Nam, Ghilsoo 2024-01-19T21:04:25Z 2024-01-19T21:04:25Z 2021-09-05 2018-12-02 1354-3776 https://pubs.kist.re.kr/handle/201004/120591 Introduction: T-type calcium channels are attractive targets for potential treatment of epilepsy inflammatory or neuropathic pain, insomnia, Parkinson's disease, and cancer. Three isoforms having different biophysical functions are expressed in peripheral and central nerve. Since the withdrawal of mibefradil, the first compound marketed for selective T-type calcium channel blockade, extensive efforts have been made to identify more selective T-type calcium channel blockers. Areas covered: This review covers the 43 patents describing 'organic small molecules as T-type calcium channel blockers'-published since 2012. The most recent similar patent review was published in 2011. Information from a recent review article and relevant research papers has been included, as well as biological data and clinical trial results where available. Expert opinion: Triazinone derivatives, carbazole compounds, and aryl triazole/imidazole amide derivatives display potent blockade activity alpha 1H, alpha 1G, and pan T-type calcium channel subtypes, respectively, though the specificity of the letter is still unsatisfactory. Nonetheless, improvements seen in the efficacy of compounds targeting alpha 1H T-type calcium channels indicate significant progress. Ongoing clinical trials are for the candidates Z944 (Phase II) and ACT-709478 (Phase II) appear promising. These studies may lead to a new generation of inhibitors with higher selectivity, improved physicochemical properties, and reduced side effects. English TAYLOR & FRANCIS LTD BIOLOGICAL EVALUATION CA2+ CHANNELS DERIVATIVES LOCALIZATION SULFONAMIDES DISCOVERY POTENT T-type calcium channel blockers: a patent review (2012-2018) Article 10.1080/13543776.2018.1541982 1 EXPERT OPINION ON THERAPEUTIC PATENTS, v.28, no.12, pp.883 - 901 EXPERT OPINION ON THERAPEUTIC PATENTS 28 12 883 901 scie scopus 000452205500004 2-s2.0-85058005418 Chemistry, Medicinal Pharmacology & Pharmacy Pharmacology & Pharmacy Article BIOLOGICAL EVALUATION CA2+ CHANNELS DERIVATIVES LOCALIZATION SULFONAMIDES DISCOVERY POTENT CNS-related disease epilepsy neuropathic pain selective T-type calcium channel blocker