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WO2009054332A1 - ピリドン置換ジヒドロピラゾロピリミジノン誘導体 - Google Patents

ピリドン置換ジヒドロピラゾロピリミジノン誘導体 Download PDF

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Publication number
WO2009054332A1
WO2009054332A1 PCT/JP2008/068932 JP2008068932W WO2009054332A1 WO 2009054332 A1 WO2009054332 A1 WO 2009054332A1 JP 2008068932 W JP2008068932 W JP 2008068932W WO 2009054332 A1 WO2009054332 A1 WO 2009054332A1
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group
alkyl group
halo
atom
hydrogen atom
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Ceased
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PCT/JP2008/068932
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English (en)
French (fr)
Inventor
Hidetomo Fruyama
Mikako Kawamura
Toshihiro Sakamoto
Fuyuki Yamamoto
Takashi Yoshizumi
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MSD KK
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Banyu Phamaceutical Co Ltd
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Application filed by Banyu Phamaceutical Co Ltd filed Critical Banyu Phamaceutical Co Ltd
Priority to JP2009538185A priority Critical patent/JPWO2009054332A1/ja
Priority to US12/738,885 priority patent/US8329711B2/en
Priority to CA2703489A priority patent/CA2703489A1/en
Priority to EP08842196.1A priority patent/EP2213673B1/en
Priority to AU2008315048A priority patent/AU2008315048A1/en
Publication of WO2009054332A1 publication Critical patent/WO2009054332A1/ja
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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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
    • A61K31/519—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
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

【構成】一般式（Ｉ－０） 【化１】 ［式中、Ｒ１はＣ１－Ｃ６アルキル基、Ｃ２－Ｃ６アルケニル基、Ｃ２－Ｃ６アルキニル基又はＣ３－Ｃ６シクロアルキル基を；Ｒ２、Ｒ３、Ｒ４及びＲ５は水素原子、ハロゲン原子、Ｃ１－Ｃ６アルキル基、ハロ－Ｃ１－Ｃ６アルキル基、Ｃ１－Ｃ６アルコキシ基又はハロ－Ｃ１－Ｃ６アルコキシ基を；Ｒ６は水素原子又はＣ１－Ｃ６アルキル基を；Ｒ７ａは水素原子、ハロゲン原子、Ｃ１－Ｃ６アルキル基、ハロ－Ｃ１－Ｃ６アルキル基、Ｃ１－Ｃ６アルコキシ基、ヒドロキシ－Ｃ１－Ｃ６アルキル基、－Ｑ２－Ｎ（Ｒ１ｃ）Ｒ１ｄ又は含窒素複素環基を；Ｒ８ａは水素原子、ハロゲン原子、Ｃ１－Ｃ６アルキル基、ハロ－Ｃ１－Ｃ６アルキル基、Ｃ１－Ｃ６アルコキシ基又はヒドロキシ－Ｃ１－Ｃ６アルキル基を意味し；あるいは、Ｒ７ａ及びＲ８ａは一緒になってＣ２－Ｃ６アルキレン基又はＲ７ａ及びＲ８ａ並びにそれらが結合する環原子は一緒になってスピロ環若しくはビシクロ環であってもよく；そして、Ｘ及びＹはメチン基又は窒素原子を意味する］で表される化合物等に関する。 【効果】 　本発明の化合物は、優れたＷｅｅ１キナーゼ阻害作用に基づく細胞増殖阻害作用及び他の抗がん剤との相加・相乗作用を有することから医薬の分野において有用である。
PCT/JP2008/068932 2007-10-23 2008-10-20 ピリドン置換ジヒドロピラゾロピリミジノン誘導体 Ceased WO2009054332A1 (ja)

Priority Applications (5)

Application Number Priority Date Filing Date Title
JP2009538185A JPWO2009054332A1 (ja) 2007-10-23 2008-10-20 ピリドン置換ジヒドロピラゾロピリミジノン誘導体
US12/738,885 US8329711B2 (en) 2007-10-23 2008-10-20 Pyridone-substituted-dihydropyrazolopyrimidinone derivative
CA2703489A CA2703489A1 (en) 2007-10-23 2008-10-20 Pyridone-substituted-dihydropyrazolopyrimidinone derivative
EP08842196.1A EP2213673B1 (en) 2007-10-23 2008-10-20 Pyridone-substituted-dihydropyrazolopyrimidinone derivative
AU2008315048A AU2008315048A1 (en) 2007-10-23 2008-10-20 Pyridone-substituted-dihydropyrazolopyrimidinone derivative

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007-275311 2007-10-23
JP2007275311 2007-10-23

Publications (1)

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WO2009054332A1 true WO2009054332A1 (ja) 2009-04-30

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PCT/JP2008/068932 Ceased WO2009054332A1 (ja) 2007-10-23 2008-10-20 ピリドン置換ジヒドロピラゾロピリミジノン誘導体

Country Status (6)

Country Link
US (1) US8329711B2 (ja)
EP (1) EP2213673B1 (ja)
JP (1) JPWO2009054332A1 (ja)
AU (1) AU2008315048A1 (ja)
CA (1) CA2703489A1 (ja)
WO (1) WO2009054332A1 (ja)

Cited By (18)

