发明名称 BORNEOL DERIVATIVES AFFECTING TUBULIN POLYMERIZATION AND DEPOLYMERIZATION
摘要 The invention relates to borneol derivatives of the general formula (I) in which R1 is C(O)-CH(OR6)-CH(NHR7)-R8, R2 is hydrogen, -OH, C1-C10-Alkyl, C1C10-alkoxy, -OC(O)R9b, -OP(O)(OH)2 or R2 and R3 are together an oxygen atom, R4 is hydrogen, C1-C10-alkyl, -(CH2)n-OR11a, R5 is hydrogen, C1-C10-alkyl, (CH2)p-OR11b, or R4 and R5 together are an oxygen atom, a =CHR10 group, n is 0 to 8, p is 1 to 8, R7 is -C(O)R12, -SO2R12, -C(O)NHR9d, -C(O)NR9dR9e, (formula), R8 is aryl, R9a-e and R12 are the same or different and represent C1-C10-akyl, C4-C8-cycloalkyl, aryl, C7-C16-aralkyl, R10 is hydrogen, C1-C10-alkyl, -(CH2)s-OR14, s is 1 to 8, R6, R11a,b and R14 are the same or different and represent hydrogen, C1-C10-alkyl, aryl, C7-C16 aralkyl, SO2R9c, P(O)(OH)2, R13 and R15a,b are the same or different and represent hydrogen, C1C10-alkyl, aryl, C7-C16-aralkyl, X1 and X2 are the same or different and mean X, X may be hydrogen, halogen, -OH, -NO2, -N3, -CN, -NR15aR15b, -NHSO2R15a, CO2R14, C1-C10-alkyl, C1-C10-alkoxy, C1-C10-acyloxy, C1-C10-acyl and, if R15 is hydrogen, their salts with physiologically tolerable bases, and .alpha.-, .beta.- or .gamma.-cyclodextrin clathrates, and the compounds of the general formula (I) encapsulated with liposomes.
申请公布号 CA2188266(A1) 申请公布日期 1995.11.16
申请号 CA19952188266 申请日期 1995.04.13
申请人 SCHERING AKTIENGESELLSCHAFT 发明人 KLAR, ULRICH;GRAF, HERMANN;NEEF, GUENTER;BLECHERT, SIEGFRIED
分类号 C07D303/31;C07C271/22;C07C309/63;C07D303/14;C07D303/16;C07F9/38;(IPC1-7):C07C271/22;C07F9/117;C08B37/16;A61K31/27;A61K31/335;C07D303/44;A61K31/66;A61K31/715 主分类号 C07D303/31
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