JP7451419B2 - 新規なインダゾール化合物又はその塩 - Google Patents
新規なインダゾール化合物又はその塩 Download PDFInfo
- Publication number
- JP7451419B2 JP7451419B2 JP2020552628A JP2020552628A JP7451419B2 JP 7451419 B2 JP7451419 B2 JP 7451419B2 JP 2020552628 A JP2020552628 A JP 2020552628A JP 2020552628 A JP2020552628 A JP 2020552628A JP 7451419 B2 JP7451419 B2 JP 7451419B2
- Authority
- JP
- Japan
- Prior art keywords
- group
- substituent
- methyl
- chloro
- tert
- 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
Classifications
-
- 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
- C07D403/14—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 three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- 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
- C07D405/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2018202226 | 2018-10-26 | ||
| JP2018202226 | 2018-10-26 | ||
| JP2019075118 | 2019-04-10 | ||
| JP2019075118 | 2019-04-10 | ||
| PCT/JP2019/041942 WO2020085493A1 (ja) | 2018-10-26 | 2019-10-25 | 新規なインダゾール化合物又はその塩 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JPWO2020085493A1 JPWO2020085493A1 (ja) | 2021-09-09 |
| JPWO2020085493A5 JPWO2020085493A5 (https=) | 2022-10-27 |
| JP7451419B2 true JP7451419B2 (ja) | 2024-03-18 |
Family
ID=70331140
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020552628A Active JP7451419B2 (ja) | 2018-10-26 | 2019-10-25 | 新規なインダゾール化合物又はその塩 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US12065430B2 (https=) |
| EP (1) | EP3871673B1 (https=) |
| JP (1) | JP7451419B2 (https=) |
| TW (1) | TWI831855B (https=) |
| WO (2) | WO2020085504A1 (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL312413B2 (en) | 2018-08-29 | 2026-01-01 | Acerta Pharma Bv | Processes for the preparation of 4-{8-amino-3-[(2s)-1-(but-2-enol)-pyrrolidin-2-yl]imidazo[1,5-a]-pyrazin-1-yl}n-(pyridin-2-yl)-benzamide |
| WO2020085504A1 (ja) | 2018-10-26 | 2020-04-30 | 大鵬薬品工業株式会社 | 光照射ザンドマイヤー反応を用いたクロロアゾールカルボキシレート誘導体の製造方法 |
| UA129778C2 (uk) | 2019-10-28 | 2025-07-30 | Мерк Шарп Енд Доум Елелсі | Низькомолекулярні інгібітори g12c-мутантного kras |
| EP4067343A4 (en) | 2019-11-29 | 2024-01-03 | Taiho Pharmaceutical Co., Ltd. | NEW PHENOLIC COMPOUND OR SALT THEREOF |
| WO2021215545A1 (en) * | 2020-04-24 | 2021-10-28 | Taiho Pharmaceutical Co., Ltd. | Anticancer combination therapy with n-(1-acryloyl-azetidin-3-yl)-2-((1h-indazol-3-yl)amino)methyl)-1h-imidazole-5-carboxamide inhibitor of kras-g12c |
| WO2021215544A1 (en) * | 2020-04-24 | 2021-10-28 | Taiho Pharmaceutical Co., Ltd. | Kras g12d protein inhibitors |
| EP3909950A1 (en) * | 2020-05-13 | 2021-11-17 | Basf Se | Heterocyclic compounds for the control of invertebrate pests |
| CN115551848A (zh) * | 2020-05-13 | 2022-12-30 | 巴斯夫欧洲公司 | 用于防治无脊椎动物害虫的杂环化合物 |
| CN111943879A (zh) * | 2020-08-03 | 2020-11-17 | 南通大学 | 一种(3s,4r)3-氨基-4(甲氧基甲基)吡咯烷-1-甲酸叔丁酯及其合成方法 |
| KR20240055778A (ko) | 2021-09-01 | 2024-04-29 | 노파르티스 아게 | Tead 억제제를 포함하는 제약 조합물 및 암의 치료를 위한 이의 용도 |
