Title:
【発明の名称】シアル酸/フコース含有薬剤
Document Type and Number:
Japanese Patent JPH10500948
Kind Code:
A
Abstract:
Compounds that are synthetically inexpensive to make relative to the naturally occuring selectin ligands and that retain selectin binding activity are described that have a three-dimensionally stable configuration for sialic acid and fucose, or analogs or derivatives of these groups, such that sialic acid and fucose are separated by a non-carbohydrate linker that permits binding between those groups and the selectins, such compounds being represented by general structural formula I(a) wherein m and n are independently an integer of from 1 to 5, Y and Z are independently a connecting moiety selected from the group consisting of -CH2-, -O-, -S-, -NR' and -NR'R"-(wherein R' and R" are independently H or an alkyl containing 1 to 4 carbon atoms); X is a connecting moiety which is selected from the group consisting of -O-, -S- and -N-; and -R''' may be -R'' or any moiety which does not interfere with the three-dimensional configuration of A or B so as to interfere with selectin binding and is preferably a moiety selected from the group consisting of -OR'', -SR'', -I, -N3, and -NR'R'', and A is selected from the group consisting of alpha and beta forms of sialic acid, Kemp's acid, Quinic acid, Glyceric acid, Lactic acid and acetic acid, and esters thereof and B is selected from the group consisting of alpha and beta forms of L-Fucose and esters and substituted forms thereof wherein one or more of the -OH groups is independently -F, or -NR, R wherein R and R are independently an alkyl containing 1 to 5 carbons.
Inventors:
Farguni, Dasgupta
Massen, John Henry
Massen, John Henry
Application Number:
JP52960695A
Publication Date:
January 27, 1998
Filing Date:
May 18, 1994
Export Citation:
Assignee:
Glycomed Incorporated
International Classes:
G01N33/566; A61K31/70; A61K31/7028; A61K49/00; A61P29/00; A61P35/00; A61P37/06; A61P43/00; C07H15/04; G01N33/53; G01N33/569; G01N33/66; G01N33/68; G01N33/94; (IPC1-7): C07H15/04; A61K31/70; A61K49/00; G01N33/566
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)