Shire LLC

Shire Holdings Ag

Shire Pharmaceuticals Inc.

Shire Biopharmaceuticals Holdings Ireland Limited

Richard Franklin

Bernard Thomas Golding

Peter A Cicala

Peter Cicala

Angus Macleod

This invention relates to the discovery of prodrugs of 3-or 5-substituted analogues of the selective platelet lowering agent anagrelide which have reduced potential for cardiovascular side-effects and which should therefore lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to prodrugs of certain imidazoquinazoline derivatives which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting the formation of blood platelets. An example of a compound of the present invention is methyl 2-(2-amino-5,6- dichloroquinazolin-3 (4H)-yl)-2-methylpropanoate or the 3,3-demethyl anagrelide open-ringed analog.

Substituted quinazolines for reducing platelet count

This invention relates to the discovery of 3- and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.

Substituted quinazolines

A method for the treatment of thrombocythemia in a subject comprising administering a therapeutically effective amount of compounds having the formulas (I) through (III) or equilibrating forms thereof.

Quinazoline derivatives and their use in the treatment of thrombocythemia

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Hampshire, United Kingdom

Richard Franklin