| EP4573095A1 (en) | 2022-08-17 | 2025-06-25 | Treeline Biosciences, Inc. | Pyridopyrimidine kras inhibitors |
| CN115260103B (zh) * | 2022-09-19 | 2023-01-17 | 苏州美诺医药科技有限公司 | 一种4,5-二卤代-1-(二氟甲基)-1h-咪唑的制备方法 |
| TW202430179A (zh) | 2022-11-21 | 2024-08-01 | 美商樹線生物科學公司 | 螺環二氫哌喃并嘧啶KRas抑制劑 |
| TW202528315A (zh) | 2023-09-21 | 2025-07-16 | 美商樹線生物科學公司 | 螺環二氫哌喃并吡啶KRas抑制劑 |
| AU2024361909A1 (en) | 2023-10-20 | 2026-03-26 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras proteins |
| WO2025245127A1 (en) | 2024-05-21 | 2025-11-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| CN120718285A (zh) * | 2025-08-14 | 2025-09-30 | 东营市黄河燃气有限责任公司 | 油气净化二氧化碳pamam接枝离子液体的制备方法 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2016519072A (ja) | 2013-03-15 | 2016-06-30 | アラクセス ファーマ エルエルシー | Krasg12cの共有結合性阻害剤 |
| JP2016532656A (ja) | 2013-10-10 | 2016-10-20 | アラクセス ファーマ エルエルシー | Krasg12cの阻害剤 |
| JP2017528498A (ja) | 2014-09-25 | 2017-09-28 | アラクセス ファーマ エルエルシー | Kras g12c変異体タンパク質のインヒビター |
| WO2018143315A1 (ja) | 2017-02-02 | 2018-08-09 | アステラス製薬株式会社 | キナゾリン化合物 |
Family Cites Families (146)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4034075A (en) | 1972-07-03 | 1977-07-05 | Allen & Hanburys Limited | Quinaldic acid derivatives |
| US6861424B2 (en) | 2001-06-06 | 2005-03-01 | Schering Aktiengesellschaft | Platelet adenosine diphosphate receptor antagonists |
| WO2005019177A1 (en) | 2003-08-14 | 2005-03-03 | Icos Corporation | Aminopiperidine amide derivatives as vla-1 integrin antagonists and uses thereof |
| US8278313B2 (en) | 2008-03-11 | 2012-10-02 | Abbott Laboratories | Macrocyclic spiro pyrimidine derivatives |
| WO2010064705A1 (ja) | 2008-12-05 | 2010-06-10 | 大日本住友製薬株式会社 | H4受容体アンタゴニスト作用を有する新規7位置換ジヒドロピラノピリミジン誘導体 |
| US20100331305A1 (en) | 2009-06-24 | 2010-12-30 | Genentech, Inc. | Oxo-heterocycle fused pyrimidine compounds, compositions and methods of use |
| AR090037A1 (es) | 2011-11-15 | 2014-10-15 | Xention Ltd | Derivados de tieno y/o furo-pirimidinas y piridinas inhibidores de los canales de potasio |
| HUE039713T2 (hu) | 2012-06-08 | 2019-02-28 | Sensorion | H4 receptor inhibitorok tinnitus kezelésére |
| JP2014111559A (ja) * | 2012-07-04 | 2014-06-19 | Nissan Chem Ind Ltd | ピラゾール誘導体および有害生物防除剤 |
| CN105189505B (zh) | 2012-09-12 | 2019-03-22 | 默克夏普&多梅有限公司 | 用作抗菌剂的三环促旋酶抑制剂 |
| WO2014164543A1 (en) | 2013-03-13 | 2014-10-09 | The Regents Of The University Of Michigan | Compositions comprising thienopyrimidine and thienopyridine compounds and methods of use thereof |
| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
| US9745319B2 (en) | 2013-03-15 | 2017-08-29 | Araxes Pharma Llc | Irreversible covalent inhibitors of the GTPase K-Ras G12C |
| DK2981963T3 (en) | 2013-04-05 | 2017-02-27 | Dolby Laboratories Licensing Corp | COMPRESSION APPARATUS AND PROCEDURE TO REDUCE QUANTIZATION NOISE USING ADVANCED SPECTRAL EXTENSION |
| JO3805B1 (ar) | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | مثبطات كراس جي12سي |
