CN110831939B - 作为erk1/2抑制剂的6-嘧啶-异吲哚衍生物 - Google Patents
作为erk1/2抑制剂的6-嘧啶-异吲哚衍生物 Download PDFInfo
- Publication number
- CN110831939B CN110831939B CN201880024602.7A CN201880024602A CN110831939B CN 110831939 B CN110831939 B CN 110831939B CN 201880024602 A CN201880024602 A CN 201880024602A CN 110831939 B CN110831939 B CN 110831939B
- Authority
- CN
- China
- Prior art keywords
- compound
- isoindol
- dihydro
- oxo
- pyrimidin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero 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
- A61K31/506—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
- 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
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Dermatology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1706327.2A GB201706327D0 (en) | 2017-04-20 | 2017-04-20 | A pharmaceutical compound |
| GB1706327.2 | 2017-04-20 | ||
| PCT/IB2018/052745 WO2018193410A1 (en) | 2017-04-20 | 2018-04-20 | 6-pyrimidin-isoindole derivative as erk1/2 inhibitor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN110831939A CN110831939A (zh) | 2020-02-21 |
| CN110831939B true CN110831939B (zh) | 2025-05-09 |
Family
ID=58795788
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201880024602.7A Active CN110831939B (zh) | 2017-04-20 | 2018-04-20 | 作为erk1/2抑制剂的6-嘧啶-异吲哚衍生物 |
Country Status (21)
| Country | Link |
|---|---|
| US (3) | US11142518B2 (enExample) |
| EP (1) | EP3612524B1 (enExample) |
| JP (1) | JP7113846B2 (enExample) |
| KR (1) | KR102652193B1 (enExample) |
| CN (1) | CN110831939B (enExample) |
| AU (1) | AU2018255935B2 (enExample) |
| CA (1) | CA3059674A1 (enExample) |
| DK (1) | DK3612524T3 (enExample) |
| ES (1) | ES2994283T3 (enExample) |
| FI (1) | FI3612524T3 (enExample) |
| GB (1) | GB201706327D0 (enExample) |
| IL (1) | IL269803B (enExample) |
| MA (1) | MA52123A (enExample) |
| MX (1) | MX2019012471A (enExample) |
| MY (1) | MY203722A (enExample) |
| PH (1) | PH12019502154A1 (enExample) |
| SA (1) | SA519410253B1 (enExample) |
| SG (1) | SG11201909189QA (enExample) |
| TW (1) | TWI813566B (enExample) |
| WO (1) | WO2018193410A1 (enExample) |
| ZA (1) | ZA201907484B (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017068412A1 (en) | 2015-10-21 | 2017-04-27 | Otsuka Pharmaceutical Co., Ltd. | Benzolactam compounds as protein kinase inhibitors |
| GB201706327D0 (en) | 2017-04-20 | 2017-06-07 | Otsuka Pharma Co Ltd | A pharmaceutical compound |
| AU2019226480B2 (en) | 2018-03-02 | 2022-12-15 | Otsuka Pharmaceutical Co., Ltd. | Pharmaceutical compounds |
| EP3827009A4 (en) | 2018-07-24 | 2022-04-27 | Taiho Pharmaceutical Co., Ltd. | HETEROBICYCLIC COMPOUNDS TO INHIBIT SHP2 ACTIVITY |
| CN109608444B (zh) * | 2018-11-27 | 2022-02-11 | 中国药科大学 | 含异吲哚啉酮的erk抑制剂及其制备方法与用途 |
| GB201911928D0 (en) | 2019-08-20 | 2019-10-02 | Otsuka Pharma Co Ltd | Pharmaceutical compounds |
| EP4093406A4 (en) * | 2020-01-24 | 2024-02-28 | Taiho Pharmaceutical Co., Ltd. | IMPROVEMENT OF THE ANTI-TUMORAL ACTIVITY OF SHP2 INHIBITOR PYRIMIDINONE IN COMBINATION WITH NEW ANTI-CANCER DRUGS AGAINST CANCER |
| AU2021262977B2 (en) * | 2020-04-30 | 2023-07-13 | Suzhou Genhouse Bio Co., Ltd. | Compounds containing benzosultam |
| CN113967198A (zh) * | 2020-07-24 | 2022-01-25 | 鲁南制药集团股份有限公司 | 一种甾体cyp17抑制剂胶囊及其制备方法 |
| JP2023538137A (ja) * | 2020-08-21 | 2023-09-06 | シャンハイ リンジーン バイオファーマ カンパニー リミテッド | 芳香環ラクタム系化合物、その製造方法及び使用 |
| CA3222540A1 (en) | 2021-06-11 | 2022-12-15 | Otsuka Pharmaceutical Co., Ltd. | Process for preparing an erk inhibitor |
| US11931370B2 (en) * | 2021-10-08 | 2024-03-19 | Slayback Pharma Llc | Stable pharmaceutical compositions of cyclophosphamide |
| US20240415835A1 (en) * | 2021-10-26 | 2024-12-19 | Otsuka Pharmaceutical Co., Ltd. | Compositions comprising an erk inhibitor |
| CN114085213B (zh) * | 2022-01-20 | 2022-03-25 | 苏州国匡医药科技有限公司 | 一种arv-471的制备方法 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108617166A (zh) * | 2015-10-21 | 2018-10-02 | 大冢制药株式会社 | 蛋白激酶抑制剂苯并内酰胺化合物 |
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| JP2003504301A (ja) | 1998-04-01 | 2003-02-04 | ブリストル−マイヤーズ スクイブ ファーマ カンパニー | インテグリンアンタゴニスト |
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| EP1618094B1 (en) | 2003-04-30 | 2007-09-05 | The Institutes for Pharmaceutical Discovery, LLC | Substituted heteroaryls as inhibitors of protein tyrosine phosphatases |
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| DK3307727T3 (da) * | 2015-06-15 | 2024-01-08 | Asana Biosciences Llc | Heterocykliske inhibitorer af erk1 og erk2 og deres anvendelse i behandlingen af kræft |
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| GB201706327D0 (en) | 2017-04-20 | 2017-06-07 | Otsuka Pharma Co Ltd | A pharmaceutical compound |
-
2017
- 2017-04-20 GB GBGB1706327.2A patent/GB201706327D0/en not_active Ceased
-
2018
- 2018-04-20 TW TW107113537A patent/TWI813566B/zh active
- 2018-04-20 MX MX2019012471A patent/MX2019012471A/es unknown
- 2018-04-20 DK DK18722731.9T patent/DK3612524T3/da active
- 2018-04-20 AU AU2018255935A patent/AU2018255935B2/en active Active
- 2018-04-20 CN CN201880024602.7A patent/CN110831939B/zh active Active
- 2018-04-20 WO PCT/IB2018/052745 patent/WO2018193410A1/en not_active Ceased
- 2018-04-20 JP JP2019555918A patent/JP7113846B2/ja active Active
- 2018-04-20 MA MA052123A patent/MA52123A/fr unknown
- 2018-04-20 CA CA3059674A patent/CA3059674A1/en active Pending
- 2018-04-20 EP EP18722731.9A patent/EP3612524B1/en active Active
- 2018-04-20 SG SG11201909189Q patent/SG11201909189QA/en unknown
- 2018-04-20 FI FIEP18722731.9T patent/FI3612524T3/fi active
- 2018-04-20 IL IL269803A patent/IL269803B/en unknown
- 2018-04-20 MY MYPI2019005656A patent/MY203722A/en unknown
- 2018-04-20 US US16/604,002 patent/US11142518B2/en active Active
- 2018-04-20 ES ES18722731T patent/ES2994283T3/es active Active
- 2018-04-20 KR KR1020197033128A patent/KR102652193B1/ko active Active
-
2019
- 2019-09-20 PH PH12019502154A patent/PH12019502154A1/en unknown
- 2019-10-03 SA SA519410253A patent/SA519410253B1/ar unknown
- 2019-11-12 ZA ZA2019/07484A patent/ZA201907484B/en unknown
-
2021
- 2021-09-01 US US17/464,166 patent/US12030873B2/en active Active
-
2024
- 2024-05-31 US US18/679,934 patent/US20250002481A1/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108617166A (zh) * | 2015-10-21 | 2018-10-02 | 大冢制药株式会社 | 蛋白激酶抑制剂苯并内酰胺化合物 |
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