CIS 3,4-DIHYDROXY-2-(3-METHYLBUTANOYL)-5-(3-METHYLBUTYL)-4-(4-METHYLPENTANOYL)CYCLOPENT-2-EN-1-ONE DERIVATIVES, SUBSTANTIALLY ENANTIOMERICALLY PURE COMPOSITIONS AND METHODS
CARROLL BRIAN,캐롤, 브라이언,DARLAND GARY,달랜드, 게리,DESAI ANURADHA,데사이, 아누라다,KONDA VEERA,콘다, 베라,DAHLBERG CLINTON J.,달버그, 클린턴, 제이.,URBAN JAN,어번, 잔
申请号：
KR1020137013796
公开号：
KR1020140027910A
申请日:
2011.10.28
申请国别(地区):
KR
年份:
2014
代理人:
摘要：
The present application provides cis 3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one derivatives and substantially enantiomerically pure compositions thereof. These derivatives include (+)-(4S,5R)-3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one, (&minus；)-(4R,5S)-3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one, and salts and crystals thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPAR&gamma；, activate GPR120, inhibit inflammation, and treat conditions responsive to PPAR&gamma； modulation, conditions responsive to GPR120 modulation, and metabolic disturbances such as diabetes.본 출원은 시스 3,4-디히드록시-2-(3-메틸부타노일)-5-(3-메틸부틸)-4-(4-메틸펜타노일)시클로펜트-2-엔-1-온 유도체 및 그의 실질적으로 거울상이성질체적으로 순수한 조성물을 제공한다. 이들 유도체에는 (+)-(4S,5R)-3,4-디히드록시-2-(3-메틸부타노일)-5-(3-메틸부틸)-4-(4-메틸펜타노일)시클로펜트-2-엔-1-온, (-)-(4R,5S)-3,4-디히드록시-2-(3-메틸부타노일)-5-(3-메틸부틸)-4-(4-메틸펜타노일)시클로펜트-2-엔-1-온, 및 이들의 염 및 결정이 포함된다. 추가적으로, 본 출원은 개시된 화합물 및 조성물을 사용하여 PPARγ을 활성화시키고, GPR120을 활성화시키고, 염증을 억제하고, PPARγ 조절에 대해 반응하는 병태, GPR120 조절에 대해 반응하는 병태 및 대사 장애, 예컨대 당뇨병을 치료하기 위한 방법을 제공한다.
