JP6999688B2 - Ｂｃｌ６阻害剤としての新規の６－アミノキノリノン化合物および誘導体 - Google Patents

Ｂｃｌ６阻害剤としての新規の６－アミノキノリノン化合物および誘導体 Download PDF

Info

Publication number
JP6999688B2
JP6999688B2 JP2019551728A JP2019551728A JP6999688B2 JP 6999688 B2 JP6999688 B2 JP 6999688B2 JP 2019551728 A JP2019551728 A JP 2019551728A JP 2019551728 A JP2019551728 A JP 2019551728A JP 6999688 B2 JP6999688 B2 JP 6999688B2
Authority
JP
Japan
Prior art keywords
alkyl
group
substituted
heterocyclyl
hydrogen
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
JP2019551728A
Other languages
English (en)
Japanese (ja)
Other versions
JP2020503374A5 (enExample
JP2020503374A (ja
Inventor
シュテファン シュトイラー
ゲオルク ダーマン
ニーナ ケレス
マンフレッド ケーグル
Original Assignee
ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング filed Critical ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
Publication of JP2020503374A publication Critical patent/JP2020503374A/ja
Publication of JP2020503374A5 publication Critical patent/JP2020503374A5/ja
Application granted granted Critical
Publication of JP6999688B2 publication Critical patent/JP6999688B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • A61K47/02—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • 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
    • C07D498/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Inorganic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biophysics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2019551728A 2016-12-13 2017-12-07 Ｂｃｌ６阻害剤としての新規の６－アミノキノリノン化合物および誘導体 Active JP6999688B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP16203746.9 2016-12-13
EP16203746 2016-12-13
PCT/EP2017/081899 WO2018108704A1 (en) 2016-12-13 2017-12-07 New 6-amino-quinolinone compounds and derivatives as bcl6 inhibitors

Publications (3)

Publication Number Publication Date
JP2020503374A JP2020503374A (ja) 2020-01-30
JP2020503374A5 JP2020503374A5 (enExample) 2021-01-21
JP6999688B2 true JP6999688B2 (ja) 2022-02-10

Family

ID=57544344

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2019551728A Active JP6999688B2 (ja) 2016-12-13 2017-12-07 Ｂｃｌ６阻害剤としての新規の６－アミノキノリノン化合物および誘導体

Country Status (4)

