticoagulating effect - Google Patents

Derivatives of partially desulphated glycogaminoglycans as heparanase inhibitors, endowed with antiangiogenic activity and devoid of anticoagulating effect Download PDF

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Publication number
AU2001292231B2
AU2001292231B2 AU2001292231A AU2001292231A AU2001292231B2 AU 2001292231 B2 AU2001292231 B2 AU 2001292231B2 AU 2001292231 A AU2001292231 A AU 2001292231A AU 2001292231 A AU2001292231 A AU 2001292231A AU 2001292231 B2 AU2001292231 B2 AU 2001292231B2
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Australia
Prior art keywords
heparin
desulphated
uronic acids
acetyl
partially
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Ceased
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AU2001292231A
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English (en)
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AU2001292231A1 (en
Inventor
Benito Casu
Giuseppe Giannini
Annamaria Naggi
Sergio Penco
Claudio Pisano
Giangiacomo Torri
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Leadiant Biosciences Sa
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Leadiant Biosciences S A
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Assigned to SIGMA-TAU RESEARCH SWITZERLAND S.A reassignment SIGMA-TAU RESEARCH SWITZERLAND S.A Request for Assignment Assignors: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A
Priority to AU2008202261A priority Critical patent/AU2008202261B2/en
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Assigned to LEADIANT BIOSCIENCES S.A. reassignment LEADIANT BIOSCIENCES S.A. Request to Amend Deed and Register Assignors: SIGMA-TAU RESEARCH SWITZERLAND S.A
Anticipated expiration legal-status Critical
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    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
    • A61K31/727—Heparin; Heparan
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08B—POLYSACCHARIDES; DERIVATIVES THEREOF
    • C08B37/00—Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
    • C08B37/006—Heteroglycans, i.e. polysaccharides having more than one sugar residue in the main chain in either alternating or less regular sequence; Gellans; Succinoglycans; Arabinogalactans; Tragacanth or gum tragacanth or traganth from Astragalus; Gum Karaya from Sterculia urens; Gum Ghatti from Anogeissus latifolia; Derivatives thereof
    • C08B37/0063—Glycosaminoglycans or mucopolysaccharides, e.g. keratan sulfate; Derivatives thereof, e.g. fucoidan
    • C08B37/0075—Heparin; Heparan sulfate; Derivatives thereof, e.g. heparosan; Purification or extraction methods thereof
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08B—POLYSACCHARIDES; DERIVATIVES THEREOF
    • C08B37/00—Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
    • C08B37/006—Heteroglycans, i.e. polysaccharides having more than one sugar residue in the main chain in either alternating or less regular sequence; Gellans; Succinoglycans; Arabinogalactans; Tragacanth or gum tragacanth or traganth from Astragalus; Gum Karaya from Sterculia urens; Gum Ghatti from Anogeissus latifolia; Derivatives thereof
    • C08B37/0063—Glycosaminoglycans or mucopolysaccharides, e.g. keratan sulfate; Derivatives thereof, e.g. fucoidan
    • C08B37/0075—Heparin; Heparan sulfate; Derivatives thereof, e.g. heparosan; Purification or extraction methods thereof
    • C08B37/0078—Degradation products

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Biochemistry (AREA)
  • Polymers & Plastics (AREA)
  • Materials Engineering (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
AU2001292231A 2001-09-12 2001-09-12 Derivatives of partially desulphated glycogaminoglycans as heparanase inhibitors, endowed with antiangiogenic activity and devoid of anticoagulating effect Ceased AU2001292231B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2008202261A AU2008202261B2 (en) 2001-09-12 2008-05-22 Derivatives of partially desulphated glycosaminoglycans as heparanase inhibitors, endowed with antiangiogenic activity and devoid of anticoagulating effect

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/IT2001/000472 WO2003022291A1 (en) 2001-09-12 2001-09-12 Derivatives of partially desulphated glycosaminoglycans as heparanase inhibitors, endowed with antiangiogenic activity and devoid of anticoagulating effect

Related Child Applications (1)

