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LITHOCHOLIC ACID DERIVATIVE HAVING VITAMIN D ACTIVITY commons meetings

Foreign code F170009150
File No. (S2016-0294-N0)
Posted date Aug 16, 2017
Country WIPO
International application number 2017JP002902
International publication number WO 2017131144
Date of international filing Jan 27, 2017
Date of international publication Aug 3, 2017
Priority data
  • P2016-014012 (Jan 28, 2016) JP
Title LITHOCHOLIC ACID DERIVATIVE HAVING VITAMIN D ACTIVITY commons meetings
Abstract The objective of the present invention is to provide: a novel lithocholic acid derivative having vitamin D activity; and a pharmaceutical product, a vitamin D receptor activator and a prophylactic and/or therapeutic agent for vitamin D receptor-related diseases, each of which contains the lithocholic acid derivative. The present invention provides a lithocholic acid derivative which has a hydroxyalkyl group in the 3-position, a salt thereof or a prodrug thereof.
Outline of related art and contending technology BACKGROUND ART
Vitamin D is, body metabolic activation 1 α, 25 - dihydroxyvitamin D3 receptor (VDR) is coupled to vitamin D, which controls the expression of specific genes. Under the control of the expression of this gene, vitamin D is, to maintain the calcium concentration in the blood, bone formation, immune function, cell differentiation, growth control responsible for the important physiological functions. So far, osteoporosis, psoriasis and cancer therapeutic agents such as for the purpose of development, a large number of VDR ligands have been developed, some of which are clinical application as a medicament. Many of the existing VDR ligand, in the natural form of 1 α, 25 - dihydroxyvitamin D3 has in the same manner as skeleton. skeleton, a derivative having a high activity useful in the development of, in general chemical stability is low, requires a complicated synthesis, various pharmaceutical applicability of the action of vitamin D is limited. Therefore, non- VDR ligand skeleton type but is desired to be developed, such non--type VDR ligand reported less.
Lithocholate, found to be the endogenous ligand VDR but, is very weak VDR affinity of lithocholic acid, the physiological significance is unknown. Patent Document 1 is, lithocholic acid propionate lithocholic acid derivative is able to activate the VDR is described, in non-patent document 1, lithocholic acid acetate and lithocholic acid propionate is described.
Scope of claims (In Japanese)[請求項1]
下記一般式(I)で示される化合物、その塩、又はそのプロドラッグ。
[化1]
(式中、R1及びR2はそれぞれ独立して、水素原子又は炭素数1から6のアルキル基を示す。R3、R4、R5及びR6はそれぞれ独立して、水素原子又は炭素数1から6のアルキル基を示す。nは1から3の整数を示す。)
[請求項2]
R1及びR2がメチル基又はエチル基である、請求項1に記載の化合物、その塩、又はそのプロドラッグ。
[請求項3]
R3、R4、R5及びR6が水素原子である、請求項1又は2に記載の化合物、その塩、又はそのプロドラッグ。
[請求項4]
nが1である、請求項1から3の何れか一項に記載の化合物、その塩、又はそのプロドラッグ。
[請求項5]
下記の何れかの化合物、その塩、又はそのプロドラッグ。
[化2]
[請求項6]
請求項1から5の何れか一項に記載の化合物、その塩、又はそのプロドラッグを含む医薬。
[請求項7]
請求項1から5の何れか一項に記載の化合物、その塩、又はそのプロドラッグを含む、ビタミンD受容体活性化剤。
[請求項8]
請求項1から5の何れか一項に記載の化合物、その塩、又はそのプロドラッグを含む、ビタミンD受容体関連疾患の予防及び/又は治療剤。
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • OCHANOMIZU UNIVERSITY
  • NATIONAL UNIVERSITY CORPORATION TOKYO MEDICAL AND DENTAL UNIVERSITY
  • Inventor
  • TANATANI Aya
  • SASAKI Harue
  • KAWASAKI Haru
  • KAGECHIKA Hiroyuki
  • MASUNO Hiroyuki
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 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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