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1. WO2009151598 - DIAZACARBAZOLES AND METHODS OF USE

Publication Number WO/2009/151598
Publication Date 17.12.2009
International Application No. PCT/US2009/003492
International Filing Date 10.06.2009
Chapter 2 Demand Filed 12.04.2010
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 31/437 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
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
437the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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 31/437
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
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
437the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4375
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
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
4375the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/496
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
496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
A61K 31/497
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
4965Non-condensed pyrazines
497containing further heterocyclic rings
A61K 31/501
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
50Pyridazines; Hydrogenated pyridazines
501not condensed and containing further heterocyclic rings
A61K 31/506
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
506not condensed and containing further heterocyclic rings
Applicants
  • GENENTECH, INC. [US]/[US] (AllExceptUS)
  • DYKE, Hazel, Joan [GB]/[GB] (UsOnly)
  • ELLWOOD, Charles [GB]/[GB] (UsOnly)
  • GANCIA, Emanuela [IT]/[GB] (UsOnly)
  • GAZZARD, Lewis, J. [GB]/[US] (UsOnly)
  • GOODACRE, Simon, Charles [GB]/[GB] (UsOnly)
  • KINTZ, Samuel, S. [US]/[US] (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
  • ELLWOOD, Charles
  • GANCIA, Emanuela
  • GAZZARD, Lewis, J.
  • GOODACRE, Simon, Charles
  • KINTZ, Samuel, S.
  • LYSSIKATOS, Joseph, P.
  • MACLEOD, Calum
  • WILLIAMS, Karen
  • CHEN, Huifen
Agents
  • BUCKWALTER, Brian, L.
Priority Data
61/060,74611.06.2008US
61/148,00128.01.2009US
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 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) 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 1,7-diazacarbazole de formule (I), (I-a) et (I-b) qui sont utiles comme inhibiteurs des kinases, plus spécifiquement utiles comme inhibiteurs des checkpoint kinases 1 (chkl), donc utiles 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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