PE20232038A1 - 3,4-dihidro-2,7-naftiridin-1,6(2h,7h)-dionas como inhibidores de mek - Google Patents
3,4-dihidro-2,7-naftiridin-1,6(2h,7h)-dionas como inhibidores de mekInfo
- Publication number
- PE20232038A1 PE20232038A1 PE2023002752A PE2023002752A PE20232038A1 PE 20232038 A1 PE20232038 A1 PE 20232038A1 PE 2023002752 A PE2023002752 A PE 2023002752A PE 2023002752 A PE2023002752 A PE 2023002752A PE 20232038 A1 PE20232038 A1 PE 20232038A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- naphthyridin
- dihydro
- mek inhibitors
- compounds
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La invencion se refiere a compuestos de Formula I en donde R1 es H, Br, C1-C6 alquilo o fenilo; R2 es H, halogeno o CH3-; R3 es hidroxiC1-C6 alquil- o (C3-C6 cicloalquil)C1-C6 alcoxi-; R4 es fenilo sustituido con 1,2 o 3 sustituyentes seleccionados de fluoroC1-C6 alcoxi o C1-C6 alquil- C(=O)-; y Ra y Rb se seleccionan independientemente de fluoroC1-C6 alquilo o C1-C6 alquil-C(=O)-. Los presentes compuestos se seleccionan de 8-((4-bromo-2-fluorofenil)amino)-2-ciclopropil-7-metil-3,4-dihidro-2,7-naftiridin-1,6(2H,7H)-diona. Asimismo, se mencionan composiciones farmaceuticas que comprenden dichos compuestos y al menos un excipiente farmaceuticamente aceptable, metodos y usos como inhibidores de MEK para el tratamiento del cancer. Tambien, refiere a formas solidas de 8-((2-fluoro-4-(metiltio)fenil)amino)-2-(2-hidroxietoxi)-7-metil-3,4-dihidro-2,7-naftiridin-1,6(2H,7H)-diona o sales de las mismas.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202163168456P | 2021-03-31 | 2021-03-31 | |
| US202263309346P | 2022-02-11 | 2022-02-11 | |
| PCT/IB2022/052952 WO2022208391A1 (en) | 2021-03-31 | 2022-03-30 | 3,4-dihydro-2,7-naphthyridine-1,6(2h,7h)-diones as mek inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20232038A1 true PE20232038A1 (es) | 2023-12-21 |
Family
ID=81308057
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2023002752A PE20232038A1 (es) | 2021-03-31 | 2022-03-30 | 3,4-dihidro-2,7-naftiridin-1,6(2h,7h)-dionas como inhibidores de mek |
Country Status (18)
| Country | Link |
|---|---|
| US (4) | US11802127B2 (es) |
| EP (1) | EP4313981A1 (es) |
| JP (1) | JP7466795B2 (es) |
| KR (1) | KR102681641B1 (es) |
| AU (1) | AU2022250102B2 (es) |
| CA (1) | CA3215293A1 (es) |
| CL (1) | CL2023002896A1 (es) |
| CO (1) | CO2023012682A2 (es) |
| CR (1) | CR20230455A (es) |
| DO (1) | DOP2023000208A (es) |
| EC (1) | ECSP23073404A (es) |
| IL (1) | IL305978A (es) |
| MX (1) | MX2023011628A (es) |
| PE (1) | PE20232038A1 (es) |
| TW (1) | TWI825637B (es) |
| UY (1) | UY39701A (es) |
| WO (1) | WO2022208391A1 (es) |
| ZA (1) | ZA202309566B (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI825637B (zh) * | 2021-03-31 | 2023-12-11 | 美商輝瑞股份有限公司 | 啶-1,6(2h,7h)-二酮 |
| BR112023019861A2 (pt) | 2021-03-31 | 2023-11-07 | Xinthera Inc | Inibidores de mk2 e usos dos mesmos |
| JP2024047569A (ja) * | 2022-09-26 | 2024-04-05 | ファイザー・インク | Mek阻害剤としての3,4-ジヒドロ-2,7-ナフチリジン-1,6(2h,7h)-ジオン |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| 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 |
