Recent Patents on Cardiovascular Drug Discovery

Advancements in technology for the treatment of valvularcardiac diseases seek to provide solutions for high risk patients in the form of percutaneous valve insertion for patients with complicated valvular disease not amenable to more traditional options. Within the last decade, cardiac valves designed for percutaneous insertion have emerged rapidly as a treatment option for valvular disease. This procedure serves as an alternative to open heart surgery, which is more invasive and requires longer ICU stay. Thus, the percutaneous valve insertion procedure has been used on older, frailer patients who are poor candidates for open heart surgery...

No abstract text is available yet for this article.

In the last decade, several direct oral anticoagulants (DOAC; dabigatran, rivaroxaban, apixaban, edoxaban) have been marketed for prophylaxis and/or treatment of thromboembolism without having specific antidotes available for their reversal. Current management of bleeding associated to DOAC includes the removal of all antithrombotic medications and supportive care. Non-specific procoagulant agents (prothrombin complex concentrates and activated factor VIIa) have been used in case of serious bleeding. Currently, some specific antidotes for the DOAC are under development...

Patients with pulmonary hypertension continue to present for both cardiac and non-cardiac surgery in greater numbers worldwide, and are usually managed by cardiothoracic anesthesiologists. These specialists have traditionally used intravenous therapy in the operating room to manipulate hemodynamics (cardiac output systemic and pulmonary vascular resistance), to effectively manage these high risk patients. General anesthesia involves the administration of both intravenous and inhaled drug therapy to achieve the desired goals, i...

Beta-adrenergic blockers remain one of the cornerstones in the management of coronary artery disease, both in chronic stable angina and myocardial infarction. These recommendations were based on studies conducted in the era prior to the establishment of the modern therapy for ischemic heart disease and myocardial infarction i.e. anti-platelet therapy, statins, and percutaneous coronary interventions. Recent studies emerged questioning the beneficial effect of beta-blockers in the management of patients with stable ischemic heart disease and myocardial infarction...

Cardiovascular disease and in particular, acute coronary syndromes are one of the principle causes of death in the industrialized countries. In the setting of acute coronary syndromes (both ST - segment or non ST - segment elevation myocardial infarction), platelets aggregation plays a key and central role in their development. Platelets are the mediators of hemostasis at sites of vascular injury, but they also mediate pathologic thrombosis; activated platelets stimulate thrombus formation in response to rupture of an atherosclerotic plaque or endothelial cell erosion promoting atherothrombotic disease...

Heart Failure (HF) is a progressive and fatal disorder, which ranks among the major public health problems in Brazil and worldwide. However, survival for patients who developed the syndrome after myocardial infarction (MI) enhanced significantly, as a result of an improvement of pharmacological therapies. A medical breakthrough was the discovery that remodelling of the left ventricle (LV) may be limited by the blockade of the renin-angiotensin system (RAS), at the level of angiotensin converting enzyme (ACE) and binding of angiotensin (Ang) II to its AT1 receptor...

The activation and aggregation of platelets at sites of vascular injury or near to implanted stent are pivotal in the development of thrombotic events during and after an acute coronary syndrome (ACS) or a percutaneous coronary intervention (PCI). For that reason, an exclusively oral dual antiplatelet treatment regimen with platelet P2Y12 receptor antagonists in addition to the cyclooxygenase inhibitor aspirin has become the cornerstone of treatment in that contest. However, every trial underlines the same problem: if maximizing antiplatelet therapy significantly attenuates ischemic events in patients with coronary artery disease, on the other side it may also increase bleeding phenomena...

Depression is a common mental health issue worldwide leading to disability, functional decline and increased mortality. Novel antidepressants have been developed during the last decades in order to treat depression syndromes. Some evidence suggests that major depression has been associated with the development of congestive heart failure and with adverse outcomes in patients with coronary heart disease. The purpose of the present article is to review the impact of novel antidepressant patent drugs on cardiovascular disease and arterial hypertension...

Steerable sheaths have been shown to reduce procedure time in the catheter ablation of atrial fibrillation (AF), where catheter positioning and stability is typically challenging. This review critically addresses and highlights the recent developments in design of sheaths used to manipulate the ablation catheter and how these developments may impact on the ablation procedure itself, in particular the likelihood of first-time success. Patents relating to steerable sheaths are reviewed and discussed to gauge potential future developments in this area...

