N-nitroso compounds, and their preparation and use

C - Chemistry – Metallurgy – 07 – D

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260/325, 260/291

C07D 295/22 (2006.01) C07C 311/47 (2006.01) C07D 295/26 (2006.01)

Patent

CA 1242200

ABSTRACT The invention concerns novel N-nitroso compounds having the general formula: Image (I) wherein A is lower alkyl or halolower alkyl; B is hydrogen; lower alkenyl; lower alkynyl; 3-6 C cycloalkyl; -RSO2NR3R4, or lower alkyl optionally monosubstituted with lower alkoxy, or 3-6 C cycloalkyl; R is straight or branched 2-5 C alkylene, optionally monosubstituted with SO2NR3R4 or CONR3R4, said alkylene always containing at least two carbon atoms separating the nitrogen atom of the urea from any SO2NR1R2 or SO2NR3R4; R1 and R2 are the same or different and selected from hydrogen, 5-6 C cycloalkyl, lower alkoxy, phenyl, benzyl, and straight or branched 1-6 C alkyl, optionally monosubstituted with hydroxy, lower alkoxy, SO2NR3R4, or CONR3R4; R1 and R2 may also together form a 4-5 C alkylene; and R3 and R4 are the same or different and selected from hydrogen or lower alkyl, or R3 and R4 together are a 4-5 C alkylene, together with pharmaceutical compositions thereof; processes for their manufacture, and methods of treatment. The compounds of formula (I) have antitumor activity.

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