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1. WO2020259366 - CRYSTAL FORM OF COAGULATION FACTOR XIA INHIBITOR AND PREPARATION METHOD THEREFOR

Publication Number WO/2020/259366
Publication Date 30.12.2020
International Application No. PCT/CN2020/096572
International Filing Date 17.06.2020
IPC
C07D 205/08 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
205Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
02not condensed with other rings
06having one double bond between ring members or between a ring member and a non-ring member
08with one oxygen atom directly attached in position 2, e.g. beta-lactams
A61K 31/397 2006.1
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
397having four-membered rings, e.g. azetidine
A61K 31/4025 2006.1
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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
4025not condensed and containing further heterocyclic rings, e.g. cromakalim
A61P 7/02 2006.1
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
CPC
A61K 31/397
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
397having four-membered rings, e.g. azetidine
A61K 31/4025
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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
4025not condensed and containing further heterocyclic rings, e.g. cromakalim
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
C07D 205/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
205Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
02not condensed with other rings
06having one double bond between ring members or between a ring member and a non-ring member
08with one oxygen atom directly attached in position 2, e.g. beta-lactams
Applicants
  • 广东东阳光药业有限公司 SUNSHINE LAKE PHARMA CO., LTD. [CN]/[CN]
Inventors
  • 张杰 ZHANG, Jie
  • 董吉川 DONG, Jichuan
  • 黄河 HUANG, He
  • 雷鑫 LEI, Xin
  • 陈勇 CHEN, Yong
  • 王仲清 WANG, Zhongqing
  • 罗忠华 LUO, Zhonghua
  • 黄芳芳 HUANG, Fangfang
Priority Data
201910554330.825.06.2019CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) CRYSTAL FORM OF COAGULATION FACTOR XIA INHIBITOR AND PREPARATION METHOD THEREFOR
(FR) FORME CRISTALLINE D'UN INHIBITEUR DU FACTEUR DE COAGULATION XIA ET SON PROCÉDÉ DE PRÉPARATION
(ZH) 一种凝血因子XIa抑制剂的晶型及其制备方法
Abstract
(EN) Disclosed are a crystal form of a coagulation factor XIa inhibitor and a preparation method therefor, wherein the X-ray powder diffraction pattern of the crystal form comprises diffraction peaks of the 2θ angle at 6.9±0.2°, 15.9±0.2°, 21.8±0.2°, 23.7±0.2° and 28.2±0.2°. The crystal form has a better performance, a high stability, and can be used to prepare medical agents for treating cardiovascular diseases.
(FR) L'invention concerne une forme cristalline d'un Inhibiteur du facteurde coagulation XIa et son procédé de préparation, le motif de diffraction de poudre de rayons X de la forme cristalline comprenant des pics de diffraction de l'angle 2θ à 6,9 ± 0,2°, 15,9 ± 0,2°, 21,8 ± 0,2°, 23,7 ± 0,2° et 28,2 ± 0,2°. La forme cristalline a une meilleure performance, une stabilité élevée, et peut être utilisée pour préparer des agents médicaux pour le traitement de maladies cardiovasculaires.
(ZH) 一种凝血因子XIa抑制剂的晶型及其制备方法,所述晶型的X射线粉末衍射图包含2θ角为6.9±0.2°,15.9±0.2°,21.8±0.2°,23.7±0.2°和28.2±0.2°的衍射峰。所述晶型具有较好的性能,稳定性高,可用于制备治疗心血管疾病的药物制剂。
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