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1. 发明公开

EP1658305A1 NOVEL FUSIDIC ACID DERIVATIVES 审中-公开
标题翻译：新夫西地衍生物
公开(公告)号：EP1658305A1
公开(公告)日：2006-05-24
申请号：EP04738988.7
申请日：2004-07-09
申请人： LEO PHARMA A/S
发明人： DUVOLD, Tore , BRETTING, Claus, Aage, Svensgaard , RASMUSSEN, Poul, Rodbroe , BOUÉRAT DUVOLD, Laetitia, Maud, Elysa , THORHAUGE, Jacob
IPC分类号： C07J9/00
CPC分类号： C07J9/00 , C07J9/005 , C07J13/00 , C07J13/002 , C07J51/00 , C07J53/00
摘要： 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, same or. different substituents selected from the group consisting of alkyl, alkenyl, aryl, alkoxy, nitro, alkylthio, halogen, azido, trifluoromethyl and cyano; Y and Z both' represent hydrogen, or together with the C-17/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 a bond,. O, S or S(O); B represents C1-6 alkyl, C2-6 alkenyl, CI-6 acyl, C3-7 cycloalkylcarbonyl or benzoyl, all of which are optionally substituted with 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; Q1 and 'Q2 independently represent. -CH2-, -C(O)-, -(CHOR)-, -(CHOR)-, -(CHSH)-, - (NH)-, -(CHNH2)- or -(CHW)-., wherein R represents CI-6alkyl and W represents halogen, cyano, azido or trifluoromethyi; Q3 represents -CH2-, -C(O)- or -CHOH-; G represents hydrogen, OH or O-CO-CH3; two bonds in the pentacyclic ring being depicted with full and dotted lines to indicate that either 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 either a single or a double bond; and pharmaceutically acceptable salts and easily hydrolysable esters thereof, to pharmaceutical compositions comprising said derivatives, as well as to their use in therapy.

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