JP7113846B2 - Ｅｒｋ１／２阻害剤としての６－ピリミジン－イソインドール誘導体 - Google Patents

Ｅｒｋ１／２阻害剤としての６－ピリミジン－イソインドール誘導体 Download PDF

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JP7113846B2
JP7113846B2 JP2019555918A JP2019555918A JP7113846B2 JP 7113846 B2 JP7113846 B2 JP 7113846B2 JP 2019555918 A JP2019555918 A JP 2019555918A JP 2019555918 A JP2019555918 A JP 2019555918A JP 7113846 B2 JP7113846 B2 JP 7113846B2
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compound
dihydro
oxo
propanamide
methoxyphenyl
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JP2020517598A (ja
JP2020517598A5 (enExample
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マイケル、リーダー
ニコラ、エリザベス、ウィルシャー
マーク、ヘンリー、サンダース
ポール、アンソニー、バグリー
コリン、トーマス、リンドリー
ロバート、クレイグ、メリング
ボツェナ、エバ、アダムチク
ミルカ、スカラティ
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Otsuka Pharmaceutical Co Ltd
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Otsuka Pharmaceutical Co Ltd
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    • 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

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  • 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)
JP2019555918A 2017-04-20 2018-04-20 Ｅｒｋ１／２阻害剤としての６－ピリミジン－イソインドール誘導体 Active JP7113846B2 (ja)

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

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JP2020517598A JP2020517598A (ja) 2020-06-18
JP2020517598A5 JP2020517598A5 (enExample) 2021-05-27
JP7113846B2 true JP7113846B2 (ja) 2022-08-05

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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)

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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

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NZ758411A (en) 2024-10-25
US12030873B2 (en) 2024-07-09
CN110831939B (zh) 2025-05-09
ES2994283T3 (en) 2025-01-21
AU2018255935B2 (en) 2022-03-17
EP3612524B1 (en) 2024-08-28
DK3612524T3 (da) 2024-09-30
CA3059674A1 (en) 2018-10-25
SG11201909189QA (en) 2019-10-30
BR112019019948A2 (pt) 2020-04-28
FI3612524T3 (fi) 2024-09-24
TW201842912A (zh) 2018-12-16
KR102652193B1 (ko) 2024-03-29
AU2018255935A1 (en) 2019-11-07
US20250002481A1 (en) 2025-01-02
IL269803A (en) 2019-11-28
RU2019135029A (ru) 2021-05-20
TWI813566B (zh) 2023-09-01
US20220169638A1 (en) 2022-06-02
WO2018193410A1 (en) 2018-10-25
MA52123A (fr) 2020-02-26
JP2020517598A (ja) 2020-06-18
GB201706327D0 (en) 2017-06-07
SA519410253B1 (ar) 2023-07-12
EP3612524A1 (en) 2020-02-26
MX2019012471A (es) 2019-12-11
CN110831939A (zh) 2020-02-21
RU2019135029A3 (enExample) 2021-07-16
KR20190140957A (ko) 2019-12-20
PH12019502154A1 (en) 2020-06-29
MY203722A (en) 2024-07-16
US11142518B2 (en) 2021-10-12
US20210101889A1 (en) 2021-04-08
ZA201907484B (en) 2024-05-30
IL269803B (en) 2022-09-01

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