BR112022009557A2 - Inibidores de kras g12c - Google Patents
Inibidores de kras g12cInfo
- Publication number
- BR112022009557A2 BR112022009557A2 BR112022009557A BR112022009557A BR112022009557A2 BR 112022009557 A2 BR112022009557 A2 BR 112022009557A2 BR 112022009557 A BR112022009557 A BR 112022009557A BR 112022009557 A BR112022009557 A BR 112022009557A BR 112022009557 A2 BR112022009557 A2 BR 112022009557A2
- Authority
- BR
- Brazil
- Prior art keywords
- kras
- inhibitors
- compounds
- salts
- formula
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 102200006538 rs121913530 Human genes 0.000 title abstract 2
- 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
INIBIDORES DE KRAS G12C. A presente invenção refere-se a compostos da fórmula, na qual R1, R2, R3, R4, R5, A, B e Y são tal como descritos no presente documento, seus sais farmaceuticamente aceitáveis, e métodos de uso destes compostos e sais para o tratamento de pacientes para o câncer.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962946586P | 2019-12-11 | 2019-12-11 | |
| PCT/US2020/063272 WO2021118877A1 (en) | 2019-12-11 | 2020-12-04 | Kras g12c inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112022009557A2 true BR112022009557A2 (pt) | 2022-08-02 |
Family
ID=74106135
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112022009557A BR112022009557A2 (pt) | 2019-12-11 | 2020-12-04 | Inibidores de kras g12c |
Country Status (32)
| Country | Link |
|---|---|
| US (2) | US11731984B2 (pt) |
| EP (1) | EP3886991B1 (pt) |
| JP (1) | JP7023421B2 (pt) |
| KR (1) | KR102546592B1 (pt) |
| CN (2) | CN117820333A (pt) |
| AR (1) | AR120700A1 (pt) |
| AU (2) | AU2020402701B2 (pt) |
| BR (1) | BR112022009557A2 (pt) |
| CA (1) | CA3161162A1 (pt) |
| CL (1) | CL2022001513A1 (pt) |
| CO (1) | CO2022008091A2 (pt) |
| CR (1) | CR20220258A (pt) |
| DK (1) | DK3886991T3 (pt) |
| DO (1) | DOP2022000117A (pt) |
| EC (1) | ECSP22046699A (pt) |
| ES (1) | ES2929700T3 (pt) |
| HR (1) | HRP20221301T1 (pt) |
| HU (1) | HUE060684T2 (pt) |
| IL (2) | IL293394B2 (pt) |
| JO (1) | JOP20220142A1 (pt) |
| LT (1) | LT3886991T (pt) |
| MA (1) | MA54327B1 (pt) |
| MD (1) | MD3886991T2 (pt) |
| MX (1) | MX2022006986A (pt) |
| PE (1) | PE20230238A1 (pt) |
| PL (1) | PL3886991T3 (pt) |
| PT (1) | PT3886991T (pt) |
| RS (1) | RS63719B1 (pt) |
| SA (1) | SA522432955B1 (pt) |
| SI (1) | SI3886991T1 (pt) |
| TW (1) | TWI765448B (pt) |
| WO (1) | WO2021118877A1 (pt) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7451419B2 (ja) | 2018-10-26 | 2024-03-18 | 大鵬薬品工業株式会社 | 新規なインダゾール化合物又はその塩 |
| IL292438A (en) | 2019-10-28 | 2022-06-01 | Merck Sharp & Dohme | Small molecules that inhibit the g12c mutant of kras |
| 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 |
| AU2021285032A1 (en) | 2020-06-02 | 2022-12-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| WO2022060583A1 (en) | 2020-09-03 | 2022-03-24 | Revolution Medicines, Inc. | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| CN114437107A (zh) * | 2020-11-06 | 2022-05-06 | 江苏先声药业有限公司 | 哌嗪类化合物及其应用 |
| US20230107642A1 (en) | 2020-12-18 | 2023-04-06 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| WO2022266206A1 (en) | 2021-06-16 | 2022-12-22 | Erasca, Inc. | Kras inhibitor conjugates |
