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)
  • Harvester Elements (AREA)
  • Combines (AREA)
  • Plural Heterocyclic Compounds (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 JP2022124458A (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 2019-12-10
EP19214941.7 2019-12-10
PCT/EP2020/084976 WO2021116055A1 (en) 2019-12-10 2020-12-08 New methylquinazolinone derivatives

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JP2021202780A Division JP2022124458A (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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EP (2) EP4483882A3 (OSRAM)
JP (2) JP7108146B2 (OSRAM)
KR (1) KR102836833B1 (OSRAM)
CN (2) CN114787156B (OSRAM)
AR (1) AR122351A1 (OSRAM)
AU (1) AU2020403443B2 (OSRAM)
CA (1) CA3162883A1 (OSRAM)
CL (1) CL2022001529A1 (OSRAM)
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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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PE20231651A1 (es) 2020-06-09 2023-10-17 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
MX2023014565A (es) * 2021-06-09 2024-02-08 Chugai Pharmaceutical Co Ltd Tratamiento conjunto para tratamiento contra el cancer.
CA3216220A1 (en) * 2021-06-09 2022-12-15 F. Hoffmann-La Roche Ag Combination of a particular braf inhibitor (paradox breaker) and a pd-1 axis binding antagonist for use in the treatment of cancer
TW202313589A (zh) * 2021-06-09 2023-04-01 瑞士商赫孚孟拉羅股份公司 （３ｒ）－ｎ－〔２－氰基－４－氟－３－（－３－甲基－４－側氧－喹唑啉－６－基）氧－苯基〕－３－氟－吡咯啶－１－磺醯胺之新穎固體形式
CN117677398A (zh) 2021-07-27 2024-03-08 东丽株式会社 用于癌的治疗和/或预防的药品
CA3230652A1 (en) 2021-11-04 2023-05-11 F. Hoffmann-La Roche Ag Novel use of quinazolinone compound for the treatment of cancer
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
EP4618994A1 (en) 2022-11-18 2025-09-24 F. Hoffmann-La Roche AG Quinazolinone compound as braf inhibitor for the treatment of advanced solid cancer or metastases
TW202438072A (zh) * 2022-12-15 2024-10-01 瑞士商赫孚孟拉羅股份公司 製備喹唑啉酮衍生物之方法
CN120359214A (zh) * 2022-12-15 2025-07-22 豪夫迈·罗氏有限公司 用于癌症治疗的组合疗法
WO2025008313A1 (en) 2023-07-04 2025-01-09 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
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

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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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BRPI0814423B1 (pt) 2007-07-17 2022-04-19 Plexxikon, Inc Compostos que modulam quinase e composição farmacêutica compreendendo os mesmos
PT2947072T (pt) 2008-03-17 2016-12-06 Ambit Biosciences Corp 1-(3-(6,7-dimetoxiquinazolin-4-iloxi)fenil)-3-(5-(1,1,1-trifluoro-2-metilpropan-2-il)isoxazol-3-il)ureia como modulador da cinase raf no tratamento de doenças oncológicas
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RU2015149937A (ru) 2013-05-30 2017-07-06 Плексксикон Инк. Соединения для модулирования киназы и показания к их применению
TWI720032B (zh) 2015-10-09 2021-03-01 比利時商葛萊伯格有限公司 Ｎ－磺醯化吡唑并﹝３，４－ｂ﹞吡啶－６－甲醯胺及其使用方法
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
JP7539892B2 (ja) 2019-01-03 2024-08-26 ジェネンテック， インコーポレイテッド 癌疾患の処置のためのエンドリボヌクレアーゼのイノシトール要求酵素ｉ（ｉｒｅｉアルファ）の阻害剤としてのピリド－ピリミジノン化合物及びプテリジノン化合物
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
PL4073044T3 (pl) * 2019-12-10 2025-05-19 F. Hoffmann-La Roche Ag Nowe inhibitory BRAF jako związki przełamujące paradoks
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PE20231651A1 (es) 2020-06-09 2023-10-17 Array Biopharma Inc Compuestos para el tratamiento de enfermedades y trastornos asociados a braf
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EP4263518A1 (en) 2020-12-18 2023-10-25 F. Hoffmann-La Roche AG New quinazolinone derivatives
AU2022290851A1 (en) 2021-06-08 2023-11-23 C4 Therapeutics, Inc. Therapeutics for the degradation of mutant braf
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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 (3)

* 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

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

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