AR117194A1 - Compuestos de anillos fusionados - Google Patents
Compuestos de anillos fusionadosInfo
- Publication number
- AR117194A1 AR117194A1 ARP190103302A ARP190103302A AR117194A1 AR 117194 A1 AR117194 A1 AR 117194A1 AR P190103302 A ARP190103302 A AR P190103302A AR P190103302 A ARP190103302 A AR P190103302A AR 117194 A1 AR117194 A1 AR 117194A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- alkoxy
- haloalkyl
- halo
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 14
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 abstract 8
- 125000001475 halogen functional group Chemical group 0.000 abstract 8
- 125000000623 heterocyclic group Chemical group 0.000 abstract 8
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 7
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 125000001424 substituent group Chemical group 0.000 abstract 6
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 5
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 5
- 125000006642 (C1-C6) cyanoalkyl group Chemical group 0.000 abstract 5
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 5
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 5
- -1 C1−6 hydroxyalkanoyl Chemical group 0.000 abstract 4
- 125000005915 C6-C14 aryl group Chemical group 0.000 abstract 4
- 125000004181 carboxyalkyl group Chemical group 0.000 abstract 4
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 3
- 125000004414 alkyl thio group Chemical group 0.000 abstract 3
- 125000005466 alkylenyl group Chemical group 0.000 abstract 3
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 3
- 125000005242 carbamoyl alkyl group Chemical group 0.000 abstract 3
- 125000004995 haloalkylthio group Chemical group 0.000 abstract 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 2
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 abstract 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000004043 oxo group Chemical group O=* 0.000 abstract 2
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 abstract 1
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 101710113436 GTPase KRas Proteins 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000001589 carboacyl group Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 102200006538 rs121913530 Human genes 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
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
- 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
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- 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
- 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
- C07B2200/07—Optical isomers
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Nutrition Science (AREA)
- Dermatology (AREA)
