IP Library Granted Patent US 10,660,893
Granted Patent B2
US 10,660,893 · App. 16/426,698 · Granted May 26, 2020

Spirocyclic compounds as tryptophan hydroxylase inhibitors

Inventors: Stéphane De Lombaert (Brisbane, CA); Daniel R. Goldberg (Seattle, WA); Kenneth Brameld (Menlo Park, CA); Eric Brian Sjogren (Mountain View, CA); Andrew Scribner (Durham, NC)
Assignee: ROIVANT SCIENCES, GmbH
A61K31/506A61K9/0014A61K9/0019A61K9/0053A61K9/0078C07D471/10C07D519/00
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Quick Facts
Patent No.
US 10,660,893
App. No.
16/426,698
Granted
May 26, 2020
Kind
B2
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.

Claims (18)

1. A method of treating idiopathic pulmonary arterial hypertension in a patient, comprising administering to the patient a therapeutically effective amount 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 or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein administration is by inhalation.

3. The method of claim 2 , wherein inhalation is with a powder.

4. The method of claim 2 , wherein inhalation is with a spray or an aerosol.

5. The method of claim 4 , wherein inhalation is via a sonic nebulizer.

6. The method of claim 1 , wherein administration is by injection.

7. The method of claim 6 , wherein injection is subcutaneous, intravenous, or intramuscular.

8. The method of claim 1 , wherein administration is by infusion.

9. The method of claim 1 , wherein administration is oral.

10. A method of lowering peripheral serotonin in a patient having idiopathic pulmonary arterial hypertension, comprising administering a therapeutically effective amount 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 or a pharmaceutically acceptable salt thereof.

11. The method of claim 10 , wherein administration is by inhalation.

12. The method of claim 11 , wherein inhalation is with a powder.

13. The method of claim 11 , wherein inhalation is with a spray or an aerosol.

14. The method of claim 13 , wherein inhalation is via a sonic nebulizer.

15. The method of claim 10 , wherein administration is by injection.

16. The method of claim 15 , wherein injection is subcutaneous, intravenous, or intramuscular.

17. The method of claim 10 , wherein injection is subcutaneous, intravenous, or intramuscular.

18. The method of claim 10 , wherein administration is oral.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 9, 2021
From: ROIVANT SCIENCES GMBH
To: ALTAVANT SCIENCES GMBH
Reel/Frame 055536/0102 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 17, 2019
From: KAROS PHARMACEUTICALS, INC.
To: ROIVANT SCIENCES GMBH
Reel/Frame 051303/0170 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 9, 2019
From: DE LOMBAERT, STÉPHANE; GOLDBERG, DANIEL R.; BRAMELD, KENNETH; SJOGREN, ERIC BRIAN; SCRIBNER, ANDREW
To: KAROS PHARMACEUTICALS, INC.
Reel/Frame 051218/0909 →
Continuity (9)
Continuation 15978361 · May 14, 2018
Continuation 15645054 · Jul 10, 2017
Continuation 15278130 · Sep 28, 2016
Continuation 14841868 · Sep 1, 2015
Continuation 14477948 · Sep 5, 2014
Provisional Application 62004385 · May 29, 2014
Provisional Application 61899943 · Nov 5, 2013
Provisional Application 61874545 · Sep 6, 2013
Related Publication 20190282575A1 · Sep 19, 2019