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1. WO2011073263 - 1, 7 - DIAZACARBAZOLES AND THEIR USE IN THE TREATMENT OF CANCER

Publication Number WO/2011/073263
Publication Date 23.06.2011
International Application No. PCT/EP2010/069771
International Filing Date 15.12.2010
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 31/4427 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
44Non-condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
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 31/439
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
439the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 31/4545
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
44Non condensed pyridines; Hydrogenated derivatives thereof
445Non condensed piperidines, e.g. piperocaine
4523containing further heterocyclic ring systems
4545containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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 31/5377
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
535having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
5377not condensed and containing further heterocyclic rings, e.g. timolol
Applicants
  • F. HOFFMANN-LA ROCHE AG [CH]/[CH] (AllExceptUS)
  • DYKE, Hazel Joan [GB]/[GB] (UsOnly)
  • GAZZARD, Lewis J. [GB]/[US] (UsOnly)
  • WILLIAMS, Karen [GB]/[GB] (UsOnly)
  • CHEN, Huifen [US]/[US] (UsOnly)
  • KINTZ, Samuel [US]/[US] (UsOnly)
  • DROBNICK, Joy [US]/[US] (UsOnly)
  • LYSSIKATOS, Joseph P. [US]/[US] (UsOnly)
  • GOODACRE, Simon [GB]/[GB] (UsOnly)
  • MACLEOD, Calum [GB]/[GB] (UsOnly)
  • ELLWOOD, Charles [GB]/[GB] (UsOnly)
Inventors
  • DYKE, Hazel Joan
  • GAZZARD, Lewis J.
  • WILLIAMS, Karen
  • CHEN, Huifen
  • KINTZ, Samuel
  • DROBNICK, Joy
  • LYSSIKATOS, Joseph P.
  • GOODACRE, Simon
  • MACLEOD, Calum
  • ELLWOOD, Charles
Agents
  • SCHIRLIN, Julien
Priority Data
61/284,41416.12.2009US
61/287,70217.12.2009US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) 1, 7 - DIAZACARBAZOLES AND THEIR USE IN THE TREATMENT OF CANCER
(FR) 1,7-DIAZACARBAZOLES ET LEUR UTILISATION DANS LE TRAITEMENT DU CANCER
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 (chk 1) 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) Cette invention concerne des composés de 1,7-diazacarbazole de Formule (I), (I-a) et (I-b) qui sont utiles à titre d'inhibiteurs de kinase, plus spécifiquement, qui sont utiles à titre d'inhibiteurs de la checkpoint kinase 1 (chk 1), et par conséquent, utiles à titre d'anticancéreux. Cette invention concerne également des compositions, plus spécifiquement, des compositions pharmaceutiques contenant lesdits composés et des méthodes les utilisant pour traiter diverses formes de cancer et autres troubles hyperprolifératifs, ainsi que des méthodes d'utilisation des composés selon l'invention pour le diagnostic ou le traitement in vitro, in situ, et in vivo de cellules de mammifères, ou d'affections pathologiques associées.
Related patent documents
RU2012127877This application is not viewable in PATENTSCOPE because the national phase entry has not been published yet or the national entry is issued from a country that does not share data with WIPO or there is a formatting issue or an unavailability of the application.
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