TWI877268B - 新穎甲基喹唑啉酮衍生物 - Google Patents

新穎甲基喹唑啉酮衍生物 Download PDF

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Publication number
TWI877268B
TWI877268B TW109143500A TW109143500A TWI877268B TW I877268 B TWI877268 B TW I877268B TW 109143500 A TW109143500 A TW 109143500A TW 109143500 A TW109143500 A TW 109143500A TW I877268 B TWI877268 B TW I877268B
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TW
Taiwan
Prior art keywords
compound
formula
pharmaceutically acceptable
acceptable salt
braf
Prior art date
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TW109143500A
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English (en)
Chinese (zh)
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TW202136245A (zh
Inventor
可西摩 多藍提
大衛 赫溫
丹尼爾 亨尼克
丹尼拉 庫曼亞契
皮爾吉奧吉奧 佩塔佐尼
裘根 衛奇曼
Original Assignee
瑞士商赫孚孟拉羅股份公司
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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
    • 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
    • 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

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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)
TW109143500A 2019-12-10 2020-12-09 新穎甲基喹唑啉酮衍生物 TWI877268B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP19214941.7 2019-12-10
EP19214941 2019-12-10

Publications (2)

Publication Number Publication Date
TW202136245A TW202136245A (zh) 2021-10-01
TWI877268B true TWI877268B (zh) 2025-03-21

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TW109143500A TWI877268B (zh) 2019-12-10 2020-12-09 新穎甲基喹唑啉酮衍生物
TW113139852A TWI908405B (zh) 2019-12-10 2020-12-09 新穎甲基喹唑啉酮衍生物

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TW113139852A TWI908405B (zh) 2019-12-10 2020-12-09 新穎甲基喹唑啉酮衍生物

Country Status (29)

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US (2) US12116349B2 (enExample)
EP (2) EP4483882A3 (enExample)
JP (2) JP7108146B2 (enExample)
KR (1) KR102836833B1 (enExample)
CN (2) CN114787156B (enExample)
AR (1) AR122351A1 (enExample)
AU (1) AU2020403443B2 (enExample)
CL (1) CL2022001529A1 (enExample)
CO (1) CO2022008968A2 (enExample)
CR (1) CR20220251A (enExample)
DK (1) DK4073065T3 (enExample)
ES (1) ES3023264T3 (enExample)
FI (1) FI4073065T3 (enExample)
HR (1) HRP20250418T1 (enExample)
HU (1) HUE071148T2 (enExample)
IL (2) IL316473A (enExample)
LT (1) LT4073065T (enExample)
MA (1) MA58087B1 (enExample)
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PE (1) PE20221778A1 (enExample)
PH (1) PH12022551119A1 (enExample)
PL (1) PL4073065T3 (enExample)
PT (1) PT4073065T (enExample)
RS (1) RS66721B1 (enExample)
SI (1) SI4073065T1 (enExample)
TW (2) TWI877268B (enExample)
UA (1) UA128299C2 (enExample)
WO (1) WO2021116055A1 (enExample)
ZA (2) ZA202204675B (enExample)

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CA3158541A1 (en) * 2019-12-10 2021-06-17 Cosimo Dolente New braf inhibitors as paradox breakers
SI4073065T1 (sl) 2019-12-10 2025-06-30 F. Hoffmann-La Roche Ag Novi derivati metilkinazolinona
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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JP4429085B2 (ja) 2004-06-08 2010-03-10 有限会社コンペックス 茸栽培用殺菌菌床組成物の製造法及び茸栽培法
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RU2015149937A (ru) 2013-05-30 2017-07-06 Плексксикон Инк. Соединения для модулирования киназы и показания к их применению
BR112017025045A2 (pt) 2015-05-22 2018-08-07 Plexxikon Inc plx-8394 ou plx-7904 para uso no tratamento de doenças relacionadas a braf-v600
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
SI4073065T1 (sl) 2019-12-10 2025-06-30 F. Hoffmann-La Roche Ag Novi derivati metilkinazolinona
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.
WO2022129259A1 (en) 2020-12-18 2022-06-23 F. Hoffmann-La Roche Ag New quinazolinone derivatives
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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

Patent Citations (1)

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Publication number Publication date
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
JP7108146B2 (ja) 2022-07-27
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
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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