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AU2008202261A Division AU2008202261B2 (en) 2001-09-12 2008-05-22 Derivatives of partially desulphated glycosaminoglycans as heparanase inhibitors, endowed with antiangiogenic activity and devoid of anticoagulating effect

Publications (2)

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AU2001292231A1 AU2001292231A1 (en) 2003-06-19
AU2001292231B2 true AU2001292231B2 (en) 2008-06-05

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AU2001292231A Ceased AU2001292231B2 (en) 2001-09-12 2001-09-12 Derivatives of partially desulphated glycogaminoglycans as heparanase inhibitors, endowed with antiangiogenic activity and devoid of anticoagulating effect

Country Status (19)

Country Link
US (1) US20050137167A1 (cg-RX-API-DMAC7.html)
EP (2) EP1427427B1 (cg-RX-API-DMAC7.html)
JP (1) JP2005506326A (cg-RX-API-DMAC7.html)
KR (1) KR100855331B1 (cg-RX-API-DMAC7.html)
CN (1) CN1547477B (cg-RX-API-DMAC7.html)
AT (1) ATE511846T1 (cg-RX-API-DMAC7.html)
AU (1) AU2001292231B2 (cg-RX-API-DMAC7.html)
BR (1) BR0117124A (cg-RX-API-DMAC7.html)
CA (1) CA2457719C (cg-RX-API-DMAC7.html)
CY (2) CY1112551T1 (cg-RX-API-DMAC7.html)
CZ (1) CZ307433B6 (cg-RX-API-DMAC7.html)
DK (1) DK1427427T3 (cg-RX-API-DMAC7.html)
ES (2) ES2431362T3 (cg-RX-API-DMAC7.html)
HU (1) HU230385B1 (cg-RX-API-DMAC7.html)
MX (1) MXPA04002217A (cg-RX-API-DMAC7.html)
PT (2) PT2343077E (cg-RX-API-DMAC7.html)
SI (1) SI1427427T1 (cg-RX-API-DMAC7.html)
SK (1) SK288335B6 (cg-RX-API-DMAC7.html)
WO (1) WO2003022291A1 (cg-RX-API-DMAC7.html)

