CA3240772A1 - Covalently binding inhibitors of g12s, g12d and/or g12e mutants of k-ras gtpase - Google Patents
Covalently binding inhibitors of g12s, g12d and/or g12e mutants of k-ras gtpase Download PDFInfo
- Publication number
- CA3240772A1 CA3240772A1 CA3240772A CA3240772A CA3240772A1 CA 3240772 A1 CA3240772 A1 CA 3240772A1 CA 3240772 A CA3240772 A CA 3240772A CA 3240772 A CA3240772 A CA 3240772A CA 3240772 A1 CA3240772 A1 CA 3240772A1
- Authority
- CA
- Canada
- Prior art keywords
- substituted
- unsubstituted
- ras
- compound
- nhc
- 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
-
- 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
- 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
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- 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
- 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
- C07D487/10—Spiro-condensed 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
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202163292910P | 2021-12-22 | 2021-12-22 | |
| US63/292,910 | 2021-12-22 | ||
| US202263313040P | 2022-02-23 | 2022-02-23 | |
| US63/313,040 | 2022-02-23 | ||
| US202263322528P | 2022-03-22 | 2022-03-22 | |
| US63/322,528 | 2022-03-22 | ||
| PCT/US2022/082136 WO2023122662A1 (en) | 2021-12-22 | 2022-12-21 | Covalently binding inhibitors of g12s, g12d and/or g12e mutants of k-ras gtpase |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3240772A1 true CA3240772A1 (en) | 2023-06-29 |
Family
ID=85278679
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3240772A Pending CA3240772A1 (en) | 2021-12-22 | 2022-12-21 | Covalently binding inhibitors of g12s, g12d and/or g12e mutants of k-ras gtpase |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20250059187A1 (https=) |
| EP (1) | EP4452416A1 (https=) |
| JP (1) | JP2025500430A (https=) |
| AU (1) | AU2022421224A1 (https=) |
| CA (1) | CA3240772A1 (https=) |
| IL (1) | IL313428A (https=) |
| MX (1) | MX2024007780A (https=) |
| TW (1) | TW202340202A (https=) |
| WO (1) | WO2023122662A1 (https=) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL318647A (en) | 2022-08-05 | 2025-03-01 | Kumquat Biosciences Inc | Heterocyclic compounds and their uses |
| CN119790059A (zh) * | 2022-08-30 | 2025-04-08 | 上海科州药物股份有限公司 | 作为kras抑制剂的杂环化合物，及其制备和治疗用途 |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| WO2025010415A1 (en) * | 2023-07-05 | 2025-01-09 | The Regents Of The University Of California | Gtpase inhibitors and uses thereof |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| US20250109147A1 (en) | 2023-09-08 | 2025-04-03 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
| US20250114339A1 (en) | 2023-10-09 | 2025-04-10 | Incyte Corporation | Combination therapy comprising a kras g12d inhibitor and an egfr inhibitor |
| US20250114346A1 (en) | 2023-10-09 | 2025-04-10 | Incyte Corporation | Combination therapy using a kras g12d inhibitor and pd-1 inhibitor or pd-l1 inhibitor |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2025096984A1 (en) * | 2023-11-02 | 2025-05-08 | The Regents Of The University Of California | Gtpase inhibitors and uses thereof |
| AU2024374420A1 (en) * | 2023-11-02 | 2026-04-16 | Kumquat Biosciences Inc. | Degraders and uses thereof |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025212580A1 (en) * | 2024-04-01 | 2025-10-09 | Xdc Precision Therapeutics Llc | Antibody-kras binder conjugates, pharmaceutical compositions, and therapeutic applications |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025255438A1 (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 |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| 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 |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LT3595B (en) * | 1993-01-21 | 1995-12-27 | Schering Corp | Spirocycloalkyl-substituted azetidinones useful as hypocholesterolemic agents |
| PT970957E (pt) * | 1998-06-12 | 2002-02-28 | Hoffmann La Roche | Derivados de diaza-espiro¬3,5|nonamo |
| PE20030762A1 (es) * | 2001-12-18 | 2003-09-05 | Schering Corp | Compuestos heterociclicos como antagonistas nk1 |
