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1. (WO2019062854) CO-CRYSTALS OF RIBOCICLIB AND CO-CRYSTALS OF RIBOCICLIB MONO-SUCCINATE, PREPARATION METHOD THEREFOR, COMPOSITIONS THEREOF, AND USES THEREOF
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Pub. No.: WO/2019/062854 International Application No.: PCT/CN2018/108334
Publication Date: 04.04.2019 International Filing Date: 28.09.2018
IPC:
C07D 487/04 (2006.01) ,A61K 31/519 (2006.01) ,A61P 35/00 (2006.01)
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
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
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
杭州领业医药科技有限公司 SOLIPHARMA LLC [CN/CN]; 中国浙江省杭州市 杭州经济技术开发区6号大街452号1幢2B05室 452 6th Ave., Bldg 1, Suite 2B05-2B10 Hangzhou Economic and Technology Development Area Hangzhou, Zhejiang 310018, CN
Inventors:
盛晓红 SHENG, Xiaohong; CN
盛晓霞 SHENG, Xiaoxia; CN
陈健 CHEN, Jian; CN
Agent:
北京纪凯知识产权代理有限公司 JEEKAI & PARTNERS; 中国北京市 丰台区广安路9号国投广场5号楼15A层 Floor 15A, Building No. 5 GTFC Plaza, 9 Guang'an Road, Fengtai District Beijing 100055, CN
Priority Data:
201710904848.029.09.2017CN
Title (EN) CO-CRYSTALS OF RIBOCICLIB AND CO-CRYSTALS OF RIBOCICLIB MONO-SUCCINATE, PREPARATION METHOD THEREFOR, COMPOSITIONS THEREOF, AND USES THEREOF
(FR) CO-CRISTAUX DE RIBOCICLIB ET DE CO-CRISTAUX DE MONO-SUCCINATE DE RIBOCICLIB, LEUR PROCÉDÉ DE PRÉPARATION, LEURS COMPOSITIONS ET LEURS UTILISATIONS
(ZH) 瑞博西林的共晶和瑞博西林单琥珀酸盐的共晶、其制备方法、组合物和用途
Abstract:
(EN) The present invention relates to co-crystals of ribociclib and co-crystals of ribociclib mono-succinate, comprising co-crystals between ribociclib and saccharin, co-crystals between ribociclib and cholic acid, co-crystals between ribociclib and orotic acid, and co-crystals between ribociclib mono-succinate and citric acid. Compared with the prior art, the co-crystals have one or more improved characters. The present invention also relates to a preparation method for the co-crystals between ribociclib and saccharin, the co-crystals between ribociclib and cholic acid, the co-crystals between ribociclib and orotic acid and the co-crystals between ribociclib mono-succinate and citric acid, pharmaceutical compositions thereof, and uses thereof in the preparation of drugs for treating and/or preventing diseases involving in one or more symptoms of protein kinase-related dysfunctions, cancers, transplant rejection and autoimmune diseases.
(FR) La présente invention concerne des co-cristaux de ribociclib et des co-cristaux de mono-succinate de ribociclib, comprenant des co-cristaux entre le ribociclib et la saccharine, des co-cristaux entre le ribociclib et l'acide cholique, des co-cristaux entre le ribociclib et l'acide orotique, et des co-cristaux entre le ribociclib mono-succinate et l'acide citrique. Les co-cristaux selon l'invention présentent un ou plusieurs caractères améliorés, par comparaison avec l'état de la technique. La présente invention concerne également un procédé de préparation des co-cristaux entre le ribociclib et la saccharine, des co-cristaux entre le ribociclib et l'acide cholique, des co-cristaux entre le ribociclib et l'acide orotique et des co-cristaux entre le ribociclib mono-succinate et l'acide citrique, des compositions pharmaceutiques de ceux-ci, et leurs utilisations dans la préparation de médicaments pour le traitement et/ou la prévention de maladies impliquant un ou plusieurs symptômes de dysfonctionnements liés à la protéine kinase, de cancers, de rejet de greffe et de maladies auto-immunes.
(ZH) 本发明涉及瑞博西林的共晶和瑞博西林单琥珀酸盐的共晶,包括瑞博西林和糖精的共晶、瑞博西林和胆酸的共晶、瑞博西林和乳清酸的共晶以及瑞博西林单琥珀酸盐和柠檬酸的共晶,与现有技术相比,所述共晶具有一种或多种改进的特性。本发明还涉及瑞博西林和糖精的共晶、瑞博西林和胆酸的共晶、瑞博西林和乳清酸的共晶以及瑞博西林单琥珀酸盐和柠檬酸的共晶的制备方法,其药物组合物及其用于制备治疗和/或预防涉及蛋白激酶相关障碍、癌症、移植排除和自身免疫疾病的一种或多种症状等疾病的药物中的用途。
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)