Recent patents on cardiovascular drug discovery最新文献_第9页

The protective effects of levosimendan on ischemia/reperfusion injury and apoptosis. 左西孟旦对缺血再灌注损伤及细胞凋亡的保护作用。

Recent patents on cardiovascular drug discovery Pub Date : 2011-01-01 DOI: 10.2174/157489011794578482

Patrick Scheiermann, Andres Beiras-Fernandez, Haitham Mutlak, Florian Weis

{"title":"The protective effects of levosimendan on ischemia/reperfusion injury and apoptosis.","authors":"Patrick Scheiermann, Andres Beiras-Fernandez, Haitham Mutlak, Florian Weis","doi":"10.2174/157489011794578482","DOIUrl":"https://doi.org/10.2174/157489011794578482","url":null,"abstract":"Levosimendan is a calcium sensitizer with positive inotropic and vasodilating properties. It increases the sensitivity of troponin C for calcium, opens adenosine triphosphate-dependent potassium K(+) channels and inhibits phosphodiesterase III. Levosimendan is approved for use in cardiac failure but large clinical trials have raised doubts whether levosimendan is superior to β-adrenergic agonists regarding long-term survival of patients. Despite this controversy, there is growing evidence of beneficial effects of levosimendan in ischemia/reperfusion (I/R) injury due to its effect on K(+) channels. As a consequence, patents on K(+) channel agonists have been granted recently for reducing injury in organs or tissue in transplants and trauma therapy. Moreover, experimental studies and clinical trials have shown that levosimendan effectively inhibits cardiomyocyte apoptosis. The underlying molecular mechanism is currently unclear. However, it is tempting to assume that levosimendan inhibits cardiomyocyte apoptosis due to its beneficial effect on I/R injury. However, the link between these two phenomena has not been well established. This review summarizes experimental studies and clinical trials on the effects of levosimendan in I/R injury and apoptosis also discussing recent patents.","PeriodicalId":20905,"journal":{"name":"Recent patents on cardiovascular drug discovery","volume":"6 1","pages":"20-6"},"PeriodicalIF":0.0,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/157489011794578482","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"29578257","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 13

Novel agents for the acute conversion of atrial fibrillation: focus on vernakalant. 房颤急性转化期的新型药物:以vernakalant为重点。

Recent patents on cardiovascular drug discovery Pub Date : 2011-01-01 DOI: 10.2174/157489011794578428

Pio Cialdella, Daniela Pedicino, Pasquale Santangeli

{"title":"Novel agents for the acute conversion of atrial fibrillation: focus on vernakalant.","authors":"Pio Cialdella, Daniela Pedicino, Pasquale Santangeli","doi":"10.2174/157489011794578428","DOIUrl":"https://doi.org/10.2174/157489011794578428","url":null,"abstract":"Vernakalant is a novel anti-arrhythmic drug, recently approved for the cardioversion of recent-onset atrial fibrillation. Its action is mainly due to the blockade of atrial-selective channels responsible of the ultra-rapid delayed rectifier current I(Kur), but has also important interactions with other channels and currents, such as I(Na) (inward sodium current), and I(KACh) (acetylcholine-regulated potassium current). Due to the relatively selective blockade of the I(Kur), vernakalant prolongs the effective refractory period of the atria with minimal effects on the ventricles, thus minimizing the risk of proarrhythmia. Thus far vernakalant has been tested in three placebo-controlled trials (ACT I, ACT II and ACT III) and in one amiodarone-controlled study (AVRO). Vernakalant has been demonstrated more effective than both placebo and amiodarone for the rapid conversion of atrial fibrillation, without significant adverse events. This article will review the recent patents on this novel atrial-selective agent, discussing its mechanisms of action and possible clinical applications in the real-world practice.","PeriodicalId":20905,"journal":{"name":"Recent patents on cardiovascular drug discovery","volume":"6 1","pages":"1-8"},"PeriodicalIF":0.0,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/157489011794578428","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"29599865","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 6

Ultrasound microbubble contrast and current clinical applications. 超声微泡造影剂及其临床应用现状。

Recent patents on cardiovascular drug discovery Pub Date : 2011-01-01 DOI: 10.2174/157489011794578446

Shiva Dindyal, Constantinos Kyriakides

引用次数: 32

Effect of doxycycline on atherosclerosis: from bench to bedside. 多西环素对动脉粥样硬化的影响:从实验到临床。

