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LEVODOPA DERIVATIVE AND USE THEREOF

外国特許コード F200010234
整理番号 (S2019-0223-N0)
掲載日 2020年10月29日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2020JP004494
国際公開番号 WO2020166473
国際出願日 令和2年2月6日(2020.2.6)
国際公開日 令和2年8月20日(2020.8.20)
優先権データ
  • 特願2019-022895 (2019.2.12) JP
発明の名称 (英語) LEVODOPA DERIVATIVE AND USE THEREOF
発明の概要(英語) [Problem] To provide a medicine in which problems associated with the use of L-DOPA in treating Parkinson's disease, for example, poor retentivity in blood are improved.
[Solution] By incorporating L-DOPA in the form of a block copolymer [PEG-b-poly(3,4-hydroxy protected L-DOPA)] into a carrier, the retentivity of the medicine in blood is significantly improved.
従来技術、競合技術の概要(英語) BACKGROUND ART
A disease in which the number of dopamine cells in the brain is reduced by gene mutation, dopamine, a neurotransmitter, is not sufficiently produced, and symptoms such as muscle solidification and tremor appear is sometimes abbreviated as Parkinson's disease (or less, PD, and). (Non-Patent Document 1), where L-dopa, which is a precursor of dopamine and is capable of passing through the blood-brain barrier (BBB), is used as PD therapeutic agent (levodopa), which is a mechanism for limiting substance exchange between blood and brain tissue fluid.
L-dopa (3,4-dihydroxy-L-phenylalanine or levodopa) is extremely excellent in that it is highly effective at the early stage of treatment, has little side effects, and is inexpensive, while it is a drawback that the half-life is the largest. In the latter stage of treatment, dopamine retention of dopamine neurons decreases with progress of primary disease, and the treatment area becomes narrower. As a result, adjustment of dosage becomes difficult due to low blood retention of L-dopa, and a wearable off phenomenon in which improvement and deterioration of symptoms are repeated in a day or dyskinesia due to excessive administration is observed.
In order to overcome such a problem, there are some reports aiming at improving retention of L-dopa in blood using (Patent Document 1) or nanoparticles of prodrugs of L-dopa such as esterification or L-dopa, for example, esters or peptides of L-dopa. As the latter, for example, nanoparticles in which PLGA is supported extend the half-life of L-dopa in blood, and (Non-Patent Document 3), and (Non-Patent Document 4) in which micelles in which chitosan is an outer shell and dopamine is supported by a core can penetrate into the brain together with micelles by loosening tight junction of BBB by chitosan. However, in the nanoparticles, it is possible to cause unexpected leakage of L-dopa due to its weak binding force, and in the latter, it is suggested that blood toxins and the like can be simultaneously transferred into the brain due to loosening of tight junction.
There are few reports on effective parkinson's disease in order to treat L-dopa. L-dopa easily causes oxidative polymerization in the atmosphere to produce a melanin-like viscous black substance, and therefore is applied as a surface modifier. however, the bond of L-dopa cannot be decomposed in vivo because of its strong carbon-carbons, and is difficult to use as a prodrug. On the other hand, there is a report example in which L-dopa is polymerized by a peptide bond degradable by an enzyme in vivo and used as a bioadhesive, but side reactions due to oxidative polymerization during synthesis are not considered. Therefore, there is also a method of protecting the two hydroxyl groups with acetyl groups in advance in order to prevent oxidative polymerization during the reaction, but the use of hydrogen chloride causes danger.
  • 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
  • UNIVERSITY OF TSUKUBA
  • 発明者(英語)
  • NAGASAKI, Yukio
  • SATO, Yuna
  • VONG, Binh Long
  • CHONPATHOMPIKUNLERT, Pennapa
  • HUTAMEKALIN, Pilaiwanwadee
  • TAKAHASHI, Reita
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 DJ DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JO JP KE KG KH KN KP KR KW 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 ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN WS 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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