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METHYLATED POLYROTAXANE AND SYNTHESIS METHOD FOR SAME

Foreign code F170009287
File No. (S2016-0657-N0)
Posted date Nov 14, 2017
Country WIPO
International application number 2017JP016390
International publication number WO 2017188257
Date of international filing Apr 25, 2017
Date of international publication Nov 2, 2017
Priority data
  • P2016-090121 (Apr 28, 2016) JP
Title METHYLATED POLYROTAXANE AND SYNTHESIS METHOD FOR SAME
Abstract The present invention provides an acid-cleavable polyrotaxane compound that includes: a plurality of methylated annular molecules; and a straight-chain molecule that has a terminal group. The acid-cleavable polyrotaxane compound that includes a plurality of methylated annular molecules can be produced by means of a production method that includes a step for reacting an acid-cleavable polyrotaxane with methyl iodide in the presence of powdered sodium hydroxide. The acid-cleavable polyrotaxane compound that includes a plurality of methylated annular molecules can be used as a therapeutic agent for diseases such as lysosomal diseases and cancer.
Scope of claims [claim1]
1. It includes with the plural annular molecules which are methylated and the direct condition molecule which possesses the end group, acid decomposition characteristic porirotakisan chemical compound.
[claim2]
2. It disassembles under acidic environment inside the cell or under the acidic environment of pH4.0-6.0, the porirotakisan chemical compound of claim 1 statement.
[claim3]
3. The annular molecule is .beta.-shikurodekisutorin, claim 1 or either of 2 the porirotakisan chemical compound of one section statement.
[claim4]
4. The hydroxyl group of B-shikurodekisutorin is methylated, the porirotakisan chemical compound of claim 3 statement.
[claim5]
5. B-shikurodekisutorin per 1 molecules the 6-21 has the methyl group, claim 3 or the porirotakisan chemical compound of 4 statements.
[claim6]
6. The direct condition molecule includes polyethylene glycol (PEG) and/or polypropylene glycol (PPG), either of the claim 1-5 the porirotakisan chemical compound of one section statement.
[claim7]
7. The direct condition molecule includes porokisama, either of the claim 1-6 the porirotakisan chemical compound of one section statement.
[claim8]
8. The molecular weight of the direct condition molecule is the 4000-7000, either of the claim 1-7 the porirotakisan chemical compound of one section statement.
[claim9]
9. Ratio of the number of molecules of direct condition molecule and annular molecule 1:10-1: 15 it features that is, either of the claim 1-8 the porirotakisan chemical compound of one section statement.
[claim10]
10. The end group, has the substituent or the O-torihueniru methyl group which it does not possess, it possesses the substituent or it possesses the S-torihueniru methyl group, and the substituent which it does not possess or it is selected from the group which consists of the N-torihueniru methyl group which it does not possess, either of the claim 1-9 the porirotakisan chemical compound of one section statement.
[claim11]
11. The end group through peptide bond, the Kaaba mate connection, ester connection or ether linkage in the direct condition molecule, it is connected, either of the claim 1-10 the porirotakisan chemical compound of one section statement.
[claim12]
12. B-shikurodekisutorin which possesses below-mentioned structural formula, is methylated being the porirotakisan chemical compound which includes the direct condition molecule,
Here, m is the integer which shows the number of repetition units of the polypropylene glycol in porokisama, n is the integer which shows the number of repetition units of polyethylene glycol, x is the integer which shows the quantity of .beta.-shikurodekisutorin,
.beta.-shikurodekisutorin per 1 molecules the 6-21 has the methyl group, the direct condition molecule includes polyethylene glycol (PEG) and/or polypropylene glycol (PPG), the average molecular weight of the direct condition molecule is the 4000-7000, several x of .beta.-shikurodekisutorin are the 10-15, the end group consists of the N-torihueniru methyl group, it is acid decomposition characteristic, the porirotakisan chemical compound where the entire average molecular weight is the 18,000-27,000.
