CA3239343A1 - Quinazoline pan-kras inhibitors - Google Patents
Quinazoline pan-kras inhibitors Download PDFInfo
- Publication number
- CA3239343A1 CA3239343A1 CA3239343A CA3239343A CA3239343A1 CA 3239343 A1 CA3239343 A1 CA 3239343A1 CA 3239343 A CA3239343 A CA 3239343A CA 3239343 A CA3239343 A CA 3239343A CA 3239343 A1 CA3239343 A1 CA 3239343A1
- Authority
- CA
- Canada
- Prior art keywords
- kras
- alkyl
- equiv
- compound
- fluoro
- 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
Links
Classifications
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
-
- 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
- C07D471/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (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)
Applications Claiming Priority (13)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202263306271P | 2022-02-03 | 2022-02-03 | |
| US63/306,271 | 2022-02-03 | ||
| US202263327625P | 2022-04-05 | 2022-04-05 | |
| US63/327,625 | 2022-04-05 | ||
| US202263352180P | 2022-06-14 | 2022-06-14 | |
| US63/352,180 | 2022-06-14 | ||
| US202263432243P | 2022-12-13 | 2022-12-13 | |
| US63/432,243 | 2022-12-13 | ||
| US202263434327P | 2022-12-21 | 2022-12-21 | |
| US63/434,327 | 2022-12-21 | ||
| US202363442648P | 2023-02-01 | 2023-02-01 | |
| US63/442,648 | 2023-02-01 | ||
| PCT/US2023/012299 WO2023150284A2 (en) | 2022-02-03 | 2023-02-03 | Quinazoline pan-kras inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3239343A1 true CA3239343A1 (en) | 2023-08-10 |
Family
ID=87552808
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3239343A Pending CA3239343A1 (en) | 2022-02-03 | 2023-02-03 | Quinazoline pan-kras inhibitors |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20240025907A1 (https=) |
| EP (1) | EP4472980A4 (https=) |
| JP (1) | JP2025506408A (https=) |
| KR (1) | KR20240145987A (https=) |
| AU (1) | AU2023216698A1 (https=) |
| CA (1) | CA3239343A1 (https=) |
| IL (1) | IL314486A (https=) |
| MX (1) | MX2024009616A (https=) |
| WO (1) | WO2023150284A2 (https=) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4373822A2 (en) | 2021-07-23 | 2024-05-29 | Theras Inc. | Compositions and methods for inhibition of ras |
| TW202328124A (zh) * | 2021-08-18 | 2023-07-16 | 大陸商北京加科思新藥研發有限公司 | 1,4-氧雜氮雜環庚烷衍生物及其用途 |
| JP2024543879A (ja) * | 2021-11-24 | 2024-11-26 | メルク・シャープ・アンド・ドーム・エルエルシー | Ｋｒａｓ変異型タンパク質の小分子阻害剤 |
| AU2023218370B2 (en) | 2022-02-09 | 2024-11-28 | Quanta Therapeutics, Inc. | Kras modulators and uses thereof |
| CN119585287A (zh) | 2022-05-06 | 2025-03-07 | Paq医疗公司 | Kras g12d蛋白水解靶向嵌合体 |
| IL317601A (en) | 2022-05-25 | 2025-02-01 | Quanta Therapeutics Inc | Pyrimidine-based modulators and their uses |
| WO2024046370A1 (zh) * | 2022-08-30 | 2024-03-07 | 上海科州药物研发有限公司 | 作为kras抑制剂的杂环化合物，及其制备和治疗用途 |
| CN117659050A (zh) * | 2022-09-08 | 2024-03-08 | 深圳福沃药业有限公司 | 用于治疗癌症的kras突变抑制剂的喹唑啉杂环类衍生物 |
| WO2024112654A1 (en) | 2022-11-21 | 2024-05-30 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| WO2024125600A1 (zh) * | 2022-12-14 | 2024-06-20 | 上海科州药物研发有限公司 | 作为kras抑制剂的杂环化合物，及其制备和治疗用途 |
| WO2024192424A1 (en) | 2023-03-15 | 2024-09-19 | Quanta Therapeutics, Inc. | Kras modulators and uses thereof |
| EP4687905A1 (en) | 2023-03-30 | 2026-02-11 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| WO2024235225A1 (zh) * | 2023-05-15 | 2024-11-21 | 苏州泽璟生物制药股份有限公司 | 取代嘧啶并环类抑制剂及其制备方法和应用 |
| IL326136A (en) | 2023-08-07 | 2026-03-01 | Revolution Medicines Inc | RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein |
| AU2024323424A1 (en) | 2023-08-17 | 2026-03-05 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| AU2024337913A1 (en) | 2023-09-08 | 2026-03-26 | Gilead Sciences, Inc. | Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds |
| 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 |
| US12599672B2 (en) | 2023-10-03 | 2026-04-14 | PAQ Therapeutics Inc. | KRAS proteolysis targeting chimeras |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025117828A1 (en) * | 2023-12-01 | 2025-06-05 | Theras, Inc. | Compositions and methods for inhibition of ras |
| WO2025145207A1 (en) | 2023-12-29 | 2025-07-03 | Bristol-Myers Squibb Company | Combination therapy of kras inhibitor and treg-depleting agent |
