JP7108146B2 - 新規メチルキナゾリノン誘導体 - Google Patents

新規メチルキナゾリノン誘導体 Download PDF

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JP7108146B2
JP7108146B2 JP2021566023A JP2021566023A JP7108146B2 JP 7108146 B2 JP7108146 B2 JP 7108146B2 JP 2021566023 A JP2021566023 A JP 2021566023A JP 2021566023 A JP2021566023 A JP 2021566023A JP 7108146 B2 JP7108146 B2 JP 7108146B2
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compound
formula
cancer
braf
compounds
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JP2022531609A (ja
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コジモ ドレンテ,
デーヴィッド スティーブン ヘウィングス,
ダニエル フンツィカー,
ダニエラ クルメナッハ,
ピエルジョルジョ フランチェスコ トンマゾ ペッタッツォーニ,
ユルゲン ヴィヒマン,
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エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト
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    • 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
    • C07D405/02—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
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/46—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
    • C07D207/48—Sulfur atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Harvester Elements (AREA)
  • Combines (AREA)
JP2021566023A 2019-12-10 2020-12-08 新規メチルキナゾリノン誘導体 Active JP7108146B2 (ja)

Priority Applications (1)

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JP2021202780A JP7802514B2 (ja) 2019-12-10 2021-12-14 新規メチルキナゾリノン誘導体

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP19214941.7 2019-12-10
EP19214941 2019-12-10
PCT/EP2020/084976 WO2021116055A1 (en) 2019-12-10 2020-12-08 New methylquinazolinone derivatives

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JP2021202780A Division JP7802514B2 (ja) 2019-12-10 2021-12-14 新規メチルキナゾリノン誘導体

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JP2022531609A JP2022531609A (ja) 2022-07-07
JP7108146B2 true JP7108146B2 (ja) 2022-07-27

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022124458A (ja) * 2019-12-10 2022-08-25 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト 新規メチルキナゾリノン誘導体
JP2023505300A (ja) * 2019-12-10 2023-02-08 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト パラドックス遮断剤としての新規braf阻害剤

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MX2022015703A (es) 2020-06-09 2023-01-24 Array Biopharma Inc Compuestos para el tratamiento de enfermedades y trastornos asociados a braf.
AU2022290851A1 (en) 2021-06-08 2023-11-23 C4 Therapeutics, Inc. Therapeutics for the degradation of mutant braf
IL308015A (en) * 2021-06-09 2023-12-01 Hoffmann La Roche Combination of a particular braf inhibitor (paradox breaker) and a pd-1 axis binding antagonist for use in the treatment of cancer
CN117642166A (zh) * 2021-06-09 2024-03-01 中外制药株式会社 用于癌症治疗的组合疗法
JP2024522603A (ja) * 2021-06-09 2024-06-21 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト (3r)-n-[2-シアノ-4-フルオロ-3-(3-メチル-4-オキソ-キナゾリン-6-イル)オキシ-フェニル]-3-フルオロ-ピロリジン-1-スルホンアミドの新規固形物
EP4378478A4 (en) 2021-07-27 2025-11-12 Toray Industries MEDICINE FOR THE TREATMENT AND/OR PREVENTION OF CANCER
IL312171A (en) 2021-11-04 2024-06-01 Hoffmann La Roche Innovative use of the quinazolinone compound for cancer treatment
TW202409040A (zh) 2022-07-19 2024-03-01 大陸商西藏海思科製藥有限公司 作為激酶抑制劑的喹唑啉酮衍生物的製備及其用途
JP2025537786A (ja) 2022-11-18 2025-11-20 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト 進行性固形がんまたは転移の治療のためのbraf阻害剤としてのキナゾリノン化合物
EP4634171A1 (en) * 2022-12-15 2025-10-22 F. Hoffmann-La Roche AG Process for the preparation of a quinazolinone derivative
JP2025541200A (ja) * 2022-12-15 2025-12-18 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト がん処置のための併用療法
IL324898A (en) 2023-07-04 2026-01-01 Hoffmann La Roche New solid forms of (3r)-n-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinozolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide
WO2025108405A1 (zh) 2023-11-22 2025-05-30 西藏海思科制药有限公司 作为激酶抑制剂的喹唑啉酮衍生物的制备及其用途
WO2025153057A1 (zh) 2024-01-17 2025-07-24 海思科医药集团股份有限公司 一种含braf抑制剂的药物组合物及其在医药上的应用
WO2026037755A1 (en) 2024-08-13 2026-02-19 F. Hoffmann-La Roche Ag New methylquinazolinone derivatives
WO2026046946A1 (en) 2024-08-28 2026-03-05 F. Hoffmann-La Roche Ag New solid forms of (3r)-n-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinazolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide

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WO2012118492A1 (en) 2011-03-01 2012-09-07 Array Biopharma Inc. Heterocyclic sulfonamides as raf inhibitors
JP2018515570A (ja) 2015-05-22 2018-06-14 プレキシコン インコーポレーテッドPlexxikon Inc. Braf−v600関連疾患の治療に使用するためのplx−8394またはplx−7904

