Acrylamide derivatives as fab i inhibitors

Details Acrylamide derivatives as fab i inhibitors Acrylamide derivatives as fab i inhibitors

C - Chemistry, Metallurgy

07

D

C07D 401/12 (2006.01) A61K 31/381 (2006.01) A61K 31/4436 (2006.01) A61K 31/4439 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) A61K 31/506 (2006.01) A61K 31/5365 (2006.01) C07D 209/14 (2006.01) C07D 209/52 (2006.01) C07D 213/75 (2006.01) C07D 215/38 (2006.01) C07D 221/02 (2006.01) C07D 239/42 (2006.01) C07D 265/36 (2006.01) C07D 405/12 (2006.01) C07D 471/02 (2006.01) C07D 471/04 (2006.01) C07D 487/04 (2006.01) C07D 495/04 (2006.01) C07D 498/02 (2006.01) C07D 498/04 (2006.01)

Patent

CA 2387016

Compounds of formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections. In said formula, (A) is (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l), (m), (n), (o) or (p); (I) wherein R1 is H or C1-4alkyl; R2 is H, C1-4alkyl or C3-6cycloalkyl; R3 is (q), (r), (s), (t), (u), (v) or (w); R4 is H or C1-4alkyl; (x) indicates that one of the two designated bonds is a double bond and the other is a single bond; R5 is CH2 when the bond to which it is attached is a double bond; or R5 is H or C1-4alkyl when the bond to which it is attached is a single bond; R6 is H or C1-4alkyl; R7 is H, C1-6alkyl or -C0-6alkyl-Ar; Y is H, C1-4alkyl, N(R')2, NHC(O)R', NHCH2C(O)R' or NHC(O)CH=CHR'; each X independently is H, C1-4alkyl, CH2OH, OR', SR', CN, N(R')2, CH2N(R')2, NO2, CF3, CO2R', CON(R')2, COR', NR'C(O)R', F, Cl, Br, I or -S(O)r CF3; W is S or O, Q is H or C1-4alkyl; M is CH2 or O; L is CH2 or C(O); E is O or NR'; each R' independently is H, C1-6alkyl or -C0-6alkyl-Ar; and r is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.

La présente invention concerne des composés représentés par la formule (I) qui sont des inhibiteurs de Fab I et qui conviennent pour le traitement d'infections bactériennes. Dans cette formule (I) (A) est (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l), (m), (n), (o), ou (p); R?1¿ est H ou C¿1-4?alkyle; R?2¿ est H, C¿1-4?alkyle ou C¿3-6?cycloalkyle; R?3¿ est (q), (r), (s), (t), (u), (v) ou (w); R?4¿ est H ou C¿1-4?alkyle; (x) indique que l'une des deux liaisons désignées est une liaison double et que l'autre est une liaison simple; R?5¿ est CH¿2? quand la liaison à laquelle il est attaché est une liaison double ou R?5¿ est H ou C¿1-4?alkyle quand la liaison à laquelle il est attaché est une liaison simple; R?6¿ est H ou C¿1-4?alkyle; R?7¿ est H, C¿1-6?alkyle ou -C¿0-6?alkyl-Ar; Y est H, C¿1-4?alkyle, N(R')¿2?, NHC(O)R', NHCH¿2?C(O)R' ou NHC(O)CH=CHR'; chaque X est indépendamment H, C¿1-4?alkyle, CH¿2?OH, OR', SR', CN, N(R')¿2?, CH¿2?N(R')¿2?, NO¿2?, CF¿3?, CO¿2?R', CON(R')¿2?, COR', NR'C(O)R', F, Cl, Br, I ou -S(O)¿r?CF¿3?; W est S ou O, Q est H ou C¿1-4?alkyle; M est CH¿2? ou O; L est CH¿2? ou C(O); E est O ou NR'; chaque R' est indépendamment H, C¿1-6?alkyle ou -C¿0-6?alkyl-Ar; et r est 0, 1 ou 2; ou un sel pharmaceutiquement acceptable de ceux-ci.

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