Journal•ISSN: 1354-3776
Expert Opinion on Therapeutic Patents
Informa
About: Expert Opinion on Therapeutic Patents is an academic journal published by Informa. The journal publishes majorly in the area(s): Cancer & Receptor. It has an ISSN identifier of 1354-3776. Over the lifetime, 2537 publications have been published receiving 60440 citations.
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TL;DR: Sulphonamide CA inhibitors (CAIs) are useful as diuretics, or in the treatment and prevention of a variety of diseases such as glaucoma, epilepsy, congestive heart failure, mountain sickness, gastric and duodenal ulcers, neurological disorders and osteoporosis among others, as well as diagnostic tools.
Abstract: Carbonic anhydrases (CAs, EC 4.2.1.1) are wide-spread zinc enzymes, present in archaeo- and eubacteria, algae, green plants and animals. Within these organisms CAs are encoded by three distinct, ev...
483 citations
TL;DR: It appears that prodrugs to overcome barriers to the delivery of problematic drug candidates are becoming an integral part of the drug discovery paradigm.
Abstract: Prodrugs are bioreversible derivatives of drug molecules used to overcome some barriers to the utility of the parent drug molecule. These barriers include, but are not limited to, solubility, permeability, stability, presystemic metabolism and targeting limitations. The patent literature shows a dramatic increase in numbers of prodrug patents (> 2000% increase in 2002 compared to 1993), with claims for cancer treatment comprising 37% of these. This increase is largely due to the rise from North American-based multinationals and some smaller drug delivery companies mirroring the overall trend. In 2001 and 2002, 14% of all new approved chemical drugs were prodrugs. It appears that prodrugs to overcome barriers to the delivery of problematic drug candidates are becoming an integral part of the drug discovery paradigm.
303 citations
TL;DR: There is an urgent need for new antiglaucoma CAIs/approaches to treat and diagnose this disease in the very near future, as the last drug which has been discovered in the field dates back > 10 years ago.
Abstract: Introduction: Glaucoma is one of the major causes of blindness, affecting together with age-related macular degeneration > 70 million people worldwide. One of the therapeutic options for its management is based on the inhibition of the metalloenyme carbonic anhydrase (CA, EC 4.2.1.1). CA inhibitors (CAIs) diminish intraocular pressure (IOP) by reducing the rate of bicarbonate formation and thus secretion of the aqueous humor. Areas covered: The main classes of clinically used antiglaucoma CAIs are the sulfonamides with systemic (acetazolamide, methazolamide, ethoxzolamide and dichlorophenamide) and topical (dorzolamide and brinzolamide) action. A patent literature review covering the period 2007 – 2013 is presented. Expert opinion: This review presents an overview of the patent literature in the CAI antiglaucoma drug design field during the past 6 years. Most of the patents deal with sulfonamide/sulfamide/sulfamate CAIs, sulfonamides incorporating NO-donating moieties, as well as hybrids incorporating sul...
262 citations
TL;DR: In this article, a review summarises patents published from 2001 to 2004 on the microcidal properties of silver-releasing materials for healthcare and medicine, including the anti-inflammatory, re-epitheliasation and anti-haemorrhagic properties of the materials.
Abstract: This review summarises patents published from 2001 to 2004 on the microcidal properties of silver-releasing materials for healthcare and medicine. The anti-inflammatory, re-epitheliasation and antihaemorrhagic properties of the silver-releasing materials are also disclosed. A biological evaluation of the anti-viral properties of silver tetra-silver tetra-oxide is discussed, but no biological data have been reported to support the claim that silver (I) has anti--viral prop-erties, as disclosed by most of the patents.
255 citations
TL;DR: These effects seem to be due to the potent inhibition of such drugs against CA isoforms present in kidneys and blood vessels, which explain both the blood pressure lowering effects as well as organ-protective activity of the drugs.
Abstract: Introduction The benzothiadiazines and high ceiling diuretics (hydrochlorothiazide, hydroflumethiazide, quinethazone, metolazone, chlorthalidone, indapamide, furosemide and bumetanide) contain primary sulfamoyl moieties acting as zinc-binding groups in the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1). These drugs are widely used clinically and were recently shown to weakly inhibit isoforms CA I and II, but to possess stronger activity against isoforms involved in other important pathologies, for example, obesity, cancer, epilepsy and hypertension. Areas covered The class of clinically used diuretics, with CA inhibitory properties, is the main topic of the review. A patent literature review covering the period from 2005 to 2013 is presented. Expert opinion This section presents an overview of the patent literature in the sulfonamide diuretic field. Most of the patents deal with the combination of diuretic sulfonamide CA inhibitors with other agents useful in the management of cardiovascular diseases and obesity. Such combinations exert a better therapeutic activity compared to similar diuretics that do not inhibit CAs, raising the question of the polypharmacological and drug repositioning effects of these old drugs. These effects seem to be due to the potent inhibition of such drugs against CA isoforms present in kidneys and blood vessels, which explain both the blood pressure lowering effects as well as organ-protective activity of the drugs. An explanation of these data is provided by the fact that inhibition of the renal CAs leads to a large increase of the nitrite excretion in urine, suggesting that renal CAs are involved in nitrite reabsorption in humans. Important lessons for the drug design of sulfonamide CA inhibitors (CAIs) can be drawn from these data.
250 citations