CN107635986A - 取代的喹喔啉衍生物 - Google Patents

取代的喹喔啉衍生物 Download PDF

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Publication number
CN107635986A
CN107635986A CN201680027578.3A CN201680027578A CN107635986A CN 107635986 A CN107635986 A CN 107635986A CN 201680027578 A CN201680027578 A CN 201680027578A CN 107635986 A CN107635986 A CN 107635986A
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Prior art keywords
methyl
quinoxalin
indol
amine
pyridin
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Pending
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CN201680027578.3A
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Chinese (zh)
Inventor
C-H·R·Y·法布里蒂乌斯
M·O·诺瓦克
K·A·维克里克
A·B·萨比尼尔兹
M·D·比恩
A·M·布达
P·S·古兹克
K·R·雅库别茨
M·马丘斯扎克
K·克维辛斯科
M·M·托姆奇克
M·M·加莱佐夫斯基
A·龚德拉
L·P·杜德克
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Selvita Sp zoo
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Selvita Sp zoo
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Publication of CN107635986A publication Critical patent/CN107635986A/zh
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/42—Benzopyrazines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D403/14—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 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
    • 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
    • C07D405/10—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 linked by a carbon chain containing aromatic 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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero 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
    • C07D417/14—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201680027578.3A 2015-05-13 2016-05-12 取代的喹喔啉衍生物 Pending CN107635986A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP15001451 2015-05-13
EP15001451.2 2015-05-13
EP15460017.5 2015-05-13
EP15460017 2015-05-14
PCT/EP2016/000783 WO2016180536A1 (en) 2015-05-13 2016-05-12 Substituted quinoxaline derivatives

Publications (1)

Publication Number Publication Date
CN107635986A true CN107635986A (zh) 2018-01-26

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CN201680027578.3A Pending CN107635986A (zh) 2015-05-13 2016-05-12 取代的喹喔啉衍生物

Country Status (9)

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US (1) US20180148429A1 (enExample)
EP (1) EP3294729A1 (enExample)
JP (1) JP2018515612A (enExample)
CN (1) CN107635986A (enExample)
AU (1) AU2016261031A1 (enExample)
CA (1) CA2979302A1 (enExample)
IL (1) IL254870A0 (enExample)
TW (1) TW201713641A (enExample)
WO (1) WO2016180536A1 (enExample)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110698418A (zh) * 2019-09-11 2020-01-17 广西师范大学 一种3-芳胺基喹喔啉-2-甲酰胺类衍生物及其制备方法和应用
CN114901654A (zh) * 2019-08-06 2022-08-12 北卡罗来纳查佩尔山大学 Rna靶向配体、其组合物以及其制备和使用方法
CN115515959A (zh) * 2020-05-08 2022-12-23 默克专利股份公司 用作tead结合剂的三环杂环
CN116134016A (zh) * 2020-07-23 2023-05-16 默克专利股份公司 三环杂环

Families Citing this family (19)

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WO2018013774A1 (en) * 2016-07-14 2018-01-18 Bristol-Myers Squibb Company Bicyclic heteroaryl substituted compounds
WO2018087021A1 (en) 2016-11-08 2018-05-17 Merck Patent Gmbh Substituted quinoxaline derivatives as inhibitors of pfkfb
GB201705263D0 (en) * 2017-03-31 2017-05-17 Probiodrug Ag Novel inhibitors
WO2019065516A1 (ja) * 2017-09-26 2019-04-04 日本曹達株式会社 キノリン化合物および農園芸用殺菌剤
CN111566105A (zh) 2018-01-08 2020-08-21 豪夫迈·罗氏有限公司 作为MAGL抑制剂的八氢吡啶并[1,2-α]吡嗪类化合物
ES2942319T3 (es) 2018-03-22 2023-05-31 Hoffmann La Roche Inhibidores de oxacina monoacilglicerol lipasa (MAGL)
US12448374B2 (en) 2018-06-07 2025-10-21 Disarm Therapeutics, Inc. Inhibitors of SARM1
HUE067912T2 (hu) 2018-08-13 2024-11-28 Hoffmann La Roche Új heterociklusos vegyületek, mint monoacil-glicerin-lipáz inhibitorok
WO2020080979A1 (en) * 2018-10-15 2020-04-23 Gero Discovery Limited Liability Company Pfkfb3 inhibitors and their uses
US11034669B2 (en) 2018-11-30 2021-06-15 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
EP3897670A4 (en) 2018-12-19 2022-09-07 Disarm Therapeutics, Inc. MRSA1 INHIBITORS IN COMBINATION WITH NEUROPROTECTIVE AGENTS
CA3151516A1 (en) 2019-09-12 2021-03-18 F. Hoffmann-La Roche Ag 4,4a,5,7,8,8a-hexapyrido[4,3-b][1,4]oxazin-3-one compounds as magl inhibitors
WO2021058416A1 (en) 2019-09-23 2021-04-01 F. Hoffmann-La Roche Ag Heterocyclic compounds
JP7785755B2 (ja) 2020-08-26 2025-12-15 エフ． ホフマン－ラ ロシュ アーゲー Ｍａｇｌ阻害剤として有用な複素環化合物
CA3190277A1 (en) 2020-09-03 2022-03-10 Joerg Benz Heterocyclic compounds
WO2022115521A1 (en) 2020-11-25 2022-06-02 Servier Pharmaceuticals, Llc (heteo)aryl substituted pyrrolo-, pyrazolo- and triazolopyridazine derivates as mat2a inhibitors
CN118119608A (zh) * 2021-06-02 2024-05-31 北卡罗来纳查佩尔山大学 Rna靶向配体、其组合物以及制备和使用其的方法
EP4543870A1 (en) 2022-06-24 2025-04-30 F. Hoffmann-La Roche AG New heterocyclic-carbonyl-cyclic compounds as magl inhibitors
WO2025084787A1 (ko) * 2023-10-17 2025-04-24 가천대학교 산학협력단 신규 퀴녹살린 화합물, 이의 제조방법 및 이의 용도

