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89 条记录 (耗时 0.041 秒)

    Process for preparation of chiral 3-amino-pyrrolidine and analogous bicyclic compounds
    3.
    发明授权
    Process for preparation of chiral 3-amino-pyrrolidine and analogous bicyclic compounds 失效
    手性3-氨基 - 吡咯烷和类似双环化合物的制备方法

    公开(公告)号：US5837868A

    公开(公告)日：1998-11-17

    申请号：US974206

    申请日：1997-11-19

    申请人： Wei-Bo Wang ,  Qun Li ,  Daniel T. Chu ,  Lisa Anne Hasvold

    发明人： Wei-Bo Wang ,  Qun Li ,  Daniel T. Chu ,  Lisa Anne Hasvold

    IPC分类号： C07D207/14 ,  C07D455/02 ,  C07D471/04 ,  C07D471/02 ,  C07D487/02

    CPC分类号： C07D207/14 ,  C07D455/02 ,  C07D471/04 ,  Y02P20/55

    摘要： A process for the preparation of chiral 3-aminopyrrolidine and analogous bicyclic derivatives from dihydroxy olefins 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.

    摘要翻译： 通过用异丙醇钛，光学活性酒石酸酯和叔丁基过氧化氢处理二羟基烯烃手性3-氨基吡咯烷和类似双环衍生物的方法，然后用烷基或链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，随后进一步保护具有氨基的环羟基的手性取代，任选的第二环的另外的取代封闭，以及氢解除去环 - 氮保护基。

    Process for preparation of chiral 3-amino-pyrrolidine and analogous bicyclic compounds
    5.
    发明授权
    Process for preparation of chiral 3-amino-pyrrolidine and analogous bicyclic compounds 失效
    手性3-氨基 - 吡咯烷和类似双环化合物的制备方法

    公开(公告)号：US5703244A

    公开(公告)日：1997-12-30

    申请号：US754641

    申请日：1996-11-21

    申请人： Qun Li ,  Wei-Bo Wang ,  Daniel T. Chu ,  Lisa Anne Hasvold

    发明人： Qun Li ,  Wei-Bo Wang ,  Daniel T. Chu ,  Lisa Anne Hasvold

    IPC分类号： C07D207/14 ,  C07D455/02 ,  C07D471/04 ,  C07D207/09

    CPC分类号： C07D207/14 ,  C07D455/02 ,  C07D471/04 ,  Y02P20/55

    摘要： A process for the preparation of chiral 3-aminopyrrolidine and analogous bicyclic derivatives from dihydroxy olefins 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.

    摘要翻译： 通过用异丙醇钛，光学活性酒石酸酯和叔丁基过氧化氢处理二羟基烯烃手性3-氨基吡咯烷和类似双环衍生物的方法，然后用烷基或链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，随后进一步保护具有氨基的环羟基的手性取代，任选的第二环的另外的取代封闭，以及氢解除去环 - 氮保护基。

    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
    9.
    发明授权
    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 失效
    苯并[5.6]吡喃并[2,3,4-ij]喹嗪和苯并[5,6]噻喃并[2,3,4-ij]喹嗪衍生物作为抗细菌和抗肿瘤剂

    公开(公告)号：US5618813A

    公开(公告)日：1997-04-08

    申请号：US451243

    申请日：1995-05-26

    申请人： Daniel T. Chu ,  Qun Li ,  Kathleen Raye

    发明人： Daniel T. Chu ,  Qun Li ,  Kathleen Raye

    IPC分类号： C07D491/16 ,  A61K31/535 ,  A61K31/44 ,  A61K31/495 ,  C07D491/147

    CPC分类号： C07D491/16

    摘要： Benzo[5.6]pyrano[2.3.4-ij]quinolizine and benzo[5.6]thiopyrano[2.3.4-ij]quinolizine compounds having the formula ##STR1## wherein A is sulfur or oxygen; R.sup.1 is selected from the group consisting of hydroxy, protected-hydroxy, C.sub.1 -C.sub.6 -alkoxy, halo, amino, C.sub.1 -C.sub.6 -alkylamino, hydroxy-C.sub.1 -C.sub.6 -alkylamino, bicyclic nitrogen-containing heterocycle, nitrogen-containing aromatic heterocycle, and nitrogen-containing heterocycle; R.sup.2 is selected from the group consisting of hydrogen, halo, C.sub.1 -C.sub.6 -alkyl, or halo-C.sub.1 -C.sub.6 -alkyl; R.sup.3 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 -alkyl or C.sub.5 -C.sub.7 -cycloalkyl; and R.sup.4 and R.sup.5 are independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkoxyl, having utility as intermediates or having antibacterial or antineoplastic activity

    摘要翻译： 苯并[5.6]吡喃并[2,3,4-ij]喹嗪和苯并[5,6]噻喃并[2,3,4-ij]喹嗪化合物，其中A为硫或氧; 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; 并且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

    Quinolizinone type compounds
    10.
    发明授权
    Quinolizinone type compounds 失效
    喹诺酮类化合物

    公开(公告)号：US5580872A

    公开(公告)日：1996-12-03

    申请号：US316319

    申请日：1994-09-30

    申请人： Daniel T. Chu ,  Qun Li ,  Curt S. Cooper ,  Anthony K. L. Fung ,  Cheuk M. Lee ,  Jacob J. Plattner

    发明人： Daniel T. Chu ,  Qun Li ,  Curt S. Cooper ,  Anthony K. L. Fung ,  Cheuk M. Lee ,  Jacob J. Plattner

    IPC分类号： A61K38/00 ,  C07D213/61 ,  C07D213/68 ,  C07D455/02 ,  C07D471/04 ,  C07D491/16 ,  C07D519/00 ,  C07K5/06 ,  A61K31/495 ,  A61K31/505 ,  C07D401/00 ,  C07D239/72

    CPC分类号： C07D471/04 ,  C07D213/61 ,  C07D213/68 ,  C07D455/02 ,  C07K5/06026 ,  A61K38/00

    摘要： Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, preferred examples of which include those compounds whereinA is .dbd.CR.sup.6 --;R.sup.1 is cycloalkyl of from three to eight carbon atoms or substituted phenyl;R.sup.2 is selected from the group consisting of ##STR2## R.sup.3 is halogen; R.sup.4 is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group;R.sup.5 is hydrogen, loweralkyl, halo(loweralkyl), or --NR.sup.13 R.sup.14 ; andR.sup.6 is halogen, loweralkyl, 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.

    摘要翻译： 具有式（I）的抗菌化合物及其药学上可接受的盐，酯和酰胺，其优选实例包括其中A = CR 6 - 的那些化合物; R1是3至8个碳原子的环烷基或取代的苯基; R2选自 R3是卤素; R4是氢，低级烷基，药学上可接受的阳离子或前药酯基; R5是氢，低级烷基，卤代（低级烷基）或-NR13R14; 并且R6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用于治疗细菌感染 。