AU2020403443B2 - New methylquinazolinone derivatives - Google Patents

New methylquinazolinone derivatives Download PDF

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Publication number
AU2020403443B2
AU2020403443B2 AU2020403443A AU2020403443A AU2020403443B2 AU 2020403443 B2 AU2020403443 B2 AU 2020403443B2 AU 2020403443 A AU2020403443 A AU 2020403443A AU 2020403443 A AU2020403443 A AU 2020403443A AU 2020403443 B2 AU2020403443 B2 AU 2020403443B2
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AU
Australia
Prior art keywords
compound
formula
cancer
treatment
braf
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AU2020403443A
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AU2020403443A1 (en
Inventor
Cosimo Dolente
David Stephen HEWINGS
Daniel Hunziker
Daniela Krummenacher
Piergiorgio Francesco Tommaso PETTAZZONI
Juergen Wichmann
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88Oxygen atoms
    • 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • 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
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/46Heterocyclic 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
    • C07D207/48Sulfur atoms

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  • 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)
AU2020403443A 2019-12-10 2020-12-08 New methylquinazolinone derivatives Active AU2020403443B2 (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 (2)

Publication Number Publication Date
AU2020403443A1 AU2020403443A1 (en) 2022-05-12
AU2020403443B2 true AU2020403443B2 (en) 2023-02-23

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ID=68848113

Family Applications (1)

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AU2020403443A Active AU2020403443B2 (en) 2019-12-10 2020-12-08 New methylquinazolinone derivatives

Country Status (29)

Country Link
US (2) US12116349B2 (https=)
EP (2) EP4483882A3 (https=)
JP (2) JP7108146B2 (https=)
KR (1) KR102836833B1 (https=)
CN (2) CN114787156B (https=)
AR (1) AR122351A1 (https=)
AU (1) AU2020403443B2 (https=)
CL (1) CL2022001529A1 (https=)
CO (1) CO2022008968A2 (https=)
CR (1) CR20220251A (https=)
DK (1) DK4073065T3 (https=)
ES (1) ES3023264T3 (https=)
FI (1) FI4073065T3 (https=)
HR (1) HRP20250418T1 (https=)
HU (1) HUE071148T2 (https=)
IL (2) IL316473A (https=)
LT (1) LT4073065T (https=)
MA (1) MA58087B1 (https=)
MX (1) MX2022006783A (https=)
PE (1) PE20221778A1 (https=)
PH (1) PH12022551119A1 (https=)
PL (1) PL4073065T3 (https=)
PT (1) PT4073065T (https=)
RS (1) RS66721B1 (https=)
SI (1) SI4073065T1 (https=)
TW (2) TWI877268B (https=)
UA (1) UA128299C2 (https=)
WO (1) WO2021116055A1 (https=)
ZA (2) ZA202204675B (https=)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2020403082A1 (en) * 2019-12-10 2022-05-12 F. Hoffmann-La Roche Ag New BRAF inhibitors as paradox breakers
PH12022551119A1 (en) 2019-12-10 2023-08-23 Hoffmann La Roche New methylquinazolinone derivatives
TW202426436A (zh) 2020-06-09 2024-07-01 美商艾瑞生藥股份有限公司 用於治療braf相關的疾病和病症之化合物
MX2023014059A (es) 2021-06-08 2024-03-12 C4 Therapeutics Inc Terapeuticos para la degradacion de una proteina quiinasa de serina/ treonina mutante.
IL307964A (en) * 2021-06-09 2023-12-01 Chugai Pharmaceutical Co Ltd Combined treatment for 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
MX2023014629A (es) * 2021-06-09 2024-01-30 Hoffmann La Roche Nuevas formas solidas de (3r)-n-[2-ciano-4-fluoro-3-(3-metil-4-oxo -quinazolin-6-il)oxi-fenil]-3-fluoro-pirrolidin-1-sulfonamida.
KR20240041917A (ko) 2021-07-27 2024-04-01 도레이 카부시키가이샤 암의 치료 및/또는 예방을 위한 의약품
EP4426305A1 (en) 2021-11-04 2024-09-11 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
WO2024126660A1 (en) * 2022-12-15 2024-06-20 F. Hoffmann-La Roche Ag Combination therapy for cancer treatment
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
KR20260032991A (ko) 2023-07-04 2026-03-10 에프. 호프만-라 로슈 아게 (3r)-n-[2-시아노-4-플루오로-3-(3-메틸-4-옥소-퀴나졸린-6-일)옥시-페닐]-3-플루오로-피롤리딘-1-설폰아미드의신규 고체 형태
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
TW202545530A (zh) * 2024-01-17 2025-12-01 大陸商海思科醫藥集團股份有限公司 含braf抑制劑的藥物組合物及其在醫藥上的應用
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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012118492A1 (en) * 2011-03-01 2012-09-07 Array Biopharma Inc. Heterocyclic sulfonamides as raf inhibitors

