PE20220931A1 - Inhibidores de shp2 fosfatasa de tipo pirazolo[3,4-b]pirazina - Google Patents
Inhibidores de shp2 fosfatasa de tipo pirazolo[3,4-b]pirazinaInfo
- Publication number
- PE20220931A1 PE20220931A1 PE2022000239A PE2022000239A PE20220931A1 PE 20220931 A1 PE20220931 A1 PE 20220931A1 PE 2022000239 A PE2022000239 A PE 2022000239A PE 2022000239 A PE2022000239 A PE 2022000239A PE 20220931 A1 PE20220931 A1 PE 20220931A1
- Authority
- PE
- Peru
- Prior art keywords
- halogen
- hydrogen
- alkyl
- pyrazine
- pyrazolo
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 102000007607 Non-Receptor Type 11 Protein Tyrosine Phosphatase Human genes 0.000 title 1
- 108010032107 Non-Receptor Type 11 Protein Tyrosine Phosphatase Proteins 0.000 title 1
- 229910052736 halogen Inorganic materials 0.000 abstract 6
- 150000002367 halogens Chemical group 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 150000002431 hydrogen Chemical group 0.000 abstract 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 3
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- -1 pyrazine derivative compound Chemical class 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 101710204864 Tyrosine-protein phosphatase 2 Proteins 0.000 abstract 1
- 102100033019 Tyrosine-protein phosphatase non-receptor type 11 Human genes 0.000 abstract 1
- 101710116241 Tyrosine-protein phosphatase non-receptor type 11 Proteins 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
- A61K31/535—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
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4816—Wall or shell material
- A61K9/4825—Proteins, e.g. gelatin
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Biophysics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Biochemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La presente invencion se refiere a un compuesto derivado de pirazina de formula (I) o un tautomero o una sal farmaceuticamente aceptable del mismo, donde: R1 es hidrogeno o hidroxilo; R2 y R3 se seleccionan independientemente de hidrogeno, halogeno, alquilo C1-C4, haloalquilo C1-C4, hidroxialquilo C1-C4, CN; X es O o CR4R5; R4 y R5 se seleccionan independientemente de hidrogeno, halogeno, entre otros; R6 y R7 son hidrogeno, alcoxi C1-4 o halogeno, o R6 y R7 se unen para formar un anillo A opcionalmente sustituido por grupos R10; el anillo A es un anillo heterociclico de cinco miembros que contiene nitrogeno, O y S, entre otros; R8 es haloalquilo C1-4, CH3 y halogeno; R9 es hidrogeno, alquilo C1-4, haloalquilo C1-4 y halogeno; R10 es halogeno, ciano, hidroxilo, oxo, alquilo C1-4, entre otros. Tambien se refiere a una composicion farmaceutica y a un proceso de preparacion. Dicho compuesto es un inhibidor de la proteina tirosina fosfatasa 2 (SHP2), siendo util en el tratamiento del cancer.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1911928.8A GB201911928D0 (en) | 2019-08-20 | 2019-08-20 | Pharmaceutical compounds |
| PCT/IB2020/057815 WO2021033153A1 (en) | 2019-08-20 | 2020-08-20 | Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20220931A1 true PE20220931A1 (es) | 2022-05-31 |
Family
ID=68099585
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2022000239A PE20220931A1 (es) | 2019-08-20 | 2020-08-20 | Inhibidores de shp2 fosfatasa de tipo pirazolo[3,4-b]pirazina |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US12458640B2 (es) |
| EP (1) | EP4017855A1 (es) |
| JP (1) | JP7698629B2 (es) |
| KR (1) | KR20220049518A (es) |
| CN (1) | CN114206885B (es) |
| AU (1) | AU2020333251A1 (es) |
| BR (1) | BR112022003184A2 (es) |
| CA (1) | CA3148312A1 (es) |
| CL (1) | CL2022000271A1 (es) |
| CO (1) | CO2022001357A2 (es) |
| CR (1) | CR20220062A (es) |
| DO (1) | DOP2022000039A (es) |
| EC (1) | ECSP22011086A (es) |
| GB (1) | GB201911928D0 (es) |
| GE (2) | GEP20257767B (es) |
| IL (1) | IL289462A (es) |
| MX (1) | MX2022001908A (es) |
| PE (1) | PE20220931A1 (es) |
| PH (1) | PH12021553238A1 (es) |
| TN (1) | TN2022000039A1 (es) |
| WO (1) | WO2021033153A1 (es) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7326305B2 (ja) | 2018-03-02 | 2023-08-15 | 大塚製薬株式会社 | 医薬化合物 |
| EP3827009A4 (en) | 2018-07-24 | 2022-04-27 | Taiho Pharmaceutical Co., Ltd. | HETEROBICYCLIC COMPOUNDS TO INHIBIT SHP2 ACTIVITY |
| GB201911928D0 (en) | 2019-08-20 | 2019-10-02 | Otsuka Pharma Co Ltd | Pharmaceutical compounds |
| TW202214253A (zh) | 2020-06-18 | 2022-04-16 | 美商銳新醫藥公司 | 延遲、預防及治療對ｒａｓ抑制劑之後天抗性之方法 |
| EP4183395A4 (en) | 2020-07-15 | 2024-07-24 | Taiho Pharmaceutical Co., Ltd. | PYRIMIDINE COMPOUND-CONTAINING COMBINATION FOR USE IN TUMOR TREATMENT |
| IL301062A (en) | 2020-09-03 | 2023-05-01 | Revolution Medicines Inc | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| CR20230165A (es) | 2020-09-15 | 2023-06-02 | Revolution Medicines Inc | Derivados indólicos como inhibidores de ras en el tratamiento del cáncer |
| CN118561952A (zh) | 2021-05-05 | 2024-08-30 | 锐新医药公司 | Ras抑制剂 |
| CN117500811A (zh) | 2021-05-05 | 2024-02-02 | 锐新医药公司 | 共价ras抑制剂及其用途 |
| CR20230558A (es) | 2021-05-05 | 2024-01-24 | Revolution Medicines Inc | Inhibidores de ras para el tratamiento del cáncer |
| TW202313041A (zh) | 2021-06-09 | 2023-04-01 | 瑞士商諾華公司 | 包含達拉菲尼、曲美替尼和shp2抑制劑之三重藥物組合 |
| TW202317100A (zh) | 2021-06-23 | 2023-05-01 | 瑞士商諾華公司 | 包含ｋｒａｓ ｇ１２ｃ抑制劑的藥物組合及其用於治療癌症之用途 |
| WO2023280283A1 (zh) * | 2021-07-07 | 2023-01-12 | 浙江同源康医药股份有限公司 | 用作shp2抑制剂的化合物及其应用 |
| TW202327569A (zh) | 2021-09-01 | 2023-07-16 | 瑞士商諾華公司 | 包含ｔｅａｄ抑制劑的藥物組合及其用於癌症治療之用途 |
| WO2023051648A1 (zh) * | 2021-09-28 | 2023-04-06 | 甘李药业股份有限公司 | 可用作shp2抑制剂的化合物及其制备方法和用途 |
| US20250059206A1 (en) * | 2021-09-29 | 2025-02-20 | Yull XIE | Fused ring compound acting as shp2 inhibitor |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| JP2025510572A (ja) | 2022-03-08 | 2025-04-15 | レボリューション メディシンズ インコーポレイテッド | 免疫不応性肺癌を治療するための方法 |
| IL316768A (en) | 2022-05-25 | 2025-01-01 | Ikena Oncology Inc | MEK inhibitors and their uses |
| EP4536364A1 (en) | 2022-06-10 | 2025-04-16 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| CN117384187A (zh) * | 2022-09-30 | 2024-01-12 | 轩竹生物科技股份有限公司 | 泛素特异性蛋白酶1抑制剂 |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| AR132338A1 (es) | 2023-04-07 | 2025-06-18 | Revolution Medicines Inc | Inhibidores de ras |
| WO2024211712A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| KR20250172857A (ko) | 2023-04-14 | 2025-12-09 | 레볼루션 메디슨즈, 인크. | Ras 억제제의 결정형 |
| AU2024252105A1 (en) | 2023-04-14 | 2025-10-16 | Revolution Medicines, Inc. | Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| KR20250014691A (ko) | 2023-07-21 | 2025-02-03 | 대한민국(질병관리청 국립보건연구원장) | 피라졸로[1,5-에이]퀴나졸린 유도체 화합물을 포함하는 인간면역결핍바이러스 억제용 조성물 |
| 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 |
| TW202515582A (zh) | 2023-08-24 | 2025-04-16 | 日商大塚製藥股份有限公司 | 西區嘧啶(cedazuridine)之固定劑量組合 |
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2019
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2020
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| Publication number | Publication date |
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| US12458640B2 (en) | 2025-11-04 |
| EP4017855A1 (en) | 2022-06-29 |
| CN114206885A (zh) | 2022-03-18 |
| TW202124383A (zh) | 2021-07-01 |
| ECSP22011086A (es) | 2022-03-31 |
| TN2022000039A1 (en) | 2023-10-09 |
| MX2022001908A (es) | 2022-04-18 |
| CR20220062A (es) | 2022-04-20 |
| BR112022003184A2 (pt) | 2022-05-17 |
| WO2021033153A1 (en) | 2021-02-25 |
| CL2022000271A1 (es) | 2022-10-28 |
| IL289462A (en) | 2022-02-01 |
| GEAP202515878A (en) | 2025-01-17 |
| GB201911928D0 (en) | 2019-10-02 |
| JP2022546213A (ja) | 2022-11-04 |
| US20230049719A1 (en) | 2023-02-16 |
| CO2022001357A2 (es) | 2022-03-18 |
| AU2020333251A1 (en) | 2022-02-17 |
| CA3148312A1 (en) | 2021-02-25 |
| PH12021553238A1 (en) | 2023-02-20 |
| DOP2022000039A (es) | 2022-06-15 |
| KR20220049518A (ko) | 2022-04-21 |
| JP7698629B2 (ja) | 2025-06-25 |
| CN114206885B (zh) | 2025-05-02 |
| GEP20257767B (en) | 2025-05-27 |
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