| WO2025148868A1 (zh) * | 2024-01-08 | 2025-07-17 | 泰励生物科技（上海）有限公司 | 一种抗体偶联药物及其用途 |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| TW202547457A (zh) * | 2024-04-08 | 2025-12-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 二氫呋喃并[3,4-f]喹唑啉類化合物、其製備方法及其在醫藥上的應用 |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025245105A1 (en) * | 2024-05-20 | 2025-11-27 | Erasca, Inc. | Kras inhibitors |
| WO2025245127A1 (en) | 2024-05-21 | 2025-11-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026002172A1 (zh) * | 2024-06-26 | 2026-01-02 | 上海青润医药科技有限公司 | Kras突变体抑制剂及其药物组合物、制备方法和应用 |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026035945A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload |
| WO2026035947A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload |
| WO2026039512A1 (en) | 2024-08-14 | 2026-02-19 | Bristol-Myers Squibb Company | Kras inhibitors |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026064527A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload |
| WO2026064520A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2018513853A (ja) * | 2015-04-10 | 2018-05-31 | アラクセス ファーマ エルエルシー | 置換キナゾリン化合物およびその使用方法 |
| WO2020146613A1 (en) * | 2019-01-10 | 2020-07-16 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| WO2021041671A1 (en) * | 2019-08-29 | 2021-03-04 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| WO2022002102A1 (en) * | 2020-06-30 | 2022-01-06 | InventisBio Co., Ltd. | Quinazoline compounds, preparation methods and uses thereof |
| CN116368130A (zh) * | 2020-08-28 | 2023-06-30 | 金橘生物科技公司 | 杂环化合物及其用途 |
| US20230081426A1 (en) * | 2020-09-18 | 2023-03-16 | Plexxikon Inc. | Compounds and methods for kras modulation and indications therefor |
| US20240109893A1 (en) * | 2020-12-22 | 2024-04-04 | Shanghai Kechow Pharma, Inc. | Preparation and application method of heterocyclic compounds as kras inhibitor |
| CN113999226B (zh) * | 2020-12-22 | 2023-01-06 | 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 |
| US20240140957A1 (en) * | 2021-01-08 | 2024-05-02 | Beigene Switzerland Gmbh | Bridged compounds as kras g12d inhibitor and degrader and the use thereof |
| BR112023015976A2 (pt) * | 2021-02-09 | 2023-12-12 | Medshine Discovery Inc | Compostos de anel aromático de pirimidina |
| WO2022173870A1 (en) * | 2021-02-09 | 2022-08-18 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| AU2022224511A1 (en) * | 2021-02-16 | 2023-08-10 | Lawrence Livermore National Security, Llc | Compositions and methods for inhibition of ras |
| WO2022187527A1 (en) * | 2021-03-05 | 2022-09-09 | Nikang Therapeutics, Inc | Quinazoline nitrile derivatives as kras inhibitors |
| WO2022184178A1 (en) * | 2021-03-05 | 2022-09-09 | Jacobio Pharmaceuticals Co., Ltd. | Kras g12d inhibitors |
| CN117500799A (zh) * | 2021-06-09 | 2024-02-02 | 伊莱利利公司 | 作为kras g12d抑制剂的取代的稠合吖嗪 |
| JP2024520791A (ja) * | 2021-06-10 | 2024-05-24 | レデックス・ファーマ・パブリック・リミテッド・カンパニー | 化合物 |
| US20240409558A1 (en) * | 2021-09-13 | 2024-12-12 | Biomea Fusion, Inc. | Irreversible inhibitors of kras |
| WO2023213269A1 (en) * | 2022-05-06 | 2023-11-09 | Zai Lab (Shanghai) Co., Ltd. | Amide-substituted heterocyclic compounds as kras g12d modulators and uses thereof |
-
2023
- 2023-02-03 IL IL314486A patent/IL314486A/en unknown
- 2023-02-03 CA CA3239343A patent/CA3239343A1/en active Pending
- 2023-02-03 WO PCT/US2023/012299 patent/WO2023150284A2/en not_active Ceased
- 2023-02-03 MX MX2024009616A patent/MX2024009616A/es unknown
- 2023-02-03 JP JP2024546129A patent/JP2025506408A/ja active Pending
- 2023-02-03 EP EP23750214.1A patent/EP4472980A4/en active Pending
- 2023-02-03 AU AU2023216698A patent/AU2023216698A1/en active Pending
- 2023-02-03 KR KR1020247025765A patent/KR20240145987A/ko active Pending
- 2023-08-02 US US18/229,662 patent/US20240025907A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| WO2023150284A3 (en) | 2023-09-14 |
| EP4472980A4 (en) | 2026-04-22 |
| EP4472980A2 (en) | 2024-12-11 |
| US20240025907A1 (en) | 2024-01-25 |
| JP2025506408A (ja) | 2025-03-11 |
| KR20240145987A (ko) | 2024-10-07 |
| MX2024009616A (es) | 2024-08-09 |
| AU2023216698A1 (en) | 2024-06-13 |
| IL314486A (en) | 2024-09-01 |
| WO2023150284A2 (en) | 2023-08-10 |
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