JP7709378B2 - Heliosの低分子分解誘導剤および使用方法 - Google Patents

Heliosの低分子分解誘導剤および使用方法

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Publication number
JP7709378B2
JP7709378B2 JP2021531100A JP2021531100A JP7709378B2 JP 7709378 B2 JP7709378 B2 JP 7709378B2 JP 2021531100 A JP2021531100 A JP 2021531100A JP 2021531100 A JP2021531100 A JP 2021531100A JP 7709378 B2 JP7709378 B2 JP 7709378B2
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compound
cancer
optionally substituted
phenyl
amino
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JP2022510313A5 (enExample
JP2022510313A (ja
Inventor
ヴェラーノ,アリッサ
ワン,エリック
ノワク,ラドスロー
ティン クリスティーン ユアン,ジン
グレイ,ナサナエル
フィッシャー,エリック
ジャン,ティンフー
フー リウ,
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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
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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
    • A61K31/435—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
    • A61K31/44—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
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • 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
    • A61K31/495—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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • 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
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Hydrogenated Pyridines (AREA)
JP2021531100A 2018-12-03 2019-12-03 Heliosの低分子分解誘導剤および使用方法 Active JP7709378B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862774482P 2018-12-03 2018-12-03
US62/774,482 2018-12-03
US201962938410P 2019-11-21 2019-11-21
US62/938,410 2019-11-21
PCT/US2019/064169 WO2020117759A1 (en) 2018-12-03 2019-12-03 Small molecule degraders of helios and methods of use

Publications (3)

Publication Number Publication Date
JP2022510313A JP2022510313A (ja) 2022-01-26
JP2022510313A5 JP2022510313A5 (enExample) 2022-12-08
JP7709378B2 true JP7709378B2 (ja) 2025-07-16

Family

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US (2) US12227488B2 (enExample)
EP (1) EP3890736A4 (enExample)
JP (1) JP7709378B2 (enExample)
KR (1) KR102972506B1 (enExample)
CN (1) CN113490495B (enExample)
AU (1) AU2019391016B2 (enExample)
CA (1) CA3119526A1 (enExample)
WO (1) WO2020117759A1 (enExample)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PH12022551482A1 (en) 2019-12-18 2023-11-29 Novartis Ag 3-(5-methoxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
US20230192644A1 (en) * 2020-05-21 2023-06-22 Dana-Farber Cancer Institute, Inc. Piperidine-2,6-diones as small molecule degraders of helios and methods of use
EP4168007A1 (en) * 2020-06-23 2023-04-26 Novartis AG Dosing regimen comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives
IL301690A (en) * 2020-10-16 2023-05-01 Dana Farber Cancer Inst Inc Piperidinyl small molecule degraders of helios and methods of use
CN116669769A (zh) * 2020-10-16 2023-08-29 达纳-法伯癌症研究所公司 Helios的哌啶基小分子降解剂和使用方法
CN113046391A (zh) * 2021-03-22 2021-06-29 上海科技大学 一种crbn基因人源化动物肿瘤细胞模型的构建方法和用途
WO2022254362A1 (en) 2021-06-03 2022-12-08 Novartis Ag 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and medical uses thereof
TW202317546A (zh) 2021-07-09 2023-05-01 美商普萊克斯姆公司 調節ikzf2之芳基化合物及醫藥組合物
EP4423078A1 (en) 2021-10-28 2024-09-04 Gilead Sciences, Inc. Pyridizin-3(2h)-one derivatives
PE20241186A1 (es) 2021-10-29 2024-06-03 Gilead Sciences Inc Compuestos de cd73
CN118488948A (zh) 2021-12-22 2024-08-13 吉利德科学公司 Ikaros锌指家族降解剂及其用途
US20240124412A1 (en) 2021-12-22 2024-04-18 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
CA3248911A1 (en) 2022-01-28 2023-08-03 Gilead Sciences, Inc. POLY(ADENOSINE DIPHOSPHATE-RIBOSE) POLYMERASE 7 INHIBITORS
PL4245756T3 (pl) 2022-03-17 2025-02-17 Gilead Sciences, Inc. Środki degradujące palec cynkowy z rodziny ikaros i ich zastosowania
EP4511127A1 (en) 2022-04-21 2025-02-26 Gilead Sciences, Inc. Kras g12d modulating compounds
WO2024006929A1 (en) 2022-07-01 2024-01-04 Gilead Sciences, Inc. Cd73 compounds
EP4638436A1 (en) 2022-12-22 2025-10-29 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
WO2024215754A1 (en) 2023-04-11 2024-10-17 Gilead Sciences, Inc. Kras modulating compounds
PE20260121A1 (es) 2023-04-21 2026-01-16 Gilead Sciences Inc Inhibidores de prmt5 y usos de los mismos
JP2026522894A (ja) 2023-06-30 2026-07-09 ギリアード サイエンシーズ, インコーポレイテッド Kras調節化合物
AU2024297978A1 (en) 2023-07-26 2026-02-05 Gilead Sciences, Inc. Parp7 inhibitors
CN121568935A (zh) 2023-07-26 2026-02-24 吉利德科学公司 Parp7抑制剂
EP4774280A1 (en) 2023-09-08 2026-07-15 Gilead Sciences, Inc. Kras g12d modulating compounds
US20250109147A1 (en) 2023-09-08 2025-04-03 Gilead Sciences, Inc. Kras g12d modulating compounds
WO2025096589A1 (en) 2023-11-03 2025-05-08 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
TW202540200A (zh) 2023-12-01 2025-10-16 美商基利科學股份有限公司 抗fap-light融合蛋白及其用途
US20250230168A1 (en) 2023-12-22 2025-07-17 Gilead Sciences, Inc. Azaspiro wrn inhibitors
WO2025245003A1 (en) 2024-05-21 2025-11-27 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
WO2026026826A1 (en) * 2024-07-31 2026-02-05 Insilico Medicine Ip Limited Crbn-binding compounds and uses thereof
US20260098049A1 (en) 2024-08-12 2026-04-09 Gilead Sciences, Inc. Kras modulating compounds
WO2026080794A1 (en) * 2024-10-11 2026-04-16 Bristol-Myers Squibb Company Chemical compounds useful for degrading proteins
US20260130893A1 (en) 2024-10-21 2026-05-14 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
WO2026102277A1 (en) * 2024-11-08 2026-05-15 Plexium, Inc. Combination therapies comprising ikzf2 degrader compounds
WO2026136515A1 (en) 2024-12-19 2026-06-25 Gilead Sciences, Inc. Parp7 inhibitors

