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Recent Patents on CNS Drug Discovery

Maurizio Bifulco, Chiara Laezza, Anna Maria Malfitano
BACKGROUND: Several studies support the evidence that the endocannabinoid system and cannabimimetic drugs might have therapeutic potential in numerous pathologies. These pathologies range from neurological disorders, atherosclerosis, stroke, cancer to obesity/metabolic syndrome and others. METHODS: In this paper we review the endocannabinoid system signaling and its alteration in neurodegenerative disorders like multiple sclerosis, Alzheimer's disease, Parkinson's disease and Huntington's disease and discuss the main findings about the use of cannabinoids in the therapy of these pathologies...
June 27, 2016: Recent Patents on CNS Drug Discovery
Roberta Ranieri, Daniela Marasco, Maurizio Bifulco, Anna Maria Malfitano
Agents acting via cannabinoid receptors have been widely developed; starting from the chemical structure of phytocannabinoids isolated from cannabis sativa plant, specific and selective compounds of these receptors have been produced ranging from partial to full agonists and /or antagonists endowed with different potency. The enhanced interest on developing such classes of drugs is due to the beneficial properties widely reported by both anecdotal reports and scientific studies describing the potential medicinal use of cannabinoids and their derivatives in numerous pathological conditions in both in vitro and in vivo models...
June 19, 2016: Recent Patents on CNS Drug Discovery
Roberta Ranieri, Daniela Marasco, Chiara Laezza, Maurizio Bifulco, Anna Maria Malfitano
Cannabinoid receptors are involved in neurophatogenic mechanisms of inflammatory disorders of the central nervous system and their expression can be modulated during the disease. Brain inflammatory processes are characterized by infiltration of numerous types of cells, peripheral immune cells, brain resident immune cells, the microglial cells and numerous other neuronal cells. The disruption of the blood brain barrier favours cell infiltration in the central nervous system with consequent neuronal damage, common event in many neuro-inflammatory diseases...
June 19, 2016: Recent Patents on CNS Drug Discovery
Sarat C Yenesetti, M J Manjunath, Cftri Muralidhara
BACKGROUND Owing to the increasing aged population globally, disorders and diseases of the CNS are anticipated to increase and heavily impact the health care. As these neurodegenerative diseases (NDD) are complex, multifactorial and do not have identified etiological factors, unfortunately drugs developed for the purpose have not met with the expected success. Hence, there has been a constant demand for development of natural therapeutic adjuvants which are safe and possess the potential to attenuate multiple pathways...
June 14, 2016: Recent Patents on CNS Drug Discovery
Andrea Chicca, Chiara Arena, Clementina Manera
BACKGROUND: Anandamide (AEA) and 2-arachidonoyl glycerol (2-AG) are signalling lipids which belong to the class of endocannabinoids (ECs) and exert their actions by activating cannabinoid receptor type-1 (CB1) and type-2 (CB2). These receptors are involved in many physiological and pathological processes in the central nervous system (CNS) and in peripheral organs. Despite many potent and selective ligands for cannabinoid receptors have been generated over the last two decades, this class of compounds achieved only a very limited therapeutic success, mainly because of the CB1-mediated side effects...
June 3, 2016: Recent Patents on CNS Drug Discovery
Clementina Manera, Chiara Arena, Andrea Chicca
BACKGROUND: Since the discovery of the cannabinoid receptors, numerous studies associate the endocannabinoid system with several physiological and pathological processes including cancer, appetite, fertility, memory, neuropathic and inflammatory pain, obesity, and neurodegenerative diseases. Over the last two decades, several researches have been dedicated extensively on the cannabinoid receptors ligands since the direct activation of cannabinoid receptors results in several beneficial effects, in the brain and in the periphery...
May 19, 2016: Recent Patents on CNS Drug Discovery
Roberta Ranieri, Daniela Marasco, Maurizio Bifulco, Anna Maria Malfitano
BACKGROUND: Starting from the chemical structure of phytocannabinoids, isolated from Cannabis sativa plant, research groups designed numerous cannabimimetic drugs. These compounds according to their activities can be partial, full agonists and antagonists of cannabinoid receptors. Anecdotal reports and scientific studies described beneficial properties of cannabinoids and their derivatives in several pathological conditions like neurological and neuropsychiatric disorders, and in many other diseases ranging from cancer, atherosclerosis, stroke, hypertension, inflammatory related disorders, and autoimmune diseases...
May 17, 2016: Recent Patents on CNS Drug Discovery
Anna Russo, Sara La Manna, Giancarlo Morelli, Ettore Novellino, Daniela Marasco
BACKGROUND Peptides are usually used to investigate regulatory networks and protein function. They can also be used in therapeutic research: they are employed both to identify and later to validate therapeutical target and in drug discovery processes. Their development enables the identification of several protein surfaces as crucial therapeutic targets and to promote the discovery of small drugs specific for these molecular interfaces. METHODS This review was developed through the research of online content related to natural and de novo designed peptides in neurological diseases studies...
April 25, 2016: Recent Patents on CNS Drug Discovery
Anna Maria Malfitano, Chiara Laezza, Simona Pisanti, Clementina Manera, Maurizio Bifulco
BACKGROUND: We have recently released the structure of a class of quinolin-2-(1H)-on-3-carboxamide derivatives and among them; the drug A2 has the highest CB2 receptor affinity and selectivity. OBJECTIVE: In this work we assessed the immuno-modulatory properties of A2 in lymphocytes isolated from peripheral blood of multiple sclerosis patients and healthy donors. METHODS: Cell proliferative response was measured by 3H-thymidine incorporation, cell viability and apoptosis by trypan blue, annexin V staining and western blot...
