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1. WO2015129603 - HIGH-PURITY CRYSTALS OF ACTIVE BLOOD COAGULATION FACTOR X (FXA) INHIBITOR

Publication Number WO/2015/129603
Publication Date 03.09.2015
International Application No. PCT/JP2015/054943
International Filing Date 23.02.2015
IPC
C07D 513/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
513Heterocyclic 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
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/444 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
444containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61P 7/02 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
A61P 43/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/-A61P41/108
CPC
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
A61P 7/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
C07B 2200/13
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
13Crystalline forms, e.g. polymorphs
C07C 309/30
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
309Sulfonic acids; Halides, esters, or anhydrides thereof
01Sulfonic acids
28having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
29of non-condensed six-membered aromatic rings
30of six-membered aromatic rings substituted by alkyl groups
C07D 513/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
513Heterocyclic 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 C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Applicants
  • 第一三共株式会社 DAIICHI SANKYO COMPANY,LIMITED [JP]/[JP]
Inventors
  • 川波 光太郎 KAWANAMI, Koutarou
  • 木谷 泰夫 KITANI, Yasuo
Agents
  • 石橋 公樹 ISHIBASHI, Koki
Priority Data
2014-03355625.02.2014JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
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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