Cryptate compounds and methods for diagnosis and therapy

Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant... – In an organic compound

Reexamination Certificate

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C424S009363, C424S001690, C424S001770, C540S465000, C540S467000, C540S469000, C540S456000

Reexamination Certificate

active

06869589

ABSTRACT:
The present invention relates to cryptate compounds useful as chelating agents. In particular, the present invention relates to functionalized derivatives of certain cryptate compounds. These functionalized derivatives are suitable for use in radiolabelling and similar applications. The present invention also relates to a method for diagnosis or therapy of a disease utilizing functionalized derivatives of cryptase compounds. In one embodiment, the present invention relates to a compound which is capable of being radiolabelled of general formula (I) in which n represents an integer from 2 to 4, where each R4and R5is independently selected from —H, CH3, COOH, NO2, CH2OH, H2PO4, HSO3, CN, C═ONH2and CHO; X and Y are the same or different and are selected from the group of C—R, N, P and C—Z in which R represents a hydrogen or halogen atom or a hydroxyl, nitro, nitroso, amino, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl or cyano group, or a group of the formula —COOR′, COCOOR′, NH—COCH2Br, —NH—CO—CH═CH—COOR′ in which R′ is a hydrogen atom or alkyl group; or, W is selected from the group of NH, S and O; and Z is a functionalized linkage group which is capable of binding said compound of formula (I) to a molecular recognition unit and wherein at least one of X and Y is C—Z; or a pharmaceutically acceptable salt thereof

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