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1. (WO2018019188) POLYMORPH OF NUCLEOSIDE PHOSPHORAMIDATE PRODRUG AND PREPARATION METHOD THEREFOR
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2018/019188 International Application No.: PCT/CN2017/093925
Publication Date: 01.02.2018 International Filing Date: 21.07.2017
IPC:
C07H 19/10 (2006.01) ,C07H 1/06 (2006.01) ,A61K 31/7068 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19
Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02
sharing nitrogen
04
Heterocyclic radicals containing only nitrogen as ring hetero atom
06
Pyrimidine radicals
10
with the saccharide radical being esterified by phosphoric or polyphosphoric acids
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
1
Processes for the preparation of sugar derivatives
06
Separation; Purification
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
70
Carbohydrates; Sugars; Derivatives thereof
7042
Compounds having saccharide radicals and heterocyclic rings
7052
having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
706
containing six-membered rings with nitrogen as a ring hetero atom
7064
containing condensed or non-condensed pyrimidines
7068
having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
博瑞生物医药(苏州)股份有限公司 BRIGHTGENE BIO-MEDICAL TECHNOLOGY CO., LTD. [CN/CN]; 中国江苏省苏州市 工业园区星湖街218号纳米科技园C25栋 Building C25, No. 218 Xinghu Street, Bio-BAY, Industrial Park Suzhou, Jiangsu 215123, CN
Inventors:
袁建栋 YUAN, Jiandong; CN
顾家宁 GU, Jianing; CN
黄仰青 HUANG, Yangqing; CN
缪琳峰 MIAO, Linfeng; CN
梁朝华 LIANG, Chaohua; CN
孙占莉 SUN, Zhanli; CN
Agent:
北京林达刘知识产权代理事务所(普通合伙) LINDA LIU & PARTNERS; 中国北京市 东城区北三环东路36号北京环球贸易中心C座16层 F16 Tower C, Beijing Global Trade Center, 36 North Third Ring East Road, Dongcheng District Beijing 100013, CN
Priority Data:
201610583741.623.07.2016CN
Title (EN) POLYMORPH OF NUCLEOSIDE PHOSPHORAMIDATE PRODRUG AND PREPARATION METHOD THEREFOR
(FR) POLYMORPHE DE PROMÉDICAMENT DE NUCLÉOSIDE PHOSPHORAMIDATE ET SON PROCÉDÉ DE PRÉPARATION
(ZH) 核苷氨基磷酸酯类前药的多晶型及其制备方法
Abstract:
(EN) Provided are a crystal form A of a nucleoside phosphoramidate prodrug as shown in formula I and a preparation method therefor. The crystal form A at least has an X-ray powder diffraction (XRPD) pattern with peaks at the 2θ angles of 6.9 ± 0.2°, 13.9 ± 0.2°, 20.8 ± 0.2° and 21.1 ± 0.2°. The crystal form A is stable in nature and suitable for being prepared into various dosage forms. The preparation method is simple in operation, and the prepared crystal form A is high in purity and low in industrialization costs.
(FR) L'invention concerne une forme cristalline A d'un promédicament de phosphoramidate de nucléoside tel que présenté dans la formule I et un procédé de préparation associé. La forme cristalline A présente au moins une diffraction des rayons X sur poudre (XRPD) avec des pics aux angles 2θ de 6.9 ± 0.2°, 13.9 ± 0.2°, 20.8 ± 0.2° et 21.1 ± 0.2°. La forme cristalline A est de nature stable et appropriée pour être préparée en diverses formes posologiques. Le procédé de préparation est simple à utiliser, et la forme cristalline préparée A est de haute pureté et présente un faible coût d'industrialisation.
(ZH) 提供一种式I所示核苷氨基酸磷酸酯类前药的晶型A及其制备方法,所述晶型A在X-射线粉末衍射(XRPD)图上至少在下述2θ角有峰:6.9±0.2、13.9±0.2、20.8±0.2和21.1±0.2。所述晶型A性质稳定,适合制成各种剂型,所述制备方法操作简单,制得的晶型A纯度高,工业化成本低。
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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)