Abstract: The present application provides novel tetrahydro-isohumulone (THIAA) derivatives and substantially enantiomerically pure compositions and pharmaceutical formulations thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPAR?, inhibit inflammation, and treat conditions associated with inflammation and conditions responsive to PPAR? modulation such as diabetes.
Type:
Grant
Filed:
November 27, 2017
Date of Patent:
July 9, 2019
Assignee:
KINDEX PHARMACEUTICALS, INC.
Inventors:
Veera Konda, Jan Urban, Anuradha Desai, Clinton J. Dahlberg, Brian J. Carroll
Abstract: The present application provides novel tetrahydro-isohumulone (THIAA) derivatives and substantially enantiomerically pure compositions and pharmaceutical formulations thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPAR?, inhibit inflammation, and treat conditions associated with inflammation and conditions responsive to PPAR? modulation such as diabetes.
Type:
Grant
Filed:
January 9, 2015
Date of Patent:
November 28, 2017
Assignee:
KINDEX PHARMACEUTICALS, INC.
Inventors:
Veera Konda, Jan Urban, Anuradha Desai, Clinton J. Dahlberg, Brian J. Carroll
Abstract: Methods of synthesizing a cis 3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one (“KDT500”) derivative are provided. Such methods may be used to synthesize any desired KDT derivative. In one embodiment, the KDT500 derivative is KDT501.
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 18, 2013
Date of Patent:
September 9, 2014
Assignee:
Kindex Pharmaceuticals, Inc.
Inventors:
Brian J. Carroll, Gary Darland, Anuradha Desai, Veera Konda, Clinton J. Dahlberg, Jan Urban