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PEPTIDOMIMETIC MACROCYCLES
专利权人:
ЭЙЛЕРОН ТЕРАПЬЮТИКС; ИНК. (US)
发明人:
КАВАХАТА Нориюки (US),ГЕРЛАВЭ Венсан (US),САМАНТ Манодж (US)
申请号:
RU2014119673/10
公开号:
RU2014119673A
申请日:
2012.10.18
申请国别(地区):
RU
年份:
2015
代理人:
摘要:
1. A peptidomimetic macrocycle containing: an amino acid sequence identical to at least about 60% GHRH 1-29, and at least two macrocycle-forming linkers, the first of the two macrocyclic-forming linkers connecting the first amino acid to the second amino acid, and the second of these two macrocyclic-forming linkers connects the third amino acid with the fourth amino acid. 2. The peptidomimetic macrocycle of claim 1, containing exactly two macrocycle-forming linkers. 3. The peptidomimetic macrocycle of claim 1, wherein each of the specified macrocycle-forming linkers connects one of the following pairs of amino acids: 4 and 8; 5 and 12; 8 and 12; 8 and 15; 9 and 16; 12 and 16; 12 and 19; 15 and 22; 18 and 25; 21 and 25; 21 and 28; 22 and 29; and 25 and 29.4. The peptidomimetic macrocycle of claim 3, wherein each of said macrocycle-forming linkers combines the following pairs of amino acids: 4 and 8; 5 and 12; 12 and 19; 15 and 22; 18 and 25; 21 and 25; and 21 and 28.5. The peptidomimetic macrocycle of claim 3, wherein the first macrocycle-forming linker connects amino acid pairs 4 and 8; 5 and 12; 8 and 12; 8 and 15; 9 and 16; 12 and 16; or 12 and 19; and the second macrocycle-forming linker connects the amino acid pairs 15 and 22; 18 and 25; 21 and 25; 21 and 28; 22 and 29; or 25 and 29.6. The peptidomimetic macrocycle of claim 3, wherein the first macrocycle-forming linker connects amino acid pairs 4 and 8; 5 and 12; or 12 and 19; and the second macrocycle-forming linker connects the amino acid pairs 15 and 22; 18 and 25; 21 and 25; or 21 and 28.7. The peptidomimetic macrocycle of claim 3, wherein the first macrocycle-forming linker connects amino acid pairs 4 and 8, and the second macrocycle-forming linker connects amino acid pairs 21 and 25.8. Peptidomimetic macrocycle containing am1. Пептидомиметический макроцикл, содержащий:аминокислотную последовательность, идентичную по меньшей мере приблизительно на 60% GHRH 1-29, ипо меньшей мере два макроцикл-образующих ли
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