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
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 102200006538 rs121913530 Human genes 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 abstract 1
- -1 hexahydropyrazino-benzooxazepine Chemical compound 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 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)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Microbiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Endocrinology (AREA)
- Mycology (AREA)
- Inorganic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (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 (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020085493A1 (ja) | 2018-10-26 | 2020-04-30 | 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 |
| JP7340100B2 (ja) | 2019-10-28 | 2023-09-06 | メルク・シャープ・アンド・ドーム・エルエルシー | Ｋｒａｓ ｇ１２ｃ変異型の小分子阻害薬 |
| 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 |
| IL298633A (en) | 2020-06-02 | 2023-01-01 | Boehringer Ingelheim Int | Cyclic 2-amino-3-cyanothiophenes and their implications for cancer therapy |
| CA3187757A1 (en) | 2020-09-03 | 2022-03-24 | Ethan AHLER | 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 |
| WO2022133345A1 (en) | 2020-12-18 | 2022-06-23 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| WO2022266206A1 (en) | 2021-06-16 | 2022-12-22 | Erasca, Inc. | Kras inhibitor conjugates |
| MX2024000965A (es) | 2021-07-27 | 2024-02-09 | Toray Industries | Medicamento para el tratamiento y/o prevencion de cancer. |
| TW202322819A (zh) | 2021-10-22 | 2023-06-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 含氮的四環化合物、其製備方法及其在醫藥上的應用 |
| CN118591540A (zh) * | 2021-12-01 | 2024-09-03 | 勃林格殷格翰国际有限公司 | 包含环状2-氨基-3-氰基噻吩的kras降解化合物 |
| 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 |
| WO2023099624A1 (en) * | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| TW202340209A (zh) * | 2021-12-01 | 2023-10-16 | 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 |
| TW202340202A (zh) | 2021-12-22 | 2023-10-16 | 美國加利福尼亞大學董事會 | Gtp酶抑制劑及其用途 |
| 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 |
| 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 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090318412A1 (en) * | 2006-07-11 | 2009-12-24 | Takahiro Matsumoto | Tricyclic heterocyclic compound and use thereof |
| JO3805B1 (ar) * | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | مثبطات كراس جي12سي |
| EP3055290B1 (en) | 2013-10-10 | 2019-10-02 | Araxes Pharma LLC | Inhibitors of kras g12c |
| JO3556B1 (ar) * | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| KR20180005178A (ko) * | 2015-04-10 | 2018-01-15 | 아락세스 파마 엘엘씨 | 치환된 퀴나졸린 화합물 및 이의 사용방법 |
| EP3621968A1 (en) | 2017-05-11 | 2020-03-18 | Astrazeneca AB | Heteroaryl compounds that inhibit g12c mutant ras proteins |
| JP7356414B2 (ja) | 2017-09-07 | 2023-10-04 | レヴォリューション・メディスンズ，インコーポレイテッド | がんを治療するためのｓｈｐ２阻害剤組成物および方法 |
| CA3075046A1 (en) * | 2017-09-08 | 2019-03-14 | Amgen Inc. | Inhibitors of kras g12c and methods of using the same |
| HRP20230377T1 (hr) * | 2017-11-15 | 2023-06-23 | Mirati Therapeutics, Inc. | Inhibitori mutacije 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 |
| 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 |
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2020
- 2020-12-04 CN CN202080085553.5A patent/CN114828964B/zh active Active
- 2020-12-04 KR KR1020227019240A patent/KR102546592B1/ko active IP Right Grant
- 2020-12-04 EP EP20834024.0A patent/EP3886991B1/en active Active
- 2020-12-04 TW TW109142894A patent/TWI765448B/zh active
- 2020-12-04 RS RS20220956A patent/RS63719B1/sr unknown
- 2020-12-04 AU AU2020402701A patent/AU2020402701B2/en active Active
- 2020-12-04 MD MDE20210978T patent/MD3886991T2/ro unknown
- 2020-12-04 CR CR20220258A patent/CR20220258A/es unknown
- 2020-12-04 US US17/111,676 patent/US11731984B2/en active Active
- 2020-12-04 CA CA3161162A patent/CA3161162A1/en active Pending
- 2020-12-04 PT PT208340240T patent/PT3886991T/pt unknown
- 2020-12-04 SI SI202030102T patent/SI3886991T1/sl unknown
- 2020-12-04 HU HUE20834024A patent/HUE060684T2/hu unknown
- 2020-12-04 LT LTEPPCT/US2020/063272T patent/LT3886991T/lt unknown
- 2020-12-04 MX MX2022006986A patent/MX2022006986A/es unknown
- 2020-12-04 MA MA54327A patent/MA54327B1/fr unknown
- 2020-12-04 JO JOP/2022/0142A patent/JOP20220142A1/ar unknown
- 2020-12-04 IL IL293394A patent/IL293394B2/en unknown
- 2020-12-04 WO PCT/US2020/063272 patent/WO2021118877A1/en active Application Filing
- 2020-12-04 PE PE2022001047A patent/PE20230238A1/es unknown
- 2020-12-04 ES ES20834024T patent/ES2929700T3/es active Active
- 2020-12-04 HR HRP20221301TT patent/HRP20221301T1/hr unknown
- 2020-12-04 BR BR112022009557A patent/BR112022009557A2/pt active Search and Examination
- 2020-12-04 PL PL20834024.0T patent/PL3886991T3/pl unknown
- 2020-12-04 JP JP2021539866A patent/JP7023421B2/ja active Active
- 2020-12-04 DK DK20834024.0T patent/DK3886991T3/da active
- 2020-12-04 CN CN202311816497.XA patent/CN117820333A/zh active Pending
- 2020-12-09 AR ARP200103420A patent/AR120700A1/es unknown
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2022
- 2022-06-07 DO DO2022000117A patent/DOP2022000117A/es unknown
- 2022-06-07 CO CONC2022/0008091A patent/CO2022008091A2/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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