| US20160318866A1 (en) | 2013-12-19 | 2016-11-03 | Bayer Pharma Aktiengesellschaft | Substituted bipiperidinyl derivatives |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| WO2016049565A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Compositions and methods for inhibition of ras |
| WO2016049568A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Methods and compositions for inhibition of ras |
| AU2016229294B2 (en) | 2015-03-06 | 2021-11-04 | Beyondspring Pharmaceuticals, Inc. | Method of treating cancer associated with a RAS mutation |
| ES2898765T3 (es) | 2015-04-10 | 2022-03-08 | Araxes Pharma Llc | Compuestos de quinazolina sustituidos y métodos de uso de los mismos |
| US10428064B2 (en) | 2015-04-15 | 2019-10-01 | Araxes Pharma Llc | Fused-tricyclic inhibitors of KRAS and methods of use thereof |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| WO2017015562A1 (en) | 2015-07-22 | 2017-01-26 | Araxes Pharma Llc | Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins |
| EP3356349A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| EP3356347A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| EP3356351A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058902A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| WO2017058805A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| WO2017058728A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3356359B1 (en) | 2015-09-28 | 2021-10-20 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017070256A2 (en) | 2015-10-19 | 2017-04-27 | Araxes Pharma Llc | Method for screening inhibitors of ras |
| KR20180081596A (ko) | 2015-11-16 | 2018-07-16 | 아락세스 파마 엘엘씨 | 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법 |
| US9988357B2 (en) | 2015-12-09 | 2018-06-05 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| WO2017172979A1 (en) | 2016-03-30 | 2017-10-05 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| KR102444509B1 (ko) | 2016-05-18 | 2022-09-19 | 미라티 테라퓨틱스, 인크. | Kras g12c 억제제 |
| WO2018022897A1 (en) | 2016-07-27 | 2018-02-01 | Padlock Therapeutics, Inc. | Covalent inhibitors of pad4 |
| WO2018064510A1 (en) | 2016-09-29 | 2018-04-05 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3523289A1 (en) | 2016-10-07 | 2019-08-14 | Araxes Pharma LLC | Heterocyclic compounds as inhibitors of ras and methods of use thereof |
| EP3538523B1 (en) * | 2016-11-08 | 2021-05-19 | Cancer Research Technology Limited | Pyrimidinone derivatives as cdc7 inhibitors |
| CN110366550A (zh) | 2016-12-22 | 2019-10-22 | 美国安进公司 | 作为用于治疗肺癌、胰腺癌或结直肠癌的KRAS G12C抑制剂的苯并异噻唑、异噻唑并[3,4-b]吡啶、喹唑啉、酞嗪、吡啶并[2,3-d]哒嗪和吡啶并[2,3-d]嘧啶衍生物 |
| WO2018140513A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer |
| EP3573966A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused n-heterocyclic compounds and methods of use thereof |
| EP3573954A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
| US11136308B2 (en) | 2017-01-26 | 2021-10-05 | Araxes Pharma Llc | Substituted quinazoline and quinazolinone compounds and methods of use thereof |
