CA2864483A1 - Aminopyrazine derivatives useful for the treatment or prevention of malaria - Google Patents

Aminopyrazine derivatives useful for the treatment or prevention of malaria Download PDF

Info

Publication number
CA2864483A1
CA2864483A1 CA2864483A CA2864483A CA2864483A1 CA 2864483 A1 CA2864483 A1 CA 2864483A1 CA 2864483 A CA2864483 A CA 2864483A CA 2864483 A CA2864483 A CA 2864483A CA 2864483 A1 CA2864483 A1 CA 2864483A1
Authority
CA
Canada
Prior art keywords
phenyl
pyrazin
amino
trifluoromethyl
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.)
Abandoned
Application number
CA2864483A
Other languages
English (en)
French (fr)
Inventor
Yassir YOUNIS
Kelly Chibale
Michael Witty
David Waterson
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 CA2864483A1 publication Critical patent/CA2864483A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic 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
    • 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
    • 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
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic 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
    • C07D241/14Heterocyclic 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
    • C07D241/20Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/10Heterocyclic 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (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)
CA2864483A 2012-02-17 2013-02-15 Aminopyrazine derivatives useful for the treatment or prevention of malaria Abandoned CA2864483A1 (en)

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 (1)

Publication Number Publication Date
CA2864483A1 true CA2864483A1 (en) 2013-08-22

Family

ID=48014134

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2864483A Abandoned CA2864483A1 (en) 2012-02-17 2013-02-15 Aminopyrazine derivatives useful for the treatment or prevention of malaria

Country Status (20)

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

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IN2014MN01622A (OSRAM) * 2012-02-17 2015-05-15 Univ Cape Town
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
ES2928240T3 (es) * 2018-01-24 2022-11-16 Glaxosmithkline Ip Dev Ltd Compuestos novedosos para el tratamiento de infecciones parasitarias
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
CA3238235A1 (en) * 2021-11-23 2023-06-01 Jorge Fernandez-Molina Pyrazine compounds useful in the treatment of parasitic protozoal infection
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
AU2023322415A1 (en) 2022-08-09 2025-03-20 Merck Patent Gmbh Furo pyrimidine derivates

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102127056B (zh) * 2003-12-03 2013-08-21 Ym生物科学澳大利亚私人有限公司 微管蛋白抑制剂
JP2009541268A (ja) * 2006-06-22 2009-11-26 ビオヴィトルム・アクチボラゲット(プブリクト) Mnkキナーゼ阻害剤としてのピリジンおよびピラジン誘導体
EP1900727A1 (en) * 2006-08-30 2008-03-19 Cellzome Ag Aminopyridine derivatives as kinase inhibitors
GB0625659D0 (en) * 2006-12-21 2007-01-31 Cancer Rec Tech Ltd Therapeutic compounds and their use
WO2011086531A2 (en) * 2010-01-18 2011-07-21 Mmv Medicines For Malaria Venture New anti-malarial agents
JP2013529200A (ja) * 2010-05-12 2013-07-18 バーテックス ファーマシューティカルズ インコーポレイテッド Atrキナーゼ阻害剤として有用な化合物
AR085607A1 (es) * 2011-03-04 2013-10-16 Lexicon Pharmaceuticals Inc Inhibidores de la mst1 quinasa y metodos para su utilizacion
IN2014MN01622A (OSRAM) * 2012-02-17 2015-05-15 Univ Cape Town

Also Published As

Publication number Publication date
ZA201406786B (en) 2015-06-24
PL2814820T3 (pl) 2017-01-31
WO2013121387A1 (en) 2013-08-22
CY1118074T1 (el) 2017-06-28
EP2814820A1 (en) 2014-12-24
US20150031682A1 (en) 2015-01-29
BR112014020212B1 (pt) 2021-11-23
ME02535B (me) 2017-02-20
HRP20161237T1 (hr) 2016-11-04
IN2014MN01622A (OSRAM) 2015-05-15
JP2015507004A (ja) 2015-03-05
BR112014020212A8 (pt) 2018-01-23
PT2814820T (pt) 2016-10-25
SMT201600441B (it) 2017-01-10
SI2814820T1 (sl) 2016-10-28
JP6226889B2 (ja) 2017-11-08
LT2814820T (lt) 2016-10-25
EP2814820B1 (en) 2016-07-20
DK2814820T3 (en) 2016-10-03
CN104136426B (zh) 2017-10-03
HK1202859A1 (en) 2015-10-09
HUE029876T2 (en) 2017-04-28
US9266842B2 (en) 2016-02-23
ES2589283T3 (es) 2016-11-11
CN104136426A (zh) 2014-11-05

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Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20180202

FZDE Discontinued

Effective date: 20221115

FZDE Discontinued

Effective date: 20221115