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Substituted quinazolines

A compound and selected technology, applied in the direction of medical preparations containing active ingredients, extracellular fluid diseases, drug combinations, etc., can solve problems such as incomplete absorption, small solubility, etc.

Inactive Publication Date: 2011-05-18
SHIRE PLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

3-Substituted compounds, usually dimethyl or spirocyclopropyl analogues, are significantly less soluble than the parent compound at physiological pH (~7), which poses a great challenge for their efficient absorption
[0006] In addition, less potent anagrelide analogs may experience incomplete absorption even though they may have better cardiovascular properties

Method used

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  • Substituted quinazolines
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  • Substituted quinazolines

Examples

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Embodiment Construction

[0152] The present invention relates to novel prodrugs of substituted analogues of the established platelet lowering agent anagrelide. These compounds spontaneously ring-close at pH 7 and above to produce 3- or 5-substituted anagrelides that retain the antimegakaryocyte properties of anagrelide (thus maintaining thrombocytopenic activity ), but with reduced PDEIII inhibitory properties and therefore lower potential for unwanted cardiovascular and anticoagulant side effects.

[0153] Appropriate substitution at the 3-position of the anagrelide molecule effectively blocks the main metabolic site, thus preventing the formation of the highly potent PDEIII inhibitor 3-OH anagrelide. The 5-substituted analogs have the potential to indirectly sterically block metabolism at the preferred 3-position. These 3- or 5-substituted analogues of anagrelide also have the potential to improve the pharmacokinetic profile, because the 3-position of the anagrelide molecule is known to be the main...

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Abstract

This invention relates to the discovery of prodrugs of 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 the general formula (I) 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 the formation of blood platelets.

Description

field of invention [0001] The present invention relates to the discovery of prodrugs of substituted analogues of the selective platelet lowering agent anagrelide which have reduced potential cardiovascular side effects and should thus lead to improved patient compliance and safety in the treatment of myeloproliferative disorders . 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 act by inhibiting the formation of platelets. Background of the invention [0002] Anagrelide hydrochloride (Agrylin Xagrid ) are novel oral imidazoquinazolines that selectively reduce platelet counts in humans and are used for this purpose in the treatment of myeloproliferative disorders (MPD), such as primary Thrombocytosis (ET), in which an increased platelet count can place the patient at increased risk of thrombosis. The chemical structure ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/84A61K31/517A61P7/02
CPCC07D239/84A61P7/02Y02P20/55
Inventor 伯纳德·戈尔丁彼得·希卡拉理查德·富兰克林安格斯·马克莱奥德
Owner SHIRE PLC
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