Mutilin-derivative substituted at position 12

Details Mutilin-derivative substituted at position 12 Mutilin-derivative substituted at position 12

C - Chemistry, Metallurgy

07

D

C07D 487/08 (2006.01) A61K 31/407 (2006.01) A61P 31/04 (2006.01) C07C 49/487 (2006.01) C07C 49/517 (2006.01)

Patent

CA 2591898

There are provided 12-position substituted derivatives, and production intermediates thereof, represented by the following chemical formula (1) which are novel analogues of mutilin capable of exhibiting powerful and wide antibacterial activities to gram-positive and gram-negative bacteria including various drug-resistant bacteria and thus being promising in application to usages as a therapeutic agent for infectious diseases. (1) wherein R1 is a hydrogen atom, formyl, lower alkyl, etc., and R2 is a hydrogen atom, lower alkyl, etc. with the proviso that with respect to R1, ethyl and vinyl are excluded.

La présente invention concerne des dérivés substitués en position 12 et la production d~intermédiaires desdits dérivés représentés par la formule chimique suivante (1) et constituant de nouveaux analogues de la mutiline capables de présenter une activité antibactérienne puissante et de grande échelle contre les bactéries à gram positif et à gram négatif, y compris diverses bactéries résistantes aux antibiotiques, et s~avérant par conséquent prometteurs employés en tant qu~agent thérapeutique pour les maladies infectieuses. (1), dans laquelle R1 est un atome d~hydrogène, formyl, alkyle inférieur, etc. et R2 est un atome d~hydrogène, alkyle inférieur, etc., sous réserve de l~exclusion de l~éthyle et du vinyle en ce qui concerne R1.

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