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 PDFInfo
- Publication number
- 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
- Authority
- JP
- Japan
- Prior art keywords
- compound
- formula
- cancer
- braf
- compounds
- 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.)
- Active
Links
Images
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
- 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
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)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021202780A Division JP7802514B2 (ja) | 2019-12-10 | 2021-12-14 | 新規メチルキナゾリノン誘導体 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2022531609A JP2022531609A (ja) | 2022-07-07 |
| JP7108146B2 true JP7108146B2 (ja) | 2022-07-27 |
Family
ID=68848113
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021566023A Active JP7108146B2 (ja) | 2019-12-10 | 2020-12-08 | 新規メチルキナゾリノン誘導体 |
| JP2021202780A Active JP7802514B2 (ja) | 2019-12-10 | 2021-12-14 | 新規メチルキナゾリノン誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021202780A Active JP7802514B2 (ja) | 2019-12-10 | 2021-12-14 | 新規メチルキナゾリノン誘導体 |
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=) |
Cited By (2)
| 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 |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Family Cites Families (21)
| 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 |
| 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 |
-
2020
- 2020-12-08 PH PH1/2022/551119A patent/PH12022551119A1/en unknown
- 2020-12-08 KR KR1020227023074A patent/KR102836833B1/ko active Active
- 2020-12-08 RS RS20250354A patent/RS66721B1/sr unknown
- 2020-12-08 CN CN202080084994.3A patent/CN114787156B/zh active Active
- 2020-12-08 FI FIEP20817377.3T patent/FI4073065T3/fi active
- 2020-12-08 WO PCT/EP2020/084976 patent/WO2021116055A1/en not_active Ceased
- 2020-12-08 LT LTEPPCT/EP2020/084976T patent/LT4073065T/lt unknown
- 2020-12-08 MX MX2022006783A patent/MX2022006783A/es unknown
- 2020-12-08 MA MA58087A patent/MA58087B1/fr unknown
- 2020-12-08 HR HRP20250418TT patent/HRP20250418T1/hr unknown
- 2020-12-08 DK DK20817377.3T patent/DK4073065T3/da active
- 2020-12-08 IL IL316473A patent/IL316473A/en unknown
- 2020-12-08 CR CR20220251A patent/CR20220251A/es unknown
- 2020-12-08 ES ES20817377T patent/ES3023264T3/es active Active
- 2020-12-08 AU AU2020403443A patent/AU2020403443B2/en active Active
- 2020-12-08 UA UAA202202163A patent/UA128299C2/uk unknown
- 2020-12-08 JP JP2021566023A patent/JP7108146B2/ja active Active
- 2020-12-08 SI SI202030605T patent/SI4073065T1/sl unknown
- 2020-12-08 HU HUE20817377A patent/HUE071148T2/hu unknown
- 2020-12-08 IL IL292161A patent/IL292161B2/en unknown
- 2020-12-08 EP EP24205932.7A patent/EP4483882A3/en active Pending
- 2020-12-08 PT PT208173773T patent/PT4073065T/pt unknown
- 2020-12-08 PE PE2022000853A patent/PE20221778A1/es unknown
- 2020-12-08 EP EP20817377.3A patent/EP4073065B1/en active Active
- 2020-12-08 CN CN202410878222.7A patent/CN118791472A/zh active Pending
- 2020-12-08 PL PL20817377.3T patent/PL4073065T3/pl unknown
- 2020-12-09 TW TW109143500A patent/TWI877268B/zh active
- 2020-12-09 TW TW113139852A patent/TWI908405B/zh active
- 2020-12-09 AR ARP200103417A patent/AR122351A1/es unknown
-
2021
- 2021-12-14 JP JP2021202780A patent/JP7802514B2/ja active Active
-
2022
- 2022-04-26 ZA ZA2022/04675A patent/ZA202204675B/en unknown
- 2022-06-08 US US17/835,245 patent/US12116349B2/en active Active
- 2022-06-09 CL CL2022001529A patent/CL2022001529A1/es unknown
- 2022-06-22 ZA ZA2022/06923A patent/ZA202206923B/en unknown
- 2022-06-28 CO CONC2022/0008968A patent/CO2022008968A2/es unknown
-
2023
- 2023-11-30 US US18/525,536 patent/US20240174621A1/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Non-Patent Citations (1)
| Title |
|---|
| Bioorganic & Medicinal Chemistry Letters,2014年,Vol.24, No.8,p.1923-1927 |
Cited By (4)
| 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 |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP7108146B2 (ja) | 新規メチルキナゾリノン誘導体 | |
| CN113966335B (zh) | 用于治疗癌症的egfr抑制剂 | |
| CN113993590B (zh) | 新型egfr抑制剂 | |
| JP7737991B2 (ja) | Egfr阻害剤 | |
| CA3162883C (en) | (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 | |
| RU2802968C1 (ru) | Новые производные метилхиназолинона | |
| HK40074142A (en) | New methylquinazolinone derivatives | |
| RU2818677C2 (ru) | Ингибитор egfr для лечения рака | |
| HK40113036A (zh) | 新颖甲基喹唑啉酮衍生物 | |
| HK40074142B (zh) | 新颖甲基喹唑啉酮衍生物 | |
| BR112022011123B1 (pt) | Composto, processo para a preparação de um composto, composição farmacêutica e uso de um composto | |
| HK40063822A (en) | Egfr inhibitor for the treatment of cancer | |
| HK40079554A (en) | Egfr inhibitors |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A524 | Written submission of copy of amendment under article 19 pct |
Free format text: JAPANESE INTERMEDIATE CODE: A524 Effective date: 20211214 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20211214 |
|
| A871 | Explanation of circumstances concerning accelerated examination |
Free format text: JAPANESE INTERMEDIATE CODE: A871 Effective date: 20211214 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20220712 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20220714 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 7108146 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |