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Title:
FGF RECEPTOR-ACTIVATING N-ACYL OCTASACCHARIDES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2011/018588
Kind Code:
A3
Abstract:
The invention relates to FGF receptor-activating N-acyl octasaccharides having Formula (I), wherein: R1 is an O-alkyl group optionally replaced by one or more aryl or cycloalkyl groups, R2 is an OSO3- or hydroxyl group, R3 is an alkyl, cycloalkyl, or alky-cycloalkyl group, R4 is a disaccharide having Formula (II), R6 is a disaccharide having Formula (III), and R8 is a disaccharide having Formula (IV), where R5, R7, and R9 have OSO3 or hydroxyl groups. The invention further relates to the preparation of said octasaccharides and to the therapeutic use thereof.

Inventors:
DRIGUEZ, Pierre Alexandre (Département Brevets174 avenue de France, Paris, F-75013, FR)
DUCHAUSSOY, Philippe (Département Brevets174 avenue de France, Paris, F-75013, FR)
FONS, Pierre (Département Brevets174 avenue de France, Paris, F-75013, FR)
HERBERT, Corentin (Département Brevets174 avenue de France, Paris, F-75013, FR)
LASSALLE, Gilbert (Département Brevets174 avenue de France, Paris, F-75013, FR)
Application Number:
FR2010/051703
Publication Date:
July 07, 2011
Filing Date:
August 12, 2010
Export Citation:
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Assignee:
SANOFI-AVENTIS (174 avenue de France, Paris, F-75013, FR)
DRIGUEZ, Pierre Alexandre (Département Brevets174 avenue de France, Paris, F-75013, FR)
DUCHAUSSOY, Philippe (Département Brevets174 avenue de France, Paris, F-75013, FR)
FONS, Pierre (Département Brevets174 avenue de France, Paris, F-75013, FR)
HERBERT, Corentin (Département Brevets174 avenue de France, Paris, F-75013, FR)
LASSALLE, Gilbert (Département Brevets174 avenue de France, Paris, F-75013, FR)
International Classes:
C08B37/00; A61K31/737; C07H13/04; C07H13/12; C07H15/203
Domestic Patent References:
WO1992018546A11992-10-29
Foreign References:
FR2800074A12001-04-27
US20040068108A12004-04-08
Other References:
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
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, XP002575370
KOVENSKY J ET AL: "Binding of Heparan Sulfate to Fibroblast Growth Factor-2 Total Synthesis of a Putative Pentasaccharide Binding Site", TETRAHEDRON ASYMMETRY, PERGAMON PRESS LTD, OXFORD, GB, vol. 7, no. 11, 8 November 1996 (1996-11-08), pages 3119 - 3128, XP004068971, ISSN: 0957-4166, DOI: DOI:10.1016/0957-4166(96)00412-0
Attorney, Agent or Firm:
BOURON, Estelle (Département Brevets174 avenue de France, Paris, F-75013, FR)
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