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1. WO2009151589 - DIAZACARBAZOLES AND METHODS OF USE

Publication Number WO/2009/151589
Publication Date 17.12.2009
International Application No. PCT/US2009/003481
International Filing Date 10.06.2009
IPC
C07D 471/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
A61K 31/519 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
A61K 2300/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
2300Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
A61K 31/519
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 35/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
02specific for leukemia
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Applicants
  • GENENTECH, INC. [US]/[US] (AllExceptUS)
  • DYKE, Hazel, Joan [GB]/[GB] (UsOnly)
  • GANCIA, Emanuela [GB]/[GB] (UsOnly)
  • GAZZARD, Lewis, J. [GB]/[US] (UsOnly)
  • GOODACRE, Simon, Charles [GB]/[GB] (UsOnly)
  • LYSSIKATOS, Joseph, P. [US]/[US] (UsOnly)
  • MACLEOD, Calum [GB]/[GB] (UsOnly)
  • WILLIAMS, Karen [GB]/[GB] (UsOnly)
  • CHEN, Huifen [US]/[US] (UsOnly)
Inventors
  • DYKE, Hazel, Joan
  • GANCIA, Emanuela
  • GAZZARD, Lewis, J.
  • GOODACRE, Simon, Charles
  • LYSSIKATOS, Joseph, P.
  • MACLEOD, Calum
  • WILLIAMS, Karen
  • CHEN, Huifen
Agents
  • WANG, Min
Priority Data
61/060,75011.06.2008US
61/148,00428.01.2009US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) DIAZACARBAZOLES AND METHODS OF USE
(FR) DIAZACARBAZOLES ET PROCÉDÉS D'UTILISATION
Abstract
(EN) The invention relates to 1,5-diazacarbazole compounds of Formula (I), (I-a), (I-b), (I-c), (I-d), (I-e), (I-f), (I-g) and (I-h) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chkl) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
(FR) La présente invention concerne des composés 1,5-diazacarbazole de formule (I), (I-a), (I-b), (I-c), (I-d), (I-e), (I-f), (I-g) et (I-h) qui peuvent être utilisés comme inhibiteurs des kinases, plus spécifiquement comme inhibiteurs des checkpoint kinases 1 (chkl), et donc comme agents thérapeutiques anticancéreux. L'invention concerne également des compositions, plus spécifiquement des compositions pharmaceutiques comprenant ces composés et des procédés permettant de les utiliser pour traiter diverses formes de cancer et de troubles hyperprolifératifs, ainsi que des procédés d'utilisation des composés pour le diagnostic ou le traitement in vitro, in situ, et in vivo de cellules de mammifères, ou d'affections pathologiques associées.
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