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
substituted
hydrogen
alkyloxy
formula
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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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    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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
    • A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-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 Expired - Fee Related KR102455518B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14161959.3 2014-03-27
EP14161959 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

Publications (2)

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

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KR1020167027337A Expired - Fee Related KR102455518B1 (ko) 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

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US (1) US10342795B2 (enExample)
EP (1) EP3126366B1 (enExample)
JP (1) JP6527167B2 (enExample)
KR (1) KR102455518B1 (enExample)
CN (1) CN106132967B (enExample)
AU (1) AU2015238298B2 (enExample)
BR (1) BR112016021507B1 (enExample)
CA (1) CA2941206C (enExample)
EA (1) EA031639B1 (enExample)
ES (1) ES2686747T3 (enExample)
IL (1) IL247948B (enExample)
MX (1) MX367913B (enExample)
WO (1) WO2015144801A1 (enExample)

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CN107737125A (zh) * 2016-11-26 2018-02-27 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
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
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
WO2021145655A1 (ko) 2020-01-13 2021-07-22 압타바이오 주식회사 신규한 피라졸 유도체
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

Citations (3)

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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
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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US5356897A (en) * 1991-09-09 1994-10-18 Fujisawa Pharmaceutical Co., Ltd. 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines
GB9204464D0 (en) * 1992-03-02 1992-04-15 Fujisawa Pharmaceutical Co New heterocyclic derivatives
CA2483306A1 (en) 2002-04-23 2003-11-06 Shionogi & Co., Ltd. Pyrazolo[1,5-a]pyrimidine derivative and nad(p)h oxidase inhibitor containing the same
PL382706A1 (pl) 2002-08-26 2007-11-26 Takeda Pharmaceutical Company Limited Związek modulujący receptor wapnia i jego zastosowanie
BR0317430A (pt) 2002-12-20 2005-10-25 Pharmacia Corp Compostos inibidores de quinase-2 de proteìna ativada por quinase de proteìna ativada por mitógeno
EP2235020A1 (en) 2007-12-21 2010-10-06 Wyeth LLC Pyrazolo [1,5-a] pyrimidine compounds
CA2722418C (en) 2008-05-13 2013-09-17 Irm Llc Fused nitrogen containing heterocycles and compositions thereof as kinase inhibitors
CN102459264A (zh) * 2009-05-27 2012-05-16 雅培制药有限公司 激酶活性的嘧啶抑制剂
JO3407B1 (ar) * 2012-05-31 2019-10-20 Eisai R&D Man Co Ltd مركبات رباعي هيدرو بيرازولو بيريميدين
TWI585088B (zh) * 2012-06-04 2017-06-01 第一三共股份有限公司 作爲激酶抑制劑之咪唑并［１，２－ｂ］嗒衍生物

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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
JP2011513334A (ja) 2008-02-29 2011-04-28 ワイス・エルエルシー ピラゾロ［１，５−ａ］ピリミジンの架橋二環式複素環式またはスピロ二環式複素環式誘導体、その調製方法および使用
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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MX2016012669A (es) 2016-12-14
US10342795B2 (en) 2019-07-09
AU2015238298B2 (en) 2019-04-18
CA2941206C (en) 2022-09-20
JP2017508777A (ja) 2017-03-30
EP3126366B1 (en) 2018-06-06
EA031639B1 (ru) 2019-01-31
IL247948B (en) 2019-03-31
CA2941206A1 (en) 2015-10-01
JP6527167B2 (ja) 2019-06-05
US20170173014A1 (en) 2017-06-22
AU2015238298A1 (en) 2016-09-15
MX367913B (es) 2019-09-11
BR112016021507A2 (enExample) 2017-08-15
KR20160137566A (ko) 2016-11-30
WO2015144801A1 (en) 2015-10-01
CN106132967B (zh) 2019-05-28
EA201691934A1 (ru) 2017-01-30
CN106132967A (zh) 2016-11-16
EP3126366A1 (en) 2017-02-08
ES2686747T3 (es) 2018-10-19
BR112016021507B1 (pt) 2022-10-18

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