Quinolizinone type compounds

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 5/00 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/55 (2006.01) A61K 38/04 (2006.01) C07D 213/61 (2006.01) C07D 213/68 (2006.01) C07D 455/02 (2006.01) C07D 471/04 (2006.01) C07D 491/16 (2006.01) C07D 519/00 (2006.01) C07K 5/06 (2006.01) C07K 7/06 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2173459

Antibacterical coumpounds having formula (I) and the pharmaceutically acceptable salts, esters and amides thereof, preferred examples of which include those coumpounds wherein R1 is cycloalkyl of from three to eight carbon atoms or substituted phenyl; R2is selected from the group consisting of (a) halogen, (b) loweralkyl, (c) loweralkenyl, (d) cycloalkyl of from three to eight carbons, (e) cycloalkenyl of from four to eight carbons, (f) loweralkoxy, (g) aryloxy, (h) aryl(loweralkyl)oxy, (i) aryl(loweralkyl), (j) cycloalkyl(loweralkyl), (k) amino, (l) (loweralkyl)amino, (m) aryl(loweralkyl)amino, (n) hydroxy substituted (loweralkyl)amino, (o) phenyl, (p) substituted phenyl, (q) bicyclic nitrogen-containing heterocycle, (r) nitrogen-containingaromatic heterocycle, and (s) nitrogen-containing heterocycle having formula (Ia) where x is between zero and three; R3 is halogen; R4 is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group; R5 is hydrogen, loweralkyl, halo(loweralkyl), or - NR13R14; and R6 is loweralkyl, as wellas pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.

Composés antibactériens de la formule (I) et sels, esters et amides pharmaceutiquement acceptables de ceux-ci, dont des exemples préférés comprennent des composés dans lesquels: R?1¿ est un cycloalcoyle avec deux à huit atomes de carbone ou un phényle substitué; R?2¿ est sélectionné dans le groupe comprenant: (a) halogène, (b) alcoyle inférieur, (c) alcényle inférieur, (c) cycloalcoyle avec trois à huit atomes de carbone, (e) cycloalcényle avec quatre à huit atomes de carbone, (f) alcoxy inférieur, (g) aroyloxy, (h) aroyl(alcoyle inférieur)oxy, (I) aroyl(alcoyle inférieur), (j) cycloalcoyle(alcoyle inférieur), (k) amino, (l) (alcoyle inférieur)amino, (m) aroyl(alcoyle inférieur)amino, (n) (alcoyle inférieur)amino substitué par hydroxy, (o) phényle, (p) phényle substitué, (q) hétérocycle dicyclique azoté, (r) hétérocycle aromatique azoté et (s) hétérocycle azoté de la formule (Ia), dans laquelle R?3¿ est un halogène; R?4¿ est l'hydrogène, un alcoyle inférieur, un cation pharmaceutiquement acceptable ou un groupe ester promédicamenteux; R?5¿ est l'hydrogène, un alcoyle inférieur, un halo(alcoyle inférieur) ou -NR?13¿R?14¿; et R?6¿ est un alcoyle inférieur. L'invention décrit également des compositions pharmaceutiques contenant ces composés et l'utilisation de celles-ci dans le traitement des infections bactériennes.

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