| KR20240041917A (ko) | 2021-07-27 | 2024-04-01 | 도레이 카부시키가이샤 | 암의 치료 및/또는 예방을 위한 의약품 |
| CA3234517A1 (en) | 2021-10-22 | 2023-04-27 | Xin Li | Nitrogen-containing tetracyclic compound, preparation method therefor, and medical use thereof |
| IL312905A (en) | 2021-12-01 | 2024-07-01 | Boehringer Ingelheim Int | 2-amino-3-cyano ring thiophenes and history for cancer therapy |
| EP4441051A1 (en) * | 2021-12-01 | 2024-10-09 | Boehringer Ingelheim International GmbH | Kras degrading compounds comprising annulated 2-amino-3-cyano thiophenes |
| EP4441050A1 (en) * | 2021-12-01 | 2024-10-09 | Boehringer Ingelheim International GmbH | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| EP4441053A1 (en) * | 2021-12-01 | 2024-10-09 | Boehringer Ingelheim International GmbH | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| CN118574836A (zh) * | 2021-12-01 | 2024-08-30 | 勃林格殷格翰国际有限公司 | 用于治疗癌症的环状2-胺基-3-氰基噻吩及衍生物 |
| WO2023122662A1 (en) | 2021-12-22 | 2023-06-29 | The Regents Of The University Of California | Covalently binding inhibitors of g12s, g12d and/or g12e mutants of k-ras gtpase |
| TW202333800A (zh) | 2021-12-28 | 2023-09-01 | 英商阿斯特捷利康英國股份有限公司 | 抗體-藥物結合物及rasg12c抑制劑之組合 |
| WO2023168036A1 (en) * | 2022-03-04 | 2023-09-07 | Eli Lilly And Company | Method of treatment including kras g12c inhibitors and shp2 inhibitors |
| US20240043451A1 (en) | 2022-03-25 | 2024-02-08 | Eli Lilly And Company | Kras inhibitors |
| WO2023196959A1 (en) | 2022-04-07 | 2023-10-12 | Eli Lilly And Company | Process for making a kras g12c inhibitor |
| WO2023196887A1 (en) | 2022-04-08 | 2023-10-12 | Eli Lilly And Company | Method of treatment including kras g12c inhibitors and aurora a inhibitors |
| WO2023205701A1 (en) | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| US20240108618A1 (en) | 2022-06-30 | 2024-04-04 | Eli Lilly And Company | Kras g12c inhibitor dosing regimens |
| WO2024031088A1 (en) | 2022-08-05 | 2024-02-08 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| WO2024040131A1 (en) | 2022-08-17 | 2024-02-22 | Treeline Biosciences, Inc. | Pyridopyrimidine kras inhibitors |
| GB202212641D0 (en) | 2022-08-31 | 2022-10-12 | Jazz Pharmaceuticals Ireland Ltd | Novel compounds |
| WO2024081674A1 (en) | 2022-10-11 | 2024-04-18 | Aadi Bioscience, Inc. | Combination therapies for the treatment of cancer |
| WO2024112654A1 (en) | 2022-11-21 | 2024-05-30 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| US20240343736A1 (en) | 2023-03-30 | 2024-10-17 | Eli Lilly And Company | Kras inhibitors |
| WO2024206766A1 (en) | 2023-03-31 | 2024-10-03 | Eli Lilly And Company | Kras inhibitors |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008007661A1 (fr) * | 2006-07-11 | 2008-01-17 | Takeda Pharmaceutical Company Limited | Composé hétérocyclique tricycique et son utilisation |
| JO3805B1 (ar) * | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | مثبطات كراس جي12سي |
| KR20160076519A (ko) | 2013-10-10 | 2016-06-30 | 아락세스 파마 엘엘씨 | Kras g12c 억제제 |
| JO3556B1 (ar) * | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| CN107849022A (zh) * | 2015-04-10 | 2018-03-27 | 亚瑞克西斯制药公司 | 取代的喹唑啉化合物和其使用方法 |
| TW201906848A (zh) * | 2017-05-11 | 2019-02-16 | 瑞典商阿斯特捷利康公司 | 化學化合物 |
| EP3678703A1 (en) | 2017-09-07 | 2020-07-15 | Revolution Medicines, Inc. | Shp2 inhibitor compositions and methods for treating cancer |
| EP4403175A3 (en) * | 2017-09-08 | 2024-10-02 | Amgen Inc. | Inhibitors of kras g12c and methods of using the same |
| LT3710439T (lt) * | 2017-11-15 | 2023-05-10 | Mirati Therapeutics, Inc. | Kras g12c inhibitoriai |
| TW202012415A (zh) * | 2018-05-08 | 2020-04-01 | 瑞典商阿斯特捷利康公司 | 化學化合物 |
| AR116604A1 (es) | 2018-10-15 | 2021-05-26 | Lilly Co Eli | Inhibidores de kras g12c |
| BR112021017408A2 (pt) | 2019-03-05 | 2022-01-18 | Astrazeneca Ab | Compostos tricíclicos fundidos úteis como agentes anticancerosos |
| 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 |
-
2020
- 2020-12-04 ES ES20834024T patent/ES2929700T3/es active Active
- 2020-12-04 BR BR112022009557A patent/BR112022009557A2/pt active Search and Examination
- 2020-12-04 PT PT208340240T patent/PT3886991T/pt unknown
- 2020-12-04 HU HUE20834024A patent/HUE060684T2/hu unknown
- 2020-12-04 JP JP2021539866A patent/JP7023421B2/ja active Active
- 2020-12-04 IL IL293394A patent/IL293394B2/en unknown
- 2020-12-04 JO JOP/2022/0142A patent/JOP20220142A1/ar unknown
- 2020-12-04 CR CR20220258A patent/CR20220258A/es unknown
- 2020-12-04 MA MA54327A patent/MA54327B1/fr unknown
- 2020-12-04 MD MDE20210978T patent/MD3886991T2/ro unknown
- 2020-12-04 US US17/111,676 patent/US11731984B2/en active Active
- 2020-12-04 KR KR1020227019240A patent/KR102546592B1/ko active IP Right Grant
- 2020-12-04 TW TW109142894A patent/TWI765448B/zh active
- 2020-12-04 EP EP20834024.0A patent/EP3886991B1/en active Active
- 2020-12-04 PE PE2022001047A patent/PE20230238A1/es unknown
- 2020-12-04 PL PL20834024.0T patent/PL3886991T3/pl unknown
- 2020-12-04 SI SI202030102T patent/SI3886991T1/sl unknown
- 2020-12-04 DK DK20834024.0T patent/DK3886991T3/da active
- 2020-12-04 MX MX2022006986A patent/MX2022006986A/es unknown
- 2020-12-04 WO PCT/US2020/063272 patent/WO2021118877A1/en active Application Filing
- 2020-12-04 AU AU2020402701A patent/AU2020402701B2/en active Active
- 2020-12-04 HR HRP20221301TT patent/HRP20221301T1/hr unknown
- 2020-12-04 CN CN202311816497.XA patent/CN117820333A/zh active Pending
- 2020-12-04 CN CN202080085553.5A patent/CN114828964B/zh active Active
- 2020-12-04 LT LTEPPCT/US2020/063272T patent/LT3886991T/lt unknown
- 2020-12-04 RS RS20220956A patent/RS63719B1/sr unknown
- 2020-12-04 CA CA3161162A patent/CA3161162A1/en active Pending
- 2020-12-09 AR ARP200103420A patent/AR120700A1/es unknown
-
2022
- 2022-06-07 CO CONC2022/0008091A patent/CO2022008091A2/es unknown
- 2022-06-07 DO DO2022000117A patent/DOP2022000117A/es unknown
- 2022-06-08 CL CL2022001513A patent/CL2022001513A1/es unknown
- 2022-06-10 EC ECSENADI202246699A patent/ECSP22046699A/es unknown
- 2022-06-12 SA SA522432955A patent/SA522432955B1/ar unknown
-
2023
- 2023-06-28 US US18/343,326 patent/US20230339968A1/en active Pending
- 2023-07-17 IL IL304534A patent/IL304534A/en unknown
-
2024
- 2024-04-18 AU AU2024202573A patent/AU2024202573A1/en active Pending
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