IP Library Granted Patent US 8,901,297
Granted Patent B2
US 8,901,297 · App. 13/614,063 · Granted Dec 2, 2014

Compositions for modulating a kinase cascade and methods of use thereof

Inventors: David G. Hangauer, Jr. (Lancaster, NY); Debasis Patra (Manlius, NY); Jeremy A. Cody (Clifton Springs, NY); Grant J. Palmer (Nashville, TN); Paul K. Isbester (Castleton on Hudson, NY); Jonathon Salsbury (Madison, WI)
Assignee: Kinex Pharmaceuticals, LLC
C07D213/56C07D213/59A61K31/44C07D413/12
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Quick Facts
Patent No.
US 8,901,297
App. No.
13/614,063
Granted
Dec 2, 2014
Kind
B2
Abstract

The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning calorimetry profile, as well as a unique crystalline structure.

Claims (10)

1. A polymorph of a salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide characterized by an X-ray diffraction pattern substantially similar to that set forth in any one of FIGS. 20-28 .

2. The polymorph of claim 1 , characterized by an X-ray diffraction pattern substantially similar to that set forth in FIG. 20 , and wherein said salt is a p-tosylate.

3. The polymorph of claim 1 , characterized by an X-ray diffraction pattern substantially similar to that set forth in FIG. 21 , and wherein said salt is a p-tosylate.

4. The polymorph of claim 1 , characterized by an X-ray diffraction pattern substantially similar to that set forth in FIG. 22 , and wherein said salt is a fumarate.

5. The polymorph of claim 1 , characterized by an X-ray diffraction pattern substantially similar to that set forth in FIG. 23 , and wherein said salt is a maleate.

6. The polymorph of claim 1 , characterized by an X-ray diffraction pattern substantially similar to that set forth in FIG. 24 , and wherein said salt is a bis-maleate.

7. The polymorph of claim 1 , characterized by an X-ray diffraction pattern substantially similar to that set forth in FIG. 25 , and wherein said salt is a bis-fumarate.

8. The polymorph of claim 1 , characterized by an X-ray diffraction pattern substantially similar to that set forth in FIG. 26 , and wherein said salt is a bis-fumarate.

9. The polymorph of claim 1 , characterized by an X-ray diffraction pattern substantially similar to that set forth in FIG. 27 , and wherein said salt is a bis-phosphate.

10. The polymorph of claim 1 , characterized by an X-ray diffraction pattern substantially similar to that set forth in FIG. 28 , and wherein said salt is a bis-p-tosylate.

Assignments (9)
SECURITY INTEREST Recorded Sep 16, 2022
From: ATHENEX, INC.
To: SAGARD HEALTHCARE ROYALTY PARTNERS, LP, AS ADMINISTRATIVE AGENT
Reel/Frame 061119/0681 →
SECURITY INTEREST Recorded Sep 16, 2022
From: ATNX SPV, LLC
To: SAGARD HEALTHCARE ROYALTY PARTNERS, LP, AS ADMINISTRATIVE AGENT
Reel/Frame 061119/0920 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 13, 2022
From: ATHENEX, INC.
To: ATNX SPV, LLC
Reel/Frame 061071/0086 →
SECURITY INTEREST Recorded Jun 22, 2020
From: ATHENEX, INC.
To: OAKTREE FUND ADMINISTRATION, LLC
Reel/Frame 053005/0657 →
RELEASE OF SECURITY INTEREST Recorded Jun 19, 2020
From: PERCEPTIVE CREDIT HOLDINGS II, LP
To: ATHENEX, INC.
Reel/Frame 052990/0677 →
PATENT SECURITY AGREEMENT Recorded Jul 3, 2018
From: ATHENEX, INC.
To: PERCEPTIVE CREDIT HOLDINGS II, LP
Reel/Frame 047247/0812 →
CHANGE OF NAME Recorded Sep 21, 2015
From: KINEX PHARMACEUTICALS, INC.
To: ATHENEX, INC.
Reel/Frame 036644/0296 →
CHANGE OF NAME Recorded Sep 10, 2015
From: KINEX PHARMACEUTICALS, LLC
To: KINEX PHARMACEUTICALS, INC.
Reel/Frame 036585/0786 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 2, 2012
From: HANGAUER, DAVID G., JR.; PATRA, DEBASIS; CODY, JEREMY A.; PALMER, GRANT J.; ISBESTER, PAUL K.; SALSBURY, JONATHON
To: KINEX PHARMACEUTICALS, LLC
Reel/Frame 029063/0654 →
Continuity (7)
Continuation 13094679 · Apr 26, 2011
Continuation 12468694 · May 19, 2009
Continuation In Part 12154056 · May 19, 2008
Continuation In Part 12005792 · Dec 28, 2007
Provisional Application 60930758 · May 17, 2007
Provisional Application 60877762 · Dec 28, 2006
Related Publication 20130210822A1 · Aug 15, 2013