Invention Grant
US08829056B2 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
有权
顺式3,4-二羟基-2-(3-甲基丁酰基)-5-(3-甲基丁基)-4-(4-甲基戊酰基)环戊-2-烯-1-酮衍生物,基本上对映体纯的组合物和方法
- Patent Title: 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
- Patent Title (中): 顺式3,4-二羟基-2-(3-甲基丁酰基)-5-(3-甲基丁基)-4-(4-甲基戊酰基)环戊-2-烯-1-酮衍生物,基本上对映体纯的组合物和方法
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Application No.: US13846790Application Date: 2013-03-18
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Publication No.: US08829056B2Publication Date: 2014-09-09
- Inventor: Brian J. Carroll , Gary Darland , Anuradha Desai , Veera Konda , Clinton J. Dahlberg , Jan Urban
- Applicant: Kindex Pharmaceuticals, Inc.
- Applicant Address: US WA Seattle
- Assignee: Kindex Pharmaceuticals, Inc.
- Current Assignee: Kindex Pharmaceuticals, Inc.
- Current Assignee Address: US WA Seattle
- Agency: Perkins Coie LLP
- Agent Patrick D. Morris
- Main IPC: A61K31/12
- IPC: A61K31/12 ; A61K31/122 ; C07C49/707 ; C07C49/00

Abstract:
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, (−)-(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 PPARγ, activate GPR120, inhibit inflammation, and treat conditions responsive to PPARγ modulation, conditions responsive to GPR120 modulation, and metabolic disturbances such as diabetes.
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