| JP7327802B2 (ja) | 2017-01-26 | 2023-08-16 | アラクセス ファーマ エルエルシー | 縮合ヘテロ-ヘテロ二環式化合物およびその使用方法 |
| WO2018140599A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Benzothiophene and benzothiazole compounds and methods of use thereof |
| EP3621968A1 (en) | 2017-05-11 | 2020-03-18 | Astrazeneca AB | Heteroaryl compounds that inhibit g12c mutant ras proteins |
| AU2018273356B2 (en) | 2017-05-22 | 2021-09-16 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| US10745385B2 (en) | 2017-05-25 | 2020-08-18 | Araxes Pharma Llc | Covalent inhibitors of KRAS |
| CN110869357A (zh) | 2017-05-25 | 2020-03-06 | 亚瑞克西斯制药公司 | 化合物及其用于治疗癌症的使用方法 |
| WO2018218069A1 (en) | 2017-05-25 | 2018-11-29 | Araxes Pharma Llc | Quinazoline derivatives as modulators of mutant kras, hras or nras |
| CN107556289A (zh) | 2017-06-22 | 2018-01-09 | 天津国际生物医药联合研究院 | 一种氯苯‑吡啶类化合物及其应用 |
| AU2018329920B2 (en) | 2017-09-08 | 2022-12-01 | Amgen Inc. | Inhibitors of KRAS G12C and methods of using the same |
| RU2764243C2 (ru) | 2017-09-22 | 2022-01-14 | ДЖУБИЛАНТ ЭПИПЭД ЭлЭлСи | Гетероциклические соединения в качестве ингибиторов PAD |
| GB201715342D0 (en) | 2017-09-22 | 2017-11-08 | Univ Nottingham | Compounds |
| CN109670389B (zh) | 2017-10-16 | 2023-04-07 | 富士通株式会社 | 评价人脸图像中的光照条件的方法和设备 |
| AU2018352142B2 (en) | 2017-10-18 | 2022-08-25 | Jubilant Epipad LLC | Imidazo-pyridine compounds as PAD inhibitors |
| US10647715B2 (en) | 2017-11-15 | 2020-05-12 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| LT3710439T (lt) | 2017-11-15 | 2023-05-10 | Mirati Therapeutics, Inc. | Kras g12c inhibitoriai |
| WO2019099703A1 (en) | 2017-11-16 | 2019-05-23 | Sidecar Therapeutics, Inc. | Apoptosis signal-regulating kinase 1 (ask 1) inhibitor compounds |
| US10597405B2 (en) | 2017-12-08 | 2020-03-24 | Astrazeneca Ab | Chemical compounds |
| TW201942116A (zh) | 2018-02-09 | 2019-11-01 | 美商輝瑞股份有限公司 | 作為抗癌劑之四氫喹唑啉衍生物 |
| IL276232B2 (en) | 2018-03-02 | 2024-04-01 | Otsuka Pharma Co Ltd | Pyrazine derivatives, pharmaceutical compositions comprising them and their use for treating diseases |
| WO2019185525A1 (en) | 2018-03-28 | 2019-10-03 | Bayer Pharma Aktiengesellschaft | 4-(3-amino-6-fluoro-1h-indazol-5-yl)-1,2,6-trimethyl-1,4-dihydropyridine-3,5-dic arbonitrile compounds for treating hyperproliferative disorders |
| CA3098574A1 (en) | 2018-05-04 | 2019-11-07 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| TW202012415A (zh) | 2018-05-08 | 2020-04-01 | 瑞典商阿斯特捷利康公司 | 化學化合物 |
| US11285156B2 (en) | 2018-06-12 | 2022-03-29 | Amgen Inc. | Substituted piperazines as KRAS G12C inhibitors |
| AU2019320945C1 (en) | 2018-08-16 | 2021-09-30 | F. Hoffmann-La Roche Ag | Fused ring compounds |
| JP6648797B2 (ja) | 2018-10-04 | 2020-02-14 | 株式会社三洋物産 | 遊技機 |
| TW202033518A (zh) | 2018-10-15 | 2020-09-16 | 美商美國禮來大藥廠 | Kras g12c 抑制劑 |
| WO2020085504A1 (ja) | 2018-10-26 | 2020-04-30 | 大鵬薬品工業株式会社 | 光照射ザンドマイヤー反応を用いたクロロアゾールカルボキシレート誘導体の製造方法 |
