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 PPAR?, activate GPR120, inhibit inflammation, and treat conditions responsive to PPAR? modulation, conditions responsive to GPR120 modulation, and metabolic disturbances such as diabetes.
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 PPAR?, activate GPR120, inhibit inflammation, and treat conditions responsive to PPAR? modulation, conditions responsive to GPR120 modulation, and metabolic disturbances such as diabetes.
Type:
Grant
Filed:
March 14, 2012
Date of Patent:
April 2, 2013
Assignee:
KinDex Therapeutics, LLC
Inventors:
Brian J. Carroll, Gary Darland, Anuradha Desai, Veera Konda, Clinton J. Dahlberg, Jan Urban
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 PPAR?, activate GPR120, inhibit inflammation, and treat conditions responsive to PPAR? modulation, conditions responsive to GPR120 modulation, and metabolic disturbances such as diabetes.
Type:
Grant
Filed:
October 28, 2011
Date of Patent:
April 2, 2013
Assignee:
KinDex Therapeutics, LLC
Inventors:
Brian J. Carroll, Gary Darland, Anuradha Desai, Veera Konda, Clinton J. Dahlberg, Jan Urban