Design and synthesis of renal dipeptidase inhibitors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...

Reexamination Certificate

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C568S008000

Reexamination Certificate

active

06927212

ABSTRACT:
Aminophosphinic acid derivatives were synthesized as potential inhibitors of renal dipeptidase, an enzyme overexpressed in benign and malignant colon tumors. Several compounds showed potent enzyme-inhibitory activity. These compounds can be used therapeutically and diagnostically for treatment and detection of tumors.

REFERENCES:
Buckhaults P., et al., “Secreted and cell surface genes expressed in benign and malignant colorectal tumors”,Cancer Research, (2001) vol. 61, pp. 6996-7001.
Parsons W., et al., “A new class of potent, slowly reversible dehydropeptidase inhibitors”,Biochemical International, (1991) vol. 23, pp. 1107-1115.
Harper C., et al., “Renal Dipeptidase: Localization and Inhibition”,Biochemica Et Biophysica Acta, (1971) vol. 242, pp. 446-458.
Accession No: 2003:114414. Tetrahedron Letters, 2003 Gurulingappa, Hallur et al., Design, synthesis and evaluation of new RDP inhibitors listed in Tetrahedron Letters (2003), vol. 44, No. 9, abstract.

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