JP2025506408A - キナゾリンpan-KRas阻害剤 - Google Patents

キナゾリンpan-KRas阻害剤 Download PDF

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Publication number
JP2025506408A
JP2025506408A JP2024546129A JP2024546129A JP2025506408A JP 2025506408 A JP2025506408 A JP 2025506408A JP 2024546129 A JP2024546129 A JP 2024546129A JP 2024546129 A JP2024546129 A JP 2024546129A JP 2025506408 A JP2025506408 A JP 2025506408A
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Prior art keywords
kras
alkyl
equiv
fluoro
methoxy
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Pending
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JP2024546129A
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Japanese (ja)
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JPWO2023150284A5 (https=
JP2025506408A5 (https=
Inventor
ワン,シャオルン
イベタック,アンソニー
クリューク,スビトラナ
ローソン,ジョン・デイビッド
マークス,マシュー・アーノルド
スミス,クリストファー・ロナルド
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Mirati Therapeutics Inc
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Mirati Therapeutics Inc
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Publication of JP2025506408A publication Critical patent/JP2025506408A/ja
Publication of JPWO2023150284A5 publication Critical patent/JPWO2023150284A5/ja
Publication of JP2025506408A5 publication Critical patent/JP2025506408A5/ja
Pending legal-status Critical Current

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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
    • A61K31/495Heterocyclic 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2024546129A 2022-02-03 2023-02-03 キナゾリンpan-KRas阻害剤 Pending JP2025506408A (ja)

Applications Claiming Priority (13)

Application Number Priority Date Filing Date Title
US202263306271P 2022-02-03 2022-02-03
US63/306,271 2022-02-03
US202263327625P 2022-04-05 2022-04-05
US63/327,625 2022-04-05
US202263352180P 2022-06-14 2022-06-14
US63/352,180 2022-06-14
US202263432243P 2022-12-13 2022-12-13
US63/432,243 2022-12-13
US202263434327P 2022-12-21 2022-12-21
US63/434,327 2022-12-21
US202363442648P 2023-02-01 2023-02-01
US63/442,648 2023-02-01
PCT/US2023/012299 WO2023150284A2 (en) 2022-02-03 2023-02-03 Quinazoline pan-kras inhibitors

Publications (3)

Publication Number Publication Date
JP2025506408A true JP2025506408A (ja) 2025-03-11
JPWO2023150284A5 JPWO2023150284A5 (https=) 2026-02-04
JP2025506408A5 JP2025506408A5 (https=) 2026-02-04

Family

ID=87552808

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2024546129A Pending JP2025506408A (ja) 2022-02-03 2023-02-03 キナゾリンpan-KRas阻害剤

Country Status (9)

Country Link
US (1) US20240025907A1 (https=)
EP (1) EP4472980A4 (https=)
JP (1) JP2025506408A (https=)
KR (1) KR20240145987A (https=)
AU (1) AU2023216698A1 (https=)
CA (1) CA3239343A1 (https=)
IL (1) IL314486A (https=)
MX (1) MX2024009616A (https=)
WO (1) WO2023150284A2 (https=)

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JP2024543879A (ja) * 2021-11-24 2024-11-26 メルク・シャープ・アンド・ドーム・エルエルシー Kras変異型タンパク質の小分子阻害剤
AU2023218370B2 (en) 2022-02-09 2024-11-28 Quanta Therapeutics, Inc. Kras modulators and uses thereof
CN119585287A (zh) 2022-05-06 2025-03-07 Paq医疗公司 Kras g12d蛋白水解靶向嵌合体
IL317601A (en) 2022-05-25 2025-02-01 Quanta Therapeutics Inc Pyrimidine-based modulators and their uses
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CN117659050A (zh) * 2022-09-08 2024-03-08 深圳福沃药业有限公司 用于治疗癌症的kras突变抑制剂的喹唑啉杂环类衍生物
WO2024112654A1 (en) 2022-11-21 2024-05-30 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
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WO2023150284A3 (en) 2023-09-14
EP4472980A4 (en) 2026-04-22
EP4472980A2 (en) 2024-12-11
CA3239343A1 (en) 2023-08-10
US20240025907A1 (en) 2024-01-25
KR20240145987A (ko) 2024-10-07
MX2024009616A (es) 2024-08-09
AU2023216698A1 (en) 2024-06-13
IL314486A (en) 2024-09-01
WO2023150284A2 (en) 2023-08-10

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