| 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 |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| 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 |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
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| BRPI0413005A (pt) | 2003-07-29 | 2006-09-26 | Irm Llc | compostos e composições como inibidores da proteìna cinase |
| US7390820B2 (en) * | 2003-08-25 | 2008-06-24 | Amgen Inc. | Substituted quinolinone derivatives and methods of use |
| UA84175C2 (ru) | 2003-11-19 | 2008-09-25 | Аррей Байофарма Инк. | Гетероциклические ингибиторы мэк и их применение |
| KR100703068B1 (ko) | 2003-12-30 | 2007-04-05 | 에스케이케미칼주식회사 | 피리딘 유도체와 이의 제조방법, 및 이를 포함하는약제조성물 |
| EP1761528B1 (en) * | 2004-06-11 | 2008-01-09 | Japan Tobacco, Inc. | 5-amino-2,4,7-trioxo-3,4,7,8-tetrahydro-2h-pyrido[2,3-d]pyrimidine derivatives and related compounds for the treatment of cancer |
| AU2006299902B2 (en) | 2005-05-18 | 2012-11-01 | Array Biopharma Inc. | Heterocyclic inhibitors of MEK and methods of use thereof |
| ES2569677T3 (es) | 2006-03-16 | 2016-05-12 | Second Genome, Inc. | Compuestos bicicloheteroarilo como moduladores de P2X7 y usos de los mismos |
| DK1937643T3 (en) | 2006-03-16 | 2016-10-10 | Second Genome Inc | Bicycloheteroarylforbindelser som p2x7-modulatorer og anvendelser deraf |
| CA2645652A1 (en) | 2006-03-16 | 2007-09-27 | Renovis, Inc. | Bicycloheteroaryl compounds as p2x7 modulators and uses thereof |
| WO2007109201A2 (en) | 2006-03-16 | 2007-09-27 | Renovis, Inc. | Bicycloheteroaryl compounds as p2x7 modulators and uses thereof |
| US20100298285A1 (en) | 2006-03-16 | 2010-11-25 | Kelly Michael G | Biclycloheteroaryl Compounds as P2x7 Modulators and Uses Thereof |
| TWI464148B (zh) | 2006-03-16 | 2014-12-11 | Evotec Us Inc | 作為p2x7調節劑之雙環雜芳基化合物與其用途 |
| JO2985B1 (ar) * | 2006-12-20 | 2016-09-05 | Takeda Pharmaceuticals Co | مثبطات كينازmapk/erk |
| US8093265B2 (en) | 2007-03-09 | 2012-01-10 | Renovis, Inc. | Bicycloheteroaryl compounds as P2X7 modulators and uses thereof |
| JP5363350B2 (ja) * | 2007-03-19 | 2013-12-11 | 武田薬品工業株式会社 | Mapk/erkキナーゼ阻害剤 |
| TW200938542A (en) | 2008-02-01 | 2009-09-16 | Irm Llc | Compounds and compositions as kinase inhibitors |
| WO2009146034A2 (en) * | 2008-03-31 | 2009-12-03 | Takeda Pharmaceutical Company Limited | Mapk/erk kinase inhibitors and methods of use thereof |
| WO2013033981A1 (zh) * | 2011-09-06 | 2013-03-14 | 江苏先声药物研究有限公司 | 一类2,7-萘啶衍生物及其制备方法和应用 |
| TR201811976T4 (tr) | 2012-03-14 | 2018-09-21 | Lupin Ltd | Mek inhibitörleri olarak heterosiklil bileşikleri. |
| EP3094627B1 (en) | 2014-01-17 | 2018-08-22 | Novartis AG | 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2 |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| CN105899493B (zh) | 2014-01-17 | 2019-03-29 | 诺华股份有限公司 | 用于抑制shp2活性的1-(三嗪-3-基/哒嗪-3-基)-哌(-嗪)啶衍生物及其组合物 |
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| WO2019071351A1 (en) | 2017-10-12 | 2019-04-18 | Trillium Therapeutics Inc. | NOVEL 4-ARYLOXYQUINAZOLINE FLUORIN DERIVATIVES AS EGFR INHIBITORS USEFUL FOR THE TREATMENT OF CANCERS |
