CN113227096A - 1,2,3-三氮唑并[1,5-a]吡嗪类衍生物的晶型及其制备方法 - Google Patents

1,2,3-三氮唑并[1,5-a]吡嗪类衍生物的晶型及其制备方法 Download PDF

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CN113227096A
CN113227096A CN202080007547.8A CN202080007547A CN113227096A CN 113227096 A CN113227096 A CN 113227096A CN 202080007547 A CN202080007547 A CN 202080007547A CN 113227096 A CN113227096 A CN 113227096A
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compound
ray powder
powder diffraction
triazole
methyl
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CN113227096B (zh
Inventor
韩龙
邵启云
冯君
贺峰
马亚辉
赵苗苗
杜振兴
王捷
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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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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/16Antivirals for RNA viruses for influenza or rhinoviruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

本公开提供了1,2,3‑三氮唑并[1,5‑a]吡嗪类衍生物的晶型及其制备方法。具体而言,本公开提供了化合物(S)‑N5‑(3,4‑二氟苯基)‑6‑甲基‑N3‑((R)‑1,1,1‑三氟丙‑2‑基)‑6,7‑二氢‑[1,2,3]三氮唑并[1,5‑a]吡嗪‑3,5(4H)‑二甲酰胺的晶型及其制备方法。制备得到的晶型具有良好的稳定性以及临床应用价值。

Description

PCT国内申请,说明书已公开。

Claims (10)

  1. PCT国内申请,权利要求书已公开。
CN202080007547.8A 2019-01-25 2020-01-22 1,2,3-三氮唑并[1,5-a]吡嗪类衍生物的晶型及其制备方法 Active CN113227096B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2019100720486 2019-01-25
CN201910072048 2019-01-25
PCT/CN2020/073802 WO2020151746A1 (zh) 2019-01-25 2020-01-22 1,2,3-三氮唑并[1,5-a]吡嗪类衍生物的晶型及其制备方法

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CN113227096A true CN113227096A (zh) 2021-08-06
CN113227096B CN113227096B (zh) 2022-04-12

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US (1) US20220081446A1 (zh)
EP (1) EP3915993A1 (zh)
JP (1) JP2022523035A (zh)
KR (1) KR20210120036A (zh)
CN (1) CN113227096B (zh)
AU (1) AU2020210998A1 (zh)
BR (1) BR112021014327A2 (zh)
CA (1) CA3126175A1 (zh)
MX (1) MX2021008929A (zh)
TW (1) TW202043233A (zh)
WO (1) WO2020151746A1 (zh)

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TW202245772A (zh) * 2021-02-04 2022-12-01 大陸商江蘇恆瑞醫藥股份有限公司 一種衣殼蛋白抑制劑的醫藥組成物及其製備方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016113273A1 (en) * 2015-01-16 2016-07-21 F. Hoffmann-La Roche Ag Pyrazine compounds for the treatment of infectious diseases
CN108727347A (zh) * 2017-04-14 2018-11-02 江苏恒瑞医药股份有限公司 一种阿片样物质受体(mor)激动剂的晶型及其制备方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101686989B (zh) * 2007-06-21 2016-10-19 卡拉治疗学股份有限公司 取代的咪唑并杂环
CN102875270B (zh) 2012-09-24 2014-12-03 巨化集团公司 一种三氟甲基代胺的合成方法
UY35834A (es) * 2013-11-14 2015-05-29 Bristol Myers Squibb Company Una Corporación Del Estado De Delaware Piperazinas de pirazolo sustituido como inhibidores de caseína quinasa 1 delta y epsilon
CA3070004A1 (en) * 2017-07-27 2019-01-31 Jiangsu Hengrui Medicine Co., Ltd. Piperazine heteroaryl derivative, preparation method therefor and use of same in medicine

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016113273A1 (en) * 2015-01-16 2016-07-21 F. Hoffmann-La Roche Ag Pyrazine compounds for the treatment of infectious diseases
CN108727347A (zh) * 2017-04-14 2018-11-02 江苏恒瑞医药股份有限公司 一种阿片样物质受体(mor)激动剂的晶型及其制备方法

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CN113227096B (zh) 2022-04-12
US20220081446A1 (en) 2022-03-17
CA3126175A1 (en) 2020-07-30
KR20210120036A (ko) 2021-10-06
WO2020151746A1 (zh) 2020-07-30
MX2021008929A (es) 2021-08-24
AU2020210998A1 (en) 2021-09-16
TW202043233A (zh) 2020-12-01
JP2022523035A (ja) 2022-04-21
BR112021014327A2 (pt) 2021-09-28
EP3915993A1 (en) 2021-12-01

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