- Physiology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable de este; caracterizado porque R¹ es un resto electrofílico capaz de formar un enlace covalente con un residuo de cisteína en la posición 12 de una proteína mutante K-Ras G12C; R² se selecciona del grupo que consiste en H, OH, NH₂, halo, alquilo C₁₋₆, haloalquilo C₁₋₆, ciclopropilo y -NHR, donde R se selecciona del grupo que consiste en alquilo C₁₋₆, alcoxi C₁₋₆, alcanoilo C₁₋₆, hidroxialcanoilo C₁₋₆, cianoalquilo C₁₋₆, alquilamino C₁₋₆, -(alquilenilo C₁₋₆)NH(CH₃)-(alquilenilo C₁₋₆)N(CH₃)₂ y -(alquilenilo C₁₋₃)(heterociclilo de 3 - 7 miembros); R³ y R⁴ se seleccionan cada uno independientemente del grupo que consiste en H, NH₂, halo, alquilo C₁₋₆, haloalquilo C₁₋₆, alcoxi C₁₋₆, haloalcoxi C₁₋₆, alquiltio C₁₋₆, haloalquiltio C₁₋₆, alquilamino C₁₋₆ y ciclopropilo; R⁵ se selecciona del grupo que consiste en H, NH₂, halo, alquilo C₁₋₆, haloalquilo C₁₋₆, alcoxi C₁₋₆, haloalcoxi C₁₋₆, alquiltio C₁₋₆, haloalquiltio C₁₋₆, alquilamino C₁₋₆ y cicloalquilo C₃₋₇, en donde al menos uno de R², R³, R⁴ y R⁵ es diferente de H; o R² y R³, R³ y R⁴, o R⁴ y R⁵, junto con los átomos a los cuales están unidos, forman un cicloalquilo C₃₋₇, heterocicloalquilo de 3 a 7 miembros, arilo C₆₋₁₄ o heteroarilo de 5 a 10 miembros; cada uno de los cuales está opcionalmente sustituido con 1 a 4 sustituyentes, en donde cada sustituyente se selecciona independientemente del grupo que consiste en OH, NH₂, halo, alquilo C₁₋₃, haloalquilo C₁₋₃, alcoxi C₁₋₃ y haloalcoxi C₁₋₃; X se selecciona del grupo que consiste en NH₂, alcoxi C₁₋₆, alquilo C₁₋₆, alquilamino C₁₋₆, alquilsulfanilo C₁₋₆, alquilsulfonilo C₁₋₆, alquiltio C₁₋₆, cicloalquilo C₃₋₇, heterociclilo de 4 a 7 miembros y heterociclilamino de 4 a 7 miembros; cada uno de los cuales está opcionalmente sustituido con 1 a 4 sustituyentes, en donde cada sustituyente se selecciona independientemente del grupo que consiste en OH, NH₂, halo, ciano, carboxi, carbamoilo, alquilo C₁₋₆, aminoalquilo C₁₋₆, carbamoilalquilo C₁₋₆, carboxialquilo C₁₋₆, cianoalquilo C₁₋₆, haloalquilo C₁₋₆, hidroxialquilo C₁₋₆ y heterociclilo de 4 a 7 miembros; en donde dos sustituyentes geminales se pueden tomar juntos para formar espirocicloalquilo C₃₋₇ o espiroheterociclilo de 4 a 7 miembros; Y se selecciona del grupo que consiste en -L-Y¹ o Y¹; Y¹ se selecciona del grupo que consiste en H, NH₂, halo, ciano, carbamoilo, alquenilo C₂₋₆, alcoxi C₁₋₆, alquilo C₁₋₆, alquilo C₁₋₆ sustituido con un heterociclilo de 4 a 10 miembros que se sustituye opcionalmente con 1 - 4 sustituyentes Y¹ᵃ, alquilo C₁₋₆ sustituido con un sustituyente dialquilamino C₁₋₆, alquilo C₁₋₆ sustituido con un dialquilamino ciclopropilo C₁₋₆, alquilsulfanilo C₁₋₆, alquilsulfonilo C₁₋₆, alquiltio C₁₋₆, alquinilo C₂₋₆, alquilamino C₁₋₆, arilo C₆₋₁₄, arilo C₆₋₁₄ sustituido con un alquilo C₁₋₆, aminoalquilo C₁₋₆, carbamoilalquilo C₁₋₆, carboxialquilo C₁₋₆, cianoalquilo C₁₋₆, cicloalquilo C₃₋₇, cicloalquilo C₃₋₇ sustituido con un dialquilamino C₁₋₆, haloalcoxi C₁₋₆, haloalquilo C₁₋₆, heteroarilo de 5 a 10 miembros, heterociclilo de 4 a 10 miembros, un heterociclilo de 4 a 10 miembros sustituido con metilo, hidroxi y oxo; cada Y¹ᵃ se selecciona independientemente del grupo que consiste en halo, alquilo C₁₋₆, alcoxi C₁₋₆, heterociclilo de 3 a 7 miembros, alcoxi C₁₋₆alquilo C₁₋₆, haloalquilo C₁₋₆, oxo, hidroxi, NH₂, ciano, carboxialquilo C₁₋₆, cianoalquilo C₁₋₆, hidroxialquilo C₁₋₆ y haloalcoxi C₁₋₆; L se selecciona del grupo que consiste en un enlace, O, S y N(Lᵃ); Lᵃ se selecciona del grupo que consiste en hidrógeno y alquilo C₁₋₃; U es C(R⁶ᵃ); V es C(R⁶ᵇ); W es C(R⁶ᶜ) o N; cada uno de R⁶ᵃ, R⁶ᵇ y R⁶ᶜ se selecciona independientemente del grupo que consiste en H, OH, NH₂, halo, ciano, carbamoilo, alquenilo C₂₋₆, alcoxi C₁₋₆, alquilo C₁₋₆, alquilo C₁₋₆ sustituido con un sustituyente heterociclilo de 4 a 10 miembros, alquilsulfanilo C₁₋₆, alquilsulfonilo C₁₋₆, alquiltio C₁₋₆, haloalquiltio C₁₋₆, alquinilo C₂₋₆, alquilamino C₁₋₆, arilo C₆₋₁₄, aminoalquilo C₁₋₆, carbamoilalquilo C₁₋₆, carboxialquilo C₁₋₆, cianoalquilo C₁₋₆, cicloalquilo C₃₋₇, haloalcoxi C₁₋₆, haloalquilo C₁₋₆, heteroarilo de 5 a 10 miembros y heterociclilo de 4 a 10 miembros; y n se selecciona del grupo que consiste en 0, 1 y 2.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2018114788 | 2018-11-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR117194A1 true AR117194A1 (es) | 2021-07-21 |
Family
ID=69232886
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP190103302A AR117194A1 (es) | 2018-11-09 | 2019-11-08 | Compuestos de anillos fusionados |
Country Status (33)
| Country | Link |
|---|---|
| US (3) | US11236068B2 (es) |
| EP (2) | EP4483881A3 (es) |
| JP (4) | JP6941241B2 (es) |
| KR (3) | KR102751492B1 (es) |
| CN (5) | CN118084866A (es) |
| AR (1) | AR117194A1 (es) |
| AU (3) | AU2019377130B2 (es) |
| BR (1) | BR112021008986A2 (es) |
| CA (1) | CA3087089C (es) |
| CL (2) | CL2021001171A1 (es) |
| CO (1) | CO2021005987A2 (es) |
| CR (1) | CR20210229A (es) |
| DK (1) | DK3735299T3 (es) |
| ES (1) | ES3004042T3 (es) |
| FI (1) | FI3735299T3 (es) |
| HR (1) | HRP20241581T1 (es) |
| HU (1) | HUE069365T2 (es) |
| IL (3) | IL311187B1 (es) |
| LT (1) | LT3735299T (es) |
| MA (1) | MA51530B1 (es) |
| MX (5) | MX2021005428A (es) |
| MY (1) | MY196726A (es) |
| PE (1) | PE20211504A1 (es) |
| PH (1) | PH12021551065A1 (es) |
| PL (1) | PL3735299T3 (es) |
| PT (1) | PT3735299T (es) |
| RS (1) | RS66280B1 (es) |
| SG (1) | SG11202103298QA (es) |
| SI (1) | SI3735299T1 (es) |
| SM (1) | SMT202400487T1 (es) |
| TW (2) | TWI784209B (es) |
| UA (1) | UA127930C2 (es) |
| WO (1) | WO2020097537A2 (es) |
Families Citing this family (86)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI831855B (zh) | 2018-10-26 | 2024-02-11 | 日商大鵬藥品工業股份有限公司 | 新穎吲唑化合物或其鹽 |
| 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 |
| US12122787B2 (en) | 2019-09-20 | 2024-10-22 | Shanghai Jemincare Pharmaceuticals Co., Ltd | Fused pyridone compound, and preparation method therefor and use thereof |
| CA3158793A1 (en) | 2019-10-28 | 2021-05-06 | Merck Sharp & Dohme Corp. | Small molecule inhibitors of kras g12c mutant |
| CN114980976A (zh) * | 2019-11-27 | 2022-08-30 | 锐新医药公司 | 共价ras抑制剂及其用途 |
| WO2021106230A1 (ja) | 2019-11-29 | 2021-06-03 | 大鵬薬品工業株式会社 | 新規なフェノール化合物又はその塩 |
| WO2021120045A1 (en) | 2019-12-18 | 2021-06-24 | InventisBio Co., Ltd. | Heterocyclic compounds, preparation methods and uses thereof |
| WO2021138391A1 (en) | 2019-12-30 | 2021-07-08 | Tyra Biosciences, Inc. | Indazole compounds |
