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1. (WO2017107972) NOVEL CRYSTALLINE FORM OF SELECTIVE S1P1 RECEPTOR AGONIST AND METHOD FOR PREPARING SAME
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/107972 International Application No.: PCT/CN2016/111689
Publication Date: 29.06.2017 International Filing Date: 23.12.2016
IPC:
C07D 277/42 (2006.01) ,A61P 17/06 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
277
Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
02
not condensed with other rings
20
having two or three double bonds between ring members or between ring members and non-ring members
32
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
38
Nitrogen atoms
42
Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17
Drugs for dermatological disorders
06
Antipsoriatics
Applicants:
苏州晶云药物科技有限公司 CRYSTAL PHARMATECH CO., LTD. [CN/CN]; 中国江苏省苏州市 苏州工业园区星湖街218号生物纳米园B4-101 B4-101, Biobay, 218 Xinghu Street, Suzhou Industrial Park Suzhou, Jiangsu 215123, CN
Inventors:
陈敏华 CHEN, Minhua; CN
张炎锋 ZHANG, Yanfeng; CN
李骄洋 LI, Jiaoyang; CN
张晓宇 ZHANG, Xiaoyu; CN
Agent:
苏州创元专利商标事务所有限公司 SUZHOU CREATOR PATENT & TREADMARK AGENCY LTD.; 中国江苏省苏州市 干将西路93号 No.93 Ganjiang West Road Suzhou, Jiangsu 215002, CN
Priority Data:
201510993103.725.12.2015CN
Title (EN) NOVEL CRYSTALLINE FORM OF SELECTIVE S1P1 RECEPTOR AGONIST AND METHOD FOR PREPARING SAME
(FR) NOUVELLE FORME CRISTALLINE D'AGONISTE SÉLECTIF DU RÉCEPTEUR S1P1 ET SON PROCÉDÉ DE PRÉPARATION
(ZH) 一种选择性S1P1受体激动剂的新晶型及其制备方法
Abstract:
(EN) Disclosed are crystalline forms 1, 2, and 3 of a selective S1P1 receptor agonist, namely Ponesimod, and a method for preparing the same. An X-ray powder diffraction pattern of the crystalline form 1 has characteristic peaks at 2 theta values of 18.1° ± 0.2°, 14.6° ± 0.2°, and 11.3° ± 0.2°. An X-ray powder diffraction pattern of the crystalline form 2 has characteristic peaks at 2 theta values of 3.8° ± 0.2°, 10.8° ± 0.2°, and 6.1° ± 0.2°. An X-ray powder diffraction pattern of the crystalline form 3 has characteristic peaks at 2 theta values of 12.2° ± 0.2°, 6.2° ± 0.2°, and 5.6° ± 0.2°. Compared with existing crystalline forms, the present invention has better stability and a greatly increased solubility, and is more suitable for development of a pharmaceutical preparation containing Ponesimod
(FR) L'invention concerne des formes cristallines 1, 2 et 3 d'un agoniste sélectif du récepteur S1P1, à savoir le Ponesimod, et un procédé de préparation associé. Un diagramme de diffraction des rayons X sur poudre de la forme cristalline 1 présente des pics caractéristiques à des valeurs 2-thêta de 18,1° ± 0,2°, 14,6° ± 0,2° et 11,3° ± 0,2 °. Un diagramme de diffraction des rayons X sur poudre de la forme cristalline 2 présente des pics caractéristiques à des valeurs 2-thêta de 3,8° ± 0,2°, 10,8° ± 0,2° et 6,1° ± 0,2 °. Un diagramme de diffraction des rayons X sur poudre de la forme cristalline 3 présente des pics caractéristiques à des valeurs 2-thêta de 12,2° ± 0,2°, 6,2° ± 0,2° et 5,6° ± 0,2 °. Par rapport aux formes cristallines existantes, la présente invention présente une meilleure stabilité et une solubilité considérablement accrue, et est plus appropriée pour le développement d'une préparation pharmaceutique contenant du Ponesimod.
(ZH) 本发明公开了一种选择性S1P1受体激动剂即Ponesimod的晶型1、2和3及其制备方法,其中晶型1的X射线粉末衍射图在2theta值为18.1°±0.2°、14.6°±0.2°、11.3°±0.2°处具有特征峰;晶型2的X射线粉末衍射图在2theta值为3.8°±0.2°、10.8°±0.2°、6.1°±0.2°处具有特征峰;晶型3的X射线粉末衍射图在2theta值为12.2°±0.2°、6.2°±0.2°、5.6°±0.2°处具有特征峰。本发明与现有晶形相比,不仅具有较好的稳定性,而且溶解性有较大提高,更适于含Ponesimod药物制剂的开发。
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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, 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 Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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)
Also published as:
CA3009713IL260254IN201817027254CN109071472