Tetra-aza macrocycles and metal complexes thereof
AssigneeCelltech Limited
InventorsDavid Parker, Thomas Andrew Millican
Life of this patent
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Abstract
1,4,7,10-Tetrazacyclododecanes carrying a side chain terminating in a group capable of reacting with an antibody, and their complexes with a di- or tripositive metal having a coordination number of 6 or more can be used to prepare imaging agents. Typical metals are indium, copper, lead, bismuth, yttrium, terbium, gadolinium, and scandium. The compounds can be reacted with a monoclonal or polyclonal antibody or antibody fragment to target the metal to a specific type of tissue.
Claims6
A compound 1,4,7,10-tetrazacyclododecane of the formula:
- wherein
- r has a value of from 0 to 6;
- X is
- —NH—
- —(CH2)sNHNH—, or
- —(OCH2CH2)t—NH—
- in which s has a value of from 0 to 4 and t has a value of from 1 to 6;
- and
- Y1 is capable of reacting with an antibody and is selected from the group consisting of —COZ1, or —CO(R)Z1 in which Z1 is maleimido,
- Hal is a halogen atom;
- R is alkylene, phenylene, phenethylene, or cyclohexylmethylene;
- R11 is alkyl of 1 to 4 carbon atoms;
- and
- t′ has a value of from 1 to 6.
A compound consisting of:
- 1,4,7,10-tetrazacyclododecane of the formula:
A conjugate comprising 1,4,7,10-tetrazacyclododecane of the formula:
- wherein
- L is an aliphatic hydrocarbon chain interrupted at a point other than that of attachment to the depicted 1,4,7,10-tetrazacyclododecane ring by one or more members selected from the group consisting of —O—, —S—, —N(R5)—, —CON(R5)—, —N(R5)CO—, a cycloalkylene ring, and a pyridine ring, in which R5 is hydrogen or alkyl of 1 to 6 carbon atoms;
- Z′ is the residue of a group capable of reacting with a site on an antibody, and
- Ab is a monoclonal or polyclonal antibody or antibody fragment.
Dependencies are inferred from the claim text.