发明名称 Structural variants of mycolactones for use in modulating inflammation, immunity and pain
摘要 The present invention is related to variants of mycolactones of formula (I), processes for the preparation thereof, pharmaceutical compositions thereof and their use in modulating inflammation, immunity and pain. Y—O—W (I), wherein Y and W are as defined in claim 1.
申请公布号 US9598393(B2) 申请公布日期 2017.03.21
申请号 US201214358501 申请日期 2012.11.16
申请人 Institut Pasteur 发明人 Demangel Caroline;Blanchard Nicolas;Bismuth Georges;Eustache Jacques;Casarotto Virginie;Chany Anne-Caroline;Guenin-Mace Laure
分类号 C07D313/00;A61K31/335;C07C69/76;C07D521/00;C07C69/732;C07C43/15;C07C59/135;C07F5/02 主分类号 C07D313/00
代理机构 Foley & Lardner LLP 代理人 Foley & Lardner LLP
主权项 1. A compound of formula (I): Y—O—W  (I) wherein: W is H or —C(═O)—X; X is Xaa, Xbb, Xcc, Xdd or Xee: Y is Z; Z is: wherein R15 is C1-C6 alkyl or L; R11 is H or CH3; is a single bond (C—C) or a double bond (C═C); L is L1, L2, or L3: R16, R17, R18, R19, R20, R21, R22, R23, R26, R27, R30, R31, R32, R33, R34, R35, R36, R37, R38, R39, R40, R41, R42, R43, R44, R45 and R46 are each independently selected from H and C1-C6 alkyl; R24, R25, R28, R29 and R47 are each independently selected from H, halogen, hydroxyl, and (C1-C6)alkoxy; with the proviso that when X is Xaa or Xbb, and when R15 is L1, then R11 cannot be CH3, with the provision that when Y is selected from C2-C6 alkenyl, C3-C10 cycloalkyl, C3-C10 cycloalkenyl, (C1-C6)alkoxy(C1-C6)alkyl, (C1-C6)alkoxy(C6-C10)aryl, then W is —C(═O)—X; with the exclusion of the compounds wherein: Y is Z; W is H; is C═C; R11 is CH3; R15 is L1 with R16, R20, R22 and R30 are CH3; R24 and R28 are OH; and the other radicals Ri are H; Y is Z; W is H; is C═C; R11 is CH3; R15 is isopropyl; and the other radicals Ri are H; and the stereoisomeric forms, or mixtures of stereoisomeric forms thereof.
地址 Paris FR