Conjugate compounds containing aza-macro-cycles and processes fo

Details Conjugate compounds containing aza-macro-cycles and processes fo Conjugate compounds containing aza-macro-cycles and processes fo

1995-05-26

1997-11-04

Chan, Christina Y.

Chemistry: natural resins or derivatives; peptides or proteins;

Proteins, i.e., more than 100 amino acid residues

Blood proteins or globulins, e.g., proteoglycans, platelet...

530350, 5303913, 5303915, 5303919, 530402, 540465, 540474, C07K 1706

Patent

active

056841353

ABSTRACT:
##STR1## Conjugate compounds are described comprising a compound of formula (1), wherein A is a group --Alk.sup.3 -- or --Alk.sup.3 N(R.sup.4)Alk.sup.1 --, Alk.sup.2, Alk.sup.3 and Alk.sup.4 which may be the same or different is each a C.sub.1-4 alkylene chain optionally substituted by one or more C.sub.1-6 alkyl groups; and R.sup.1, R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, is each a hydrogen atom or a group--AlkR.sup.5 where Alk is an optionally substituted straight or branched C.sub.1-6 alkyl group and R.sup.5 is a hydrogen atom or a --CO.sub.2 H, --CONR.sup.6 R.sup.7 (where R.sup.6 and R.sup.7, which may be the same or different is each a hydrogen atom or an alkyl group) or --P(X.sup.1)(X.sup.2 R.sup.8)L group where X.sup.1 and X.sup.2 is each an oxygen or sulphur atom. R.sup.8 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 R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is a group AlkP(X.sup.1)(X.sup.2 R.sup.8)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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