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LACTATE DEHYDROGENASE INHIBITOR AND ANTIEPILEPTIC DRUG CONTAINING SAME UPDATE

外国特許コード F160008857
整理番号 (S2015-0530-N0)
掲載日 2016年9月23日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2016JP053764
国際公開番号 WO 2016129583
国際出願日 平成28年2月9日(2016.2.9)
国際公開日 平成28年8月18日(2016.8.18)
優先権データ
  • 特願2015-023572 (2015.2.9) JP
発明の名称 (英語) LACTATE DEHYDROGENASE INHIBITOR AND ANTIEPILEPTIC DRUG CONTAINING SAME UPDATE
発明の概要(英語) The invention provides a lactate dehydrogenase inhibitor that makes it possible to suppress refractory epilepsy in which conventional antiepileptic drugs are ineffective, and an antiepileptic drug containing said inhibitor. The lactate dehydrogenase inhibitor of the invention contains a compound represented by formula (III); i.e., isosafrole or a compound having isosafrole as a scaffold, and the antiepileptic drug of the invention has these compounds as an active ingredient.
従来技術、競合技術の概要(英語) BACKGROUND ART
Epilepsy, of electrical activity of the brain and neurological disease caused by hyperexcitability, characteristic to be diagnosed by the brain waves (epilepsy brain wave). Prevalence, of the total population as high as about 1%. As a method for the treatment of epilepsy is mainly drug therapy, the therapeutic agent is one or more of the epileptic 20 used in clinical practice (non-patent document 1). However, about 3 to interrupt epilepsy patients, these existing epilepsy of the use of the therapeutic agent is not known. Against this backdrop, the sole so that existing drugs' refractory epilepsy ' with respect to the therapeutic agent, which is now a need.
Epilepsy, which causes the excess for neuro-electrical excitement, electrical control the activities of therapeutic agents that target molecules is in most cases. Specifically, ion channel, a receptor at a synapse, a neurotransmitter transporter (non-patent document 2) in. On the other hand, the sole so that these existing drugs against a portion of the patients with epilepsy, the ketogenic diet called 'diet' is effective, clinically known (non-patent document 3). Recently, ketone diet revealed one after another anti-epileptic mechanism by which (non-patent document 4-6). That is, if the energy metabolism pathways agent, refractory epilepsy promise as therapeutic agents.
One of the anti-epileptic drug, stiripentol (CAS: 49763-96 - 4, 4 - dimethyl -1 - [(3, 4 - methylenedioxy) - phenyl] -1 - pentene -3 - ol, see the following formula (I) ) is present. First stiripentol, developed as a brain disease (Patent Document 1), then one of the refractory epilepsy Dravet syndrome (pediatric epilepsy one) has been revealed that works on the (non-patent document 7, 8). The current, as a therapeutic Dravet syndrome, Europe (2007 year approval) in Japan (2012 year approval), under the trade name deer commit are in clinical use. However, although successfully Dravet syndrome, with respect to the other of the epileptic (particularly adult epilepsy), stiripentol has failed in clinical trials at present (non-patent document 9) in.
Recently, stiripentol is, lactate dehydrogenase (lactate dehydrogenase; LDH) is an inhibitor of have been reported (patent document 2). Lactate dehydrogenase enzyme which is, 'energy metabolism path' present, lactic acid and pyruvate can convert 'metabolic enzyme' in. Lactate dehydrogenase inhibitor itself, up to now, the development of anti-malarial agent mainly (non-patent document 10, 11), and anti-cancer agent that is (non-patent document 12, 13) have been created for the purpose. However, these lactate dehydrogenase inhibitor, whether a seizure is unknown. That is, in the present stage, stiripentol 'inhibitory effect on lactate dehydrogenase' the only 'anti-epileptic agent' is.
  • 出願人(英語)
  • ※2012年7月以前掲載分については米国以外のすべての指定国
  • NATIONAL UNIVERSITY CORPORATION OKAYAMA UNIVERSITY
  • 発明者(英語)
  • INOUE TSUYOSHI
  • SADA NAGISA
国際特許分類(IPC)
指定国 National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JP KE KG KN KP KR KZ LA LC LK LR LS LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SA SC SD SE SG SK SL SM ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN ST TD TG

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