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METASTIN DERIVATIVE AND USE THEREOF

外国特許コード F140007896
整理番号 2043
掲載日 2014年8月13日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2009JP058409
国際公開番号 WO 2009139298
国際出願日 平成21年4月28日(2009.4.28)
国際公開日 平成21年11月19日(2009.11.19)
優先権データ
  • 特願2008-119235 (2008.4.30) JP
発明の名称 (英語) METASTIN DERIVATIVE AND USE THEREOF
発明の概要(英語) Disclosed is a metastin derivative represented by formula (I) (wherein the symbols are as defined in the description), a salt thereof, or a pharmaceutical composition containing the metastin derivative or a salt thereof. The metastin derivative or a salt thereof exhibits excellent stability in the blood and has cancer metastasis suppressing activity or cancer growth suppressing activity.
従来技術、競合技術の概要(英語) Background of the invention) many hormone and neurotransmitter is present in the cell membrane via specific receptors modulating the function of a living body. Many of these receptors is conjugated to the guanine nucleotide-binding protein (guanine nucleotide-binding protein, hereinafter, abbreviated as g protein) through the activation of the intracellular signal transduction. In addition, these receptors, cells having a common transmembrane region 7 and has a structure in which it is possible to, g protein-coupled receptor is a membrane-receptor or collectively referred to as 7.
G protein-coupled receptor such as one of the protein, a human GPR54 receptor protein encoded by the gene known to non-patent document 1.
In addition, the above physiologically active peptides as a function as a ligand for GPR54, 2 (also known as: ) non-patent document is known. Metastasis of cancer in the patient's life expectancy is the important factors influencing. GPR54 Acts as an agonist in the lung is migration inhibiting the expression of GPR54 melanoma cells in Non-Patent Document 2 is known. In addition, expression of GPR54 in the same manner as pancreatic cancer cells to inhibition of the transfer may also be in the non-patent document 3]. On the other hand, in the brain by acting GPR54 agonists to release of the sex hormones such as gonadotropin is promoted by the non-patent document 4, the function of the loss of hypogonadism GPR54 to cause the non-patent document 5 has been recently revealed one after another. As described above /GPR54 system is a cancer metastasis suppressing and sexual function in both faces of the disease a very attractive target for drug discovery.
The inventors of the present invention, the basic functional group N end groups and bis -2 -, GPR54 having agonist pentapeptide derivative was found to be non-patent document 6]. Further, the ligand having 4 - fluorobenzoyl group N-terminus, thus far reported demonstrate agonist activity a compound which is the most potent biological activity has been found that, by quantitative structure activity relationship studies and its structure and activity associated with the obtained information relating to non-patent document 7]. In addition, N-terminus or as a whole (i) an electron-withdrawing nature of the aryl group is an aryl group, (ii) a nitrogen atom, oxygen atom and a sulfur atom species selected from the group consisting of at least 1 hetero atom containing substituted or unsubstituted aromatic heterocyclic group, or (iii) a lower alkoxy group, hydroxy lower alkyl group, amino lower alkyl group, lower lower alkyl group, hydroxy substituted group, amino groups and hydroxyl groups are selected from the group consisting of 1-3 substituted with an electron donating group with an aryl group has been so modified as to have excellent pentapeptides are found that have agonist activity on GPR54 Patent Document 1.
On the other hand, associated peptide can , the dipeptide Gly-Leu C-terminus of the peptide bond between a plurality of matrix metalloproteinase (MMP) receive decomposed by has been reported, and clinical application of related peptide when taking into account, or a combination of MMP inhibitor is not subject to degradation by MMP derivatives suggests that requires the use of a non-Patent Document 8.
CITATION LIST
  • 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
  • Kyoto University
  • TAKEDA PHARMACEUTICAL COMPANY LIMITED
  • 発明者(英語)
  • FUJII, Nobutaka
  • OISHI, Shinya
  • TOMITA, Kenji
国際特許分類(IPC)
指定国 National States: AE AG AL AM AO AT AU AZ BA BB BG BH BR BW BY BZ CA CH 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 IS JP KE KG KM KN KP KR KZ LA LC LK LR LS LT LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PG PH PL PT RO RS RU SC SD SE SG SK SL SM ST SV SY TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LS MW MZ NA SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ MD RU TJ TM
EPO: 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 SE SI SK TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG
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