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:
April 16, 2020
Date of Patent:
March 16, 2021
Assignee:
Roivant Sciences GmbH
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:
Application
Filed:
April 16, 2020
Publication date:
July 30, 2020
Applicant:
Roivant Sciences GmbH
Inventors:
Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
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:
August 21, 2019
Date of Patent:
July 14, 2020
Assignee:
Roivant Sciences GmbH
Inventors:
Stéphane De Lombaert, Daniel R. Goldberg
Abstract: There is a crystalline compound of (S)-ethyl 8-(2-amino-6-((R)-1-(5-chloro-[1,1?-biphenyl]-2-yl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)-2,8-diazaspiro[4.5]decane-3-carboxylate that exhibits an XRPD pattern having a characteristic peak at 19.05±0.20 (° 2?). There is also a pharmaceutical composition containing the compound. There is also a dosage form containing the crystalline compound and one or more pharmaceutically acceptable excipients. There is also a method for crystallizing/recrystallizing the compound. There is also a method for treating or preventing a disease with the compound.
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:
Application
Filed:
August 21, 2019
Publication date:
December 12, 2019
Applicant:
Roivant Sciences GmbH
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:
May 14, 2018
Date of Patent:
July 16, 2019
Assignee:
Roivant Sciences GmbH
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:
July 10, 2017
Date of Patent:
August 14, 2018
Assignee:
Roivant Sciences GmbH
Inventors:
Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner