6,11-BRIDGED ERYTHROMYCIN DERIVATIVES

    公开(公告)号:SK6342000A3

    公开(公告)日:2000-09-12

    申请号:SK6342000

    申请日:1998-10-29

    Applicant: ABBOTT LAB

    Abstract: Novel 6,11-bridged erythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having formula (I) or (II); compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier; a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention; and processes for their preparation.

    6-0-substituted erythromycin compounds and medicaments

    公开(公告)号:NZ332320A

    公开(公告)日:2000-07-28

    申请号:NZ33232097

    申请日:1997-05-06

    Applicant: ABBOTT LAB

    Abstract: The erythromycin derivative has one of the formulae II to IX or a pharmaceutically acceptable salt, ester or prodrug thereof wherein: X is =O, =NOH, =NOR1 or =NOC(R5)(R6)-O-R1; Ra and Rb are independently H or OH; one of Rc and Rd is H and the other is OH, protected OH, halogen, NR6R7, OCO-NH-aryl, O-CO-NH-heteroaryl, O-CO-NR7R8, O-SO2-(optionally substituted alkyl) or O-SO2-(CH2)2-NR7R8 or together form =O, =NOH or =NOR1; R3 is methoxy, F or OH; Rf is H or a hydroxy protecting group; W is absent, O, NH-CO, N=CH or NH; Rg is H, cycloalkyl or optionally substituted alkyl, aryl or heteroaryl; Rh is H, OH, O-C(O)-imidazolyl, O-C(O)-O-alkyl, O-C(O)-O-(optionally substituted aryl), O-C(O)-Cl or O-C(O)-NH2; R is substituted methyl or optionally substituted C2-10 alkyl, C3-10 alkenyl or C3-10 alkynyl; one of Y and Z is hydrogen and the other is H, OH, protected OH or NR7R8; A, B, D and E are independently H, cycloalkyl or optionally substituted alkyl, aryl or heteroaryl, heterocycloalkyl or is optionally substituted aryl, heteroaryl, OH, alkoxy, halo or NR9R10 further substituted with MR11 or any of AB, AD, AE, BD, BE or DE together with the atoms to which they are attached form a 3-7 membered ring optionally containing O, NR', S(O)n, C(O)-NH, C(O)-NR12, NH-C(O), NR12-C(O)- or C(=NH)-NH provided that at least two of A, B, D and E are hydrogen and the rest of the variables are defined in the specification. A pharmaceutical composition thereof is useful for treating bacterial infections.

Patent Agency Ranking