Pyrazine derivatives: a patent review (June 2012 - present)
Language English Country England, Great Britain Media print
Document type Journal Article, Research Support, Non-U.S. Gov't, Review
- Keywords
- 1,4-diazines, amiloride derivatives, anticancer drugs, antiprotozoal activity, kinase inhibitors, pyrazinamide, pyrazines, sodium channel blockers,
- MeSH
- Alzheimer Disease drug therapy enzymology MeSH
- Drug Industry legislation & jurisprudence MeSH
- Protein Kinase Inhibitors pharmacology MeSH
- Humans MeSH
- Molecular Structure MeSH
- Neuroprotective Agents pharmacology MeSH
- Patents as Topic * MeSH
- Cell Proliferation drug effects MeSH
- Pyrazines chemistry pharmacology therapeutic use MeSH
- Drug Design MeSH
- Amyloid Precursor Protein Secretases antagonists & inhibitors metabolism MeSH
- Structure-Activity Relationship MeSH
- Animals MeSH
- Check Tag
- Humans MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Review MeSH
- Names of Substances
- Protein Kinase Inhibitors MeSH
- Neuroprotective Agents MeSH
- Pyrazines MeSH
- Amyloid Precursor Protein Secretases MeSH
INTRODUCTION: Pyrazine is a member of 1,4-diazines, which constitute an important class of heterocycles. Various pyrazine derivatives have been synthesized and successfully evaluated as agents with diverse pharmacological effects (including but not limited to antiproliferative, anti-infective, and effects on cardiovascular or nervous system) and some of them have become clinically used drugs worldwide. AREA COVERED: This review is a survey of important patents on pyrazine derivatives with pharmacological activity published in the period June 2012 - July 2014. The patent databases SciFinder and esp@cenet were used to locate patent applications. EXPERT OPINION: Pyrazine derivatives possess numerous noteworthy pharmacological effects, including antimycobacterial, antibacterial, antifungal, antidiabetic, diuretic, anticancer, antiviral, hypnotic, and analgesic. The class of pyrazine-based candidate drugs has experienced a rapid growth both in absolute numbers of investigated compounds and in the spectrum of diverse biological activities. We expect that several of these compounds will add to existing pharmaceuticals in the very near future. According to the number of compounds and filed patents, the most promising areas are: i) inhibitors of protein kinases (applicable as antiproliferatives); and ii) inhibitors of β-secretase (applicable for the treatment of Alzheimer's disease).
References provided by Crossref.org
Synthesis and Biological Evaluation of N-Alkyl-3-(alkylamino)-pyrazine-2-carboxamides
