Conjugate compounds containing aza-macrocycles, and...

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01) A61K 49/00 (2006.01) A61K 49/06 (2006.01) C07D 257/02 (2006.01) C07F 9/6524 (2006.01) C07K 16/00 (2006.01)

Patent

CA 2058985

2058985 9116078 PCTABS00007 Conjugate compounds are described comprising a compound of formula (1), wherein A is a group -Alk3- or -Alk3N(R4)Alk4-; Alk1, Alk2, Alk3 and Alk4 which may be the same or different is each a C1-4alkylene chain optionally substituted by one or more C1-6alkyl groups; and R1, R2, R3 and R4, which may be the same or different, is each a hydrogen atom or a group-AlkR5 where Alk is an optionally substituted straight or branched C1-6 alkyl group and R5 is a hydrogen atom or a -CO2H, -CONR6R7 (where R6 and R7, which may be the same or different is each a hydrogen atom or an alkyl group) or -P(X1)(X2R8)L group where X1 and X2 is each an oxygen or sulphur atom, R8 is a hydrogen atom or an alkyl group and L is an aliphatic, aromatic, or heteroaromatic group or a linker group with the proviso that at least one of R1, R2, R3 and R4 is a group AlkP(X1)(X2R8)L where L is a linker group; and a metal complexes and/or salts thereof, coupled to a protein, peptide or carbohydrate. The conjugates are useful for imaging and in the treatment of abnormal cell disorders, such as in the treatment of tumours.

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