Recent patents on cardiovascular drug discovery Pub Date : 2011-01-01 DOI: 10.2174/157489011794578419

Gastón A Rodriguez-Granillo, Agustina Rodriguez-Granillo, José Milei

{"title":"Effect of doxycycline on atherosclerosis: from bench to bedside.","authors":"Gastón A Rodriguez-Granillo, Agustina Rodriguez-Granillo, José Milei","doi":"10.2174/157489011794578419","DOIUrl":"https://doi.org/10.2174/157489011794578419","url":null,"abstract":"Matrix metalloproteinases (MMPs) have a pivotal role in the natural history of atherosclerosis and its cardiovascular consequences. Non-selective MMP inhibition with doxycycline appears as a potential strategy to reduce the residual risk observed in patients already at intensive lipid lowering strategies. However, specific MMPs have different and even contradicting roles in the natural history of atherosclerosis, rendering broad spectrum MMP inhibition an important yet somewhat simplistic approach towards residual risk reduction in coronary atherosclerosis. Overall, the balance of non-selective MMP inhibition might shift to the favorable side in particular settings such as in acute coronary syndromes, where in addition to its potential plaque stabilization properties, doxycycline shows promise in preventing ischemia-reperfusion injury and left ventricular remodeling. Nevertheless, to date, most animal models used do not represent advanced coronary atherosclerosis seen in humans, and large and well-designed clinical studies are lacking. We discuss the available evidence and recent patents supporting the role of doxycycline in atherosclerosis.","PeriodicalId":20905,"journal":{"name":"Recent patents on cardiovascular drug discovery","volume":"6 1","pages":"42-54"},"PeriodicalIF":0.0,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/157489011794578419","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"29577649","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 5

Latest therapeutic novelties and patents in pulmonary hypertension. 肺动脉高压的最新治疗方法和专利。

Recent patents on cardiovascular drug discovery Pub Date : 2011-01-01 DOI: 10.2174/157489011794578491

Georgia F Hardavella, Georgios S Dionellis, Christina G Kantza, Nikolaos G Koulouris, Manos Alchanatis

引用次数: 2

Interactive effect of combined exposure to active and passive smoking on cardiovascular system. 主动和被动吸烟联合暴露对心血管系统的交互作用。

Recent patents on cardiovascular drug discovery Pub Date : 2011-01-01 DOI: 10.2174/157489011794578437

Aurelio Leone

{"title":"Interactive effect of combined exposure to active and passive smoking on cardiovascular system.","authors":"Aurelio Leone","doi":"10.2174/157489011794578437","DOIUrl":"https://doi.org/10.2174/157489011794578437","url":null,"abstract":"A great number of observations show that cardiovascular damage from smoking may be a consequence of both active and passive smoking exposure. Some findings identify an increase in cardiovascular events in active smokers as well as in non-smokers exposed to passive smoking. The type and extension of damage seem to be similar qualitatively either in active smokers or in exposed never smokers. Artery vessels and myocardium feel particularly the effects of smoking. Ischaemic heart disease and atherosclerosis progression are the common alterations observed. Individuals exposed to both active and passive smoking feel the adverse effects of smoking. Result of the interaction consists primarily of increased rate of clinical events whereas the type of anatomical alterations is similar to those which characterize respectively isolated exposure to active or passive smoking. However, the extension of cardiovascular damage may vary even if, usually, in the same location of pre-existing lesions. The article also presents some of the patents regarding the effects of smoking on cardiovascular system.","PeriodicalId":20905,"journal":{"name":"Recent patents on cardiovascular drug discovery","volume":"6 1","pages":"61-9"},"PeriodicalIF":0.0,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/157489011794578437","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"29589106","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 23

Review on bosentan, a dual endothelin receptor antagonist for the treatment of pulmonary arterial hypertension. 双内皮素受体拮抗剂波生坦治疗肺动脉高压的研究进展。

Recent patents on cardiovascular drug discovery Pub Date : 2010-11-01 DOI: 10.2174/157489010793351944

Eva Serasli, Vassilis Michaelidis, Andreas Kosmas, Maria Antoniadou, Venetia Tsara

引用次数: 3

Prevention of left ventricular remodelling after acute myocardial infarction: an update. 急性心肌梗死后左心室重构的预防:最新进展。

