SA519410253B1 - Erk1/2 مشتق 6- بيريميدين أيزوإندول كمثبط - Google Patents

Erk1/2 مشتق 6- بيريميدين أيزوإندول كمثبط

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Publication number
SA519410253B1
SA519410253B1 SA519410253A SA519410253A SA519410253B1 SA 519410253 B1 SA519410253 B1 SA 519410253B1 SA 519410253 A SA519410253 A SA 519410253A SA 519410253 A SA519410253 A SA 519410253A SA 519410253 B1 SA519410253 B1 SA 519410253B1
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SA
Saudi Arabia
Prior art keywords
compound
pyrimidin
erk1
inhibitor
isoindole derivative
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SA519410253A
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English (en)
Inventor
إيوا أدامكزيك بوزينا
أنتوني باجولي بول
كريج ميلينج روبرت
توماس ليندلي كولين
هنري ساوندرز مارك
ريدر مايكل
سكاراتي ميركا
اليزابيث ويلشير نيكولا
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أوتسوكا فارماسوتيكال كو.، ليمتد
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Application filed by أوتسوكا فارماسوتيكال كو.، ليمتد filed Critical أوتسوكا فارماسوتيكال كو.، ليمتد
Publication of SA519410253B1 publication Critical patent/SA519410253B1/ar

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19Particulate 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (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)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Dermatology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

يتعلق الاختراع الحالي بالمركب (2R)-2-(6-{5- كلورو -2-[(أوكسان -4- يل) أمينو] بيريميدين -4- يل}-1- أوكسو -2، 3- داي هيدرو -1H- أيزو إندول -2- يل)-N-[(1S)-1-(3- فلورو -5- ميثوكسي فينيل) -2- هيدروكسي إيثيل] بروباناميد (2R)-2-(6-{5-chloro-2-[(oxan-4-yl)amino]pyrimidin-4-yl}-1-oxo-2,3-dihydro-1H-isoindol-2-yl)-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide ، وبصفة خاصة بالأشكال الفيزيائية الجديدة للمركب، وعملية لتحضير المركب والمركبات الوسيطة التخليقية لاستخدامها في العملية، وصيغ جديدة تحتوي على المركب، وكذلك الاستخدامات العلاجية للمركب. شكل 1.
SA519410253A 2017-04-20 2019-10-03 Erk1/2 مشتق 6- بيريميدين أيزوإندول كمثبط SA519410253B1 (ar)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB1706327.2A GB201706327D0 (en) 2017-04-20 2017-04-20 A pharmaceutical compound

Publications (1)

Publication Number Publication Date
SA519410253B1 true SA519410253B1 (ar) 2023-07-12

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SA519410253A SA519410253B1 (ar) 2017-04-20 2019-10-03 Erk1/2 مشتق 6- بيريميدين أيزوإندول كمثبط

Country Status (17)

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US (2) US11142518B2 (ar)
EP (1) EP3612524A1 (ar)
JP (1) JP7113846B2 (ar)
KR (1) KR102652193B1 (ar)
CN (1) CN110831939A (ar)
AU (1) AU2018255935B2 (ar)
BR (1) BR112019019948A2 (ar)
CA (1) CA3059674A1 (ar)
GB (1) GB201706327D0 (ar)
IL (1) IL269803B (ar)
MA (1) MA52123A (ar)
MX (1) MX2019012471A (ar)
PH (1) PH12019502154A1 (ar)
SA (1) SA519410253B1 (ar)
SG (1) SG11201909189QA (ar)
TW (1) TWI813566B (ar)
WO (1) WO2018193410A1 (ar)

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Also Published As

Publication number Publication date
SG11201909189QA (en) 2019-10-30
JP2020517598A (ja) 2020-06-18
RU2019135029A3 (ar) 2021-07-16
BR112019019948A2 (pt) 2020-04-28
AU2018255935B2 (en) 2022-03-17
US20210101889A1 (en) 2021-04-08
CA3059674A1 (en) 2018-10-25
JP7113846B2 (ja) 2022-08-05
KR20190140957A (ko) 2019-12-20
MA52123A (fr) 2020-02-26
CN110831939A (zh) 2020-02-21
MX2019012471A (es) 2019-12-11
TW201842912A (zh) 2018-12-16
IL269803B (en) 2022-09-01
RU2019135029A (ru) 2021-05-20
US11142518B2 (en) 2021-10-12
EP3612524A1 (en) 2020-02-26
KR102652193B1 (ko) 2024-03-29
PH12019502154A1 (en) 2020-06-29
IL269803A (en) 2019-11-28
TWI813566B (zh) 2023-09-01
WO2018193410A1 (en) 2018-10-25
AU2018255935A1 (en) 2019-11-07
GB201706327D0 (en) 2017-06-07
US20220169638A1 (en) 2022-06-02

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