CN108495855B - 作为mnk抑制剂的稠合噻唑并嘧啶衍生物 - Google Patents

作为mnk抑制剂的稠合噻唑并嘧啶衍生物 Download PDF

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Publication number
CN108495855B
CN108495855B CN201680079581.XA CN201680079581A CN108495855B CN 108495855 B CN108495855 B CN 108495855B CN 201680079581 A CN201680079581 A CN 201680079581A CN 108495855 B CN108495855 B CN 108495855B
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compound
substituted
heterocycloalkyl
alkyl
mixture
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CN108495855A (zh
Inventor
乔恩·詹姆斯·温特-霍尔特
爱德华·贾尔斯·麦基弗
马丁·安布勒
史蒂芬·里维斯
乔安妮·奥萨波尼
凯利·韦伯-史密斯
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LifeArc
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LifeArc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/429Thiazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201680079581.XA 2015-11-20 2016-11-16 作为mnk抑制剂的稠合噻唑并嘧啶衍生物 Expired - Fee Related CN108495855B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1520500.8A GB201520500D0 (en) 2015-11-20 2015-11-20 Compounds
GB1520500.8 2015-11-20
PCT/GB2016/053580 WO2017085484A1 (en) 2015-11-20 2016-11-16 Fused thiazolopyrimidine derivatives as mnks inhibitors

Publications (2)

Publication Number Publication Date
CN108495855A CN108495855A (zh) 2018-09-04
CN108495855B true CN108495855B (zh) 2022-05-31

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CN201680079581.XA Expired - Fee Related CN108495855B (zh) 2015-11-20 2016-11-16 作为mnk抑制剂的稠合噻唑并嘧啶衍生物

Country Status (9)

Country Link
US (2) US10669284B2 (https=)
EP (2) EP3377501B1 (https=)
JP (2) JP6928605B2 (https=)
CN (1) CN108495855B (https=)
AU (1) AU2016355104B2 (https=)
CA (2) CA3240011A1 (https=)
ES (2) ES2981048T3 (https=)
GB (1) GB201520500D0 (https=)
WO (1) WO2017085484A1 (https=)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI713455B (zh) 2014-06-25 2020-12-21 美商伊凡克特治療公司 MnK抑制劑及其相關方法
CA3053493A1 (en) 2017-02-14 2018-08-23 Effector Therapeutics, Inc. Piperidine-substituted mnk inhibitors and methods related thereto
CN109020957B (zh) * 2017-06-12 2023-01-13 南京天印健华医药科技有限公司 作为mnk抑制剂的杂环化合物
CN113286592A (zh) 2018-10-24 2021-08-20 效应治疗股份有限公司 Mnk抑制剂的结晶形式
CN110903286B (zh) * 2019-12-16 2021-09-24 沈阳药科大学 4,6-双取代吡啶[3,2-d]嘧啶类化合物及其制备和应用
JP2023533616A (ja) * 2020-06-30 2023-08-03 4イー セラピューティクス, インコーポレイテッド Mnk阻害を示すピリジン-1,5-ジオン及びそれらの使用方法
CN118146134A (zh) * 2024-02-07 2024-06-07 南方海洋科学与工程广东省实验室(湛江) 一种3-羟基吡咯烷衍生物及其制备方法与应用

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005067546A2 (en) * 2004-01-13 2005-07-28 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
WO2008057402A2 (en) * 2006-11-02 2008-05-15 Cytovia, Inc. N-aryl-isoxazolopyrimidin-4-amines and related compounds as activators of caspases and inducers of apoptosis and the use thereof
WO2009065596A2 (en) * 2007-11-22 2009-05-28 Develogen Aktiengesellschaft Use of mnk inhibitors for the treatment of alzheimer's disease
CN102002044A (zh) * 2010-09-29 2011-04-06 中国药科大学 嘌呤-8-酮类及噻唑并嘧啶类衍生物及其制备方法和医药用途
CN102858783A (zh) * 2010-02-26 2013-01-02 贝林格尔.英格海姆国际有限公司 用于药物组合物的含取代的烷基的噻吩并嘧啶
WO2014135480A1 (en) * 2013-03-06 2014-09-12 Bayer Pharma Aktiengesellschaft Substituted thiazolopyrimidines

