Polycyclic conjugates

Details Polycyclic conjugates Polycyclic conjugates

C - Chemistry, Metallurgy

07

H

C07H 15/26 (2006.01) A61K 31/70 (2006.01) C07H 19/02 (2006.01)

Patent

CA 2082216

4-18840/A Polycyclic conjugates Abstract Staurosporin derivatives of the formula I are described, Image (I) in which R1 is hydrogen, hydroxyl, lower alkoxy or oxo and R2 is a radical of the formula II Image (II) *(D) or (L) configuration in which the configuration of the sugar moiety is derived from D-glucose, D-galactose or D-mannose, and R3 is hydrogen, hydroxyl, lower alkanoyloxy, lower alkoxy, or benzyloxy, benzoyloxy or phenyloxy, each of which is unsubstituted or substituted in the phenyl moiety by halogen, hydroxyl, trifluoromethyl, lower alkyl or lower alkoxy, R4 is hydroxyl, lower alkanoyloxy, benzoyloxy, benzyloxy, amino, lower alkylamino, di-lower alkylamino, lower alkoxycarbonylamino, C2-C20alkanoylamino, or benzoylamino, benzyloxycarbonylamino or phenyloxycarbonylamino, each of which is unsubstituted or substituted in the phenyl moiety by halogen, hydroxyl, trifluoromethyl, lower alkyl or lower alkoxy, R5 is hydrogen or lower alkyl, R6 is hydroxyl which is free or esterified with an aliphatic C2-C22carboxylic acid, or is lower alkoxycarbonyloxy, lower alkylsulfonyloxy, amino which is free or acylated with an aliphatic C2-C22carboxylic acid, or is lower alkoxycarbonylamino, azido, or benzoyloxy, benzyloxycarbonyloxy, benzoylamino, benzyloxycarbonylamino or phenylsulfonyloxy, each of which is unsubstituted or substituted in the phenyl moiety by halogen, hydroxyl, trifluoromethyl, lower alkyl or lower alkoxy, and R7 is hydroxyl which is free or esterified with an aliphatic C2-C22carboxylic acid, or is lower alkoxycarbonyloxy, lower alkylsulfonyloxy, azido, amino which is free or acylated with an aliphatic C2-C22carboxylic acid, or is lower alkylamino, di-lower alkylamino, lower alkoxycarbonylamino, carbamoylamino, or is benzoyloxy, benzyloxycarbonyloxy, phenylsulfonyloxy, benzoylamino, benzylamino or benzyloxycarbonylamino, each of which is unsubstituted or substituted in the phenyl moiety by halogen, hydroxyl, trifluoromethyl, lower alkyl, lower alkoxy or lower alkoxycarbonyl. These compounds have a pronounced and selective inhibitory action on the enzyme proteinkinase C and have, inter alia, an antitumour action.

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