IP Library Granted Patent US 8,741,922
Granted Patent B2
US 8,741,922 · App. 13/751,656 · Granted Jun 3, 2014

Solid forms of N-(4-(7-azabicyclo[2.2,1]heptan-7-yl)-2-trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide

Inventors: Beili Zhang (San Diego, CA); Mariusz Krawiec (Marlborough, MA); Brian Luisi (Mansfield, MA); Ales Medek (Winchester, MA)
Assignee: Vertex Pharmaceuticals Incorporated
A61K31/4748C07B2200/13
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Quick Facts
Patent No.
US 8,741,922
App. No.
13/751,656
Granted
Jun 3, 2014
Kind
B2
Abstract

The present invention relates to substantially crystalline and solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide (Form A-HCl, Form B, Form B-HCl, or any combination of these forms), pharmaceutical compositions thereof, and methods of treatment 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, and dry-eye disease, said method comprising the step of administering to said patient an effective amount of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide characterized as Form A-HCl, Form B, Form B-HCl, or any combination of these forms.

2. The method according to claim 1 , wherein said disease is cystic fibrosis, COPD, smoke induced COPD, hereditary emphysema, or dry-eye disease.

3. The method of claim 2 , wherein disease is cystic fibrosis, hereditary emphysema, or dry-eye disease.

4. The method of claim 3 , wherein the disease is cystic fibrosis.

5. A method of modulating CFTR activity in a biological sample comprising the step of contacting said CFTR with N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide characterized as Form A-HCl, Form B, Form B-HCl, or any combination of these forms.

6. The method of claim 4 , wherein the patient is homozygous for ΔF508 mutation.

7. The method of claim 4 , wherein the patient is homozygous for G551D mutation.

8. The method of claim 4 , wherein the patient is heterozygous for ΔF508 mutation.

9. The method of claim 4 , wherein the patient is heterozygous for G551D mutation.

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 Mar 29, 2013
From: ZHANG, BEILI; KRAWIEC, MARIUSZ; LUISI, BRIAN; MEDEK, ALES
To: VERTEX PHARMACEUTICALS INCORPORATED
Reel/Frame 030115/0833 →
Continuity (3)
Continuation 12909789 · Oct 21, 2010
Provisional Application 61254614 · Oct 23, 2009
Related Publication 20130137722A1 · May 30, 2013