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    BENZO[5.6]PYRANO[2.3.4-IJ]QUINOLIZINE AND BENZO[5.6]THIOPYRANO[2.3.4-IJ]QUINOLIZINE DERIVATIVES AS ANTIBACTERIAL AND ANTINEOPLASTIC AGENTS
    3.
    发明申请
    BENZO[5.6]PYRANO[2.3.4-IJ]QUINOLIZINE AND BENZO[5.6]THIOPYRANO[2.3.4-IJ]QUINOLIZINE DERIVATIVES AS ANTIBACTERIAL AND ANTINEOPLASTIC AGENTS 审中-公开
    苯并[5.6] PYRANO [2.3.4-IJ]喹唑啉和苯并[5.6]噻吩并[2.3.4-IJ]喹唑啉衍生物作为抗细菌和抗原性试剂

    公开(公告)号：WO1996037495A1

    公开(公告)日：1996-11-28

    申请号：PCT/US1996006813

    申请日：1996-05-13

    Applicant: ABBOTT LABORATORIES

    Inventor： ABBOTT LABORATORIES ,  CHU, Daniel, T. ,  LI, Qun ,  RAYE, Kathleen

    IPC: C07D491/16

    CPC classification number: C07D491/16

    Abstract: Benzo[5.6]pyrano[2.3.4-ij]quinolizine and benzo[5.6]thiopyrano[2.3.4-ij]quinolizine compounds having formula (I), wherein A is sulfur or oxygen; R is selected from the group consisting of hydroxy, protected-hydroxy, C1-C6-alkoxy, halo, amino, C1-C6-alkylamino, hydroxy-C1-C6-alkylamino, bicyclic nitrogen-containing heterocycle, nitrogen-containing aromatic heterocycle, and nitrogen-containing heterocycle; R is selected from the group consisting of hydrogen, halo, C1-C6-alkyl, or halo-C1-C6-alkyl; R is selected from the group consisting of hydrogen, C1-C6-alkyl or C5-C7-cycloalkyl; and R and R are independently selected from the group consisting of hydrogen, C1-C6-alkyl or C1-C6-alkoxyl, having utility as intermediates or having antibacterial or antineoplastic activity.

    Abstract translation: 苯并[5.6]吡喃并[2,3,4-ij]喹嗪和具有式（I）的苯并[5,6]噻喃并[2,3,4-ij]喹嗪化合物，其中A是硫或氧; R 1选自羟基，被保护的羟基，C 1 -C 6 - 烷氧基，卤素，氨基，C 1 -C 6烷基氨基，羟基-C 1 -C 6 - 烷基氨基，双环含氮杂环，含氮 芳族杂环和含氮杂环; R 2选自氢，卤素，C 1 -C 6 - 烷基或卤代-C 1 -C 6 - 烷基; R 3选自氢，C 1 -C 6 - 烷基或C 5 -C 7 - 环烷基; R 4和R 5独立地选自氢，C 1 -C 6烷基或C 1 -C 6烷氧基，其可用作中间体或具有抗细菌或抗肿瘤活性。

    PROCESS FOR PREPARATION OF CHIRAL 3-AMINOPYRROLIDINE AND ANALOGOUS BICYCLIC COMPOUNDS
    4.
    发明申请
    PROCESS FOR PREPARATION OF CHIRAL 3-AMINOPYRROLIDINE AND ANALOGOUS BICYCLIC COMPOUNDS 审中-公开
    制备三氨基吡啶和类似物双环化合物的方法

    公开(公告)号：WO1998022437A1

    公开(公告)日：1998-05-28

    申请号：PCT/US1997021081

    申请日：1997-11-18

    Applicant: ABBOTT LABORATORIES

    Inventor： ABBOTT LABORATORIES ,  WANG, Wei-bo ,  LI, Qun ,  CHU, Daniel, T. ,  HASVOLD, Lisa, Anne

    IPC: C07D207/14

    CPC classification number: C07D207/14 ,  C07D455/02 ,  C07D471/04 ,  Y02P20/55

    Abstract: A process for the preparation of chiral 3-aminopyrrolidine of formula (I) and analogous bicyclic derivatives of formula (II) from dihydroxy olefins such as for the formula: HO-CH2-CH=CH-CH2-OAr by treatment with titanium isopropoxide, an optically active tartrate ester and tert-butyl hydroperoxide, followed by subsequent alkylation of the intermediate with an alkyl or alkenyl magnesium halide, then pyrrolidine ring formation by condensation with an arylmethylamine, subsequent chiral replacement of a ring hydroxyl group with an amino group with further protection thereof, optional additional substitution closing of the second ring, and hydrogenolysis to remove a ring-nitrogen protecting group.