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018144649A1 (en) 2017-01-31 2018-08-09 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
WO2019079701A1 (en) 2017-10-20 2019-04-25 Dana-Farber Cancer Institute, Inc. HETEROBIFUNCTIONAL COMPOUNDS HAVING IMPROVED SPECIFICITY FOR BRD4 BROMODOMAINE
WO2020012334A1 (en) 2018-07-10 2020-01-16 Novartis Ag 3-(5-hydroxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and their use in the treatment of ikaros family zinc finger 2 (ikzf2)-dependent diseases

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8143283B1 (en) * 1993-03-01 2012-03-27 The Children's Medical Center Corporation Methods for treating blood-born tumors with thalidomide
JP4361273B2 (ja) * 2001-02-27 2009-11-11 アメリカ合衆国 潜在的な血管形成阻害剤としてのサリドマイド類似体
US7968569B2 (en) 2002-05-17 2011-06-28 Celgene Corporation Methods for treatment of multiple myeloma using 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione
CA2957226C (en) * 2008-10-29 2018-08-14 Celgene Corporation Isoindoline compounds for use in the treatment of cancer
WO2016196580A1 (en) 2015-06-02 2016-12-08 Celgene Corporation Methods for determining drug efficacy for treatment of cancer using ratios of cereblon associated proteins
CN121974842A (zh) 2016-05-10 2026-05-05 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
TWI793151B (zh) 2017-08-23 2023-02-21 瑞士商諾華公司 3-(1-氧異吲哚啉-2-基)之氫吡啶-2,6-二酮衍生物及其用途
CN118108706A (zh) 2017-09-04 2024-05-31 C4医药公司 戊二酰亚胺
US11512080B2 (en) 2018-01-12 2022-11-29 Kymera Therapeutics, Inc. CRBN ligands and uses thereof
EP3924054B1 (en) 2019-02-15 2025-04-02 Novartis AG 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
CA3123519A1 (en) 2019-02-15 2020-08-20 Novartis Ag Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
US20230192644A1 (en) * 2020-05-21 2023-06-22 Dana-Farber Cancer Institute, Inc. Piperidine-2,6-diones as small molecule degraders of helios and methods of use

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018144649A1 (en) 2017-01-31 2018-08-09 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
WO2019079701A1 (en) 2017-10-20 2019-04-25 Dana-Farber Cancer Institute, Inc. HETEROBIFUNCTIONAL COMPOUNDS HAVING IMPROVED SPECIFICITY FOR BRD4 BROMODOMAINE
WO2020012334A1 (en) 2018-07-10 2020-01-16 Novartis Ag 3-(5-hydroxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and their use in the treatment of ikaros family zinc finger 2 (ikzf2)-dependent diseases

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Publication number Publication date
WO2020117759A1 (en) 2020-06-11
CN113490495A (zh) 2021-10-08
CN113490495B (zh) 2024-09-27
AU2019391016B2 (en) 2025-05-29
EP3890736A1 (en) 2021-10-13
US20250388562A1 (en) 2025-12-25
KR102972506B1 (ko) 2026-06-04
JP2022510313A (ja) 2022-01-26
US20220177443A1 (en) 2022-06-09
US12227488B2 (en) 2025-02-18
KR20210098960A (ko) 2021-08-11
AU2019391016A1 (en) 2021-05-13
CA3119526A1 (en) 2020-06-11
EP3890736A4 (en) 2022-08-10

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