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Substituted quinazolines

A technology of metabolic reactions and compounds, applied in the field of imidazoquinazoline derivatives, can solve the problem of not realizing the anti-megakaryocyte potential and so on

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
  • Substituted quinazolines
  • Substituted quinazolines

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Embodiment Construction

[0086] The present invention relates to 3-substituted analogs of the established platelet reducing agent anagrelide. It was expected that a substitution at the 3-position of the anagrelide molecule would block or impede a major site of metabolism and potentially prevent the formation of the highly potent PDE III inhibitor 3-OH anagrelide, while it was unexpectedly found that a substitution at the 1-position Substitution eliminates 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.

[0087] Pharmaceutically acceptable acid addition salts of certain compounds of formula (I) can also be prepared in a conventional mann...

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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 (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 a patient at increased risk for blood clots. The chemical ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04A61K31/519A61P7/00
CPCC07D487/04A61P35/00A61P35/02A61P7/00A61P7/02
Inventor 伯纳德·戈尔丁理查德·富兰克林
Owner SHIRE PLC
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