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1. (WO2018218963) PHARMACEUTICALLY ACCEPTABLE SALT OF EGFR INHIBITOR, CRYSTAL FORM THEREOF, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2018/218963 International Application No.: PCT/CN2018/070011
Publication Date: 06.12.2018 International Filing Date: 02.01.2018
IPC:
C07D 471/04 (2006.01) ,C07C 309/04 (2006.01) ,C07C 309/30 (2006.01) ,C07C 59/265 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
309
Sulfonic acids; Halides, esters, or anhydrides thereof
01
Sulfonic acids
02
having sulfo groups bound to acyclic carbon atoms
03
of an acyclic saturated carbon skeleton
04
containing only one sulfo group
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
309
Sulfonic acids; Halides, esters, or anhydrides thereof
01
Sulfonic acids
28
having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
29
of non-condensed six-membered aromatic rings
30
of six-membered aromatic rings substituted by alkyl groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
59
Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O-metal, -CHO, keto, ether, groups, groups, or groups
235
Saturated compounds having more than one carboxyl group
245
containing hydroxy or O-metal groups
265
Citric acid
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
无锡双良生物科技有限公司 WUXI SHUANGLIANG BIOTECHNOLOGY CO., LTD. [CN/CN]; 中国江苏省江阴市 城东街道东盛西路6号A5楼4单元 Unit 4, Building A5, 6 Dongsheng West Road, Chengdong Sub-District Jiangyin, Jiangsu 214437, CN
Inventors:
周平 ZHOU, Ping; CN
吴家权 WU, Jiaquan; US
金深霜 JIN, Shenshuang; CN
李莉 LI, Li; 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:
201710408362.802.06.2017CN
Title (EN) PHARMACEUTICALLY ACCEPTABLE SALT OF EGFR INHIBITOR, CRYSTAL FORM THEREOF, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
(FR) SEL PHARMACEUTIQUEMENT ACCEPTABLE D'INHIBITEUR D'EGFR, FORME CRISTALLINE DE CELUI-CI, SON PROCÉDÉ DE PRÉPARATION ET SON APPLICATION
(ZH) 一种EGFR抑制剂的药用盐及其晶型、制备方法和应用
Abstract:
(EN) Provided in the present invention are a pharmaceutically acceptable salt of an epidermal growth factor receptor (EGFR) inhibitor, a crystal form thereof, a preparation method therefor and an application thereof. The structural formula of the EGFR inhibitor is as shown in formula I, and the pharmaceutically acceptable salt is a mesylate, p-toluenesulfonate, phosphate, hydrochloride or citrate salt of the EGFR inhibitor. The pharmaceutically acceptable salt of the EGFR inhibitor of the present invention has a specific crystal form, is more soluble and stable than a corresponding free base, is more suitable for preparing medicine for use in treating cancer (especially non-small cell lung cancer), and satisfies the requirements for bioavailability and efficacy.
(FR) La présente invention concerne un sel pharmaceutiquement acceptable d'un inhibiteur du récepteur de facteur de croissance épidermique (EGFR), une forme cristalline de celui-ci, un procédé de préparation associé et une application correspondante. La formule structurale de l'inhibiteur d'EGFR est telle que représentée dans la formule I, et le sel pharmaceutiquement acceptable est un sel mésylate, p-toluènesulfonate, phosphate, chlorhydrate ou citrate de l'inhibiteur EGFR. Le sel pharmaceutiquement acceptable de l'inhibiteur d'EGFR selon la présente invention a une forme cristalline spécifique, est plus soluble et stable qu'une base libre correspondante, est plus approprié pour préparer un médicament destiné à être utilisé dans le traitement du cancer (en particulier le cancer du poumon non à petites cellules), et répond aux exigences de biodisponibilité et d'efficacité.
(ZH) 本发明提供一种EGFR抑制剂的药用盐及其晶型、制备方法和应用。所述EGFR抑制剂的结构式如式I所示,所述药用盐为所述EGFR抑制剂的甲磺酸盐、对甲苯磺酸盐、磷酸盐、盐酸盐或柠檬酸盐。本发明的EGFR抑制剂的药用盐具有特定的晶型,比相应的游离碱的溶解性和稳定性更高,更适合于制备治疗癌症(特别是非小细胞肺癌)的药物,满足生物利用度和药效要求。
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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)