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    • 3. 发明申请
    • 4-QUINOLINE-3-CARBOXYLIC ACID DERIVATIVES AND THEIR USE AS ANTIBACTERIAL AGENTS
    • 4-QUINOLIN-3-羧酸衍生物及其作为抗菌剂的用途
    • WO1989001933A2
    • 1989-03-09
    • PCT/US1988002938
    • 1988-08-23
    • WARNER-LAMBERT COMPANYCULBERTSON, Townley, PayneDOMAGALA, John, MichaelHAGEN, Susan, ElizabethSANCHEZ, Josheph, Peter
    • WARNER-LAMBERT COMPANY
    • C07D215/56
    • C07D207/08C07D207/09C07D207/12C07D207/20C07D211/34C07D211/52C07D211/70C07D215/56C07D401/04
    • A novel series of quinoline-, naphthyridine- and benzoxazine-carboxylic acids (I), useful as antibacterial agents is described. Novel methods for preparing the compounds as well as novel intermediates are also described as are methods for their formulation and the use thereof in treating bacterial infections. In formula (I), where Z is (II), wherein one endocyclic double bond may be present between any two consecutive ring positions or two alternating or nonalternating endocyclic double bonds may be present in the ring; wherein n, n', n''', and n"" are each independently 0, 1, or 2; n'' is 0, 1, 2, or 3; y is 0 or 1; x is 0 or 1; A and B are each independently CH, CH2, NR7 wherein R7 is hydrogen or R7 is R8CO wherein R8 is alkyl of from one to ten carbon atoms, arylalkyl, aryl wherein the aryl or alkyl may be substituted by hydroxy, halogen, COOH, or CONHR9 where R9 is hydrogen or alkyl of from one to four carbon atoms and when A is NR7, B can be O or S or when B is NR7, A can be absent; (CR13R14)n''' wherein R13 and R14 are each independently hydrogen or lower alkyl and E is hydrogen, alkyl, OR10 wherein R10 is hydrogen or alkyl, NR11R12 wherein R11 and R12 are each independently hydrogen, lower alkyl, cycloalkyl, alkylaryl, alkylheteroaryl, alkanoyl, amidine, peptide, urethane, or R11 and R14 when taken together with the nitrogen to which they are attached form a ring of from three to six carbon atoms or (a), (b), or (c).
    • 描述了一系列可用作抗菌剂的喹啉 - ,萘啶 - 和苯并恶嗪羧酸(I)。 还公开了制备这些化合物的新方法以及新的中间体。 还描述了它们的制剂方法和它们在治疗细菌感染中的用途。 这些新的酸具有其中Z是由式(II)表示,其中桥环双键可以是连续的周期的任何两个位置,或两个双键内环交替或之间存在的式(I)不交替可 目前的周期; 其中n,n',n''和n“'独立地为0,1或2; n“是0,1,2或3; y是0或1; x是0或1; A和B各自独立地为CH,CH 2,NR 7,其中R 7为氢或R 7为R 8 CO,其中R 8为1-10个碳原子的烷基,芳基烷基,芳基,芳基等。 该烷基可以被羟基,卤素,COOH或CONHR9取代,其中R9是氢或具有1至4个碳原子的烷基,并且当A是NR7时,B是O或S,或者当B是 NR7,A可能不存在; 其中R 13和R 14各自独立地为氢或低级烷基,E为氢,烷基,OR 10,其中R 10为氢或烷基,NR 11 R 12,其中R 11和R 12各自独立地为 氢,低级烷基,环烷基,烷基芳基,烷基杂芳基,生物碱,脒,肽,氨基甲酸酯或R 11和R 14与它们所连接的氮一起形成环 (a),(b)或(c)。