IP Library › Granted Patent US 10,570,115
Granted Patent B2
US 10,570,115 · App. 15/721,390 · Granted Feb 25, 2020

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

Inventors: Timothy Alcacio (San Diego, CA); Minson Baek (San Diego, CA); Peter Grootenhuis (Del Mar, CA); Sara Sabina Hadida Ruah (La Jolla, CA); Robert M. Hughes (San Diego, CA); Ali Keshavarz-Shokri (San Diego, CA); Rachel McAuley-Aoki (San Diego, CA); Jason McCartney (Cardiff by the Sea, CA); Mark Thomas Miller (San Diego, CA); Fredrick Van Goor (San Diego, CA); Beili Zhang (San Diego, CA); Corey Anderson (San Diego, CA); Thomas Cleveland (San Marcos, CA); Bryan A. Frieman (La Jolla, CA); Haripada Khatuya (San Diego, CA); Pramod Virupax Joshi (San Diego, CA); Paul John Krenitsky (San Diego, CA); Vito Melillo (Escondido, CA); Fabrice Jean Denis Pierre (La Jolla, CA); Andreas P. Termin (Encinitas, CA); Johnny Uy (San Diego, CA); Jinglan Zhou (San Diego, CA); Alexander Russell Abela (San Diego, CA); Brett Bradley Busch (San Diego, CA); Prasuna Paraselli (San Diego, CA); David Andrew Siesel (San Diego, CA)
Assignee: Vertex Pharmaceuticals Incorporated
C07D401/14C07B59/002C07D471/14C07D498/14C07B2200/05
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Quick Facts
Patent No.
US 10,570,115
App. No.
15/721,390
Granted
Feb 25, 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.

Claims (30)

1. A compound having the following formula:

a pharmaceutical acceptable salt thereof, or a deuterated derivative of any of the foregoing.

2. A pharmaceutical composition comprising the compound, pharmaceutically acceptable salt, or deuterated derivative of claim 1 , a pharmaceutically acceptable carrier and optionally one or more of:

(a) Compound II:

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

(b) Compound III:

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

3. A method of treating cystic fibrosis comprising administering to a patient in need thereof a pharmaceutical composition according to claim 2 .

4. A compound of the formula:

in the form of a pharmaceutically acceptable salt.

5. A compound having the following formula:

6. A pharmaceutical composition comprising the compound of claim 1 .

7. A pharmaceutical composition comprising the compound of claim 4 .

8. A pharmaceutical composition comprising the compound of claim 5 .

9. A pharmaceutical composition comprising a compound having the following formula:

or a pharmaceutically acceptable salt thereof; a pharmaceutically acceptable carrier; and optionally one or more of:

(a) Compound II:

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

(b) Compound III:

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

10. The pharmaceutical composition of claim 9 , wherein the compound having the following formula:

is in the form of a pharmaceutically acceptable salt.

11. A method of treating cystic fibrosis comprising administering to a patient in need thereof the compound according to claim 1 .

12. A method of treating cystic fibrosis comprising administering to a patient in need thereof the compound according to claim 4 .

13. A method of treating cystic fibrosis comprising administering to a patient in need thereof the compound according to claim 5 .

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

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

16. A method of treating cystic fibrosis comprising administering to a patient in need thereof the pharmaceutical composition according to claim 8 .

17. A method of treating cystic fibrosis comprising administering to a patient in need thereof the pharmaceutical composition according to claim 9 .

18. A method of treating cystic fibrosis comprising administering to a patient in need thereof the pharmaceutical composition according to claim 10 .

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 15, 2017
From: ABELA, ALEXANDER RUSSELL; KHATUYA, HARIPADA; MELILLO, VITO; PARASELLI, PRASUNA; PIERRE, FABRICE JEAN DENIS
To: VERTEX PHARMACEUTICALS INCORPORATED
Reel/Frame 044408/0071 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 15, 2017
From: VERTEX PHARMACEUTICALS (SAN DIEGO) LLC
To: VERTEX PHARMACEUTICALS INCORPORATED
Reel/Frame 044408/0083 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 15, 2017
From: ANDERSON, COREY; BUSCH, BRETT BRADLEY; CLEVELAND, THOMAS; FRIEMAN, BRYAN A.; KRENITSKY, PAUL JOHN; SIESEL, DAVID ANDREW; TERMIN, ANDREAS P.; UY, JOHNNY; ZHOU, JINGLAN; JOSHI, PRAMOD VIRUPAX; ALCACIO, TIMOTHY; BAEK, MINSON; GROOTENHUIS, PETER; HADIDA RUAH, SARA SABINA; HUGHES, ROBERT M.; KESHAVARZ-SHOKRI, ALI; MCAULEY-AOKI, RACHEL; MCCARTNEY, JASON; MILLER, MARK THOMAS; VAN GOOR, FREDRICK; ZHANG, BEILI
To: VERTEX PHARMACEUTICALS (SAN DIEGO) LLC
Reel/Frame 044744/0897 →
Continuity (5)
Provisional Application 62402838 · Sep 30, 2016
Provisional Application 62410353 · Oct 19, 2016
Provisional Application 62415409 · Oct 31, 2016
Provisional Application 62419935 · Nov 9, 2016
Related Publication 20180093969A1 · Apr 5, 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