CN102812006B - 新型抗疟疾试剂 - Google Patents

新型抗疟疾试剂 Download PDF

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Publication number
CN102812006B
CN102812006B CN201180005928.3A CN201180005928A CN102812006B CN 102812006 B CN102812006 B CN 102812006B CN 201180005928 A CN201180005928 A CN 201180005928A CN 102812006 B CN102812006 B CN 102812006B
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base
phenyl
pyridine
amine
amino
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Expired - Fee Related
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CN102812006A (zh
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M·J·韦提
D·哈迪克
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MMV Medicines for Malaria Venture
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MMV Medicines for Malaria Venture
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
    • 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
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/10—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • 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

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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)
CN201180005928.3A 2010-01-18 2011-01-17 新型抗疟疾试剂 Expired - Fee Related CN102812006B (zh)

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
CN102812006A CN102812006A (zh) 2012-12-05
CN102812006B true CN102812006B (zh) 2016-01-20

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CN201180005928.3A Expired - Fee Related CN102812006B (zh) 2010-01-18 2011-01-17 新型抗疟疾试剂

Country Status (17)

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

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ES2663222T3 (es) 2008-12-19 2018-04-11 Vertex Pharmaceuticals Incorporated Derivados de pirazina útiles como inhibidores de la quinasa ATR
US9630956B2 (en) 2010-05-12 2017-04-25 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
JP5856151B2 (ja) * 2010-05-12 2016-02-09 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ａｔｒキナーゼ阻害剤として有用な２−アミノピリジン誘導体
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
AR085607A1 (es) * 2011-03-04 2013-10-16 Lexicon Pharmaceuticals Inc Inhibidores de la mst1 quinasa y metodos para su utilizacion
WO2013049859A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Treating pancreatic cancer and non-small cell lung cancer with atr inhibitors
SG10201606774UA (en) 2011-09-30 2016-10-28 Vertex Pharma Processes for making compounds useful as inhibitors of atr kinase
JP6226889B2 (ja) * 2012-02-17 2017-11-08 ユニバーシティ・オブ・ケープ・タウンＵｎｉｖｅｒｓｉｔｙ Ｏｆ Ｃａｐｅ Ｔｏｗｎ 新規抗マラリア薬
CA2869309C (en) 2012-04-05 2021-02-09 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase and combination therapies thereof
US8999632B2 (en) 2012-10-04 2015-04-07 Vertex Pharmaceuticals Incorporated Method for measuring ATR inhibition mediated increases in DNA damage
EP2970186B1 (en) * 2013-03-15 2020-06-10 Dow AgroSciences LLC 4-amino-6-(heterocyclic)picolinates and 6-amino-2-(heterocyclic) pyrimidine-4-carboxylates and their use as herbicides
CN110583663A (zh) 2013-03-15 2019-12-20 美国陶氏益农公司 式(i)化合物及其作为除草剂的用途
EP3134397A1 (en) 2014-04-24 2017-03-01 Novartis AG Amino pyrazine derivatives as phosphatidylinositol 3-kinase inhibitors
KR20160145780A (ko) 2014-04-24 2016-12-20 노파르티스 아게 포스파티딜이노시톨 3-키나제 억제제로서의 아미노 피리딘 유도체
KR20160141856A (ko) 2014-04-24 2016-12-09 노파르티스 아게 포스파티딜이노시톨 3-키나제 억제제로서의 피라진 유도체
JP7109919B2 (ja) * 2015-03-20 2022-08-01 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト Ｕｓｐ７阻害剤化合物及び使用方法
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
BR112020012651A2 (pt) * 2017-12-22 2020-12-01 Ravenna Pharmaceuticals, Inc. compostos derivados de aril-bipiridina amina como inibidores da fosfatidilinositol fosfato quinase, composição farmacêutica compreendendo os mesmos e usos terapêuticos dos ditos compostos
BR112020018094A2 (pt) 2018-03-08 2020-12-22 Incyte Corporation Compostos de aminopirazina diol como inibidores de pi3k-¿
US11046658B2 (en) 2018-07-02 2021-06-29 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
JP2025531008A (ja) 2022-08-09 2025-09-19 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング フロピリミジン誘導体
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

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US7220863B2 (en) * 2004-08-31 2007-05-22 Korea Research Institute Of Chemical Technology Process for preparing 2-aminopyridine derivatives
CN101555248A (zh) * 2009-05-22 2009-10-14 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

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US7220863B2 (en) * 2004-08-31 2007-05-22 Korea Research Institute Of Chemical Technology Process for preparing 2-aminopyridine derivatives
WO2007032016A1 (en) * 2005-09-12 2007-03-22 Council Of Scientific And Industrial Research An antimalarial baylis-hillman adducts and a process for the preparation thereof
CN101555248A (zh) * 2009-05-22 2009-10-14 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

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Identification and characterisation of 2-aminopyridine inhibitors of checkpoint kinase 2;Stephen Hilton，等;《Bioorganic & Medicinal Chemistry》;20091206;第18卷;第708-711页 *
Palladium-Catalyzed Cross-Coupling Reactions of Pyridylboronic Acids with Heteroaryl Halides Bearing a Primary Amine Group: Synthesis of Highly Substituted Bipyridines and Pyrazinopyridines;Amy E. Thompson，等;《J. Org. Chem》;20041213;第79卷(第1期);第390页化合物33 *
Total Synthesis of the Indolizidinium Alkaloid Ficuseptine;Franz Bracher，等;《Eur. J. Org. Chem》;20020701(第14期);第2289页化合物4 *

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US9024033B2 (en) 2015-05-05
WO2011086531A2 (en) 2011-07-21
HK1175472A1 (zh) 2013-07-05
CA2787121A1 (en) 2011-07-21
CA2787121C (en) 2018-07-17
HUE027946T2 (en) 2016-11-28
SI2526090T1 (sl) 2015-11-30
BR112012017713A2 (pt) 2020-06-23
US20120295905A1 (en) 2012-11-22
WO2011086531A3 (en) 2011-09-29
RS54339B1 (sr) 2016-02-29
EP2526090B1 (en) 2015-08-19
ME02315B (me) 2016-06-20
PL2526090T3 (pl) 2016-04-29
EP2526090A2 (en) 2012-11-28
DK2526090T3 (en) 2015-10-19
ES2551875T3 (es) 2015-11-24
CN102812006A (zh) 2012-12-05
JP2013517264A (ja) 2013-05-16
PT2526090E (pt) 2015-11-30
JP5735986B2 (ja) 2015-06-17
SMT201500291B (it) 2016-01-08
HRP20151143T1 (hr) 2015-12-04

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