ATE400274T1 - Hemmstoffe der akt aktivität - Google Patents

Hemmstoffe der akt aktivität

Info

Publication number
ATE400274T1
ATE400274T1 AT02721697T AT02721697T ATE400274T1 AT E400274 T1 ATE400274 T1 AT E400274T1 AT 02721697 T AT02721697 T AT 02721697T AT 02721697 T AT02721697 T AT 02721697T AT E400274 T1 ATE400274 T1 AT E400274T1
Authority
AT
Austria
Prior art keywords
compounds
activity inhibitors
act activity
act
directed
Prior art date
Application number
AT02721697T
Other languages
English (en)
Inventor
Stanley Barnett
Samuel Graham
David Remy
Original Assignee
Merck & Co Inc
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
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Application granted granted Critical
Publication of ATE400274T1 publication Critical patent/ATE400274T1/de

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40Benzopyrazines
    • C07D241/42Benzopyrazines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • General Preparation And Processing Of Foods (AREA)
  • Seeds, Soups, And Other Foods (AREA)
AT02721697T 2001-04-10 2002-04-08 Hemmstoffe der akt aktivität ATE400274T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US28278101P 2001-04-10 2001-04-10

Publications (1)

Publication Number Publication Date
ATE400274T1 true ATE400274T1 (de) 2008-07-15

Family

ID=23083087

Family Applications (1)

Application Number Title Priority Date Filing Date
AT02721697T ATE400274T1 (de) 2001-04-10 2002-04-08 Hemmstoffe der akt aktivität

Country Status (8)

Country Link
US (1) US7034026B2 (de)
EP (1) EP1379251B1 (de)
JP (1) JP4361276B2 (de)
AT (1) ATE400274T1 (de)
AU (1) AU2002252614B2 (de)
CA (1) CA2442270C (de)
DE (1) DE60227492D1 (de)
WO (1) WO2002083138A1 (de)

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Also Published As

Publication number Publication date
EP1379251A4 (de) 2005-05-25
JP4361276B2 (ja) 2009-11-11
DE60227492D1 (de) 2008-08-21
US7034026B2 (en) 2006-04-25
AU2002252614B2 (en) 2006-09-14
EP1379251A1 (de) 2004-01-14
CA2442270C (en) 2009-09-08
EP1379251B1 (de) 2008-07-09
CA2442270A1 (en) 2002-10-24
JP2004525961A (ja) 2004-08-26
WO2002083138A1 (en) 2002-10-24
US20040143117A1 (en) 2004-07-22

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