Chiesi Farmaceutici S.p.a.

Apotex Inc.

Apotex Technologies Inc.

Michael Spino

Bernard Charles Sherman

Tim Fat Tam

Yanqing Zhao

Yingsheng Wang

Wanren Li

Arnold Munnich

Birenkumar Hasmukhbhai Shah

Anita Hui

Cihua Yang

Antonio Piga

Mohammed N Kabir

Ioav Cabantchik

The invention is directed to pharmaceutical compositions such as tablets that exhibit delayed release properties when administered as either whole or half tablets. The invention is also directed to delayed release tablets comprising deferiprone for oral administration, for which twice daily administration is bioequivalent to the same daily dose of an immediate release tablet administered thrice daily. The invention is also directed to methods of making and using the same.

Delayed release deferiprone tablets and methods of using the same

An oral pharmaceutical liquid formulation comprising deferiprone and a taste masking composition, said taste masking composition comprising an effective amount of a sweetener (such as sucralose) per liter of liquid composition, an effective amount of a thickening and suspension aid, (for example hydroxyethylcellulose), per liter of liquid composition, an effective amount of a humectant (such as glycerin) per liter of liquid composition, and an effective amount of at least one flavoring agent, wherein a final form of said taste-masked pharmaceutical has a substantially non-bitter and palatable taste.

Liquid formulation for deferiprone with palatable taste

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 Ris X with the proviso that Ris Y; or Ris T with the proviso that Ris W; or Ris X with the proviso that RRN 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 Cto Calkyl groups. X is C-Ccycloalkyl; Y is selected from the group consisting of Cto Ccycloalkyl; Cto Calkyl, and Cto Calkyl monosubstituted with a C-Ccycloalkyl; T is Cto Calkyl; W is C-Ccycloalkyl; Ris selected from the group consisting of hydrogen and Cto Calkyl; Ris selected from the group consisting of hydrogen and Cto Calkyl; Ris selected from the group consisting of hydrogen and Cto Calkyl; 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.

Cycloalkyl derivatives of 3-hydroxy-4-pyridinones

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 Ris X with the proviso that Ris Y; or Ris T with the proviso that Ris W; or Ris X with the proviso that RRN 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 Cto Calkyl groups. X is C-Ccycloalkyl; Y is selected from the group consisting of Cto Ccycloalkyl; Cto Calkyl, and Cto Calkyl monosubstituted with a C-Ccycloalkyl; T is Cto Calkyl; W is C-Ccycloalkyl; Ris selected from the group consisting of hydrogen and Cto Calkyl; Ris selected from the group consisting of hydrogen and Cto Calkyl; Ris selected from the group consisting of hydrogen and Cto Calkyl; 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. 

A method of treating iron induced cardiac disease in a patient with iron overload, such as in thalassemia or the like comprising administering to the patient a therapeutically effective amount of deferiprone or a physiologically acceptable salt thereof sufficient to treat iron induced cardiac disease normally associated with iron overload.

Use for deferiprone

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Pickering, Canada

Michael Spino