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1. WO2014110971 - OXAZOLIDONE COMPOUND, PREPARING METHOD AND APPLICATION THEREOF

Publication Number WO/2014/110971
Publication Date 24.07.2014
International Application No. PCT/CN2013/090833
International Filing Date 30.12.2013
IPC
C07D 498/06 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
498Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
02in which the condensed system contains two hetero rings
06Peri-condensed systems
A61K 31/5383 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
535having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
5383ortho- or peri-condensed with heterocyclic ring systems
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
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
C07D 498/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
498Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 519/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
519Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Applicants
  • 中国科学院上海药物研究所 SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES [CN]/[CN]
  • 浙江巨泰药业有限公司 ZHE JIANG JUTAI PHARMACEUTICAL CO., LTD [CN]/[CN]
Inventors
  • 杨玉社 YANG, Yushe
  • 薛涛 XUE, Tao
  • 丁实 DING, Shi
  • 郭彬 GUO, Bin
Agents
  • 上海一平知识产权代理有限公司 XU & PARTNERS, LLC.
Priority Data
201310020040.818.01.2013CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) OXAZOLIDONE COMPOUND, PREPARING METHOD AND APPLICATION THEREOF
(FR) COMPOSÉS D'OXAZOLIDINONE, LEUR PROCÉDÉ DE PRÉPARATION ET LEURS UTILISATIONS
(ZH) 噁唑烷酮类化合物及其制备方法和用途
Abstract
(EN) The present invention relates to the field of a pharmaceutical compound, and more specifically, relates to a new oxazolidone compound, an enantiomer, a diastereoisomer and a raceme thereof, and a mixture thereof, and a pharmaceutically acceptable salt thereof, a preparation method thereof, an application thereof as a bioactive substance in a drug. The compound in the present invention has strong anticoagulant activity, does not affect the activity of thrombin, and can reduce the risk of hemorrhage. A pharmacokinetics experiment shows that the compound in the present invention further has good metabolic characteristics, and has a far better oral bioavailability than a positive contrastive agent rivaroxaban.
(FR) Le domaine technique de l'invention est celui des composés pharmaceutiques, en particulier des nouveaux composés d'oxazolidinone, leurs énantiomères, leurs diastéréoisomères, leurs racémates et leurs combinaisons, ainsi que leurs sels pharmaceutiquement acceptables, leur procédé de préparation et leurs utilisations comme substances biologiquement actives dans des médicaments. Les composés de cette invention possèdent une forte activité anticoagulante sans pour autant affecter l'activité de la thrombine tout en réduisant le risque de saignement. Les expériences en pharmacocinétique ont démontré que les composés de cette invention présentent des caractéristiques métaboliques idéales et leur biodisponibilité orale est nettement supérieure aux résultats du médicament rivaroxaban.
(ZH) 本发明涉及药物化合物领域,更具体而言,涉及一种新型噁唑烷酮类化合物,其对映异构体、非对映异构体、外消旋体及其混合物,以及其药学上可接受的盐,其制备方法及其作为药物中生物活性物质的用途。本发明的化合物具有很强的抗凝活性,而且其不影响凝血酶的活性,有可能降低出血的风险。药代实验证明,本发明化合物还具有理想的代谢特征,口服生物利用度远远优于阳性对照药物利伐沙班。
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