CA2740885C - Fused ring heteroaryl kinase inhibitors - Google Patents

Fused ring heteroaryl kinase inhibitors Download PDF

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Publication number
CA2740885C
CA2740885C CA2740885A CA2740885A CA2740885C CA 2740885 C CA2740885 C CA 2740885C CA 2740885 A CA2740885 A CA 2740885A CA 2740885 A CA2740885 A CA 2740885A CA 2740885 C CA2740885 C CA 2740885C
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substituted
unsubstituted
compound
salt
leu
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French (fr)
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CA2740885A1 (en
Inventor
Arvin Dar
Kevan M. Shokat
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University of California San Diego UCSD
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University of California San Diego UCSD
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    • CCHEMISTRY; METALLURGY
    • 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
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2740885A 2008-10-16 2009-10-16 Fused ring heteroaryl kinase inhibitors Active CA2740885C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US10613708P 2008-10-16 2008-10-16
US61/106,137 2008-10-16
US10645308P 2008-10-17 2008-10-17
US61/106,453 2008-10-17
PCT/US2009/060985 WO2010045542A2 (en) 2008-10-16 2009-10-16 Fused ring heteroaryl kinase inhibitors

Publications (2)

Publication Number Publication Date
CA2740885A1 CA2740885A1 (en) 2010-04-22
CA2740885C true CA2740885C (en) 2018-04-03

Family

ID=42107267

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2740885A Active CA2740885C (en) 2008-10-16 2009-10-16 Fused ring heteroaryl kinase inhibitors

Country Status (8)

Country Link
US (1) US8697709B2 (enExample)
EP (1) EP2358720B1 (enExample)
JP (2) JP5819195B2 (enExample)
AU (4) AU2009305669A1 (enExample)
CA (1) CA2740885C (enExample)
DK (1) DK2358720T3 (enExample)
ES (1) ES2570429T3 (enExample)
WO (1) WO2010045542A2 (enExample)

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CA2740885C (en) * 2008-10-16 2018-04-03 The Regents Of The University Of California Fused ring heteroaryl kinase inhibitors
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