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Substituted quinazolines

A compound and selected technology, which can be used in medical preparations containing active ingredients, extracellular fluid diseases, drug combinations, etc., can solve the problem of not realizing the anti-megakaryocyte potential, etc.

Inactive Publication Date: 2011-05-25
SHIRE PLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the disclosure does not recognize the fully isolated anti-megakaryocyte potential (decreased platelet count), which may be associated with some analogs

Method used

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  • Substituted quinazolines
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  • Substituted quinazolines

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Embodiment Construction

[0084] The present invention relates to novel prodrugs of substituted analogues of the established platelet reducing agent anagrelide. These compounds spontaneously ring-close at pH 7 and above to produce 3- or 5-substituted anagrelide, which retain the antimegakaryocyte properties of anagrelide (thus maintaining thrombocytopenic activity), but have reduced PDEIII inhibitory properties, and thus Has a lower potential for adverse cardiovascular and antiaggregative side effects.

[0085] Appropriate substitution at the 3-position of the anagrelide molecule effectively blocks the main metabolic site and thus prevents the formation of the highly potent PDE III inhibitor 3-OH anagrelide. 5-Substituted analogs have the potential to indirectly sterically interfere with metabolism at the preferred 3-position. These 3- or 5-substituted analogs of anagrelide also have the potential to improve the pharmacokinetic profile, since the 3-position of the anagrelide molecule is known to be th...

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Abstract

This invention relates to the discovery of 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 the general formula shown below wherein the substituents have the meanings defined in claim 1: and 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.

Description

technical field [0001] The present invention relates to the discovery of substituted analogs of the selective thrombocytopenic agent anagrelide which have a reduced potential for cardiovascular side effects and should therefore lead to improved patient compliance and safety in the treatment of myeloproliferative disorders sex. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have utility as platelet reducing agents in humans. The compounds of the present invention act by inhibiting megakaryocytopoeisis, and thus the formation of platelets. Background technique [0002] Anagrelide Hydrochloride is a novel oral imidazoquinazoline that selectively reduces platelet count in humans and is used for this purpose in the treatment of myeloproliferative disorders (MPD) such as essential thrombocythemia etiology (ET), in which an increased platelet count can place a patient at increased risk for blood clots. The chemical structure of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/84A61K31/517A61P7/02
CPCC07D239/84A61P7/02A61P35/02
Inventor 伯纳德·戈尔丁理查德·富兰克林彼得·希卡拉
Owner SHIRE PLC
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