C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 303/17 (2006.01) A61K 31/16 (2006.01) A61K 31/21 (2006.01) A61K 31/27 (2006.01) A61K 31/275 (2006.01) A61K 31/325 (2006.01) A61K 31/335 (2006.01) A61K 31/675 (2006.01) A61K 31/715 (2006.01) C07C 271/22 (2006.01) C07C 333/04 (2006.01) C07D 303/16 (2006.01) C07F 9/117 (2006.01) C08B 37/16 (2006.01)
Patent
CA 2213211
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.
La présente invention concerne des dérivés de bornéol ayant pour formule générale (I) dans laquelle: C(O)-CH(OR?6¿)-CH(NR?7a¿R?7b¿)-R?8¿, C(O)-CH(OR?6a¿)-CH[NH(C(O)-CH(OR?6b¿)-CH(NR?7a¿R?7b¿)-R?8¿)]-R?8¿; R?6a¿ et R?6b¿ sont identiques ou non et représentent R?6¿; R?7a¿ et R?7b¿ sont identiques ou non et représentent R?7¿; R?7¿ représente -C(O)R?12¿, -SO¿2?R?12¿, -C(O)OR?12¿, -C(O)SR?12¿, -C(O)NHR?9d¿, -C(O)NR?9d¿R?9a¿, (a), alkyle; R?8¿ représente phényle; R?Qa-e¿, R?12¿ sont identiques ou non et représentent alkyle, cycloalkyle, aryle, aralkyle; les groupes R?6¿ sont identiques ou non et représentent hydrogène, alkyle, aryle, acyle, aralkyle, -SO¿2?R?9c¿, -P(O) (OH)¿2?; R?13¿ représente hydrogène, alkyle, aryle, aralkyle et leurs sels avec des bases tolérables physiologiquement ainsi que leurs .alpha.-, .beta.-, ou .gamma.-clathrates de cyclodextrine et les composés de formule générale (I) ci-dessus, encapsulés avec des liposomes. Ces composés agissent en tant qu'antagonistes de la polymérisation de la tubuline.
Blechert Siegfried
Graf Hermann
Klar Ulrich
Neef Gunter
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Schering Aktiengesellschaft
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