| PE20260440A1 (es) | 2018-11-09 | 2026-02-19 | Hoffmann La Roche | Compuestos de anillo fusionado |
| AU2019384118B2 (en) | 2018-11-19 | 2025-06-12 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| EP3887373A1 (en) | 2018-11-29 | 2021-10-06 | Araxes Pharma LLC | Compounds and methods of use thereof for treatment of cancer |
| EP3908283A4 (en) | 2019-01-10 | 2022-10-12 | Mirati Therapeutics, Inc. | KRAS G12C INHIBITORS |
| EP3919483A4 (en) | 2019-01-29 | 2022-02-09 | Brightgene Bio-medical Technology Co., Ltd. | HETEROCYCLIC BENZOPYRIDONE COMPOUND AND USE THEREOF |
| WO2020177629A1 (zh) | 2019-03-01 | 2020-09-10 | 劲方医药科技(上海)有限公司 | 螺环取代的嘧啶并环类化合物,其制法与医药上的用途 |
| KR102934231B1 (ko) | 2019-03-05 | 2026-03-06 | 아스트라제네카 아베 | 항암제로 유용한 융합 삼환식 화합물 |
| KR20220012255A (ko) | 2019-04-28 | 2022-02-03 | 젠플리트 테라퓨틱스 (상하이) 아이엔씨. | 옥사아자퀴나졸린-7(8h)-케톤 화합물, 이의 제조 방법 및 이의 약학적 응용 |
| JP7502337B2 (ja) | 2019-05-20 | 2024-06-18 | カリフォルニア インスティチュート オブ テクノロジー | Kras g12cインヒビター及びその使用 |
| WO2020234103A1 (en) | 2019-05-21 | 2020-11-26 | Bayer Aktiengesellschaft | Identification and use of kras inhibitors |
| CN114437065A (zh) | 2019-05-21 | 2022-05-06 | 益方生物科技(上海)股份有限公司 | 杂环化合物,其制备方法和用途 |
| TW202110837A (zh) | 2019-05-24 | 2021-03-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 氫化吡啶并嘧啶類衍生物、其製備方法及其在醫藥上的應用 |
| WO2020239077A1 (zh) | 2019-05-29 | 2020-12-03 | 上海翰森生物医药科技有限公司 | 含氮杂环类衍生物调节剂、其制备方法和应用 |
| CN113396147B (zh) | 2019-05-31 | 2024-06-18 | 上海翰森生物医药科技有限公司 | 芳香杂环类衍生物调节剂、其制备方法和应用 |
| PH12021553058A1 (en) | 2019-06-06 | 2022-07-25 | Hutchison Medipharma Ltd | Tricyclic compounds and their use |
| AU2020308353B9 (en) | 2019-06-24 | 2024-01-25 | Guangdong Newopp Biopharmaceuticals Co., Ltd. | Heterocyclic compounds as inhibitors of KRAS G12C |
| US12421236B2 (en) | 2019-06-25 | 2025-09-23 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Seven-membered heterocyclic derivative acting as KRAS G12C mutant protein inhibitor |
| CN110256421A (zh) | 2019-06-26 | 2019-09-20 | 微境生物医药科技(上海)有限公司 | Kras-g12c抑制剂 |
| WO2021000885A1 (zh) | 2019-07-01 | 2021-01-07 | 江苏恒瑞医药股份有限公司 | 喹唑啉酮类衍生物、其制备方法及其在医药上的应用 |
| JP7756069B6 (ja) | 2019-08-02 | 2025-11-27 | 上海済▲ユウ▼医薬科技股▲フン▼有限公司 | 四環式化合物、その調製と使用の方法 |
| CN112341457A (zh) | 2019-08-07 | 2021-02-09 | 北京加科思新药研发有限公司 | Kras突变蛋白抑制剂 |
| CN114174298B (zh) | 2019-08-14 | 2023-08-01 | 正大天晴药业集团南京顺欣制药有限公司 | 哒嗪酮并嘧啶类衍生物及其医药用途 |
| CN112390797A (zh) | 2019-08-15 | 2021-02-23 | 微境生物医药科技(上海)有限公司 | 新型螺环类K-Ras G12C抑制剂 |
| WO2021031952A1 (zh) | 2019-08-16 | 2021-02-25 | 劲方医药科技(上海)有限公司 | 氧代六元环并嘧啶类化合物,其制法与医药上的用途 |
| CN114269735B (zh) | 2019-08-26 | 2024-02-23 | 南京创济生物医药有限公司 | 二氢或四氢喹唑啉类化合物及其中间体、制备方法和应用 |
| CN112430234B (zh) | 2019-08-26 | 2023-04-28 | 信达生物制药(苏州)有限公司 | 一种新型kras g12c蛋白抑制剂及其制备方法和用途 |
| MX2022002465A (es) | 2019-08-29 | 2022-05-19 | Mirati Therapeutics Inc | Inhibidores de kras g12d. |
| WO2021043322A1 (zh) | 2019-09-06 | 2021-03-11 | 正大天晴药业集团南京顺欣制药有限公司 | 氮杂环庚烷并嘧啶类衍生物及其医药用途 |
