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    GYRASE INHIBITORS
    3.
    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。

    Gyrase inhibitors
    4.
    发明授权
    Gyrase inhibitors 有权
    促旋酶抑制剂

    公开(公告)号：US09481675B2

    公开(公告)日：2016-11-01

    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 ,  C07D519/00 ,  C07D471/04 ,  C07D487/16 ,  C07D491/048 ,  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: 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。

    Protein kinase inhibitors
    9.
    发明授权
    Protein kinase inhibitors 失效
    蛋白激酶抑制剂

    公开(公告)号：US08598184B2

    公开(公告)日：2013-12-03

    申请号：US12919216

    申请日：2009-02-28

    申请人： Junhu Zhang

    发明人： Junhu Zhang

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00

    CPC分类号： C07D487/04

    摘要： The present invention is directed to low molecular weight and orally bioavailable 3H-[1,2,3]triazolo[4,5-d]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the tyrosine kinase MET. The invention is also directed to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

    摘要翻译： 本发明涉及低分子量和口服生物可利用的3H- [1,2,3]三唑并[4,5-d]嘧啶衍生物，其可用于治疗细胞增殖性疾病，用于治疗与MET活性相关的疾病，以及 用于抑制酪氨酸激酶MET。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。