    Abstract translation: 通过用异丙醇钛处理从二羟基烯烃如式HO-CH2-CH = CH-CH2-OAr制备式（I）的手性3-氨基吡咯烷和式（Ⅱ）的类似双环衍生物的方法， 光学活性酒石酸酯和叔丁基过氧化氢，然后用烷基或烯基卤化镁随后烷基化中间体，然后通过与芳基甲胺缩合形成吡咯烷环，随后进一步用氨基取代环羟基 其保护，第二环的任选的另外的取代封闭，以及氢解以除去环 - 氮保护基。

    QUINOLIZINONE TYPE COMPOUNDS
    5.
    发明申请
    QUINOLIZINONE TYPE COMPOUNDS 审中-公开
    喹诺酮类化合物

    公开(公告)号：WO1996039407A1

    公开(公告)日：1996-12-12

    申请号：PCT/US1996008991

    申请日：1996-06-05

    Applicant: ABBOTT LABORATORIES

    Inventor： ABBOTT LABORATORIES ,  CHU, Daniel, T. ,  LI, Qun ,  COOPER, Curt, S. ,  FUNG, Anthony, K., L. ,  LEE, Cheuk, M. ,  PLATTNER, Jacob, J. ,  MA, Zhenkun ,  WANG, Wei-Bo

    IPC: C07D471/04

    CPC classification number: C07D471/04 ,  A61K38/00 ,  C07D213/61 ,  C07D213/68 ,  C07D455/02 ,  C07K5/06026

    Abstract: Antibacterial compounds having formula (I) and the pharmaceutically acceptable salts, esters and amides thereof, selected preferred examples of which include those compounds wherein A is =CR -; R is cycloalkyl of from three to eight carbon atoms or substituted phenyl; R is selected from the group consisting of (a), (b), (c) and (d); R is halogen; R is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group; R is hydrogen, loweralkyl, halo(loweralkyl), or -NR R ; and R is halogen, loeralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy, or amino(loweralkyl), as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.

    Abstract translation: 具有式（I）的抗菌化合物及其药学上可接受的盐，酯和酰胺，其选择的优选实例包括其中A = CR 6 - 的那些化合物; R 1是3至8个碳原子的环烷基或取代的苯基; R 2选自（a），（b），（c）和（d）; R 3是卤素; R 4是氢，低级烷基，药学上可接受的阳离子或前药酯基; R 5是氢，低级烷基，卤代（低级烷基）或-NR 13 R 14; 和R 6是卤素，低级烷基，卤代（低级烷基），羟基取代的低级烷基，低级烷氧基（低级烷基），低级烷氧基或氨基（低级烷基），以及含有这些化合物的药物组合物及其在治疗中的用途 的细菌感染。

    QUINOLIZINONE TYPE COMPOUNDS
    10.
    发明申请
    QUINOLIZINONE TYPE COMPOUNDS 审中-公开
    喹诺酮类化合物

    公开(公告)号：WO1995010519A1

    公开(公告)日：1995-04-20

    申请号：PCT/US1994011166

    申请日：1994-09-30

    Applicant: ABBOTT LABORATORIES

    Inventor： ABBOTT LABORATORIES ,  CHU, Daniel, T. ,  LI, Qun ,  COOPER, Curt, S. ,  FUNG, Anthony, K., L. ,  LEE, Cheuk, M. ,  PLATTNER, Jacob, J.

    IPC: C07D455/02

    CPC classification number: C07D471/04 ,  A61K38/00 ,  C07D213/61 ,  C07D213/68 ,  C07D455/02 ,  C07K5/06026

    Abstract: Antibacterical coumpounds having formula (I) and the pharmaceutically acceptable salts, esters and amides thereof, preferred examples of which include those coumpounds wherein R is cycloalkyl of from three to eight carbon atoms or substituted phenyl; R is selected from the group consisting of (a) halogen, (b) loweralkyl, (c) loweralkenyl, (d) cycloalkyl of from three to eight carbons, (e) cycloalkenyl of from four to eight carbons, (f) loweralkoxy, (g) aryloxy, (h) aryl(loweralkyl)oxy, (i) aryl(loweralkyl), (j) cycloalkyl(loweralkyl), (k) amino, (l) (loweralkyl)amino, (m) aryl(loweralkyl)amino, (n) hydroxy substituted (loweralkyl)amino, (o) phenyl, (p) substituted phenyl, (q) bicyclic nitrogen-containing heterocycle, (r) nitrogen-containingaromatic heterocycle, and (s) nitrogen-containing heterocycle having formula (Ia) where x is between zero and three; R is halogen; R is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group; R is hydrogen, loweralkyl, halo(loweralkyl), or -NR R ; and R is loweralkyl, as wellas pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.

    Abstract translation: 具有式（I）的抗菌配方及其药学上可接受的盐，酯和酰胺，其优选实例包括其中R 1为3至8个碳原子的环烷基或取代的苯基的那些芳族基团; R 2选自（a）卤素，（b）低级烷基，（c）低级烯基，（d）3至8个碳的环烷基，（e）4至8个碳的环烯基，（f ）低级烷氧基，（g）芳氧基，（h）芳基（低级烷基）氧基，（i）芳基（低级烷基），（j）环烷基（低级烷基），（k）氨基，（1）（低级烷基）氨基，（m） （低级烷基）氨基，（n）羟基取代的（低级烷基）氨基，（o）苯基，（p）取代的苯基，（q）双环含氮杂环，（r）含氮芳族杂环，和 具有式（Ia）的杂环，其中x在0和3之间; R 3是卤素; R 4是氢，低级烷基，药学上可接受的阳离子或前药酯基; R 5是氢，低级烷基，卤代（低级烷基）或-NR 13 R 14; R 6为低级烷基，以及含有这些化合物的药物组合物及其在治疗细菌感染中的用途。

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