CN105051027A - 作为转染期间重排(ret)激酶抑制剂的吡啶衍生物 - Google Patents

作为转染期间重排(ret)激酶抑制剂的吡啶衍生物 Download PDF

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Publication number
CN105051027A
CN105051027A CN201480015907.3A CN201480015907A CN105051027A CN 105051027 A CN105051027 A CN 105051027A CN 201480015907 A CN201480015907 A CN 201480015907A CN 105051027 A CN105051027 A CN 105051027A
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China
Prior art keywords
alkyl
ethoxy
fluorophenyl
trifluoromethyl
acetamide
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Pending
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CN201480015907.3A
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English (en)
Chinese (zh)
Inventor
H.S.艾达姆
M.P.德马蒂诺
Z.龚
A.H.管
K.雷哈
C.吴
H.杨
H.于
Z.张
M.张
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GlaxoSmithKline Intellectual Property Development Ltd
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GlaxoSmithKline Intellectual Property Development Ltd
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Priority to CN201480015907.3A priority Critical patent/CN105051027A/zh
Publication of CN105051027A publication Critical patent/CN105051027A/zh
Pending legal-status Critical Current

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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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
CN201480015907.3A 2013-03-15 2014-03-14 作为转染期间重排(ret)激酶抑制剂的吡啶衍生物 Pending CN105051027A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201480015907.3A CN105051027A (zh) 2013-03-15 2014-03-14 作为转染期间重排(ret)激酶抑制剂的吡啶衍生物

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN2013072683 2013-03-15
CN2013090059 2013-12-20
CN2014072449 2014-02-24
CN201480015907.3A CN105051027A (zh) 2013-03-15 2014-03-14 作为转染期间重排(ret)激酶抑制剂的吡啶衍生物
PCT/IB2014/059817 WO2014141187A1 (en) 2013-03-15 2014-03-14 Pyridine derivatives as rearranged during transfection (ret) kinase inhibitors

Publications (1)

Publication Number Publication Date
CN105051027A true CN105051027A (zh) 2015-11-11

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Country Status (33)

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US (2) US9382238B2 (https=)
EP (1) EP2970191B1 (https=)
JP (1) JP2016516026A (https=)
CN (1) CN105051027A (https=)
AU (1) AU2014229233B2 (https=)
BR (1) BR112015023618A2 (https=)
CA (1) CA2905627A1 (https=)
CL (1) CL2015002514A1 (https=)
CR (1) CR20150490A (https=)
CY (1) CY1118730T1 (https=)
DK (1) DK2970191T3 (https=)
DO (1) DOP2015000244A (https=)
EA (1) EA029296B1 (https=)
ES (1) ES2616655T3 (https=)
HR (1) HRP20170363T1 (https=)
HU (1) HUE033423T2 (https=)
IL (1) IL241161A0 (https=)
LT (1) LT2970191T (https=)
ME (1) ME02664B (https=)
MX (1) MX2015012286A (https=)
NZ (1) NZ628388A (https=)
PE (1) PE20151538A1 (https=)
PH (1) PH12015502044A1 (https=)
PL (1) PL2970191T3 (https=)
PT (1) PT2970191T (https=)
RS (1) RS55710B1 (https=)
SG (1) SG11201506695UA (https=)
SI (1) SI2970191T1 (https=)
SM (1) SMT201700152T1 (https=)
TW (1) TW201524958A (https=)
UA (1) UA115264C2 (https=)
UY (1) UY35465A (https=)
WO (1) WO2014141187A1 (https=)

