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Substituted quinazolines as blood platelet lowering agents

A technology of solvates, compounds, applied in the field of substituted quinazolines as platelet reducing agents, able to solve problems such as unrecognized anti-megakaryocyte potential

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

AI Technical Summary

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 as blood platelet lowering agents
  • Substituted quinazolines as blood platelet lowering agents
  • Substituted quinazolines as blood platelet lowering agents

Examples

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Embodiment Construction

[0121] The present invention relates to novel 3- or 5-substituted analogs of the established platelet reducing agent anagrelide. Substitutions at the 3- or adjacent 5-position of the anagrelide molecule were expected to block or impede major sites of metabolism and potentially prevent the formation of the highly potent PDE III inhibitor 3-OH anagrelide, while unexpectedly Surprisingly, it was found that substitution at the 1-position abolishes PDE III inhibition. The compounds of the present invention retain the antimegakaryocyte properties (and thus the thrombocytopenic activity) of the parent drug molecule, but have reduced PDE III inhibitory properties and therefore have a lower potential for adverse cardiovascular and antiaggregative side effects. They also have the potential to improve the pharmacokinetic profile as a result of inhibited metabolism.

[0122] Pharmaceutically acceptable acid addition salts of certain compounds of formula (I) can also be prepared in a conv...

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Abstract

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 the general formula (I) shown below wherein the meanings of the substituents are 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 3- and 5-substituted analogs of the selective thrombocytopenic agent anagrelide which have a reduced potential for cardiovascular side effects and should therefore lead to improved outcomes in the treatment of myeloproliferative disorders Patient compliance and safety. 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 counts in humans and is used for this purpose in the treatment of myeloproliferative disorders (MPD), such as idiopathic platelet Hypertrichosis (ET), in which an increased platelet count can place a patient at increased risk for blood clots. The chemi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/14A61K31/519A61P7/00C07D487/14C07D495/14C07D491/147
CPCC07D487/14C07D495/14C07D471/14C07D491/147A61P7/00A61P7/02A61P9/10
Inventor 伯纳德·戈尔丁理查德·富兰克林基姆·赫尔斯特
Owner SHIRE PLC
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