Heterobifunctional linking agents derived from N-succinimido-dithio-alpha methyl-methylene-benzoates
First Claim
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1. A compound of the formula:
- ##STR3## wherein X is a C1 -C4 alkyl group and Y is H or a C1 -C4 alkyl group and Z.sup.⊕
is a pharmaceutically acceptable cation.
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Abstract
The efficacy of immunotoxins having an antibody that recognizes a tumour associated antigen linked to a cytotoxin through a heterobifunctional agent of the disulphide type is improved by providing in the heterobifunctional agent a molecular grouping creating steric hindrance in relation to the disulphide link. This steric hindrance can be provided by a methyl substituted methylene group located in the heterobifunctional link adjacent to the disulphide bond.
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4 Claims
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1. A compound of the formula:
- ##STR3## wherein X is a C1 -C4 alkyl group and Y is H or a C1 -C4 alkyl group and Z.sup.⊕
is a pharmaceutically acceptable cation. - View Dependent Claims (2)
- ##STR3## wherein X is a C1 -C4 alkyl group and Y is H or a C1 -C4 alkyl group and Z.sup.⊕
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3. A compound of the formula:
- ##STR4## wherein X is a C1 -C4 alkyl group and Y is H or a C1 -C4 alkyl group and Z.sup.⊕
is a pharmaceutically acceptable cation. - View Dependent Claims (4)
- ##STR4## wherein X is a C1 -C4 alkyl group and Y is H or a C1 -C4 alkyl group and Z.sup.⊕
Specification
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Current AssigneeICRF Limited
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Original AssigneeICRF Limited
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InventorsThorpe, Philip E.
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Primary Examiner(s)Rotman, Alan L.
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Application NumberUS07/090,386Time in Patent Office810 DaysField of Search548/542, 546/281US Class Current546/278.7CPC Class CodesC07D 207/46 with hetero atoms directly ...C07D 401/12 linked by a chain containin...
