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1. (WO2019042219) CRYSTALLINE FORM OF OZANIMOD HYDROCHLORIDE AND PREPARATION METHOD THEREFOR
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Pub. No.: WO/2019/042219 International Application No.: PCT/CN2018/102034
Publication Date: 07.03.2019 International Filing Date: 23.08.2018
IPC:
C07D 271/06 (2006.01) ,A61K 31/4245 (2006.01) ,A61P 37/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
271
Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
02
not condensed with other rings
06
1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4245
Oxadiazoles
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37
Drugs for immunological or allergic disorders
Applicants:
苏州科睿思制药有限公司 CRYSTAL PHARMACEUTICAL (SUZHOU) CO., LTD. [CN/CN]; 中国江苏省苏州市 工业园区星湖街218号生物纳米园B4-301赵林林 ZHAO, Linlin B4-301, Biobay, 218 Xinghu Street, Suzhou Industrial Park Suzhou, Jiangsu 215123, CN
Inventors:
陈敏华 CHEN, Minhua; CN
张炎锋 ZHANG, Yanfeng; CN
翟晓婷 ZHAI, Xiaoting; CN
鄢楷强 YAN, Kaiqiang; CN
杨朝惠 YANG, Chaohui; CN
Priority Data:
201710768645.331.08.2017CN
Title (EN) CRYSTALLINE FORM OF OZANIMOD HYDROCHLORIDE AND PREPARATION METHOD THEREFOR
(FR) FORME CRISTALLINE DU CHLORHYDRATE D'OZANIMOD ET PROCÉDÉ DE PRÉPARATION CORRESPONDANT
(ZH) 奥扎莫德盐酸盐的晶型及其制备方法
Abstract:
(EN) The present invention relates to a crystalline form of ozanimod hydrochloride and a preparation method therefor. The crystalline form of ozanimod hydrochloride provided by the present invention can be used to treat autoimmune diseases, particularly multiple sclerosis and ulcerative colitis. The crystalline form of ozanimod hydrochloride provided by the present invention has advantages in at least one aspect of solubility, melting point, stability, dissolubility, bioavailability, processing properties, and purification, provides new and better choices for preparation of ozanimod-containing pharmaceutical preparations and is of great significance for drug development.
(FR) La présente invention concerne une forme cristalline du chlorhydrate d'ozanimod et un procédé de préparation correspondant. La forme cristalline du chlorhydrate d'ozanimod selon la présente invention peut être utilisée pour traiter des maladies auto-immunes, en particulier la sclérose en plaques et la colite ulcéreuse. La forme cristalline du chlorhydrate d'ozanimod fournie par l'invention présente des avantages dans au moins un aspect relatif à la solubilité, point de fusion, stabilité, dissolubilité, biodisponibilité, propriétés de traitement, et de purification, présente de nouveaux, et de meilleurs choix pour la préparation de formulations pharmaceutiques contenant de l'ozanimod et est d'une grande importance pour le développement de médicaments.
(ZH) 本发明涉及奥扎莫德盐酸盐的晶型及其制备方法。本发明提供的奥扎莫德盐酸盐的晶型可用于治疗自身免疫疾病,特别是多发性硬化症和溃疡性结肠炎。本发明提供的奥扎莫德盐酸盐的晶型在溶解度、熔点、稳定性、溶出度、生物有效性以及加工性能、提纯等方面中的至少一方面上存在优势,为含奥扎莫德的药物制剂的制备提供了新的更好的选择,对于药物开发具有重要意义。
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: Chinese (ZH)
Filing Language: Chinese (ZH)