Cardiovascular disease is the leading cause of death in American adults. Furthermore, the incidence of congestive heart failure is on the rise as a major cause of hospitalization and mortality in this population. Angiotensin Converting Enzyme (ACE) inhibitors prevent the production of angiotensin II, which has been shown to reduce mortality in patients with congestive heart failure. Angiotensin II receptor blockers (ARB) were developed as a direct inhibitor of angiotensin II. ARBs have been shown to be effective in the treatment of patients with systolic heart failure but do not cause chronic coughing which is a common side effect of ACE inhibitors...

Canagliflozin-with the patent number WO2011142478A1- belongs to a novel class of antidiabetic drugs known as SGLT2 inhibitors, which has been approved by FDA in March 2013. This medication acts through the inhibition of glucose reabsorption in the kidney resulting in glucosuria and thus lowering of glucose blood levels. There are several phase III clinical ongoing trials involving this new class of medications. So far promising results have been shown. This review article summarizes current knowledge regarding the novel SGLT2 inhibitor canagliflozin and its future perspectives in the treatment of type 2 diabetes mellitus...

Ablation of atrial fibrillation (AF) is increasingly common. Newer techniques have been developed and indications broadened to a greater number of patients with drug-resistant AF. The first end point of ablation is to cure AF without further need for Anti Arrhythmic Drugs (AADs), but the success rate at 1 year and over, after a single procedure, though higher than the success rate of AADs alone, is not 100% yet. The aim of the present work is to understand the added value of a persistent administration of previously ineffective AADs on the long-term success rate and to evaluate the timing of AADs suspension after ablation in different types of FA, when patients are in constant sinus rhythm after several months...

The most widely used heart valve worldwide is the Edwards Sapien, which currently has 60% of the worldwide transcatheter aortic valve implantation (TAVI) market. The CoreValve is next in line in popularity, encompassing 35% of the worldwide TAVI market. Although these two valves dominate the TAVI market, a number of newer transcatheter valves have been introduced and others are in early clinical evaluation. The new valves are designed to reduce catheter delivery diameter, improve ease of positioning and sealing, and facilitate repositioning or removal...

Coronary artery disease is the major cause of mortality and morbidity in the industrialized countries; in the United States of America and in Europe, it is responsible for one of every six deaths per year. In the setting of ischemic heart disease, angina pectoris and chest pain, in particular, are the major causes of emergency department accesses. Angina pectoris is a clinical syndrome characterized by discomfort typically in the chest, neck, chin and left arm induced by physical exertion, emotional stress and cold and is relieved by rest or by taking of nitrates...

The rationale for intracoronary administration of abciximab is discussed. The data on use of intracoronary abciximab in percutaneous coronary interventions in acute coronary syndromes and STEMI are reviewed. Evaluation of the niche where intracoronary administration of abciximab may be useful and future research into the subject and relevant patents are discussed.

Endothelial dysfunction represents an imbalance between vasodilatory and vasoconstrictory molecules secreted by endothelium. Oxidative stress is a major factor leading to endothelial dysfunction with significant prognostic implications for cardiovascular events. The generation of reactive oxygen species is strongly related to various oxidase enzymes such as xanthine oxidase, uncoupled endothelial nitric oxide synthase, cyclooxygenase, glucose oxidase, lipooxygenase, nicotinamide-adenine dinucleotide phosphate oxidase and to mitochondrial electron transport mechanisms...

In the last decades, the outstanding role of Thyroid gland in regulating both physiological and pathological operation of cardiovascular system has been acknowledged worldwide. Three main domains of Thyroid function, that is to say, euthyroidism -hyperthyroidism-hypothyroidism, have a direct impact on cardiac response through a variety of mechanisms. Cellular pathways mediate in cardiac contractility, cardiac output, cardiac rhythm, arterial blood pressure and peripheral vessel resistance. Particular biochemical algorithms exist not only between Thyroid hormones' serum concentration and thyroid gland but also between the hormones' serum level and heart muscle genes...

Valvular heart disease affects millions of Americans yearly and currently requires surgical intervention to repair or replace the defective valves. Through a close-knit collaboration between physicians, scientists and biomedical engineers, a vast degree of research and development has been aimed towards the optimization of prosthetic heart valves. Although various methods have made fantastic strides in producing durable prostheses, the therapeutic efficacy of prosthetic valves is inherently limited by a dependency upon lifelong anticoagulant regimens for recipients - a difficult challenge for many in clinical setting...

The assessment of tissue contact is an area undergoing much research as a means of improving the outcomes of cardiac radiofrequency ablation. This review provides an overview of RF ablation with specific reference to the relevance of good tissue contact to adequate RF lesion formation. An up-to-date review of the clinical evidence is provided, and recent patents of novel contact-sensing technologies in the field of cardiac RF ablation are presented.