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1. (WO2015129603) HIGH-PURITY CRYSTALS OF ACTIVE BLOOD COAGULATION FACTOR X (FXA) INHIBITOR
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2015/129603 International Application No.: PCT/JP2015/054943
Publication Date: 03.09.2015 International Filing Date: 23.02.2015
IPC:
C07D 513/04 (2006.01) ,A61K 31/444 (2006.01) ,A61P 7/02 (2006.01) ,A61P 43/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
513
Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/, C07D477/232
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4427
containing further heterocyclic ring systems
444
containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
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
43
Drugs for specific purposes, not provided for in groups A61P1/-A61P41/108
Applicants:
第一三共株式会社 DAIICHI SANKYO COMPANY,LIMITED [JP/JP]; 東京都中央区日本橋本町三丁目5番1号 3-5-1,Nihonbashi Honcho,Chuo-ku, Tokyo 1038426, JP
Inventors:
川波 光太郎 KAWANAMI, Koutarou; JP
木谷 泰夫 KITANI, Yasuo; JP
Agent:
石橋 公樹 ISHIBASHI, Koki; JP
Priority Data:
2014-03355625.02.2014JP
Title (EN) HIGH-PURITY CRYSTALS OF ACTIVE BLOOD COAGULATION FACTOR X (FXA) INHIBITOR
(FR) CRISTAUX DE HAUTE PURETÉ D'INHIBITEUR ACTIF DU FACTEUR DE COAGULATION SANGUINE X (FXA)
(JA) 活性化血液凝固第X因子(FXa)阻害剤の高純度結晶
Abstract:
(EN) The present invention addresses the problem of providing high-purity crystals of a compound which is represented by formula (1a) and is an active blood coagulation factor X (FXa) inhibitor. High-purity crystals of a compound represented by formula (1a) which: are characterised by being obtained by a step for dissolving crystals in a solvent and thereafter performing recrystallisation; have a 0.03% or less maximum content of one impurity as the impurity content by percentage; and have a 0.13% or less total impurity content.
(FR) Le problème abordé dans la présente invention est de pourvoir à des cristaux de haute pureté d'un composé qui est représenté par la formule (1a) et qui est un inhibiteur actif du facteur de coagulation sanguine X (FXa). La solution selon l'invention porte sur des cristaux de haute pureté d'un composé représenté par la formule (1a) qui : sont caractérisés en ce qu'ils sont obtenus par une étape consistant à dissoudre des cristaux dans un solvant, puis à les soumettre à recristallisation ; en ce qu'ils ont une teneur maximale en impureté d'un seul type en tant que teneur en impureté en pourcentage de 0,03 % ou moins ; et une teneur en impuretés totale de 0,13 % ou moins.
(JA) 活性化血液凝固第X因子(FXa)阻害剤である、式(1a)で表される化合物の高純度結晶を提供することが課題である。 解決手段:下記式(1a)で表される化合物の高純度結晶であって、結晶を溶媒に溶解した後に、再度結晶化する工程により得ること特徴とする、不純物の含有率として、1つの不純物の最大含量が0.03%以下であり、かつ、不純物の合計含量が0.13%以下である式(1a)で表される化合物の高純度結晶。
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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: Japanese (JA)
Filing Language: Japanese (JA)
Also published as:
EP3112371US20170022220JPWO2015129603