JP2025500430A - Ｋ－ＲＡＳ ＧＴＰａｓｅのＧ１２Ｓ、Ｇ１２Ｄ、及び／又はＧ１２Ｅ変異体の共有結合阻害剤 - Google Patents

Ｋ－ＲＡＳ ＧＴＰａｓｅのＧ１２Ｓ、Ｇ１２Ｄ、及び／又はＧ１２Ｅ変異体の共有結合阻害剤 Download PDF

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JP2025500430A
JP2025500430A JP2024537994A JP2024537994A JP2025500430A JP 2025500430 A JP2025500430 A JP 2025500430A JP 2024537994 A JP2024537994 A JP 2024537994A JP 2024537994 A JP2024537994 A JP 2024537994A JP 2025500430 A JP2025500430 A JP 2025500430A
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substituted
unsubstituted
ras
nhc
och
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JP2025500430A5 (https=
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ショカット，ケバン・エム
ジャン，ジーヤン
ジェン，チンヘン
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ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア
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    • 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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • 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
    • 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
    • C07D487/08—Bridged 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
    • C07D487/10—Spiro-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
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2024537994A 2021-12-22 2022-12-21 Ｋ－ＲＡＳ ＧＴＰａｓｅのＧ１２Ｓ、Ｇ１２Ｄ、及び／又はＧ１２Ｅ変異体の共有結合阻害剤 Pending JP2025500430A (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US202163292910P 2021-12-22 2021-12-22
US63/292,910 2021-12-22
US202263313040P 2022-02-23 2022-02-23
US63/313,040 2022-02-23
US202263322528P 2022-03-22 2022-03-22
US63/322,528 2022-03-22
PCT/US2022/082136 WO2023122662A1 (en) 2021-12-22 2022-12-21 Covalently binding inhibitors of g12s, g12d and/or g12e mutants of k-ras gtpase

Publications (2)

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JP2025500430A true JP2025500430A (ja) 2025-01-09
JP2025500430A5 JP2025500430A5 (https=) 2026-01-05

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JP2024537994A Pending JP2025500430A (ja) 2021-12-22 2022-12-21 Ｋ－ＲＡＳ ＧＴＰａｓｅのＧ１２Ｓ、Ｇ１２Ｄ、及び／又はＧ１２Ｅ変異体の共有結合阻害剤

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US (1) US20250059187A1 (https=)
EP (1) EP4452416A1 (https=)
JP (1) JP2025500430A (https=)
AU (1) AU2022421224A1 (https=)
CA (1) CA3240772A1 (https=)
IL (1) IL313428A (https=)
MX (1) MX2024007780A (https=)
TW (1) TW202340202A (https=)
WO (1) WO2023122662A1 (https=)

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AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ｒａｓ相關疾病或病症之組合療法
WO2025010415A1 (en) * 2023-07-05 2025-01-09 The Regents Of The University Of California Gtpase inhibitors and uses thereof
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
US20250109147A1 (en) 2023-09-08 2025-04-03 Gilead Sciences, Inc. Kras g12d modulating compounds
US20250114339A1 (en) 2023-10-09 2025-04-10 Incyte Corporation Combination therapy comprising a kras g12d inhibitor and an egfr inhibitor
US20250114346A1 (en) 2023-10-09 2025-04-10 Incyte Corporation Combination therapy using a kras g12d inhibitor and pd-1 inhibitor or pd-l1 inhibitor
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2025096984A1 (en) * 2023-11-02 2025-05-08 The Regents Of The University Of California Gtpase inhibitors and uses thereof
AU2024374420A1 (en) * 2023-11-02 2026-04-16 Kumquat Biosciences Inc. Degraders and uses thereof
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WO2025212580A1 (en) * 2024-04-01 2025-10-09 Xdc Precision Therapeutics Llc Antibody-kras binder conjugates, pharmaceutical compositions, and therapeutic applications
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
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WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
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TW202340202A (zh) 2023-10-16
IL313428A (en) 2024-08-01
AU2022421224A1 (en) 2024-06-20
US20250059187A1 (en) 2025-02-20
CA3240772A1 (en) 2023-06-29
EP4452416A1 (en) 2024-10-30
MX2024007780A (es) 2024-09-11
WO2023122662A1 (en) 2023-06-29

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