JP6522646B2 - ＲＯＳ１阻害剤としての置換４，５，６，７−テトラヒドロ−ピラゾロ［１，５−α］ピラジン誘導体および５，６，７，８−テトラヒドロ−４Ｈ−ピラゾロ［１，５−α］［１，４］ジアゼピン誘導体 - Google Patents

ＲＯＳ１阻害剤としての置換４，５，６，７−テトラヒドロ−ピラゾロ［１，５−α］ピラジン誘導体および５，６，７，８−テトラヒドロ−４Ｈ−ピラゾロ［１，５−α］［１，４］ジアゼピン誘導体 Download PDF

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JP6522646B2
JP6522646B2 JP2016559326A JP2016559326A JP6522646B2 JP 6522646 B2 JP6522646 B2 JP 6522646B2 JP 2016559326 A JP2016559326 A JP 2016559326A JP 2016559326 A JP2016559326 A JP 2016559326A JP 6522646 B2 JP6522646 B2 JP 6522646B2
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alkyl
substituted
alkyloxy
hydrogen
cyano
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JP2017508779A5 (enExample
JP2017508779A (ja
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メヴェレク，ローレンス，アン
パスクエ，エリザベス，テレーゼ，ジャンヌ
デキャン，ソフィー
マーシー，ギヨーム，ジーン，モーリス
ヴロブロウスキ，ベルトールド
ヴィアラード，ジョルジ，エドゥアルド
メーアポエル，リーヴェン
ジーンティ，マチウ，ルドヴィク
ジョーシオウメ，ティエリー，フランソワ，アラン，ジーン
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ヤンセン ファーマシューティカ エヌ．ベー．
ヤンセン ファーマシューティカ エヌ．ベー．
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    • 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
    • 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
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • 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
    • C07D487/10—Spiro-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
    • C07D487/12—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 three hetero rings
    • C07D487/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2016559326A 2014-03-27 2015-03-26 ＲＯＳ１阻害剤としての置換４，５，６，７−テトラヒドロ−ピラゾロ［１，５−α］ピラジン誘導体および５，６，７，８−テトラヒドロ−４Ｈ−ピラゾロ［１，５−α］［１，４］ジアゼピン誘導体 Active JP6522646B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14161950.2 2014-03-27
EP14161950 2014-03-27
PCT/EP2015/056498 WO2015144799A1 (en) 2014-03-27 2015-03-26 SUBSTITUTED 4,5,6,7-TETRAHYDRO-PYRAZOLO[1,5-a]PYRAZINE DERIVATIVES AND 5,6,7,8-TETRAHYDRO-4H-PYRAZOLO[1,5-a][1,4]DIAZEPINE DERIVATIVES AS ROS1 INHIBITORS

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JP2017508779A JP2017508779A (ja) 2017-03-30
JP2017508779A5 JP2017508779A5 (enExample) 2019-02-28
JP6522646B2 true JP6522646B2 (ja) 2019-05-29

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EP (1) EP3129376B1 (enExample)
JP (1) JP6522646B2 (enExample)
KR (1) KR102455519B1 (enExample)
CN (1) CN106164076B (enExample)
AU (1) AU2015238296B2 (enExample)
BR (1) BR112016022105B1 (enExample)
CA (1) CA2940918C (enExample)
EA (1) EA032255B1 (enExample)
ES (1) ES2715676T3 (enExample)
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JP6116782B1 (ja) 2015-08-28 2017-04-19 積水メディカル株式会社 ベンジル化合物
TWI782056B (zh) 2017-07-14 2022-11-01 日商鹽野義製藥股份有限公司 具有ｍｇａｔ２抑制活性的縮合環衍生物
WO2019233456A1 (zh) * 2018-06-08 2019-12-12 贝达药业股份有限公司 Erk抑制剂及其应用
MX2021008050A (es) * 2019-01-11 2021-08-05 Shionogi & Co Derivado de dihidropirazolopirazinona que tiene actividad inhibidora de monoacilglicerol aciltransferasa 2 (mgat2).
JP7068743B2 (ja) * 2019-01-11 2022-05-17 塩野義製薬株式会社 Ｍｇａｔ２阻害活性を有する縮合環誘導体を含有する医薬組成物
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
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN114315866B (zh) * 2020-09-30 2023-10-31 烟台药物研究所 一种盐酸左旋咪唑的合成方法
TW202229282A (zh) * 2020-09-30 2022-08-01 美商史考皮恩治療有限公司 治療癌症之方法
US20250276972A1 (en) * 2020-12-15 2025-09-04 Gritscience Biopharmaceuticals Co.,Ltd. Compounds as casein kinase inhibitors
CN114957259A (zh) * 2021-02-25 2022-08-30 南京明德新药研发有限公司 氰基取代的芳香双环类化合物及其应用

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US5356897A (en) 1991-09-09 1994-10-18 Fujisawa Pharmaceutical Co., Ltd. 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines
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
JP2005343889A (ja) 2004-05-06 2005-12-15 Taisho Pharmaceut Co Ltd イミダゾピリジン誘導体
WO2009076440A2 (en) 2007-12-12 2009-06-18 E.I. Du Pont De Nemours And Company Fungicidal bicyclic pyrazoles
EP2235020A1 (en) 2007-12-21 2010-10-06 Wyeth LLC Pyrazolo [1,5-a] pyrimidine compounds
US20100029657A1 (en) 2008-02-29 2010-02-04 Wyeth Bridged, Bicyclic Heterocyclic or Spiro Bicyclic Heterocyclic Derivatives of Pyrazolo[1, 5-A]Pyrimidines, Methods for Preparation and Uses Thereof
JP5214799B2 (ja) * 2008-04-07 2013-06-19 アイアールエム・リミテッド・ライアビリティ・カンパニー キナーゼ阻害剤としての化合物および組成物
AU2009233964B2 (en) 2008-04-07 2012-06-07 Irm Llc Compounds and compositions as protein kinase inhibitors
CA2722418C (en) * 2008-05-13 2013-09-17 Irm Llc Fused nitrogen containing heterocycles and compositions thereof as kinase inhibitors
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Publication number Publication date
WO2015144799A1 (en) 2015-10-01
MX367914B (es) 2019-09-11
BR112016022105B1 (pt) 2023-01-31
IL247947B (en) 2019-03-31
CN106164076B (zh) 2019-03-26
EP3129376A1 (en) 2017-02-15
EA032255B1 (ru) 2019-04-30
KR20160137576A (ko) 2016-11-30
MX2016012668A (es) 2016-12-14
EA201691930A1 (ru) 2017-02-28
EP3129376B1 (en) 2018-12-26
KR102455519B1 (ko) 2022-10-14
AU2015238296B2 (en) 2018-10-18
JP2017508779A (ja) 2017-03-30
AU2015238296A1 (en) 2016-09-08
US10280170B2 (en) 2019-05-07
ES2715676T3 (es) 2019-06-05
CN106164076A (zh) 2016-11-23
CA2940918A1 (en) 2015-10-01
BR112016022105A2 (enExample) 2017-08-15
US20170174690A1 (en) 2017-06-22
CA2940918C (en) 2023-10-24

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