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POLYION COMPLEX OF POLY(L-ARGININE) SEGMENT-CONTAINING BLOCK COPOLYMER AND POLYANIONIC POLYMER

外国特許コード F170008918
整理番号 (S2015-0978-N0)
掲載日 2017年1月13日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2016JP062062
国際公開番号 WO 2016167333
国際出願日 平成28年4月15日(2016.4.15)
国際公開日 平成28年10月20日(2016.10.20)
優先権データ
  • 特願2015-083987 (2015.4.16) JP
発明の名称 (英語) POLYION COMPLEX OF POLY(L-ARGININE) SEGMENT-CONTAINING BLOCK COPOLYMER AND POLYANIONIC POLYMER
発明の概要(英語) [Problem] To provide a composition that can become an effective arginine matrix for intratumoral inducible NO synthase (iNOS). [Solution] A polyion complex (PIC) of PEG-b-poly(L-Arg) or poly(L-Arg)-b-PEG-b-poly(L-Arg) and a polyanionic polymer, and the use of the complex.
特許請求の範囲(英語) [claim1]
1. Including the poly- cation characteristic polymer and the poly- anionic characteristic polymer, the poly- ion complex which becomes (PIC) being,
Poly- cation characteristic polymer, formula (i)
In formula,
As for A,
(i) Hydrogen, non substitution or substitution C [1] - you display C [12] alkyl group, the formyl basis, formula R (1) R (2) CH- (here, R (1) and R (2) becoming independent, C [1] - C [4] alkoxy or R (1) and as for R (2) becoming simultaneous, - OCH [2] CH [2] O-, - O (CH [2]) [3] [O]-MOSHIKUHA-O (CH [2]) [4] [O]-wo you display the substituent when it is substituted.)The basis is displayed or, or
(ii) Formula
Displaying,
L and as for L' becoming independent, displaying the connected basis
Y and the group where, Y' becoming independent, H, C [1-21] alkyl carbonyl and substitution C [1-4] alkyl carbonyl, non substitution or substitution C [3-7] [shikuroarukirukaruboniru], non substitution or substitution aryl carbonyl, or non substitution or substitution displays 5 or 6 member hetero aryl carbonyl, here, as for the substituent of substitution C [1-4] alkyl carbonyl, the halogen atom, hydroxyl, carboxyl, non substitution or substitution C [3-7] [shikuroarukiru], non substitution or substitution aryl and non substitution or substitution 5 or 6 member hetero aryls, non substitution or substitution [adamanchiru], consists of the non substitution or substitution cholesterol residueFrom to be chosen, the substituent when these substituents are substituted C [1-4] alkyl and C [1-4] alkyl oxy, hydroxyl, carboxyl and cyano, nitro, the halogen atom, or mono - or to be able be [ji] C [1-4] alkyl amino,
m and m' becoming independent, is integer of the 5-300,
n is integer of the 5-1,000,
M in formula or m' [amijino] basis (C (=NH) NH [2]) it is possible to be H up to 80%,
So it is the copolymer which is shown,
The poly- anionic characteristic polymer the poly- anionic characteristic polysaccharide, the poly- anionic characteristic polypeptide, poly- (acrylic acid), and poly- (meta acrylic acid) to be chosen from the group which consists of, at the same time,
The description above PIC when making melt or making water disperse, or, mean diameter nano- meter (nm) is a form of the PIC micelle of order,
The aforementioned poly- ion complex.
[claim2]
2. Being the poly- ion complex of statement in claim 1, A is defined with (i), the poly- ion complex.
[claim3]
3. Being the poly- ion complex of statement in claim 1, A is defined with (ii), the poly- ion complex.
[claim4]
4. Either of the claim 1-3 it includes the poly- ion complex of statement in 1 as the active ingredient in mammal organizing, the composition in order to offer the substrate L-Arg of the induction type NO synthetase which is derived from the cell which is activated.
[claim5]
5. In mammal organizing, the cell which is activated as for the tumor organizational inner thigh is the adjacent macrophage, in claim 4 the composition of statement.
[claim6]
6. In mammal organizing, the cell which is activated it is the macrophage which is activated attendant upon the inflammation inside the heart muscle, in claim 4 the composition of statement.
[claim7]
7. The composition in order it prevents or to remedy the tumor which either of the claim 1-3 includes the poly- ion complex of statement in 1 in mammal organizing as the active ingredient.