April 21, 2016: Recent Patents on CNS Drug Discovery
Miao-Kun Sun
No abstract text is available yet for this article.
2015: Recent Patents on CNS Drug Discovery
Lorena Urbanelli, Sandra Buratta, Krizia Sagini, Giuseppina Ferrara, Marco Lanni, Carla Emiliani
Exosomes are small extracellular vesicles (30-120 nm) of endosomal origin, which are gaining the attention of the scientific community. Originally considered only a waste disposal system, they are now emerging as another class of signal mediators. Exosomes are secreted by any cell type and retrieved in every body fluid, such as blood, urine, saliva and amniotic liquid. Remarkably, their biochemical content includes not only lipids and proteins, but also nucleic acids, mainly miRNA and mRNA, with a few reports also indicating the presence of genomic and mitochondrial DNA...
2015: Recent Patents on CNS Drug Discovery
Leonard L L Yeo, Benjamin Y Q Tan, Wan Yee, Amit Kulkarni, Vijay K Sharma
Acute Ischemic stroke (IS) remains a leading cause of mortality and long-term disability. Owing to the time-constraints, only a fraction of acute IS patients receive the established and approved thrombolytic therapy and a sizeable proportion of acute IS stroke survivors remain permanently disabled. Rapid advances in various recanalization strategies have aimed at improving functional outcome and reducing mortality. Existing literature on various treatment approaches, including the evolution of various thrombolytic agents and interventional devices is presented in this review...
2015: Recent Patents on CNS Drug Discovery
Stephen H Curry, Anne M Schneiderman
Pharmaceutical patenting involves writing claims based on both discoveries already made, and on prophesy of future developments in an ongoing project. This is necessitated by the very different timelines involved in the drug discovery and product development process on the one hand, and successful patenting on the other. If patents are sought too early there is a risk that patent examiners will disallow claims because of lack of enablement. If patenting is delayed, claims are at risk of being denied on the basis of existence of prior art, because the body of relevant known science will have developed significantly while the project was being pursued...
2015: Recent Patents on CNS Drug Discovery
Jens Hagenow, Holger Stark
Tinnitus, a disorder with disruptive sound perception in the head without an external source, affects around 15 % of the worldwide adult population. Since there is no approved drug for the treatment for this symptom, novel strategies need to be developed to provide relief for the patient. A patent from the small French start-up company Sensorion suggests the use of histamine H4 receptor (H4R) inhibitors as potential treatment. Since histamine and its receptor subtypes are strongly involved in neuronal and inflammatory processes in vestibular areas, targeting the H4R could be a novel way to gain a treatment for tinnitus...
2015: Recent Patents on CNS Drug Discovery
Luis F Alguacil, Gonzalo Herradón
Pleiotrophin (PTN) and Midkine (MK) are neurotrophines with documented protective actions in experimental models of neurodegenerative diseases and beneficial effects on toxicity and addictive behaviours related to drug abuse. Concerning the latter, both PTN and MK prevent the neurotoxic effects of amphetamine on nigrostriatal pathways and endogenous PTN also limits amphetamine reward. Moreover, endogenous PTN overexpression in the prefontral cortex abolishes alcohol- induced conditioned place preference. This review summarizes the existing patents for using PTN and MK in the treatment and diagnosis of neuropsychiatric disorders with a focus on neurotoxicity, neurodegeneration and substance use disorders...
2015: Recent Patents on CNS Drug Discovery
Antonio Martocchia, Martina Curto, Fabrizia Comite, Sergio Scaccianoce, Paolo Girardi, Stefano Ferracuti, Ferdinando Nicoletti, Paolo Falaschi
Osteoporotic hip fracture needs a specific approach and treatment, since elderly patients are at high risk for adverse outcomes after surgery. In particular, delirium often occurs in the peri-operative period, and it is associated with death, hospital-acquired complications, persistent cognitive impairments, poor functional recovery after surgery and increased healthcare costs. The pre-operative assessment of the risk factors for delirium improves the preventive measures. The delirium diagnostic tools should be included in the standard of orthogeriatric cure for hip fracture...
2015: Recent Patents on CNS Drug Discovery
Vincenzo Di Marzo
No abstract text is available yet for this article.
April 2014: Recent Patents on CNS Drug Discovery
Manuela Stefanelli, Antonio Martocchia, Elisabetta Adele De Marinis, Giulia Maria Falaschi, Gloria Romano, Maddalena Rufo, Paolo Falaschi
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...
April 2014: Recent Patents on CNS Drug Discovery
Gerardo Caruso, Maria Caffo
Gliomas are the most common and malignant primary brain tumors in the adult population. Despite the intensive research on cancer pathology, real mechanisms concerning glioma progression are not completely understood. The prognosis in patients affected by malignant gliomas is still very unfavorable. Recent genomic analyses have revealed patterns of molecular changes within tumor subclasses that harbor distinct underlying biology, clinical prognosis, and pathogenic routes. So, novel treatments will have to be able to interfere at different molecular levels in gliomagenesis minimizing the toxicity...
April 2014: Recent Patents on CNS Drug Discovery
Robert Belvis, Natalia Mas, Azahara Aceituno
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...
April 2014: Recent Patents on CNS Drug Discovery
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