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1. (WO2018059420) E52862 HYDROCHLORIDE SALT CRYSTAL FORM H AND PREPARATION METHOD THEREFOR
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Pub. No.: WO/2018/059420 International Application No.: PCT/CN2017/103579
Publication Date: 05.04.2018 International Filing Date: 27.09.2017
IPC:
C07D 231/22 (2006.01) ,A61K 31/4155 (2006.01) ,A61P 25/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
231
Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02
not condensed with other rings
10
having two or three double bonds between ring members or between ring members and non-ring members
14
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
18
One oxygen or sulfur atom
20
One oxygen atom attached in position 3 or 5
22
with aryl radicals attached to ring nitrogen atoms
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
415
1,2-Diazoles
4155
not condensed and containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
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李贝贝 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
刁小娟 DIAO, Xiaojuan; CN
黄春香 HUANG, Chunxiang; CN
张晓宇 ZHANG, Xiaoyu; CN
Priority Data:
201610852043.127.09.2016CN
Title (EN) E52862 HYDROCHLORIDE SALT CRYSTAL FORM H AND PREPARATION METHOD THEREFOR
(FR) FORME H DE CRISTAL DE SEL D'HYDROCHLORURE E52862 H ET SON PROCÉDÉ DE PRÉPARATION
(ZH) E52862盐酸盐晶型H及其制备方法
Abstract:
(EN) The present invention relates to a crystal form of a Sigma-1 receptor antagonist drug, preparation method therefor and use thereof. The crystal form of E52862 hydrochloride salt provided in the present invention, named crystal form H, can be used in preparation of a pharmaceutical formulation for treating multiple neuralgia. The E52862 hydrochloride salt crystal form provided in the present invention has a low hygroscopicity, a high solubility, a good compressibility, a proper particle size and has a better stability and flowability, which provides a new and better choice for the preparation of a pharmaceutical formulation comprising E52862 and is of great significance to the development of drugs.
(FR) La présente invention concerne une forme cristalline d'un médicament antagoniste du récepteur Sigma-1, son procédé de préparation et son utilisation. La forme cristalline du sel d'hydrochlorure E52862 selon la présente invention, nommée forme cristalline H, peut être utilisée dans la préparation d'une formulation pharmaceutique pour le traitement de la névralgie multiple. La forme cristalline du sel d'hydrochlorure E52862 selon la présente invention présente une faible hygroscopicité, une solubilité élevée, une bonne compressibilité, une taille de particule appropriée et présente une meilleure stabilité et une bonne aptitude à l'écoulement, qui fournit un nouveau et meilleur choix pour la préparation d'une formulation pharmaceutique comprenant l'E52862 et présente une grande importance pour la mise au point de médicaments.
(ZH) 本发明涉及一种Sigma 1受体拮抗剂药物的晶型及其制备方法和用途。本发明提供的E52862盐酸盐的一种晶型,命名为晶型H,可用于制备治疗多发性神经痛药物制剂。本发明提供的E52862盐酸盐晶型引湿性低、溶解度高、可压性好、粒度合适且具有较好的稳定性和流动性,为含E52862的药物制剂的制备提供了新的更好的选择,对于药物开发具有非常重要的意义。
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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)