Recent patents on CNS drug discovery最新文献_第3页

Migraine attack treatment : a tailor-made suit, not one size fits all. 偏头痛的治疗:量身定做的西装，不是一刀切的。

Recent patents on CNS drug discovery Pub Date : 2014-04-01 DOI: 10.2174/1574889809666140307115100

Robert Belvis, Natalia Mas, Azahara Aceituno

{"title":"Migraine attack treatment : a tailor-made suit, not one size fits all.","authors":"Robert Belvis, Natalia Mas, Azahara Aceituno","doi":"10.2174/1574889809666140307115100","DOIUrl":"https://doi.org/10.2174/1574889809666140307115100","url":null,"abstract":"About 15% of people in the world suffer migraine attacks. Migraine can induce a great impact in the quality of life, and the costs of medical care and loss of productivity can be also high. Non-steroidal anti-inflammatory drugs (NSAIDs) are the best treatment in mild-to-moderate migraine attacks and triptans are the first line option in the acute treatment of moderate-to-severe migraine attacks. At present, there are seven marketed triptans: sumatriptan, rizatriptan, zolmitriptan, eletriptan, naratriptan, almotriptan and frovatriptan. Obviously, every drug presents different pharmacokinetic and pharmacodynamics properties and, moreover, some triptans have several formulations. The prescription of one of these seven triptans for a specified patient is based in the drug profile: efficacy, safety, pharmacokinetics and pharmacodynamics. Other data to take account in the final prescription are clinical characteristics of the migraine attack (speed of onset, intensity of pain, lasting of the attack) and patient characteristics as working habits, life style or medical history. It is therefore mandatory to perform an individualization of the treatment of migraine attack. In recent years, several new patents of drugs have been registered in the treatment of migraine attack, although most of these are already known drugs that only provide new routes of administration. We present an update on the treatment of the migraine attack. ","PeriodicalId":87737,"journal":{"name":"Recent patents on CNS drug discovery","volume":" ","pages":"26-40"},"PeriodicalIF":0.0,"publicationDate":"2014-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1574889809666140307115100","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40291123","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

Treatment of insulin resistance in the neurodegeneration. 神经退行性疾病胰岛素抵抗的治疗。

Recent patents on CNS drug discovery Pub Date : 2014-04-01 DOI: 10.2174/1574889809666140410093006

Manuela Stefanelli, Antonio Martocchia, Elisabetta Adele De Marinis, Giulia Maria Falaschi, Gloria Romano, Maddalena Rufo, Paolo Falaschi

{"title":"Treatment of insulin resistance in the neurodegeneration.","authors":"Manuela Stefanelli, Antonio Martocchia, Elisabetta Adele De Marinis, Giulia Maria Falaschi, Gloria Romano, Maddalena Rufo, Paolo Falaschi","doi":"10.2174/1574889809666140410093006","DOIUrl":"https://doi.org/10.2174/1574889809666140410093006","url":null,"abstract":"The association between diabetes and neurodegenerative diseases is increasing with aging. Several common mechanisms are involved in both these diseases. The endothelial cells of the blood brain barrier, neurons and glia express typical and different receptors of the glucose metabolism (glucose transporters, insulin receptors and glucagon-like peptide-1 receptors). The impairment in insulin signaling leads to an impairment of neuronal function and increases neurodegeneration, and, conversely, neurodegeneration causes a reduction of insulin signaling on neurons. Increased detailed knowledge of common physiological processes opens up the opportunities for developing new treatments that may prevent or reduce the onset of neurodegenerative diseases. The aim of the review is to discuss the potential neuroprotective effects of the antidiabetic drugs. The article presents some promising patents on the treatment of insulin resistance in the neurodegeneration.","PeriodicalId":87737,"journal":{"name":"Recent patents on CNS drug discovery","volume":"9 1","pages":"54-63"},"PeriodicalIF":0.0,"publicationDate":"2014-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1574889809666140410093006","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"32255661","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: 4

Recent advances in the treatment of neurogenic erectile dysfunction. 神经源性勃起功能障碍的治疗进展。

Recent patents on CNS drug discovery Pub Date : 2014-04-01 DOI: 10.2174/2212798406666140131122641

Rocco S Calabro, Giovanni Polimeni, Placido Bramanti

引用次数: 12

This first 2014 issue of Recent Patents in CNS Drug Discovery covers a range of rather diverse, but not necessarily unrelated topics. Introduction. 这是2014年第一期《中枢神经系统药物发现最新专利》，涵盖了一系列相当多样化但不一定不相关的主题。介绍。

Recent patents on CNS drug discovery Pub Date : 2014-04-01 DOI: 10.2174/157488980901140428100532