| WO2008033447A1 (en) * | 2006-09-15 | 2008-03-20 | Schering Corporation | Azetidine and azetidone derivatives useful in treating pain and disorders of lipid metabolism |
| PL2748166T3 (pl) * | 2011-08-23 | 2019-05-31 | Asana Biosciences Llc | Związki pirimido-pirydazynonowe oraz ich zastosowanie |
| CN105481858B (zh) * | 2014-10-11 | 2019-05-17 | 上海医药集团股份有限公司 | 一种含氮稠杂环化合物、其制备方法、组合物及应用 |
| CN108473498B (zh) * | 2015-12-22 | 2021-11-02 | 豪夫迈·罗氏有限公司 | 作为IRAK4调节剂的吡唑并[1,5a]嘧啶衍生物 |
| US10759750B2 (en) * | 2016-04-29 | 2020-09-01 | Temple University—Of the Commonwealth System of Higher Education | Beta lactams as modulators of glutamate uptake and methods for use thereof |
| KR102444509B1 (ko) | 2016-05-18 | 2022-09-19 | 미라티 테라퓨틱스, 인크. | Kras g12c 억제제 |
| WO2018187294A1 (en) * | 2017-04-03 | 2018-10-11 | Asana Biosciences, Llc | Pyrimido-pyridazinone compound combinations, methods, kits and formulations thereof |
| EP3612526A2 (en) * | 2017-04-20 | 2020-02-26 | The Regents of the University of California | K-ras modulators |
| AU2018273356B2 (en) | 2017-05-22 | 2021-09-16 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| US10961209B2 (en) * | 2017-08-10 | 2021-03-30 | Novomer, Inc. | Processes for producing beta-lactone and beta-lactone derivatives with heterogenous catalysts |
| US12098138B2 (en) * | 2018-05-25 | 2024-09-24 | The Board Of Regents Of The University Of Texas System | Substituted pyridinyl azetidinone derivatives for use in treating cancer and other diseases |
| PE20260440A1 (es) | 2018-11-09 | 2026-02-19 | Hoffmann La Roche | Compuestos de anillo fusionado |
| EP3738593A1 (en) | 2019-05-14 | 2020-11-18 | Amgen, Inc | Dosing of kras inhibitor for treatment of cancers |
| WO2020236947A1 (en) | 2019-05-21 | 2020-11-26 | Amgen Inc. | Solid state forms |
| GB201910168D0 (en) * | 2019-07-16 | 2019-08-28 | Syngenta Crop Protection Ag | Improvements in or relating to organic compounds |
| 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 |
| 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 |
| WO2021120890A1 (en) | 2019-12-20 | 2021-06-24 | Novartis Ag | Pyrazolyl derivatives useful as anti-cancer agents |
| AR121719A1 (es) * | 2020-04-03 | 2022-06-29 | Petra Pharma Corp | Inhibidores alostéricos de cromenona del fosfoinosítido 3-quinasa (pi3k) para el tratamiento de enfermedades |
| 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 |
-
2022
- 2022-12-21 TW TW111149250A patent/TW202340202A/zh unknown
- 2022-12-21 US US18/720,571 patent/US20250059187A1/en active Pending
- 2022-12-21 CA CA3240772A patent/CA3240772A1/en active Pending
- 2022-12-21 WO PCT/US2022/082136 patent/WO2023122662A1/en not_active Ceased
- 2022-12-21 EP EP22859496.6A patent/EP4452416A1/en active Pending
- 2022-12-21 JP JP2024537994A patent/JP2025500430A/ja active Pending
- 2022-12-21 IL IL313428A patent/IL313428A/en unknown
- 2022-12-21 MX MX2024007780A patent/MX2024007780A/es unknown
- 2022-12-21 AU AU2022421224A patent/AU2022421224A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| TW202340202A (zh) | 2023-10-16 |
| IL313428A (en) | 2024-08-01 |
| AU2022421224A1 (en) | 2024-06-20 |
| US20250059187A1 (en) | 2025-02-20 |
| EP4452416A1 (en) | 2024-10-30 |
| JP2025500430A (ja) | 2025-01-09 |
| MX2024007780A (es) | 2024-09-11 |
| WO2023122662A1 (en) | 2023-06-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| P22 | Classification modified |
Free format text: ST27 STATUS EVENT CODE: A-1-1-P10-P22-P110 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CLASSIFICATION MODIFIED Effective date: 20241030 |
|
| P13 | Application amended |
Free format text: ST27 STATUS EVENT CODE: A-1-1-P10-P13-P146 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: BSL VERIFIED - NO DEFECTS Effective date: 20241105 |
|
| MFA | Maintenance fee for application paid |
Free format text: FEE DESCRIPTION TEXT: MF (APPLICATION, 2ND ANNIV.) - STANDARD Year of fee payment: 2 |
|
| U00 | Fee paid |
Free format text: ST27 STATUS EVENT CODE: A-1-1-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED Effective date: 20241213 |
|
| U11 | Full renewal or maintenance fee paid |
Free format text: ST27 STATUS EVENT CODE: A-1-1-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL Effective date: 20241213 |