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Propylene oligoribose copolymer
专利权人:
SAREPTA THERAPEUTICS; INC.
发明人:
SAREPTA THERAPEUTICS, INC.
申请号:
ARP160103839
公开号:
AR107220A1
申请日:
2016.12.15
申请国别(地区):
AR
年份:
2018
代理人:
摘要:
Claim 1: A peptide-oligomer conjugate of formula (1) or a pharmaceutically acceptable salt thereof, wherein R³ is selected from OH, -N (H) CH₂C (O) NH₂,-N (c832131-8326262 tar) ch8322; C (o) n8322;1. A formula compound (2) and a formula compound (3);R⁵ is -C (O) (O-alkyl) ˣOH, where x is 3-10 and each alkyl group is, independently in each case, C₂₋₆-alkyl, or R⁵ is selected from the group consisting of -C ( O) C₁₋₆-alkyl, trityl, monomethoxytrityl, - (C₁₋₆-alkyl) R⁶,-(c83218331-832626-heterogeneous) - r8310a;aril-R⁶,Infidel r8310a,-C (O) O- (C -alquil) -R-C (O) O-aril-R-C (o) o-heteromorphic-r8310 and R1;R8310 is selected from Oh, SH and n832222;O r8310es o, s or NH, proportional to a solid support; R1 is a separate oh-nr8311; R12 o-nr8311; r831222;each R⁷ and R⁸ is, independently in each case, H or -C₁₋₆-alkyl; R² is selected, independently in each case, from the group consisting of H, a nucleobase and a nucleobase functionalized with a protective chemical group, where the nucleobase, independently in each case, comprises a C₃₋₆ heterocyclic ring selected from pyridine, pyrimidine, triazinan, purine and deaza-purine; z is 8-40; R⁴ is selected from H, -C₁₋₆-alkyl, -C (O) C₁₋₆-alkyl, benzyl, stearyl, trityl, monomethoxytrityl, dimethoxytrityl, trimethoxytrityl, a compound of formula (4) and R²;R es -C (O) (CH) C (O) - o -C (O) (CH) S (CH) C (O) -R es - (CH) OC (O) N ((CH) N (H) C (3DNH) NH)R1 was selected from Oh y-nr8311; r831222;R2. Select from the group consisting of formula group (5);N is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10; P is 2, 3, 4 or 5; R 1 cube is a link or is selected from the formula group (6);R¹⁵ and R¹⁹ are selected, independently in each case, from the group consisting of H, -C₁₋₄-alkyl, -CH (-C₁₋₄-alkyl) ₂ and - (CH₂) ₃NH-C (= NH) -NH₂ ;T and W are 2, 3, 4 or 5, respectively; r830808 is selected from the formula group (7);R¹⁷ is H or -C₁₋₄-alkyl; R²⁰ is selected from the group consisting of H, -C₁₋₄-alkyl, -CH (-C₁₋₄-alkyl) ₂ and - (CH₂) ₃NH-C (= NH) -N
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