| EP4168002A1 (en) | 2020-06-18 | 2023-04-26 | Revolution Medicines, Inc. | Methods for delaying, preventing, and treating acquired resistance to ras inhibitors |
| BR112023002591A2 (pt) * | 2020-08-12 | 2023-04-04 | Genentech Inc | Processo para a preparação de um composto e composto |
| IL300708A (en) * | 2020-08-17 | 2023-04-01 | Betta Pharmaceuticals Co Ltd | Bicyclic compounds, their compositions and use |
| JP2023540270A (ja) | 2020-08-28 | 2023-09-22 | カムクワット バイオサイエンシーズ インコーポレイテッド | 複素環式化合物およびその使用 |
| CA3187757A1 (en) | 2020-09-03 | 2022-03-24 | Ethan AHLER | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| KR20230137286A (ko) | 2020-09-11 | 2023-10-04 | 미라티 테라퓨틱스, 인크. | Kras g12c 억제제의 결정 형태 |
| WO2022066805A1 (en) | 2020-09-23 | 2022-03-31 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| CN116323624A (zh) * | 2020-09-30 | 2023-06-23 | 上海医药集团股份有限公司 | 一种喹唑啉类化合物及其应用 |
| US20240034733A1 (en) * | 2020-11-03 | 2024-02-01 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| TWI886356B (zh) * | 2020-11-13 | 2025-06-11 | 美商建南德克公司 | 用於治療實性瘤之方法與包含ｋｒａｓｇ１２ｃ抑制劑及ｖｅｇｆ抑制劑之組成物 |
| MX2023005530A (es) * | 2020-11-13 | 2023-05-25 | Genentech Inc | Metodos y composiciones que comprenden un inhibidor de krasg12c y un antagonista de union a pd-l1 para tratar cancer de pulmon. |
| US20240025918A1 (en) * | 2020-11-20 | 2024-01-25 | Jacobio Pharmaceuticals Co., Ltd | KRAS G12D Inhibitors |
| WO2022105855A1 (en) * | 2020-11-20 | 2022-05-27 | Jacobio Pharmaceuticals Co., Ltd. | Kras g12d inhibitors |
| TWI895563B (zh) * | 2020-12-08 | 2025-09-01 | 美商建南德克公司 | 用於治療實性瘤之包含ｋｒａｓｇ１２ｃ抑制劑及ｅｇｆｒ抑制劑之組成物及方法 |
| MX2023007084A (es) | 2020-12-15 | 2023-08-30 | Mirati Therapeutics Inc | Inhibidores de pan-kras de azaquinazolina. |
| EP4262803A4 (en) | 2020-12-16 | 2025-03-12 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-kras inhibitors |
| CA3203080A1 (en) * | 2020-12-22 | 2022-06-30 | Hongqi Tian | Preparation and application method of heterocyclic compound 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 |
| CN114685532A (zh) * | 2020-12-31 | 2022-07-01 | 正大天晴药业集团股份有限公司 | 大环类化合物及其医药用途 |
| WO2022171018A1 (zh) * | 2021-02-09 | 2022-08-18 | 苏州泽璟生物制药股份有限公司 | 取代苯并或吡啶并嘧啶胺类抑制剂及其制备方法和应用 |
| AU2022220678A1 (en) * | 2021-02-09 | 2023-09-21 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| WO2022171013A1 (zh) * | 2021-02-09 | 2022-08-18 | 南京明德新药研发有限公司 | 四氢喹唑啉类化合物 |
| CA3210167A1 (en) * | 2021-02-09 | 2022-08-18 | Genentech, Inc. | Tetracyclic oxazepine compounds and uses thereof |
| IL304986A (en) * | 2021-02-16 | 2023-10-01 | Theras Inc | Compositions and methods for inhibition of ras |
| US20250255868A1 (en) * | 2021-04-09 | 2025-08-14 | Hangzhou Innogate Pharma Co., Ltd. | Heterocyclic compound acting as kras g12d inhibitor |
| WO2022221386A1 (en) * | 2021-04-14 | 2022-10-20 | Erasca, Inc. | Selective kras inhibitors |
| EP4322954A4 (en) * | 2021-04-16 | 2025-01-29 | Merck Sharp & Dohme LLC | SMALL MOLECULAR INHIBITORS OF THE KRAS G12D MUTANT |
| MX2023012726A (es) * | 2021-04-29 | 2024-01-04 | Amgen Inc | Compuestos heterociclicos y metodos de uso. |
