Expert opinion on therapeutic patents
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Selectins play a significant and well-documented role in inflammation and immune response. They initiate tethering and rolling of blood borne leukocytes leading to their activation, adhesion and subsequent extravazation into tissues. This is important for healthy immune response and tissue repair. However, dysregulation of selectins leads to exacerbation of disease. Atherosclerosis, restenosis, deep venous thrombosis and tumor metastasis are just a few of the diseases in which selectin blockade has been demonstrated to ameliorate disease pathology. Thus, selectins remain attractive targets for amelioration of disease. ⋯ The field of selectin inhibition has matured significantly in recent years in the ability to inhibit selectin/ligand interactions with drug-like molecules and to demonstrate disease modification in human trials.
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Expert Opin Ther Pat · May 2010
Patent reform in the US: what's at stake for pharmaceutical innovation?
The current patent landscape in the US has not undergone major legislative reform since 1952. The US Senate version of the most recently proposed patent reform legislation puts forward a number of rule changes that could impact the pharmaceutical industry. ⋯ Various industries with a stake in patent reform have responded to the proposed changes. The need for balanced reform makes the stakes particularly high for the pharmaceutical industry which must invest a significant amount of time and money in the research and development process in exchange for already abbreviated patent lifetimes due to the lengthy clinical trial process.
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Expert Opin Ther Pat · Feb 2010
ReviewThyromimetics: a review of recent reports and patents (2004 - 2009).
Thyroid hormones are produced by the thyroid gland and peripheral tissues, and control metabolic rate, including oxygen consumption, lipid metabolism and the cardiovascular system, mainly through binding to and activating thyroid hormone receptors (TRs). Abnormal elevation or lowering of circulating thyroid hormone induces various physiological disorders. As candidates for the treatment of such diseases, various thyromimetics, such as subtype- or tissue-selective TR agonists and antagonists, have been developed. ⋯ Some thyromimetics are subtype- or tissue-selective TR agonists and antagonists, and such compounds have the potential to become novel therapeutic agents, especially in the field of metabolic diseases.
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Sirtuin 1-7 (SIRT1-7) are deacetylases that are dependent on NAD(+) for their activity. SIRT1 down-regulates p53 activity, increasing lifespan, cell survival, and neuroprotection; it also deacetylates peroxisome proliferator-activated receptor-gamma and its coactivator 1alpha, promoting fat mobilization, increasing mitochondrial size and number, and positively regulating insulin secretion. Sirtuins link nutrient availability and energy metabolism. Calorie restriction, which increases lifespan and is beneficial in age-related disorders, activates sirtuin. Major efforts are thus focused to developing sirtuin activators. ⋯ To date, resveratrol is the most potent natural compound able to activate SIRT1, mimicking the positive effect of calorie restriction. Resveratrol might help in the treatment or prevention of obesity and in preventing the aging-related decline in heart function and neuronal loss. As resveratrol has low bioavailability and interacts with multiple molecular targets, the development of new molecules with better bioavailability and targeting sirtuin at lower concentrations is a promising field of the medicinal chemistry. New SIRT1 activators that are up to 1000 times more effective than resveratrol have recently been identified. These improve the response to insulin and increase the number and activity of mitochondria in obese mice. Human trials with a formulation of resveratrol with improved bioavailability and with a synthetic SIRT1 activator are in progress.
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Expert Opin Ther Pat · Feb 2009
ReviewCheckpoint kinase inhibitors: a review of the patent literature.
The checkpoint kinases, Chk1 and Chk2 are Ser/Thr protein kinases, which function as key regulatory kinases in cellular DNA damage response pathways limiting cell-cycle progression in the presence of DNA damage. The development of checkpoint kinase inhibitors for the treatment of cancer has been a major objective in drug discovery over the past decade, as evidenced by three checkpoint kinase inhibitors entering clinic trials since late 2005. ⋯ A large number of chemically diverse Chk1 and Chk2 kinase inhibitors have appeared in the recent patent literature. Common structural motifs of the checkpoint kinase inhibitors were identified. There are currently three checkpoint kinase inhibitors in clinical development, a continuing effort by the pharmaceutical industry to identify novel scaffolds for checkpoint kinase inhibition.