AR120700A1 - Inhibidores de kras g12c - Google Patents
Inhibidores de kras g12cInfo
- Publication number
- AR120700A1 AR120700A1 ARP200103420A ARP200103420A AR120700A1 AR 120700 A1 AR120700 A1 AR 120700A1 AR P200103420 A ARP200103420 A AR P200103420A AR P200103420 A ARP200103420 A AR P200103420A AR 120700 A1 AR120700 A1 AR 120700A1
- Authority
- AR
- Argentina
- Prior art keywords
- kras
- inhibitors
- compounds
- benzooxazepine
- krasg12c
- Prior art date
Links
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)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (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)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Compuestos derivados de tetrahidro o hexahidropirazino-benzooxazepina como inhibidores de KRas, en particular del KRasG12C, composición farmacéutica que comprende a uno de esos compuestos y el uso de los mismos para el tratamiento del cáncer. Reivindicación 1: Un compuesto de la fórmula (1) en donde: A es -OCH₂-, -N(R⁶)CH₂, -OCH₂CH₂-, -N(R⁶)CH₂CH₂-, -CH₂OCH₂-, o - CH₂N(R⁶)CH₂-; B es -CH₂- o -C(O)-; Y es -C(CN)- o -N-; R¹ es -CN, -C(O)C&
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962946586P | 2019-12-11 | 2019-12-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR120700A1 true AR120700A1 (es) | 2022-03-09 |
Family
ID=74106135
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP200103420A AR120700A1 (es) | 2019-12-11 | 2020-12-09 | Inhibidores de kras g12c |
Country Status (31)
| Country | Link |
|---|---|
| US (2) | US11731984B2 (es) |
| EP (1) | EP3886991B1 (es) |
| JP (1) | JP7023421B2 (es) |
| KR (1) | KR102546592B1 (es) |
| CN (2) | CN114828964B (es) |
| AR (1) | AR120700A1 (es) |
| AU (2) | AU2020402701B2 (es) |
| BR (1) | BR112022009557A2 (es) |
| CA (1) | CA3161162A1 (es) |
| CL (1) | CL2022001513A1 (es) |
| CO (1) | CO2022008091A2 (es) |
| CR (1) | CR20220258A (es) |
| DK (1) | DK3886991T3 (es) |
| DO (1) | DOP2022000117A (es) |
| EC (1) | ECSP22046699A (es) |
| ES (1) | ES2929700T3 (es) |
| HR (1) | HRP20221301T1 (es) |
| HU (1) | HUE060684T2 (es) |
| IL (2) | IL293394B2 (es) |
| JO (1) | JOP20220142A1 (es) |
| LT (1) | LT3886991T (es) |
| MA (1) | MA54327B1 (es) |
| MD (1) | MD3886991T2 (es) |
| MX (1) | MX2022006986A (es) |
| PE (1) | PE20230238A1 (es) |
| PL (1) | PL3886991T3 (es) |
| PT (1) | PT3886991T (es) |
| RS (1) | RS63719B1 (es) |
| SI (1) | SI3886991T1 (es) |
| TW (1) | TWI765448B (es) |
| WO (1) | WO2021118877A1 (es) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4051678A1 (en) | 2019-10-28 | 2022-09-07 | Merck Sharp & Dohme Corp. | Small molecule inhibitors of kras g12c mutant |
| KR20230019462A (ko) | 2020-06-02 | 2023-02-08 | 베링거 인겔하임 인터내셔날 게엠베하 | 암 치료용 고리형 2-아미노-3-시아노 티오펜 및 유도체 |
| EP4208261A1 (en) | 2020-09-03 | 2023-07-12 | Revolution Medicines, Inc. | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| 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 |
| WO2023008462A1 (ja) | 2021-07-27 | 2023-02-02 | 東レ株式会社 | 癌の治療及び／又は予防のための医薬品 |
| WO2023099623A1 (en) * | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| WO2023099612A1 (en) * | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| WO2023099620A1 (en) * | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | Kras degrading compounds comprising annulated 2-amino-3-cyano thiophenes |
| TW202337431A (zh) * | 2021-12-01 | 2023-10-01 | 德商百靈佳殷格翰國際股份有限公司 | 用於治療癌症之環狀2-胺基-3-氰基噻吩及衍生物 |
| WO2023099592A1 (en) * | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| 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 |
| 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 |
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 |
| UA119971C2 (uk) | 2013-10-10 | 2019-09-10 | Араксіс Фарма Ллк | Інгібітори g12c kras |
| TWI659021B (zh) | 2013-10-10 | 2019-05-11 | 亞瑞克西斯製藥公司 | Ｋｒａｓ ｇ１２ｃ之抑制劑 |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| US10246424B2 (en) | 2015-04-10 | 2019-04-02 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| TW201906848A (zh) | 2017-05-11 | 2019-02-16 | 瑞典商阿斯特捷利康公司 | 化學化合物 |
| WO2019051084A1 (en) | 2017-09-07 | 2019-03-14 | Revolution Medicines, Inc. | SHP2 INHIBITOR COMPOSITIONS AND METHODS OF TREATING CANCER |
| ES2928576T3 (es) | 2017-09-08 | 2022-11-21 | Amgen Inc | Inhibidores de KRAS G12C y métodos de uso de los mismos |
| EA202091186A1 (ru) | 2017-11-15 | 2020-10-01 | Мирати Терапьютикс, Инк. | ИНГИБИТОРЫ KRas G12C |
| 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 |
| SG11202109451TA (en) * | 2019-03-05 | 2021-09-29 | 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 |
-
2020
- 2020-12-04 HU HUE20834024A patent/HUE060684T2/hu unknown
- 2020-12-04 AU AU2020402701A patent/AU2020402701B2/en active Active
- 2020-12-04 CN CN202080085553.5A patent/CN114828964B/zh active Active
- 2020-12-04 JP JP2021539866A patent/JP7023421B2/ja active Active
- 2020-12-04 ES ES20834024T patent/ES2929700T3/es active Active
- 2020-12-04 JO JOP/2022/0142A patent/JOP20220142A1/ar unknown
- 2020-12-04 SI SI202030102T patent/SI3886991T1/sl unknown
- 2020-12-04 HR HRP20221301TT patent/HRP20221301T1/hr unknown
- 2020-12-04 CR CR20220258A patent/CR20220258A/es unknown
- 2020-12-04 CA CA3161162A patent/CA3161162A1/en active Pending
- 2020-12-04 MX MX2022006986A patent/MX2022006986A/es unknown
- 2020-12-04 BR BR112022009557A patent/BR112022009557A2/pt unknown
- 2020-12-04 CN CN202311816497.XA patent/CN117820333A/zh active Pending
- 2020-12-04 LT LTEPPCT/US2020/063272T patent/LT3886991T/lt unknown
- 2020-12-04 MD MDE20210978T patent/MD3886991T2/ro unknown
- 2020-12-04 PE PE2022001047A patent/PE20230238A1/es unknown
- 2020-12-04 IL IL293394A patent/IL293394B2/en unknown
- 2020-12-04 PL PL20834024.0T patent/PL3886991T3/pl unknown
- 2020-12-04 TW TW109142894A patent/TWI765448B/zh active
- 2020-12-04 DK DK20834024.0T patent/DK3886991T3/da active
- 2020-12-04 WO PCT/US2020/063272 patent/WO2021118877A1/en active Application Filing
- 2020-12-04 EP EP20834024.0A patent/EP3886991B1/en active Active
- 2020-12-04 RS RS20220956A patent/RS63719B1/sr unknown
- 2020-12-04 KR KR1020227019240A patent/KR102546592B1/ko active IP Right Grant
- 2020-12-04 US US17/111,676 patent/US11731984B2/en active Active
- 2020-12-04 PT PT208340240T patent/PT3886991T/pt unknown
- 2020-12-04 MA MA54327A patent/MA54327B1/fr unknown
- 2020-12-09 AR ARP200103420A patent/AR120700A1/es unknown
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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
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2023
- 2023-06-28 US US18/343,326 patent/US20230339968A1/en active Pending
- 2023-07-17 IL IL304534A patent/IL304534A/en unknown
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2024
- 2024-04-18 AU AU2024202573A patent/AU2024202573A1/en active Pending
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