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INTERNALLY DEGRADABLE POLYROTAXANE AND SYNTHESIS METHOD THEREFOR

Foreign code F170009292
File No. (S2016-0719-N0)
Posted date Nov 21, 2017
Country WIPO
International application number 2017JP017133
International publication number WO 2017191827
Date of international filing May 1, 2017
Date of international publication Nov 9, 2017
Priority data
  • P2016-092550 (May 2, 2016) JP
Title INTERNALLY DEGRADABLE POLYROTAXANE AND SYNTHESIS METHOD THEREFOR
Abstract The present invention provides a degradable polyrotaxane compound that is easily produced and has large changes in physical properties during degradation. More specifically, said polyrotaxane compound is provided as a result of synthesizing a polyrotaxane compound including at least two linear polymer moieties wherein linear polymers are linked via at least one degradable section. This kind of polyrotaxane compound has a degradable section inside a linear polymer main chain and, as a result, is capable of having a greater change in molecular weight during degradation, compared to conventional degradable polyrotaxane compounds having degradable bonds at both terminals thereof, and is capable of dramatically changing basic physical properties of the polymer such as viscosity, solubility, and glass transition point.
Scope of claims [claim1]
1. The plural annular molecules and, it includes with one linear macromolecule which possesses the end group, said linear macromolecule through one disassembly characteristic part at least, it includes two which is connected linear high-molecular parts at least, porirotakisan chemical compound.
[claim2]
2. The aforementioned linear macromolecule formula below:
X (1)-Y (0) (- Z (i)-Y (i)) [i] - X (2)
It possesses the structure which is shown, here, X (1) and X (2) equality or is the end group which differs, Y (0) and Y (i) equality or is the linear high-molecular part which differs, Z (i) is the disassembly characteristic part, (- Z (i)-Y (i)) [as for i], the repetition unit which consists of the disassembly characteristic part Y and the linear high-molecular part Z i shows the fact that it exists, each Z (i) and Y (i) in the linear macromolecule may be being identical, differing, i is integer of the 1-500, the porirotakisan chemical compound of claim 1 statement.
[claim3]
3. The aforementioned linear macromolecule formula below:
X (1)-Y (0) - Z (1)-Y (1)-X (2)
It possesses the structure which is shown, here, X (1) and X (2) equality or is the end group which differs, Y (0) and Y (1) equality or is the linear high-molecular part which differs, Z (1) is the disassembly characteristic part, the porirotakisan chemical compound of claim 1 statement.
[claim4]
4. Are connected to the aforementioned disassembly characteristic part ratio of length of two linear high-molecular parts which the 1:1-1: It is included in 4, either of the claim 1-3 the porirotakisan chemical compound of one section statement.
[claim5]
5. The aforementioned disassembly characteristic part, is acid decomposition characteristic, enzyme disassembly characteristic, thermal decomposition characteristic or photolysis characteristic, either of the claim 1-4 the porirotakisan chemical compound of one section statement.
[claim6]
6. The aforementioned disassembly characteristic part, to include one disassembly characteristic basis at least, the said disassembly characteristic basis, the p-metokishihuenashiru basis, 2 - the nitro benzyl basis, 2 - the nitro benzyl oxy carbonyl group, 2 - the nitro phenyl ethylene glycol basis and the benzyl oxy carbonyl group, 3,5 - the dimethoxy benzyl oxy carbonyl group, I, .alpha.-jimechiru - 3,5 - the dimethoxy benzyl oxy carbonyl group, 3 - nitro phenyl group, 3 - the nitro phenoxy basis, 3,5 - the jinitorohuenokishi basis, 3 - the nitro phenoxy carbonyl group and the huenashiru basis, 4 - the metokishihuenashiru basis and the .alpha.-mechiruhuenashiru basis, 3,5 - the jimetokishibenzoiniru basis, 2,4 - dinitrobenzene sail phenyl group, (coumarin - 4- iru) the methyl group, 7 - the nitoroindoriniru basis, the aryl azo phosphate, ester connection, Schiff base connection, the Kaaba mate connection, peptide bond, ether linkage, acetal connection, hemiacetal connection and disulfide bond, it is selected from organic peroxide, and the group which consists of acyl hydrazine connection, either of the claim 1-5 the porirotakisan chemical compound of one section statement.
