ATE482213T1 - Als inhibitoren von proteinkinasen geeignete pyrazoloä1,5-aüpyrimidine - Google Patents

Als inhibitoren von proteinkinasen geeignete pyrazoloä1,5-aüpyrimidine

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Publication number
ATE482213T1
ATE482213T1 AT05816516T AT05816516T ATE482213T1 AT E482213 T1 ATE482213 T1 AT E482213T1 AT 05816516 T AT05816516 T AT 05816516T AT 05816516 T AT05816516 T AT 05816516T AT E482213 T1 ATE482213 T1 AT E482213T1
Authority
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Austria
Prior art keywords
inhibitors
protein kinases
aüpyrimidines
compounds
compositions
Prior art date
Application number
AT05816516T
Other languages
German (de)
English (en)
Inventor
Juan-Miguel Jimenez
Ronald Knegtel
Jean-Damien Charrier
Dean Stamos
Pan Li
Jon Come
Alex Aronov
Original Assignee
Vertex Pharma
Priority date (The priority date 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 date listed.)
Filing date
Publication date
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Application granted granted Critical
Publication of ATE482213T1 publication Critical patent/ATE482213T1/de

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
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    • A61P35/00Antineoplastic agents
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    • A61P37/08Antiallergic agents
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    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • 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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    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
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  • Engineering & Computer Science (AREA)
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  • Dermatology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Virology (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biochemistry (AREA)
  • Rheumatology (AREA)
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  • AIDS & HIV (AREA)
  • Child & Adolescent Psychology (AREA)
  • Neurosurgery (AREA)
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  • Tropical Medicine & Parasitology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
AT05816516T 2004-11-04 2005-11-04 Als inhibitoren von proteinkinasen geeignete pyrazoloä1,5-aüpyrimidine ATE482213T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US62544604P 2004-11-04 2004-11-04
PCT/US2005/040344 WO2006052913A1 (en) 2004-11-04 2005-11-04 PYRAZOLO[1,5-a]PYRIMIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES

Publications (1)

Publication Number Publication Date
ATE482213T1 true ATE482213T1 (de) 2010-10-15

Family

ID=35809833

Family Applications (1)

Application Number Title Priority Date Filing Date
AT05816516T ATE482213T1 (de) 2004-11-04 2005-11-04 Als inhibitoren von proteinkinasen geeignete pyrazoloä1,5-aüpyrimidine

Country Status (20)

Country Link
US (1) US7528138B2 (enExample)
EP (1) EP1812440B1 (enExample)
JP (2) JP5030229B2 (enExample)
KR (1) KR20070090172A (enExample)
CN (1) CN101094853B (enExample)
AT (1) ATE482213T1 (enExample)
AU (1) AU2005304784B2 (enExample)
CA (1) CA2586375A1 (enExample)
DE (1) DE602005023763D1 (enExample)
DK (1) DK1812440T3 (enExample)
ES (1) ES2354824T3 (enExample)
IL (1) IL182893A0 (enExample)
MX (1) MX337817B (enExample)
NO (1) NO20072795L (enExample)
NZ (1) NZ555236A (enExample)
PT (1) PT1812440E (enExample)
RU (1) RU2417996C2 (enExample)
SI (1) SI1812440T1 (enExample)
WO (1) WO2006052913A1 (enExample)
ZA (1) ZA200704476B (enExample)

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