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1. (WO2017152707) CRYSTALLINE FORMS OF MESYLATE SALT OF PYRIDINYL AMINO PYRIMIDINE DERIVATIVE, PREPARATION METHODS THEREFOR, AND APPLICATIONS THEREOF
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Pub. No.: WO/2017/152707 International Application No.: PCT/CN2017/000203
Publication Date: 14.09.2017 International Filing Date: 01.03.2017
IPC:
C07D 401/14 (2006.01) ,A61K 31/506 (2006.01) ,A61P 35/00 (2006.01) ,A61P 35/02 (2006.01)
[IPC code unknown for C07D 401/14][IPC code unknown for A61K 31/506][IPC code unknown for A61P 35][IPC code unknown for A61P 35/02]
Applicants:
上海艾力斯医药科技有限公司 SHANGHAI ALLIST PHARMACEUTICAL AND MEDICAL TECHNOLOGY CORPORATIONS [CN/CN]; 中国上海市自由贸易试验区蔡伦路720弄2号304室 304, Building 2 No.720 Cailun Road, Pilot Free Trade Zone Shanghai 201203, CN
Inventors:
罗会兵 LUO, Huibing; CN
张强 ZHANG, Qiang; CN
Agent:
中国专利代理(香港)有限公司 CHINA PATENT AGENT (H.K.) LTD.; CN
Priority Data:
201610127022.307.03.2016CN
Title (EN) CRYSTALLINE FORMS OF MESYLATE SALT OF PYRIDINYL AMINO PYRIMIDINE DERIVATIVE, PREPARATION METHODS THEREFOR, AND APPLICATIONS THEREOF
(FR) FORMES CRISTALLINES DE SEL DE MÉSYLATE DE DÉRIVÉ DE PYRIDINYL-AMINOPYRIMIDINE, PROCÉDÉS DE PRÉPARATION ET APPLICATIONS ASSOCIÉS
(ZH) 吡啶胺基嘧啶衍生物甲磺酸盐的结晶形式及其制备和应用
Abstract:
(EN) The present invention provides crystalline form I and crystalline form II of a mesylate salt of a pyridinyl amino pyrimidine derivative and preparation methods therefor, a pharmaceutical composition containing the crystalline forms, and applications of the crystalline forms in the treatment of activated EGFR mutant- or drug-resistant mutant-mediated diseases, especially cancer, in mammals, particularly humans. The crystalline forms of the mesylate salt of the compound represented by formula (I) have good solubility and high bioavailability in animals.
(FR) L'invention concerne la forme cristalline I et la forme cristalline II d'un sel de mésylate d'un dérivé de pyridinyl-aminopyrimidine et leurs procédés de préparation, une composition pharmaceutique contenant ces formes cristallines, ainsi que des applications des formes cristallines selon l'invention dans le traitement de maladies induites par un mutant EGFR activé ou un mutant pharmacorésistant, en particulier le cancer, chez des mammifères, en particulier des humains. Les formes cristallines du sel de mésylate du composé de formule (I) sont dotées d'une bonne solubilité et d'une biodisponibilité élevée chez les animaux.
(ZH) 本发明提供式(I)化合物的甲磺酸盐的结晶形式I、结晶形式II,其制备方法,包含该结晶形式的药物组合物及该结晶形式在治疗哺乳动物尤其人类由EGFR激活型或耐药型突变体介导的疾病、特别是癌症中的应用。本发明式(I)化合物的甲磺酸盐的结晶形式具有良好的溶解度,在动物体内的生物利用度高。
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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 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)