Nitrosourea derivatives, pharmaceutical compositions thereof...

C - Chemistry – Metallurgy – 07 – C

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260/540.95

C07C 127/00 (1980.01)

Patent

CA 1142183

ABSTRACT OF THE DISCLOSURE The present invention relates to novel aminoalkyl sub- stituted nitrosourea derivatives as well as their acid adaition salts with pharmaceutically acceptable acids showing pronounced antineoplastic effectiveness in animal experiments. The novel compounds of the present invention may be re- presented by the following formula: Image I wherein X and Y are the same or different, and are selected from the group consisting of a phenyl group and a cyclohexyl group, said phenyl and cyclohexyl groups being optionally substituted with one or two substituents selected from a halogen atom, a lower alkyl group having from one to four carbon atoms inclusive, a trifIuore methyl group, a cyano group, a phenyl group, a cyclohexyl group und a lower alkyloxy group having from one to four carbon atoms inclusive. "Alkylenen" is an alkylene group, branched or unbranched, having from one to four carbon atoms inclusive, and R1 and R2 are the same or different, and are each selected from the group consisting of lower alkyl groups having from one to four carbon atoms inclusive, and benzyl groups, or they form together with the nitrogen atom a sturated five- or six-membered heterocyclic ring, such as a pyrrolidine, piperidine, morfoline, thio- morfoline, or N-lower-alkyl-piperazine ring, said hetero- cyclic ring being optionally substituted with lower alkyl qroups having from one to four carbon atoms inclusive, well as pharmaceutically acceptable acid addition salts thereof.

361277

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