CN115515955A - 4-[(7-氯-2-甲氧基苯并[b][1,5]萘啶-10-基)氨基]-2,6-双(吡咯烷-1-基甲基)苯酚及其盐的结晶形式 - Google Patents

4-[(7-氯-2-甲氧基苯并[b][1,5]萘啶-10-基)氨基]-2,6-双(吡咯烷-1-基甲基)苯酚及其盐的结晶形式 Download PDF

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Publication number
CN115515955A
CN115515955A CN202180028991.2A CN202180028991A CN115515955A CN 115515955 A CN115515955 A CN 115515955A CN 202180028991 A CN202180028991 A CN 202180028991A CN 115515955 A CN115515955 A CN 115515955A
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Prior art keywords
powder
crystalline
ylmethyl
methoxybenzo
naphthyridin
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CN202180028991.2A
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Chinese (zh)
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A·贝克
D-M·格鲁亚
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Merck Patent GmbH
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Merck Patent GmbH
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06Antimalarials
    • 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
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN202180028991.2A 2020-04-17 2021-04-14 4-[(7-氯-2-甲氧基苯并[b][1,5]萘啶-10-基)氨基]-2,6-双(吡咯烷-1-基甲基)苯酚及其盐的结晶形式 Pending CN115515955A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP20170197.6 2020-04-17
EP20170197 2020-04-17
PCT/EP2021/059604 WO2021209477A1 (en) 2020-04-17 2021-04-14 Crystalline forms of 4-[(7-chloro-2-methoxybenzo[b][1,5]naphthyridin-10-yl)amino]-2,6-bis(pyrrolidin-1-ylmethyl)phenol and salts thereof

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CN115515955A true CN115515955A (zh) 2022-12-23

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CN202180028991.2A Pending CN115515955A (zh) 2020-04-17 2021-04-14 4-[(7-氯-2-甲氧基苯并[b][1,5]萘啶-10-基)氨基]-2,6-双(吡咯烷-1-基甲基)苯酚及其盐的结晶形式

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US (1) US20230295156A1 (https=)
EP (1) EP4136087A1 (https=)
JP (1) JP2023522023A (https=)
CN (1) CN115515955A (https=)
BR (1) BR112022018436A2 (https=)
CA (1) CA3175552A1 (https=)
PH (1) PH12022552366A1 (https=)
WO (1) WO2021209477A1 (https=)

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101544638A (zh) * 2009-05-12 2009-09-30 重庆通天药业有限公司 乳酸咯萘啶及其药物组合物
KR20090114029A (ko) * 2008-04-29 2009-11-03 강민석 피로나리딘의 제조방법 및 이를 위한 중간체
CN103373995A (zh) * 2012-04-28 2013-10-30 上海迪赛诺药业有限公司 一种制备咯萘啶的方法
CN105461713A (zh) * 2014-09-25 2016-04-06 刘力 苯并萘啶类的新化合物及其组合物和用途
CN109843876A (zh) * 2016-10-13 2019-06-04 Mmv疟疾药物投资公司 新的抗疟剂

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2902143T3 (es) * 2014-07-04 2022-03-25 Merck Patent Gmbh Derivados de azepanilo y composiciones farmacéuticas que los comprenden con actividad antiparasitaria
HUE069225T2 (hu) * 2018-04-11 2025-02-28 Merck Patent Gmbh Kinolin-4-karboxamidok és benzonaftiridin származékok kombinációja maláriaellenes gyógyszer-kombinációként
CN112209926A (zh) * 2019-07-12 2021-01-12 中国中医科学院中药研究所 磷酸咯萘啶的多晶型物及其制备方法、应用
CA3182616A1 (en) * 2020-06-15 2021-12-23 Lukas Shinji OKITSU Tlr7/8 antagonists and uses thereof

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20090114029A (ko) * 2008-04-29 2009-11-03 강민석 피로나리딘의 제조방법 및 이를 위한 중간체
CN101544638A (zh) * 2009-05-12 2009-09-30 重庆通天药业有限公司 乳酸咯萘啶及其药物组合物
CN103373995A (zh) * 2012-04-28 2013-10-30 上海迪赛诺药业有限公司 一种制备咯萘啶的方法
CN105461713A (zh) * 2014-09-25 2016-04-06 刘力 苯并萘啶类的新化合物及其组合物和用途
CN109843876A (zh) * 2016-10-13 2019-06-04 Mmv疟疾药物投资公司 新的抗疟剂

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
郑贤育等: "抗疟新药咯萘啶及其类似物的合成", 药学学报, vol. 17, no. 2, 28 February 1982 (1982-02-28), pages 123 *

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Publication number Publication date
WO2021209477A1 (en) 2021-10-21
JP2023522023A (ja) 2023-05-26
PH12022552366A1 (en) 2024-03-18
CA3175552A1 (en) 2021-10-21
BR112022018436A2 (pt) 2022-11-01
US20230295156A1 (en) 2023-09-21
EP4136087A1 (en) 2023-02-22

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