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
GB0525068D0 (en) 2005-12-08 2006-01-18 Novartis Ag Organic compounds
GB0525069D0 (en) 2005-12-08 2006-01-18 Novartis Ag Organic compounds
WO2009012283A1 (en) 2007-07-17 2009-01-22 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
EP3147281A1 (en) 2008-03-17 2017-03-29 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
AU2013318283A1 (en) 2012-09-19 2015-03-05 Novartis Ag Dihydropyrrolidino-pyrimidines as kinase inhibitors
CN105228983A (zh) 2013-05-30 2016-01-06 普莱希科公司 用于激酶调节的化合物及其适应症
US9814714B2 (en) 2015-05-22 2017-11-14 Plexxikon Inc. Kinase modulation, and indications therefor
RU2724345C2 (ru) 2015-10-09 2020-06-23 Галапагос Нв N-СУЛЬФОНИЛИРОВАННЫЕ ПИРАЗОЛО[3,4-b]ПИРИДИН-6-КАРБОКСАМИДЫ И СПОСОБ ИХ ПРИМЕНЕНИЯ
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
WO2020142612A1 (en) 2019-01-03 2020-07-09 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
AU2020403082A1 (en) * 2019-12-10 2022-05-12 F. Hoffmann-La Roche Ag New BRAF inhibitors as paradox breakers
PH12022551119A1 (en) 2019-12-10 2023-08-23 Hoffmann La Roche New methylquinazolinone derivatives
TW202426436A (zh) 2020-06-09 2024-07-01 美商艾瑞生藥股份有限公司 用於治療braf相關的疾病和病症之化合物
WO2022129259A1 (en) 2020-12-18 2022-06-23 F. Hoffmann-La Roche Ag New quinazolinone derivatives
JP2023554062A (ja) 2020-12-18 2023-12-26 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト 新規アリール-ピリド-ピリミジン-オン誘導体
MX2023014059A (es) 2021-06-08 2024-03-12 C4 Therapeutics Inc Terapeuticos para la degradacion de una proteina quiinasa de serina/ treonina mutante.
US20250011304A1 (en) 2021-12-08 2025-01-09 Array Biopharma Inc. Crystalline form of n-(2-chloro-3-((5-chloro-3-methyl-4-oxo-3,4-dihydroquinazolin-6-yl)amino)-4-fluorophenyl)-3-fluoroazetidine-1-sulfonamide

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012118492A1 (en) * 2011-03-01 2012-09-07 Array Biopharma Inc. Heterocyclic sulfonamides as raf inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
WENGLOWSKY STEVE; REN LI; GRINA JONAS; HANSEN JOSHUA D.; LAIRD ELLEN R.; MORENO DAVID; DINKEL VICTORIA; GLOOR SUSAN L.; HASTINGS G: "Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-RafV600Ekinase", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ELSEVIER, AMSTERDAM NL, vol. 24, no. 8, 13 March 2014 (2014-03-13), Amsterdam NL , pages 1923 - 1927, XP028841756, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2014.03.007 *

Also Published As

Publication number Publication date
UA128299C2 (uk) 2024-05-29
JP7108146B2 (ja) 2022-07-27
BR112022011123A2 (pt) 2022-08-23
EP4483882A2 (en) 2025-01-01
FI4073065T3 (fi) 2025-04-16
KR102836833B1 (ko) 2025-07-22
SI4073065T1 (sl) 2025-06-30
PL4073065T3 (pl) 2025-05-19
PT4073065T (pt) 2025-04-15
JP2022531609A (ja) 2022-07-07
AR122351A1 (es) 2022-09-07
US20240174621A1 (en) 2024-05-30
MA58087B1 (fr) 2025-04-30
DK4073065T3 (da) 2025-04-22
PH12022551119A1 (en) 2023-08-23
WO2021116055A1 (en) 2021-06-17
JP2022124458A (ja) 2022-08-25
RS66721B1 (sr) 2025-05-30
TWI877268B (zh) 2025-03-21
US20220298119A1 (en) 2022-09-22
AU2020403443A1 (en) 2022-05-12
CA3162883A1 (en) 2021-06-17
HRP20250418T1 (hr) 2025-06-06
CN118791472A (zh) 2024-10-18
PE20221778A1 (es) 2022-11-16
CL2022001529A1 (es) 2023-02-10
JP7802514B2 (ja) 2026-01-20
TWI908405B (zh) 2025-12-11
CN114787156A (zh) 2022-07-22
ZA202204675B (en) 2022-12-21
IL316473A (en) 2024-12-01
TW202504895A (zh) 2025-02-01
KR20220110554A (ko) 2022-08-08
CO2022008968A2 (es) 2022-07-19
US12116349B2 (en) 2024-10-15
EP4073065B1 (en) 2025-02-19
LT4073065T (lt) 2025-04-25
MX2022006783A (es) 2022-07-11
EP4073065A1 (en) 2022-10-19
TW202136245A (zh) 2021-10-01
CR20220251A (es) 2022-07-11
CN114787156B (zh) 2024-07-26
ZA202206923B (en) 2024-10-30
ES3023264T3 (en) 2025-05-30
IL292161B2 (en) 2025-04-01
NZ787393A (en) 2025-07-25
IL292161B1 (en) 2024-12-01
HUE071148T2 (hu) 2025-08-28
IL292161A (en) 2022-06-01
EP4483882A3 (en) 2025-03-05

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