MA54327B1 - Inhibiteurs de kras g12c - Google Patents
Inhibiteurs de kras g12cInfo
- Publication number
- MA54327B1 MA54327B1 MA54327A MA54327A MA54327B1 MA 54327 B1 MA54327 B1 MA 54327B1 MA 54327 A MA54327 A MA 54327A MA 54327 A MA54327 A MA 54327A MA 54327 B1 MA54327 B1 MA 54327B1
- Authority
- MA
- Morocco
- Prior art keywords
- kras
- inhibitors
- compounds
- salts
- formula
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- 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
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- 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
- A61K31/555—Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/24—Heavy metals; Compounds thereof
- A61K33/243—Platinum; Compounds thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
- A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Mycology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Microbiology (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Inorganic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La présente invention concerne des composés de formule : où r1, r2, r3, r4, r5, a, b et y sont tels que décrits dans la description, des sels pharmaceutiquement acceptables de ceux-ci, ainsi que des procédés d'utilisation de ces composés et de ces sels pour traiter des patients atteints d'un cancer.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962946586P | 2019-12-11 | 2019-12-11 | |
| PCT/US2020/063272 WO2021118877A1 (fr) | 2019-12-11 | 2020-12-04 | Inhibiteurs de kras g12c |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MA54327A MA54327A (fr) | 2022-04-13 |
| MA54327B1 true MA54327B1 (fr) | 2022-12-30 |
Family
ID=74106135
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MA54327A MA54327B1 (fr) | 2019-12-11 | 2020-12-04 | Inhibiteurs de kras g12c |
Country Status (34)
| Country | Link |
|---|---|
| US (2) | US11731984B2 (fr) |
| EP (1) | EP3886991B1 (fr) |
| JP (1) | JP7023421B2 (fr) |
| KR (1) | KR102546592B1 (fr) |
| CN (2) | CN117820333A (fr) |
| AR (1) | AR120700A1 (fr) |
| AU (2) | AU2020402701B2 (fr) |
| CA (1) | CA3161162A1 (fr) |
| CL (1) | CL2022001513A1 (fr) |
| CO (1) | CO2022008091A2 (fr) |
| CR (1) | CR20220258A (fr) |
| DK (1) | DK3886991T3 (fr) |
| DO (1) | DOP2022000117A (fr) |
| EC (1) | ECSP22046699A (fr) |
| ES (1) | ES2929700T3 (fr) |
| HR (1) | HRP20221301T1 (fr) |
| HU (1) | HUE060684T2 (fr) |
| IL (2) | IL304534B1 (fr) |
| JO (2) | JOP20220142B1 (fr) |
| LT (1) | LT3886991T (fr) |
| MA (1) | MA54327B1 (fr) |
| MD (1) | MD3886991T2 (fr) |
| MX (2) | MX2022006986A (fr) |
| PE (1) | PE20230238A1 (fr) |
| PH (1) | PH12022551424A1 (fr) |
| PL (1) | PL3886991T3 (fr) |
| PT (1) | PT3886991T (fr) |
| RS (1) | RS63719B1 (fr) |
| SA (1) | SA522432955B1 (fr) |
| SI (1) | SI3886991T1 (fr) |
| TW (1) | TWI765448B (fr) |
| UA (1) | UA128806C2 (fr) |
| WO (1) | WO2021118877A1 (fr) |
| ZA (1) | ZA202205218B (fr) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020085504A1 (fr) | 2018-10-26 | 2020-04-30 | 大鵬薬品工業株式会社 | Procédé de production d'un dérivé de carboxylate de chloroazole par réaction de sandmeyer avec exposition à la lumière |
| CN114867726B (zh) | 2019-10-28 | 2023-11-28 | 默沙东有限责任公司 | Kras g12c突变体的小分子抑制剂 |
| US12479834B2 (en) | 2019-11-29 | 2025-11-25 | Taiho Pharmaceutical Co., Ltd. | Phenol compound or salt thereof |
| WO2023205701A1 (fr) | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Hétérocycles macrocycliques et leurs utilisations |
| TWI799871B (zh) * | 2020-05-27 | 2023-04-21 | 大陸商勁方醫藥科技(上海)有限公司 | 三環并環類化合物，其製法與醫藥上的用途 |
| WO2021245055A1 (fr) | 2020-06-02 | 2021-12-09 | Boehringer Ingelheim International Gmbh | 2-amino-3-cyanothiophènes annelés et dérivés pour le traitement du cancer |
| 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 |
| MX2023002248A (es) | 2020-09-03 | 2023-05-16 | Revolution Medicines Inc | Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2. |
| AU2021347232A1 (en) | 2020-09-23 | 2023-04-27 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| CN114437107B (zh) * | 2020-11-06 | 2025-04-04 | 江苏先声药业有限公司 | 哌嗪类化合物及其应用 |
| TWI880049B (zh) * | 2020-12-04 | 2025-04-11 | 美商美國禮來大藥廠 | Kras g12c抑制劑 |
| WO2022133345A1 (fr) | 2020-12-18 | 2022-06-23 | Erasca, Inc. | Pyridones et pyrimidones tricycliques |
| US20240293558A1 (en) | 2021-06-16 | 2024-09-05 | Erasca, Inc. | Kras inhibitor conjugates |
| CN117677398A (zh) | 2021-07-27 | 2024-03-08 | 东丽株式会社 | 用于癌的治疗和/或预防的药品 |
| WO2023066371A1 (fr) | 2021-10-22 | 2023-04-27 | 江苏恒瑞医药股份有限公司 | Composé tétracyclique contenant de l'azote, son procédé de préparation et son utilisation médicale |
| US20250129096A1 (en) * | 2021-12-01 | 2025-04-24 | Boehringer Ingelheim Int'l GmbH Corp. | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| US20250313553A1 (en) * | 2021-12-01 | 2025-10-09 | Boehringer Ingelheim Int'l GmbH Corp. | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| US20250145608A1 (en) * | 2021-12-01 | 2025-05-08 | Boehringer Ingelheim Int'l GmbH Corp. | Kras degrading compounds comprising annulated 2-amino-3-cyano thiophenes |
| WO2023099624A1 (fr) | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | 2-amino-3-cyano thiophènes annelés et leurs dérivés pour le traitement du cancer |
| CN118647620A (zh) * | 2021-12-01 | 2024-09-13 | 勃林格殷格翰国际有限公司 | 用于治疗癌症的环状2-氨基-3-氰基噻吩及其衍生物 |
| US20250059187A1 (en) | 2021-12-22 | 2025-02-20 | The Regents Of The University Of California | Covalently binding inhibitors of g12s, g12d and/or g12e mutants of k-ras gtpase |
| CN118434422A (zh) | 2021-12-28 | 2024-08-02 | 阿斯利康(英国)有限公司 | 抗体-药物缀合物和rasg12c抑制剂的组合 |
| EP4486345A1 (fr) * | 2022-03-04 | 2025-01-08 | Eli Lilly and Company | Procédé de traitement comprenant des inhibiteurs de kras g12c et des inhibiteurs de shp2 |
| KR20240163107A (ko) | 2022-03-11 | 2024-11-18 | 컴쿼트 바이오사이언시즈 인크. | 헤테로환 화합물 및 이의 용도 |
| JP7676677B2 (ja) | 2022-03-25 | 2025-05-14 | イーライ リリー アンド カンパニー | Ｋｒａｓ阻害剤 |
| JP2025511697A (ja) * | 2022-04-07 | 2025-04-16 | イーライ リリー アンド カンパニー | Ｋｒａｓ ｇ１２ｃ阻害剤を作製するための方法 |
| CA3247183A1 (fr) | 2022-04-08 | 2023-10-12 | Eli Lilly And Company | Méthode de traitement comprenant des inhibiteurs de kras g12c et des inhibiteurs d’aurora a |
| WO2023246903A1 (fr) * | 2022-06-24 | 2023-12-28 | 暨南大学 | Composé hétérocyclique contenant du sélénium, composition pharmaceutique associée et son utilisation |
| EP4547251A1 (fr) * | 2022-06-30 | 2025-05-07 | Eli Lilly and Company | Inhibiteur de kras g12c pour le traitement du cancer |
| KR20250042155A (ko) | 2022-07-27 | 2025-03-26 | 지앙수 헨그루이 파마슈티컬스 컴퍼니 리미티드 | 축합 고리계 화합물, 이의 제조 방법 및 이의 의학적 응용 |
| CA3261681A1 (fr) | 2022-08-05 | 2024-02-08 | Kumquat Biosciences Inc. | Composés hétérocycliques et leurs utilisations |
| EP4573095A1 (fr) | 2022-08-17 | 2025-06-25 | Treeline Biosciences, Inc. | Inhibiteurs de pyridopyrimidine kras |
| GB202212641D0 (en) | 2022-08-31 | 2022-10-12 | Jazz Pharmaceuticals Ireland Ltd | Novel compounds |
| AU2023349002A1 (en) | 2022-09-30 | 2025-05-15 | Trasveda Ltd. | Compounds with anti-kras mutant tumor activity |
| WO2024081674A1 (fr) | 2022-10-11 | 2024-04-18 | Aadi Bioscience, Inc. | Polythérapies pour le traitement du cancer |
| WO2024112654A1 (fr) | 2022-11-21 | 2024-05-30 | Treeline Biosciences, Inc. | Inhibiteurs de kras spirocycliques de dihydropyranopyrimidine |
| WO2024206747A1 (fr) | 2023-03-30 | 2024-10-03 | Eli Lilly And Company | Inhibiteurs de kras |
| EP4688792A1 (fr) | 2023-03-31 | 2026-02-11 | Eli Lilly and Company | Inhibiteurs de kras |
| EP4700027A1 (fr) | 2023-04-21 | 2026-02-25 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Forme cristalline d'un composé tétracyclique contenant de l'azote et son procédé de préparation |
| CN120981456A (zh) | 2023-05-24 | 2025-11-18 | 金橘生物科技公司 | 杂环化合物及其用途 |
| WO2024248123A1 (fr) | 2023-06-02 | 2024-12-05 | 第一三共株式会社 | Combinaison d'un conjugué (anticorps anti-her3)-médicament et d'un inhibiteur de rasg12c |
| CN121605110A (zh) | 2023-06-06 | 2026-03-03 | 金橘生物科技公司 | 取代杂环化合物及其用途 |
| WO2025054347A1 (fr) | 2023-09-08 | 2025-03-13 | Gilead Sciences, Inc. | Composés de modulation de kras g12d |
| 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 |
| WO2025072457A1 (fr) | 2023-09-27 | 2025-04-03 | Eli Lilly And Company | Inhibiteurs de kras |
| TW202529768A (zh) | 2023-09-29 | 2025-08-01 | 大陸商德昇濟醫藥（無錫）有限公司 | 癌症治療的療法 |
| AU2024358622A1 (en) | 2023-10-11 | 2026-04-16 | Eli Lilly And Company | Process for making a kras g12c inhibitor |
| WO2025085748A1 (fr) | 2023-10-20 | 2025-04-24 | Merck Sharp & Dohme Llc | Inhibiteurs à petites molécules de protéines kras |
| WO2025245127A1 (fr) | 2024-05-21 | 2025-11-27 | Treeline Biosciences, Inc. | Inhibiteurs de dihydropyranopyrimidine kras spirocycliques |
| WO2026035947A1 (fr) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Conjugués médicamenteux à induction par liaison covalente ciblant kras comprenant une charge utile de topo-isomérase |
| WO2026035945A1 (fr) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Conjugués médicamenteux induits par covalence ciblant kras et comprenant une charge utile de topoisomérase |
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| WO2026064527A1 (fr) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Conjugués médicamenteux à induction covalente ciblant kras comprenant une charge utile d'inhibiteur de tubuline |
| WO2026064520A1 (fr) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Conjugués médicamenteux à induction covalente ciblant kras et comprenant une charge utile inhibitrice de tubuline |
| US12600733B2 (en) | 2024-10-01 | 2026-04-14 | Eli Lilly And Company | KRAS inhibitors |
| WO2026075942A1 (fr) | 2024-10-01 | 2026-04-09 | Eli Lilly And Company | Inhibiteurs de kras |
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| TW202012415A (zh) * | 2018-05-08 | 2020-04-01 | 瑞典商阿斯特捷利康公司 | 化學化合物 |
| TW202033518A (zh) | 2018-10-15 | 2020-09-16 | 美商美國禮來大藥廠 | Kras g12c 抑制劑 |
| ES3010507T3 (en) * | 2019-03-05 | 2025-04-03 | Astrazeneca Ab | Fused tricyclic compounds useful as anticancer agents |
| CN112390818B (zh) | 2019-08-12 | 2023-08-22 | 劲方医药科技(上海)有限公司 | 取代的杂芳环并二氢嘧啶酮衍生物，其制法与医药上的用途 |
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