CN104136426B - 抗疟剂 - Google Patents

抗疟剂 Download PDF

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Publication number
CN104136426B
CN104136426B CN201380009373.9A CN201380009373A CN104136426B CN 104136426 B CN104136426 B CN 104136426B CN 201380009373 A CN201380009373 A CN 201380009373A CN 104136426 B CN104136426 B CN 104136426B
Authority
CN
China
Prior art keywords
phenyl
pyrazin
trifluoromethyl
amino
alkyl
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.)
Expired - Fee Related
Application number
CN201380009373.9A
Other languages
English (en)
Chinese (zh)
Other versions
CN104136426A (zh
Inventor
Y·尤尼斯
K·奇贝勒
M·J·韦提
D·沃特森
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.)
MMV Medicines for Malaria Venture
University of Cape Town
Original Assignee
MMV Medicines for Malaria Venture
University of Cape Town
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 MMV Medicines for Malaria Venture, University of Cape Town filed Critical MMV Medicines for Malaria Venture
Publication of CN104136426A publication Critical patent/CN104136426A/zh
Application granted granted Critical
Publication of CN104136426B publication Critical patent/CN104136426B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/20—Nitrogen atoms
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
CN201380009373.9A 2012-02-17 2013-02-15 抗疟剂 Expired - Fee Related CN104136426B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261600324P 2012-02-17 2012-02-17
US61/600,324 2012-02-17
PCT/IB2013/051235 WO2013121387A1 (en) 2012-02-17 2013-02-15 Anti -malarial agents

Publications (2)

Publication Number Publication Date
CN104136426A CN104136426A (zh) 2014-11-05
CN104136426B true CN104136426B (zh) 2017-10-03

Family

ID=48014134

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201380009373.9A Expired - Fee Related CN104136426B (zh) 2012-02-17 2013-02-15 抗疟剂

Country Status (20)

Country Link
US (1) US9266842B2 (enExample)
EP (1) EP2814820B1 (enExample)
JP (1) JP6226889B2 (enExample)
CN (1) CN104136426B (enExample)
BR (1) BR112014020212B1 (enExample)
CA (1) CA2864483A1 (enExample)
CY (1) CY1118074T1 (enExample)
DK (1) DK2814820T3 (enExample)
ES (1) ES2589283T3 (enExample)
HR (1) HRP20161237T1 (enExample)
HU (1) HUE029876T2 (enExample)
IN (1) IN2014MN01622A (enExample)
LT (1) LT2814820T (enExample)
ME (1) ME02535B (enExample)
PL (1) PL2814820T3 (enExample)
PT (1) PT2814820T (enExample)
SI (1) SI2814820T1 (enExample)
SM (1) SMT201600441B (enExample)
WO (1) WO2013121387A1 (enExample)
ZA (1) ZA201406786B (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2589283T3 (es) * 2012-02-17 2016-11-11 University Of Cape Town Agentes anti-malaria
EP3118198A1 (en) 2015-07-13 2017-01-18 MMV Medicines for Malaria Venture Anti-malarial agents
WO2017067881A1 (en) * 2015-10-19 2017-04-27 Glaxosmithkline Intellectual Property Development Limited Pyrazine compounds for use in the treatment of parasitic protozoal infections
JP7057427B2 (ja) * 2018-01-24 2022-04-19 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッド 寄生虫感染の処置のための新規化合物
CN112142715A (zh) * 2020-10-10 2020-12-29 鲁南制药集团股份有限公司 一种2-氨基-5-杂环基取代的吡嗪衍生物及其用途
WO2023094305A1 (en) * 2021-11-23 2023-06-01 Glaxosmithkline Intellectual Property Development Limited Pyrazine compounds useful in the treatment of parasitic protozoal infection
CN119948032A (zh) 2022-08-09 2025-05-06 默克专利股份有限公司 呋喃并嘧啶衍生物
WO2024033280A1 (en) 2022-08-09 2024-02-15 Merck Patent Gmbh Furopyridin and furopyrimidin, inhibitors of pi4k, for use in the treatment of parasite infection and malaria

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007147874A1 (en) * 2006-06-22 2007-12-27 Biovitrum Ab (Publ) Pyridine and pyrazine derivatives as mnk kinase inhibitors
WO2008074997A1 (en) * 2006-12-21 2008-06-26 Cancer Research Technology Limited Pyridine benzamides and pyrazine benzamides used as pkd inhibitors
WO2011086531A2 (en) * 2010-01-18 2011-07-21 Mmv Medicines For Malaria Venture New anti-malarial agents
WO2011143423A2 (en) * 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
CN104136426A (zh) * 2012-02-17 2014-11-05 开普敦大学 抗疟剂

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4772690B2 (ja) * 2003-12-03 2011-09-14 ワイエム・バイオサイエンシズ・オーストラリア・ピーティーワイ・リミテッド チューブリン阻害剤
EP1900727A1 (en) * 2006-08-30 2008-03-19 Cellzome Ag Aminopyridine derivatives as kinase inhibitors
AU2012225805B2 (en) 2011-03-04 2017-03-02 Lexicon Pharmaceuticals, Inc. MST1 kinase inhibitors and methods of their use

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007147874A1 (en) * 2006-06-22 2007-12-27 Biovitrum Ab (Publ) Pyridine and pyrazine derivatives as mnk kinase inhibitors
WO2008074997A1 (en) * 2006-12-21 2008-06-26 Cancer Research Technology Limited Pyridine benzamides and pyrazine benzamides used as pkd inhibitors
WO2011086531A2 (en) * 2010-01-18 2011-07-21 Mmv Medicines For Malaria Venture New anti-malarial agents
WO2011143423A2 (en) * 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
CN104136426A (zh) * 2012-02-17 2014-11-05 开普敦大学 抗疟剂

Also Published As

Publication number Publication date
SI2814820T1 (sl) 2016-10-28
PT2814820T (pt) 2016-10-25
HK1202859A1 (en) 2015-10-09
HRP20161237T1 (hr) 2016-11-04
BR112014020212B1 (pt) 2021-11-23
BR112014020212A8 (pt) 2018-01-23
CN104136426A (zh) 2014-11-05
HUE029876T2 (en) 2017-04-28
US20150031682A1 (en) 2015-01-29
EP2814820A1 (en) 2014-12-24
JP6226889B2 (ja) 2017-11-08
JP2015507004A (ja) 2015-03-05
WO2013121387A1 (en) 2013-08-22
US9266842B2 (en) 2016-02-23
CA2864483A1 (en) 2013-08-22
IN2014MN01622A (enExample) 2015-05-15
ES2589283T3 (es) 2016-11-11
LT2814820T (lt) 2016-10-25
CY1118074T1 (el) 2017-06-28
ME02535B (me) 2017-02-20
EP2814820B1 (en) 2016-07-20
SMT201600441B (it) 2017-01-10
PL2814820T3 (pl) 2017-01-31
ZA201406786B (en) 2015-06-24
DK2814820T3 (en) 2016-10-03

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