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    • 10. 发明专利
    • Semisynthetic glycopeptides with antibiotic activity
    • 具有抗生素活性的半胱氨酸蛋白酶
    • JP2009102446A
    • 2009-05-14
    • JP2009035666
    • 2009-02-18
    • Novartis Vaccines & Diagnostic Incノバルティス ヴァクシンズ アンド ダイアグノスティクス, インコーポレイテッド
    • CHU DANIELPREOBRAZHENSKAYA MARIAPRINTSEVSKAYA SVETLANAOLSUFYEVA EUGENIA
    • C07K7/54A61K38/00A61P31/04
    • A61K38/14C07K9/008
    • PROBLEM TO BE SOLVED: To identify new derivative compounds having improved effectiveness and unpredictable selectivity for targeted microorganisms. SOLUTION: Semisynthetic glycopeptides having antibacterial activity are produced based on modifications of eremomycin, A82846B, vancomycin, teicoplanin, or A-40,926 scaffolds, acylation of the sugar moieties on these scaffolds with certain acyl groups (in particular, amino acids and their derivatives); and/or conversion of an acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides; or having a combination of an alkylation modification of the amino substituent on the amino-substituted sugar moiety on these scaffolds with certain alkyl groups or acylation modification of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain alkyl groups (including β-amino acids or their derivatives), and conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. COPYRIGHT: (C)2009,JPO&INPIT
    • 要解决的问题:鉴定具有改善的有效性和不可预测的靶向微生物选择性的新衍生化合物。 解决方案:具有抗菌活性的半合成糖肽基于依依霉素,A82846B,万古霉素,替考拉宁或A-40,926支架的修饰产生,在这些支架上的糖部分用某些酰基(特别是氨基酸和它们的 衍生物); 和/或将这些支架的大环上的酸部分转化为某些取代的酰胺; 或具有这些支架上的氨基取代的糖部分上的氨基取代基的烷基化修饰与某些烷基的组合或在该支架上的氨基取代的糖部分上的氨基取代基的某些烷基(包括β - 氨基酸或其衍生物),并将该支架的大环上的酸部分转化为某些取代的酰胺。 版权所有(C)2009,JPO&INPIT