Antibiotic 107891, its factors a1 and a2, pharmaceutically...

C - Chemistry – Metallurgy – 12 – N

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C12N 1/20 (2006.01) A23K 1/17 (2006.01) A61K 9/14 (2006.01) A61K 38/16 (2006.01) A61P 31/04 (2006.01) C07K 1/14 (2006.01) C07K 14/195 (2006.01) C12P 1/04 (2006.01) C12P 21/02 (2006.01)

Patent

CA 2593801

The invention relates to an antibiotic substance of microbial origin, arbitrarily denominated antibiotic 107891 which is produced by fermentation of Microbispora sp. ATCC PTA-5024, the pharmaceutically acceptable salts and compositions thereof, and their use as an antibacterial agent having inhibitory activity versus susceptible microbes. Antibiotic 107891, which is a complex comprising two Factors, denominated Factors A1 and A2, has a peptide structure containing lanthionine and methyllanthionine as constituents which are typical characteristics of the antibiotics of the lantibiotics group. Antibiotic 107891 and its Factors A1 and A2 show a good antibacterial activity against Gram-positive bacteria including methicillin resistant and vancomycin resistant strains, and is active also against some Gram-negative bacteria such as M. catharralis, Neisseria species and H. influenzae and Mycobacteria.

L'invention concerne une substance antibiotique d'origine microbienne, arbitrairement désignée sous le nom d'antibiotique 107891, obtenu par fermentation de Microbispora sp. ATCC PTA-5024, les sels et compositions acceptables d'un point de vue pharmaceutique de celui-ci, et leur utilisation comme agents antibactériens à activité d'inhibition contre des microbes potentiels. L'antibiotique 107891, qui est un complexe comprenant deux facteurs désignés sous le nom de facteurs A1 et A2, présente une structure peptidique contenant de la lanthionine et de la méthyllanthionine comme constituants, caractérisant les antibiotiques du groupe des lantibiotiques. L'antibiotique 107891 et ses facteurs A1 et A2 possèdent une bonne activité antibactérienne contre les bactéries gram positif, y compris les souches résistant à la méthicilline et à la vancomycine, et est également actif contre certaines bactéries gram-négatif telles que M. catharralis, Neisseria, H. influenzae et les mycobactéries.

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