IP Library Granted Patent US 9,353,097
Granted Patent B2
US 9,353,097 · App. 14/746,666 · Granted May 31, 2016

Solid state forms of a quinazoline derivative and its use as a BRAF inhibitor

Inventors: Stephen J. Bierlmaier (Thorndale, PA); Ralph C. Haltiwanger (West Chester, PA); Martin J. Jacobs (Versailles, KY)
Assignee: Ignyta, Inc.
C07D413/12A61K9/20A61K9/48A61K31/517C07D239/88
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Quick Facts
Patent No.
US 9,353,097
App. No.
14/746,666
Granted
May 31, 2016
Kind
B2
Abstract

This application relates to various salts and solid state forms of Compound (I). This application also relates to pharmaceutical compositions and therapeutic uses of these materials and compositions.

Claims (12)

1. A crystalline form of the hydrochloride salt of N-[3-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl]-N′-[5-(2,2,2-trifluoro-1,1-dimethylethyl)-3-isoxazolyl]-urea, wherein said crystalline form is characterized by an x-ray powder diffraction pattern comprising a peak at a 2-theta value of about 5.67±0.2 degrees.

2. A crystalline form according to claim 1 , wherein said x-ray powder diffraction pattern further comprises a peak at a 2-theta value of about 14.48±0.2 degrees.

3. A crystalline form according to claim 2 , wherein said x-ray powder diffraction pattern further comprises a peak at a 2-theta value of about 15.89±0.2 degrees.

4. A crystalline form according to claim 3 , wherein said x-ray powder diffraction pattern further comprises peaks at 2-theta values of about 8.55±0.2 degrees, 9.96±0.2 degrees, 19.36±0.2 degrees, 26.83±0.2 degrees, and 27.56±0.2 degrees.

5. A crystalline form according to claim 1 , wherein said crystalline form is further characterized by exhibiting a peak in a differential scanning calorimetry scan of about 236° C.

6. A pharmaceutical composition, comprising a crystalline form of the hydrochloride salt of N-[3-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl]-N′-[5-(2,2,2-trifluoro-1,1-dimethylethyl)-3-isoxazolyl]-urea and a pharmaceutically acceptable excipient, wherein said crystalline form is characterized by an x-ray powder diffraction pattern comprising a peak at a 2-theta value of about 5.67±0.2 degrees.

7. A pharmaceutical composition according to claim 6 , wherein said composition is in a form suitable for oral administration to a subject.

8. A pharmaceutical composition according to claim 7 , wherein said composition is in the form of a tablet, pill, powder, capsule, or troche.

9. A pharmaceutical composition according to claim 8 , wherein said composition is in the form of a tablet, pill, or capsule.

10. A pharmaceutical composition according to claim 9 , wherein said composition is in the form of a tablet or capsule.

11. A pharmaceutical composition according to claim 10 , wherein said composition is in the form of a tablet.

12. A pharmaceutical composition according to claim 10 wherein said composition is in the form of a capsule.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 13, 2017
From: CEPHALON, INC.
To: IGNYTA, INC.
Reel/Frame 041243/0001 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 13, 2017
From: BIERLMAIER, STEPHEN J.; JACOBS, MARTIN J.; HALTIWANGER, RALPH C.
To: CEPHALON, INC.
Reel/Frame 041243/0034 →
Continuity (3)
Continuation PCTUS2014023110 · Mar 11, 2014
Provisional Application 61776081 · Mar 11, 2013
Related Publication 20150376171A1 · Dec 31, 2015