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42. 发明授权

US6001819A Bacterial inhibition with an oligosaccharide compound 失效
标题翻译：用寡糖化合物进行细菌抑制
公开(公告)号：US6001819A
公开(公告)日：1999-12-14
申请号：US54890
申请日：1998-04-03
申请人： Paul M. Simon , David Zopf , Roger A. Barthelson , Karl F. Johnson
发明人： Paul M. Simon , David Zopf , Roger A. Barthelson , Karl F. Johnson
IPC分类号： C12P19/26 , A61K9/12 , A61K31/70 , A61K31/7008 , A61K31/7012 , A61K31/715 , A61P11/00 , A61P27/16 , A61P29/00 , A61P31/04 , C07H3/06 , C07H5/04 , C07H7/027 , A01N43/04
CPC分类号： A61K31/702 , A61K31/715 , C07H3/06 , Y10S514/885
摘要： The present invention is directed to compositions for the treatment of respiratory infections caused by a bacteria selected from the group consisting of S. pneumoniae, H. influenzae, H. parainfluenza, Burkholderia (Pseudomonas) cepacia, and a mixture thereof, comprising a binding inhibiting effective amount of the compound of Formula I, ##STR1## where R.sub.1 is H, (.beta.-1)GalNAc-, SO.sub.3 B (where B is H or a cation) or a sialic acid of Formula II; ##STR2## where R.sub.6, R.sub.7, R.sub.8, and R.sub.10 are each independently H, C.sub.1-6 acyl, lactyl, C.sub.1-6 alkyl, sulfate, phosphate, anhydro, a sialic acid of Formula II, (.alpha.-1)Fuc, (.beta.-1)Glc or (.beta.-1)Gal;R.sub.9 is NH--C.sub.1-6 acyl, glycolylamido, amino or hydroxyl; andA is H or a cation;R.sub.2 is H or (.alpha.-1)Fuc-;R.sub.3 and R.sub.4 are each independently OH or NHAc;R.sub.5 is H, SO.sub.3 B (where B is H or a cation), or a sialic acid of Formula II as defined above; ##STR3## Y is a chemical bond or a linking group; Z is H or a multivalent support;m is 0 or 1; andp is an integer of 1 to 1,000; with the proviso that the compound is not Gal.beta.1-4-GlcNAc.beta.1-3-Gal.beta.1-4-Glc.
摘要翻译：本发明涉及用于治疗由选自肺炎链球菌，流感嗜血杆菌，副流感病毒，伯克霍尔德氏菌（Pseudomonas））洋葱的细菌及其混合物引起的呼吸道感染的组合物，其包含结合抑制式（I）化合物，其中R1为H，（β-1）GalNAc-，SO3B（其中B为H或阳离子）或式Ⅱ的唾液酸; 其中R 6，R 7，R 8和R 10各自独立地为H，C 1-6酰基，乳酰基，C 1-6烷基，硫酸酯，磷酸酯，脱水，式II的唾液酸，（α-1）Fuc，（β-1 ）Glc或（β-1）Gal; R9是NH-C1-6酰基，乙酰氨基，氨基或羟基; A为H或阳离子; R2是H或（α-1）Fuc-; R3和R4各自独立地为OH或NHAc; R5是H，SO3B（其中B是H或阳离子）或如上定义的式II的唾液酸; Y是化学键或连接基团; Z是H或多价载体; m为0或1; p为1〜1000的整数。条件是该化合物不是Galβ1-4-GlcNAcβ1-3-Galβ1-4-Glc。

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