WO2011018587A3 - OLIGOSACCHARIDES N-SULFATES ACTIVATEURS DES RECEPTEURS DES FGFs, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE - Google Patents

OLIGOSACCHARIDES N-SULFATES ACTIVATEURS DES RECEPTEURS DES FGFs, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE Download PDF

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Publication number
WO2011018587A3
WO2011018587A3 PCT/FR2010/051702 FR2010051702W WO2011018587A3 WO 2011018587 A3 WO2011018587 A3 WO 2011018587A3 FR 2010051702 W FR2010051702 W FR 2010051702W WO 2011018587 A3 WO2011018587 A3 WO 2011018587A3
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WIPO (PCT)
Prior art keywords
formula
activating
preparation
therapeutic use
fgf receptor
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PCT/FR2010/051702
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English (en)
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WO2011018587A2 (fr
Inventor
Philippe Duchaussoy
Pierre Fons
Alexandre Froidbise
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Sanofi-Aventis
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Priority to RU2012109572/04A priority Critical patent/RU2559629C2/ru
Priority to SG2012010211A priority patent/SG178406A1/en
Priority to BR112012002980A priority patent/BR112012002980A2/pt
Priority to EP10761048A priority patent/EP2464359A2/fr
Priority to KR1020127006509A priority patent/KR20120059552A/ko
Priority to MX2012001945A priority patent/MX2012001945A/es
Priority to CN201080046342.7A priority patent/CN102625704B/zh
Priority to JP2012524264A priority patent/JP5732460B2/ja
Application filed by Sanofi-Aventis filed Critical Sanofi-Aventis
Priority to CA2771055A priority patent/CA2771055C/fr
Priority to AU2010283613A priority patent/AU2010283613B2/en
Publication of WO2011018587A2 publication Critical patent/WO2011018587A2/fr
Publication of WO2011018587A3 publication Critical patent/WO2011018587A3/fr
Priority to US13/369,677 priority patent/US9527930B2/en
Priority to IL218069A priority patent/IL218069A/en

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    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08BPOLYSACCHARIDES; DERIVATIVES THEREOF
    • C08B37/00Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
    • C08B37/006Heteroglycans, 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
    • C08B37/0063Glycosaminoglycans or mucopolysaccharides, e.g. keratan sulfate; Derivatives thereof, e.g. fucoidan
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/737Sulfated polysaccharides, e.g. chondroitin sulfate, dermatan sulfate
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    • C08B37/00Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
    • C08B37/006Heteroglycans, 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
    • C08B37/0063Glycosaminoglycans or mucopolysaccharides, e.g. keratan sulfate; Derivatives thereof, e.g. fucoidan
    • C08B37/0075Heparin; Heparan sulfate; Derivatives thereof, e.g. heparosan; Purification or extraction methods thereof

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Abstract

Oligosaccharides N-sulfates activateurs des récepteurs des FGFs, répondant à la formule (I); dans laquelle; R1, R4, R6 et R8 représentent des groupes -OSO3 - ou hydroxyle, R2 représente un groupe -O-alkyle ou un monosaccharide de formule (II), R3 représente un disaccharide de formule (III), R5 représente un disaccharide de formule (IV), R7 représente un groupe hydroxyle ou un disaccharide de formule (Vl) : R9 représente un groupe hydroxyle ou -O-alkyle ou un disaccharide de formule (VII), où R10 représente un groupe -O-alkyle : Leur préparation et leur application en thérapeutique.
PCT/FR2010/051702 2009-08-14 2010-08-12 OLIGOSACCHARIDES N-SULFATES ACTIVATEURS DES RECEPTEURS DES FGFs, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE WO2011018587A2 (fr)

Priority Applications (12)

