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    GYRASE INHIBITORS
    6.
    发明申请
    GYRASE INHIBITORS 有权
    GYRASE抑制剂

    公开(公告)号：US20130079323A1

    公开(公告)日：2013-03-28

    申请号：US13394985

    申请日：2010-09-10

    申请人： Christopher J. Creighton ,  Leslie William Tari ,  Zhiyong Chen ,  Mark Hilgers ,  Thanh To Lam ,  Xiaoming Li ,  Michael Trzoss ,  Junhu Zhang ,  John Finn ,  Daniel Bensen

    发明人： Christopher J. Creighton ,  Leslie William Tari ,  Zhiyong Chen ,  Mark Hilgers ,  Thanh To Lam ,  Xiaoming Li ,  Michael Trzoss ,  Junhu Zhang ,  John Finn ,  Daniel Bensen

    IPC分类号： C07D487/04 ,  C07D471/04 ,  C07D491/048 ,  C07D487/16 ,  C07D513/04

    CPC分类号： C07D519/00 ,  C07D471/04 ,  C07D471/16 ,  C07D487/04 ,  C07D487/16 ,  C07D491/048 ,  C07D513/04

    摘要： Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth. Compounds of Formula (I), are disclosed: Formula (I), wherein Y is N or CH; Z is N or CR5; R5 is H, a substituted or unsubstituted hydrocarbyl residue (1-3C) containing 0-2 heteroatoms selected from O, S and N, or is an inorganic residue; L is O, S, NR7, or CR8R9; R7 is H or C1-3 alkyl; R8 and R9 are each independently H or C1-3 alkyl; R2 is H, a hydrocarbyl residue (1-40C) containing 0-10 heteroatoms selected from O, S and N optionally substituted with an inorganic residue; R4 is H, an inorganic residue, or a hydrocarbyl residue (1-30C) containing 0-12 heteroatoms selected from O, S and N and containing 0-10 inorganic residues, wherein R5 and R4 together may join to form a fused ring; and R6 is selected from the group consisting of H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halo C1-5 alkyl, halo C2-5 alkenyl, halo C2-5 alkynyl, C1-5 hydroxyalkyl, C1-5 alkyl chloride, C2-5 alkenyl chloride, and C2-5 alkynyl chloride; or a pharmaceutically-acceptable salt, ester, or prodrug thereof.

    摘要翻译： 新型促旋酶抑制剂和相关组合物和方法可用于阻止细菌生长。 公开了式（I）的化合物：式（I），其中Y是N或CH; Z为N或CR5; R5是H，含有0-2个选自O，S和N的杂原子的取代或未取代的烃基残基（1-3C），或是无机残基; L是O，S，NR7或CR8R9; R7是H或C1-3烷基; R 8和R 9各自独立地为H或C 1-3烷基; R2是H，含有0-10个选自O，S和N的杂原子的烃基残基（1-40℃），任选被无机残基取代; R4是H，无机残基或含有0-12个选自O，S和N的杂原子并含有0-10个无机残基的烃基残基（1-30C），其中R 5和R 4可以连接形成稠环; 并且R 6选自H，C 1-5烷基，C 2-5烯基，C 2-5炔基，卤代C 1-5烷基，卤素C 2-5烯基，卤代C 2-5炔基，C 1-5羟基烷基，C 1 -5烷基氯，C2-5烯基氯和C2-5炔基氯; 或其药学上可接受的盐，酯或前药。

    N-substituted alkylamino acids for use as amino-protecting groups
    7.
    发明授权
    N-substituted alkylamino acids for use as amino-protecting groups 失效
    用作氨基保护基团的N-取代的烷基氨基酸

    公开(公告)号：US06417397B1

    公开(公告)日：2002-07-09

    申请号：US09609565

    申请日：2000-06-30

    申请人： Murray Goodman ,  Christopher J. Creighton

    发明人： Murray Goodman ,  Christopher J. Creighton

    IPC分类号： C07C23300

    CPC分类号： C07C237/22 ,  A61K38/00 ,  C07K5/06034 ,  Y02P20/55

    摘要： This invention relates to chemical compositions useful in protecting amino functional groups, e.g., during synthetic organic chemistry procedures or in the formulation and/or delivery of prodrugs. The present invention relates particularly to amino-protecting species comprising an acyl group that can form an amide bond with an amino group. The protecting groups of the present invention can be conveniently removed under a wide variety of conditions.

    摘要翻译： 本发明涉及用于保护氨基官能团的化学组合物，例如在合成有机化学过程中或在制备和/或递送前药中。 本发明特别涉及包含可与氨基形成酰胺键的酰基的氨基保护物质。 本发明的保护基可以在多种条件下方便地除去。