FACTOR XIa INHIBITORS

Selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein, as represented by Formula I, address the inadequacies in managing thrombosis and inflammation by effectively targeting these key enzymes, offering improved treatment options for thrombosis and embolism.

WO2015164308A1 Publication Date: 2015-10-29MERCK SHARP & DOHME CORP +22
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Patent Information

Application Number
PCT/US2015/026774
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2014-04-22
Filing Date
2015-04-21
Publication Date
2015-10-29

AI Technical Summary

Technical Problem

Current treatments for thrombosis, embolism, and hypercoagulability lack effective inhibitors for Factor XIa and plasma kallikrein, which are key players in blood coagulation and inflammation, leading to inadequate management of conditions like thromboembolic disorders and diabetic macular edema.

Method used

Development of selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein compounds, specifically represented by Formula I, which can be used alone or in combination with other therapeutic agents to treat thrombosis, embolism, and fibrotic changes.

Benefits of technology

The compounds effectively inhibit Factor XIa and plasma kallikrein, providing therapeutic benefits in conditions such as thrombosis, embolism, and inflammatory disorders, including diabetic macular edema, by reducing thrombogenicity and improving vascular permeability.

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Abstract

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
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