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AssigneeCrystal Pharmaceutical (Suzhou) Co., Ltd.
InventorsMinhua CHEN, Yanfeng ZHANG, Xiaoting ZHAI, Kaiqiang YAN, Chaohui YANG, Xiaoyu ZHANG
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The present disclosure is directed to novel crystalline forms of ozanimod and ozanimod hydrochloride, as well as preparation method thereof. Said crystalline forms of ozanimod and ozanimod hydrochloride can be used for treating autoimmune diseases, particularly used for preparing drugs for treating multiple sclerosis and ulcerative colitis. The crystalline forms of the present disclosure have one or more advantages in solubility, melting point, stability, dissolution, bioavailability and processability and provide new and better choices for the preparation of ozanimod drug product, and are very valuable for drug development.
A crystalline Form CS1 of ozanimod, wherein the X-ray powder diffraction pattern shows characteristic peaks at 2 theta values of 12.1°±0.2°, 10.4°±0.2° and 4.2°±0.2° using CuKα radiation.
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A crystalline Form CS2 of ozanimod, wherein the X-ray powder diffraction pattern shows characteristic peaks at 2 theta values of 23.2°±0.2°, 18.5°±0.2° and 13.3°±0.2° using CuKα radiation.
A crystalline Form CS3 of ozanimod, wherein the X-ray powder diffraction pattern shows characteristic peaks at 2 theta values of 4.4°±0.2°, 13.0°±0.2°, 26.0°±0.2° and 11.0°±0.2° using CuKα radiation.
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A crystalline Form CS5 of ozanimod, wherein the X-ray powder diffraction pattern shows characteristic peaks at 2 theta values of 4.3°±0.2°, 6.8°±0.2° and 16.4°±0.2° using CuKα radiation.
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A crystalline Form CS6 of ozanimod, wherein the X-ray powder diffraction pattern shows characteristic peaks at 2 theta values of 4.4°±0.2°, 24.5±0.2°, 26.5°±0.2° and 13.8°±0.2° using CuKα radiation.
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A crystalline Form CS1 of ozanimod hydrochloride, wherein the X-ray powder diffraction pattern shows characteristic peaks at 2 theta values of 26.1°±0.20°, 24.4°±0.20° and 20.1°±0.20° using CuKα radiation.
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Dependencies are inferred from the claim text.