[claim13]
13. The plural annular molecules which are methylated are included, being production method of acid decomposition characteristic porirotakisan chemical compound, under powdered sodium hydroxide existing it includes acid decomposition characteristic porirotakisan and the process which reacts iodide methyl, production method.
[claim14]
14. The plural annular molecules which are methylated are included, being production method of acid decomposition characteristic porirotakisan chemical compound, reacting with process, aforementioned porokisama and .beta.-shikurodekisutorin which obtain porokisama which possesses one class amino group in both ends of porokisama both ends of process and aforementioned pseudo porirotakisan which obtain pseudo porirotakisan with N-torichirugurishin it includes acid decomposition characteristic porirotakisan and the process which reacts iodide methyl under process, and the powdered sodium hydroxide existence which the capping are done, production method.
[claim15]
15. The plural shikurodekisutorin molecules which are methylated are included, acid decomposition characteristic porirotakisan chemical compound is contained, the composition in order to induce automatic fuzzy in the cell.
[claim16]
16. The plural shikurodekisutorin molecules which are methylated are included, the medicine composition in order contains acid decomposition characteristic porirotakisan chemical compound, to remedy the cancer.
[claim17]
17. The cancer is the cancer of apotoshisu tolerance, the medicine composition of claim 15 statement.
[claim18]
18. The plural shikurodekisutorin molecules which are methylated are included, the medicine composition in order the disease which contains acid decomposition characteristic porirotakisan chemical compound, originates in the cholesterol accumulation inside the cell or the disease which originates in automatic fuzzy dysfunction it remedies or to prevent, or.
[claim19]
19. The plural shikurodekisutorin molecules which are methylated are included, acid decomposition characteristic porirotakisan chemical compound is contained, C types of the knee man pick illness (NPC) the medicine composition in order it remedies or to prevent, or.
[claim20]
20. It includes with porokisama which possesses the N-torihueniru methyl group in the end as .beta.-shikurodekisutorin and the direct condition molecule which possess the substituent as the annular molecule, acid decomposition characteristic porirotakisan chemical compound.
[claim21]
21. It includes with porokisama which possesses the N-torihueniru methyl group in the end as .beta.-shikurodekisutorin and the direct condition molecule which possess the substituent as the annular molecule, acid decomposition characteristic porirotakisan chemical compound is contained, C types of the knee man pick illness (NPC) the medicine composition in order it remedies or to prevent, or.
[claim22]
22. It possesses the below-mentioned structural formula, the hydroxy ethoxy .beta.-shikurodekisutorin which ethylates being the porirotakisan chemical compound which includes the direct condition molecule,
Here, m is the integer which shows the number of repetition units of the polypropylene glycol in porokisama, n is the integer which shows the number of repetition units of polyethylene glycol, x is the integer which shows the quantity of .beta.-shikurodekisutorin,
.beta.-shikurodekisutorin per 1 molecules the 6-21 has the hydroxy ethoxy ethyl group, the direct condition molecule includes polyethylene glycol (PEG) and/or polypropylene glycol (PPG), the average molecular weight of the direct condition molecule is the 4000-7000, several x of .beta.-shikurodekisutorin are the 10-15, the end group consists of the N-torihueniru methyl group, the porirotakisan chemical compound which is acid decomposition characteristic.
[claim23]
23. The porirotakisan chemical compound of statement is included in claim 22, the composition in order to induce automatic fuzzy in the cell and the medicine composition in order to remedy the cancer of apotoshisu tolerance, the medicine composition in order the disease which originates in the cholesterol accumulation inside the cell or the disease which originates in automatic fuzzy dysfunction it remedies or to prevent, or, or, C types of the knee man pick illness (NPC) the medicine composition in order it remedies or to prevent, or.
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • TOKYO MEDICAL AND DENTAL UNIVERSITY
  • Inventor
  • YUI NOBUHIKO
  • TAMURA ATSUSHI
  • NISHIDA KEI
IPC(International Patent Classification)
Specified countries (WO2017188257)
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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