BIOREDUCTIVELY-ACTIVATED PRODRUGS
Application 2380/CHENP/2005 published 2007-08-03, filed 2005-09-23
The present invention relates to a compound of formula (1), or a pharmaceutically acceptable salt thereof, wherein: Ar is a substituted aryl or heteroaryl group bearing at least one nitro or azido group or is a group of formula (2) or (3) wherein R1 and R2, which may be the same or different are independently optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, aryl, COR3 or, together with the intervening carbon atom, form an optionally substituted heterocycloalkyl or carbocyclic ring; L is -OC(O)- or -OP(0)(OR6)-; n isOorl; X is O, S, NR7 or a single covalent bond; R3 is OR4 or NR4R5; R4, R5, R6 and R7 are each independently hydrogen or optionally substituted alkyl or, where R3 is NR4R5 and R5 can be joined to form, together with the intervening nitrogen atom, a heterocycloalkyl ring; R8 is hydrogen, alkoxy or dialkylaminoalkyl; R9 is optionally substituted alkyl; Rio is hydrogen, alkyl, alkoxy or dialkylaminoalkyl; Rn and R12 are independently hydrogen, alkyl, alkoxy, thioalkoxy, amino, alkylamino, dialkylamino, morpholino, piperidino,piperazino or 1-aziridinyl; A is an optionally substituted aryl or heteroaryl ring; and Dr is a moiety such that DrXH represents a cytotoxic or cytostatic compound.
Applicant
1)ANGIOGENE PHARMACEUTICALS LTD.
:THE MAGDALEN CENTER, THE OXFORD SCIENCE PARK, OXFORDSHIRE OX4 4GA, UNITED KINGDOM U.K. 2)GRAY LABORATORY CANCER RESEARCH TRUST
Inventor
1)DAVIS, PETER, DAVID 2)NAYLOR, MATTHEW, ALEXANDER 3)THOMSON, PETER 4)EVERETT, STEVEN, ALBERT 5)STRATFORD, MICHAEL, RICHARD, LACEY 6)WARDMAN, PETER
International Info
Classification: C07D 333/36
Publication Number: WO 2004/085421 A2
Application Date: 2004-03-26
Priority Information
0306907.7 U.K. 2003-03-26