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| WO2020072492A1 (en) | 2018-10-02 | 2020-04-09 | Baruch S. Blumberg Institute | Benzamide derivatives as cgas-sting pathway agonists |
| CN114341124B (zh) | 2018-10-17 | 2024-09-20 | Array生物制药公司 | 蛋白质酪氨酸磷酸酶抑制剂 |
| CN113645964B (zh) | 2018-11-20 | 2024-10-11 | 恩福莱克逊治疗有限公司 | 用于胎记治疗的芳基苯胺和杂芳基苯胺化合物 |
| PE20220141A1 (es) | 2019-04-02 | 2022-01-27 | Array Biopharma Inc | Inhibidores de la proteina tirosina fosfatasa |
| TWI817018B (zh) | 2019-06-28 | 2023-10-01 | 美商艾瑞生藥股份有限公司 | 用於治療braf相關的疾病和失調症之化合物 |
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| TWI825637B (zh) * | 2021-03-31 | 2023-12-11 | 美商輝瑞股份有限公司 | 啶-1,6(2h,7h)-二酮 |
-
2022
- 2022-03-28 TW TW111111624A patent/TWI825637B/zh active
- 2022-03-29 UY UY0001039701A patent/UY39701A/es unknown
- 2022-03-30 IL IL305978A patent/IL305978A/en unknown
- 2022-03-30 JP JP2023559675A patent/JP7466795B2/ja active Active
- 2022-03-30 US US17/708,072 patent/US11802127B2/en active Active
- 2022-03-30 CR CR20230455A patent/CR20230455A/es unknown
- 2022-03-30 WO PCT/IB2022/052952 patent/WO2022208391A1/en not_active Ceased
- 2022-03-30 EP EP22716496.9A patent/EP4313981A1/en active Pending
- 2022-03-30 KR KR1020237032578A patent/KR102681641B1/ko active Active
- 2022-03-30 CA CA3215293A patent/CA3215293A1/en active Pending
- 2022-03-30 AU AU2022250102A patent/AU2022250102B2/en active Active
- 2022-03-30 MX MX2023011628A patent/MX2023011628A/es unknown
- 2022-03-30 PE PE2023002752A patent/PE20232038A1/es unknown
- 2022-12-01 US US18/060,864 patent/US11691973B2/en active Active
-
2023
- 2023-09-18 US US18/469,132 patent/US20240002384A1/en not_active Abandoned
- 2023-09-26 CO CONC2023/0012682A patent/CO2023012682A2/es unknown
- 2023-09-27 EC ECSENADI202373404A patent/ECSP23073404A/es unknown
- 2023-09-28 DO DO2023000208A patent/DOP2023000208A/es unknown
- 2023-09-28 CL CL2023002896A patent/CL2023002896A1/es unknown
- 2023-10-12 ZA ZA2023/09566A patent/ZA202309566B/en unknown
-
2025
- 2025-04-30 US US19/195,259 patent/US20250263411A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| KR20230146655A (ko) | 2023-10-19 |
| DOP2023000208A (es) | 2023-10-31 |
| JP7466795B2 (ja) | 2024-04-12 |
| US20240002384A1 (en) | 2024-01-04 |
| MX2023011628A (es) | 2023-10-13 |
| TWI825637B (zh) | 2023-12-11 |
| US20250263411A1 (en) | 2025-08-21 |
| EP4313981A1 (en) | 2024-02-07 |
| JP2024512624A (ja) | 2024-03-19 |
| CA3215293A1 (en) | 2022-10-06 |
| US11691973B2 (en) | 2023-07-04 |
| US11802127B2 (en) | 2023-10-31 |
| AU2022250102B2 (en) | 2024-05-16 |
| AU2022250102A1 (en) | 2023-10-05 |
| BR112023019849A2 (pt) | 2023-11-07 |
| US20220324861A1 (en) | 2022-10-13 |
| WO2022208391A1 (en) | 2022-10-06 |
| CO2023012682A2 (es) | 2023-10-09 |
| KR102681641B1 (ko) | 2024-07-05 |
| ZA202309566B (en) | 2024-06-26 |
| IL305978A (en) | 2023-11-01 |
| ECSP23073404A (es) | 2023-10-31 |
| TW202304903A (zh) | 2023-02-01 |
| CR20230455A (es) | 2024-01-08 |
| CL2023002896A1 (es) | 2024-02-02 |
| UY39701A (es) | 2022-10-31 |
| US20230120188A1 (en) | 2023-04-20 |
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