JP5030229B2 - プロテインキナーゼのインヒビターとして有用なピラゾロ[1,5−a]ピリミジン - Google Patents

プロテインキナーゼのインヒビターとして有用なピラゾロ[1,5−a]ピリミジン Download PDF

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JP5030229B2
JP5030229B2 JP2007540144A JP2007540144A JP5030229B2 JP 5030229 B2 JP5030229 B2 JP 5030229B2 JP 2007540144 A JP2007540144 A JP 2007540144A JP 2007540144 A JP2007540144 A JP 2007540144A JP 5030229 B2 JP5030229 B2 JP 5030229B2
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JP2008519059A (ja
JP2008519059A5 (enExample
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ファン−ミゲル ヒメネス,
ロナルド クネグテル,
ジャン−ダミアン シャリエ,
ディーン スタモス,
パン リー,
ジョン アール. コム,
アレックス アロノフ,
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • C07ORGANIC CHEMISTRY
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    • 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
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    • 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
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    • 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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  • Veterinary Medicine (AREA)
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  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (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)
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  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
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JP2007540144A 2004-11-04 2005-11-04 プロテインキナーゼのインヒビターとして有用なピラゾロ[1,5−a]ピリミジン Expired - Fee Related JP5030229B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US62544604P 2004-11-04 2004-11-04
US60/625,446 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

Related Child Applications (1)

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JP2008278235A Division JP2009067803A (ja) 2004-11-04 2008-10-29 プロテインキナーゼのインヒビターとして有用なピラゾロ[1,5−a]ピリミジン

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JP2008519059A JP2008519059A (ja) 2008-06-05
JP2008519059A5 JP2008519059A5 (enExample) 2008-12-18
JP5030229B2 true JP5030229B2 (ja) 2012-09-19

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JP2007540144A Expired - Fee Related JP5030229B2 (ja) 2004-11-04 2005-11-04 プロテインキナーゼのインヒビターとして有用なピラゾロ[1,5−a]ピリミジン
JP2008278235A Pending JP2009067803A (ja) 2004-11-04 2008-10-29 プロテインキナーゼのインヒビターとして有用なピラゾロ[1,5−a]ピリミジン

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JP2008278235A Pending JP2009067803A (ja) 2004-11-04 2008-10-29 プロテインキナーゼのインヒビターとして有用なピラゾロ[1,5−a]ピリミジン

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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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