| US20220402916A1 (en) | 2019-09-18 | 2022-12-22 | Merck Sharp & Dohme Corp. | Small molecule inhibitors of kras g12c mutant |
| WO2021052499A1 (zh) | 2019-09-20 | 2021-03-25 | 上海济煜医药科技有限公司 | 稠合吡啶酮类化合物及其制备方法和应用 |
| TW202115062A (zh) | 2019-09-25 | 2021-04-16 | 大陸商北京加科思新藥研發有限公司 | Kras突變蛋白抑制劑 |
| WO2021058018A1 (en) | 2019-09-29 | 2021-04-01 | Beigene, Ltd. | Inhibitors of kras g12c |
| WO2021063346A1 (zh) | 2019-09-30 | 2021-04-08 | 上海迪诺医药科技有限公司 | Kras g12c抑制剂及其应用 |
| CN112694475B (zh) | 2019-10-23 | 2025-09-23 | 苏州泽璟生物制药股份有限公司 | 环烷基类和杂环烷基类抑制剂及其制备方法和应用 |
| EP4048671B1 (en) | 2019-10-24 | 2026-03-18 | Amgen Inc. | Pyridopyrimidine derivatives useful as kras g12c and kras g12d inhibitors in the treatment of cancer |
| UA129778C2 (uk) | 2019-10-28 | 2025-07-30 | Мерк Шарп Енд Доум Елелсі | Низькомолекулярні інгібітори g12c-мутантного kras |
| CN114585610A (zh) | 2019-10-28 | 2022-06-03 | 日本曹达株式会社 | 2,6-二氧代-3,6-二氢嘧啶化合物以及农业园艺用杀菌剂、杀线虫剂、及医疗用·动物用抗真菌剂 |
| JP7601869B2 (ja) | 2019-10-30 | 2024-12-17 | ▲勁▼方医▲薬▼科技(上海)有限公司 | 置換された複素環-環系化合物、その調製方法及び医薬への応用 |
| WO2021084765A1 (en) | 2019-10-31 | 2021-05-06 | Taiho Pharmaceutical Co., Ltd | 4-aminobut-2-enamide derivatives and salts thereof |
| US20230023023A1 (en) | 2019-10-31 | 2023-01-26 | Taiho Pharmaceutical Co., Ltd. | 4-aminobut-2-enamide derivatives and salts thereof |
| CN113286794B (zh) | 2019-11-04 | 2024-03-12 | 北京加科思新药研发有限公司 | Kras突变蛋白抑制剂 |
| CN114630832A (zh) | 2019-11-15 | 2022-06-14 | 四川海思科制药有限公司 | 一种嘧啶并环衍生物及其在医药上的应用 |
| CN112824410A (zh) | 2019-11-21 | 2021-05-21 | 苏州泽璟生物制药股份有限公司 | 氮杂七元环类抑制剂及其制备方法和应用 |
| CN113614080B (zh) | 2019-11-29 | 2022-06-28 | 苏州信诺维医药科技股份有限公司 | Kras g12c抑制剂化合物及其用途 |
| WO2021106231A1 (en) | 2019-11-29 | 2021-06-03 | Taiho Pharmaceutical Co., Ltd. | A compound having inhibitory activity against kras g12d mutation |
| EP4067343A4 (en) | 2019-11-29 | 2024-01-03 | Taiho Pharmaceutical Co., Ltd. | NEW PHENOLIC COMPOUND OR SALT THEREOF |
| WO2021109737A1 (zh) | 2019-12-02 | 2021-06-10 | 上海璎黎药业有限公司 | 一种含氧杂环化合物、其制备方法及应用 |
| WO2021113595A1 (en) | 2019-12-06 | 2021-06-10 | Beta Pharma, Inc. | Phosphorus derivatives as kras inhibitors |
| PT3886991T (pt) | 2019-12-11 | 2022-10-17 | Lilly Co Eli | Inibidores de kras g12c |
| WO2021120045A1 (en) | 2019-12-18 | 2021-06-24 | InventisBio Co., Ltd. | Heterocyclic compounds, preparation methods and uses thereof |
| CN114761408B (zh) | 2019-12-19 | 2023-09-15 | 贝达药业股份有限公司 | Kras g12c抑制剂及其在医药上的应用 |
| IL293962B2 (en) | 2019-12-19 | 2025-10-01 | Jacobio Pharmaceuticals Co Ltd | Mutant KRAS protein inhibitors |
| CA3164995A1 (en) | 2019-12-20 | 2021-06-24 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| WO2021120890A1 (en) | 2019-12-20 | 2021-06-24 | Novartis Ag | Pyrazolyl derivatives useful as anti-cancer agents |
| CN113045565A (zh) | 2019-12-27 | 2021-06-29 | 微境生物医药科技(上海)有限公司 | 新型K-Ras G12C抑制剂 |
| CN115003668A (zh) | 2020-01-21 | 2022-09-02 | 南京明德新药研发有限公司 | 作为kras抑制剂的大环类化合物 |
| WO2021215544A1 (en) | 2020-04-24 | 2021-10-28 | Taiho Pharmaceutical Co., Ltd. | Kras g12d protein inhibitors |
