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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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/69—Two or more oxygen atoms
    • 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
    • C07D413/12—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 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)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (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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US (2) US9382238B2 (enExample)
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)
UY (1) UY35465A (enExample)
WO (1) WO2014141187A1 (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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AU2015313894A1 (en) * 2014-09-08 2017-03-23 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
BR112017004897A2 (pt) * 2014-09-10 2017-12-12 Glaxosmithkline Ip Dev Ltd compostos inovadores como inibidores rearranjados durante a transfecção (ret)
EP3517526B1 (en) 2014-09-10 2020-08-19 GlaxoSmithKline Intellectual Property Development Limited Pyridinones as rearranged during transfection (ret) inhibitors
US10202365B2 (en) 2015-02-06 2019-02-12 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors
CA2992586A1 (en) 2015-07-16 2017-01-19 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
US10829484B2 (en) 2015-07-28 2020-11-10 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
RS65069B1 (sr) * 2015-11-02 2024-02-29 Blueprint Medicines Corp Inhibitori ret-a
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
US10160747B2 (en) 2016-03-16 2018-12-25 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
AR107912A1 (es) 2016-03-17 2018-06-28 Blueprint Medicines Corp Inhibidores de ret
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JP2018052878A (ja) 2016-09-29 2018-04-05 第一三共株式会社 ピリジン化合物
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
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
JP6888101B2 (ja) 2017-01-18 2021-06-16 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置換ピラゾロ[1,5−a]ピラジン化合物
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US20210290620A1 (en) 2017-05-15 2021-09-23 Blueprint Medicines Corporation Combinations of RET Inhibitors and mTORC1 Inhibitors and Uses Thereof for the Treatment of Cancer Mediated by Aberrant RET Activity
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
TWI876442B (zh) 2017-10-10 2025-03-11 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
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
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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
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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UA115264C2 (uk) 2017-10-10
PH12015502044A1 (en) 2016-01-18
BR112015023618A2 (pt) 2017-07-18
CN105051027A (zh) 2015-11-11
HRP20170363T1 (hr) 2017-04-21
SMT201700152T1 (it) 2017-05-08
SG11201506695UA (en) 2015-09-29
ME02664B (me) 2017-06-20
CL2015002514A1 (es) 2016-02-05
US20160002215A1 (en) 2016-01-07
WO2014141187A1 (en) 2014-09-18
CY1118730T1 (el) 2017-07-12
CR20150490A (es) 2015-11-20
HUE033423T2 (en) 2017-11-28
AU2014229233B2 (en) 2016-08-11
UY35465A (es) 2014-10-31
LT2970191T (lt) 2017-03-10
ES2616655T3 (es) 2017-06-13
EP2970191B1 (en) 2016-12-21
CA2905627A1 (en) 2014-09-18
US9789100B2 (en) 2017-10-17
PT2970191T (pt) 2017-03-23
EP2970191A1 (en) 2016-01-20
NZ628388A (en) 2016-09-30
SI2970191T1 (sl) 2017-04-26
DK2970191T3 (en) 2017-03-20
PL2970191T3 (pl) 2017-07-31
DOP2015000244A (es) 2015-12-31
AU2014229233A1 (en) 2015-09-24
PE20151538A1 (es) 2015-11-18
EA029296B1 (ru) 2018-03-30
TW201524958A (zh) 2015-07-01
MX2015012286A (es) 2016-05-31
EA201591738A1 (ru) 2016-01-29
RS55710B1 (sr) 2017-07-31
IL241161A0 (en) 2015-11-30
US20160271123A1 (en) 2016-09-22
US9382238B2 (en) 2016-07-05

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