KR102455518B1 - ROS1 저해제로서 치환된 4,5,6,7-테트라히드로피라졸로[1,5-a]피리미딘 유도체 및 2,3-디히드로-1H-이미다조[1,2-b]피라졸 유도체 - Google Patents

ROS1 저해제로서 치환된 4,5,6,7-테트라히드로피라졸로[1,5-a]피리미딘 유도체 및 2,3-디히드로-1H-이미다조[1,2-b]피라졸 유도체 Download PDF

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KR102455518B1
KR102455518B1 KR1020167027337A KR20167027337A KR102455518B1 KR 102455518 B1 KR102455518 B1 KR 102455518B1 KR 1020167027337 A KR1020167027337 A KR 1020167027337A KR 20167027337 A KR20167027337 A KR 20167027337A KR 102455518 B1 KR102455518 B1 KR 102455518B1
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alkyl
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hydrogen
alkyloxy
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KR20160137566A (ko
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라우렌스 앤 메벨렉
마태우 루도빅 진티
티에리 프란체스코 알랭 쟌 주젬무
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얀센 파마슈티카 엔.브이.
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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
    • A61K31/495Heterocyclic 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/4151,2-Diazoles
    • A61K31/41621,2-Diazoles 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
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41881,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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
    • A61K31/4409Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
KR1020167027337A 2014-03-27 2015-03-26 ROS1 저해제로서 치환된 4,5,6,7-테트라히드로피라졸로[1,5-a]피리미딘 유도체 및 2,3-디히드로-1H-이미다조[1,2-b]피라졸 유도체 Active KR102455518B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14161959 2014-03-27
EP14161959.3 2014-03-27
PCT/EP2015/056501 WO2015144801A1 (en) 2014-03-27 2015-03-26 SUBSTITUTED 4,5,6,7-TETRAHYDRO-PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AND 2,3-DIHYDRO-1H-IMIDAZO[1,2-b]PYRAZOLE DERIVATIVES AS ROS1 INHIBITORS

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KR20160137566A KR20160137566A (ko) 2016-11-30
KR102455518B1 true KR102455518B1 (ko) 2022-10-14

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US (1) US10342795B2 (cg-RX-API-DMAC7.html)
EP (1) EP3126366B1 (cg-RX-API-DMAC7.html)
JP (1) JP6527167B2 (cg-RX-API-DMAC7.html)
KR (1) KR102455518B1 (cg-RX-API-DMAC7.html)
CN (1) CN106132967B (cg-RX-API-DMAC7.html)
AU (1) AU2015238298B2 (cg-RX-API-DMAC7.html)
BR (1) BR112016021507B1 (cg-RX-API-DMAC7.html)
CA (1) CA2941206C (cg-RX-API-DMAC7.html)
EA (1) EA031639B1 (cg-RX-API-DMAC7.html)
ES (1) ES2686747T3 (cg-RX-API-DMAC7.html)
IL (1) IL247948B (cg-RX-API-DMAC7.html)
MX (1) MX367913B (cg-RX-API-DMAC7.html)
WO (1) WO2015144801A1 (cg-RX-API-DMAC7.html)

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CN106580982B (zh) * 2016-11-26 2017-09-22 王玉美 一种治疗药物流产后子宫出血的药物
CN106866536A (zh) * 2017-04-12 2017-06-20 中国农业大学 一种制备4‑卤代‑5‑氨基吡唑的方法
JP7069295B2 (ja) * 2017-08-17 2022-05-17 エックスダブリューファルマ リミテッド 活性酸素種スカベンジャー誘導体の調製および使用
CN114364798A (zh) 2019-03-21 2022-04-15 欧恩科斯欧公司 用于治疗癌症的Dbait分子与激酶抑制剂的组合
US20220401436A1 (en) 2019-11-08 2022-12-22 INSERM (Institute National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
CN111087398A (zh) * 2019-12-24 2020-05-01 上海万巷制药有限公司 一种制备拉罗替尼中间体的清洁工艺
EP4105206A4 (en) 2020-01-13 2024-08-14 Aptabio Therapeutics Inc. NOVEL PYRAZOLE DERIVATIVE
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN113416140B (zh) * 2021-06-03 2023-01-13 万华化学集团股份有限公司 一种制备2-甲基戊二胺的方法
US20250145628A1 (en) * 2022-02-15 2025-05-08 Novo Nordisk A/S Pyrazolopyrimidines, compositions comprising them and uses thereof

