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1. (WO2018028420) POLYCRYSTALLINE FORM OF DEHYDROPHENYLAHISTIN-LIKE COMPOUND, AND MANUFACTURING AND PURIFICATION METHOD AND APPLICATION THEREOF.
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.:    WO/2018/028420    International Application No.:    PCT/CN2017/094066
Publication Date: 15.02.2018 International Filing Date: 24.07.2017
IPC:
C07D 403/06 (2006.01), A61K 31/496 (2006.01), A61P 35/00 (2006.01), A61P 31/10 (2006.01)
Applicants: MARINE BIOMEDICAL RESEARCH INSTITUTE OF QINGDAO CO., LTD. [CN/CN]; LIU, Lili No.23 Hongkong East Road, Laoshan District Qingdao, Shandong 266061 (CN)
Inventors: LI, Wenbao; (CN).
WANG, Shixiao; (CN).
DING, Zhongpeng; (CN).
HOU, Yingwei; (CN).
GUAN, Huashi; (CN)
Agent: QINGDAO HECHUANG INTELLECTUAL PROPERTY AGENCY FIRM (GENERAL PARTNERSHIP ); WANG, Xiaoxiao Room 1803, Building B, Hisense Chuangzhi Valley, 20 Zhuzhou Road, Laoshan District Qingdao, Shandong 266101 (CN)
Priority Data:
201610664088.6 12.08.2016 CN
201610665377.8 12.08.2016 CN
201610664196.3 12.08.2016 CN
Title (EN) POLYCRYSTALLINE FORM OF DEHYDROPHENYLAHISTIN-LIKE COMPOUND, AND MANUFACTURING AND PURIFICATION METHOD AND APPLICATION THEREOF.
(FR) FORME POLYCRISTALLINE DE COMPOSÉ DE TYPE DÉHYDROPHÉNYLAHISTINE, SON PROCÉDÉ DE FABRICATION ET DE PURIFICATION ET SON APPLICATION.
(ZH) 脱氢苯基阿夕斯丁类化合物的多晶型及其制备纯化方法和应用
Abstract: front page image
(EN)A polycrystalline form of a dehydrophenylahistin-like compound, and a manufacturing and purification method and application thereof. A (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)deuteromethylene]piperazine-2,5-dione monohydrate crystal and a (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)methylene]piperazine-2,5-dione monohydrate crystal are more competitive crystalline forms with stable quality. The manufacturing and purification method is simple and easy to operate, and can effectively control the generation of a trans-isomer contaminant to obtain a high purity product. The polycrystalline form of the dehydrophenylahistin-like compound has a certain value in an application for manufacturing an antitumor pharmaceutical product.
(FR)L'invention concerne une forme polycristalline d'un composé de type déhydrophénylahistine, ainsi qu'un procédé de fabrication et de purification et son application. Le cristal monohydrate (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)deuteromethylene]piperazine-2,5-dione et le cristal monohydrate (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)methylene]piperazine-2,5-dione sont des formes cristallines plus compétitives avec une qualité stable. Le procédé de fabrication et de purification est simple et facile à utiliser, et peut efficacement contrôler la génération d'un contaminant d'isomère trans pour obtenir un produit de haute pureté. La forme polycristalline du composé de type déhydrophénylahistine a une certaine valeur dans une application pour la fabrication d'un produit pharmaceutique antitumoral.
(ZH)脱氢苯基阿夕斯丁类化合物的多晶型及其制备纯化方法和应用。其中(3Z,6Z)-3-苯亚甲基-6-[(5-叔丁基-1H-咪唑-4-基)氘代亚甲基]哌嗪-2,5-二酮一水合物晶型和(3Z,6Z)-3-苯亚甲基-6-[(5-叔丁基-1H-咪唑-4-基)亚甲基]哌嗪-2,5-二酮一水合物晶型为质量稳定的优势晶型,其制备纯化方法简单易操作,可有效的控制反式异构体杂质的产生,得到高纯度的产物。脱氢苯基阿夕斯丁类化合物的多种晶型在制备抗肿瘤的药物中具有一定的应用价值。
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 (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)