CN111094241A - 一种氧代吡啶酰胺类衍生物的晶型及其制备方法 - Google Patents

一种氧代吡啶酰胺类衍生物的晶型及其制备方法 Download PDF

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CN111094241A
CN111094241A CN201980004501.8A CN201980004501A CN111094241A CN 111094241 A CN111094241 A CN 111094241A CN 201980004501 A CN201980004501 A CN 201980004501A CN 111094241 A CN111094241 A CN 111094241A
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solvent
crystallization
formula
crystal form
ray powder
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CN111094241B (zh
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杨俊然
王林
邵启云
杜振兴
王立坤
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Jiangsu Hengrui Medicine Co Ltd
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Jiangsu Hengrui Medicine Co Ltd
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    • 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
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • 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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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Cardiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

本披露提供了一种氧代吡啶酰胺类衍生物的晶型及其制备方法。具体而言，本披露提供式(I)所示化合物的A、B、C、D、E、F晶型及制备方法。本披露所得到式(I)化合物的A、B、C、D、E、F晶型具备良好的晶型稳定性和化学稳定性，可更好地用于临床治疗。

Description

PCT国内申请，说明书已公开。

Claims (23)

  1. PCT国内申请，权利要求书已公开。
CN201980004501.8A 2018-02-27 2019-02-26 一种氧代吡啶酰胺类衍生物的晶型及其制备方法 Active CN111094241B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201810163529 2018-02-27
CN2018101635293 2018-02-27
PCT/CN2019/076132 WO2019165951A1 (zh) 2018-02-27 2019-02-26 一种氧代吡啶酰胺类衍生物的晶型及其制备方法

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CN111094241A true CN111094241A (zh) 2020-05-01
CN111094241B CN111094241B (zh) 2022-06-21

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US (1) US11299462B2 (zh)
EP (1) EP3741746A4 (zh)
JP (1) JP2021514944A (zh)
KR (1) KR20200127196A (zh)
CN (1) CN111094241B (zh)
AU (1) AU2019227332A1 (zh)
BR (1) BR112020016856A2 (zh)
CA (1) CA3091528A1 (zh)
MX (1) MX2020008488A (zh)
RU (1) RU2020125154A (zh)
TW (1) TWI802654B (zh)
UA (1) UA126251C2 (zh)
WO (1) WO2019165951A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023208169A1 (zh) * 2022-04-29 2023-11-02 江苏恒瑞医药股份有限公司 一种凝血XIa抑制剂的离子液体

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116120240A (zh) * 2019-09-27 2023-05-16 深圳信立泰药业股份有限公司 FXIa抑制剂化合物及其制备方法和医药用途

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014160592A2 (en) * 2013-03-27 2014-10-02 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
CN104136431A (zh) * 2011-12-21 2014-11-05 小野药品工业株式会社 作为凝血因子XIa抑制剂的吡啶酮和嘧啶酮衍生物
CN105164122A (zh) * 2013-03-28 2015-12-16 拜耳制药股份公司 取代的氧代吡啶衍生物及其在治疗心血管病症方面的用途
CN106687458A (zh) * 2014-09-24 2017-05-17 拜耳制药股份公司 取代的氧代吡啶衍生物

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7453002B2 (en) * 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
US9765070B2 (en) 2013-10-30 2017-09-19 Bayer Pharma Aktiengesellschaft Substituted oxopyridine derivatives
CN105829298B (zh) * 2014-02-14 2019-02-01 四川海思科制药有限公司 一种吡啶酮或嘧啶酮衍生物、及其制备方法和应用
WO2016011940A1 (zh) * 2014-07-25 2016-01-28 江苏恒瑞医药股份有限公司 氮茚-酰胺类衍生物、其制备方法及其在医药上的应用
ES2694189T3 (es) * 2014-09-24 2018-12-18 Bayer Pharma Aktiengesellschaft Derivados de oxopiridina sustituidos
CN113912586B (zh) * 2016-08-31 2023-04-07 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

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104136431A (zh) * 2011-12-21 2014-11-05 小野药品工业株式会社 作为凝血因子XIa抑制剂的吡啶酮和嘧啶酮衍生物
WO2014160592A2 (en) * 2013-03-27 2014-10-02 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
CN105164122A (zh) * 2013-03-28 2015-12-16 拜耳制药股份公司 取代的氧代吡啶衍生物及其在治疗心血管病症方面的用途
CN106687458A (zh) * 2014-09-24 2017-05-17 拜耳制药股份公司 取代的氧代吡啶衍生物

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023208169A1 (zh) * 2022-04-29 2023-11-02 江苏恒瑞医药股份有限公司 一种凝血XIa抑制剂的离子液体

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Publication number Publication date
RU2020125154A (ru) 2022-03-28
US11299462B2 (en) 2022-04-12
JP2021514944A (ja) 2021-06-17
KR20200127196A (ko) 2020-11-10
MX2020008488A (es) 2022-08-04
WO2019165951A1 (zh) 2019-09-06
TWI802654B (zh) 2023-05-21
EP3741746A1 (en) 2020-11-25
AU2019227332A1 (en) 2020-08-27
EP3741746A4 (en) 2020-12-16
UA126251C2 (uk) 2022-09-07
CA3091528A1 (en) 2019-09-06
CN111094241B (zh) 2022-06-21
US20200385353A1 (en) 2020-12-10
BR112020016856A2 (pt) 2020-12-22
TW201936580A (zh) 2019-09-16

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