JP2016516026A - Rearrangedduringtransfection(ret)キナーゼ阻害剤としてのピリジン誘導体 - Google Patents

Rearrangedduringtransfection(ret)キナーゼ阻害剤としてのピリジン誘導体 Download PDF

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Publication number
JP2016516026A
JP2016516026A JP2015562529A JP2015562529A JP2016516026A JP 2016516026 A JP2016516026 A JP 2016516026A JP 2015562529 A JP2015562529 A JP 2015562529A JP 2015562529 A JP2015562529 A JP 2015562529A JP 2016516026 A JP2016516026 A JP 2016516026A
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alkyl
ethoxy
fluorophenyl
acetamide
trifluoromethyl
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Japanese (ja)
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JP2016516026A5 (enExample
Inventor
ヒラリー、シェンク、アイダム
マイケル、ピー.デマーティノ
ゴン、ゼン
エイミー、ホイピン、グアン
カウシク、ラハ
チェンデ、ウー
ヤン、ハイイン
ユ、ハイユ
チャン、ジリウ
ムイ、チュン
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GlaxoSmithKline Intellectual Property Development Ltd
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GlaxoSmithKline Intellectual Property Development Ltd
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Publication of JP2016516026A publication Critical patent/JP2016516026A/ja
Publication of JP2016516026A5 publication Critical patent/JP2016516026A5/ja
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    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • C07D401/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/69Two or more oxygen atoms
    • 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
    • C07D413/12Heterocyclic 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 chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
JP2015562529A 2013-03-15 2014-03-14 Rearrangedduringtransfection(ret)キナーゼ阻害剤としてのピリジン誘導体 Pending JP2016516026A (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
CNPCT/CN2013/072683 2013-03-15
CN2013072683 2013-03-15
CN2013090059 2013-12-20
CNPCT/CN2013/090059 2013-12-20
CNPCT/CN2014/072449 2014-02-24
CN2014072449 2014-02-24
PCT/IB2014/059817 WO2014141187A1 (en) 2013-03-15 2014-03-14 Pyridine derivatives as rearranged during transfection (ret) kinase inhibitors

Publications (2)

Publication Number Publication Date
JP2016516026A true JP2016516026A (ja) 2016-06-02
JP2016516026A5 JP2016516026A5 (enExample) 2017-04-13

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JP2015562529A Pending JP2016516026A (ja) 2013-03-15 2014-03-14 Rearrangedduringtransfection(ret)キナーゼ阻害剤としてのピリジン誘導体

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EP (1) EP2970191B1 (enExample)
JP (1) JP2016516026A (enExample)
CN (1) CN105051027A (enExample)
AU (1) AU2014229233B2 (enExample)
BR (1) BR112015023618A2 (enExample)
CA (1) CA2905627A1 (enExample)
CL (1) CL2015002514A1 (enExample)
CR (1) CR20150490A (enExample)
CY (1) CY1118730T1 (enExample)
DK (1) DK2970191T3 (enExample)
DO (1) DOP2015000244A (enExample)
EA (1) EA029296B1 (enExample)
ES (1) ES2616655T3 (enExample)
HR (1) HRP20170363T1 (enExample)
HU (1) HUE033423T2 (enExample)
IL (1) IL241161A0 (enExample)
LT (1) LT2970191T (enExample)
ME (1) ME02664B (enExample)
MX (1) MX2015012286A (enExample)
NZ (1) NZ628388A (enExample)
PE (1) PE20151538A1 (enExample)
PH (1) PH12015502044A1 (enExample)
PL (1) PL2970191T3 (enExample)
PT (1) PT2970191T (enExample)
RS (1) RS55710B1 (enExample)
SG (1) SG11201506695UA (enExample)
SI (1) SI2970191T1 (enExample)
SM (1) SMT201700152T1 (enExample)
TW (1) TW201524958A (enExample)
UA (1) UA115264C2 (enExample)
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JP2023512546A (ja) * 2020-02-20 2023-03-27 広州白雲山医薬集団股▲フン▼有限公司白雲山制薬総廠 キノリン系化合物

