CA2787121C - Aminopyridine derivatives as anti-malarial agents - Google Patents

Aminopyridine derivatives as anti-malarial agents Download PDF

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Publication number
CA2787121C
CA2787121C CA2787121A CA2787121A CA2787121C CA 2787121 C CA2787121 C CA 2787121C CA 2787121 A CA2787121 A CA 2787121A CA 2787121 A CA2787121 A CA 2787121A CA 2787121 C CA2787121 C CA 2787121C
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Prior art keywords
pyridin
phenyl
amine
amino
methylsulfonyl
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CA2787121A
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English (en)
French (fr)
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CA2787121A1 (en
Inventor
Michael John Witty
David Hardick
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MMV Medicines for Malaria Venture
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MMV Medicines for Malaria Venture
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72Nitrogen atoms
    • C07D213/73Unsubstituted amino or imino radicals
    • 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
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72Nitrogen atoms
    • C07D213/74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • 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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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CA2787121A 2010-01-18 2011-01-17 Aminopyridine derivatives as anti-malarial agents Active CA2787121C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US29582110P 2010-01-18 2010-01-18
US61/295,821 2010-01-18
PCT/IB2011/050192 WO2011086531A2 (en) 2010-01-18 2011-01-17 New anti-malarial agents

Publications (2)

Publication Number Publication Date
CA2787121A1 CA2787121A1 (en) 2011-07-21
CA2787121C true CA2787121C (en) 2018-07-17

Family

ID=43759659

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2787121A Active CA2787121C (en) 2010-01-18 2011-01-17 Aminopyridine derivatives as anti-malarial agents

Country Status (17)

Country Link
US (1) US9024033B2 (enExample)
EP (1) EP2526090B1 (enExample)
JP (1) JP5735986B2 (enExample)
CN (1) CN102812006B (enExample)
BR (1) BR112012017713A2 (enExample)
CA (1) CA2787121C (enExample)
DK (1) DK2526090T3 (enExample)
ES (1) ES2551875T3 (enExample)
HR (1) HRP20151143T1 (enExample)
HU (1) HUE027946T2 (enExample)
ME (1) ME02315B (enExample)
PL (1) PL2526090T3 (enExample)
PT (1) PT2526090E (enExample)
RS (1) RS54339B1 (enExample)
SI (1) SI2526090T1 (enExample)
SM (1) SMT201500291B (enExample)
WO (1) WO2011086531A2 (enExample)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ593969A (en) 2008-12-19 2013-11-29 Vertex Pharma Pyrazine derivatives useful as inhibitors of atr kinase
SG185524A1 (en) 2010-05-12 2012-12-28 Vertex Pharma Compounds useful as inhibitors of atr kinase
AU2011253021A1 (en) * 2010-05-12 2012-11-29 Vertex Pharmaceuticals Incorporated 2 -aminopyridine derivatives useful as inhibitors of ATR kinase
JP2013526540A (ja) 2010-05-12 2013-06-24 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
MX2013009953A (es) * 2011-03-04 2013-09-26 Lexicon Pharmaceuticals Inc Inhibidores de cinasa de mst1 y metodos de su uso.
WO2013049859A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Treating pancreatic cancer and non-small cell lung cancer with atr inhibitors
MX353461B (es) 2011-09-30 2018-01-15 Vertex Pharma PROCESOS PARA PREPARAR COMPUESTOS ÚTILES COMO INHIBIDORES DE CINASA ATAXIA TELANGIECTASIA MUTADA Y Rad3 RELACIONADOS (ATR).
BR112014020212B1 (pt) 2012-02-17 2021-11-23 University Of Cape Town Aminopirazina, formulação farmacêutica, método para prevenir ou tratar malária em um paciente, processo para a preparação de um derivado de aminopirazina, e, intermediário
PT2833973T (pt) 2012-04-05 2017-12-21 Vertex Pharma Compostos úteis como inibidores da cinase atr e terapias de combinação dos mesmos
DK2904406T3 (en) 2012-10-04 2018-06-18 Vertex Pharma METHOD OF DETERMINING THE ATR INHIBITION, INCREASED DNA DAMAGE
MY184855A (en) 2013-03-15 2021-04-27 Dow Agrosciences Llc 4-amino-6-(heterocyclic)picolinates and 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their use as herbicides
US9006250B2 (en) * 2013-03-15 2015-04-14 Dow Agrosciences Llc 4-amino-6-(heterocyclic)picolinates and 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their use as herbicides
US9862711B2 (en) 2014-04-24 2018-01-09 Novartis Ag Pyrazine derivatives as phosphatidylinositol 3-kinase inhibitors
US10112926B2 (en) * 2014-04-24 2018-10-30 Novartis Ag Amino pyridine derivatives as phosphatidylinositol 3-kinase inhibitors
WO2015162459A1 (en) 2014-04-24 2015-10-29 Novartis Ag Amino pyrazine derivatives as phosphatidylinositol 3-kinase inhibitors
CN107531683B (zh) * 2015-03-20 2022-05-13 豪夫迈·罗氏有限公司 Usp7抑制剂化合物及使用方法
EP3118198A1 (en) 2015-07-13 2017-01-18 MMV Medicines for Malaria Venture Anti-malarial agents
HK1258570A1 (zh) 2015-09-30 2019-11-15 Vertex Pharmaceuticals Inc. 使用dna损伤剂及atr抑制剂的组合治疗癌症的方法
WO2017067881A1 (en) * 2015-10-19 2017-04-27 Glaxosmithkline Intellectual Property Development Limited Pyrazine compounds for use in the treatment of parasitic protozoal infections
GB201603104D0 (en) * 2016-02-23 2016-04-06 Ucb Biopharma Sprl Therapeutic agents
EP3254679A1 (de) 2016-06-09 2017-12-13 Christian-Albrechts-Universität zu Kiel Wirkstoffe gegen protozoen und bakterien
US11919902B2 (en) * 2017-12-22 2024-03-05 Hibercell, Inc. Aryl-bipyridine amine derivatives as phosphatidylinositol phosphate kinase inhibitors
BR112020018094A2 (pt) 2018-03-08 2020-12-22 Incyte Corporation Compostos de aminopirazina diol como inibidores de pi3k-¿
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
EP3842100A1 (en) * 2019-12-24 2021-06-30 The Board Of Regents Of The University Of Texas System Anti-malarial agents
CA3264304A1 (en) 2022-08-09 2024-02-15 Merck Patent Gmbh FURO-PYRIMIDINE DERIVATIVES
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
EP4574143A1 (en) 2023-12-21 2025-06-25 Universität Regensburg Inhibitors of plasmodia remodeling enzymes

