C - Chemistry – Metallurgy – 07 – G
Patent
C - Chemistry, Metallurgy
07
G
C07G 11/00 (2006.01)
Patent
CA 2599336
Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of a rearranged vancomycin or desmethyl-vancomycin scaffold, in particular, alkylation or acylation of the amino substituent on the amino- substituted sugar moiety on this scaffold with certain acyl groups; and/or conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. Also provided are methods for synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.
L'invention concerne des glycopeptides semi-synthétiques présentant une activité antibactérienne, qui sont fondés sur des modifications d'une structure vancomycine ou desméthylvancomycine réagencée, en particulier, sur l'alkylation ou l'acylation du substituant amino sur le fragment sucre amino-substitué sur ladite structure avec certains groupes acyle ; et/ou la sur conversion du fragment acide sur l'anneau macrocyclique de ladite structure en certains amides substitués. L'invention concerne également des procédés de synthèse desdits composés, des compositions pharmaceutiques contenant ceux-ci, ainsi que des procédés d'utilisation de ceux-ci pour le traitement et/ou la prophylaxie de certaines maladies, en particulier d'infections bactériennes.
Bai Yu
Chu Daniel
Lei Yaohui
Ni Zhi-Jie
Wang John Jian-Xin
Borden Ladner Gervais Llp
Novartis Vaccines And Diagnostics Inc.
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