发明名称 Pyrido(3,2,1-IJ)-1,3,4-benzoxadiazine derivatives
摘要 The invention is concerned with tricyclic compounds of the 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 heterocyclic ring may further contain -NR7-, -O-, -S-, -SO-, -SO2- or -NR7-CO-, and also 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 formula -(CH2)nCOR8 (II) in which n is an integer from 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, intermediates useful in said process, and methods of using them. The end products have antimicrobial activity.
申请公布号 US4864023(A) 申请公布日期 1989.09.05
申请号 US19880236822 申请日期 1988.08.26
申请人 HOFFMANN-LA ROCHE INC. 发明人 YOKOSE, KAZUTERU;SHIMMA, NOBUO;KAMATA, MIKAYO;AOKI, MASAHIRO;OHTSUKA, TATSUO
分类号 C07D215/58;C07D498/06;C07D521/00 主分类号 C07D215/58
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