| WO2021215545A1 (en) | 2020-04-24 | 2021-10-28 | Taiho Pharmaceutical Co., Ltd. | Anticancer combination therapy with n-(1-acryloyl-azetidin-3-yl)-2-((1h-indazol-3-yl)amino)methyl)-1h-imidazole-5-carboxamide inhibitor of kras-g12c |
| WO2021219072A1 (zh) | 2020-04-30 | 2021-11-04 | 上海科州药物研发有限公司 | 作为kras抑制剂的杂环化合物的制备及其应用方法 |
| US20230357277A1 (en) | 2020-09-22 | 2023-11-09 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| EP4247807A4 (en) | 2020-11-23 | 2024-10-16 | Merck Sharp & Dohme LLC | 6,7-DIHYDRO-PYRANO[2,3-D PYRIMIDINE AS INHIBITORS OF THE KRAS G12C MUTANT |
| US20240124478A1 (en) | 2020-11-23 | 2024-04-18 | Merck Sharp & Dohme Llc | SPIROCYCLIC-SUBSTITUTED 6,7-DIHYDRO-PYRANO[2,3-d]PYRIMIDINE INHIBITORS OF KRAS G12C MUTANT |
| JP2023553492A (ja) | 2020-12-15 | 2023-12-21 | ミラティ セラピューティクス, インコーポレイテッド | アザキナゾリン汎KRas阻害剤 |
| EP4262803A4 (en) | 2020-12-16 | 2025-03-12 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-kras inhibitors |
| EP4291199A4 (en) | 2021-02-09 | 2025-06-18 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| BR112023016299A2 (pt) | 2021-02-16 | 2023-11-28 | L Livermore Nat Security Llc | Composições e métodos para inibir kras |
| EP4322954A4 (en) | 2021-04-16 | 2025-01-29 | Merck Sharp & Dohme LLC | SMALL MOLECULAR INHIBITORS OF THE KRAS G12D MUTANT |
| US20240262842A1 (en) | 2021-04-27 | 2024-08-08 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras g12c mutant |
| US20240246968A1 (en) | 2021-04-27 | 2024-07-25 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras g12c mutant |
| EP4347606A4 (en) | 2021-05-28 | 2025-04-02 | Merck Sharp & Dohme LLC | SMALL MOLECULES INHIBITING THE G12C KRAS MUTANT |
| EP4347041A1 (en) | 2021-05-28 | 2024-04-10 | Taiho Pharmaceutical Co., Ltd. | Small molecule inhibitors of kras mutated proteins |
| WO2022256459A1 (en) | 2021-06-01 | 2022-12-08 | Quanta Therapeutics, Inc. | Kras modulators and uses thereof |
| EP4436571A4 (en) | 2021-11-24 | 2025-10-15 | Merck Sharp & Dohme Llc | SMALL MOLECULE INHIBITORS OF KRAS MUTATIONAL PROTEINS |
| US20260083750A1 (en) | 2022-08-26 | 2026-03-26 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras proteins |
-
2019
- 2019-10-25 WO PCT/JP2019/042005 patent/WO2020085504A1/ja not_active Ceased
- 2019-10-25 EP EP19874827.9A patent/EP3871673B1/en active Active
- 2019-10-25 WO PCT/JP2019/041942 patent/WO2020085493A1/ja not_active Ceased
- 2019-10-25 JP JP2020552628A patent/JP7451419B2/ja active Active
- 2019-10-25 US US17/288,780 patent/US12065430B2/en active Active
- 2019-10-25 TW TW108138686A patent/TWI831855B/zh active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2016519072A (ja) | 2013-03-15 | 2016-06-30 | アラクセス ファーマ エルエルシー | Krasg12cの共有結合性阻害剤 |
| JP2016532656A (ja) | 2013-10-10 | 2016-10-20 | アラクセス ファーマ エルエルシー | Krasg12cの阻害剤 |
| JP2017528498A (ja) | 2014-09-25 | 2017-09-28 | アラクセス ファーマ エルエルシー | Kras g12c変異体タンパク質のインヒビター |
| WO2018143315A1 (ja) | 2017-02-02 | 2018-08-09 | アステラス製薬株式会社 | キナゾリン化合物 |
