Expert opinion on therapeutic patents
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Expert Opin Ther Pat · May 2012
ReviewSelective cannabinoid receptor 2 modulators: a patent review 2009--present.
The activation of the cannabinoid receptor 2 (CB2) affects a myriad of immune responses from inflammation to neuroprotection, demonstrates analgesic effects and suppresses responses in many animal models of pain. Questions around the involvement of CB1 activation in these effects remain, but efforts have been directed toward the discovery of highly selective CB2 modulators lacking the psychotropic effects of cannabinoids, which are mediated by the CB1 receptor. ⋯ There is a continuous interest in the CB2 receptor as a drug target. Many highly selective compounds of various chemotypes have been identified and their analgesic effects in animal models further support the potential of this mechanism in pain therapy. Several companies have initiated clinical trials. While some of these have been terminated for various reasons, one can anticipate the emergence of new drugs from CB2 modulation once a better understanding around the cannabinoid receptors is gained.
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Expert Opin Ther Pat · Sep 2010
Transplantation of two populations of stem cells to improve engraftment: WO2008060932.
The application is in the field of haematopoietic stem cells (HSCs) and cellular therapy. ⋯ The application claims the transplantation of at least two populations of HSCs, separated by an interval of time between 2 and 24 h, to improve the outcome of HSC transplantation for the treatment of haematologic diseases. The procedure may be extended to other types of stem cells for treating a broad range of diseases and injuries.
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Expert Opin Ther Pat · Sep 2010
ReviewTransient receptor potential vanilloid-1 antagonists: a survey of recent patent literature.
Transient receptor potential vanilloid-1 (TRPV1, vanilloid receptor-1) is a nonspecific cation channel that can be activated by multiple endogenous stimuli and by capsaicin, the active ingredient in chili peppers. TRPV1 is expressed predominantly on sensory neurons where it is proposed to serve as a key nodal point in pain transmission pathways. Pharmacological blockade of TRPV1 represents a compelling strategy for the treatment of a variety of disease states, particularly those requiring chronic pain management. AREA COVERED IN THE REVIEW: This review summarizes patent literature and progress in defining the utility of small molecule TRPV1 antagonists during 2008-2009. ⋯ The continued profusion of reports, in both the primary and patent literature, attests to the sustained interest in the TRPV1 class of therapeutics. Although a number of compounds have now been brought forward for human clinical trials, the therapeutic utility of TRPV1 antagonists is yet to be validated unequivocally.
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Expert Opin Ther Pat · Sep 2010
Ex vivo fucosylation of stem cells to improve engraftment: WO2004094619.
The application is in the field of haematopoietic stem cell (HSC) and umbilical cord blood (CB) transplantation. ⋯ Treatment of CB stem cells with FTVI, ex vivo prior to transplantation, may reduce the delay of engraftment of CB stem cells to the BM and the risk of early infections associated with CB transplants, particularly in adults. It may improve the outcome and rate of success of CB transplantation. The application claims the use of fucosyltransferase for improving the engraftment of CB HSCs to the BM for the treatment of haematologic diseases. The procedure may be used to improve the engraftment of HSCs from other sources and other types of stem cells, on transplantation, particularly when administered intravenously.
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The voltage-gated sodium channels (VGSCs) play a fundamental role in controlling cellular excitability and their abnormal activity is related to several pathological processes, including cardiac arrhythmias, epilepsy, neurodegenerative diseases, spasticity, chronic and neuropathic pain. In particular, neuropathic pain (e.g., postherpetic and trigeminal neuralgia, diabetic neuropathy and spinal cord injury) is a serious clinical problem that affects a high percentage of the world population. Because an altered sodium channel isoform expression profile has been considered one reason for the changes in neuronal excitability, there is a continuous quest for new selective molecules targeting sodium channels for the treatment of chronic pain. ⋯ The continuous discoveries in the field of sodium channel blockers, highlighted by the increasing numbers of patent applications published in the last few years and by the numbers of compounds currently in clinical development, underline the importance of this target for the treatment of neuropathic pain. The great difficulty in the design of new selective and active structures, not obtained from old VGSC blockers that are often associated with high risk of adverse effects, is a strong challenge for medicinal chemistry research.