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Imidazo [2,1-b] quinazolin-2-one derivatives and their use as platelet anti-aggregative agents

A technology of drugs and compounds, applied in the field of imidazo[2,1-b]quinazolin-2-one derivatives and their use as platelet anti-coagulation agents, can solve the problem of unaware anti-megakaryocyte potential, etc. question

Inactive Publication Date: 2011-05-18
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 anti-megakaryocyte potential (decreased platelet count) entirely alone, which may be associated with certain analogs

Method used

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  • Imidazo [2,1-b] quinazolin-2-one derivatives and their use as platelet anti-aggregative agents
  • Imidazo [2,1-b] quinazolin-2-one derivatives and their use as platelet anti-aggregative agents
  • Imidazo [2,1-b] quinazolin-2-one derivatives and their use as platelet anti-aggregative agents

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Embodiment Construction

[0129] The present invention relates to 3-substituted analogs of the established platelet lowering agent anagrelide. Substitution at the 3-position of the anagrelide molecule would be expected to block or inhibit a major site of metabolism and potentially prevent the formation of the highly potent PDE III inhibitor 3-OH anagrelide, while it has been surprisingly found that at the 1-position The 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 lower potential for unwanted cardiovascular and anticoagulant side effects. They also have the potential to improve pharmacokinetic profiles due to inhibition of metabolism.

[0130] Pharmaceutically acceptable acid addition salts of certain compounds of formula (I) can also be prepared in a conventional manner. For example, a sol...

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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 where the substituents have the meanings defined in claim (I): 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

field of invention [0001] The present invention relates to the discovery of substituted analogs of the selective platelet lowering 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 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 act by inhibiting megakaryocytopoeisis and thus 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 chemi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04A61K31/5025A61P7/02
CPCC07D487/04A61P19/08A61P35/02A61P7/02
Inventor 伯纳德·T·戈尔丁理查德·富兰克林安格斯·马克莱奥德彼得·希卡拉
Owner SHIRE PLC
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