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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JP2022510313A (ja
JPWO2020117759A5 (https=
JP2022510313A5 (https=
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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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 (4)

Publication Number Publication Date
JP2022510313A JP2022510313A (ja) 2022-01-26
JPWO2020117759A5 JPWO2020117759A5 (https=) 2022-12-08
JP2022510313A5 JP2022510313A5 (https=) 2022-12-08
JP7709378B2 true JP7709378B2 (ja) 2025-07-16

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US (2) US12227488B2 (https=)
EP (1) EP3890736A4 (https=)
JP (1) JP7709378B2 (https=)
KR (1) KR20210098960A (https=)
CN (1) CN113490495B (https=)
AU (1) AU2019391016B2 (https=)
CA (1) CA3119526A1 (https=)
WO (1) WO2020117759A1 (https=)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7682181B2 (ja) 2019-12-18 2025-05-23 ノバルティス アーゲー 3-(5-メトキシ-1-オキソイソインドリン-2-イル)ピペリジン-2,6-ジオン誘導体及びその使用
AU2021275146A1 (en) * 2020-05-21 2022-09-29 Dana-Farber Cancer Institute, Inc. Piperidine-2,6-diones as small molecule degraders of Helios and methods of use
CN115916199A (zh) * 2020-06-23 2023-04-04 诺华股份有限公司 包含3-(1-氧代异吲哚啉-2-基)哌啶-2,6-二酮衍生物的给药方案
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
PY2243958A (es) * 2021-06-03 2023-01-20 Novartis Ag Derivados de 3–(5–oxi)–1–oxoisoindolin–2–il)piperidina–2,6–diona y sus usos
KR20240035820A (ko) 2021-07-09 2024-03-18 플렉시움 인코포레이티드 Ikzf2를 조절하는 아릴 화합물 및 약학 조성물
US20230183216A1 (en) 2021-10-28 2023-06-15 Gilead Sciences, Inc. Pyridizin-3(2h)-one derivatives
EP4422756A1 (en) 2021-10-29 2024-09-04 Gilead Sciences, Inc. Cd73 compounds
EP4452415B1 (en) 2021-12-22 2026-02-25 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
CN118488946A (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
TW202340168A (zh) 2022-01-28 2023-10-16 美商基利科學股份有限公司 Parp7抑制劑
CA3253296A1 (en) 2022-03-17 2023-09-21 Gilead Sciences, Inc. Zinc Finger Degradation Agents of the Ikaros Family and Their Uses
WO2023205719A1 (en) 2022-04-21 2023-10-26 Gilead Sciences, Inc. Kras g12d modulating compounds
US20240116928A1 (en) 2022-07-01 2024-04-11 Gilead Sciences, Inc. Cd73 compounds
EP4638436A1 (en) 2022-12-22 2025-10-29 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
CN120882725A (zh) 2023-04-11 2025-10-31 吉利德科学公司 Kras调节化合物
WO2024220917A1 (en) 2023-04-21 2024-10-24 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
US20250042922A1 (en) 2023-06-30 2025-02-06 Gilead Sciences, Inc. Kras modulating compounds
US20250066328A1 (en) 2023-07-26 2025-02-27 Gilead Sciences, Inc. Parp7 inhibitors
AU2024297978A1 (en) 2023-07-26 2026-02-05 Gilead Sciences, Inc. Parp7 inhibitors
AU2024337913A1 (en) 2023-09-08 2026-03-26 Gilead Sciences, Inc. Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds
WO2025054347A1 (en) 2023-09-08 2025-03-13 Gilead Sciences, Inc. Kras g12d modulating compounds
US20250154172A1 (en) 2023-11-03 2025-05-15 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
AR134514A1 (es) 2023-12-01 2026-01-21 Gilead Sciences Inc Proteína de fusión anti-fap-ligera y uso de esta
WO2025137640A1 (en) 2023-12-22 2025-06-26 Gilead Sciences, Inc. Azaspiro wrn inhibitors
US20250376484A1 (en) 2024-05-21 2025-12-11 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
WO2026039365A1 (en) 2024-08-12 2026-02-19 Gilead Sciences, Inc. Kras modulating compounds
WO2026080794A1 (en) * 2024-10-11 2026-04-16 Bristol-Myers Squibb Company Chemical compounds useful for degrading proteins

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
AU2002306596B2 (en) * 2001-02-27 2008-01-17 The Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Analogs of thalidomide as potential angiogenesis inhibitors
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
PE20110547A1 (es) 2008-10-29 2011-08-04 Celgene Corp Compuestos de isoindolina con actividad anticancerigena
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
CN109790143A (zh) 2016-05-10 2019-05-21 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
WO2019140387A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
CN113490528B (zh) 2019-02-15 2024-12-03 诺华股份有限公司 3-(1-氧代-5-(哌啶-4-基)异吲哚啉-2-基)哌啶-2,6-二酮衍生物及其用途
EP3924055B1 (en) 2019-02-15 2024-04-03 Novartis AG Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
AU2021275146A1 (en) * 2020-05-21 2022-09-29 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

Also Published As

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

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