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DIPEPTIDE-related MEDICINES
专利权人:
ИНДИАНА ЮНИВЕРСИТИ РИСЕРЧ ЭНД ТЕКНОЛОДЖИ КОРПОРЕЙШН (US)
发明人:
ДИМАРЧИ Ричард Д. (US)
申请号:
RU2013102991/04
公开号:
RU2013102991A
申请日:
2011.06.09
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
1. A prodrug comprising the structure: ABQ; where Q is a bioactive peptide; where AB comprises the structure: where (I) R and R are independently selected from the group consisting of H, C-C1-6 alkyl, C-C1-6 alkenyl, (C-C1-6 alkyl) OH, (C-Ci-alkyl) SH, (C-Ci-alkyl) SCH, (C-Ci-alkyl) CONH, (C-Ci-alkyl) COOH, (C-Ci-alkyl) NH, (C-Ci-alkyl) NHC (NH) NH, (C -Calkyl) (C-Cycloalkyl), (C-Ci -alkyl) (C-Ceterocyclic radical), (C-Ci -alkyl) (C-Caryl) R, (C-Ci-alkyl) (C-Ci-heteroaryl) and C-Ci-alkyl (W) C-C 1-6 alkyl, where W is a heteroatom selected from the group consisting of N, S and O, or R and R, together with the atoms to which they are attached, form C-C cycloalkyl; R is C-Calkyl; each R and R is H; R is NHR or R and R, together with the atoms to which they are attached, form a 4-, 5- or 6-membered heterocyclic ring; R is H or C-Ci-alkyl ; and R is selected from the group consisting of H and OH; wherein AB is linked to Q via an amide bond between AB and the aliphatic amino group Q; and the half-life of chemical cleavage of (t) AB from Q is at least about 1 hour - about 1 week in PBS under physiological conditions; provided that when both R and R are H, R is C-Calkyl; (II) R and R are independently selected from the group consisting of H, C-Calkyl, C-Calkenyl, (C- C1-6alkyl) OH, (C1-6alkyl) SH, (C1-6alkyl) SCH, (C1-6alkyl) CONH, (C1-6alkyl) COOH, (C1-6alkyl) NH, (C1-6alkyl) NHC (NH) NH, (C-Alkyl) (C-Cycloalkyl), (C-Alkyl k) (C-C heterocyclic radical), (C-Ci-alkyl) (C-Caryl) R, (C-Ci-alkyl) (C-Ci-heteroaryl) and C-Ci-alkyl (W) C-Ci-alkyl, where W is a heteroatom selected from the group consisting of N, S and O, or R and R together with the atoms to which they are attached form C-Cycloalkyl; R is C-Calkyl; R is selected from the group consisting of �1. Пролекарство, включающее структуру:A-B-Q;где Q представляет собой биоактивный пептид;где А-В включает структуру:где(I) Rи Rнезависимо выбирают из группы, состоящей из Н, C-Cалкила, C-Cалкенила, (C-Cалкил)ОН, (C-Cалкил)SH, (С
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