Abstract: The present invention relates to processes for the preparation of (R)-1-(5-chloro-[1,1?-biphenyl]-2-yl)-2,2,2-trifluoroethanol, 1-(5-chloro-[1,1?-biphenyl]-2-yl)-2,2,2-trifluoroethanone, and intermediates thereof, which are useful in the preparation of inhibitors of TPH1 for the treatment of, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, low bone mass diseases, serotonin syndrome, and cancer.
Type:
Grant
Filed:
March 3, 2016
Date of Patent:
April 4, 2017
Assignee:
Karos Pharmaceuticals, Inc.
Inventors:
Stéphane De Lombaert, Daniel R. Goldberg
Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
Type:
Grant
Filed:
September 1, 2015
Date of Patent:
December 6, 2016
Assignee:
Karos Pharmaceuticals, Inc.
Inventors:
Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
Type:
Grant
Filed:
September 5, 2014
Date of Patent:
December 1, 2015
Assignee:
Karos Pharmaceuticals, Inc.
Inventors:
Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren