申请人:Hubschwerlen Christian
公开号:US09346804B2
公开(公告)日:2016-05-24
The present invention relates to antibacterial compounds of formula (I) wherein “----” is a bond or is absent, V is CH, CR6 or N; R0 is H or, if “----” is a bond, may also be alkoxy; R1 is cyano, alkyl, or ethynyl; U is CH or N when “----” is a bond, or, if “----” is absent, U is CH2, NH or NH9; R2 is H, alkylcarbonyl or CH2—R3; R3 is H, alkyl or hydroxyalkyl; R4 is H or, if n is not 0 and R5 is H, may also be OH; R5 is H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; R6 is hydroxyalkyl, carboxy, alkoxycarbonyl or —(CH2)q—NR7R8, q being 1, 2 or 3 and each of R7 and R8 independently being H or alkyl or R7 and R8 forming with the N atom bearing them a ring; R9 is alkyl or hydroxyalkyl; A is —(CH2)p—, —CH2CH2CH(OH)— or —COCH2CH(OH)—; G is substituted phenyl or G1 or G2, wherein Q is O or S and X is CH or N; and Y1, Y2 and Y3 may each be CH or N; and n is 0 when A is —CH2CH2CH(OH)— or —COCH2CH(OH)—, and n is 0, 1 or 2 when A is —(CH2)p—, p being 1, 2, 3 or 4, with the proviso that the sum of n and p is then 2, 3 or 4; and to salts of such compounds.
本发明涉及具有以下式(I)的抗菌化合物,“----”表示键合或不存在,V为CH,CR6或N;R0为H或,如果“----”为键合,则也可以为烷氧基;R1为氰基,烷基或乙炔基;当“----”为键合时,U为CH或N,如果“----”不存在,则U为CH2,NH或NH9;R2为H,烷基羰基或CH2—R3;R3为H,烷基或羟基烷基;R4为H或,如果n不为0且R5为H,则也可以为OH;R5为H,烷基,羟基烷基,氨基烷基,烷氧基烷基,羧基或烷氧羰基;R6为羟基烷基,羧基,烷氧羰基或—(CH2)q—NR7R8,其中q为1、2或3,R7和R8各自独立地为H或烷基,或R7和R8与它们所带的N原子形成环;R9为烷基或羟基烷基;A为—(CH2)p—,—CH2CH2CH(OH)—或—COCH2CH(OH)—;G为取代苯基或G1或G2,其中Q为O或S,X为CH或N;Y1、Y2和Y3可以分别为CH或N;当A为—CH2CH2CH(OH)—或—COCH2CH(OH)—时,n为0,当A为—(CH2)p—时,n为0、1或2,p为1、2、3或4,但n和p的总和为2、3或4;以及这些化合物的盐。