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CN112004810A - 一种氧代吡啶酰胺类衍生物的晶型及制备方法 - Google Patents

一种氧代吡啶酰胺类衍生物的晶型及制备方法 Download PDF

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Publication number
CN112004810A
CN112004810A CN201980027589.5A CN201980027589A CN112004810A CN 112004810 A CN112004810 A CN 112004810A CN 201980027589 A CN201980027589 A CN 201980027589A CN 112004810 A CN112004810 A CN 112004810A
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crystal form
preparation
oxopyridine
amide derivatives
compound
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CN112004810B (zh
Inventor
马亚辉
张浩宇
韩龙
邵启云
杜振兴
王捷
冯君
贺峰
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen directly attached to ring carbon atoms
    • C07D211/86—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—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
    • C07D213/02—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 having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—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 having three double bonds between ring members or between ring members and non-ring members 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
    • C07D213/60—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 having three double bonds between ring members or between ring members and non-ring members 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 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/69—Two or more oxygen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

本发明涉及一种氧代吡啶酰胺类衍生物的晶型及制备方法。具体地，本发明涉及式(I)化合物的A、B、C、D、E、F晶型及制备方法。本发明式(I)化合物的晶型具备良好的晶型稳定性，可更好地用于临床。
Figure DDA0002737496000000011

Description

PCT国内申请，说明书已公开。

Claims (15)

  1. PCT国内申请，权利要求书已公开。
CN201980027589.5A 2018-07-02 2019-07-01 一种氧代吡啶酰胺类衍生物的晶型及制备方法 Active CN112004810B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2018107100371 2018-07-02
CN201810710037 2018-07-02
PCT/CN2019/094170 WO2020007256A1 (zh) 2018-07-02 2019-07-01 一种氧代吡啶酰胺类衍生物的晶型及制备方法

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CN112004810A true CN112004810A (zh) 2020-11-27
CN112004810B CN112004810B (zh) 2022-04-08

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US (1) US11225462B2 (zh)
EP (1) EP3822264A4 (zh)
JP (1) JP2021529201A (zh)
KR (1) KR20210028232A (zh)
CN (1) CN112004810B (zh)
WO (1) WO2020007256A1 (zh)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018041122A1 (zh) * 2016-08-31 2018-03-08 江苏恒瑞医药股份有限公司 氧代吡啶酰胺类衍生物、其制备方法及其在医药上的应用
CN107793396A (zh) * 2016-08-31 2018-03-13 江苏恒瑞医药股份有限公司 环氧基取代的氧代吡啶类衍生物、其制备方法及其在医药上的应用

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WO1996030396A1 (en) 1995-03-24 1996-10-03 Molecumetics Ltd. β-SHEET MIMETICS AND USE THEREOF AS PROTEASE INHIBITORS
CA2319766A1 (en) 1998-02-12 1999-08-19 Molecumetics Ltd. .beta.-sheet mimetics and methods relating to the use thereof
WO2004002405A2 (en) 2002-06-26 2004-01-08 Bristol-Myers Squibb Company Amino-bicyclic pyrazinones and pyridinones
US7208601B2 (en) 2003-08-08 2007-04-24 Mjalli Adnan M M Aryl and heteroaryl compounds, compositions, and methods of use
IT1395963B1 (it) * 2009-06-04 2012-11-02 Rottapharm Spa Forme cristalline di 6-(1h-imidazol-1-il)-2-fenil chinazolina e dei suoi sali
SI2766346T1 (sl) 2011-10-14 2017-05-31 Bristol-Myers Squibb Company Substituirane tetrahidroizokinolinske spojine kot faktor xia inhibitorji
ES2655669T3 (es) 2011-12-21 2018-02-21 Ono Pharmaceutical Co., Ltd. Derivados de piridinona y pirimidinona como inhibidores del factor XIa
CN105849109B (zh) 2013-10-30 2018-01-23 拜耳制药股份公司 取代的氧代吡啶衍生物
JO3703B1 (ar) 2015-07-09 2021-01-31 Bayer Pharma AG مشتقات أوكسوبيريدين مستبدلة
CN108137549B (zh) 2015-08-05 2021-07-20 百时美施贵宝公司 取代的甘氨酸衍生的fxia抑制剂
US10143681B2 (en) 2016-08-22 2018-12-04 Merck Sharp & Dohme Corp. Factor XIa inhibitors
BR112021000439A2 (pt) * 2018-07-19 2021-04-06 Jiangsu Hengrui Medicine Co., Ltd. Método para preparar o inibidor do fator de coagulação xia e intermediário do mesmo
US20220127648A1 (en) 2019-01-23 2022-04-28 Integrated Lipid Biofuels Llc Genetically engineered yeast yarrowia lipolytica and methods for producing bio-based glycolic acid

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018041122A1 (zh) * 2016-08-31 2018-03-08 江苏恒瑞医药股份有限公司 氧代吡啶酰胺类衍生物、其制备方法及其在医药上的应用
CN107793396A (zh) * 2016-08-31 2018-03-13 江苏恒瑞医药股份有限公司 环氧基取代的氧代吡啶类衍生物、其制备方法及其在医药上的应用

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JP2021529201A (ja) 2021-10-28
CN112004810B (zh) 2022-04-08
KR20210028232A (ko) 2021-03-11
EP3822264A4 (en) 2021-11-10
WO2020007256A1 (zh) 2020-01-09
EP3822264A1 (en) 2021-05-19
US20210122714A1 (en) 2021-04-29
US11225462B2 (en) 2022-01-18

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