JP7426398B2 - Ｒａｓ阻害剤としての新規イソインドリノン置換インドールおよび誘導体 - Google Patents

Ｒａｓ阻害剤としての新規イソインドリノン置換インドールおよび誘導体 Download PDF

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JP7426398B2
JP7426398B2 JP2021549575A JP2021549575A JP7426398B2 JP 7426398 B2 JP7426398 B2 JP 7426398B2 JP 2021549575 A JP2021549575 A JP 2021549575A JP 2021549575 A JP2021549575 A JP 2021549575A JP 7426398 B2 JP7426398 B2 JP 7426398B2
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methyl
indol
dihydro
hydroxy
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アンドレアス マントウリディス
アンドレアス ゴルナー
ディルク ケスラー
レティシア ジャニーヌ マルタン
ハーラルト ヴァインスタブル
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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
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    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
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    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • 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
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    • 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
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    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
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    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2021549575A 2019-02-26 2020-02-25 Ｒａｓ阻害剤としての新規イソインドリノン置換インドールおよび誘導体 Active JP7426398B2 (ja)

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EP19159299 2019-02-26
EP19159299.7 2019-02-26
PCT/EP2020/054897 WO2020173935A1 (en) 2019-02-26 2020-02-25 New isoindolinone substituted indoles and derivatives as ras inhibitors

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JP2022523201A JP2022523201A (ja) 2022-04-21
JP2022523201A5 JP2022523201A5 (https=) 2023-03-03
JP7426398B2 true JP7426398B2 (ja) 2024-02-01

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US (1) US12281099B2 (https=)
EP (1) EP3931188B1 (https=)
JP (1) JP7426398B2 (https=)
CN (1) CN113474340B (https=)
WO (1) WO2020173935A1 (https=)

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WO2019195609A2 (en) 2018-04-04 2019-10-10 Arvinas Operations, Inc. Modulators of proteolysis and associated methods of use
EP4143196A4 (en) 2020-04-29 2024-04-17 Relay Therapeutics, Inc. PI3K-A INHIBITORS AND METHODS OF USE THEREOF
CA3194067A1 (en) 2020-09-15 2022-03-24 Revolution Medicines, Inc. Ras inhibitors
GB202104609D0 (en) 2021-03-31 2021-05-12 Sevenless Therapeutics Ltd New Treatments for Pain
EP4313151A1 (en) 2021-03-31 2024-02-07 Sevenless Therapeutics Limited Sos1 inhibitors and ras inhibitors for use in the treatment of pain
CN115232108B (zh) 2021-04-23 2025-04-18 领泰生物医药(绍兴)有限公司 Sos1降解剂及其制备方法和应用
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
EP4416131A4 (en) * 2021-10-15 2025-07-30 Genetolead Inc RAS INHIBITORS, COMPOSITIONS AND METHODS OF USE THEREOF
TW202334136A (zh) * 2021-11-03 2023-09-01 美商傳達治療有限公司 PI3Kα抑制劑及其製造與使用方法
WO2023114973A1 (en) 2021-12-17 2023-06-22 Shure Acquisition Holdings, Inc. Adaptive acoustic echo cancellation for a stereo audio signal
CN119212994A (zh) 2021-12-17 2024-12-27 建新公司 作为shp2抑制剂的吡唑并吡嗪化合物
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
EP4473970A4 (en) 2022-03-31 2026-01-21 Eisai R&D Man Co Ltd PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF TUMORS
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
EP4598538A1 (en) 2022-10-05 2025-08-13 Sevenless Therapeutics Limited New treatments for pain
US12448399B2 (en) 2023-01-26 2025-10-21 Arvinas Operations, Inc. Cereblon-based KRAS degrading PROTACs and uses related thereto
AU2023439518A1 (en) 2023-04-06 2025-08-28 Eisai R&D Management Co., Ltd. Pharmaceutical composition for treating tumors
CR20250420A (es) 2023-04-07 2025-11-20 Revolution Medicines Inc Inhibidores macrocíclicos de ras
AR132338A1 (es) 2023-04-07 2025-06-18 Revolution Medicines Inc Inhibidores de ras
CN121100123A (zh) 2023-04-14 2025-12-09 锐新医药公司 Ras抑制剂的结晶形式
CN121464140A (zh) 2023-04-14 2026-02-03 锐新医药公司 Ras抑制剂的结晶形式、含有其的组合物及其使用方法

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WO2018068017A1 (en) 2016-10-07 2018-04-12 Araxes Pharma Llc Heterocyclic compounds as inhibitors of ras and methods of use thereof
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CN113474340B (zh) 2024-07-23
EP3931188A1 (en) 2022-01-05
US12281099B2 (en) 2025-04-22
JP2022523201A (ja) 2022-04-21
WO2020173935A1 (en) 2020-09-03
EP3931188B1 (en) 2023-08-30
US20220144810A1 (en) 2022-05-12
CN113474340A (zh) 2021-10-01

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