JP2020506922A - セレブロンリガンド、およびセレブロンリガンドを含有する二官能性化合物 - Google Patents

セレブロンリガンド、およびセレブロンリガンドを含有する二官能性化合物 Download PDF

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JP2020506922A
JP2020506922A JP2019541254A JP2019541254A JP2020506922A JP 2020506922 A JP2020506922 A JP 2020506922A JP 2019541254 A JP2019541254 A JP 2019541254A JP 2019541254 A JP2019541254 A JP 2019541254A JP 2020506922 A JP2020506922 A JP 2020506922A
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JP2020506922A5 (enExample
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クルー，アンドリュー・ピィ
バーリン，マイケル
ドン，ハンチン
ホーンバーガー，キース・アール
チエン，イミン
スナイダー，ローレンス・ビィ
ワン，ジン
ジマーマン，カート
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Arvinas Operations Inc
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Arvinas Operations Inc
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Publication of JP2020506922A publication Critical patent/JP2020506922A/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • 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
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • 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
    • C07D471/10—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
    • C07D487/02—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
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

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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)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyridine Compounds (AREA)
JP2019541254A 2017-01-31 2018-01-31 セレブロンリガンド、およびセレブロンリガンドを含有する二官能性化合物 Pending JP2020506922A (ja)

Priority Applications (1)

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JP2023192138A JP2024023277A (ja) 2017-01-31 2023-11-10 セレブロンリガンド、およびセレブロンリガンドを含有する二官能性化合物

Applications Claiming Priority (3)

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US201762452972P 2017-01-31 2017-01-31
US62/452,972 2017-01-31
PCT/US2018/016315 WO2018144649A1 (en) 2017-01-31 2018-01-31 Cereblon ligands and bifunctional compounds comprising the same

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JP2020506922A true JP2020506922A (ja) 2020-03-05
JP2020506922A5 JP2020506922A5 (enExample) 2021-03-11

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JP2023192138A Pending JP2024023277A (ja) 2017-01-31 2023-11-10 セレブロンリガンド、およびセレブロンリガンドを含有する二官能性化合物

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US (3) US20180215731A1 (enExample)
EP (1) EP3577109A4 (enExample)
JP (2) JP2020506922A (enExample)
KR (1) KR102747905B1 (enExample)
CN (2) CN110612294B (enExample)
AU (3) AU2018215212B2 (enExample)
BR (1) BR112019015484A2 (enExample)
CA (1) CA3050309A1 (enExample)
CO (1) CO2019009424A2 (enExample)
IL (3) IL319363A (enExample)
MX (2) MX2019009046A (enExample)
WO (1) WO2018144649A1 (enExample)

Cited By (11)

* Cited by examiner, † Cited by third party
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JP2020519582A (ja) * 2017-05-12 2020-07-02 コリア リサーチ インスティチュート オブ ケミカル テクノロジーＫｏｒｅａ Ｒｅｓｅａｒｃｈ Ｉｎｓｔｉｔｕｔｅ Ｏｆ Ｃｈｅｍｉｃａｌ Ｔｅｃｈｎｏｌｏｇｙ 新規なピペリジン−２，６−ジオン誘導体及びその用途
WO2021210878A1 (ko) * 2020-04-17 2021-10-21 광주과학기술원 Crbn 결합 펩티드 및 이를 이용한 알츠하이머 병 예방 또는 치료용 조성물
JP2023507570A (ja) * 2019-12-19 2023-02-24 アルビナス・オペレーションズ・インコーポレイテッド アンドロゲン受容体の標的分解のための化合物および方法
JP2023517393A (ja) * 2020-03-17 2023-04-25 メッドシャイン ディスカバリー インコーポレイテッド タンパク質分解調整剤およびその使用方法
JP2023518202A (ja) * 2020-03-18 2023-04-28 ダナ－ファーバー キャンサー インスティテュート，インコーポレイテッド Ｐｅｔトレーサーｐｂｂ３に基づく異常タウの標的化ディグレーダー
JP2023531390A (ja) * 2020-06-12 2023-07-24 シャンハイ ジェミンケア ファーマシューティカルズ カンパニー、リミテッド フタラジノン化合物、並びにその調製方法及びその医薬用途
JP2023535054A (ja) * 2020-07-21 2023-08-15 ユービックス セラピューティクス インコーポレイテッド アンドロゲン受容体分解用化合物及びその医薬用途
JP2023541522A (ja) * 2020-08-03 2023-10-03 キャプター セラピューティクス エス．エー． 低分子量タンパク質分解物質及びその適用
JP2023543299A (ja) * 2020-09-30 2023-10-13 アストラゼネカ・アクチエボラーグ 化合物及び癌の治療におけるそれらの使用
JP2024519628A (ja) * 2021-05-26 2024-05-21 イノキュア セラピューティクス インコーポレイテッド ピペリジンジオン誘導体
JP2024539269A (ja) * 2021-10-22 2024-10-28 グルータクス セラピューティクス （シャンハイ） カンパニー、リミテッド Ｃｒｂｎ ｅ３リガーゼリガンド化合物、当該リガンド化合物に基づいて開発したタンパク質分解剤及びそれらの応用

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US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
US20180147202A1 (en) 2015-06-05 2018-05-31 Arvinas, Inc. TANK-BINDING KINASE-1 PROTACs AND ASSOCIATED METHODS OF USE
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EP3535265A4 (en) 2016-11-01 2020-07-08 Arvinas, Inc. PROTACS TARGETING ON TAU PROTEIN AND RELATED METHODS FOR USE
RS64976B1 (sr) 2016-12-01 2024-01-31 Arvinas Operations Inc Derivati tetrahidronaftalena i tetrahidroizohinolina kao degradatori estrogenih receptora
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
RU2019121527A (ru) 2016-12-23 2021-01-15 Эрвинэс Оперейшнс, Инк. Химерные молекулы, нацеливающиеся на протеолиз egfr, и связанные с ними способы применения
WO2018118598A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
JP7679173B2 (ja) 2016-12-23 2025-05-19 アルビナス・オペレーションズ・インコーポレイテッド Ｒａｆ（急速進行性線維肉腫）ポリペプチドの標的分解のための化合物および方法
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WO2019099926A1 (en) 2017-11-17 2019-05-23 Arvinas, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides
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JP7252973B2 (ja) 2018-03-26 2023-04-05 ノバルティス アーゲー Ｎ－（３－（７Ｈ－ピロロ［２，３－ｄ］ピリミジン－４－イル）フェニル）ベンズアミド誘導体
FI3774789T3 (fi) 2018-04-01 2025-06-17 Arvinas Operations Inc Brm:ään kohdentuvia yhdisteitä ja niihin liittyviä käyttömenetelmiä
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