Vincenzo Di Marzo

引用次数: 17

Pathophysiology and treatment of nonfamilial hyperparathyroidism. 非家族性甲状旁腺功能亢进的病理生理及治疗。

Recent patents on CNS drug discovery Pub Date : 2014-01-01 DOI: 10.2174/1574889810666150131141054

Franco Lumachi, Stefano M M Basso

{"title":"Pathophysiology and treatment of nonfamilial hyperparathyroidism.","authors":"Franco Lumachi, Stefano M M Basso","doi":"10.2174/1574889810666150131141054","DOIUrl":"https://doi.org/10.2174/1574889810666150131141054","url":null,"abstract":"Primary hyperparathyroidism (HPT) is the main cause of hypercalcemia and the most common parathyroid glands disease. The diagnosis is easy in patients with hypercalcemia and elevated PTH serum level. Minimally invasive parathyroidectomy (PTx) represents the treatment of choice for symptomatic patients, leading to several advantages, including immediate normalization of hypercalcemia and significant improvement of bone mineral density, cardiovascular dysfunctions, neuropsychological symptoms and quality of life. Secondary and tertiary HPT are relatively common complications in patients with chronic kidney disease (CKD) or advanced kidney failure, and in kidney transplant recipients who did not achieve complete calcium/phosphate metabolism normalization, respectively. The drugs available for patients with secondary HPT, and to treat hyperphosphatemia include non-calcium-containing phosphate binder, calcitriol analogues, calcimimetic agents, or a combination of two or more drugs. Although recent studies report that PTx significantly improves survival also in patients with CKD and severe secondary HPT, the indications for surgery are not yet well established. Subtotal or total PTx with or without autotransplantation are the surgical options for treating all patients with secondary HPT. Total PTx leads to a faster reduction in serum calcium level and normalization of PTH, but the risk of hypoparathyroidism is higher than after subtotal PTx. Further studies are needed to confirm the usefulness of the drugs currently recommended, and others will have to be tested in the near future. ","PeriodicalId":87737,"journal":{"name":"Recent patents on CNS drug discovery","volume":"9 3","pages":"164-72"},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33022138","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

Pharmacological approaches to targeting muscarinic acetylcholine receptors. 靶向毒蕈碱乙酰胆碱受体的药理学方法。

Recent patents on CNS drug discovery Pub Date : 2014-01-01 DOI: 10.2174/1574889809666141120131238

Carlo Matera, Ada M Tata

{"title":"Pharmacological approaches to targeting muscarinic acetylcholine receptors.","authors":"Carlo Matera, Ada M Tata","doi":"10.2174/1574889809666141120131238","DOIUrl":"https://doi.org/10.2174/1574889809666141120131238","url":null,"abstract":"The presence of cholinergic system markers and muscarinic receptor subtypes in several tissues also of nonneuronal type has been largely demonstrated. Acetylcholine, synthesized in the nervous system, can locally contribute to modulate cell proliferation, survival and apoptosis. Considering that the cholinergic system functions are impaired in a number of disorders, the identification of new drugs regulating these functions appears of great clinical relevance. The possible involvement of muscarinic acetylcholine receptors in different pathologies has been proposed in recent years and is becoming an important area of study. However, the lack of selective muscarinic receptor ligands has for long time limited the therapeutic treatment based on muscarinic receptors as targets. To date, some muscarinic ligands such as xanomeline (patent, US5980933) or cevimeline (patents US4855290, US5571918) have been developed for the treatment of several pathologies (Alzheimer's and Sjogren's diseases). The present review will be focused on the potential effects produced by muscarinic receptor activation in different pathologies, including tumors. In fact, the potential use of muscarinic ligands in therapeutic protocols in cancer therapy will be discussed, considering that several muscarinic antagonists, already used in the treatment of genitourinary diseases (e.g. darifenacin, patent, US5096890, US6106864), have also been demonstrated to arrest the tumor growth in vivo. Moreover, the contribution of muscarinic receptors to analgesia is also reviewed. Finally, some of the most significant achievements in the field of bitopic/dualsteric ligands will be discussed and the molecules patented so far will be presented. ","PeriodicalId":87737,"journal":{"name":"Recent patents on CNS drug discovery","volume":"9 2","pages":"85-100"},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"32827546","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: 30

Treatment of chronic migraine with intramuscular pericranial injections of onabotulinumtoxin a. 肌周注射肉毒杆菌毒素a治疗慢性偏头痛。

Recent patents on CNS drug discovery Pub Date : 2014-01-01 DOI: 10.2174/1574889810666150131124603

Robert Belvis, Natalia Mas

引用次数: 5

Possible physiopathological roles of the transglutaminase activity in the etiopathogenesis of human neurodegenerative diseases. 转谷氨酰胺酶活性在人类神经退行性疾病发病机制中的可能的生理病理作用。