Application Number Priority Date Filing Date Title
CN201080046342.7A CN102625704B (zh) 2009-08-14 2010-08-12 活化成纤维细胞生长因子受体的n-硫酸盐低聚糖,其制备,及其治疗用途
BR112012002980A BR112012002980A2 (pt) 2009-08-14 2010-08-12 oligossacarídeo n-sulfatos ativadores dos receptores dos fgfs, o respectivo preparo e a repectiva utilização em terapêutica
EP10761048A EP2464359A2 (fr) 2009-08-14 2010-08-12 OLIGOSACCHARIDES N-SULFATES ACTIVATEURS DES RECEPTEURS DES FGFs, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE
KR1020127006509A KR20120059552A (ko) 2009-08-14 2010-08-12 Fgf 수용체-활성화 n-술페이트 올리고사카라이드, 그의 제조법, 및 그의 치료 용도
MX2012001945A MX2012001945A (es) 2009-08-14 2010-08-12 Oligosacaridos n-sulfatados activadores de los receptores de fgf, su preparacion y su uso en terapeutica.
RU2012109572/04A RU2559629C2 (ru) 2009-08-14 2010-08-12 N-сульфатированные олигосахариды, активирующие рецепторы fgf, их получение и применение в терапии
JP2012524264A JP5732460B2 (ja) 2009-08-14 2010-08-12 Fgf受容体活性化n−硫酸塩オリゴ糖、該オリゴ糖の調製および該オリゴ糖の治療用途
SG2012010211A SG178406A1 (en) 2009-08-14 2010-08-12 Fgf receptor-activating n-sulfate oligosaccharides, preparation thereof, and therapeutic use thereof
CA2771055A CA2771055C (fr) 2009-08-14 2010-08-12 Oligosaccharides n-sulfates activateurs des recepteurs des fgfs, leur preparation et leur application en therapeutique
AU2010283613A AU2010283613B2 (en) 2009-08-14 2010-08-12 FGF receptor-activating N-sulfate oligosaccharides, preparation thereof, and therapeutic use thereof
US13/369,677 US9527930B2 (en) 2009-08-14 2012-02-09 FGF receptor-activating N-sulfate oligosaccharides, preparation thereof, and therapeutic use thereof
IL218069A IL218069A (en) 2009-08-14 2012-02-12 Oligoscride compounds, drug, pharmaceutical, and compound for its use in therapy

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR0903969 2009-08-14
FR0903969A FR2949115B1 (fr) 2009-08-14 2009-08-14 OLIGOSACCHARIDES N-SULFATES ACTIVATEURS DES RECEPTEURS DES FGFs, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US13/369,677 Continuation US9527930B2 (en) 2009-08-14 2012-02-09 FGF receptor-activating N-sulfate oligosaccharides, preparation thereof, and therapeutic use thereof

Publications (2)

Publication Number Publication Date
WO2011018587A2 WO2011018587A2 (fr) 2011-02-17
WO2011018587A3 true WO2011018587A3 (fr) 2011-07-07

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Application Number Title Priority Date Filing Date
PCT/FR2010/051702 WO2011018587A2 (fr) 2009-08-14 2010-08-12 OLIGOSACCHARIDES N-SULFATES ACTIVATEURS DES RECEPTEURS DES FGFs, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE

Country Status (16)

Country Link
US (1) US9527930B2 (fr)
EP (1) EP2464359A2 (fr)
JP (1) JP5732460B2 (fr)
KR (1) KR20120059552A (fr)
CN (2) CN102625704B (fr)
AR (1) AR078093A1 (fr)
AU (1) AU2010283613B2 (fr)
BR (1) BR112012002980A2 (fr)
CA (1) CA2771055C (fr)
FR (1) FR2949115B1 (fr)
IL (1) IL218069A (fr)
MX (1) MX2012001945A (fr)
MY (1) MY160505A (fr)
RU (1) RU2559629C2 (fr)
SG (1) SG178406A1 (fr)
WO (1) WO2011018587A2 (fr)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
GB201516066D0 (en) * 2015-09-10 2015-10-28 Young & Co Llp D Treatment of retinitis pigmentosa

Citations (3)

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WO1992018546A1 (fr) * 1991-04-17 1992-10-29 Glycomed, Inc. Polysaccharides sulfates en tant qu'inhibiteurs de la proliferation cellulaire dans les muscles lisses
FR2800074A1 (fr) * 1999-10-22 2001-04-27 Aventis Pharma Sa Nouveaux oligosaccharides, leur preparation et les compositions pharmaceutiques les contenant
US20040068108A1 (en) * 1996-06-14 2004-04-08 Philippe Duchaussoy Synthetic polysaccharides, process for their preparation and pharmaceutical compositions containing them

