EA200200078A1 - Птеридиноны в качестве ингибиторов киназ - Google Patents

Птеридиноны в качестве ингибиторов киназ

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Publication number
EA200200078A1
EA200200078A1 EA200200078A EA200200078A EA200200078A1 EA 200200078 A1 EA200200078 A1 EA 200200078A1 EA 200200078 A EA200200078 A EA 200200078A EA 200200078 A EA200200078 A EA 200200078A EA 200200078 A1 EA200200078 A1 EA 200200078A1
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EA
Eurasian Patent Office
Prior art keywords
substituted
hydrogen
compounds
lower alkyl
members
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Application number
EA200200078A
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English (en)
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EA005287B1 (ru
Inventor
Уильям Эликзэндер Денни
Эллен Майра Добрусин
Джеймс Бернард Крамер
Деннис Джозеф Мак Намара
Гордон Уильям Рукасл
Хауард Дэниэл Холлис Шоуолтер
Питер Лоренс Тугуд
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Уорнер-Ламберт Компани
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Publication of EA200200078A1 publication Critical patent/EA200200078A1/ru
Publication of EA005287B1 publication Critical patent/EA005287B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D475/00Heterocyclic compounds containing pteridine ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D475/00Heterocyclic compounds containing pteridine ring systems
    • C07D475/02Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4
    • C07D475/04Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
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  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
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  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Biotechnology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • AIDS & HIV (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
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  • Tropical Medicine & Parasitology (AREA)
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Abstract

Описаны соединения формул (Ia), (Ib), (Ic), (Id), где W представляет собой NH, S, SO или SO; Rпредставляет собой (не)замещенный арил, (не)замещенный гетероарил или (не)замещенный карбоцикл или гетероцикл; Q представляет собой водород или низший алкил; Rи Rявляются одинаковыми или разными и представляют собой водород, галоген, низший алкил, низший алкокси, (не)замещенный арил, (не)замещенный гетероарил, (не)замещенный арилалкил или (не)замещенный гетероарилалкил; а Rпредставляет собой водород, низший алкил или (не)замещенную карбоциклическую группу, содержащую от 3 до 7 членов, из которых до двух членов возможно представляют собой гетероатомы, выбранные из кислорода и азота; либо Rпредставляет собой (не)замещенный арил, (не)замещенный гетероарил, (не)замещенный арилалкил или (не)замещенный гетероарилалкил. Эти соединения полезны для лечения клеточных пролиферативных расстройств, таких как рак и рестеноз. Эти соединения являются сильнодействующими ингибиторами циклинзависимых киназ (cdk) и фактор роста-опосредуемых киназ. В соответствии с настоящим изобретением также предложен способ лечения клеточных пролиферативных расстройств. Также в соответствии с настоящим изобретением предложена фармацевтически приемлемая композиция, содержащая соединение формулы (I).Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200200078A 1999-09-15 2000-06-21 Птеридиноны в качестве ингибиторов киназ EA005287B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15409599P 1999-09-15 1999-09-15
PCT/US2000/017037 WO2001019825A1 (en) 1999-09-15 2000-06-21 Pteridinones as kinase inhibitors

Publications (2)

Publication Number Publication Date
EA200200078A1 true EA200200078A1 (ru) 2002-12-26
EA005287B1 EA005287B1 (ru) 2004-12-30

Family

ID=22549985

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200200078A EA005287B1 (ru) 1999-09-15 2000-06-21 Птеридиноны в качестве ингибиторов киназ

Country Status (29)

Country Link
US (2) US7169778B2 (ru)
EP (1) EP1409487A1 (ru)
JP (1) JP2003509425A (ru)
KR (1) KR20020027649A (ru)
CN (1) CN1373763A (ru)
AP (1) AP2002002479A0 (ru)
AU (1) AU777468B2 (ru)
BG (1) BG106594A (ru)
BR (1) BR0013952A (ru)
CA (1) CA2393896A1 (ru)
CR (1) CR6586A (ru)
CZ (1) CZ2002846A3 (ru)
DZ (1) DZ3186A1 (ru)
EA (1) EA005287B1 (ru)
EE (1) EE200200140A (ru)
HK (1) HK1048992A1 (ru)
HU (1) HUP0202713A3 (ru)
IL (1) IL148614A0 (ru)
IS (1) IS6298A (ru)
MA (1) MA26819A1 (ru)
MX (1) MXPA02001108A (ru)
NO (1) NO20021239D0 (ru)
NZ (1) NZ516872A (ru)
OA (1) OA12010A (ru)
PL (1) PL353269A1 (ru)
SK (1) SK3542002A3 (ru)
WO (1) WO2001019825A1 (ru)
YU (1) YU18502A (ru)
ZA (1) ZA200200896B (ru)

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