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KR102015402B1 (ko) 2010-05-20 2019-08-28 어레이 바이오파마 인크. Trk 키나제 저해제로서의 매크로시클릭 화합물
WO2016038519A1 (en) * 2014-09-08 2016-03-17 Glaxosmithkline Intellectual Property Development Limited Crystalline forms of 2-(4-(4-ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-n-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)acetamide
CR20170094A (es) 2014-09-10 2017-05-08 Glaxosmithkline Ip Dev Ltd Nuevos compuestos como inhibidores de reorganizado durante la transfección (ret)
AU2015313841B2 (en) 2014-09-10 2018-03-08 Glaxosmithkline Intellectual Property Development Limited Pyridone derivatives as rearranged during transfection (RET) kinase inhibitors
WO2016127074A1 (en) 2015-02-06 2016-08-11 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as ret inhibitors
HUE053067T2 (hu) 2015-07-16 2021-06-28 Array Biopharma Inc Helyettesített pirazolo[1,5-A]piridin vegyületek, mint RET kináz inhibitorok
WO2017019804A2 (en) 2015-07-28 2017-02-02 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
NZ742351A (en) 2015-11-02 2023-03-31 Blueprint Medicines Corp Inhibitors of ret
WO2017145050A1 (en) 2016-02-23 2017-08-31 Glaxosmithkline Intellectual Property Development Limited Pyridylpyridone derivative useful as a ret kinase inhibitor in the treatment of ibs and cancer
EP3430005B1 (en) 2016-03-16 2021-12-08 Plexxikon Inc. Compounds and methods for kinase modulation and indications therefore
UY37155A (es) 2016-03-17 2017-10-31 Blueprint Medicines Corp Inhibidores de ret
AU2017263174A1 (en) 2016-05-13 2018-12-13 Instituto de Medicina Molecular João Lobo Antunes Methods of treating diseases associated with ILC3 cells
WO2018017983A1 (en) 2016-07-22 2018-01-25 Blueprint Medicines Corporation Compounds useful for treating disorders related to ret
JP2018052878A (ja) * 2016-09-29 2018-04-05 第一三共株式会社 ピリジン化合物
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
TWI752098B (zh) 2016-10-10 2022-01-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
US11168090B2 (en) 2017-01-18 2021-11-09 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
CN110891573A (zh) 2017-05-15 2020-03-17 缆图药品公司 Ret抑制剂和mtorc1抑制剂的组合及其用于治疗由异常ret活性介导的癌症的用途
US10093648B1 (en) * 2017-09-22 2018-10-09 Celgene Corporation Crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione hemihydrate, compositions and methods of use thereof
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
TWI812649B (zh) 2017-10-10 2023-08-21 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
EP3740490A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors
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CN109096264B (zh) * 2018-08-28 2019-08-23 山东理工职业学院 Ret抑制剂及其制备方法、组合物和用途
JP2022500383A (ja) 2018-09-10 2022-01-04 アレイ バイオファーマ インコーポレイテッド Retキナーゼ阻害剤としての縮合複素環式化合物
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TWI777509B (zh) * 2020-04-27 2022-09-11 美商美國禮來大藥廠 用於抑制ret激酶之化合物
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IL302542A (en) 2020-11-06 2023-07-01 Lilly Co Eli Pyrazole derivatives as RET KINASE inhibitors
JP2024522938A (ja) 2021-06-03 2024-06-21 フンダサン デー.アンナ ジ ソーメル チャンパリマウド エー ドクトル カルロス モンテス チャンパリマウド 脳-脂肪回路を介してilc2および肥満度を制御する神経-間葉単位
CN115626880B (zh) * 2022-11-15 2023-11-14 常州大学 3-硝基-5-氰基三氟甲苯的合成方法
CN116925023B (zh) * 2023-07-18 2025-11-21 江苏桐孚高新材料有限公司 2-全氟烷基-4h-吡喃-4-酮衍生物的改进合成方法
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Cited By (3)

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Publication number Priority date Publication date Assignee Title
JP2023512546A (ja) * 2020-02-20 2023-03-27 広州白雲山医薬集団股▲フン▼有限公司白雲山制薬総廠 キノリン系化合物
JP7461605B2 (ja) 2020-02-20 2024-04-04 広州白雲山医薬集団股▲フン▼有限公司白雲山制薬総廠 キノリン系化合物
US12565481B2 (en) 2020-02-20 2026-03-03 Guangzhou Baiyunshan Pharmaceutical Holdings Co., Ltd. Baiyunshan Pharmaceutical General Factory 6,7-dimethoxy-3-(pyridin-2-yl)quinoline compounds for inhibiting RET

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CY1118730T1 (el) 2017-07-12
WO2014141187A1 (en) 2014-09-18
CL2015002514A1 (es) 2016-02-05
DOP2015000244A (es) 2015-12-31
RS55710B1 (sr) 2017-07-31
CA2905627A1 (en) 2014-09-18
SMT201700152T1 (it) 2017-05-08
UA115264C2 (uk) 2017-10-10
SI2970191T1 (sl) 2017-04-26
LT2970191T (lt) 2017-03-10
EP2970191A1 (en) 2016-01-20
AU2014229233B2 (en) 2016-08-11
BR112015023618A2 (pt) 2017-07-18
PH12015502044A1 (en) 2016-01-18
HUE033423T2 (en) 2017-11-28
NZ628388A (en) 2016-09-30
US9382238B2 (en) 2016-07-05
ME02664B (me) 2017-06-20
AU2014229233A1 (en) 2015-09-24
TW201524958A (zh) 2015-07-01
SG11201506695UA (en) 2015-09-29
US9789100B2 (en) 2017-10-17
PT2970191T (pt) 2017-03-23
PL2970191T3 (pl) 2017-07-31
US20160271123A1 (en) 2016-09-22
US20160002215A1 (en) 2016-01-07
EP2970191B1 (en) 2016-12-21
PE20151538A1 (es) 2015-11-18
IL241161A0 (en) 2015-11-30
EA201591738A1 (ru) 2016-01-29
CR20150490A (es) 2015-11-20
MX2015012286A (es) 2016-05-31
UY35465A (es) 2014-10-31
HRP20170363T1 (hr) 2017-04-21
ES2616655T3 (es) 2017-06-13
DK2970191T3 (en) 2017-03-20
EA029296B1 (ru) 2018-03-30
CN105051027A (zh) 2015-11-11

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