Staurosporine derivatives substituted at methylamino nitrogen

Claim 1

A N-substituted staurosporine compound of formula (I) [Stau]--N(CH.sub.3)--R in which [Stau] represents a residue of the formula ##STR15## and R represents an acyl radical selected from the group consisting of: (a) an acyl radical of the formula Z--C(═W)-- in which W is oxygen or sulfur, and Z represents C 1 -C 7 -alkyl, which is optionally substituted by halogen, by carboxy or by C 1 -C 4 -alkoxycarbonyl, or phenyl, pyridyl, furyl, thienyl, imidazolyl, quinolyl, isoquinolyl, benzofuranyl or benzimidazolyl, each of which is unsubstituted or substituted by C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy, halogen, nitro, trifluoromethyl, carboxy, C 1 -C 4 -alkoxycarbonyl, methylenedioxy, cyano or combinations thereof; (b) an acyl radical of the formula R b o --CO-- in which R b o represents hydrogen, a C 1 -C 19 -alkyl group or such an alkyl group substituted by amino, halogen and/or carboxy in the form of a free acid, a salt, a cyano group or a C 1 -C 4 -alkyl ester; (c) an acyl radical of the formula R o --SO 2 -- in which R o represents C 1 -C 7 -alkyl or phenyl, pyridyl, furyl, thienyl, imidazolyl, quinolyl, isoquinolyl, benzofuranyl or benzimidazolyl, each of which is unsubstituted or is substituted by C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy, halogen, nitro, trifluoromethyl, carboxy, C 1 -C 4 -alkoxycarbonyl, methylenedioxy, cyano or combinations thereof; (d) an acyl radical of the formula R o --O--CO in which R o represents C 1 -C 7 -alkyl or phenyl, pyridyl, furyl, thienyl, imidazolyl, quinolyl, isoquinolyl, benzofuranyl or benzimidazolyl, each of which is unsubstituted or is substituted by C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy, halogen, nitro, trifluoromethyl, carboxy, C 1 -C 4 -alkoxycarbonyl, methylenedioxy, cyano or combinations thereof; (e) an acyl radical of the formula ##STR16## in which W represents sulfur or oxygen, R 1 is hydrogen and R 2 represents C 1 -C 7 -alkyl, C 3 -C 7 -alkenyl or phenyl, pyridyl, furyl, thienyl, imidazolyl, quinolyl, isoquinolyl, benzofuranyl or benzimidazolyl, each of which is unsubstituted or is substituted by C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy, halogen, nitro, trifluoromethyl, carboxy, C 1 -C 4 -alkoxycarbonyl, methylenedioxy, cyano or combinations thereof; (f) an acyl radical of a naturally occurring α-amino acid of the L series; (g) an acyl radical of a naturally occurring α-amino acid of the L-series wherein the α-amino group is protected by an amino-protecting group, and when said α-amino acid contains a hydroxy radical, said hydroxy radical is either unprotected or protected by a hydroxy-protecting group and when said α-amino acid contains a carboxy group, said carboxy group is either unprotected or esterified by a lower alkanol or a phenyl-lower alkanol; and (h) an acyl radical of a naturally occuring α-amino acid of the L-series which carries a hydroxy radical that is protected by a hydroxy-protecting group and pharmaceutically acceptable salts thereof.