Novel thiazole derivatives: a patent review (2008 – 2012; Part 1)

Introduction: Thiazole is a well-known five-membered heterocyclic compound. Various methods have been worked out for its synthesis. In the last few decades, a lot of work has been done on thiazole ring in order to find new compounds related to this scaffold acting as an antioxidant, analgesic, anti-inflammatory, antimicrobial, antifungal, antiviral, diuretic, anticonvulsant, neuroprotective and antitumor or cytotoxic drugs with lesser side effects. This review presents the up to date development of different thiazole derivatives. Areas covered: This review gives an account of the recent therapeutic patent literature (2008 - 2012) describing the applications of thiazole and its derivatives on selected activities. In this review, many of the therapeutic applications of thiazole derivatives reported in international patents have been discussed. In addition to selected biological data, some of pharmaceutical applications are also summarized. Because of the large number of patents registered in this period relative to thiazole derivatives the attention was focused, in this first part of the review, on inhibitors of phosphatidylinositol-3-kinase, inhibitors of protein kinase and derivatives modulating enzymes related to metabolism. Expert opinion: This review of patented products presents the thiazole ring as the nucleus of the derivatives considered from a medicinal chemistry perspective. The applications are based firstly on the specific enzyme target with very low development in the disease treatment. Most of the described compounds are shown to have beneficial therapeutic effects but at the same time these compounds, selective for 'multi-signaling pathway' targets, may also increase the side-effect potential

Novel thiazole derivatives: a patent review (2008-2012. Part.2)

Thiazole is a well-known five-membered heterocyclic compound. Various methods have been worked out for its synthesis. In the last few decades, a lot of work has been done on thiazole ring in order to find new compounds related to this scaffold acting as antioxidant, analgesic, anti-inflammatory, antimicrobial, antifungal, antiviral, diuretic, anticonvulsant, neuroprotective and antitumor or cytotoxic drugs with lesser side effects. This review presents the up to date development of different thiazole derivatives. The present review gives an account of the recent therapeutic patent literature (2008-2012) describing the applications of thiazole and its derivatives on selected activities. In this review many of relevant biological properties and the therapeutic applications of thiazole derivatives reported in international patents from all companies have been discussed; an overview of the chemical matter has also been given. Because of the huge amount of patents registered in this period relative to thiazole derivatives, we focused our attention, in the first part of the review just published, on inhibitors of phosphatidylinositol-3-kinase, inhibitors of protein kinase and derivatives modulating enzymes related to metabolism, whereas in this second part we focused on thiazole derivatives having pharmacological activity towards receptors. Based on the large variety of possible therapeutic applications proposed in patents for thiazole derivatives having pharmacological activity towards receptors, it is possible to point out the unpredictability of pharmacological activity consequent to structural modification, more or less simple, of a prototype drug molecule. In any case the thiazole scaffold remains one of great potential for the chemical pharmaceutical research