EP 0057700 A4 19821117 - Nitrosourea derivatives having antitumour activity and pharmaceutical compositions containing the same.
Title (en)
Nitrosourea derivatives having antitumour activity and pharmaceutical compositions containing the same.
Title (de)
Nitrosoharnstoffabkömmlinge mit Antitumoraktivität und diese enthaltende pharmazeutische Zusammensetzungen.
Title (fr)
Dérivés de nitroso-urées possédant une activité antitumorale et compositions pharmaceutiques les contenant.
Publication
Application
Priority
US 17794080 A 19800814
Abstract (en)
[origin: WO8200642A1] Novel, highly effective nitrosoureas useful in the treatment of mammaliam tumors. The high degree of selectivity of the compounds is attributed to the positioning of certain electronegative groups on the ss-carbon of the unnitrosated side of the molecule. Hypothetically, this may aid in hydrogen bonding to certain enzyme active sites, thereby more selectively eliminating enzymatic maintenance of proteins masking tumor cell surface antigens, which in turn prevent normal immune system destruction of neoplastic tissue. The activity of the compounds is further shown to be superior to that of MeCCNU (1-(4-trans-methylcyclohexyl)-3-(2-chloroethyl)-3-nitrosourea), a highly active compound commonly employed in cancer chemotherapy. Compounds of the following general formula are disclosed: (FORMULA) and pharmaceutically acceptable salts thereof, wherein hal is chlorine or fluorine; R is a hydroxy, halogen, carboxylic acid group or derivatives thereof; n is 4 to 7, wherein the cycycloalkyl group may be optionally substituted with one or more methyl groups or hydroxyl groups.
IPC 1-7
IPC 8 full level
C07D 307/62 (2006.01); C07D 407/00 (2006.01); C07D 407/04 (2006.01)
CPC (source: EP)
C07D 307/62 (2013.01); C07D 407/04 (2013.01)
Designated contracting state (EPC)
AT CH DE FR GB LI LU NL SE
DOCDB simple family (publication)
WO 8200642 A1 19820304; DK 167182 A 19820414; DK 167282 A 19820414; EP 0057699 A1 19820818; EP 0057699 A4 19821108; EP 0057700 A1 19820818; EP 0057700 A4 19821117; HU 185969 B 19850428; JP S57501580 A 19820902; JP S57501581 A 19820902; NO 821220 L 19820414; NO 821221 L 19820414; WO 8200644 A1 19820304
DOCDB simple family (application)
US 8101089 W 19810814; DK 167182 A 19820414; DK 167282 A 19820414; EP 81902234 A 19810814; EP 81902235 A 19810814; HU 300481 A 19810814; JP 50279781 A 19810814; JP 50279881 A 19810814; NO 821220 A 19820414; NO 821221 A 19820414; US 8101088 W 19810814