| EP4340883A1 (en) * | 2021-05-19 | 2024-03-27 | Genentech, Inc. | Combination therapy |
| WO2022247760A1 (zh) * | 2021-05-22 | 2022-12-01 | 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 |
| US20240261444A1 (en) * | 2021-05-26 | 2024-08-08 | Cornell University | Rigidified macrocycles, complexes with radionuclides, and use in targeted radiotherapy of cancer |
| AU2022315228A1 (en) | 2021-07-23 | 2024-02-08 | Lawrence Livermore National Security, Llc | Compositions and methods for inhibition of ras |
| US20240376128A1 (en) * | 2021-08-18 | 2024-11-14 | Jacobio Pharmaceuticals Co., Ltd. | N-cyclopropylpyrido [4, 3-d] pyrimidin-4-amine derivatives and uses thereof |
| TW202315626A (zh) * | 2021-08-31 | 2023-04-16 | 大陸商勁方醫藥科技(上海)有限公司 | 嘧啶并環類化合物及其製法和用途 |
| IL309086A (en) | 2021-09-01 | 2024-02-01 | Novartis Ag | Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers |
| JP2024541508A (ja) | 2021-11-24 | 2024-11-08 | ジェネンテック， インコーポレイテッド | 治療用インダゾール化合物およびがんの治療における使用方法 |
| 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 |
| EP4436969A2 (en) | 2021-11-24 | 2024-10-02 | Genentech, Inc. | Bicyclic therapeutic compounds and methods of use in the treatment of cancer |
| EP4452416A1 (en) | 2021-12-22 | 2024-10-30 | The Regents Of The University Of California | Covalently binding inhibitors of g12s, g12d and/or g12e mutants of k-ras gtpase |
| US20250188085A1 (en) * | 2022-01-06 | 2025-06-12 | Theras, Inc. | Compositions and methods for inhibition of ras |
| US20250084079A1 (en) * | 2022-01-06 | 2025-03-13 | Theras, Inc. | Compositions and methods for inhibition of ras |
| CA3250773A1 (en) * | 2022-02-07 | 2023-08-10 | Genentech, Inc. | PROCESS FOR THE SYNTHESIS OF QUINAZOLINE COMPOUNDS |
| WO2023150706A1 (en) * | 2022-02-07 | 2023-08-10 | Genentech, Inc. | Solid forms of 1-((s)-4-((r)-7-(6-amino-4-methyl-3- (trifluoromethyl)pyridin-2-yl)-6-chloro-8-fluoro-2-(((s)-1- methylpyrrolidin-2-yl)methoxy)quinazolin-4-yl)-3- methylpiperazin-1-yl)prop-2-en-1-one |
| KR20240163107A (ko) | 2022-03-11 | 2024-11-18 | 컴쿼트 바이오사이언시즈 인크. | 헤테로환 화합물 및 이의 용도 |
| AU2023246216A1 (en) | 2022-03-31 | 2024-09-19 | Eisai R&D Management Co., Ltd. | Pharmaceutical composition for treating tumors |
| KR20240167654A (ko) * | 2022-04-06 | 2024-11-27 | 제넨테크, 인크. | 암의 치료를 위한 gdc-6036 및 gdc-0077을 포함하는 병용 요법 |
| JP7735594B2 (ja) | 2022-05-19 | 2025-09-08 | ジェネンテック， インコーポレイテッド | アザ四環式オキサゼピン化合物及びその使用 |
| CN115043729B (zh) * | 2022-07-04 | 2024-09-27 | 青岛大学 | 一种2,2’-二氟联芳基化合物的不对称合成方法 |
| JP2025525946A (ja) | 2022-08-05 | 2025-08-07 | カムクワット バイオサイエンシーズ インコーポレイテッド | 複素環式化合物およびその使用 |
| KR20250048078A (ko) | 2022-08-11 | 2025-04-07 | 브리스톨-마이어스 스큅 컴퍼니 | Kras 억제제 |
| EP4573095A1 (en) | 2022-08-17 | 2025-06-25 | Treeline Biosciences, Inc. | Pyridopyrimidine kras inhibitors |
| WO2024081674A1 (en) | 2022-10-11 | 2024-04-18 | Aadi Bioscience, Inc. | Combination therapies for the treatment of cancer |
| CN121039137A (zh) | 2022-11-21 | 2025-11-28 | 树线生物科学公司 | 螺环二氢吡喃并嘧啶KRas抑制剂 |
| CN115920658B (zh) * | 2023-01-15 | 2023-10-20 | 安徽科博瑞环境科技有限公司 | 低表面能抗污染中空纤维膜及其制备方法 |
| CN120548318A (zh) * | 2023-01-18 | 2025-08-26 | 苏州赞荣医药科技有限公司 | Kras g12d抑制剂和其用途 |
| EP4655298A1 (en) * | 2023-01-24 | 2025-12-03 | Theras Inc. | Compositions and methods for inhibition of ras |
| IL322247A (en) | 2023-01-26 | 2025-09-01 | Arvinas Operations Inc | Cerebellon-based KRAS-disrupting proteins and related uses |
| CR20250458A (es) | 2023-03-30 | 2025-11-21 | Revolution Medicines Inc | Composiciones para inducir la hidrólisis de ras gtp y sus usos |
| WO2024209717A1 (ja) | 2023-04-06 | 2024-10-10 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 腫瘍治療用医薬組成物 |
| CN116396202A (zh) * | 2023-04-17 | 2023-07-07 | 南京优氟医药科技有限公司 | 一种（2s，4s）-4-氟代吡咯烷-2-羧酸的制备方法 |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| US20250000802A1 (en) | 2023-06-09 | 2025-01-02 | Hoffmann-La Roche Inc. | Solid formulations comprising an inhibitor of the k-ras protein having a g12c mutation, and a process for preparing |
| 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 |
| 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 |
| WO2025067459A2 (en) | 2023-09-29 | 2025-04-03 | D3 Bio (Wuxi) Co., Ltd. | Therapies for the treatment of cancer |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| US12466840B2 (en) | 2023-10-20 | 2025-11-11 | Merck Sharp & Dohme Llc | Small molecule inhibitors of KRAS proteins |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025245127A1 (en) | 2024-05-21 | 2025-11-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| 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 |
| 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 |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999002557A1 (en) | 1997-07-11 | 1999-01-21 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V | Novel pharmaceutically active compounds interacting with gtp-binding proteins |
| CA2727036C (en) | 2008-06-20 | 2017-03-21 | Genentech, Inc. | Triazolopyridine jak inhibitor compounds and methods |
| EP2836482B1 (en) | 2012-04-10 | 2019-12-25 | The Regents of The University of California | Compositions and methods for treating cancer |
| AU2014331794C1 (en) * | 2013-10-10 | 2019-09-12 | Araxes Pharma Llc | Inhibitors of KRAS G12C |
| JO3805B1 (ar) | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | مثبطات كراس جي12سي |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| US10011600B2 (en) | 2014-09-25 | 2018-07-03 | Araxes Pharma Llc | Methods and compositions for inhibition of Ras |
| US9862701B2 (en) | 2014-09-25 | 2018-01-09 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| MX382355B (es) | 2015-04-10 | 2025-03-13 | Araxes Pharma Llc | Compuestos de quinazolina sustituidos y métodos de uso de los mismos. |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| 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 |
| WO2017100546A1 (en) | 2015-12-09 | 2017-06-15 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| US10822312B2 (en) | 2016-03-30 | 2020-11-03 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| ES2863873T3 (es) | 2016-05-18 | 2021-10-11 | Mirati Therapeutics Inc | Inhibidores de KRAS G12C |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| US11639346B2 (en) | 2017-05-25 | 2023-05-02 | Araxes Pharma Llc | Quinazoline derivatives as modulators of mutant KRAS, HRAS or NRAS |
| 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 |
| KR20200010306A (ko) | 2017-05-25 | 2020-01-30 | 아락세스 파마 엘엘씨 | Kras의 공유적 억제제 |
| IL274601B2 (en) | 2017-11-15 | 2024-04-01 | Mirati Therapeutics Inc | Kras g12c inhibitors |
| MX2020006045A (es) | 2017-12-19 | 2020-08-17 | Merck Patent Gmbh | Antagonistas de receptores tipo toll 7 y 8 (tlr7/8) y usos de los mismos. |
| TW201942115A (zh) | 2018-02-01 | 2019-11-01 | 美商輝瑞股份有限公司 | 作為抗癌藥之經取代的喹唑啉和吡啶並嘧啶衍生物 |
-
2019
- 2019-11-08 CN CN202410280860.9A patent/CN118084866A/zh active Pending
- 2019-11-08 CN CN202410281087.8A patent/CN118084870A/zh active Pending
- 2019-11-08 SG SG11202103298QA patent/SG11202103298QA/en unknown
- 2019-11-08 CN CN202410280943.8A patent/CN118084867A/zh active Pending
- 2019-11-08 DK DK19842848.4T patent/DK3735299T3/da active
- 2019-11-08 SI SI201930862T patent/SI3735299T1/sl unknown
- 2019-11-08 AU AU2019377130A patent/AU2019377130B2/en active Active
- 2019-11-08 LT LTEPPCT/US2019/060578T patent/LT3735299T/lt unknown
- 2019-11-08 IL IL311187A patent/IL311187B1/en unknown
- 2019-11-08 PE PE2021000682A patent/PE20211504A1/es unknown
- 2019-11-08 KR KR1020237033977A patent/KR102751492B1/ko active Active
- 2019-11-08 RS RS20241331A patent/RS66280B1/sr unknown
- 2019-11-08 CR CR20210229A patent/CR20210229A/es unknown
- 2019-11-08 SM SM20240487T patent/SMT202400487T1/it unknown
- 2019-11-08 PT PT198428484T patent/PT3735299T/pt unknown
- 2019-11-08 PL PL19842848.4T patent/PL3735299T3/pl unknown
- 2019-11-08 BR BR112021008986-1A patent/BR112021008986A2/pt unknown
- 2019-11-08 KR KR1020207024122A patent/KR102587544B1/ko active Active
- 2019-11-08 AR ARP190103302A patent/AR117194A1/es unknown
- 2019-11-08 ES ES19842848T patent/ES3004042T3/es active Active
- 2019-11-08 FI FIEP19842848.4T patent/FI3735299T3/fi active
- 2019-11-08 UA UAA202101478A patent/UA127930C2/uk unknown
- 2019-11-08 WO PCT/US2019/060578 patent/WO2020097537A2/en not_active Ceased
- 2019-11-08 HU HUE19842848A patent/HUE069365T2/hu unknown
- 2019-11-08 MY MYPI2021002582A patent/MY196726A/en unknown
- 2019-11-08 CN CN202410281112.2A patent/CN118084868A/zh active Pending
- 2019-11-08 CN CN201980026181.6A patent/CN112105419B/zh active Active
- 2019-11-08 MX MX2021005428A patent/MX2021005428A/es unknown
- 2019-11-08 US US16/679,104 patent/US11236068B2/en active Active
- 2019-11-08 TW TW108140719A patent/TWI784209B/zh active
- 2019-11-08 KR KR1020257000144A patent/KR20250012188A/ko active Pending
- 2019-11-08 TW TW111140273A patent/TWI883352B/zh active
- 2019-11-08 EP EP24198360.0A patent/EP4483881A3/en active Pending
- 2019-11-08 IL IL282916A patent/IL282916B2/en unknown
- 2019-11-08 EP EP19842848.4A patent/EP3735299B1/en active Active
- 2019-11-08 JP JP2020542808A patent/JP6941241B2/ja active Active
- 2019-11-08 HR HRP20241581TT patent/HRP20241581T1/hr unknown
- 2019-11-08 CA CA3087089A patent/CA3087089C/en active Active
- 2019-11-08 MA MA51530A patent/MA51530B1/fr unknown
-
2021
- 2021-05-04 CL CL2021001171A patent/CL2021001171A1/es unknown
- 2021-05-07 MX MX2025002975A patent/MX2025002975A/es unknown
- 2021-05-07 MX MX2024008118A patent/MX2024008118A/es unknown
- 2021-05-07 PH PH12021551065A patent/PH12021551065A1/en unknown
- 2021-05-07 CO CONC2021/0005987A patent/CO2021005987A2/es unknown
- 2021-05-07 MX MX2025002980A patent/MX2025002980A/es unknown
- 2021-05-07 MX MX2025002979A patent/MX2025002979A/es unknown
- 2021-07-15 JP JP2021116809A patent/JP7374960B2/ja active Active
- 2021-12-17 US US17/644,993 patent/US12084429B2/en active Active
-
2022
- 2022-03-01 AU AU2022201413A patent/AU2022201413B9/en active Active
- 2022-03-22 CL CL2022000698A patent/CL2022000698A1/es unknown
-
2023
- 2023-10-25 JP JP2023183500A patent/JP7579414B2/ja active Active
-
2024
- 2024-02-13 AU AU2024200904A patent/AU2024200904A1/en active Pending
- 2024-06-18 US US18/747,054 patent/US20250059163A1/en active Pending
- 2024-10-25 JP JP2024187827A patent/JP2025026853A/ja active Pending
-
2025
- 2025-10-20 IL IL324078A patent/IL324078A/en unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR117194A1 (es) | Compuestos de anillos fusionados | |
| AR095706A1 (es) | Indazoles sustituidos con heteroarilo | |
| AR101102A1 (es) | Herbicidas de piperidinona | |
| AR113964A1 (es) | Carbamoíl ciclohexil ácidos ligados a n de triazol como antagonistas de lpa | |
| AR100438A1 (es) | Pirazolopiridinas y pirazolopirimidinas | |
| AR088449A1 (es) | Benzilindazoles sustituidos | |
| AR127309A2 (es) | Derivados de piridazinona | |
| AR092349A1 (es) | Imidazotriazincarbonitrilos utiles como inhibidores de quinasa | |
| AR109788A1 (es) | Compuestos de benzo[b]tiofeno como agonistas de sting | |
| AR108875A1 (es) | COMPUESTOS HETEROCÍCLICOS COMO INHIBIDORES DE PI3K-g | |
| AR101265A1 (es) | Ácidos carboxílicos heterocíclicos como activadores de guanilato ciclasa soluble | |
| AR108325A1 (es) | Isoquinolin-3-il carboxamidas y preparación y uso de las mismas | |
| AR116109A1 (es) | Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos | |
| AR113929A1 (es) | Compuestos heterocíclicos | |
| AR103064A1 (es) | Compuestos moduladores de fxr (nr1h4) | |
| AR089568A1 (es) | Compuestos heterociclicos y sus metodos de usos | |
| AR095708A1 (es) | Indazoles sustituidos con diaminoheteroarilo | |
| DOP2018000187A (es) | Derivados de pirazolo[1,5-a]pirazin-4-ilo | |
| AR119657A1 (es) | Compuestos de pirimidina y composiciones farmacéuticas para prevenir o tratar cánceres que incluyen los mismos | |
| AR095311A1 (es) | 3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de idh mutante | |
| AR104963A1 (es) | Derivados de 2-(pirazolopiridin-3-il)pirimidina como inhibidores de jak | |
| AR094857A1 (es) | Derivados de pirrolo[2,3-d]pirimidina | |
| AR107042A1 (es) | Inhibidores de la tirosina quinasa de bruton y métodos de su uso | |
| AR110026A1 (es) | Inhibidores de pde2 | |
| AR104461A1 (es) | Pirrolo[2,3-d]pirimidinil, pirrolo[2,3-b]pirazinil, pirrolo[2,3-b]piridinil acrilamidas y epóxidos de estas |