[claim7]
7. The annular molecule, is selected from the group which consists of .alpha.-shikurodekisutorin, .beta.-shikurodekisutorin, and .gamma.-shikurodekisutorin, either of the claim 1-6 the porirotakisan chemical compound of one section statement.
[claim8]
8. The annular molecule one or has the plural substituents, either of the claim 1-7 the porirotakisan chemical compound of one section statement.
[claim9]
9. The substituent, 2 - hydroxy ethoxy ethyl (HEE) the basis, the hydroxyethyl basis, the hydroxypropyl basis, the hydroxy butyl basis and the hydroxy ethoxy ethyl group, N, the N-jimechiru amino ethyl group and the carboxyl group, the methyl group and the sulfo group, one class amino group, polyethylene glycol, the collagen, toransuhuerin, RGD peptide, origoaruginin, (the meta) akuriroiru basis, (the meta) akuriroiruokishi basis, (meta) akuriroiruamino , (the meta) akuriroiruchio basis, the vinyl basis, the aryl basis and the suchiriru basis, and (is selected from the group which consists of the meta) acrylamide basis, the porirotakisan chemical compound of claim 8 statement.
[claim10]
10. The linear high-molecular part, the copolymer and polyethylene imine of polyethylene glycol, polypropylene glycol, polyethylene glycol and polypropylene glycol, is chosen from the polyamino acid, and the group which consists of poly- methyl vinyl ether, either of the claim 1-9 the porirotakisan chemical compound of one section statement.
[claim11]
11. The end group, 2,4 - the dinitrophenyl basis, 3,5 - the dinitrophenyl basis, shikurodekisutorin and the adamantan basis, O-torihueniru methyl (O-Trt) the basis, S-torihueniru methyl (S-Trt) the basis, N-torihueniru methyl (N-Trt) basis and N-torichirugurishin, benzyl oxy carbonyl (Z) the basis, 9 - hureorenirumechiruokishikaruboniru (Fmoc) the basis, benzyl ester (OBz) the basis, third butyl carbonyl (Boc) the basis, amino acid third butyl ester (the OBu basis), the torichiru basis, fluorescein, pyrene and substitution benzene, the multinucleate aromatic which is possible to be substituted, MPC (2 - metakuriroiruokishiechiruhosuhorirukorin), BMA (n-buchiru methacrylate), MPC and BMAIt is selected from the group which consists of combination, and the steroid, either of the claim 1-10 the porirotakisan chemical compound of one section statement.
[claim12]
12. It possesses the below-mentioned structural formula, .alpha.-shikurodekisutorin being the porirotakisan chemical compound which includes the direct condition molecule,
Here, n is the integer which shows the number of repetition units of polyethylene glycol,
The direct condition molecule is polyethylene glycol, the quantity of .alpha.-shikurodekisutorin is the 20-40, the end group consists of the adamantan basis, the disassembly characteristic basis 2 - the porirotakisan chemical compound which is the nitro benzyl basis.
[claim13]
13. It possesses the below-mentioned structural formula, .alpha.-shikurodekisutorin which the metakuriroiru basis and the buchiruisoshianato basis connect being the porirotakisan chemical compound which includes the direct condition molecule,
Here, n is the integer which shows the number of repetition units of polyethylene glycol,
Per .alpha.-shikurodekisutorin 1 molecule the 1-10 the metakuriroiru basis and the 5-20 it possesses the buchiruisoshianato basis, the direct condition molecule is polyethylene glycol, the quantity of .alpha.-shikurodekisutorin is the 20-40, the end group consists of the adamantan basis, the disassembly characteristic basis 2 - the porirotakisan chemical compound which is the nitro benzyl basis.
[claim14]
14. The plural annular molecules and, it includes with one linear macromolecule which possesses the end group, said linear macromolecule through one disassembly characteristic part at least, it includes two which is connected linear high-molecular parts at least, porirotakisan chemical compound is contained, the composition for gluing.