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CN109096264A (zh) * 2018-08-28 2018-12-28 山东理工职业学院 Ret抑制剂及其制备方法、组合物和用途
CN110036007A (zh) * 2016-09-29 2019-07-19 第一三共株式会社 吡啶化合物
WO2022017524A1 (zh) * 2020-07-23 2022-01-27 深圳晶泰科技有限公司 吡啶酮类化合物及其制备方法和应用
CN115626880A (zh) * 2022-11-15 2023-01-20 常州大学 3-硝基-5-氰基三氟甲苯的合成方法
CN115667253A (zh) * 2020-04-27 2023-01-31 伊莱利利公司 可用于抑制ret激酶的化合物
CN116438179A (zh) * 2020-11-06 2023-07-14 伊莱利利公司 作为ret激酶抑制剂的吡唑衍生物
CN116925023A (zh) * 2023-07-18 2023-10-24 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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NZ604708A (en) 2010-05-20 2015-05-29 Array Biopharma Inc Macrocyclic compounds as trk kinase inhibitors
KR20170047396A (ko) * 2014-09-08 2017-05-04 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 2-(4-(4-에톡시-6-옥소-1,6-디히드로피리딘-3-일)-2-플루오로페닐)-n-(5-(1,1,1-트리플루오로-2-메틸프로판-2-일)이속사졸-3-일)아세트아미드의 결정질 형태
EA032030B1 (ru) 2014-09-10 2019-03-29 Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед Соединения в качестве ингибиторов реаранжированной во время трансфекции (ret) киназы
PE20170705A1 (es) 2014-09-10 2017-05-21 Glaxosmithkline Ip Dev Ltd Nuevos compuestos como inhibidores de ret (reorganizado durante la transfeccion)
US10202365B2 (en) 2015-02-06 2019-02-12 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors
BR112018000808A2 (pt) 2015-07-16 2018-09-04 Array Biopharma Inc compostos de pirazolo[1,5-a]piridina substituída como inibidores de ret cinase
US10829484B2 (en) 2015-07-28 2020-11-10 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
PL3371171T3 (pl) * 2015-11-02 2024-03-25 Blueprint Medicines Corporation Inhibitory 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
WO2017161045A1 (en) * 2016-03-16 2017-09-21 Plexxikon Inc. Compounds and methods for kinase modulation and indications therefore
TW201738228A (zh) 2016-03-17 2017-11-01 藍圖醫藥公司 Ret之抑制劑
BR112018073300A2 (pt) 2016-05-13 2019-03-26 Instituto De Medicina Molecular métodos para tratamento de doenças associadas com as células ilc3
US10227329B2 (en) 2016-07-22 2019-03-12 Blueprint Medicines Corporation Compounds useful for treating disorders related to RET
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
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
US11168090B2 (en) 2017-01-18 2021-11-09 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
JP2020519672A (ja) 2017-05-15 2020-07-02 ブループリント メディシンズ コーポレイション RET阻害剤とmTORC1阻害剤との組合せ及び異常なRET活性によって媒介されるがんを処置するためのその使用
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
WO2019143991A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. SUBSTITUTED PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS AS RET KINASE INHIBITORS
EP3740491A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
CN111615514B (zh) 2018-01-18 2022-10-11 奥瑞生物药品公司 作为ret激酶抑制剂的取代的吡唑并[4,3-c]吡啶化合物
SI3773589T1 (sl) 2018-04-03 2024-03-29 Blueprint Medicines Corporation Inhibitor RET za uporabo pri zdravljenju raka, ki ima RET spremembo
EP3849986B1 (en) 2018-09-10 2022-06-08 Array Biopharma, Inc. Fused heterocyclic compounds as ret kinase inhibitors
NZ780966A (en) 2019-04-18 2026-02-27 Univ Johns Hopkins Substituted 2-amino-pyrazolyl-[1,2,4]triazolo[1,5a] pyridine derivatives and use thereof
CN115210226B (zh) * 2020-02-20 2024-01-09 广州白云山医药集团股份有限公司白云山制药总厂 喹啉类化合物
JP2023527412A (ja) 2020-05-29 2023-06-28 ブループリント メディシンズ コーポレイション プラルセチニブの固体形態
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
EP4650002A1 (en) * 2024-05-15 2025-11-19 Ludwig-Maximilians-Universität Aniline-based modulators of the nuclear receptor tlx (nr2e1)

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Cited By (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110036007A (zh) * 2016-09-29 2019-07-19 第一三共株式会社 吡啶化合物
CN110036007B (zh) * 2016-09-29 2021-10-15 第一三共株式会社 吡啶化合物
CN113788824A (zh) * 2016-09-29 2021-12-14 第一三共株式会社 吡啶化合物
CN109096264A (zh) * 2018-08-28 2018-12-28 山东理工职业学院 Ret抑制剂及其制备方法、组合物和用途
CN115667253A (zh) * 2020-04-27 2023-01-31 伊莱利利公司 可用于抑制ret激酶的化合物
WO2022017524A1 (zh) * 2020-07-23 2022-01-27 深圳晶泰科技有限公司 吡啶酮类化合物及其制备方法和应用
TWI786742B (zh) * 2020-07-23 2022-12-11 大陸商深圳晶泰科技有限公司 吡啶酮類化合物及其製備方法和應用
CN115803316B (zh) * 2020-07-23 2024-12-06 深圳晶泰科技有限公司 吡啶酮类化合物及其制备方法和应用
CN115803316A (zh) * 2020-07-23 2023-03-14 深圳晶泰科技有限公司 吡啶酮类化合物及其制备方法和应用
CN116438179A (zh) * 2020-11-06 2023-07-14 伊莱利利公司 作为ret激酶抑制剂的吡唑衍生物
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
CN115626880A (zh) * 2022-11-15 2023-01-20 常州大学 3-硝基-5-氰基三氟甲苯的合成方法
CN116925023A (zh) * 2023-07-18 2023-10-24 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
WO2025016082A1 (zh) * 2023-07-18 2025-01-23 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
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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HUE033423T2 (en) 2017-11-28
SI2970191T1 (sl) 2017-04-26
MX2015012286A (es) 2016-05-31
AU2014229233A1 (en) 2015-09-24
TW201524958A (zh) 2015-07-01
ES2616655T3 (es) 2017-06-13
HRP20170363T1 (hr) 2017-04-21
US20160002215A1 (en) 2016-01-07
CA2905627A1 (en) 2014-09-18
EP2970191B1 (en) 2016-12-21
EA201591738A1 (ru) 2016-01-29
CY1118730T1 (el) 2017-07-12
PH12015502044A1 (en) 2016-01-18
CL2015002514A1 (es) 2016-02-05
BR112015023618A2 (pt) 2017-07-18
PE20151538A1 (es) 2015-11-18
LT2970191T (lt) 2017-03-10
SG11201506695UA (en) 2015-09-29
UY35465A (es) 2014-10-31
WO2014141187A1 (en) 2014-09-18
DK2970191T3 (en) 2017-03-20
US9382238B2 (en) 2016-07-05
IL241161A0 (en) 2015-11-30
EP2970191A1 (en) 2016-01-20
SMT201700152T1 (it) 2017-05-08
PT2970191T (pt) 2017-03-23
US9789100B2 (en) 2017-10-17
CR20150490A (es) 2015-11-20
JP2016516026A (ja) 2016-06-02
NZ628388A (en) 2016-09-30
UA115264C2 (uk) 2017-10-10
EA029296B1 (ru) 2018-03-30
AU2014229233B2 (en) 2016-08-11
ME02664B (me) 2017-06-20
US20160271123A1 (en) 2016-09-22
RS55710B1 (sr) 2017-07-31
PL2970191T3 (pl) 2017-07-31
DOP2015000244A (es) 2015-12-31

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