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PROMOTOR FOR PERMEATION INTO CELL LAYER, COMPOSITION FOR FACILITATING DRUG AGENT ABSORPTION, AND PHARMACEUTICAL COMPOSITION

Foreign code F200010255
File No. (S2019-0227-N0)
Posted date Nov 5, 2020
Country WIPO
International application number 2020JP012446
International publication number WO2020196315
Date of international filing Mar 19, 2020
Date of international publication Oct 1, 2020
Priority data
  • P2019-057323 (Mar 25, 2019) JP
Title PROMOTOR FOR PERMEATION INTO CELL LAYER, COMPOSITION FOR FACILITATING DRUG AGENT ABSORPTION, AND PHARMACEUTICAL COMPOSITION
Abstract Provided is a technique for promoting permeation of a substance into a cell layer. Provided are: a promotor for permeation into a cell layer, constituted of a compound represented by general formula (1); a composition for facilitating drug agent absorption, containing said promotor for permeation into a cell layer and configured to facilitate drug agent absorption into a living body; and a pharmaceutical composition containing said promotor for permeation into a cell layer, and further containing a drug agent to be absorbed by a living body.
Outline of related art and contending technology BACKGROUND ART
In a cell layer forming epithelial tissue or the like, a gap between adjacent cells is sealed by a cell adhesion structure such as a tight junction (TJ: Tight Junction) or the like to fulfill a barrier function against foreign matter. Therefore, the permeability of the intercellular pathway through the intercellular pathway is very limited to maintain the homeostasis of the living body. There is a concept of a drug delivery system (DDS: Drug Delivery System) in which the cell adhesion structure is primarily relaxed to allow a desired substance to permeate through the intercellular pathway, thereby enhancing absorption of a drug or the like into a living body. Some biopharmaceuticals and candidates thereof which are actively developed, such as peptides, proteins, antibodies, vaccines, nucleic acids, etc., have low bioavailability, The development of techniques is desired because the range of applicability of such drugs is widened and the improvement of Quality of Life in a patient is also achieved by non-invasive administration methods such as oral, transdermal, nasal, pulmonary, transmucosal or the like instead of injection administration.
On the other hand, the following Non-Patent Document 6 reports cyclic lipopeptides as antibacterial substances derived from Pseudomonas bacteria.
Scope of claims (In Japanese)[請求項1]
 下記一般式(1)で表わされる化合物からなる細胞層透過促進剤。
[化1]
(省略)
(一般式(1)中、Rは、置換基を有してもよい炭素数1~9のアルキル基であり、
 Xは、ロイシン又はその保存的置換、より好ましくは、ロイシン、イソロイシン、ノルロイシン、tert-ブチルアラニン、tert-ロイシン、バリン、シクロへキシルグリシン、又はシクロヘキシルアラニン、又はアラニンであり、
 XXは、バリン又はその保存的置換、より好ましくは、バリン、イソロイシン、ノルロイシン、tert-ブチルアラニン、tert-ロイシン、ロイシン、シクロへキシルグリシン、又はシクロヘキシルアラニン、又はアラニンであり、
 Yは、グルタミン酸又はその保存的置換、より好ましくは、グルタミン酸又はアスパラギン酸、又はアラニンであり、
 Zは、グルタミン又はその保存的置換、より好ましくは、グルタミン又はアスパラギン、又はアラニンであり、
 ZZは、任意のα-アミノ酸、より好ましくは、グルタミン又はアラニンであり、
 YZは、セリン、スレオニン、ホモセリン、ジアミノプロパノイックアシッド、又はジアミノブチリックアシッドであり、
 R’は、sec-ブチル又はその保存的置換、より好ましくは、sec-ブチル、イソプロピル、イソペンチル、n-ブチル、tert-ブチル、シクロへキシル、又はシクロへキシルメチルである。)

[請求項2]
 前記一般式(1)で表わされる化合物は、下記一般式(2)で表わされる化合物である、請求項1記載の細胞層透過促進剤。
[化2]
(省略)
(一般式(2)中、Rは、置換基を有してもよい炭素数1~9のアルキル基であり、
 ZZは、任意のα-アミノ酸、より好ましくは、グルタミン又はアラニンである。)

[請求項3]
 請求項1又は2に記載の細胞層透過促進剤を含み、生体への薬剤の吸収を補助するためのものである、薬剤吸収補助用組成物。

[請求項4]
 請求項1又は2に記載の細胞層透過促進剤を含み、生体に吸収させるべき薬剤を更に含む、医薬組成物。
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • UNIVERSITY OF TSUKUBA
  • TOKYO UNIVERSITY OF PHARMACY AND LIFE SCIENCES
  • Inventor
  • USUI Takeo
  • NAGUMO Yoko
  • MUKAIYAMA Minagi
  • HAYASHI Yoshio
  • TANIGUCHI Atsuhiko
  • UCHIYAMA Chihiro
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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