IP Library Granted Patent US 10,882,830
Granted Patent B2
US 10,882,830 · App. 16/333,075 · Granted Jan 5, 2021

Crystal form of ozanimod hydrochloride and processes for preparation therefor

Inventors: Minhua Chen (Jiangsu, CN); Yanfeng Zhang (Jiangsu, CN); Xiaoting Zhai (Jiangsu, CN); Kaiqiang Yan (Jiangsu, CN); Chaohui Yang (Jiangsu, CN); Xiaoyu Zhang (Jiangsu, CN)
Assignee: RECEPTOS LLC
C07D273/02A61K9/00A61K31/41A61K31/425A61P1/04A61P37/00A61P37/02C07D271/06C07B2200/13
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Quick Facts
Patent No.
US 10,882,830
App. No.
16/333,075
Granted
Jan 5, 2021
Kind
B2
Abstract

The present disclosure relates to crystalline form CS3 of ozanimod hydrochloride which can be used for treating autoimmune diseases, particularly used for preparing drugs for treating multiple sclerosis and ulcerative colitis and preparation method thereof.

Claims (14)

1. A crystalline form CS3 of ozanimod hydrochloride, wherein the X-ray powder diffraction pattern shows characteristic peaks at 2 theta values of 19.6°±0.2°, 24.9°±0.2° and 5.8°±0.2° using CuKα radiation.

2. The crystalline form CS3 of ozanimod hydrochloride according to claim 1 , wherein the X-ray powder diffraction pattern shows one or two or three characteristic peaks at 2 theta values of 7.8°±0.2°, 11.7°±0.2° and 29.5°±0.2° using CuKα radiation.

3. The crystalline form CS3 of ozanimod hydrochloride according to claim 1 , wherein the X-ray powder diffraction pattern shows one or two or three characteristic peaks at 2 theta values of 3.9°±0.2°, 14.2°±0.2° and 20.7°±0.2° using CuKα radiation.

4. A process for preparing crystalline form CS3 of ozanimod hydrochloride according to claim 1 , wherein the process comprises:

dissolving ozanimod hydrochloride into ethanol or a mixture of solvents selected from an alcohol and an arene, an alcohol and a nitrile, an alcohol and an acid, an acid and water,

filtering and adding a polymer into the solution and then evaporating at room temperature to obtain a white solid.

5. The process for preparing crystalline form CS3 of ozanimod hydrochloride according to claim 4 , wherein each said alcohol is methanol or ethanol; each said acid is acetic acid; said arene is toluene; said nitrile is acetonitrile.

6. A pharmaceutical composition, wherein said pharmaceutical composition comprises a therapeutically effective amount of crystalline form CS3 of ozanimod hydrochloride according to claim 1 and a pharmaceutically acceptable carrier, a diluent or an excipient.

7. A method for treating ulcerative colitis, comprising administering to a patient in need thereof a therapeutically effective amount of the crystalline form CS3 of ozanimod hydrochloride according to claim 1 .

8. A method for treating multiple sclerosis, comprising administering to a patient in need thereof a therapeutically effective amount of the crystalline form CS3 of ozanimod hydrochloride according to claim 1 .

9. The crystalline form CS3 of ozanimod hydrochloride according to claim 2 , wherein the X-ray powder diffraction pattern shows one or two or three characteristic peaks at 2 theta values of 3.9°±0.2°, 14.2°±0.2° and 20.7°±0.2° using CuKα radiation.

10. A pharmaceutical composition, wherein said pharmaceutical composition comprises a therapeutically effective amount of crystalline form CS3 of ozanimod hydrochloride according to claim 9 and a pharmaceutically acceptable carrier, a diluent or an excipient.

11. A method for treating ulcerative colitis, comprising administering to a patient in need thereof a therapeutically effective amount of the crystalline form CS3 of ozanimod hydrochloride according to claim 9 .

12. A method for treating multiple sclerosis, comprising administering to a patient in need thereof a therapeutically effective amount of the crystalline form CS3 of ozanimod hydrochloride according to claim 9 .

Assignments (3)
CHANGE OF ADDRESS OF ASSIGNEE Recorded May 4, 2024
From: RECEPTOS LLC
To: RECEPTOS LLC
Reel/Frame 068258/0194 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 24, 2020
From: CRYSTAL PHARMACEUTICAL (SUZHOU) CO., LTD.
To: RECEPTOS LLC
Reel/Frame 053570/0814 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 13, 2019
From: CHEN, MINHUA; ZHANG, YANFENG; ZHAI, XIAOTING; YAN, KAIQIANG; YANG, CHAOHUI; ZHANG, XIAOYU
To: CRYSTAL PHARMACEUTICAL (SUZHOU) CO., LTD.
Reel/Frame 048589/0606 →
Priority Claims (1)
CN 2016 1 0822328 · Sep 14, 2016 · national
Continuity (1)
Related Publication 20190248755A1 · Aug 15, 2019