KR102652193B1 - Erk1/2 억제제로서의 6-피리미딘-이소인돌 유도체 - Google Patents

Erk1/2 억제제로서의 6-피리미딘-이소인돌 유도체 Download PDF

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KR102652193B1
KR102652193B1 KR1020197033128A KR20197033128A KR102652193B1 KR 102652193 B1 KR102652193 B1 KR 102652193B1 KR 1020197033128 A KR1020197033128 A KR 1020197033128A KR 20197033128 A KR20197033128 A KR 20197033128A KR 102652193 B1 KR102652193 B1 KR 102652193B1
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compound
cancer
formula
dihydro
oxo
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KR20190140957A (ko
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마이클 리더
니콜라 엘리자베스 윌셔
마크 헨리 사운더스
폴 앤서니 바걸리
콜린 토마스 린들리
로버트 크레이그 멜링
보제나 이와 아담칙
미르카 스카라티
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오츠카 세이야쿠 가부시키가이샤
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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)
KR1020197033128A 2017-04-20 2018-04-20 Erk1/2 억제제로서의 6-피리미딘-이소인돌 유도체 Active KR102652193B1 (ko)

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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KR20190140957A KR20190140957A (ko) 2019-12-20
KR102652193B1 true KR102652193B1 (ko) 2024-03-29

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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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US20210101889A1 (en) 2021-04-08
RU2019135029A3 (enExample) 2021-07-16
TWI813566B (zh) 2023-09-01
US11142518B2 (en) 2021-10-12
BR112019019948A2 (pt) 2020-04-28
AU2018255935B2 (en) 2022-03-17
IL269803B (en) 2022-09-01
KR20190140957A (ko) 2019-12-20
SA519410253B1 (ar) 2023-07-12
MA52123A (fr) 2020-02-26
US20220169638A1 (en) 2022-06-02
US20250002481A1 (en) 2025-01-02
WO2018193410A1 (en) 2018-10-25
IL269803A (en) 2019-11-28
TW201842912A (zh) 2018-12-16
AU2018255935A1 (en) 2019-11-07
MY203722A (en) 2024-07-16
RU2019135029A (ru) 2021-05-20
EP3612524B1 (en) 2024-08-28
US12030873B2 (en) 2024-07-09
JP7113846B2 (ja) 2022-08-05
DK3612524T3 (da) 2024-09-30
CN110831939A (zh) 2020-02-21
EP3612524A1 (en) 2020-02-26
ES2994283T3 (en) 2025-01-21
MX2019012471A (es) 2019-12-11
JP2020517598A (ja) 2020-06-18
CA3059674A1 (en) 2018-10-25
CN110831939B (zh) 2025-05-09
PH12019502154A1 (en) 2020-06-29
SG11201909189QA (en) 2019-10-30
FI3612524T3 (fi) 2024-09-24
GB201706327D0 (en) 2017-06-07
NZ758411A (en) 2024-10-25
ZA201907484B (en) 2024-05-30

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