Recent patents on CNS drug discovery Pub Date : 2014-01-01 DOI: 10.2174/1574889809666140613114850

Federica Titta, Martina Iannaccone, Antonio Martin, Vittorio Gentile

{"title":"Possible physiopathological roles of the transglutaminase activity in the etiopathogenesis of human neurodegenerative diseases.","authors":"Federica Titta, Martina Iannaccone, Antonio Martin, Vittorio Gentile","doi":"10.2174/1574889809666140613114850","DOIUrl":"https://doi.org/10.2174/1574889809666140613114850","url":null,"abstract":"Transglutaminases are ubiquitous enzymes which catalyze post-translational modifications of proteins. The main activity of these enzymes is the cross-linking of glutaminyl residues of a protein/peptide substrate to lysyl residues of a protein/peptide co-substrate. In addition to lysyl residues, other second nucleophilic co-substrates may include monoamines or polyamines (to form mono- or bi-substituted /crosslinked adducts) or -OH groups (to form ester linkages). In the absence of co-substrates, the nucleophile may be water, resulting in the net deamidation of the glutaminyl residue. Transglutaminase activity has been suggested to be involved in molecular mechanisms responsible for both physiological or pathological processes. For example, neurodegenerative diseases, such as Alzheimer's Disease, Parkinson's Disease, supranuclear palsy, Huntington's Disease and other polyglutamine diseases, are characterized in part by aberrant cerebral transglutaminase activity and by increased cross-linked proteins in affected brains. This review focuses on the possible molecular mechanisms responsible for such diseases and on the possible therapeutic effects of transglutaminase inhibitors for patients with diseases characterized by aberrant transglutaminase activity. ","PeriodicalId":87737,"journal":{"name":"Recent patents on CNS drug discovery","volume":"9 2","pages":"101-9"},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"32418754","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: 2

Patents on potential drugs to treat Alzheimer's disease: special emphasis on small peptides. 治疗阿尔茨海默病的潜在药物专利:特别强调小肽。

Recent patents on CNS drug discovery Pub Date : 2014-01-01 DOI: 10.2174/1574889809666140919123006

Pazhani Sundaram, Aravind K Nambiar, Ranjini K Sundaram

引用次数: 1

Advancing drug therapy for brain tumours: a current review of the pro-inflammatory peptide Substance P and its antagonists as anti-cancer agents. 推进脑肿瘤的药物治疗:促炎肽P物质及其拮抗剂作为抗癌药物的最新进展。

Recent patents on CNS drug discovery Pub Date : 2014-01-01 DOI: 10.2174/1574889809666141111142740

Kimberley Mander, Elizabeth Harford-Wright, Kate M Lewis, Robert Vink

{"title":"Advancing drug therapy for brain tumours: a current review of the pro-inflammatory peptide Substance P and its antagonists as anti-cancer agents.","authors":"Kimberley Mander, Elizabeth Harford-Wright, Kate M Lewis, Robert Vink","doi":"10.2174/1574889809666141111142740","DOIUrl":"https://doi.org/10.2174/1574889809666141111142740","url":null,"abstract":"Evidence for the involvement of the Substance P (SP)/NK1 receptor system in the development and progression of cancer strongly supports its potential as a therapeutic target in malignancies. Novel strategies for approaching cancer treatment are urgently required particularly with regard to tumours of the central nervous system (CNS), which are notoriously difficult to effectively treat and associated with extremely poor prognosis for many patients. This is due, in part, to the presence of the highly specialised blood-brain barrier, which is known to restrict common treatments such as chemotherapy and hinder early tumour diagnosis. Additionally, tumours of the CNS are difficult to surgically resect completely, often contributing to the resurgence of the disease many years later. Interestingly, despite the presence of the blood-brain barrier, circulating tumour cells are able to gain entry to the brain and form secondary brain tumours; however, the underlying mechanisms of this process remain unclear. Tachykinins, in particular Substance P, have been implicated in early blood-brain barrier disruption via neurogenic inflammation in a number of other CNS pathologies. Recent evidence also suggests that Substance P may play a central role in the development of CNS tumours. It has been well established that a number of tumour cells express Substance P, NK1 receptors and mRNA for the tachykinin NK1 receptor. This increase in the Substance P/NK1 receptor system is known to induce proliferation and migration of tumour cells as well as stimulate angiogenesis, thus contributing to tumour progression. Accordingly, the NK1 receptor antagonist presents a novel target for anti-cancer therapy for which a number of patents have been filed. This review will examine the role of Substance P in the development of CNS tumours and its potential application as an anti-cancer agent. ","PeriodicalId":87737,"journal":{"name":"Recent patents on CNS drug discovery","volume":"9 2","pages":"110-21"},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"32806514","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: 4