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CARBOHYDRATE LIGANDS THAT BIND TO ANTIBODIES AGAINST GLYCOEPITOPES OF GLYCOSPHINGOLIPIDS
专利权人:
ウニヴェルズィテート バーゼル
发明人:
ヘレンドルフ, ルーベン,エルンスト, ビート,ステック, アンドレアス,フィスター, ヘレーネ,ナヴァーラ, ジュリオ
申请号:
JP2018513509
公开号:
JP2018534246A
申请日:
2016.09.14
申请国别(地区):
JP
年份:
2018
代理人:
摘要:
The invention relates to carbohydrate ligands and moieties, respectively, mimicking glycoepitopes comprised by glycosphingolipids of the nervous system, particularly glycoepitopes comprised by glycosphingolipids of the cerebroside, the globoside-, the ganglioside- and the sulfoglucuronyl paragloboside type, which are bound by anti-glycan antibodies associated with neurological diseases. The invention further relates to the use of these carbohydrate ligands/moieties, in diagnosis as well as for the treatment of neurological diseases associated with anti-glycan antibodies. In particular, the invention relates to compounds of formula (I) and (II) and to therapeutically acceptable polymers comprising a multitude of these compounds, including polymers with loading of one compound of formula (I) or (II) or combinations of several compounds of formula (I), and/or (II). The compounds of formula (I) are defined as: formula (I), wherein RI1 is Z or (AA) or (BB) or (CC) or (DD) wherein RI2 is H, SO3H, or (EE) or (FF) or (GG) or (HH) or (JJ) or (KK) or (LL), wherein RI3 is H or (MM) wherein RI4 is H or (NN) or (OO), wherein RI5 and RI6 are independently H or (EE) wherein RI7 is H or (EE) or (FF) and compounds of formula (II) are defined as: formula (II), wherein RII1 is Z or (PP), wherein RII2 is Z or (QQ) or (RR) or (SS) or (TT), wherein Z is -N(Ra)-A-B-CH2-(CH2)q-SH, wherein Ra is H, C1-C4-alkyl, C1-C4-alkoxy, CH2C6H5, CH2CH2C6H5, OCH2C6H5, or OCH2CH2C6H5 A is C1-C7-alkylene, C1-C7-alkoxy, C1-C4-alkyl–(OCH2CH2)pO–C1-C4-alkyl, or C1-C7-alkoxy-Rb, wherein Rb is an optionally substituted aryl or an optionally substituted heteroaryl, and wherein p is 0 to 6, preferably p is 1, 2 or 3, and further preferably p is 1 B is NHC(O), S or CH2 q is 0 to 6, preferably q is 1, 2, 3 or 4, and further preferably q is 1 or 2.La présente invention concerne des ligands et des fractions glucidiques respectivement, qui imitent des glycoépitopes constitués par des glycosphingolipides du système ne
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