Invention Grant
US08410178B2 CIS 3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-derivatives, substantially enantiomerically pure compositions and methods
有权
CIS 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-derivatives, substantially enantiomerically pure compositions and methods
- Patent Title (中): CIS 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.: US13284852Application Date: 2011-10-28
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Publication No.: US08410178B2Publication Date: 2013-04-02
- Inventor: Brian J. Carroll , Gary Darland , Anuradha Desai , Veera Konda , Clinton J. Dahlberg , Jan Urban
- Applicant: Brian J. Carroll , Gary Darland , Anuradha Desai , Veera Konda , Clinton J. Dahlberg , Jan Urban
- Applicant Address: US WA Seattle
- Assignee: KinDex Therapeutics, LLC
- Current Assignee: KinDex Therapeutics, LLC
- Current Assignee Address: US WA Seattle
- Agency: Perkins Coie LLP
- Agent Patrick D. Morris
- Main IPC: A61K31/12
- IPC: A61K31/12 ; 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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