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WO2009108838A1 (en) 2008-02-29 2009-09-03 Wyeth Bridged, bicyclic heterocyclic or spiro bicyclic heterocyclic derivatives of pyrazolo[1,5-a]pyrimidines, methods for preparation and uses thereof
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition

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GB9204464D0 (en) * 1992-03-02 1992-04-15 Fujisawa Pharmaceutical Co New heterocyclic derivatives
US5356897A (en) * 1991-09-09 1994-10-18 Fujisawa Pharmaceutical Co., Ltd. 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines
AU2003227437A1 (en) 2002-04-23 2003-11-10 Shionogi And Co., Ltd. PYRAZOLO(1,5-a)PYRIMIDINE DERIVATIVE AND NAD(P)H OXIDASE INHIBITOR CONTAINING THE SAME
JP4494205B2 (ja) 2002-08-26 2010-06-30 武田薬品工業株式会社 カルシウム受容体調節化合物およびその用途
MXPA05006568A (es) 2002-12-20 2005-09-22 Pharmacia Corp Compuestos de pirazol aciclico para la inhibicion de proteina cinasa-2 activada por proteina cinasa activada por mitogenos.
BRPI0822239A2 (pt) 2007-12-21 2015-06-30 Wyeth Llc Composto de pirazolo[1,5-a] pirimidina
ES2548135T3 (es) 2008-05-13 2015-10-14 Novartis Ag Heterociclos condensados que contienen nitrógeno y composiciones de los mismos como inhibidores de quinasa
JP2012528175A (ja) * 2009-05-27 2012-11-12 アボット・ラボラトリーズ キナーゼ活性のピリミジン阻害剤
JO3407B1 (ar) * 2012-05-31 2019-10-20 Eisai R&D Man Co Ltd مركبات رباعي هيدرو بيرازولو بيريميدين
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JP2006502165A (ja) 2002-09-06 2006-01-19 バイオジェン・アイデック・エムエイ・インコーポレイテッド ピラゾロピリジンならびにその作製および使用方法
WO2009108838A1 (en) 2008-02-29 2009-09-03 Wyeth Bridged, bicyclic heterocyclic or spiro bicyclic heterocyclic derivatives of pyrazolo[1,5-a]pyrimidines, methods for preparation and uses thereof
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WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition

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ES2686747T3 (es) 2018-10-19
EA031639B1 (ru) 2019-01-31
AU2015238298A1 (en) 2016-09-15
AU2015238298B2 (en) 2019-04-18
BR112016021507A2 (cg-RX-API-DMAC7.html) 2017-08-15
KR20160137566A (ko) 2016-11-30
IL247948B (en) 2019-03-31
BR112016021507B1 (pt) 2022-10-18
WO2015144801A1 (en) 2015-10-01
EP3126366B1 (en) 2018-06-06
EA201691934A1 (ru) 2017-01-30
MX2016012669A (es) 2016-12-14
JP2017508777A (ja) 2017-03-30
CA2941206C (en) 2022-09-20
MX367913B (es) 2019-09-11
US10342795B2 (en) 2019-07-09
CA2941206A1 (en) 2015-10-01
EP3126366A1 (en) 2017-02-08
CN106132967A (zh) 2016-11-16
CN106132967B (zh) 2019-05-28
US20170173014A1 (en) 2017-06-22
JP6527167B2 (ja) 2019-06-05

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