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NZ207394A (en) 1983-03-08 1987-03-06 Commw Serum Lab Commission Detecting or determining sequence of amino acids
WO2005080377A1 (ja) 2004-02-20 2005-09-01 Kirin Beer Kabushiki Kaisha TGFβ阻害活性を有する化合物およびそれを含んでなる医薬組成物
JPWO2005095419A1 (ja) 2004-04-01 2008-02-21 武田薬品工業株式会社 チアゾロピリミジン誘導体
US7977345B2 (en) 2004-07-02 2011-07-12 Exelixis, Inc. c-MET modulators and method of use
CA2651898A1 (en) 2006-04-07 2007-10-18 Develogen Aktiengesellschaft Thienopyrimidines having mnk1/mnk2 inhibiting activity for pharmaceutical compositions
EP1889847A1 (en) 2006-07-10 2008-02-20 DeveloGen Aktiengesellschaft Pyrrolopyrimidines for pharmaceutical compositions
UY32072A (es) * 2008-08-26 2010-03-26 Boehringer Ingelheim Int Tienopirimidinas para composiciones farmacéuticas
UY33241A (es) 2010-02-26 2011-09-30 Boehringer Ingelheim Int ?Tienopirimidinas que contienen heterocicloalquilo para composiciones farmacéuticas?.
JP5575274B2 (ja) 2010-02-26 2014-08-20 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 医薬組成物のためのmnkl/mnk2阻害活性を有する4−[シクロアルキルオキシ(ヘテロ)アリールアミノ]チエノ「2,3−d]ピリミジン
CA2899662A1 (en) 2013-02-01 2014-08-07 Bayer Pharma Aktiengesellschaft Substituted pyrazolopyrimidinylamino-indazoles
JP2016527216A (ja) * 2013-07-08 2016-09-08 バイエル・ファルマ・アクティエンゲゼルシャフト 置換ピラゾロピリジン

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005067546A2 (en) * 2004-01-13 2005-07-28 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
WO2008057402A2 (en) * 2006-11-02 2008-05-15 Cytovia, Inc. N-aryl-isoxazolopyrimidin-4-amines and related compounds as activators of caspases and inducers of apoptosis and the use thereof
WO2009065596A2 (en) * 2007-11-22 2009-05-28 Develogen Aktiengesellschaft Use of mnk inhibitors for the treatment of alzheimer's disease
CN102858783A (zh) * 2010-02-26 2013-01-02 贝林格尔.英格海姆国际有限公司 用于药物组合物的含取代的烷基的噻吩并嘧啶
CN102002044A (zh) * 2010-09-29 2011-04-06 中国药科大学 嘌呤-8-酮类及噻唑并嘧啶类衍生物及其制备方法和医药用途
WO2014135480A1 (en) * 2013-03-06 2014-09-12 Bayer Pharma Aktiengesellschaft Substituted thiazolopyrimidines

Also Published As

Publication number Publication date
JP6928605B2 (ja) 2021-09-01
US20180346483A1 (en) 2018-12-06
JP2018534314A (ja) 2018-11-22
EP3377501B1 (en) 2021-08-18
US20200247822A1 (en) 2020-08-06
CA3240011A1 (en) 2017-05-26
EP3939981A1 (en) 2022-01-19
JP2021073306A (ja) 2021-05-13
AU2016355104A1 (en) 2018-05-24
US11136338B2 (en) 2021-10-05
GB201520500D0 (en) 2016-01-06
EP3939981B1 (en) 2024-04-03
HK1253575A1 (en) 2019-06-21
ES2893154T3 (es) 2022-02-08
WO2017085484A1 (en) 2017-05-26
CN108495855A (zh) 2018-09-04
JP7181647B2 (ja) 2022-12-01
AU2016355104B2 (en) 2021-01-28
EP3939981C0 (en) 2024-04-03
ES2981048T3 (es) 2024-10-07
CA3003559A1 (en) 2017-05-26
CA3003559C (en) 2024-09-10
US10669284B2 (en) 2020-06-02
EP3377501A1 (en) 2018-09-26

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