IP Library Granted Patent US 9,150,567
Granted Patent B2
US 9,150,567 · App. 14/468,253 · Granted Oct 6, 2015

Substituted tetrazol-1-yl-phenoxymethyl-thiazol-2-yl-piperidinyl-pyrimidine salts

Inventors: Jiangao Song (Hayward, CA); Charles A. McWherter (Hayward, CA); Fang Ma (Hayward, CA); Mark Andres (West Lafayette, IN); Igor Ivanisevic (West Lafayette, IN); Ekaterina Albert (Lafayette, IN); Patricia Andres (West Lafayette, IN)
Assignee: Cymabay Therapeutics, Inc.
C07D417/14C07B2200/13
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Quick Facts
Patent No.
US 9,150,567
App. No.
14/468,253
Granted
Oct 6, 2015
Kind
B2
Abstract

Crystalline salts of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine, compositions thereof, methods for their preparation, and methods for their use are disclosed.

Claims (5)

1. A method for preparing a polymorph (Form I) of a crystalline hydrochloride salt having a XRPD pattern comprising peaks at degrees 2-theta diffraction angles of about 8.8, 10.8, 16.1, 17.4, 20.4, 20.9, 21.5, 21.7, 26.6, and 28.1 comprising crystallizing 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine hydrochloride from a solution comprising one or more of acetone, acetonitrile, dichloromethane, diethyl ether, ethyl acetate, ethanol, heptane, hexane, hexafluoroisopropanol, isopropyl alcohol, isopropyl ether, methyl ethyl ketone, methanol, methyl-tert-butyl ether, 2,2,2-trifluoroethanol, or tetrahydrofuran.

2. A method for preparing a polymorph (Form II) of a crystalline hydrochloride salt having a XRPD pattern comprising peaks at degrees 2-theta diffraction angles of about 7.8, 10.1, 12.5, 18.4, 19.0, 20.8, 23.0, and 23.5 comprising crystallizing 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine hydrochloride from a solution comprising one or more of acetone, acetonitrile, dichloromethane, diethyl ether, ethyl acetate, ethanol, heptane, hexane, hexafluoroisopropanol, isopropyl alcohol, isopropyl ether, methyl ethyl ketone, methanol, methyl-tert-butyl ether, 2,2,2-trifluoroethanol, or tetrahydrofuran.

3. The method of claim 1 , wherein the solution is an acetone solution.

4. The method of claim 2 wherein the solution is a methanol solution.

5. The method of claim 2 wherein the solution is a methanol solution further comprising ethyl acetate or acetone.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 31, 2015
From: SONG, JIANGAO; MCWHERTER, CHARLES A.; MA, FANG
To: METABOLEX, INC.
Reel/Frame 035304/0429 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 31, 2015
From: ANDRES, MARK; IVANISEVIC, IGOR; ALBERT, EKATERINA; ANDRES, PATRICIA
To: APTUIT, INC.
Reel/Frame 035304/0438 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 31, 2015
From: APTUIT, INC.
To: METABOLEX, INC.
Reel/Frame 035304/0448 →
CHANGE OF NAME Recorded Mar 31, 2015
From: METABOLEX, INC.
To: CYMABAY THERAPEUTICS, INC.
Reel/Frame 035345/0408 →
Continuity (4)
Continuation 13853000 · Mar 28, 2013
Division 12886470 · Sep 20, 2010
Provisional Application 61247936 · Oct 1, 2009
Related Publication 20150197518A1 · Jul 16, 2015