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1. (WO2018086608) CRYSTALLINE FORM OF GNRH RECEPTOR ANTAGONIST AND PREPARATION METHOD THEREFOR
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2018/086608 International Application No.: PCT/CN2017/110685
Publication Date: 17.05.2018 International Filing Date: 13.11.2017
IPC:
A61K 31/519 (2006.01) ,C07D 487/04 (2006.01) ,A61P 15/00 (2006.01)
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
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15
Drugs for genital or sexual disorders; Contraceptives
Applicants:
江苏恒瑞医药股份有限公司 JIANGSU HENGRUI MEDICINE CO., LTD. [CN/CN]; 中国江苏省连云港市 经济技术开发区昆仑山路7号 No.7 Kunlunshan Road, Economic and Technological Development Zone Lianyungang, Jiangsu 222047, CN
成都盛迪医药有限公司 SUNCADIA PHARMACEUTICALS CO., LTD [CN/CN]; CN
Inventors:
张全良 ZHANG, Quanliang; CN
贾君磊 JIA, Junlei; CN
边林 BIAN, Lin; CN
高晓晖 GAO, Xiaohui; CN
Agent:
北京戈程知识产权代理有限公司 GE CHENG & CO.,LTD.; 中国北京市 东城区东长安街1号东方广场东三办公楼19层 Level 19, Tower E3, The Towers, Oriental Plaza, No.1, East Chang An Avenue, Dongcheng District Beijing 100738, CN
Priority Data:
201610999743.314.11.2016CN
Title (EN) CRYSTALLINE FORM OF GNRH RECEPTOR ANTAGONIST AND PREPARATION METHOD THEREFOR
(FR) FORME CRISTALLINE D’ANTAGONISTE DU RÉCEPTEUR DE GNRH ET SON PROCÉDÉ DE PRÉPARATION
(ZH) 一种GnRH受体拮抗剂的结晶形式及其制备方法
Abstract:
(EN) Provided are a crystalline form of a GnRH receptor antagonist and a preparation method therefor. Specifically, provided are a crystalline form I of 1-(4-(7-(2,6-difluorobenzyl)-3-((dimethylamino)methyl)-5-(6-methoxypyridazin-3-yl)-4,6-dicarbonyl-4,5,6,7-tetrahydro-2H-pyrazolo[3,4-d]pyrimidin-2-yl)phenyl)-3-methoxyurea (a compound of formula I) and a preparation method, the use of same in a pharmaceutical composition and the use of the crystalline form I and the composition in the preparation of a drug for treating diseases associated with a GnRH receptor antagonist.
(FR) L'invention concerne une forme cristalline d'un antagoniste du récepteur d'hormone libérant de la gonadotrophine (GnRH) et un procédé de préparation associé. Spécifiquement, l'invention concerne une forme cristalline I de 1-(4-(7-(2,6-difluorobenzyl)-3-((diméthylamino)méthyle)-5-(6-méthoxypyridazin-3-yl)-4,6-dicarbonyle-4,5,6,7-tétrahydro-2H-pyrazolo[3,4-d]pyrimidin-2-yl)phényl)-3-méthoxyurée (un composé de formule I) et un procédé de préparation, l'utilisation de celle-ci dans une composition pharmaceutique et l'utilisation de la forme cristalline I et de la composition dans la préparation d'un médicament pour le traitement de maladies associées à un antagoniste du récepteur de GnRH.
(ZH) 本发明提供了一种GnRH受体拮抗剂的结晶形式及其制备方法。具体地,本发明提供了1-(4-(7-(2,6-二氟苄基)-3-((二甲氨基)甲基)-5-(6-甲氧基哒嗪-3-基)-4,6-二羰基-4,5,6,7-四氢-2 H-吡唑并[3,4- d]嘧啶-2-基)苯基)-3-甲氧基脲(式I化合物)的I晶型及制备方法,其在药物组合物的应用以及该I晶型和组合物在制备治疗具有GnRH受体拮抗剂有关疾病中的用途。
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)