CA3162883A1 - (3r)-and (3s)-n-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinazolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide compounds and their use as braf inhibitors - Google Patents

(3r)-and (3s)-n-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinazolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide compounds and their use as braf inhibitors

Info

Publication number
CA3162883A1
CA3162883A1 CA3162883A CA3162883A CA3162883A1 CA 3162883 A1 CA3162883 A1 CA 3162883A1 CA 3162883 A CA3162883 A CA 3162883A CA 3162883 A CA3162883 A CA 3162883A CA 3162883 A1 CA3162883 A1 CA 3162883A1
Authority
CA
Canada
Prior art keywords
compound
formula
cancer
braf
treatment
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CA3162883A
Other languages
English (en)
French (fr)
Inventor
Cosimo Dolente
David Stephen HEWINGS
Daniel Hunziker
Daniela Krummenacher
Piergiorgio Francesco Tommaso PETTAZZONI
Juergen Wichmann
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of CA3162883A1 publication Critical patent/CA3162883A1/en
Pending legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (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)
  • Combines (AREA)
  • Harvester Elements (AREA)
CA3162883A 2019-12-10 2020-12-08 (3r)-and (3s)-n-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinazolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide compounds and their use as braf inhibitors Pending CA3162883A1 (en)

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

Publications (1)

Publication Number Publication Date
CA3162883A1 true CA3162883A1 (en) 2021-06-17

Family

ID=68848113

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3162883A Pending CA3162883A1 (en) 2019-12-10 2020-12-08 (3r)-and (3s)-n-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinazolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide compounds and their use as braf inhibitors

Country Status (31)

Country Link
US (2) US12116349B2 (enExample)
EP (2) EP4483882A3 (enExample)
JP (2) JP7108146B2 (enExample)
KR (1) KR102836833B1 (enExample)
CN (2) CN118791472A (enExample)
AR (1) AR122351A1 (enExample)
AU (1) AU2020403443B2 (enExample)
CA (1) CA3162883A1 (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) IL292161B2 (enExample)
LT (1) LT4073065T (enExample)
MA (1) MA58087B1 (enExample)
MX (1) MX2022006783A (enExample)
NZ (1) NZ787393A (enExample)
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 (1) TWI877268B (enExample)
UA (1) UA128299C2 (enExample)
WO (1) WO2021116055A1 (enExample)
ZA (2) ZA202204675B (enExample)

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MX2022006711A (es) * 2019-12-10 2022-07-12 Hoffmann La Roche Nuevos inhibidores de braf como rompedores de la paradoja.
WO2021116055A1 (en) 2019-12-10 2021-06-17 F. Hoffmann-La Roche Ag New methylquinazolinone derivatives
US12303509B2 (en) 2020-06-09 2025-05-20 Pfizer Inc. Compounds for the treatment of BRAF-associated diseases and disorders
MX2023014059A (es) 2021-06-08 2024-03-12 C4 Therapeutics Inc Terapeuticos para la degradacion de una proteina quiinasa de serina/ treonina mutante.
WO2022258584A1 (en) * 2021-06-09 2022-12-15 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
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
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
WO2023078881A1 (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
CN120265291A (zh) 2022-11-18 2025-07-04 豪夫迈·罗氏有限公司 喹唑啉酮化合物的新用途和制剂
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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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
EP3941919B1 (en) 2019-01-03 2025-12-24 Genentech, Inc. Pyrido-pyrimidinone and pteridinone compounds as inhibitors of endoribonuclease inositol requiring enzyme i (ire i alpha) for the treatment of cancer diseases.
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
WO2021116055A1 (en) 2019-12-10 2021-06-17 F. Hoffmann-La Roche Ag New methylquinazolinone derivatives
MX2022006711A (es) 2019-12-10 2022-07-12 Hoffmann La Roche Nuevos inhibidores de braf como rompedores de la paradoja.
US12303509B2 (en) 2020-06-09 2025-05-20 Pfizer Inc. Compounds for the treatment of BRAF-associated diseases and disorders
JP2023554442A (ja) 2020-12-18 2023-12-27 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト 新規キナゾリノン誘導体
CN118561841A (zh) 2020-12-18 2024-08-30 豪夫迈·罗氏有限公司 新的芳基-吡啶并-嘧啶-酮衍生物
MX2023014059A (es) 2021-06-08 2024-03-12 C4 Therapeutics Inc Terapeuticos para la degradacion de una proteina quiinasa de serina/ treonina mutante.
JP2024545073A (ja) 2021-12-08 2024-12-05 アレイ バイオファーマ インコーポレイテッド Ｎ－（２－クロロ－３－（（５－クロロ－３－メチル－４－オキソ－３，４－ジヒドロキナゾリン－６－イル）アミノ）－４－フルオロフェニル）－３－フルオロアゼチジン－１－スルホンアミドの結晶形態

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HUE071148T2 (hu) 2025-08-28
IL292161A (en) 2022-06-01
US20240174621A1 (en) 2024-05-30
JP2022531609A (ja) 2022-07-07
EP4483882A3 (en) 2025-03-05
US20220298119A1 (en) 2022-09-22
IL292161B2 (en) 2025-04-01
TWI877268B (zh) 2025-03-21
WO2021116055A1 (en) 2021-06-17
RS66721B1 (sr) 2025-05-30
CR20220251A (es) 2022-07-11
CN114787156A (zh) 2022-07-22
MX2022006783A (es) 2022-07-11
ZA202206923B (en) 2024-10-30
PH12022551119A1 (en) 2023-08-23
CO2022008968A2 (es) 2022-07-19
ES3023264T3 (en) 2025-05-30
AR122351A1 (es) 2022-09-07
IL292161B1 (en) 2024-12-01
AU2020403443B2 (en) 2023-02-23
PL4073065T3 (pl) 2025-05-19
KR20220110554A (ko) 2022-08-08
ZA202204675B (en) 2022-12-21
DK4073065T3 (da) 2025-04-22
EP4073065B1 (en) 2025-02-19
PT4073065T (pt) 2025-04-15
JP7108146B2 (ja) 2022-07-27
NZ787393A (en) 2025-07-25
CN114787156B (zh) 2024-07-26
LT4073065T (lt) 2025-04-25
SI4073065T1 (sl) 2025-06-30
JP2022124458A (ja) 2022-08-25
EP4073065A1 (en) 2022-10-19
US12116349B2 (en) 2024-10-15
UA128299C2 (uk) 2024-05-29
TW202504895A (zh) 2025-02-01
TW202136245A (zh) 2021-10-01
IL316473A (en) 2024-12-01
CN118791472A (zh) 2024-10-18
CL2022001529A1 (es) 2023-02-10
AU2020403443A1 (en) 2022-05-12
BR112022011123A2 (pt) 2022-08-23
EP4483882A2 (en) 2025-01-01
FI4073065T3 (fi) 2025-04-16
KR102836833B1 (ko) 2025-07-22
PE20221778A1 (es) 2022-11-16
MA58087B1 (fr) 2025-04-30
HRP20250418T1 (hr) 2025-06-06

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