[claim15]
15. The plural annular molecules and, it includes with one linear macromolecule which possesses the end group, said linear macromolecule through one disassembly characteristic part at least, it includes two which is connected linear high-molecular parts at least, porirotakisan chemical compound is contained, the dentistry material composition.
[claim16]
16. The plural annular molecules and, it includes with one linear macromolecule which possesses the end group, said linear macromolecule through one disassembly characteristic part at least, it includes two which is connected linear high-molecular parts at least, porirotakisan chemical compound is contained, the surface coating medicine.
[claim17]
17. The plural annular molecules and, it includes with one linear macromolecule which possesses the end group, said linear macromolecule through one disassembly characteristic part at least, it includes two which is connected linear high-molecular parts at least, porirotakisan chemical compound is contained, the adhesion inhibiter.
[claim18]
18. The plural annular molecules and, it includes with one linear macromolecule which possesses the end group, said linear macromolecule through one disassembly characteristic part at least, it includes two which is connected linear high-molecular parts at least, porirotakisan chemical compound is contained, the internal burying planting medicine.
[claim19]
19. The plural annular molecules and, it includes with one linear macromolecule which possesses the end group, said linear macromolecule through one disassembly characteristic part at least, it includes two which is connected linear high-molecular parts at least, porirotakisan chemical compound is contained, the organizational playback equipment.
[claim20]
20. The plural annular molecules and, it includes with one linear macromolecule which possesses the end group, said linear macromolecule through one disassembly characteristic part at least, it includes two which is connected linear high-molecular parts at least, the medicine composition in order contains porirotakisan chemical compound, to use for the remedy or prevention of the disease.
[claim21]
21. Claim 12 or the porirotakisan chemical compound of statement is contained in claim 13, the composition and the dentistry material composition for gluing, the surface coating medicine, the adhesion inhibiter and the internal burying planting medicine, the medicine composition in order to use for the organizational playback equipment, or the remedy or prevention of the disease.
[claim22]
22. The plural annular molecules and, it includes with one linear macromolecule which possesses the end group, said linear macromolecule through one disassembly characteristic part at least, it includes two which is connected linear high-molecular parts at least, being production method of porirotakisan chemical compound, a) process and b which add the reactivity basis to both ends of the linear high-molecular part) the linear high-molecular part which adds the reactivity basis to both ends through the disassembly characteristic part, making connect, through one disassembly characteristic part at least, the process which obtains the linear macromolecule which at least includes two which is connected linear high-molecular parts, c) linear macromolecule it reacts with the annular moleculeBeing able to point, process, and d which obtain pseudo porirotakisan) it includes the process which adds the end group to both ends of pseudo porirotakisan, production method.
[claim23]
23. The reactivity basis which is added to both ends of the linear high-molecular part, is selected from the group which consists of the amino group, the carboxyl group, the aldehyde basis, the sulfanilic basis, the azide basis, the arukiniru basis, the toshiru basis, and the active ester basis, production method of claim 22 statement.
[claim24]
24. Claim 12 or being production method of the porirotakisan chemical compound of statement in claim 13, a) process and b which add the reactivity basis to both ends of the linear high-molecular part) the linear high-molecular part which adds the reactivity basis to both ends through the disassembly characteristic part, making connect, through one disassembly characteristic part at least, the process which obtains the linear macromolecule which at least includes two which is connected linear high-molecular parts, reacting c) linear macromolecule with the annular molecule, process, and d which obtain pseudo porirotakisan) it includes the process which adds the end group to both ends of pseudo porirotakisan, production method.
[claim25]
25. The reactivity basis which is added to both ends of the linear high-molecular part, is selected from the group which consists of the amino group, the carboxyl group, the aldehyde basis, the sulfanilic basis, the azide basis, the arukiniru basis, the toshiru basis, and the active ester basis, production method of claim 24 statement.
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • TOKYO MEDICAL AND DENTAL UNIVERSITY
  • Inventor
  • YUI NOBUHIKO
  • TAMURA ATSUSHI
  • ARISAKA YOSHINORI
  • FUSHIMI MAYU
IPC(International Patent Classification)
Specified countries (WO2017191827)
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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