Cycloalkyl derivatives of 3-hydroxy-4-pyridinones

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C546S296000

Reexamination Certificate

active

07410985

ABSTRACT:
The present invention provides an cycloalkyl derivative of 3-hydroxy-4-pyridinone which is useful for the chelation of metal ions such as iron. Its preparation and use is described. In particular, the invention concerns the removal of iron in chemical and biological systems including chelating agents having the formula (I); wherein R1is X with the proviso that R2is Y; or R1is T with the proviso that R2is W; or R1is X with the proviso that R2R5N when taken together form a heterocyclic ring selected from piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl, wherein the group piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl is either unsubstituted or substituted with one to three C1to C6alkyl groups. X is C3-C6cycloalkyl; Y is selected from the group consisting of C1to C6cycloalkyl; C1to C6alkyl, and C1to C6alkyl monosubstituted with a C3-C6cycloalkyl; T is C1to C6alkyl; W is C3-C6cycloalkyl; R3is selected from the group consisting of hydrogen and C1to C6alkyl; R4is selected from the group consisting of hydrogen and C1to C6alkyl; R5is selected from the group consisting of hydrogen and C1to C6alkyl; and its pharmaceutically acceptable salt thereof. Pharmaceutical compositions of such compounds are useful in the removal of excess body iron from patients with iron overload diseases.

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