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US5633218A (en) * 1995-05-24 1997-05-27 E. I. Du Pont De Nemours And Company Herbicidal benzodioxoles and benzodioxanes
WO2011103557A1 (en) * 2010-02-22 2011-08-25 Advanced Cancer Therapeutics, Llc Small molecule inhibitors of pfkfb3 and glycolytic flux and their methods of use as anti-cancer therapeutics
WO2012176856A2 (en) * 2011-06-24 2012-12-27 Ishihara Sangyo Kaisha, Ltd. Pesticide
US20140128392A1 (en) * 2009-03-19 2014-05-08 Bioenergenix Heterocyclic compounds for the inhibition of pask
CN104520274A (zh) * 2012-03-29 2015-04-15 先进癌症治疗有限责任公司 Pfkfb3抑制剂和用作抗癌治疗剂的方法

Patent Citations (5)

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US5633218A (en) * 1995-05-24 1997-05-27 E. I. Du Pont De Nemours And Company Herbicidal benzodioxoles and benzodioxanes
US20140128392A1 (en) * 2009-03-19 2014-05-08 Bioenergenix Heterocyclic compounds for the inhibition of pask
WO2011103557A1 (en) * 2010-02-22 2011-08-25 Advanced Cancer Therapeutics, Llc Small molecule inhibitors of pfkfb3 and glycolytic flux and their methods of use as anti-cancer therapeutics
WO2012176856A2 (en) * 2011-06-24 2012-12-27 Ishihara Sangyo Kaisha, Ltd. Pesticide
CN104520274A (zh) * 2012-03-29 2015-04-15 先进癌症治疗有限责任公司 Pfkfb3抑制剂和用作抗癌治疗剂的方法

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Title
DARBY G. BROOKE, ET AL: "Targeting the Warburg Effect in cancer; relationships for 2-arylpyridazinones as inhibitors of the key glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3)", 《BIOORGANIC & MEDICINAL CHEMISTRY》 *

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114901654A (zh) * 2019-08-06 2022-08-12 北卡罗来纳查佩尔山大学 Rna靶向配体、其组合物以及其制备和使用方法
CN114901654B (zh) * 2019-08-06 2025-08-05 北卡罗来纳查佩尔山大学 Rna靶向配体、其组合物以及其制备和使用方法
CN110698418A (zh) * 2019-09-11 2020-01-17 广西师范大学 一种3-芳胺基喹喔啉-2-甲酰胺类衍生物及其制备方法和应用
CN110698418B (zh) * 2019-09-11 2022-07-01 广西师范大学 一种3-芳胺基喹喔啉-2-甲酰胺类衍生物及其制备方法和应用
CN115515959A (zh) * 2020-05-08 2022-12-23 默克专利股份公司 用作tead结合剂的三环杂环
CN116134016A (zh) * 2020-07-23 2023-05-16 默克专利股份公司 三环杂环

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US20180148429A1 (en) 2018-05-31
TW201713641A (zh) 2017-04-16
WO2016180536A1 (en) 2016-11-17
EP3294729A1 (en) 2018-03-21
JP2018515612A (ja) 2018-06-14
CA2979302A1 (en) 2016-11-17
AU2016261031A1 (en) 2017-10-05
IL254870A0 (en) 2017-12-31

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Application publication date: 20180126