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    MACROCYCLIC LACTONES, COMPOSITIONS, AND METHODS OF USE
    2.
    发明授权
    MACROCYCLIC LACTONES, COMPOSITIONS, AND METHODS OF USE 失效
    万家乐CYCLICAL内酯，组合物及其使用方法

    公开(公告)号：EP1000053B1

    公开(公告)日：2004-06-30

    申请号：EP98935844.5

    申请日：1998-07-23

    申请人： THE GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES

    发明人： BOYD, Michael, R. ,  MCKEE, Tawnya, C. ,  CARDELLINA, John, H., II ,  BEUTLER, John, A. ,  ERICKSON, Karen ,  GALINIS, Deborah ,  PANNELL, Lewis

    IPC分类号： C07D313/00 ,  C07D321/00 ,  A61K31/365

    CPC分类号： C07D321/00 ,  C07D313/00

    摘要： The present invention provides a compound of formula (I), wherein R?1 and R2¿ are the same or different and are independently H, C¿1?-C6 straight-chain or branched-chain saturated or unsaturated alkyl, aryl, R?6CH¿2-, R6CO-, or R6SO2-, wherein R6 is H, C¿1?-C6 straight-chain or branched-chain saturated or unsaturated alkyl, or aryl; R?3¿ is H, C¿1?-C6 straight-chain or branched-chain saturated alkyl, aryl, an oxime, or an oxime methyl ether; at least one aromatic ring position is optionally substituted with a substituent selected from the group consisting of halo, nitro, amino, hydroxyl, thio, acyl, C1-C6 alkyl, and cyano; and Z is a contiguous linker comprising a chain of 7-10 atoms (including heteroatoms) which atoms, together with the five atoms beginning with the carbon of the aromatic ring in meta-relationship with OR?1¿ and ending with the carbon directly attached to the alkyl oxygen of the lactone, which carbons are covalently bonded to either end of linker Z, integrally form a 12-15 membered ring; or a pharmaceutically acceptable salt, an ester, or a prodrug thereof. The present invention further provides a pharmaceutical composition, and a method of preventing or treating cancer, using at least one compound of the present invention, optionally in conjunction with an additional compound other than a compound of the present invention.

    BIOLOGICALLY ACTIVE MACROLIDES, COMPOSITIONS, AND USES THEREOF
    4.
    发明授权
    BIOLOGICALLY ACTIVE MACROLIDES, COMPOSITIONS, AND USES THEREOF 有权
    生物活性大环内酯类，组成与应用

    公开(公告)号：EP1303522B1

    公开(公告)日：2011-04-06

    申请号：EP01959257.5

    申请日：2001-07-24

    申请人： THE GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES

    发明人： BOYD, Michael, R. ,  GUSTAFSON, Kirk, R. ,  CANTRELL, Charles, L.

    IPC分类号： C07D498/08

    CPC分类号： A61K31/395 ,  A61K31/365 ,  A61K31/7048 ,  C07D498/06 ,  C07D498/08

    摘要： The present invention provides a compound of the formula (I) or (II), wherein R1 is H, alkyl, alkenyl or aryl, R2 is H, alkyl, alkenyl or aryl, R3 is H, alkyl, alkenyl or aryl, R?4 and R4-R8¿ are independently R?10, C(O)R10¿ or SO¿2R?10, wherein R10 is H, alkyl, alkenyl or aryl, and R?9 is R9a, C(O)R9a¿ or SO¿2R?9a, wherein R9a is H, alkyl, alkenyl or aryl. R9a can be unsubstituted or substituted with one or more oxo(=O), OR9b, OC(O)R9b, OSO2R?9b, NHR9b¿, NHC(O)R9b and NHSO¿2R?9b groups. R9b is H, alkyl, alkenyl, or aryl. R9b can be unsubstituted or substituted with one or more groups such as oxo(=O), OR9c, CO2R9c, CO2R9c and OC(O)R9c. R9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent. The present invention further provides a method of treating a condition treatable by the inhibition of vacuolar-type (H+)-ATPase and a method of treating cancer.