首页> 外国专利> An amphipathic polyamino acid, a block copolymer using the amphipathic polyamino acid, and a complex containing the amphipathic polyamino acid or the block copolymer and nucleic acid.

An amphipathic polyamino acid, a block copolymer using the amphipathic polyamino acid, and a complex containing the amphipathic polyamino acid or the block copolymer and nucleic acid.

机译:使用两亲多氨基酸的嵌段共聚物,以及含有两性聚氨基酸或嵌段共聚物和核酸的复合物。

摘要

According to the present invention, an amphipathic polyamino acid for nucleic acid delivery represented by the following formula (1) is provided.(During the ceremony, R 1 represents a hydroxyl group, an oxybenzyl group, an -O-R 1a group or an -NH-R 1b group, where R 1a and R 1b are independently unsubstituted or substituted linear or branched. Represents an alkyl group having 1 to 12 carbon atoms. R 2 is a hydrogen atom, an unsubstituted or substituted linear or branched alkyl group having 1 to 12 carbon atoms, or an unsubstituted or substituted linear or branched alkyl carbonyl group having 1 to 24 carbon atoms. Represent, R 3a , R 3b , R 4a and R 4b independently represent a methylene group or an ethylene group. R 5a and R 5b represent -O- or -NH- independently of each other. R 6a and R 6b represent unsubstituted or substituted aliphatic hydrocarbon groups having 7 to 12 carbon atoms, which may contain an alicyclic independently of each other. R 7a and R 7b are independent of each other and have the following groups: -NH- (CH 2 ) p1- [NH- (CH 2 ) q1- ] r1 NH 2 (i); −NH − (CH 2 ) p2 −N [− (CH 2 ) q2 −NH 2 ] 2 (ii); -NH- (CH2) p3 -N {[-(CH 2) q3 -NH 2][-(CH 2) q4 -NH-] r2 H} (iii); and -NH- (CH2) p4 - N {-(CH 2 ) q5- N [-(CH 2 ) q6 -NH 2 ] 2 } 2 (iv) Selected from the same or different groups of groups consisting of Here, p1 to p4, q1 to q6, and r1 to 2 are integers of 1 to 5 independently of each other. R 8 represents ornithine, lysine, homolysine, arginine, a side chain of an amino acid selected from the group consisting of homo arginine and histidine, m is an integer of 9 or more, n is an integer from 0 to m. x is an integer of 2 to 300 and y is an integer from 0 to x z is an integer from 0 to x However, the relation of y + z ≦ x and the relation of 11 ≦ m + x ≦ 400 are satisfied, and each repeating unit in the above formula (1) can exist at random. )
机译:根据本发明,提供了由下式(1)表示的核酸输送的两亲性聚氨基酸。(在仪式期间,R 1表示羟基,氧苄基,-OR 1A组或-NH -R 1b组,其中R 1a和R 1b独立地未取代或取代的线性或支链。表示具有1至12个碳原子的烷基。R 2是氢原子,未取代的或取代的直链或具有1的支链烷基。 12个碳原子,或具有1-24个碳原子的未取代或取代的直链或支链烷基羰基。表示,R 3a,R 3b,R 4a和R 4b独立地表示亚甲基或乙烯。R 5a和R 5b彼此独立地表示-O-或-NH-。R 6a和R 6b表示具有7-12个碳原子的未取代的或取代的脂族烃基,其可以彼此独立地含有脂环族。R 7a和R 7b与每个OT她并具有以下组:-NH-(CH 2)P1- [NH-(CH 2)Q1-] R1 NH 2(i); -NH - (CH 2)P2-N [ - (CH 2)Q2-N-N 2] 2(ii); -NH-(CH2)P3-N {[ - (CH 2)Q3-N-NH 2] [ - (CH 2)Q4-NH-] R2 H}(III); - -NH-(CH2)P4 - N - N - ( - (CH 2)Q5-N [ - (CH 2)Q6-N-NH 2] 2} 2(IV)选自本文组成的相同或不同组组P1 P4,Q1至Q6和R1至2是彼此独立地为1至5的整数。 R 8代表鸟氨酸,赖氨酸,均溶胶,精氨酸,选自HOMO精氨酸和组氨酸中选择的氨基酸的侧链,M是9或更多的整数,N是0至m的整数。 x是2到300的整数,Y为0到XZ的整数是从0到x的整数,但是,满足Y +z≤x的关系和11≤m+x≤400的关系上式(1)中的重复单元可以随机存在。的)

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