Modulator of the cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator

Patent metadata

Field	Value
Publication number	US-10793547-B2
Application number	US-201715836627-A
Country	US
Kind code	B2
Filing date	Dec 8, 2017
Priority date	Dec 9, 2016
Publication date	Oct 6, 2020
Grant date	Oct 6, 2020

Abstract

Compounds of Formula (I):

pharmaceutically acceptable salts thereof, deuterated derivatives of any of the foregoing, and metabolites of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed. Also disclosed are solid state forms of Compound 1 and salts and solvates thereof.

First claim

The invention claimed is:

1. A compound selected from Compound I:

deuterated derivatives thereof, and pharmaceutically acceptable salts of any of the foregoing.

2. A compound selected from the following formula:

a pharmaceutically acceptable salt thereof, and a deuterated derivative of any of the foregoing.

3. A compound of the following formula:

4. A pharmaceutical composition comprising:
(a) a compound of the following formula:

and
(b) a pharmaceutically acceptable carrier.

5. The pharmaceutical composition of claim 4 further comprising Compound II:

6. The pharmaceutical composition of claim 4 further comprising Compound III:

7. The pharmaceutical composition of claim 5 further comprising Compound III:

8. A method of treating cystic fibrosis comprising administering to a patient in need thereof a compound of the following formula:

9. A method of treating cystic fibrosis comprising administering to a patient in need thereof a pharmaceutical composition comprising:
(a) a compound of the following formula:

and
(b) a pharmaceutically acceptable carrier.

10. A pharmaceutically acceptable salt of Compound 1:

11. A pharmaceutical composition comprising:
(a) a pharmaceutically acceptable salt of Compound I:

and
(b) a pharmaceutically acceptable carrier.

12. The pharmaceutical composition of claim 11 , further comprising Compound II:

13. The pharmaceutical composition of claim 11 , further comprising Compound III:

14. The pharmaceutical composition of claim 12 , further comprising Compound III:

15. A method of treating cystic fibrosis comprising administering to a patient in need thereof a pharmaceutically acceptable salt of Compound 1:

16. A method of treating cystic fibrosis comprising administering to a patient in need thereof a pharmaceutical composition of claim 12 .

17. A method of treating cystic fibrosis comprising administering to a patient in need thereof a pharmaceutical composition of claim 13 .

18. A method of treating cystic fibrosis comprising administering to a patient in need thereof a pharmaceutical composition of claim 14 .

19. A method of treating cystic fibrosis comprising administering to a patient in need thereof a pharmaceutical composition of claim 5 .

20. A method of treating cystic fibrosis comprising administering to a patient in need thereof a pharmaceutical composition of claim 6 .

21. A method of treating cystic fibrosis comprising administering to a patient in need thereof a pharmaceutical composition of claim 7 .

Assignees

• Vertex Pharma

Inventors

• Abela Alexander Russell
• Alcacio Timothy
• Anderson Corey
• Angell Paul Timothy
• Baek Minson
• Clemens Jeremy J
• Cleveland Thomas
• Ferris Lori Ann
• Grootenhuis Peter Diederik Jan
• Gross Raymond Stanley
• Gulevich Anton V
• Hadida Ruah Sara Sabina
• Hsia Clara Kuang-Ju
• Hughes Robert M
• Joshi Pramod Virupax
• Kang Ping
• Keshavarz-Shokri Ali
• Khatuya Haripada
• Krenitsky Paul John
• Mccartney Jason
• Miller Mark Thomas
• Paraselli Prasuna
• Pierre Fabrice Jean Denis
• Shi Yi
• Shrestha Muna
• Siesel David Andrew
• Stavropoulos Kathy
• Termin Andreas P
• Van Goor Fredrick F
• Uy Johnny
• Young Timothy John
• Zhou Jinglan

Classifications

• C07B2200/13

  Crystalline forms, e.g. polymorphs · CPC title

• C07B2200/05

  Isotopically modified compounds, e.g. labelled · CPC title

• A61P11/00

  Drugs for disorders of the respiratory system · CPC title

• C07D231/20

  One oxygen atom attached in position 3 or 5 · CPC title

• C07D401/04

  directly linked by a ring-member-to-ring-member bond · CPC title