NEW BORNEOL DERIVATIVES, PROCESS FOR THEIR PRODUCTION, AND THEIR PHARMACEUTICAL USE

摘要

The invention concerns borneol derivatives of general formula (I), wherein: R1 represents C(O)-CH(OR6)-CH(NR7aR7b)-R8, C(O)-CH(OR6a)-CH¢NH(C(O)-CH(OR6b)-CH(NR7aR7b)-R8)! -R8; R6a and R6b are identical or different and the same as R6; R7a and R7b are identical or different and the same as R7; R7 is -C(O)R12, -SO2R12, -C(O)OR12, -C(O)SR12, -C(O)NHR9d, -C(O)NR9dR9a, (a), alkyl; R8 is phenyl; RQa-e and R12 are identical or different and stand for alkyl, cycloalkyl, aryl or aralkyl; R6 are identical or different and stand for hydrogen, alkyl, aryl, acyl, aralkyl, -SO2R9c, -P(O) (OH)2; R13 stands for hydrogen, alkyl, aryl, aralkyl. The invention also concerns salts of the said compounds with physiologically tolerable bases, .alpha.-, .beta.- or .gamma.cyclodextrine clathrates of the said compounds and compounds of formula (I) encapsulated with liposomes. The compounds are active as tubulin polymerisation antagonists.