US 5,780,585 AGranted

Bacterial nitroreductase for the reduction of CB 1954 and analogues thereof to a cytotoxic form

AssigneeCancer Research Campaign Technology Limited

InventorsGillian Anlezark, Roger Melton, Roger Sherwood, Thomas Connors, Frank Friedlos, Michael Jarman, Richard Knox, Anthony Mauger, Caroline Joy Springer

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Abstract

A prodrug of the formula (I): ##STR1## where R.sup.1 is a group such that the compound R--NH.sub.2 represents actinomycin D, doxorubicin, mitomycin C, or a nitrogen mustard of the formula (IV): ##STR2## a prodrug of the formula (II): ##STR3## where R.sup.1 is a group such that the compound R.sup.2 OH is a phenolic nitrogen mustard; and processes whereby the prodrugs shown above are made in which a prodrug precursor compound is reacted with 4-nitrobenzyl chloroformate under anhydrous conditions.

Claims8

Dependent claims

A compound of the formula (I):

##STR34## where R.sup.1 is a group such that the compound R.sup.1 NH.sub.2 represents a nitrogen mustard of the formula (IV):
##STR35## where R' and R" are H, F, or CH.sub.3.

Dependencies are inferred from the claim text.

Facts

Application: 08/504,047Filed 7 Jun 1995 · division
Priority: GB 912246423 Oct 1991
Granted: 14 Jul 1998
Term ends: Not estimatedThe source records don’t support an estimate.

Classification21 codes

C07D 203/14
With only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring nitrogen atom: with carbocyclic rings…
C07C 219/34
Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton: having amino groups and esterified hydroxy groups…
C07C 271/18
With the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms: to carbon atoms of hydrocarbon radicals…
C07D 487/14
In which the condensed system contains three hetero rings: ortho-condensed systems