Pyrido [3,2,1,ij]-1,3,4-benzoxadiazine derivatives

Details Pyrido [3,2,1,ij]-1,3,4-benzoxadiazine derivatives Pyrido [3,2,1,ij]-1,3,4-benzoxadiazine derivatives

C - Chemistry, Metallurgy

07

D

167/180, 260/244

C07D 498/06 (2006.01) A61K 31/535 (2006.01) A61K 31/55 (2006.01) C07D 215/58 (2006.01) C07D 521/00 (2006.01)

Patent

CA 1336905

The invention is concerned with tricyclic compounds of the general formula Image (I) wherein R1 is a hydrogen atom or a carboxy-protecting radical; R2 is a hydrogen atom or a lower alkyl radical which may be substituted with a halogen atom; R3 and R4 independently are a hydrogen atom or a lower alkyl radical which may be substituted with a hydroxy radical or a substituted or unsubstituted amino radical; X is a halogen atom; and R5 and R6 are independently a hydrogen atom or a lower alkyl radical which may be substituted with a hydroxy radical, a lower alkoxy radical or a substituted or unsubstituted amino radical; or R5 and R6, taken together with the adjacent nitrogen atom, may form a 5 to 7 membered heterocyclic ring which may be substituted with one or more substituents at the carbon atom(s), and the hetero- cyclic ring may further contain -NR7-, -O-, -S-, -SO-, -SO2- or -NR7-CO-, [R7 is a hydrogen atom, a lower alkenyl radical, a lower alkyl or aralkyl radical which may be substituted, or a radical represented by the general formula -(CH2)nCOR8 (II) (in which n is 0 to 4 and R8 is a hydrogen atom, a lower alkoxy radical, or an amino, lower alkyl or aryl radical which may be substituted)], as well as pharmaceutically acceptable salts thereof, and hydrates or solvates of the compounds of the formula I or their salts. Also included is a process for the manufacture of these compounds, pharmaceutical preparations containing them and intermediates useful in said process. The end products have antimicrobial antivity.

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