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

Info

Publication number
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
Authority
CN
China
Prior art keywords
compound
ray powder
powder diffraction
triazole
methyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
CN202080007547.8A
Other languages
English (en)
Other versions
CN113227096B (zh
Inventor
韩龙
邵启云
冯君
贺峰
马亚辉
赵苗苗
杜振兴
王捷
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
Original Assignee
Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Jiangsu Hengrui Medicine Co Ltd, Shanghai Hengrui Pharmaceutical Co Ltd filed Critical Jiangsu Hengrui Medicine Co Ltd
Publication of CN113227096A publication Critical patent/CN113227096A/zh
Application granted granted Critical
Publication of CN113227096B publication Critical patent/CN113227096B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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

Landscapes

  • 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
CN201910072048 2019-01-25
CN2019100720486 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

Publications (2)

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

Family

ID=71735561

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202080007547.8A Active CN113227096B (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

Country Status (11)

Country Link
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)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
ES2439255T3 (es) * 2007-06-21 2014-01-22 Cara Therapeutics, Inc. Imidazoheterociclos sustituidos
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
AR098414A1 (es) * 2013-11-14 2016-05-26 Bristol Myers Squibb Co PIPERAZINAS DE PIRAZOLO SUSTITUIDO COMO INHIBIDORES DE CASEÍNA QUINASA 1 d/e
KR20200032702A (ko) * 2017-07-27 2020-03-26 지앙수 헨그루이 메디슨 컴퍼니 리미티드 피페라진 헤테로아릴 유도체, 그 제조 방법 및 의약에서 이의 용도

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

Also Published As

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

Similar Documents

Publication Publication Date Title
US10017513B2 (en) Crystalline forms of sodium 4-{[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido [5,4-D][2]benzazepin-2-YL]amino}-2-methoxybenzoate
CN110577536B (zh) 苯甲酰氨基吡啶衍生物的盐及其在药物中的应用
PL172789B1 (pl) Sposób wytwarzania nowych makrolidów imidazolilowych PL PL PL
US20210387989A1 (en) Pyrrolo[2,3-d]pyrimidine tosylate salt, crystalline form thereof and manufacturing process and intermediates thereto
US20090076272A1 (en) Polymorphs of eszopiclone malate
EP0918777A1 (en) SELECTED DERIVATIVES OF K-252a
CN113227096B (zh) 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
KR20200092946A (ko) 결정질 리나글립틴 중간체 및 리나글립틴 제조 공정
CN114728973B (zh) 一种核蛋白抑制剂的晶型及其应用
US11230559B2 (en) Solid forms of [(1 S)-1 -[(2S,4R,5R)-5-(5-amino-2-oxo-thiazolo[4,5-D]pyrimidin-3-yl)-4-hydroxy-tetrahydrofuran-2-Yl]proptl] acetate
CN111484498B (zh) 咪唑并[1,5-a]吡嗪类化合物的晶型及其制备方法
CN111484497B (zh) 咪唑并[1,5-a]吡嗪类衍生物的可药用盐、晶型及其制备方法
US20220119415A1 (en) Solid forms of [(1s)-1-[(2s,4r,5r)-5-(5-amino-2-oxo-thiazolo[4,5-d]pyrimidin-3-yl)-4-hydroxy-tetrahydrofuran-2-yl]propyl] acetate
CN112830919B (zh) 苯并哌啶衍生物可药用盐及其制备方法
RU2793918C2 (ru) Ингибитор некроза клеток, способ его получения и применения
US20090082386A1 (en) Ascomycin and pimecrolimus having reduced levels of desmethylascomycin and 32-deoxy-32-epichloro-desmethylascomycin respectively, and methods for preparation thereof
CN111718340A (zh) 氘代Palbociclib化合物的晶型、制备方法及应用
CN109824606A (zh) 一种瑞舒伐他汀钙杂质以及瑞舒伐他汀钙质量控制方法
EP2109613A2 (en) Polymorphs of eszopiclone malate

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40060005

Country of ref document: HK