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1. (WO2015176591) BETRIXABAN SALTS AND PREPARATION METHOD AND USE THEREOF
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2015/176591 International Application No.: PCT/CN2015/077077
Publication Date: 26.11.2015 International Filing Date: 21.04.2015
IPC:
C07D 213/75 (2006.01) ,A61K 31/44 (2006.01) ,A61P 7/02 (2006.01) ,A61P 11/00 (2006.01) ,A61P 9/10 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
04
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
72
Nitrogen atoms
75
Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7
Drugs for disorders of the blood or the extracellular fluid
02
Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11
Drugs for disorders of the respiratory system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
10
for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Applicants:
四川海思科制药有限公司 SICHUAN HAISCO PHARMACEUTICAL CO., LTD. [CN/CN]; 中国四川省成都市 温江区海峡两岸科技园区百利路136号 No.136 Beverley Road, Across the Taiwan Strait Technology Industry Development Park, Wenjiang District Chengdu, Sichuan 611130, CN
Inventors:
陈大峰 CHEN, Dafeng; CN
惠帅 HUI, Shuai; CN
赵永龙 ZHAO, Yonglong; CN
程睿 CHENG, Rui; CN
贾晓曼 JIA, Xiaoman; CN
刘晓凤 LIU, Xiaofeng; CN
冯舟 FENG, Zhou; CN
闫树军 YAN, Shujun; CN
罗杰 LUO, Jie; CN
向志祥 XIANG, Zhixiang; CN
Agent:
北京三友知识产权代理有限公司 BEIJING SANYOU INTELLECTUAL PROPERTY AGENCY LTD.; 中国北京市 金融街35号国际企业大厦A座16层 16th Fl., Block A, Corporate Square No.35 Jinrong Street Beijing 100033, CN
Priority Data:
201410214710.420.05.2014CN
Title (EN) BETRIXABAN SALTS AND PREPARATION METHOD AND USE THEREOF
(FR) SELS DE BETRIXABAN, PROCEDE DE PREPARATION ET UTILISATION DE CEUX-CI
(ZH) 贝曲西班盐及其制备方法和用途
Abstract:
(EN) The present invention relates to betrixaban salts as shown by formula II, wherein the method for preparing these salts is simple, the crystal form is easy to control, the stability and solubility are good, and the salts are suitable for preparing a variety of preparations. The present invention also relates to the method for preparing these salts, pharmaceutical compositions comprising these salts, and the use of these salts in the preparation of medicaments for the prevention and treatment of diseases characterized by adverse thrombus formation in mammals.
(FR) La présente invention concerne des sels de bétrixaban représentés par la formule II. Le procédé de préparation de ces sels est simple, la forme cristalline est facile à maîtriser, la stabilité et la solubilité sont bonnes, et ces sels conviennent pour la préparation de diverses préparations. La présente invention concerne également le procédé de préparation de ces sels, des compositions pharmaceutiques comprenant ces sels ainsi que l'utilisation de ces sels dans la préparation de médicaments destinés à prévenir ou à traiter des maladies caractérisées par la formation néfaste d'un thrombus chez des mammifères.
(ZH) 本发明涉及式II所示的贝曲西班盐,这些盐制备方法简单、晶型易于控制、稳定性和溶解性良好,适宜于制备多种制剂;本发明还涉及这些盐的制备方法,含有这些盐的药物组合物,以及这些盐在制备用于预防或治疗哺乳动物以不良血栓形成为特征的病症的药物的用途。
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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, 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, KN, KP, KR, 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 Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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)
Also published as:
CN106458905