IP Library Granted Patent US 9,657,023
Granted Patent B2
US 9,657,023 · App. 14/446,011 · Granted May 23, 2017

Polymorph of Syk inhibitors

Inventors: Tim G. Elford (Sherwood Park, CA); Peter Chee-Chu Fung (San Mateo, CA); Michael Laird Hurrey (San Ramon, CA); Dimitrios Stefanidis (Mountain View, CA); Dragos Vizitiu (Edmonton, CA)
Assignee: Gilead Connecticut, Inc.
C07D487/04C07C309/04
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Quick Facts
Patent No.
US 9,657,023
App. No.
14/446,011
Granted
May 23, 2017
Kind
B2
Abstract

Polymorphs of a bis-mesylate salt of a compound of Formula I: or a hydrate thereof, are provided. The bis-mesylate salt may also be depicted as a compound of Formula IA: Provided herein are also compositions thereof, methods for their preparation and methods for such polymorphs.

Claims (14)

1. Polymorph Form 3 of a monohydrate bis-mesylate salt of a compound of Formula I

2. A pharmaceutical composition comprising:

Form 3 of a mononhydrate bis-mesylate salt of a compound of formula I:

and a pharmaceutical carrier, excipient, adjuvant, or vehicle.

3. The pharmaceutical composition of claim 2 , wherein the bis-mesylate salt is a monohydrate, bis-mesylate salt polymorph characterized by;

an X-ray diffraction pattern comprising 2θ-reflections, plus or minus 0.2 degrees 2θ, at 13.8, 16.9, 22.9, and 26.1; or

an X-ray diffraction pattern substantially as shown in FIG. 1A or 1B .

4. The pharmaceutical composition of claim 2 , wherein the bis-mesylate salt is a monohydrate, bis-mesylate salt polymorph characterized by:

an X-ray diffraction pattern comprising 2θ-reflections, plus or minus 0.2 degrees 2θ, at 13.8, 16.9, 22.9, and 26.1.

5. The pharmaceutical composition of claim 2 , wherein the bis-mesylate salt is a monohydrate, bis-mesylate salt polymorph characterized by an X-ray diffraction pattern substantially as shown in FIG. 1A .

6. The pharmaceutical composition of claim 2 , wherein the bis-mesylate salt is a monohydrate, bis-mesylate salt polymorph characterized by an X-ray diffraction pattern substantially as shown in FIG. 1B .

7. The polymorph of claim 1 , wherein said polymorph is characterized by an X-ray diffraction pattern comprising 2θ-reflections, plus or minus 0.2 degrees 2θ, at 13.8, 16.9, 22.9, and 26.1.

8. The polymorph of claim 1 , wherein said polymorph is characterized by an Xray diffraction pattern substantially as shown in FIG. 1A .

9. The polymorph of claim 1 , wherein said polymorph is characterized by an X-ray diffraction pattern substantially as shown in FIG. 1B .

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 30, 2020
From: GILEAD CONNECTICUT, INC.
To: KRONOS BIO, INC.
Reel/Frame 053927/0969 →
MERGER AND CHANGE OF NAME Recorded Sep 17, 2020
From: COUGAR MERGER SUB, INC.; CGI PHARMACEUTICALS, INC.; CGI PHARMACEUTICALS, INC.
To: GILEAD CONNECTICUT, INC.
Reel/Frame 053799/0190 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 31, 2014
From: FUNG, PETER CHEE-CHU; STEFANIDIS, DIMITRIOS; VIZITIU, DRAGOS; ELFORD, TIM G.; HURREY, MICHAEL LAIRD
To: GILEAD CONNECTICUT, INC.
Reel/Frame 033439/0601 →
Continuity (2)
Provisional Application 61860197 · Jul 30, 2013
Related Publication 20150038505A1 · Feb 5, 2015