6-o-substituted macrolides having antibacterial activity

C - Chemistry – Metallurgy – 07 – H

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C07H 17/08 (2006.01) A61K 31/70 (2006.01) A61K 31/7042 (2006.01) A61P 31/04 (2006.01)

Patent

CA 2367431

The instant invention provides novel macrolide compounds and compositions useful in treating bacterial infections. Also provided are processes for preparing same. These macrolides are substituted on the 6-O- position with X'-Y'-Z', wherein X' is selected from the group consisting of C1-C10 alkyl, C3-C10 alkenyl, and C3-C10 alkynyl; Y' and Z' are independently selected from the group consisting of: (c) optionally substituted aryl, and (d) optionally substituted heteroaryl, with the proviso that both Y' and Z' are not both phenyl, and with the further proviso that Y' is not isoxazole when Z' is thiophenyl.

L'invention porte sur un nouveau composé de macrolides, sur des compositions servant à traiter les infections bactériennes, ainsi que sur leurs procédés de préparation. Lesdits macrolides sont substitués en position 6-O par X'-Y'-Z', où X' est choisi parmi C1-C10 alkyle, C3-C10 alcényle, et C3-C10 alkynyle; Y' et Z' sont choisis indépendamment parmi: (c) aryle facultativement substitué, et (d) hétéroaryle facultativement substitué, sous réserve que Y' et Z' ne soient pas tous deux phényle, et que Y' ne soit pas isoxazole quand Z' est thiophényle.

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