Title:
PHOSPHORYL MANNOSE PENTASACCHARIDE AND DERIVATIVES THEREOF, AND PREPARATION METHOD AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2017/071152
Kind Code:
A1
Abstract:
Provided are a phosphoryl mannose pentasaccharide as shown in formula (I) and derivatives of the phosphoryl mannose pentasaccharide as shown in formulas (II)-(XI), and a preparation method thereof. In the preparation method of this invention, by means of designing the hydroxy protective group of the mannose thioglycoside donor to regulate the reactivity, side reactions in the glycosylation reaction are few, and the reaction yield is high, thus being suitable for large-scale modular synthesis. The phosphoryl mannose pentasaccharide and derivatives thereof in the present invention have the activity for inhibiting angiogenesis, and have an application prospect as anti-tumour drugs.
Inventors:
HU WENHAO (CN)
ZHOU JUN (CN)
ZHOU JUN (CN)
Application Number:
PCT/CN2016/077370
Publication Date:
May 04, 2017
Filing Date:
March 25, 2016
Export Citation:
Assignee:
RUDONG RUIEN PHARMACEUTICAL TECH CO LTD (CN)
International Classes:
C07H11/04; A61P35/00; C07H1/00; C07H15/04; C07H15/203
Domestic Patent References:
| WO2012167434A1 | 2012-12-13 |
Other References:
GU, GUOFENG ET AL.: "Synthesis of a 6V-Sulfated Mannopentasaccharide Analogue Related to PI-88", CARBOHYDRATE RESEARCH, vol. 339, 31 December 2004 (2004-12-31), XP004500597
TOMISLAV, K. ET AL.: "Synthesis, Biological Activity, and Preliminary Pharmacokinetic Evaluation of Analogues of a Phosphosulfomannan Angiogenesis Inhibitor (PI-88", J. MED. CHEM., vol. 48, no. 26, 17 November 2005 (2005-11-17), pages 8229 - 8236, XP055381748
PAROLIS, L.A.S. ET AL.: "The Extracellular Polysaccharide of Pichia (Hansenula) Holstii NRRL Y-2448: the Phosphorylated Side Chains", CARBOHYDRATE RESEARCH, vol. 309, no. 1, 31 December 1998 (1998-12-31), pages 78 - 87, XP027355043
YU , GUANGLI ET AL.: "Preparation and Anticoagulant Activity of the Phosphosulfomannan PI-88", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 37, 31 December 2002 (2002-12-31), pages 783 - 791, XP004393911
TOMISLAV, K. ET AL.: "Synthesis, Biological Activity, and Preliminary Pharmacokinetic Evaluation of Analogues of a Phosphosulfomannan Angiogenesis Inhibitor (PI-88", J. MED. CHEM., vol. 48, no. 26, 17 November 2005 (2005-11-17), pages 8229 - 8236, XP055381748
PAROLIS, L.A.S. ET AL.: "The Extracellular Polysaccharide of Pichia (Hansenula) Holstii NRRL Y-2448: the Phosphorylated Side Chains", CARBOHYDRATE RESEARCH, vol. 309, no. 1, 31 December 1998 (1998-12-31), pages 78 - 87, XP027355043
YU , GUANGLI ET AL.: "Preparation and Anticoagulant Activity of the Phosphosulfomannan PI-88", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 37, 31 December 2002 (2002-12-31), pages 783 - 791, XP004393911
Attorney, Agent or Firm:
MSJ LAW OFFICE (CN)
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