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FR2597484B1 (fr) * 1986-04-17 1988-12-23 Sanofi Sa Glycosaminoglycanes de type heparine ou heparane-sulfate dotes d'une activite sur la division et la differentiation cellulaires, leur preparation et leurs applications therapeutiques.
EP0300099A1 (fr) 1987-07-20 1989-01-25 Akzo N.V. Pentasaccharides
IL102758A (en) 1991-08-23 1997-03-18 Akzo Nv Glycosaminoglycanoid derivatives, their preparation and pharmaceutical compositions comprising them
FR2704226B1 (fr) 1993-04-22 1995-07-21 Sanofi Elf 3-desoxy oligosaccharides, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent.
NZ264340A (en) 1993-09-01 1995-04-27 Akzo Nobel Nv Bisconjugate comprising two saccharides and a spacer, use in pharmaceutical compositions
FR2751334B1 (fr) 1996-07-19 1998-10-16 Sanofi Sa Polysaccharides synthetiques, procede pour leur preparation et compositions pharmaceutiques les contenant
FR2773804B1 (fr) 1998-01-19 2000-02-18 Sanofi Sa Polysaccharides de synthese, procede pour leur preparation et compositions pharmaceutiques le contenant
US6617316B1 (en) 1999-10-22 2003-09-09 Aventis Pharma Oligosaccharides, their preparation and pharmaceutical compositions containing them
PT2343077E (pt) * 2001-09-12 2013-08-29 Sigma Tau Res Switzerland Sa Derivados de glicosaminoglicanos totalmente n-dessulfatados como inibidores da heparanase, capazes de atividade antiangiogénica e desprovidos de efeito anticoagulante
RU2333222C2 (ru) * 2002-06-18 2008-09-10 Гликорес 2000 С.Р.Л. Эпимеризованные производные полисахарида к5 с высокой степенью сульфатирования
US7582737B2 (en) * 2004-07-20 2009-09-01 Academia Sinica Orthogonally protected disaccharide building blocks for synthesis of heparin oligosaccharides
FR2873377B1 (fr) 2004-07-23 2006-10-13 Sanofi Synthelabo Derives d'azasucre, inhibiteurs d'heparanases, leur procede de preparation, les compositions en contenant et leur utilisation
FR2949114B1 (fr) * 2009-08-14 2011-08-26 Sanofi Aventis OCTASACCHARIDES N-ACYLES ACTIVATEURS DES RECEPTEURS DES FGFs, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992018546A1 (fr) * 1991-04-17 1992-10-29 Glycomed, Inc. Polysaccharides sulfates en tant qu'inhibiteurs de la proliferation cellulaire dans les muscles lisses
US20040068108A1 (en) * 1996-06-14 2004-04-08 Philippe Duchaussoy Synthetic polysaccharides, process for their preparation and pharmaceutical compositions containing them
FR2800074A1 (fr) * 1999-10-22 2001-04-27 Aventis Pharma Sa Nouveaux oligosaccharides, leur preparation et les compositions pharmaceutiques les contenant

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Title
C. TABEUR ET AL.: "Oligosaccharides corresponding to the regular sequence of heparin: chemical synthesis and interaction with FGF-2", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 7, 1999, pages 2003 - 2012, XP002575365 *
CODEE J D C ET AL: "The synthesis of well-defined heparin and heparan sulfate fragments", DRUG DISCOVERY TODAY: TECHNOLOGIES, ELSEVIER, vol. 1, no. 3, 1 December 2004 (2004-12-01), pages 317 - 326, XP004767969, ISSN: 1740-6749 *

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AU2010283613B2 (en) 2016-03-10
RU2559629C2 (ru) 2015-08-10
RU2012109572A (ru) 2013-09-20
CN102625704A (zh) 2012-08-01
IL218069A (en) 2015-04-30
CA2771055C (fr) 2017-05-09
JP5732460B2 (ja) 2015-06-10
US20120202769A1 (en) 2012-08-09
KR20120059552A (ko) 2012-06-08
IL218069A0 (en) 2012-04-30
MY160505A (en) 2017-03-15
FR2949115A1 (fr) 2011-02-18
MX2012001945A (es) 2012-06-27
BR112012002980A2 (pt) 2016-04-19
FR2949115B1 (fr) 2012-11-02
EP2464359A2 (fr) 2012-06-20
US9527930B2 (en) 2016-12-27
CN104945524A (zh) 2015-09-30
AU2010283613A1 (en) 2012-03-08
AR078093A1 (es) 2011-10-12
CN102625704B (zh) 2015-05-06
JP2013501838A (ja) 2013-01-17
SG178406A1 (en) 2012-03-29
CA2771055A1 (fr) 2011-02-17
WO2011018587A2 (fr) 2011-02-17

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