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JP5404406B2 (ja) * 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 細胞外マトリクスの分解の阻害
WO2009007224A1 (en) * 2007-07-10 2009-01-15 Sigma-Tau Industrie Farmaceutiche Riunite S.P.A. Low molecular weight heparin derivatives having neuroprotective activity
WO2009059284A2 (en) 2007-11-02 2009-05-07 Momenta Pharmaceuticals, Inc. Non-anticoagulant polysaccharide compositions
US8592393B2 (en) 2007-11-02 2013-11-26 Momenta Pharmaceuticals, Inc. Polysaccharide compositions and methods of use for the treatment and prevention of disorders associated with progenitor cell mobilization
US8569262B2 (en) 2007-11-02 2013-10-29 Momenta Pharmaceuticals, Inc. Polysaccharide compositions and methods of use for the treatment and prevention of disorders associated with progenitor cell mobilization
FI20085308A0 (fi) * 2008-04-11 2008-04-11 Polysackaridforskning I Uppsal Heparanaasittomia ihmiskuntaan kuulumattomia nisäkkäitä
FR2949115B1 (fr) * 2009-08-14 2012-11-02 Sanofi Aventis OLIGOSACCHARIDES N-SULFATES ACTIVATEURS DES RECEPTEURS DES FGFs, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE
AU2011226755A1 (en) * 2010-03-12 2012-10-04 The Australian National University Heparan sulfate replacement therapy
US9387256B2 (en) 2010-04-16 2016-07-12 Momenta Pharmaceuticals, Inc. Tissue targeting
JP5905455B2 (ja) 2010-06-17 2016-04-20 モメンタ ファーマシューティカルズ インコーポレイテッド 発毛を促進する方法および組成物
FR2970969B1 (fr) * 2011-01-27 2013-10-18 Sanofi Aventis Oligosaccharides 3-o-alkyles activateurs des recepteurs des fgfs, leur preparation et leur application en therapeutique
KR101522604B1 (ko) * 2013-03-21 2015-05-26 대한민국 곤충 글라이코자미노글라이칸 유래 헤파린 단편 및 이의 제조 방법
CN105408361B (zh) * 2013-05-16 2019-09-06 新加坡科技研究局 硫酸乙酰肝素
CA2910837A1 (en) 2013-05-28 2014-12-04 Momenta Pharmaceuticals, Inc. Pharmaceutical compositions
ITLO20130005A1 (it) * 2013-10-31 2015-05-01 He E Biochimiche G Ronzonr S R Derivati di glucosamminoglicani n-desolfatati e loro uso come farmaci
ITLO20130006A1 (it) * 2013-11-06 2015-05-07 He E Biochimiche G Ronzoni S R Derivati carbossilati di glucosamminoglicani e loro uso come farmaci
ES2715556T3 (es) 2015-03-06 2019-06-04 Leadiant Biosciences Sa In Liquidazione Terapia combinada con roneparstat del mieloma múltiple
US11787783B2 (en) 2016-12-13 2023-10-17 Beta Therapeutics Pty Ltd Heparanase inhibitors and use thereof
BR112019012045A2 (pt) 2016-12-13 2020-08-18 Beta Therapeutics Pty Ltd inibidores de heparanase e uso dos mesmos
CN108424474B (zh) * 2017-02-15 2023-07-25 清华大学 去抗凝肝素衍生物及其用于炎症性肠病的治疗
US11186603B2 (en) * 2017-03-23 2021-11-30 Victoria Link Limited Heparan sulfate glycomimetic compounds and their pharmaceutical and cosmeceutical uses
EP3388439A1 (en) 2017-04-11 2018-10-17 Leadiant Biosciences SA Biotin-conjugated n-acetyl glycol split heparin
US11225531B2 (en) * 2018-02-02 2022-01-18 Shenzhen Hepalink Pharmaceutical Group Co., Ltd. Glycosaminoglycan derivative and preparation method therefor and use thereof
EP3705126A1 (en) 2019-03-05 2020-09-09 Leadiant Biosciences S.p.A. Roneparstat for the treatment of amyloidosis
WO2021128253A1 (zh) * 2019-12-27 2021-07-01 深圳市海普瑞药业集团股份有限公司 一种糖胺聚糖衍生物及其应用
CA3187652A1 (en) * 2020-07-02 2022-01-06 Institut Francais De Recherche Pour L'exploitation De La Mer (Ifremer) Marine bacterial exopolysaccharide derivatives and uses thereof in the treatment of mucopolysaccharidoses

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SK1602004A3 (en) 2004-08-03
WO2003022291A1 (en) 2003-03-20
PT2343077E (pt) 2013-08-29
EP2343077B1 (en) 2013-07-17
HUP0401693A2 (hu) 2004-12-28
ES2431362T3 (es) 2013-11-26
CZ2004255A3 (cs) 2004-11-10
HK1069537A1 (en) 2005-05-27
BR0117124A (pt) 2004-09-28
DK1427427T3 (da) 2011-09-19
CY1112551T1 (el) 2016-02-10
CN1547477A (zh) 2004-11-17
KR20040048404A (ko) 2004-06-09
JP2005506326A (ja) 2005-03-03
SI1427427T1 (sl) 2011-10-28
PT1427427E (pt) 2011-09-13
HU230385B1 (hu) 2016-03-29
SK288335B6 (sk) 2016-02-02
EP2343077A1 (en) 2011-07-13
CY1114544T1 (el) 2016-10-05
KR100855331B1 (ko) 2008-09-04
ATE511846T1 (de) 2011-06-15
EP1427427A1 (en) 2004-06-16
CZ307433B6 (cs) 2018-08-22
ES2367778T3 (es) 2011-11-08
CA2457719A1 (en) 2003-03-20
CN1547477B (zh) 2010-12-22
MXPA04002217A (es) 2004-07-08
US20050137167A1 (en) 2005-06-23
CA2457719C (en) 2012-01-03
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