Country Link
US (1) US11001570B2 (enExample)
EP (1) EP3555063B1 (enExample)
JP (1) JP6999688B2 (enExample)
WO (1) WO2018108704A1 (enExample)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2975661T3 (es) * 2017-05-26 2024-07-11 Cancer Research Tech Ltd Inhibidores de BCL6 derivados de la 2-quinolona
CN111163839B (zh) 2017-05-26 2024-05-28 癌症研究科技有限公司 苯并咪唑酮衍生的bcl6抑制剂
CA3086368A1 (en) * 2017-12-22 2019-06-27 Ontario Institute For Cancer Research (Oicr) Novel deuterated compounds as inhibitors of the bcl6 btb domain protein-protein interaction and/or as bcl6 degraders
CA3086362A1 (en) 2017-12-22 2019-06-27 Ontario Institute For Cancer Research (Oicr) Quinolone compounds as inhibitors of the bcl6 btb domain protein-p rotein interaction and/or as bcl6 degraders
JP7493454B2 (ja) 2018-04-13 2024-05-31 キャンサー・リサーチ・テクノロジー・リミテッド Ｂｃｌ６阻害剤
EP3820500A4 (en) * 2018-07-13 2022-04-13 Teqla Therapeutics, Inc. USE OF BCL6 INHIBITORS FOR THE TREATMENT OF AUTOIMMUNE DISEASES
GB201819126D0 (en) * 2018-11-23 2019-01-09 Cancer Research Tech Ltd Inhibitor compounds
GB201909573D0 (en) 2019-07-03 2019-08-14 Cancer Research Tech Ltd Modulation of T cell cytotoxicity and related therapy
GB201914860D0 (en) * 2019-10-14 2019-11-27 Cancer Research Tech Ltd Inhibitor compounds
AU2020368542B2 (en) * 2019-10-17 2024-02-29 Arvinas Operations, Inc. Bifunctional molecules containing an E3 ubiquitine ligase binding moiety linked to a BCL6 targeting moiety
EP4323352A1 (en) 2021-04-16 2024-02-21 Arvinas Operations, Inc. Modulators of bcl6 proteolysis and associated methods of use
US20250074890A1 (en) * 2021-08-02 2025-03-06 Dana-Farber Cancer Institute, Inc. Cyanopyridine and cyanopyrimidine bcl6 degraders
EP4448487A4 (en) * 2021-12-17 2025-12-03 Dana Farber Cancer Inst Inc BCL6 DEGRADING AGENTS AND THEIR USES
KR20250020448A (ko) * 2022-06-02 2025-02-11 시젱 하이스코 파마수티칼 씨오., 엘티디. Bcl6을 억제하거나 분해하는 화합물 및 의약학에서의 응용
CN119317623A (zh) 2022-06-06 2025-01-14 树线生物科学公司 三环喹诺酮bcl6双功能降解剂
KR20250023483A (ko) 2022-06-13 2025-02-18 트리라인 바이오사이언시스, 인크. 퀴놀론 bcl6 이작용성 분해제
AU2023295387A1 (en) 2022-06-13 2025-01-09 Treeline Biosciences, Inc. 1,8-naphthyridin-2-one heterobifunctional bcl6 degraders
EP4558487A1 (en) * 2022-07-19 2025-05-28 Dana-Farber Cancer Institute, Inc. Quinoxalinedione and pyrido [2, 3-b]pyrazine-2, 3-dione b cell lymphoma 6 (bcl6) degraders and uses thereof
EP4568946A1 (en) * 2022-08-09 2025-06-18 Dana-Farber Cancer Institute, Inc. Macrocyclic bcl6 degraders
CN120813582A (zh) * 2023-03-17 2025-10-17 西藏海思科制药有限公司 一种含氮三并环衍生物及其在医药上的应用
CN117003735A (zh) * 2023-08-08 2023-11-07 西南交通大学 一种靶向bcl6蛋白降解的二价配体分子及其应用
WO2025049968A1 (en) * 2023-09-01 2025-03-06 Treeline Biosciences, Inc. Tricyclic quinolone and 1,8-naphthyridin-2-one bcl6 bifunctional degraders
WO2025049964A1 (en) * 2023-09-01 2025-03-06 Treeline Biosciences, Inc. Bcl6 bifunctional degraders
CN120987969A (zh) * 2024-05-21 2025-11-21 中国药科大学 一类蛋白靶向降解嵌合体及其用途

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007136592A2 (en) 2006-05-18 2007-11-29 Amphora Discovery Corporation 2-0x0-l,2-dihydr0quin0line derivatives, compositions, and uses thereof as antiproliferative agents
WO2008066887A2 (en) 2006-11-30 2008-06-05 Albert Einstein College Of Medicine Of Yeshiva University Small molecule inhibitors of bcl6
JP2008543778A (ja) 2005-06-08 2008-12-04 ライジェル ファーマシューティカルズ， インコーポレイテッド Ｊａｋ経路の阻害のための組成物および方法
JP2009519249A (ja) 2005-12-09 2009-05-14 アムジエン・インコーポレーテツド プロリルヒドロキシラーゼ阻害活性を示すキノロンベースの化合物、およびこの組成物、およびこの使用
JP2011518157A (ja) 2008-04-16 2011-06-23 ポートラ ファーマシューティカルズ， インコーポレイテッド Ｓｙｋ又はｊａｋキナーゼ阻害剤としての２，６−ジアミノ−ピリミジン−５−イル−カルボキサミド類
CN105037265A (zh) 2015-05-20 2015-11-11 南京大学 一类含查尔酮骨架的喹啉酮衍生物的制备方法及在抗癌药物中的应用

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3086362A1 (en) * 2017-12-22 2019-06-27 Ontario Institute For Cancer Research (Oicr) Quinolone compounds as inhibitors of the bcl6 btb domain protein-p rotein interaction and/or as bcl6 degraders
CA3086368A1 (en) * 2017-12-22 2019-06-27 Ontario Institute For Cancer Research (Oicr) Novel deuterated compounds as inhibitors of the bcl6 btb domain protein-protein interaction and/or as bcl6 degraders

