Antimicrobial biaryl compounds

Details Antimicrobial biaryl compounds Antimicrobial biaryl compounds

C - Chemistry, Metallurgy

07

D

C07D 403/14 (2006.01) A61K 31/18 (2006.01) A61K 31/34 (2006.01) A61K 31/35 (2006.01) A61K 31/38 (2006.01) A61K 31/40 (2006.01) A61K 31/415 (2006.01) A61K 31/42 (2006.01) A61K 31/425 (2006.01) A61K 31/44 (2006.01) A61K 31/445 (2006.01) A61K 31/495 (2006.01) A61K 31/50 (2006.01) A61K 31/505 (2006.01) A61K 31/52 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) C07C 233/00 (2006.01) C07C 235/00 (2006.01) C07C 237/00 (2006.01) C07C 239/00 (2006.01) C07C 303/00 (2006.01) C07C 307/00 (2006.01) C07C 309/00 (200

Patent

CA 2418121

Provided are antibacterial compounds having Formula (I) wherein X is CH, O, S, N or NH; Y is CH or N; n is 0 or 1; one of R~1 and R~1' is -C(O)NR~5R~5', - C(O)-Q-NR~5R~5', -CH~2NR~5R~5' or -S(O)~2NR~5R~5' and the other is H or R~3, one of R~2 and R~2' is -NHC(O)R~6 or -NHS(O)~2R~6 or -NHS(O)R~6 and the other is H or R~4; Q is an amino acid or peptide; R~3 is H, halogen, -NR~5R~5' or - NHC(O)R~6; R~4 is selected from the group consisting of H, halogen, hydroxyl, amino, carboxyl, alkyl, alkenyl and alkynyl; R~5 is selected from the group consisting of H, alkyl, alkenyl or alkynyl optionally substituted with halogen, OH, amino, amidinyl, guanidinyl, urea, alkyl, carboxyl, oxo, carboxamide; R~5' is H or R~5 and R~5' together form a 5-16 member heterocycle optionally substituted with halogen, OH, amino, alkyl, carboxyl, carbonyl or carboxamide; and R~6 is selected from the group consisting of H; amino, alkyl, alkenyl or alkynyl, each optionally substituted with halogen, amino, amidinyl, guanidinyl, urea, carboxyl or carbvoxamide; a 5-16 member carbocycle or heterocycle; and a 5-16 member heterocycle-substituted alkyl or carbocycle- substituted alkyl, wherein said carbocycle and heterocycle are optionally substituted with halogen, OH, amino, alkyl, carboxyl, oxo or carboxamide.

L'invention concerne des composants antibact~riens de formule I : (I) dans laquelle X repr~sente CH, O, S, N ou NH; Y repr~sente CH ou N; n repr~sente 0 ou 1; l'un de R´1? ou R´1'? repr~sente -C(O)NR´5?R´5'?, -C(O)-Q-NR´5?R´5'?, -CH´2?NR´5?R´5'? ou -S(O)´2?NR´5?R´5'? et l'autre, H or R´3?, un de R´2? ou R´2'? repr~sente-NHC(O)R´6? ou -NHS(O)´2?R´6? ou -NHS(O)R´6? et l'autre repr~sente H ou R´4?; Q est un aminoacide ou un peptide; R´3? repr~sente H, halog­ne, -NR´5?R´5'? ou -NHC(O)R´6?; R´4? est s~lectionn~ dans le groupe compos~ de H, halog­ne, hydroxyle, amino, carboxyle, alkyle, alk~nyle et alkynyle; R´5? est s~lectionn~ dans le groupe compos~ de H, alkyle, alk~nyle ou alkynyle ~ventuellement substitu~ par un halog­ne, OH, amino, amidinyle, guanidinyle, ur~e, alkyle, carboxyle, oxo, carboxamide; R´5'? repr~sente H ou R´5? et R´5'? forment ensemble un h~t~rocycle membre 5, 16 ~ventuellement susbstitu~ par un halog­ne, OH, amino, alkyle, carboxyle, carbonyle ou carboxamide; et R´6? est s~lectionn~ s~lectionn~ dans un groupe compos~ de H; amino, alkyle, alk~nyle ou alkynyle, chacun ~ventuellement substitu~ par un halog­ne, amino, amidinyle, guanidinyle, ur~e, carboxyle ou carboxamide; un carbocycle ou un h~t~rocycle membre 5,16; et un alkyle h~t~rocycle substitu~ membre 5,16 ou un alkyle carbocycle substitu~ dans lesquels lesdits carbocycle et h~t~rocycle sont ~ventuellement substitu~s par un halog­ne, OH, amino, alkyle, carboxyle, oxo ou carboxamide.

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