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。