IP Library Granted Patent US 8,785,476
Granted Patent B2
US 8,785,476 · App. 13/682,075 · Granted Jul 22, 2014

Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide

Inventors: Sneha G. Arekar (Brighton, MA); Steven C. Johnston (Litchfield, NH); Mariusz Krawiec (Marlborough, MA); Ales Medek (Winchester, MA); Praveen Mudunuri (Waltham, MA); Mark Jeffrey Sullivan (Framingham, MA)
Assignee: Vertex Pharmaceuticals Incorporated
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Quick Facts
Patent No.
US 8,785,476
App. No.
13/682,075
Granted
Jul 22, 2014
Kind
B2
Abstract

The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.

Claims (9)

1. A method of treating or lessening the severity of a disease in a patient, wherein said disease is selected from cystic fibrosis, smoke induced COPD, pancreatitis, pancreatic insufficiency, hereditary emphysema, COPD, or dry-eye disease, said method comprising the step of administering to said patient an effective amount of crystalline N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide characterized as Form C.

2. The method according to claim 1 , wherein said disease is cystic fibrosis.

3. The method according to claim 1 , wherein the patient possesses one or more of the following mutations of human CFTR: ΔF508, R117H, and G551D.

4. The method according to claim 3 , wherein the method includes treating or lessening the severity of cystic fibrosis in a patient possessing the ΔF508 mutation of human CFTR.

5. The method according to claim 3 , wherein the method includes treating or lessening the severity of cystic fibrosis in a patient possessing the G551D mutation of human CFTR.

6. The method according to claim 4 , wherein the method includes treating or lessening the severity of cystic fibrosis in a patient possessing the ΔF508 mutation of human CFTR on at least one allele.

7. The method according to claim 4 , wherein the method includes treating or lessening the severity of cystic fibrosis in a patient possessing the ΔF508 mutation of human CFTR on both alleles.

8. The method according to claim 5 wherein the method includes treating or lessening the severity of cystic fibrosis in a patient possessing the G551D mutation of human CFTR on at least one allele.

9. The method according to claim 5 , wherein the method includes treating or lessening the severity of cystic fibrosis in a patient possessing the G551D mutation of human CFTR on both alleles.

Assignments (4)
RELEASE OF SECURITY INTEREST Recorded Oct 14, 2016
From: MACQUARIE US TRADING LLC
To: VERTEX PHARMACEUTICALS INCORPORATED; VERTEX PHARMACEUTICALS (SAN DIEGO) LLC
Reel/Frame 040357/0001 →
ASSIGNEE CHANGE OF ADDRESS Recorded Feb 17, 2016
From: VERTEX PHARMACEUTICALS INCORPORATED
To: VERTEX PHARMACEUTICALS INCORPORATED
Reel/Frame 037845/0106 →
SECURITY INTEREST Recorded Jul 10, 2014
From: VERTEX PHARMACEUTICALS INCORPORATED; VERTEX PHARMACEUTICALS (SAN DIEGO) LLC
To: MACQUARIE US TRADING LLC
Reel/Frame 033292/0311 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 30, 2013
From: AREKAR, SNEHA G.; JOHNSTON, STEVEN C.; KRAWIEC, MARIUSZ; MEDEK, ALES; MUDUNURI, PRAVEEN; SULLIVAN, MARK JEFFREY
To: VERTEX PHARMACEUTICALS INCORPORATED
Reel/Frame 030313/0968 →
Continuity (3)
Division 13053172 · Mar 21, 2011
Provisional Application 61315885 · Mar 19, 2010
Related Publication 20130079367A1 · Mar 28, 2013