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    • 4. 发明申请
    • PYRIDO[3,2,1-i,j][3,1]BENZOXAZINE DERIVATIVES
    • 吡啶并[3,2,1-I,J] [3,1]苯并恶嗪
    • WO1996001829A1
    • 1996-01-25
    • PCT/EP1995002510
    • 1995-06-28
    • BAYER AKTIENGESELLSCHAFTHALLENBACH, WernerHIMMLER, ThomasJAETSCH, ThomasMIELKE, BurkhardBREMM, Klaus, DieterENDERMANN, RainerPIRRO, FranzSTEGEMANN, MichaelWETZSTEIN, Heinz-Georg
    • BAYER AKTIENGESELLSCHAFT
    • C07D498/06
    • C07D498/06C07C17/16C07D519/00C07C21/19
    • The present invention relates to novel pyrido[3,2,1-i,j][3,1]benzoxazine derivatives of the formula (I) in which R is hydrogen or C1-C4 alkyl possibly substituted by hydroxy or halogen; R is hydrogen or methyl independently of R ; R is hydrogen or C1-C4 alkyl; R is hydrogen or methyl; R is hydrogen, alkyl with 1 to 4 carbon atoms, possibly substituted by hydroxy, methoxy, amino, methyl amino or dimethyl amino or (5-methyl-2-oxo-1,3-dioxol-4-yl)-methyl; X is hydrogen or halogen; Z is radicals of the structures ((a), (b), (c)) in which R is hydrogen, hydroxy, -NR R , hydroxy methyl or -CH2-NR R , carboxyl, methoxy carbonyl or ethoxy carbonyl, where R is hydrogen, possibly hydroxy-substituted C1-C3 alkyl, alkoxy carbonyl with 1 to 4 C atoms in the alkoxy part or C1-C3-acyl, and R is hydrogen or methyl; R is hydrogen, straight or branched chained C1-C3 alkyl or cyclopropyl; R is hydrogen or methyl; R is hydrogen or methyl; R is hydrogen, methyl or radicals of the structures -CH=CH-CO2R , -CH2-CH2-CO2R , -CH2-CO-CH3, -CH2-CH2-CN; R is methyl or ethyl; and B is -CH2-, O or a direct bond, their production and use for the therapy or the prevention of bacterial infections.
    • 本发明涉及新的吡啶并[3,2,1-I,J] [3,1]式(I),其中R <1>代表氢或任选经羟基或卤素取代的C1-C4烷基的苯并恶嗪衍生物 ,R <2>是,独立于R <1>表示氢或甲基,R <3>是氢或C1-C4烷基,R <3“>是氢或甲基,R <4>是氢,任选 被羟基,甲氧基,氨基,甲氨基或二甲氨基,具有1至4个碳原子或(5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基) - 甲基烷基取代的,X <1>是氢或卤素 ; Z表示的结构((a)中,(B),(C)),其中R <7>是氢,羟基,-NR <10> - [R <11>,羟甲基或-CH 2 NR <10>的R基团 <11>,羧基,甲氧羰基或乙氧羰基,其中R <10>代表氢,任选地羟基取代的C1-C3烷基,具有在烷氧基部分或C1-C3酰基1至4个碳原子的烷氧基羰基,并且R < 11>是氢或甲基,R <8>为氢,直链或支链的C1-C3烷基或环丙基; [R <9>是氢或甲基,R <6>是氢或甲基,R <5>是氢,甲基或结构的基团-CH = CH-CO 2 R <5“>,-CH2-CH2-CO 2 R < 5 '>,-CH2-CO-CH3,-CH2-CH2-CN,R <5'>是甲基或乙基; B表示-CH 2 - ,O或直键,其制备方法及其用于细菌感染的治疗或预防的用途。