Antibacterial Biaromatic Derivatives
    1.
    发明申请
    Antibacterial Biaromatic Derivatives 有权
    抗菌双酚衍生物

    公开(公告)号:US20160075722A1

    公开(公告)日:2016-03-17

    申请号:US14784602

    申请日:2014-04-15

    摘要: The invention relates to antibacterial compounds of formula I (I) wherein R is H, cyano, alkoxy, cyanomethoxy, cycloalkylmethoxy, hydroxyalkoxy, alkoxyalkoxy, alkoxycarbonyl, 2-ethoxy-2-oxoethoxy, 2-(methylamino)-2-oxoethoxy, (1-cyanocyclobutyl)methoxy, 3-hydroxy-pyrrolidin-1-yl or 3,4-dihydroxycyclopentyl)methoxy; U1 is N or CR1, U2 is N or CR1, U3 is N or CR3 and U4 is N or CR1, it being understood that at most three of U1, U2, U3 and U4 can be N at the same time; V1 is N or CR5, V2 is N or CR6, V3 is N or CR7 and V4 is N or CH, it being understood that at most two of V1, V2, V3 and V4 can be N at the same time; R1 is H, cyano, hydroxy or alkoxy; R2 is H, hydroxy or alkoxy; R3 is H, cyano, hydroxy, alkoxy or carboxamido; R4 is H or alkoxy; R5 is H, hydroxy or halogen; R6 is H, hydroxy or halogen; R7 is H; the dotted line “______” represents a bond or is absent; W represents CH or N when the dotted line “______” is a bond, or W represents CH2 when the dotted line “______” is absent; X represents CH or N; and Q represents O or S; and salts thereof.

    摘要翻译: 本发明涉及式I(I)的抗菌化合物,其中R为H,氰基,烷氧基,氰基甲氧基,环烷基甲氧基,羟基烷氧基,烷氧基烷氧基,烷氧基羰基,2-乙氧基-2-氧代乙氧基,2-(甲基氨基)-2-氧代乙氧基,( 1-氰基环丁基)甲氧基,3-羟基 - 吡咯烷-1-基或3,4-二羟基环戊基)甲氧基; U1是N或CR1,U2是N或CR1,U3是N或CR3,U4是N或CR1,可以理解U1,U2,U3和U4中的至多三个可以同时为N; V1是N或CR5,V2是N或CR6,V3是N或CR7,V4是N或CH,可以理解,V1,V2,V3和V4中的至多两个可以同时为N; R1是H,氰基,羟基或烷氧基; R2是H,羟基或烷氧基; R3是H,氰基,羟基,烷氧基或甲酰氨基; R4是H或烷氧基; R5是H,羟基或卤素; R6是H,羟基或卤素; R7为H; 虚线“______”代表债券或不存在; 当虚线“______”为键时,W表示CH或N,或当虚线“______”不存在时,W表示CH2; X表示CH或N; Q表示O或S; 及其盐。

    TRICYCLIC OXAZOLIDINONE ANTIBIOTIC COMPOUNDS
    4.
    发明申请
    TRICYCLIC OXAZOLIDINONE ANTIBIOTIC COMPOUNDS 有权
    三氧化二氮唑酮类抗生素化合物

    公开(公告)号:US20160237088A1

    公开(公告)日:2016-08-18

    申请号:US15135352

    申请日:2016-04-21

    摘要: The invention relates to 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 H or halogen; U is CH or N when “” is a bond, or, if “” is absent, U is CH2, NH or NRg; 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 thereof.

    摘要翻译: 本发明涉及式I化合物,其中“”是键或不存在,V是CH,CR 6或N; R 0是H,或者如果“”是键,也可以是烷氧基; R1是H或卤素; 当“”是键时,U是CH或N,或者如果不存在,则U是CH 2,NH或NR g; R2是H,烷基羰基或-CH2-R3; R3是H,烷基或羟烷基; R4是H或如果n不为0且R5是H,也可以是OH; R5是H,烷基,羟基烷基,氨基烷基,烷氧基烷基,羧基或烷氧基羰基; R6是羟基烷基,羧基,烷氧基羰基或 - (CH2)q-NR7R8,q是1,2或3,R7和R8各自独立地是H或烷基或R7和R8与带有它们的N原子形成环; R9是烷基或羟烷基; A是 - (CH 2)p - , - CH 2 CH 2 CH(OH) - 或-COCH 2 CH(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各自为CH或N; 当A为-CH 2 CH 2 CH(OH) - 或-COCH 2 CH(OH) - 时,n为0,当A为 - (CH 2)p - ,p为1,2,3或4时,n为0,1或2, 条件是n和p之和为2,3或4; 及其盐。

    Antibacterial Oxadiazolone Derivatives
    6.
    发明申请
    Antibacterial Oxadiazolone Derivatives 有权
    抗菌恶二唑酮衍生物

    公开(公告)号:US20150353547A1

    公开(公告)日:2015-12-10

    申请号:US14760096

    申请日:2014-01-08

    摘要: The invention relates to antibacterial compounds of formula I wherein U represents CH or N; V represents CH or N, provided that at least one of U and V does not represent N; R represents H, halogen, methyl, methoxy, cyano or ethynyl; either W represents a phenyl group substituted in para position with (C1-C3)alkyl, (C1-C3)alkoxy or (C1-C3)thioalkoxy and optionally in meta position with halogen, or W is a group having one of the formulae W1 and W2 below wherein Q is O or S and X is CH or N; and salts of such compounds.

    摘要翻译: 本发明涉及式I的抗菌化合物,其中U代表CH或N; V表示CH或N,条件是U和V中的至少一个不表示N; R代表H,卤素,甲基,甲氧基,氰基或乙炔基; W表示在对位被(C 1 -C 3)烷基,(C 1 -C 3)烷氧基或(C 1 -C 3)硫代烷氧基任选取代的苯基,并且任选地在与卤素的间位置,或W是具有式W1之一的基团 和W2,其中Q是O或S,X是CH或N; 和这些化合物的盐。