Non-Patent Citations (3)
| Title |
|---|
| CHUANG, H. et al.,Pharmacological strategies to target oncogenic KRAS signaling in pancreatic cancer,Pharmacological Research,2017年,117,pp. 370-376 |
| JANES, M. R. et al.,Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor,Cell,2018年01月25日,172(3),pp. 578-589,https://doi.org/10.1016/j.cell.2018.01.006 |
| PATRICELLI, M. P. et al.,Selective Inhibition of Oncogenic KRAS Output with Small Molecules Targeting the Inactive State,CANCER DISCOVERY,2016年,6(3),pp. 316-329,http://cancerdiscovery.aacrjournals.org/content/6/3/316 |
Also Published As
| Publication number | Publication date |
|---|---|
| TWI831855B (zh) | 2024-02-11 |
| WO2020085504A1 (ja) | 2020-04-30 |
| US20210395234A1 (en) | 2021-12-23 |
| EP3871673A4 (en) | 2022-06-22 |
| EP3871673A1 (en) | 2021-09-01 |
| TW202029960A (zh) | 2020-08-16 |
| EP3871673B1 (en) | 2024-01-03 |
| US12065430B2 (en) | 2024-08-20 |
| WO2020085493A1 (ja) | 2020-04-30 |
| JPWO2020085493A1 (ja) | 2021-09-09 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP7451419B2 (ja) | 新規なインダゾール化合物又はその塩 | |
| US20230181536A1 (en) | Anticancer combination therapy with n-(1-acryloyl-azetidin-3-yl)-2-((1h-indazol-3-yl)amino)methyl)-1h-imidazole-5-carboxamide inhibitor of kras-g12c | |
| JP6918838B2 (ja) | 第三級アミド基を有するベンズアゼピンジカルボキサミド化合物 | |
| JP6549703B2 (ja) | 新規化合物 | |
| JP4632544B2 (ja) | アミノピラゾール誘導体 | |
| KR101953272B1 (ko) | 키나제 억제제로서 활성인 치환된 인다졸 유도체 | |
| AU2009245715B2 (en) | Trisubstituted pyrazoles as acetylcholine receptor modulators | |
| WO2021106230A1 (ja) | 新規なフェノール化合物又はその塩 | |
| TWI802591B (zh) | 具有環狀構造的化合物 | |
| JP5938038B2 (ja) | ピラゾロフェニル−ベンゼンスルホンアミド化合物の誘導体及びその抗腫瘍薬としての使用 | |
| JP5653842B2 (ja) | レニン阻害剤としての3,4−置換ピペリジン誘導体 | |
| EP2746265A1 (en) | Heterocyclic derivative and pharmaceutical drug | |
| EA019041B1 (ru) | Карбазолкарбоксамидные соединения, применимые в качестве ингибиторов киназы | |
| JP2007509917A (ja) | グルコキナーゼ調節剤としてのピリジンカルボン酸誘導体 | |
| KR20130097776A (ko) | 사이클로프로판 화합물 | |
| KR20110059778A (ko) | H-pgds 억제제로서 다중헤테로아릴 화합물 및 프로스타글란딘 d2 매개된 질병의 치료를 위한 그의 용도 | |
| EA034201B1 (ru) | Соединения в качестве модуляторов ror-гамма | |
| WO2012133607A1 (ja) | ピラゾール化合物 | |
| IL263793B2 (en) | Compounds and preparations for the treatment of cancer | |
| AU2016297037B9 (en) | Nitrogen-containing heterocyclic compound | |
| EP4240738B1 (en) | Pyrazole derivatives as ret kinase inhibitors | |
| WO2002092593A1 (fr) | Derives de 4-(4-pyridazinyl)pyrazole |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20221019 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20221019 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20231031 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20231225 |
|
| 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: 20240206 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20240306 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 7451419 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |