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PHYTIC ACID ESTER DERIVATIVE

Foreign code F200010171
File No. (S2018-0906-N0)
Posted date Jun 3, 2020
Country WIPO
International application number 2019JP034220
International publication number WO 2020045653
Date of international filing Aug 30, 2019
Date of international publication Mar 5, 2020
Priority data
  • P2018-161944 (Aug 30, 2018) JP
Title PHYTIC ACID ESTER DERIVATIVE
Abstract The present invention relates to a phytic acid ester derivative and a use of the phytic acid ester derivative. A phytic acid ester derivative according to the present invention has the structure of formula I. [Chemical formula 1] (In formula I, each of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 independently represents H or a structure selected from the group consisting of structures of formula II, structures of formula III and structures of formula IV, excluding the cases where all of the R1-R12 moieties are H.) [Chemical formula 2] (In formula II, -CH2- may optionally be substituted by one or two substituents.) [Chemical formula 3] (In formula III, -CH2-C6H4- may optionally be substituted by one or more substituents.) [Chemical formula 4] (In formula IV, -CH2-CH2- may optionally be substituted by one or more substituents.)
Outline of related art and contending technology BACKGROUND ART
Phytic acid (myo - inositol phosphate-1, 2, 3, 4, 5, 6, IP6) within the cells of the human is a mammal such biosynthetic, the number of seeds are also present in the plant tissue is a major storage form of phosphorus. Grain, beans are also be taken from the food or the like. A portion thereof is absorbed, and the like may be captured by pinocytosis cell.
A high concentration of the cancer when added to the cells IP6, cell growth inhibition effect is well studied, has been of interest. JP-2003-238414 is, inositol phosphates acids (inositol 6 phosphoric acid) as an active ingredient is disclosed an anti-tumor agent. Also is IP6, an increase in immunity, kidney stone formation is suppressed, lowering cholesterol, to reduce the risk of coronary artery disease and diabetes and the like are known to have a variety of activity. Vucenik l.et al., Nutrion and Cancer, 2006, 55, 109 is, the anti-oxidant, an increase in immunity, anti-inflammatory, an enzyme and the enzyme modified Phase I Pjase II, cancer gene control, anti-angiogenic, anti-metastatic tumor, induction of apoptosis, cell differentiation increases, such as inhibition of cell proliferation is to have a variety of effects such as IP6 is described.
IP6 In this manner is achieved a beneficial effect of the many, many of the phosphate group 6 from having a negative charge of the cell through the membrane is difficult for, is limited in the amount of cells is IP6. Chelating with the metal IP6 also has a property of blocking the absorption of the mineral body, side effects due to the ingestion of large quantities have been noted.
Is disclosed in JP-2009-541222, any combination of the IP-6, a pharmaceutically acceptable salt, or a pharmaceutically acceptable derivative thereof, an effective amount of a pharmaceutical composition comprising the step of administering to the mammal, ionizing radiation exposure in a mammal, short-term acute health and method for preventing or treating affected (claim 1) is described. Is disclosed in JP-2009-541222 paragraph 0015, " is the object of the present application and/or pyrophosphoric acid as well as IP-6 inositol for derivatives thereof, those skilled in the art, ' 6 inositol phosphate, IP-6, and its analogs are entered as a drug test. One of the challenge 1, to facilitate the passage of molecules into cells in order, a phosphate protecting group in the cover. (DOE report of 13 July 2005) ' has been concluded. And/or pyrophosphoric acid as well as IP-6 and its derivatives containing inositol, the effect as the current protection concept that is not suggested. " In the drawing. IP6 In the cell in order to facilitate the passage of molecules to, phosphate protecting group is referred to as covering. However, it is described that, in particular phosphate protecting groups such as any one of the cover, even if the protecting group is covered with a phosphate compound added into the cell is actually of one of the molecules is promoted, the compound into the cell in the cell has what function is not at all suggested.
IP6 Poor uptake into cells, is limited in the amount, and in spite of the problem, the concrete method to solve the problem has not been provided.
Scope of claims (In Japanese)[請求項1]
 以下の式Iの化合物。
[化1]
(省略)
 [式I中、R 1、R 2、R 3、R 4、R 5、R 6、R 7、R 8、R 9、R 10、R 11およびR 12は、各々独立に、H、式II
[化2]
(省略)
 (式II中、-CH 2-は所望により1若しくは2の置換基により置換されていてもよい)、
式III
[化3]
(省略)
 (式III中、-CH 2-C 6H 4-は所望により1若しくは複数の置換基により置換されていてもよい)、
および、式IV
[化4]
(省略)
 (式IV中、-CH 2-CH 2-は所望により1若しくは複数の置換基により置換されていてもよい)
からなるグループから選択される、
 ただし、R 1-R 12の全てがHである場合を除く。

[請求項2]
 式II、式IIIまたは式IVにおいて、置換若しくは未置換のC 1-6アルキル若しくはアリールが、置換若しくは未置換のメチル、置換若しくは未置換のエチルおよび置換若しくは未置換のブチルからなる群から選択される、請求項1の化合物。

[請求項3]
 R 1、R 2、R 3、R 4、R 5、R 6、R 7、R 8、R 9、R 10、R 11およびR 12の6個以上がHではない、請求項1または2に記載の化合物。

[請求項4]
 R 1、R 2、R 3、R 4、R 5、R 6、R 7、R 8、R 9、R 10、R 11およびR 12の全てがHではない、請求項1-3のいずれか1項に記載の化合物。

[請求項5]
 C 1-6アルキル若しくはアリールが、ハロゲン、C 1-4アルキル、アミノ基、ニトロ基、フェニル基、ヒドロキシル基、チオール基、C 1-4アシルおよびアリル基からなる群から選択される置換基で置換されている、請求項1-4のいずれか1項に記載の化合物。

[請求項6]
 式II中の-CH 2-、式III中の-CH 2-C 6H 4-、および式IV中の-CH 2-CH 2-の1以上が、ハロゲン、C 1-4アルキル、アミノ基、ニトロ基、フェニル基、ヒドロキシル基、チオール基、C 1-4アシルおよびアリル基からなる群から選択される置換基で置換されている、請求項1-5のいずれか1項に記載の化合物。

[請求項7]
 R 1、R 2、R 3、R 4、R 5、R 6、R 7、R 8、R 9、R 10、R 11およびR 12の全てが、ブチリルオキチメチルまたはアセトキシメチルである、請求項1に記載の化合物。

[請求項8]
 生体内で加水分解されて、R 1、R 2、R 3、R 4、R 5、R 6、R 7、R 8、R 9、R 10、R 11およびR 12の一部または全てがHになる、請求項1-7のいずれか1項に記載の化合物。

[請求項9]
 請求項1-8のいずれか1項に記載の式Iの化合物を含む、医薬組成物。

[請求項10]
 細胞増殖抑制、細胞傷害抑制、免疫力上昇、コレステロール低下、腎結石形成抑制、がん転移抑制、および繊維化抑制からなる群から選択される活性を有する、請求項9に記載の医薬組成物。

[請求項11]
 がん、冠動脈疾患、糖尿病および結石症からなる群から選択される疾患を予防または処置するための請求項9または10に記載の医薬組成物。

[請求項12]
 がんが白血病、リンパ腫、骨髄腫からなる群から選択されるがんである、請求項11に記載の医薬組成物。

[請求項13]
 経口投与、経皮投与、腹腔内投与または静脈内投与される、請求項9-12のいずれか1項に記載の医薬組成物。

[請求項14]
 式Iの化合物が生体内で加水分解されて、R 1、R 2、R 3、R 4、R 5、R 6、R 7、R 8、R 9、R 10、R 11およびR 12の一部または全てがHになる、請求項9-13のいずれか1項に記載の医薬組成物。

[請求項15]
 請求項1-8のいずれか1項に記載の式Iの化合物の医薬組成物の製造のための使用。

[請求項16]
 請求項1-8のいずれか1項に記載の式Iの化合物を含む、化粧用組成物。

[請求項17]
 美白作用または美肌作用を有する請求項16に記載の化粧用組成物。

[請求項18]
 請求項1-8のいずれか1項に記載の式Iの化合物を含む、研究用試薬。
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • NATIONAL UNIVERSITY CORPORATION KUMAMOTO UNIVERSITY
  • Inventor
  • FUJITA MIKAKO
  • OTSUKA MASAMI
  • OHSUGI TAKEO
  • TATEISHI HIROSHI
  • MURAO NAOKI
  • MASUNAGA TAKUYA
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 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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