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    • 1. 发明申请
      WO1998025932A1 ANTIBACTERIAL AGENTS 审中-公开
    • ANTIBACTERIAL AGENTS
    • 抗菌剂
    • WO1998025932A1
    • 1998-06-18
    • PCT/US1997022356
    • 1997-12-05
    • WARNER-LAMBERT COMPANY , DOMAGALA, John, Michael , ELLSWORTH, Edmund, Lee , STIER, Michael, Andrew , HUANG, Liren , MICETICH, Ronald, George , SINGH, Rajeshwar , WRIGLEY, Stephen, Keith , WANG, Shouming , ROE, Michael , THORNTON, David, Michael
    • WARNER-LAMBERT COMPANY
    • C07D498/04
    • C07D487/04 , C07D513/04
    • Described are antibacterial agents of formula (I): X is O, S or N-R8; R1, R2, R3 and R8 are independently H, straight or branched alkyl of 1-6 carbons, cycloalkyl of 3-6 carbons, alkenyl or alkynyl of from 2 to 6 atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur, or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR2, NR'COR', CN, CO2R' or CONR2', halogen, CN, CO2R, COR, CON(R)2, CON(R")2, SR, SON, SCO2R or SCON(R)2; R4 is H, straight or branched alkyl of from 1-6 carbon atoms, alkenyl or alkynyl of from 2 to 6 atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR2, NR'COR', CN, CO2R' or CONR2', halogen, CN, NO2, N(R)2, NRCOR, NRCOR", COR, CO2R, CON(R)2, CON(R")2, NRCON(R)2, NRCO2R; R5 is 1-6 straight or branched alkyl, a cycloalkyl of 3-6 carbons, alkenyl or alkynyl of from 2 to 6 atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR2, NR'COR', CN, CO2R' or CONR2', halogen, OR, N(R)2, NRCOR, NRCOR", COR, CON(R)2, CON(R")2, SR or SO2R; R6, R7 are independently H, straight or branched alkyl of 1-6 carbons, cycloalkyl of 3-6 carbons, COR, COR", SO2NR2, CONR2 and these may be optionally substituted by any of the groups listed for R5; R is H, straight or branched alkyl of 1-6 carbon atoms, cycloalkyl of from 3-6 carbon atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur, or pheny, all of which may be optionally substituted by halogen, OR', NR'2, NR'COR', CN, CO2R', CONR'2; R' is H, alkyl of from 1-3 carbon atoms or Ph; R" is part of a naturally occurring amino acid connected via an amide or acyl bond as determined by the formula; halogen is any one of fluoro, chloro, bromo or iodo; or a pharmaceutically acceptable salt.
    • 描述了式（I）的抗菌剂：X是O，S或N-R8; R1，R2，R3和R8独立地为H，1-6个碳的直链或支链烷基，3-6个碳原子的环烷基，2-6个碳原子的烯基或炔基，5-8个原子的杂环，1-3个 杂原子作为氮，氧或硫或苯基，所有这些环可以任选被卤素，OR，NR 2，NR'COR'，CN，CO 2 R'或CONR 2'，卤素，CN，CO 2 R，COR ，CON（R）2，CON（R“）2，SR，SON，SCO 2 R或SCON R 2; R 4是H，1-6个碳原子的直链或支链烷基，2至6的烯基或炔基 原子，5-8个原子与1-3个杂原子作为氮原子的杂环，氧或硫或苯基，所有这些环可以任选地被卤素OR，NR 2，NR'COR'，CN， CO 2 R，CONR 2，CON（R“）2，NRCON（R）2，NRCO 2 R; R 5是 1-6个直链或支链烷基，3-6个碳原子的环烷基，2-6个碳原子的烯基或炔基，5-8个原子的杂环和1-3个杂原子 作为氮，氧或硫或苯基，所有这些环可以任选被卤素，OR，NR 2，NR'COR'，CN，CO 2 R'或CONR 2'，卤素，OR，N（R） 2，NRCOR，NRCOR“，COR，CON（R）2，CON（R”）2，SR或SO2R; R 6，R 7独立地是H，1-6个碳的直链或支链烷基，3-6个碳的环烷基，COR，COR“，SO2NR2，CONR2，并且它们可以任选被R5所列的任何基团取代; R是H ，1-6个碳原子的直链或支链烷基，3-6个碳原子的环烷基，5-8个原子的杂环，1-3个杂原子作为氮，氧或硫或苯基，所有这些可以是任选的 被卤素取代，OR'，NR'2，NR'COR'，CN，CO2R'，CONR'2; R'是H，1-3个碳原子的烷基或Ph; R“是天然存在的氨基 通过由式决定的酰胺或酰基键连接酸; 卤素是氟，氯，溴或碘中的任何一种; 或药学上可接受的盐。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 5. 发明申请
      WO1989001933A2 4-QUINOLINE-3-CARBOXYLIC ACID DERIVATIVES AND THEIR USE AS ANTIBACTERIAL AGENTS 审中-公开
    • 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 COMPANY , CULBERTSON, Townley, Payne , DOMAGALA, John, Michael , HAGEN, Susan, Elizabeth , SANCHEZ, Josheph, Peter
    • WARNER-LAMBERT COMPANY
    • C07D215/56
    • C07D207/08 , C07D207/09 , C07D207/12 , C07D207/20 , C07D211/34 , C07D211/52 , C07D211/70 , C07D215/56 , C07D401/04
    • 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）。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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