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JP2014506929A (ja) * 2011-02-28 2014-03-20 アッヴィ・インコーポレイテッド 三環式キナーゼ阻害薬
JP2014521624A (ja) * 2011-07-27 2014-08-28 エービー サイエンス 選択的プロテインキナーゼ阻害剤
JP2015017105A (ja) * 2009-03-25 2015-01-29 アッヴィ・インコーポレイテッド 抗ウィルス性化合物およびこの使用
JP2017500335A (ja) * 2013-12-19 2017-01-05 アルマック・ディスカバリー・リミテッドＡｌｍａｃ Ｄｉｓｃｏｖｅｒｙ Ｌｉｍｉｔｅｄ Ｗｅｅ−１キナーゼ阻害剤として有用なピリミドピリミジノン
CN109810111A (zh) * 2017-11-20 2019-05-28 上海医药集团股份有限公司 一种吡唑酮并嘧啶类化合物、其制备方法及应用
WO2019165204A1 (en) 2018-02-23 2019-08-29 Newave Pharmaceutical Inc. 1,2-dihydro-3h-pyrazolo[3,4-d]pyrimidine-3-one compounds as inhibitors of wee-1 kinase
JP2020510630A (ja) * 2017-01-23 2020-04-09 シージャーズォアン サガシティ ニュー ドラッグ デベロップメント カンパニー リミテッド Ｗｅｅ１阻害剤としての１，２−ジヒドロ−３Ｈ−ピラゾロ［３，４−ｄ］ピリミジン−３−オン誘導体
JP2020511520A (ja) * 2017-03-23 2020-04-16 シャンハイ ドーァ ノボ ファーマテック カンパニー，リミティド ピラゾロ［３，４−ｄ］ピリミジン−３−オンの大環状誘導体、その医薬組成物及び応用
JP2020529993A (ja) * 2017-08-01 2020-10-15 リキュリウム アイピー ホールディングス リミテッド ライアビリティー カンパニー １，２−ジヒドロ−３Ｈ−ピラゾロ［３，４−ｄ］ピリミジン−３−オン類似体
US10807994B2 (en) 2017-10-09 2020-10-20 Nuvation Bio Inc. Heterocyclic compounds and uses thereof
KR20200130834A (ko) * 2018-03-09 2020-11-20 리커리엄 아이피 홀딩스, 엘엘씨 치환된 1,2-다이하이드로-3H-피라졸로[3,4-d]피리미딘-3-온
CN112142763A (zh) * 2019-06-28 2020-12-29 上海医药集团股份有限公司 一种吡唑酮并嘧啶类化合物、其制备方法及应用
WO2021254389A1 (zh) * 2020-06-17 2021-12-23 微境生物医药科技(上海)有限公司 作为Wee-1抑制剂的吡唑并[3，4-d]嘧啶-3-酮衍生物
US11299493B2 (en) 2017-10-09 2022-04-12 Nuvation Bio Inc. Heterocyclic compounds and uses thereof
US11332473B2 (en) 2019-04-09 2022-05-17 Nuvation Bio Inc. Substituted pyrazolo[3,4-d]pyrimidines as Wee1 inhibitors
CN114591334A (zh) * 2020-12-04 2022-06-07 山东轩竹医药科技有限公司 二氢吡唑并嘧啶酮衍生物
JP2022539460A (ja) * 2019-06-28 2022-09-09 シャンハイ ファーマシューティカルズ ホールディング カンパニー，リミティド ピラゾロン縮合ピリミジン化合物、その製造方法及び使用
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors

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WO2015019037A1 (en) * 2013-08-05 2015-02-12 Almac Discovery Limited Pharmaceutical compounds
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CN109422754A (zh) * 2017-08-24 2019-03-05 上海迪诺医药科技有限公司 吡唑并[3,4-d]嘧啶-3-酮衍生物、其药物组合物及应用
HRP20241020T1 (hr) * 2017-11-01 2024-11-08 Wuxi Biocity Biopharmaceutics Co., Ltd. Makrociklički spoj koji služi kao wee1 inhibitor i njegove primjene
WO2019134539A1 (zh) * 2018-01-05 2019-07-11 四川科伦博泰生物医药股份有限公司 二氢吡唑酮并嘧啶类化合物及其制备方法和用途
CN110872296B (zh) * 2018-08-31 2023-05-23 上海弘翊生物科技有限公司 一种二氢异吲哚-1H-吡唑并[3,4-d]嘧啶酮化合物、其制备方法和应用
US12180184B2 (en) 2018-10-26 2024-12-31 Wuxi Biocity Biopharmaceutics Co., Ltd. Pyrimidopyrazolone derivative as Wee1 inhibitor and use thereof
WO2020210381A1 (en) * 2019-04-09 2020-10-15 Nuvation Bio Inc. Heterocyclic compounds and uses thereof
WO2020210380A1 (en) * 2019-04-09 2020-10-15 Nuvation Bio Inc. Heterocyclic compounds and uses thereof
WO2020210320A1 (en) * 2019-04-11 2020-10-15 Recurium Ip Holdings, Llc Substituted l,2-dihydro-3h-pyrazolo[3,4-d]pyrimidin-3-ones
SI3964510T1 (sl) 2019-04-30 2024-10-30 Wuxi Biocity Biopharmaceutics Co., Ltd. Kristalna oblika WEE1 inhibitorske spojine in njena uporaba
TW202128699A (zh) * 2019-11-27 2021-08-01 美商建南德克公司 治療性化合物
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US8329711B2 (en) 2012-12-11
EP2213673A4 (en) 2011-09-07
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CA2703489A1 (en) 2009-04-30

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