CN114569552A - 抗疟疾组合物及其用途 - Google Patents

抗疟疾组合物及其用途 Download PDF

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Publication number
CN114569552A
CN114569552A CN202111196136.0A CN202111196136A CN114569552A CN 114569552 A CN114569552 A CN 114569552A CN 202111196136 A CN202111196136 A CN 202111196136A CN 114569552 A CN114569552 A CN 114569552A
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formula
compounds
crystalline
alkyl
optionally substituted
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CN202111196136.0A
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English (en)
Chinese (zh)
Inventor
维尔·约瑟夫·安达哈叙
阿纳布·K·查特吉
卡斯·W·麦克纳马拉
费德里科·C·比斯利
安德斯·米卡尔·伊莱亚森
汉克·迈克尔·詹姆斯·佩特拉希
詹森·T·罗兰
蒂莫西·威尔斯
奥尔加·弗拉基米罗芙娜·萨托洛赫纳亚
周飞
彼得·G·舒尔茨
阿尼尔·库马尔·古普塔
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Scripps Research Institute
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Scripps Research Institute
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C50/00Quinones
    • C07C50/26Quinones containing groups having oxygen atoms singly bound to carbon atoms
    • C07C50/32Quinones containing groups having oxygen atoms singly bound to carbon atoms the quinoid structure being part of a condensed ring system having two rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/62Halogen-containing esters
    • C07C69/65Halogen-containing esters of unsaturated acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/12Ketones
    • A61K31/122Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/222Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/23Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
    • A61K31/232Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having three or more double bonds, e.g. etretinate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/12Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14The ring being saturated
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material 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)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Emergency Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dispersion Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN202111196136.0A 2016-06-20 2017-06-19 抗疟疾组合物及其用途 Pending CN114569552A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201662352455P 2016-06-20 2016-06-20
US62/352,455 2016-06-20
CN201780050449.0A CN109715147A (zh) 2016-06-20 2017-06-19 抗疟疾组合物及其用途
PCT/US2017/038173 WO2017222996A1 (en) 2016-06-20 2017-06-19 Antimalarial compositions and uses thereof

Related Parent Applications (1)

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CN201780050449.0A Division CN109715147A (zh) 2016-06-20 2017-06-19 抗疟疾组合物及其用途

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CN114569552A true CN114569552A (zh) 2022-06-03

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CN201780050449.0A Pending CN109715147A (zh) 2016-06-20 2017-06-19 抗疟疾组合物及其用途

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US (3) US10947176B2 (enExample)
EP (1) EP3471711A4 (enExample)
JP (1) JP2019523779A (enExample)
KR (1) KR20190020774A (enExample)
CN (2) CN114569552A (enExample)
AU (1) AU2017281426B2 (enExample)
BR (1) BR112018076619A2 (enExample)
CA (1) CA3028392A1 (enExample)
EA (1) EA201990064A1 (enExample)
MA (1) MA45411A (enExample)
SG (2) SG10202112759SA (enExample)
WO (1) WO2017222996A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10947176B2 (en) * 2016-06-20 2021-03-16 The Scripps Research Institute Antimalarial compositions and uses thereof
US12520840B2 (en) * 2018-09-04 2026-01-13 President And Fellows Of Harvard College Method for reducing parasite burden in a mosquito
EP4149510A4 (en) 2020-05-11 2024-05-22 Oregon Health & Science University Novel intermediates and synthesis for endochin-like quinolone compounds
WO2022144920A1 (en) * 2020-12-30 2022-07-07 Ipca Laboratories Limited Atovaquone prodrugs
WO2025151263A1 (en) * 2024-01-09 2025-07-17 Sri International Oil-based compositions and methods of making and use thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0580185A1 (en) * 1988-08-16 1994-01-26 The Wellcome Foundation Limited Medicaments

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5206268A (en) * 1988-08-16 1993-04-27 Burroughs Wellcome Co. Medicaments
GB8819477D0 (en) * 1988-08-16 1988-09-21 Wellcome Found Medicaments
US5021426A (en) * 1990-02-26 1991-06-04 Merck & Co., Inc. Method of traeting malaria with cyproheptadine derivatives
GB9207517D0 (en) 1992-04-06 1992-05-20 Wellcome Found Heterocyclic compounds
MY118354A (en) * 1995-05-01 2004-10-30 Scarista Ltd 1,3-propane diol derivatives as bioactive compounds
ITMI20070941A1 (it) * 2007-05-09 2008-11-10 Chimico Internazi0Nale S P A L Procedimento per la preparazione di naftochinoni trans2,3-disostituiti
US10947176B2 (en) * 2016-06-20 2021-03-16 The Scripps Research Institute Antimalarial compositions and uses thereof

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0580185A1 (en) * 1988-08-16 1994-01-26 The Wellcome Foundation Limited Medicaments

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
SALOME´ EL HAGE等: "Synthesis and antimalarial activity of new atovaquone derivatives", 《EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY》 *
曹丹: "纳米混悬剂的研究新进展", 《科技信息》 *

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CA3028392A1 (en) 2017-12-28
BR112018076619A2 (pt) 2019-04-02
EA201990064A1 (ru) 2019-05-31
US10947176B2 (en) 2021-03-16
US20210179524A1 (en) 2021-06-17
KR20190020774A (ko) 2019-03-04
SG11201811434RA (en) 2019-01-30
US20190202766A1 (en) 2019-07-04
WO2017222996A1 (en) 2017-12-28
MA45411A (fr) 2019-04-24
AU2017281426A1 (en) 2019-01-17
AU2017281426B2 (en) 2021-10-14
CN109715147A (zh) 2019-05-03
SG10202112759SA (en) 2021-12-30
US11485697B2 (en) 2022-11-01
EP3471711A1 (en) 2019-04-24
EP3471711A4 (en) 2020-02-19
JP2019523779A (ja) 2019-08-29
US20230111793A1 (en) 2023-04-13

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Application publication date: 20220603