Recent patents on cardiovascular drug discovery Pub Date : 2010-11-01 DOI: 10.2174/157489010793351999

Roberta Rossini, Michele Senni, Giuseppe Musumeci, Paolo Ferrazzi, Antonello Gavazzi

{"title":"Prevention of left ventricular remodelling after acute myocardial infarction: an update.","authors":"Roberta Rossini, Michele Senni, Giuseppe Musumeci, Paolo Ferrazzi, Antonello Gavazzi","doi":"10.2174/157489010793351999","DOIUrl":"https://doi.org/10.2174/157489010793351999","url":null,"abstract":"Left ventricular remodelling is a progressive process, which starts immediately after acute myocardial infarction and evolves in the chronic phase of heart failure. It is characterized by left ventricular chamber dilatation and increased wall stress, which results in alteration of the contractile properties of the non-infarct zone and impairment of the systolic and diastolic performances of the left ventricle. Neurohormonal activation and increased sympathetic stimulation are among the factors that have been linked to the development and progression of left ventricular dysfunction after acute myocardial infarction. The present review will address recent insights from new patents and experimental studies of drugs, which ought to prevent left ventricular remodelling. Angiotensin-Converting Enzyme Inhibitors, Angiotensin Receptor Blockers and Beta-Blockers have been proven effective in modulating the process of remodelling and in reducing the occurrence of adverse events. However, in most of the trials high risk patients have been excluded, and uncertainty still exists regarding a number of clinically relevant questions. Data from experimental studies have identified new targets for interventions to prevent reverse left ventricular remodelling, i.e. stem cell transfer, activation of cardiac and leukocyte-dependent oxidant stress pathways, inflammatory pathway activation, matrix-metalloproteinase activation.","PeriodicalId":20905,"journal":{"name":"Recent patents on cardiovascular drug discovery","volume":"5 3","pages":"196-207"},"PeriodicalIF":0.0,"publicationDate":"2010-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/157489010793351999","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"29310044","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 22

Angiogenesis and the heart. 血管生成和心脏。

Recent patents on cardiovascular drug discovery Pub Date : 2010-11-01 DOI: 10.2174/157489010793351953

Shree G Sharma, Sudip Nanda, Santo Longo

引用次数: 0

Challenges and promises of developing thrombin receptor antagonists. 开发凝血酶受体拮抗剂的挑战和前景。

Recent patents on cardiovascular drug discovery Pub Date : 2010-11-01 DOI: 10.2174/157489010793351980

Jing Yang, Ke Xu, Dietmar Seiffert

{"title":"Challenges and promises of developing thrombin receptor antagonists.","authors":"Jing Yang, Ke Xu, Dietmar Seiffert","doi":"10.2174/157489010793351980","DOIUrl":"https://doi.org/10.2174/157489010793351980","url":null,"abstract":"Despite the availability of dual antiplatelet therapy comprised of aspirin and clopidogrel, there is still significant unmet medical need for treating and preventing arterial thrombotic diseases. To achieve further reduction of cardiovascular events without exceeding bleeding tolerability and safety limits, novel antiplatelet strategies might need to trade in antiplatelet efficacy by partial inhibition of an important platelet activation pathway or by differentially targeting pathological versus physiological thrombogenesis pathways. Thrombin, the central enzyme in coagulation and the most potent platelet agonist tested in vitro, is one of the key factors driving the formation of occlusive thrombi. Platelet thrombin receptors, namely protease-activated receptor 1 (PAR-1) and protease-activated receptor 4 (PAR-4), act in concert to elicit robust platelet responses to thrombin. PAR-1 is the high affinity thrombin receptor and represents a novel antithrombotic target. PAR-4 is a low affinity thrombin receptor with less understood function. This review discusses the genetic and pharmacological evidence for PAR-1 target validation and highlights the progresses and challenges in developing oral PAR-1 antagonists, especially SCH 530348 from Merck/Schering-Plough and E-5555 from Eisai Co. Recent patents disclosing several novel chemical series of PAR-1 antagonists from Sanofi-Aventis and Pierre Fabre are also presented.","PeriodicalId":20905,"journal":{"name":"Recent patents on cardiovascular drug discovery","volume":"5 3","pages":"162-70"},"PeriodicalIF":0.0,"publicationDate":"2010-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/157489010793351980","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"29310046","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 8