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LEVODOPA DERIVATIVE AND USE THEREOF

Foreign code F200010234
File No. (S2019-0223-N0)
Posted date 2020年10月29日
Country 世界知的所有権機関(WIPO)
International application number 2020JP004494
International publication number WO2020166473
Date of international filing 令和2年2月6日(2020.2.6)
Date of international publication 令和2年8月20日(2020.8.20)
Priority data
  • 特願2019-022895 (2019.2.12) JP
Title LEVODOPA DERIVATIVE AND USE THEREOF
Abstract [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.
Outline of related art and contending technology 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.
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • UNIVERSITY OF TSUKUBA
  • Inventor
  • NAGASAKI, Yukio
  • SATO, Yuna
  • VONG, Binh Long
  • CHONPATHOMPIKUNLERT, Pennapa
  • HUTAMEKALIN, Pilaiwanwadee
  • TAKAHASHI, Reita
IPC(International Patent Classification)
Specified countries 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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