CN107709328A - 咪唑衍生物及其中间体的制备方法和晶型 - Google Patents

咪唑衍生物及其中间体的制备方法和晶型 Download PDF

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Publication number
CN107709328A
CN107709328A CN201680031461.2A CN201680031461A CN107709328A CN 107709328 A CN107709328 A CN 107709328A CN 201680031461 A CN201680031461 A CN 201680031461A CN 107709328 A CN107709328 A CN 107709328A
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China
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preparation
crystal form
liters
compound
solvent
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CN201680031461.2A
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CN107709328B (zh
Inventor
石卫华
徐峰
王峥
李卫东
吴灵慧
李宏伟
曾明高
赖焜民
江志赶
贺海鹰
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Medshine Discovery Inc
Shandong Danhong Pharmaceutical Co Ltd
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Shandong Danhong Pharmaceutical Co Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B01PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01DSEPARATION
    • B01D9/00Crystallisation
    • B01D9/0004Crystallisation cooling by heat exchange
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B01PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01DSEPARATION
    • B01D9/00Crystallisation
    • B01D9/005Selection of auxiliary, e.g. for control of crystallisation nuclei, of crystal growth, of adherence to walls; Arrangements for introduction thereof
    • B01D9/0054Use of anti-solvent
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B41/00Formation or introduction of functional groups containing oxygen
    • C07B41/06Formation or introduction of functional groups containing oxygen of carbonyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B43/00Formation or introduction of functional groups containing nitrogen
    • C07B43/04Formation or introduction of functional groups containing nitrogen of amino groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56Ring systems containing three or more rings
    • C07D209/96Spiro-condensed ring systems
    • 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
    • C07D487/10Spiro-condensed systems
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Physics & Mathematics (AREA)
  • Thermal Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

本发明公开了一种咪唑衍生物的制备方法及其A晶型和B晶型,本发明还公开了式(Ⅰ)化合物及其中间体的制备方法。

Description

PCT国内申请,说明书已公开。

Claims (18)

  1. PCT国内申请,权利要求书已公开。
CN201680031461.2A 2015-06-08 2016-06-07 咪唑衍生物及其中间体的制备方法和晶型 Active CN107709328B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201510309106 2015-06-08
CN2015103091064 2015-06-08
PCT/CN2016/085104 WO2016197908A1 (zh) 2015-06-08 2016-06-07 咪唑衍生物及其中间体的制备方法和晶型

Publications (2)

Publication Number Publication Date
CN107709328A true CN107709328A (zh) 2018-02-16
CN107709328B CN107709328B (zh) 2021-03-05

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US (3) US10227309B2 (zh)
EP (1) EP3305790B1 (zh)
JP (1) JP6548751B2 (zh)
CN (1) CN107709328B (zh)
ES (1) ES2821649T3 (zh)
HK (1) HK1244807A1 (zh)
PT (1) PT3305790T (zh)
TW (1) TWI695005B (zh)
WO (1) WO2016197908A1 (zh)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT3305790T (pt) 2015-06-08 2020-10-19 Shangdong Danhong Pharmaceutical Co Ltd Método para preparação de um derivado de imidazol e seu intermediário e forma cristalina
CN112057453B (zh) * 2019-08-26 2022-06-28 中检科医药科技(北京)集团有限公司 Enc002及其类似物在治疗或预防肠道病毒感染中的应用

Citations (3)

* Cited by examiner, † Cited by third party
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CN103347881A (zh) * 2010-12-16 2013-10-09 爱尔兰詹森研发公司 作为呼吸道合胞病毒抗病毒剂的氮杂苯并咪唑
WO2014060411A1 (en) * 2012-10-16 2014-04-24 Janssen R&D Ireland Rsv antiviral compounds
CN105793265B (zh) * 2013-12-10 2018-02-13 山东丹红制药有限公司 作为抗病毒剂的咪唑衍生物及其制药用途

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US4175289A (en) 1978-06-05 1979-11-20 International Business Machines Corporation Serrated Y-bar magnetic bubble switch
US4324794A (en) 1980-08-26 1982-04-13 Research Triangle Institute Inhibition of respiratory syncytial virus-induced cell fusion by amidino compounds
DK154078C (da) 1981-02-06 1989-05-22 Ucb Sa Analogifremgangsmaade til fremstilling af 2-(2-(4-(diphenyl-methyl)-1-piperazinyl)ethoxy)-acetamider eller syreadditionssalte heraf
US5256668A (en) 1993-03-17 1993-10-26 American Home Products Corporation Aminopyrimidine derivatives as antiviral agents for respiratory syncytial virus
ZA971185B (en) 1996-02-13 1998-08-12 American Cyanamid Co Triazine containing compounds useful as antiviral agents
MXPA00007394A (es) 1998-01-29 2003-08-01 Viropharma Inc Compuestos, composiciones y metodos para tratar o evitar infeccion de neumovirus y enfermedades asociadas.
EP1098644A1 (en) 1998-07-20 2001-05-16 Bristol-Myers Squibb Company Substituted benzimidazole antiviral agents
WO2010103306A1 (en) 2009-03-10 2010-09-16 Astrazeneca Uk Limited Benzimidazole derivatives and their use as antivaral agents
MX2013005046A (es) 2010-11-03 2013-12-12 Immunogen Inc Agentes citotoxicos que comprenden nuevos derivados de ansamitocina.
GB201119538D0 (en) 2011-11-10 2011-12-21 Viral Ltd Pharmaceutical compounds
CN103319599B (zh) 2013-05-27 2015-02-18 上海交联药物研发有限公司 一种抗人ErbB2抗体—美登木素偶联物及其应用
TWI671299B (zh) 2014-04-14 2019-09-11 愛爾蘭商健生科學愛爾蘭無限公司 作為rsv抗病毒化合物之螺脲化合物
GB201417707D0 (en) * 2014-10-07 2014-11-19 Viral Ltd Pharmaceutical compounds
PT3305790T (pt) * 2015-06-08 2020-10-19 Shangdong Danhong Pharmaceutical Co Ltd Método para preparação de um derivado de imidazol e seu intermediário e forma cristalina

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103347881A (zh) * 2010-12-16 2013-10-09 爱尔兰詹森研发公司 作为呼吸道合胞病毒抗病毒剂的氮杂苯并咪唑
WO2014060411A1 (en) * 2012-10-16 2014-04-24 Janssen R&D Ireland Rsv antiviral compounds
CN105793265B (zh) * 2013-12-10 2018-02-13 山东丹红制药有限公司 作为抗病毒剂的咪唑衍生物及其制药用途

Also Published As

Publication number Publication date
PT3305790T (pt) 2020-10-19
EP3305790A1 (en) 2018-04-11
US10227309B2 (en) 2019-03-12
US20200223802A1 (en) 2020-07-16
ES2821649T3 (es) 2021-04-27
JP2018517719A (ja) 2018-07-05
TW201704238A (zh) 2017-02-01
WO2016197908A1 (zh) 2016-12-15
HK1244807A1 (zh) 2018-08-17
CN107709328B (zh) 2021-03-05
US10858322B2 (en) 2020-12-08
US20190218189A1 (en) 2019-07-18
US20180141915A1 (en) 2018-05-24
EP3305790A4 (en) 2018-10-03
TWI695005B (zh) 2020-06-01
EP3305790B1 (en) 2020-08-05
JP6548751B2 (ja) 2019-07-24
US10633347B2 (en) 2020-04-28

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