IP Library › Granted Patent US 10,793,547
Granted Patent B2
US 10,793,547 · App. 15/836,627 · Granted Oct 6, 2020

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

Inventors: Alexander Russell Abela (San Diego, CA); Timothy Alcacio (San Diego, CA); Corey Anderson (San Diego, CA); Paul Timothy Angell (Carlsbad, CA); Minson Baek (San Diego, CA); Jeremy J. Clemens (San Diego, CA); Thomas Cleveland (San Marcos, CA); Lori Ann Ferris (Wilmington, MA); Peter Diederik Jan Grootenhuis (Del Mar, CA); Raymond Stanley Gross (Poway, CA); Anton V. Gulevich (San Diego, CA); Sara Sabina Hadida Ruah (La Jolla, CA); Clara Kuang-Ju Hsia (San Diego, CA); Robert M. Hughes (San Diego, CA); Pramod Virupax Joshi (San Diego, CA); Ping Kang (San Diego, CA); Ali Keshavarz-Shokri (San Diego, CA); Haripada Khatuya (San Diego, CA); Paul John Krenitsky (San Diego, CA); Jason McCartney (Cardiff by the Sea, CA); Mark Thomas Miller (San Diego, CA); Prasuna Paraselli (San Diego, CA); Fabrice Jean Denis Pierre (La Jolla, CA); Yi Shi (Natick, MA); Muna Shrestha (Belmont, MA); David Andrew Siesel (San Diego, CA); Kathy Stavropoulos (Quincy, MA); Andreas P. Termin (Encinitas, CA); Fredrick F. Van Goor (San Diego, CA); Johnny Uy (San Diego, CA); Timothy John Young (San Diego, CA); Jinglan Zhou (San Diego, CA)
Assignee: Vertex Pharmaceuticals Incorporated
C07D401/14A61P11/00C07D231/20C07D401/04C07D471/14C07D498/14C07B2200/13
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Quick Facts
Patent No.
US 10,793,547
App. No.
15/836,627
Granted
Oct 6, 2020
Kind
B2
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.

Claims (32)

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 .

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 26, 2018
From: ALCACIO, TIMOTHY; ANGELL, PAUL TIMOTHY; GROOTENHUIS, PETER DIEDERIK JAN; RUAH, SARA SABINA HADIDA; HUGHES, ROBERT M.; MILLER, MARK THOMAS; KESHAVARZ-SHOKRI, ALI; SIESEL, DAVID ANDREW; VAN GOOR, FREDRICK F.; YOUNG, TIMOTHY JOHN
To: VERTEX PHARMACEUTICALS (SAN DIEGO) LLC
Reel/Frame 045038/0036 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 26, 2018
From: KHATUYA, HARIPADA; PIERRE, FABRICE JEAN DENIS; ABELA, ALEXANDER RUSSELL; GULEVICH, ANTON V.; PARASELLI, PRASUNA; FERRIS, LORI ANN; STAVROPOULOS, KATHY; SHI, YI; SHRESTHA, MUNA
To: VERTEX PHARMACEUTICALS INCORPORATED
Reel/Frame 045038/0054 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 26, 2018
From: BAEK, MINSON; MCCARTNEY, JASON; ANDERSON, COREY; JOSHI, PRAMOD VIRUPAX; CLEMENS, JEREMY J.; CLEVELAND, THOMAS; GROSS, RAYMOND STANLEY; KRENITSKY, PAUL JOHN; TERMIN, ANDREAS P.; UY, JOHNNY; ZHOU, JINGLAN; KANG, PING; HSIA, CLARA KUANG-JU
To: VERTEX PHARMACEUTICALS (SAN DIEGO) LLC
Reel/Frame 045038/0075 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 26, 2018
From: VERTEX PHARMACEUTICALS (SAN DIEGO) LLC
To: VERTEX PHARMACEUTICALS INCORPORATED
Reel/Frame 045038/0117 →
Continuity (2)
Provisional Application 62432537 · Dec 9, 2016
Related Publication 20180162839A1 · Jun 14, 2018
Cited By (10)
US 12,186,306 US 12,269,831 US 12,319,693 US 12,324,802 US 12,350,262 US 12,384,762 US 12,415,798 US 12,421,251 US 12,552,810 US 12,612,416