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CHIRAL DIACYLHYDRAZINE LIGANDS FOR MODULATION OF EXPRESSION OF EXOGENOUS GENES USING THE EXDISON RECEPTOR COMPLEX
专利权人:
Интрексон Корпорейшн (US)
发明人:
ХОРМАНН Роберт И. (US),ЛИ Бинг (US)
申请号:
RU2013121780/04
公开号:
RU2013121780A
申请日:
2013.05.06
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
1. The enantiomerically enriched compound of Formula II where A is (C-C) alkyl-O-, phenyl- (C-C) alkyl-O-; aryl selected from phenyl, naphthyl, and which is optionally substituted with 1-3 substituents, where the substituents are selected from (C-C) alkyl, (C-C) cycloalkyl, (C-C) alkyl-O-, hydroxy, amino and halogen; or heteroaryl having four or five carbon atoms and one heteroatom selected from oxygen, nitrogen and sulfur, which is optionally substituted with 1-3 substituents, where the substituents are selected from (CC) alkyl, (CC) cycloalkyl, (CC) alkyl-O- , hydroxy, amino and halogen; B is phenyl optionally substituted with 1-3 substituents, where the substituents are selected from (CC) alkyl, (CC) cycloalkyl, (CC) alkyl-O-, hydroxy, amino and halo; and R and R independently represent (CC) alkyl, phenyl- (CC) alkyl, hydroxy- (CC) alkyl, (CC) cycloalkyl, (CC) alkenyl or (CC) alkynyl; provided that R differs from R; where the absolute configuration the asymmetric carbon atom bearing R and R is preferably the S configuration; or a pharmaceutically acceptable salt thereof. 2. The compound according to claim 1, where A represents-OS (CH), -OCHPh; aryl selected from phenyl, naphthyl, and which is optionally substituted with 1-3 substituents, where the substituents are selected from (C-C) alkyl, (C-C) cycloalkyl, (C-C) alkyl-O-, hydroxy, amino and halogen; or heteroaryl having four or five carbon atoms and one heteroatom selected from oxygen, nitrogen and sulfur, which is optionally substituted with 1-3 substituents, where the substituents are selected from (CC) alkyl, (CC) cycloalkyl, (CC) alkyl-O- , hydroxy, amino and halogen; B is phenyl, optionally substituted with 1-3 substituents, where the substituents are selected from (CC) alkyl, (CC) alkyl-O- and halogen; R is (CC) alkyl, hydroxy (CC) alkyl or (CC) al1. Энантиомерно обогащенное соединение Формулы IIгдеA представляет собой (C-C)алкил-O-, фенил-(C-C)алкил-O-; арил, выбранный из фенила, нафтила,и, который возмо
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