申请人:Merck Sharp & Dohme Corp.
公开号:US20170037059A1
公开(公告)日:2017-02-09
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 CR
5
; R
5
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, NR
7
, or CR
8
R
9
; R
7
is H or C
1-3
alkyl; R
8
and R
9
are each independently H or C
1-3
alkyl; R
2
is H, a hydrocarbyl residue (1-40C) containing 0-10 heteroatoms selected from O, S and N optionally substituted with an inorganic residue; R
4
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 R
5
and R
4
together may join to form a fused ring; and R
6
is selected from the group consisting of H, C
1-5
alkyl, C
2-5
alkenyl, C
2-5
alkynyl, halo C
1-5
alkyl, halo C
2-5
alkenyl, halo C
2-5
alkynyl, C
1-5
hydroxyalkyl, C
1-5
alkyl chloride, C
2-5
alkenyl chloride, and C
2-5
alkynyl chloride; or a pharmaceutically-acceptable salt, ester, or prodrug thereof.