Claims
- 1. A polysubstituted diethylenetriaminepentaacetic acid (DTPA) chelating agent of the following formula 2 to 3 having one side chain attached to the carbon backbone of the DTPA, said side chain being an alkyl-aryl group with n=1-5, and which contains a functional moiety X selected from the group consisting of nitro, methoxy, hydroxy, isothiocyanate and haloacetamide groups, and which has one or more additional side chains (R.sub.1 -R.sub.4) and (R'.sub.1 -R'.sub.4) linked to the carbon backbone of the DTPA, said (R.sub.1 -R.sub.4) and (R'.sub.1 -R'.sub.4) being selected from the group consisting of hydrogen, straight or branched chain alkyl group with 1-15 carbon atoms, aryl group with 1-15 carbon atoms, and mixtures thereof, wherein at least one of the additional side chains must contain at least one carbon atom: ##STR2## being conjugated with a protein.
- 2. The polysubstituted diethylenetriaminepentaacetic acid chelating agent conjugate of claim 1 in which X is a hydroxysuccinimide ester group.
- 3. The polysubstituted DTPA chelating agent conjugate of claim 1, having the following formula 4 or 5: ##STR3## wherein X is nitro, amino or isothiocyanate group; and wherein (R.sub.1 -R.sub.4) and (R'.sub.1 -R'.sub.4) groups are as follows:
- ______________________________________Formula R.sub.1, R.sub.1 ' R.sub.2, R.sub.2 ' R.sub.3, R.sub.3 ' R.sub.4, R.sub.4 '______________________________________4 H H, H CH.sub.3, H H, H4 H H, H H, H CH.sub.3, H4 H H, H CH.sub.3, H CH.sub.3, H5 H, H H CH.sub.3, H H, H5 H, H H H, H CH.sub.3, H5 H, H H CH.sub.3, H CH.sub.3, H.______________________________________
- 4. The DTPA conjugate of claim 1 wherein said protein is a mono- or poly-clonal antibody or a fragment thereof.
- 5. The DTPA conjugate of claim 4 being radiolabelled.
- 6. The DTPA conjugate of claim 5 wherein radiolabel is selected from the group consisting of In-.sup.111, Y-90, Bi-212, Ga-68 and Sc-47.
- 7. A method of delivering radiolabelled compound to a target site in a host comprising administering to a host an amount of the compound of claim 6 effective to produce radiotherapeutic or radioimaging effect at a target site in said host.
Parent Case Info
This application is a divisional of copending application Ser. No. 07/285,025 filed on Dec. 16, 1988, now U.S. Pat. No. 5,099,069, which is a divisional of application Ser. No. 06/903,723, filed Sep. 5, 1986, now U.S. Pat. No. 4,831,175, both of which applications are, in their entirety, incorporated by reference herein.
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Divisions (2)
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Number |
Date |
Country |
Parent |
285025 |
Dec 1988 |
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Parent |
903723 |
Sep 1986 |
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