Synthesis of 4-substituted-trans-1, 2-diaminocyclohexyl polyamin

Organic compounds -- part of the class 532-570 series – Organic compounds – Carboxylic acids and salts thereof

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5303915, 564217, 558 17, C07C 6108

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active

052929388

ABSTRACT:
Cyclo agents useful in forming antibody-metal conjugates useful for diagnostic and therapeutic purposes. New compounds and processes of forming these compounds are disclosed including 4-haloacetamido-trans-1,2-diaminocyclohexyl polyaminocarboxylate and 4-isothiocyanato-trans-1,2-diamino cyclohexane-N,N,N',N'-tetra acetic acid.

REFERENCES:
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patent: 5021571 (1991-06-01), Mease et al.
patent: 5089663 (1992-02-01), Mease et al.
Mease, Supplement to J. Nucl. Med. 32, p. 1023 abstract No. 482. (May, 1991).
Witiak et al., "Stereocontrolled Syntheses for the Six Diastereomeric 1,2-Dihydroxy-4,5-diaminocyclohexanes: Pt.sup.II Complexes and P-388 Antitumor Properties", J. Med. Chem., 30, pp. 1327-1336, 1987.
Srivastava, et al., "CDTA-In-111-Anti-CEA F(ab').sub.2 Immunoconjugates Produce Improved Biodistribution and Better Images in Nude Tumor Mice", J. Nucl. Med., 32, p. 1023, 1991.
Mease, et al., "Effect of Chelate Rigidity On In Vivo Radioimmunoconjugate Distribution", J. Label. Comp. Radiopharm., 30, p. 319, 1991.

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