IP Library › Granted Patent US 11,453,655
Granted Patent B2
US 11,453,655 · App. 16/994,875 · Granted Sep 27, 2022

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 11,453,655
App. No.
16/994,875
Granted
Sep 27, 2022
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 (8)

1. Crystalline Form A of Compound 1:

2. Crystalline Form A according to claim 1 in substantially pure form.

3. Crystalline Form A according to claim 1 , characterized by an X-ray powder diffractogram having a signal at at least three two-theta values chosen from 6.6±0.2, 7.6±0.2, 9.6±0.2, 12.4±0.2, 13.1±0.2, 15.2±0.2, 16.4±0.2, 18.2±0.2, and 18.6±0.2.

4. Crystalline Form A according to claim 1 , characterized by an X-ray powder diffractogram having a signal at at least three two-theta values chosen from 6.6±0.2, 9.6±0.2, 13.1±0.2, 15.2±0.2, 18.2±0.2, and 18.6±0.2.

5. Crystalline Form A according to claim 1 , characterized by an X-ray powder diffractogram having a signal at three two-theta values of 6.6±0.2, 13.1±0.2, 18.2±0.2.

6. Crystalline Form A according to claim 1 , characterized by an X-ray powder diffractogram having a signal at six two-theta values of 6.6±0.2, 9.6±0.2, 13.1±0.2, 15.2±0.2, 18.2±0.2, and 18.6±0.2.

7. Crystalline Form A according to claim 1 , characterized by an X-ray powder diffractogram substantially similar to that in FIG. 2 .

8. A pharmaceutical formulation comprising at least one crystalline form according to claim 1 and a pharmaceutically acceptable carrier.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 29, 2021
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 INCOPORATED
Reel/Frame 057635/0244 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 29, 2021
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 057635/0271 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 29, 2021
From: ALCACIO, TIMOTHY; ANGELL, PAUL TIMOTHY; GROOTENHULS, PETER DIEDERIK JAN; HADIDA RUAH, SARA SABINA; 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 057635/0332 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 29, 2021
From: VERTEX PHARMACEUTICALS (SAN DIEGO) LLC
To: VERTEX PHARMACEUTICALS INCORPORATED
Reel/Frame 057635/0352 →
Continuity (3)
Division 15836627 · Dec 8, 2017
Provisional Application 62432537 · Dec 9, 2016
Related Publication 20210047295A1 · Feb 18, 2021
Cited By (5)
US 12,269,831 US 12,324,802 US 12,350,262 US 12,384,762 US 12,415,798