Novel P2Y12 receptor antagonists

Simple SummaryContent extracted from patent full text and abstract with AI.

This patent discloses novel compounds that function as selective P2Y12 receptor antagonists. The P2Y12 receptor, mainly found on blood platelets, plays a critical role in platelet aggregation. The invention includes specific chemical classes (notably certain naphthalene, anthracene, and their derivatives) and new synthetic methods for producing these compounds. These antagonists are proposed for use as antithrombotic drugs for inhibiting platelet aggregation, thereby preventing or treating conditions associated with abnormal blood clotting, such as heart attacks and strokes. The invention addresses limitations of existing drugs like clopidogrel by offering faster, more controllable, and potentially more effective platelet inhibition.

Use CasesContent extracted from patent full text and abstract with AI.

• Prevention and treatment of arterial thrombosis (e.g., heart attacks, strokes)
• Acute treatment of myocardial infarction or unstable angina to prevent further clot formation
• Treatment of patients with vascular diseases (e.g. atherosclerosis, peripheral artery disease, cerebrovascular disease)
• Prophylaxis for patients at high risk of thromboembolic events (such as after certain surgeries or in atrial fibrillation)
• Adjunct therapy in percutaneous coronary intervention (PCI)
• Treatment of embolism or other clotting-related disorders
• Potential use in neuroinflammatory and neurodegenerative diseases (such as Alzheimer's and Parkinson's), due to P2Y12 receptor roles in the brain

BenefitsContent extracted from patent full text and abstract with AI.

• High specificity and selectivity for the P2Y12 receptor, reducing off-target effects
• Potential for faster onset and shorter/controllable duration of action compared to current drugs (like thienopyridines)
• Effective oral bioavailability and improved metabolic stability
• Reduced risk of irreversible inhibition and drug resistance seen with some current platelet inhibitors
• Broader therapeutic applicability, including possible CNS (central nervous system) applications
• Improved synthetic process yielding higher product with less time and milder conditions (via microwave-assisted reactions)
• Potential to combine with other antithrombotics for synergistic treatment

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

The present invention relates to compounds of Formula I, in which A and B are independently CH 2 , O, S, NH, C=O, C=NH, C=S or C=N-OH; X is NH, O, S, C=O or CH 2 and R 1 -R 5 are as defined in claim 1, which are P2Y 12 receptor antagonists and useful for treating, alleviating and/or preventing diseases and disorders related to P2Y 12 receptor function as well as pharmaceutical compositions comprising such compounds and methods for preparing such compounds. The present invention is further directed to the use of these compounds, alone or in combination with other therapeutic agents, for the alleviation, prevention and/or treatment of diseases and disorders, especially the use as antithrombotic agents for inhibiting platelet aggregation.