C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 303/16 (2006.01) A61K 31/00 (2006.01) A61K 31/275 (2006.01) A61K 31/335 (2006.01) A61K 31/395 (2006.01) A61K 31/655 (2006.01) A61K 31/66 (2006.01) C07C 247/16 (2006.01) C07C 255/49 (2006.01) C07C 271/22 (2006.01) C07C 309/63 (2006.01) C07C 311/22 (2006.01) C07C 311/30 (2006.01) C07D 333/24 (2006.01) C07D 405/12 (2006.01) C07F 9/655 (2006.01) C08B 37/16 (2006.01)
Patent
CA 2216655
The invention concernes borneol esters of general formula (I), in which R1 means T-C(O)-CH(OR6)-CH(NR7aR7b)-R8, C(O)-CH(OR6a)-CH[NR7(C(O)-CH(OR6b)- CH(NR7aR7b)-R8a)]-R8b; R7a R7b are identical or different and means R7; R7 means hydrogen, A, -C(O)R12, -C(O)OR12, -C(O)SR12, -C(O)NHR9d, -C(O)NR9dR9e, - SO2R12, C1-C10 alkyl; R8a, R8b are identical or different and mean R8; R8 means (i), heteroaryl substituted by X3, C7-C16 aralkyl, alkyl; A is B-[O- (CH2)t-C(O)]0 or 1-, farnesyl-P(O)(OR9d)-O-(CH2)t-C(O)-; B means protein kinase-inhibitors or farnesyl protein transferase-inhibitors such as for example farnesyl (ii); and T is a bond, Zi or a group (iii). The borneol esters can influence tubulin polymerisation and tubulin depolymerisation.
L'invention concerne des esters de bornéol de formule générale (I), où R?1¿ représente T-C(O)-CH(OR?6¿)-CH(NR?7a¿R?7b¿)-R?8¿, C(O)-CH(OR?6a¿)-CH[NR?7¿(C(O)-CH(OR?6b¿)-CH(NR?7a¿R?7b¿)-R?8a¿)]-R?8b¿; R?7a¿, R?7b¿ sont identiques or différents et représentent R?7¿; R?7¿ représente hydrogène, A, -C(O)R?12¿, -C(O)OR?12¿, -C(O)SR?12¿, -C(O)NHR?9d¿, -C(O)NR?9d¿R?9e¿, -SO¿2?R?12¿, C¿1?-C¿10? alkyl; R?8a¿, R?8b¿ sont identiques ou différents et représentent R?8¿; R?8¿ représente (i), hétéroaryle substitué par X?3¿, aralkyle C¿7?-C¿16?, alkyle; A représente B-[O-(CH¿2?)¿t?-C(O)]¿0 or 1?-, farnésyle-P(O)(OR?9d¿)-O-(CH¿2?)¿t?-C(O)-; B représente des inhibiteurs des protéines kinases ou des inhibiteurs de la farnésyl protéine transférase, par ex. farnésyl, (ii); T représente une liaison, Z?i¿ ou un groupe (iii). Ces esters de bornéol peuvent influencer la polymérisation de la tubuline ou la dépolymerisation 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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