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100574350B1 (ko) 2004-08-31 2006-04-27 한국화학연구원 2-아미노피리딘 유도체의 제조방법
JP2009507824A (ja) * 2005-09-12 2009-02-26 カウンシル・オブ・サイエンティフィック・アンド・インダストリアル・リサーチ 抗マラリアベイリス−ヒルマン付加物およびその調製方法
EP1900727A1 (en) * 2006-08-30 2008-03-19 Cellzome Ag Aminopyridine derivatives as kinase inhibitors
CN101555248B (zh) 2009-05-22 2011-06-22 北京欧凯纳斯科技有限公司 一种多取代1,5-萘啶化合物的制备方法

Also Published As

Publication number Publication date
JP2013517264A (ja) 2013-05-16
SMT201500291B (it) 2016-01-08
HK1175472A1 (zh) 2013-07-05
CA2787121A1 (en) 2011-07-21
ME02315B (me) 2016-06-20
HRP20151143T1 (hr) 2015-12-04
ES2551875T3 (es) 2015-11-24
WO2011086531A2 (en) 2011-07-21
RS54339B1 (sr) 2016-02-29
PL2526090T3 (pl) 2016-04-29
EP2526090B1 (en) 2015-08-19
HUE027946T2 (en) 2016-11-28
JP5735986B2 (ja) 2015-06-17
US9024033B2 (en) 2015-05-05
CN102812006A (zh) 2012-12-05
WO2011086531A3 (en) 2011-09-29
CN102812006B (zh) 2016-01-20
US20120295905A1 (en) 2012-11-22
SI2526090T1 (sl) 2015-11-30
EP2526090A2 (en) 2012-11-28
DK2526090T3 (en) 2015-10-19
PT2526090E (pt) 2015-11-30
BR112012017713A2 (pt) 2020-06-23

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