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GB0525069D0 (en) 2005-12-08 2006-01-18 Novartis Ag Organic compounds
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JP2010533729A (ja) 2007-07-17 2010-10-28 プレキシコン,インコーポレーテッド キナーゼ調節のための化合物と方法、及びそのための適応
AU2009226136B2 (en) 2008-03-17 2013-08-15 Ambit Biosciences Corporation Quinazoline derivatives as RAF kinase modulators and methods of use thereof
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
TW201041888A (en) 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
AR091876A1 (es) 2012-07-26 2015-03-04 Novartis Ag Combinaciones farmaceuticas para el tratamiento de enfermedades proliferativas
CA2882410A1 (en) 2012-09-19 2014-03-27 Novartis Ag Dihydropyrrolidino-pyrimidines as kinase inhibitors
RU2015149937A (ru) 2013-05-30 2017-07-06 Плексксикон Инк. Соединения для модулирования киназы и показания к их применению
PL3359541T3 (pl) 2015-10-09 2021-01-11 AbbVie Overseas S.à r.l. N-SULFONYLOWANE PIRAZOLO[3,4-b]PIRYDYNO-6-KARBOKSAMIDY I SPOSÓB ZASTOSOWANIA
RU2687107C1 (ru) 2018-06-18 2019-05-07 федеральное государственное автономное образовательное учреждение высшего образования "Московский физико-технический институт (государственный университет)" Ингибитор braf киназы n-(3-(5-(4-хлорофенил)-1h-пиразоло[3,4-b]пиридин-3-карбонил)-2,4-дифторофенил) пропан-1-сульфонамид
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TWI817018B (zh) * 2019-06-28 2023-10-01 美商艾瑞生藥股份有限公司 用於治療braf相關的疾病和失調症之化合物
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CA3158541A1 (en) * 2019-12-10 2021-06-17 Cosimo Dolente New braf inhibitors as paradox breakers
MX2022015703A (es) 2020-06-09 2023-01-24 Array Biopharma Inc Compuestos para el tratamiento de enfermedades y trastornos asociados a braf.
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AU2022290851A1 (en) 2021-06-08 2023-11-23 C4 Therapeutics, Inc. Therapeutics for the degradation of mutant braf
KR20240115893A (ko) 2021-12-08 2024-07-26 어레이 바이오파마 인크. N-(2-클로로-3-((5-클로로-3-메틸-4-옥소-3,4-다이하이드로퀴나졸린-6-일)아미노)-4-플루오로페닐)-3-플루오로아제티딘-1-설폰아미드의결정질 형태

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WO2012118492A1 (en) 2011-03-01 2012-09-07 Array Biopharma Inc. Heterocyclic sulfonamides as raf inhibitors
JP2018515570A (ja) 2015-05-22 2018-06-14 プレキシコン インコーポレーテッドPlexxikon Inc. Braf−v600関連疾患の治療に使用するためのplx−8394またはplx−7904

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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022124458A (ja) * 2019-12-10 2022-08-25 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト 新規メチルキナゾリノン誘導体
JP2023505300A (ja) * 2019-12-10 2023-02-08 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト パラドックス遮断剤としての新規braf阻害剤
JP7788380B2 (ja) 2019-12-10 2025-12-18 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト パラドックス遮断剤としての新規braf阻害剤
JP7802514B2 (ja) 2019-12-10 2026-01-20 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト 新規メチルキナゾリノン誘導体

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CN114787156B (zh) 2024-07-26
EP4073065B1 (en) 2025-02-19
BR112022011123A2 (pt) 2022-08-23
LT4073065T (lt) 2025-04-25
MA58087B1 (fr) 2025-04-30
CN118791472A (zh) 2024-10-18
PH12022551119A1 (en) 2023-08-23
TW202136245A (zh) 2021-10-01
ZA202204675B (en) 2022-12-21
HRP20250418T1 (hr) 2025-06-06
AU2020403443A1 (en) 2022-05-12
SI4073065T1 (sl) 2025-06-30
US20240174621A1 (en) 2024-05-30
KR102836833B1 (ko) 2025-07-22
KR20220110554A (ko) 2022-08-08
PE20221778A1 (es) 2022-11-16
EP4483882A3 (en) 2025-03-05
ES3023264T3 (en) 2025-05-30
IL316473A (en) 2024-12-01
PT4073065T (pt) 2025-04-15
HUE071148T2 (hu) 2025-08-28
IL292161A (en) 2022-06-01
RS66721B1 (sr) 2025-05-30
MX2022006783A (es) 2022-07-11
CL2022001529A1 (es) 2023-02-10
PL4073065T3 (pl) 2025-05-19
US20220298119A1 (en) 2022-09-22
IL292161B2 (en) 2025-04-01
EP4483882A2 (en) 2025-01-01
FI4073065T3 (fi) 2025-04-16
AR122351A1 (es) 2022-09-07
TWI877268B (zh) 2025-03-21
WO2021116055A1 (en) 2021-06-17
CA3162883A1 (en) 2021-06-17
NZ787393A (en) 2025-07-25
ZA202206923B (en) 2024-10-30
CR20220251A (es) 2022-07-11
US12116349B2 (en) 2024-10-15
CN114787156A (zh) 2022-07-22
IL292161B1 (en) 2024-12-01
DK4073065T3 (da) 2025-04-22
TW202504895A (zh) 2025-02-01
EP4073065A1 (en) 2022-10-19
TWI908405B (zh) 2025-12-11
JP7802514B2 (ja) 2026-01-20
JP2022531609A (ja) 2022-07-07
AU2020403443B2 (en) 2023-02-23
UA128299C2 (uk) 2024-05-29
CO2022008968A2 (es) 2022-07-19
JP2022124458A (ja) 2022-08-25

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