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008543778A (ja) 2005-06-08 2008-12-04 ライジェル ファーマシューティカルズ， インコーポレイテッド Ｊａｋ経路の阻害のための組成物および方法
JP2009519249A (ja) 2005-12-09 2009-05-14 アムジエン・インコーポレーテツド プロリルヒドロキシラーゼ阻害活性を示すキノロンベースの化合物、およびこの組成物、およびこの使用
WO2007136592A2 (en) 2006-05-18 2007-11-29 Amphora Discovery Corporation 2-0x0-l,2-dihydr0quin0line derivatives, compositions, and uses thereof as antiproliferative agents
WO2008066887A2 (en) 2006-11-30 2008-06-05 Albert Einstein College Of Medicine Of Yeshiva University Small molecule inhibitors of bcl6
JP2011518157A (ja) 2008-04-16 2011-06-23 ポートラ ファーマシューティカルズ， インコーポレイテッド Ｓｙｋ又はｊａｋキナーゼ阻害剤としての２，６−ジアミノ−ピリミジン−５−イル−カルボキサミド類
CN105037265A (zh) 2015-05-20 2015-11-11 南京大学 一类含查尔酮骨架的喹啉酮衍生物的制备方法及在抗癌药物中的应用

Also Published As

Publication number Publication date
EP3555063A1 (en) 2019-10-23
US11001570B2 (en) 2021-05-11
US20200071297A1 (en) 2020-03-05
JP2020503374A (ja) 2020-01-30
EP3555063B1 (en) 2020-09-16
WO2018108704A1 (en) 2018-06-21

Similar Documents

Publication Publication Date Title
JP6999688B2 (ja) Ｂｃｌ６阻害剤としての新規の６－アミノキノリノン化合物および誘導体
US11814380B2 (en) Benzylamino substituted pyridopyrimidinones and derivatives as SOS1 inhibitors
JP6591532B2 (ja) ＭＤＭ２−ｐ５３阻害剤としての新しいスピロ［３Ｈ−インドール−３，２’−ピロリジン］−２（１Ｈ）−オン化合物および誘導体
JP6602470B2 (ja) Ｍｄｍ２−ｐ５３阻害薬としてのスピロ［３ｈ−インドール−３，２‘−ピロリジン］−２（１ｈ）−オン化合物及び誘導体
RU2629194C2 (ru) Производные 1,5- и 1,7-нафтиридина, полезные при лечении заболеваний, опосредованных fgfr
RU2701517C2 (ru) Производные хиназолинона, применимые в качестве модуляторов fgfr киназы
RU2702906C2 (ru) Птеридины в качестве fgfr ингибиторов
JP2023528623A (ja) がんを治療するための縮合環化２－アミノ－３－シアノチオフェン及び誘導体
JP5868992B2 (ja) 癌疾患の治療のためのｆｇｆｒキナーゼ阻害剤としての置換ベンゾピラジン誘導体
JP6577958B2 (ja) スピロ［３Ｈ−インドール−３，２’−ピロリジン］−２（１Ｈ）−オン誘導体およびＭＤＭ２−ｐ５３阻害剤としてのそれらの使用
JP5871896B2 (ja) Ｂ−ｒａｆキナーゼインヒビター
JP6503386B2 (ja) ＭＤＭ２−ｐ５３阻害剤としての新しいスピロ［３Ｈ−インドール−３，２’−ピロリジン］−２（１Ｈ）−オン化合物および誘導体
JP6128133B2 (ja) Ｉｇｆ−１ｒ／ｉｒ阻害剤としての５，８−ジヒドロ−６ｈ−ピラゾロ［３，４−ｈ］キナゾリン
JP5824068B2 (ja) セリン／トレオニンキナーゼ阻害剤としての新規トリアゾリルフェニルスルホンアミド
JP2020504742A (ja) 新規のベンジルアミノ置換キナゾリンおよびｓｏｓ１阻害剤としての誘導体
JP2021514373A (ja) Ｅｇｆｒ阻害剤としての新たなベンズイミダゾール化合物および誘導体
HK40097417A (en) Benzylamino substituted pyridopyrimidinones and derivatives as sos1 inhibitors

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20201207

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20201207

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20211122

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20211125

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20211222

R150 Certificate of patent or registration of utility model

Ref document number: 6999688

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250