compound, pharmaceutically acceptable salt of a compound, pharmaceutical composition, method of treating, preventing or ameliorating infections in a patient, use of a compound, and method of preparing a compound

摘要

"COMPOUND, PHARMACEUTICALLY ACCEPTABLE SALT OF A COMPOUND, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT, PREVENTION OR IMPROVEMENT OF INFECTIONS IN A PATIENT, USE OF A COMPOUND, AND METHOD OF PREPARING A COMPOUND". The present invention relates to novel fusidic acid derivatives of general formula (I) wherein X represents halogen, trifluoromethyl, cyano, azido, alkyl, alkenyl or aryl, wherein said alkyl, alkenyl or aryl are optionally substituted by one. or more, the same or different substituents selected from the group consisting of alkyl, alkenyl, aryl, alkoxy, nitro, alkylthio, halogen, azide, trifluoromethyl and cyano; Y and Z both represent hydrogen or together with the C17 / C-20 bond form a double bond between C-17 and C-20 or together are methylene and form a cyclopropane ring in combination with C-17 and C-20; A represents an O, S or S (O) bond; B represents C 1-6 alkyl, C 2-6 alkenyl, C 1-6 acyl, C 3-7 cycloalkylcarbonyl or benzoyl all being optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, alkoxy, aryl, heteroaryl and azido, or, if A represents a bond, B may also represent hydrogen; Q ~ 1 ~ and Q ~ 2 ~ independently represent -CH ~ 2 ~ -, -C (O) - OR (CHOH) -, - (CHOR) -, - (CHSH) -, - (NH) -, - ( CHNH (2) - or - (CHW) - wherein R represents C 1-6 alkyl and W represents halogen, cyano, azido or trifluoromethyl; Q 3 represents -CH 2 2- -, -C (O) - or -CHOH-; G represents hydrogen, OH or O-CO-CH 3 -; two bonds in the pentacyclic ring being represented with full and dotted lines to indicate that one of the two bonds may be a double bond, in which case Y is absent and Z represents hydrogen; the bond between C-1 and C-2 being a single bond or a double bond; and pharmaceutically acceptable salts and readily hydrolysable esters thereof. to pharmaceutical compositions comprising said derivative as well as their use in therapy.