Organic compounds -- part of the class 532-570 series – Organic compounds – Amino nitrogen containing
Patent
1985-12-30
1987-03-17
Warren, Charles F.
Organic compounds -- part of the class 532-570 series
Organic compounds
Amino nitrogen containing
546332, 548567, 514331, 514408, 514428, 514595, C07C12717, C07D23902
Patent
active
046509003
ABSTRACT:
The present invention relates to novel amino alkyl substituted urea derivatives as well as their acid addition salts with pharmaceutically acceptable acids, to methods for the preparation of said derivatives and pharmaceutical compositions containing same, and a method for the treatment of tumors therewith.
The novel urea derivatives have shown pronounced anti-neoplastic activity when tested against various tumor models in animals.
The novel compounds of the present invention may be represented by the following formula: ##STR1## wherein X and Y are the same or different and are selected from the group consisting of a phenyl group, each of said phenyl groups being optionally substituted with one or two groups selected from halogen, CF.sub.3, OH, or alkoxy (1-4 C-atoms); and R.sup.1 and R.sup.2 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, or they form together with the nitrogen atom a saturated five- or six-membered heterocyclic ring; R.sup.3 and R.sup.4 are each selected from hydrogen, lower alkyl or alkenyl groups with from 1-6 carbon atoms inclusive, cyclopentyl or cyclohexyl; and n is 0 or 1, as well as pharmaceutically acceptable acid addition salts thereof.
When X is different from Y and/or R.sup.3 is different from R.sup.4 the compounds of Formula I exist as optical isomers, which may be separated in the individual enantiomers, which often show the activity in different degree. These individual isomers as well as their isolation fall within the scope of the present invention.
REFERENCES:
patent: 3388158 (1968-06-01), Surrey
patent: 4216228 (1980-08-01), Yamada et al.
Bogeso Klaus P.
Jensen Klaus G.
Lassen Niels
Flaherty Elizabeth A.
H. Lundbeck A/S
Hueschen Gordon W.
Warren Charles F.
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