[claim8]
8. Formula (i)
In formula,
As for A,
(i) Hydrogen, non substitution or substitution C [1] - you display C [12] alkyl group, the formyl basis, formula R (1) R (2) CH- (here, R (1) and R (2) becoming independent, C [1] - C [4] alkoxy or R (1) and as for R (2) becoming simultaneous, - OCH [2] CH [2] O-, - O (CH [2]) [3] [O]-MOSHIKUHA-O (CH [2]) [4] [O]-wo you display the substituent when it is substituted.)The basis is displayed or, or
(ii) Formula
Displaying,
L and as for L' becoming independent, displaying the connected basis
Y and the group where, Y' becoming independent, H, C [1-21] alkyl carbonyl and substitution C [1-4] alkyl carbonyl, non substitution or substitution C [3-7] [shikuroarukirukaruboniru], non substitution or substitution aryl carbonyl, or non substitution or substitution displays 5 or 6 member hetero aryl carbonyl, here, as for the substituent of substitution C [1-4] alkyl carbonyl, the halogen atom, hydroxyl, carboxyl, non substitution or substitution C [3-7] [shikuroarukiru], non substitution or substitution aryl and non substitution or substitution 5 or 6 member hetero aryls, non substitution or substitution [adamanchiru], consists of the non substitution or substitution cholesterol residueFrom to be chosen, the substituent when these substituents are substituted C [1-4] alkyl and C [1-4] alkyl oxy, hydroxyl, carboxyl and cyano, nitro, the halogen atom, or mono - or to be able be [ji] C [1-4] alkyl amino,
m and m' becoming independent, is integer of the 5-300,
n is integer of the 5-1,000,
M in formula or m' [amijino] basis (C (=NH) NH [2]) it is possible to be H up to 80%,
So being production method of the block copolymer which is shown,
Formula (ii)
In formula,
As for A,
(i) As defined' concerning (i) above-mentioned formula (i) is or, or,
(ii)' Formula
Displaying,
L, L', Y, Y' and n, m and m' is as defined concerning above-mentioned formula (i),
Reacting in the reaction non active solvent so N and N' - bis ([tert]-butokishikaruboniru) - *** H-pirazoru - 1 - [karubokisamijin], on the block copolymer which is shown in accordance with necessary, including the process which to guanidinoacetic it converts, ***.delta.-amino in the segment which is derived from ornithine it becomes, method.
[claim9]
9. Being production method of the block copolymer of statement in claim 8, A formula (ii) is defined with (i)', method.
[claim10]
10. Being production method of the block copolymer of statement in claim 8, A formula (ii) is defined with (ii), method.
[claim11]
11. Formula (iii)
In formula,
L and as for L' becoming independent, displaying the connected basis
Y and the group where, Y' becoming independent, H, C [1-21] alkyl carbonyl and substitution C [1-4] alkyl carbonyl, non substitution or substitution C [3-7] [shikuroarukirukaruboniru], non substitution or substitution aryl carbonyl, or non substitution or substitution displays 5 or 6 member hetero aryl carbonyl, here, as for the substituent of substitution C [1-4] alkyl carbonyl, the halogen atom, hydroxyl, carboxyl, non substitution or substitution C [3-7] [shikuroarukiru], non substitution or substitution aryl and non substitution or substitution 5 or 6 member hetero aryls, non substitution or substitution [adamanchiru], consists of the non substitution or substitution cholesterol residueFrom to be chosen, the substituent when these substituents are substituted C [1-4] alkyl and C [1-4] alkyl oxy, hydroxyl, carboxyl and cyano, nitro, the halogen atom, or mono - or to be able be [ji] C [1-4] alkyl amino,
m and m' becoming independent, is integer of the 5-300,
n is integer of the 5-1,000,
M in formula or m' [amijino] basis (C (=NH) NH [2]) it is possible to be H up to 80%,
So the copolymer which is shown.
  • 出願人(英語)
  • ※2012年7月以前掲載分については米国以外のすべての指定国
  • UNIVERSITY OF TSUKUBA
  • 発明者(英語)
  • NAGASAKI YUKIO
  • KUDO SHINPEI
  • HIRAMATSU YUJI
  • SAKAMOTO HIROAKI
  • BUI QUOC THANG
  • VONG BINH LONG
国際特許分類(IPC)
指定国 (WO2016167333)
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 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 KN KP KR 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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