10-(3-cyclopropylaminomethyl-1-pyrrolidinyl)pyridobenzoxazin...

C - Chemistry – Metallurgy – 07 – D

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C07D 498/06 (2006.01) A61K 31/5383 (2006.01) A61P 31/04 (2006.01)

Patent

CA 2478763

A compound represented by the general formula (I): (I) wherein R1 represents methyl, fluoromethyl, methoxymethyl, acetoxymethyl, hydroxymethyl, or methylene; R2 represents hydrogen, C1-3 alkyl, or a pharmaceutically acceptable ester group of a cation and a prodrug; R3 represents hydrogen or halogeno; R4 represents hydrogen, C1-3 alkyl, fluoromethyl, trifluoromethyl, or fluorine; and R5 represents hydrogen or fluorine. It has excellent antibacterial activity against gram-positive bacteria, in particular, resistant bacteria such as MRSA, PRSP, and VRE.

L'invention concerne un composé représenté par la formule générale (I), dans laquelle R1 représente méthyle, fluorométhyle, méthoxyméthyle, acétoxyméthyle, hydroxyméthyle, ou méthylène ; R2 représente hydrogène, alkyle C¿1-3?, ou un groupe ester pharmaceutiquement acceptable d'un cation et un promédicament ; R3 représente hydrogène ou halogéno ; R4 représente hydrogène, alkyle C¿1-3?, fluorométhyle, trifluorométhyle, ou fluor ; et R5 représente hydrogène ou fluor. Ce composé présente une excellente activité antibactérienne contre les bactéries Gram positif, en particulier contre les bactéries résistantes, telles que MRSA, PRSP, et VRE.

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