12-09-2013 дата публикации
Номер: US20130237595A1
Принадлежит:
The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein Ya, Yb, R1, R2, and G are as described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as inhibitors of bacterial RNA polymerase and as antibacterial agents. 2. The compound of wherein:{'sup': '2', 'Ris hydrogen;'}{'sup': a', 'b', 'a', 'b', 'a', 'b, 'sub': 1', '4', '1', '10', '2', '12', '2', '12', '2', '12, 'one of Yand Yis hydrogen or C-Cstraight alkyl, and the other of Yand Yis C-Cstraight or branched alkyl, C-Cstraight or branched hydroxyalkyl, C-Cstraight or branched alkenyl, C-Cstraight or branched hydroxyalkenyl, or Yand Yare taken together with their intervening atom to form a 4-6 membered ring having 0-1 ring heteroatoms selected from nitrogen, oxygen or sulfur;'}{'sup': 3', '3', '3', '3', '3', '3, 'sub': 2', '2', '2', '2', '2', '2, 'G is —CH═CH—NHC(O)—R, —CH═CH—NHC(S)—R, —CHCHNHC(O)—R, —CHCHNHC(S)—R, —CHNHNHC(O)—R, or —CHNHNHC(S)—R;'}{'sup': 3', '4, 'sub': 1', '6', '1', '6', '1', '6', '2, 'Ris C-Calkyl, —O(C-Calkyl), —S(C-Calkyl), or —N(R); and'}{'sup': 4', '4, 'sub': 1', '6, 'one Ris hydrogen and the other Ris hydrogen or —C-Calkyl.'}3. The compound of wherein:{'sup': a', 'b', 'a', 'b, 'sub': 3', '2', '3', '1', '10', '2', '12', '2', '12', '2', '12, 'one of Yand Yis hydrogen, —CH, or —CHCH, and the other of Yand Yis C-Cstraight or branched alkyl, C-Cstraight or branched hydroxyalkyl, C-Cstraight or branched alkenyl or C-Cstraight or branched hydroxyalkenyl;'}{'sup': 3', '3', '3, 'sub': 2', '2', '2, 'G is —CH═CH—NHC(O)—R, —CHCHNHC(O)—R, or —CHNHNHC(O)—R;'}{'sup': 3', '4, 'sub': 1', '6', '1', '6', '2, 'Ris C-Calkyl, —O(C-Calkyl), or —N(R); and'}{'sup': 4', '4, 'sub': 1', '4, 'one Ris hydrogen and the other Ris hydrogen or —C-Calkyl.'}4. The compound of wherein:{'sup': a', 'b', 'a', 'b, 'sub': 3', '1', '10', '3', '2', '2', 't', '2', '2', '3', '2', '2', 't', '2', '2', '3', '2', 't', '2', '3', '2', '3 ...
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