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1. WO2009093012 - INDOLYL- PYRIDONE DERIVATIVES HAVING CHECKPOINT KINASE 1 INHIBITORY ACTIVITY

Publication Number WO/2009/093012
Publication Date 30.07.2009
International Application No. PCT/GB2009/000149
International Filing Date 20.01.2009
IPC
C07D 401/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14containing three or more hetero rings
A61K 31/4412 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
4412having oxo groups directly attached to the heterocyclic ring
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 31/4439
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
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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
A61P 17/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
A61P 19/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
02for joint disorders, e.g. arthritis, arthrosis
Applicants
  • VERNALIS (R & D) LTD [GB]/[GB] (AllExceptUS)
  • STOKES, Stephen [GB]/[GB] (UsOnly)
  • FOLOPPE, Nicolas [FR]/[GB] (UsOnly)
  • FIUMANA, Andrea [IT]/[GB] (UsOnly)
  • DRYSDALE, Martin [GB]/[GB] (UsOnly)
  • BEDFORD, Simon [GB]/[GB] (UsOnly)
  • WEBB, Paul [GB]/[GB] (UsOnly)
Inventors
  • STOKES, Stephen
  • FOLOPPE, Nicolas
  • FIUMANA, Andrea
  • DRYSDALE, Martin
  • BEDFORD, Simon
  • WEBB, Paul
Agents
  • WALLS, Alan, James
Priority Data
0801090.222.01.2008GB
0818695.911.10.2008GB
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) INDOLYL- PYRIDONE DERIVATIVES HAVING CHECKPOINT KINASE 1 INHIBITORY ACTIVITY
(FR) DÉRIVÉS D'INDOLYL-PYRIDONE
Abstract
(EN) Compounds of formula (I) have checkpoint kinase 1 (CHK1 ) inhibitory activity: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R3, and R4 are independently selected from hydrogen, hydroxy, C1-C3 alkyl, fluoro-(C1-C3)-alkyl, hydroxy-(C1C3)-alkyl, C1-C3 alkoxy, fluoro-(C1-C3)-alkoxy, hydroxy-(C1-C3)-alkoxy, -N(R11)-R12, -AIk-N(R11)-R12, -0-AIk-N(R11)-R12, -C(=O)OH, carboxy-(C1-C3)-alkyl, or -C(=O)-NH-R13; AIk is a straight or branched chain divalent C1-C6 alkylene radical; R7 and R8 are independently selected from hydrogen, hydroxy, or C1-C3 alkoxy; X is a straight chain divalent C1-C3 alkylene radical, optionally substituted on one or more carbons by R9 and/or R10; W is selected from -C(=O)-N(-R16)- or -N(-R17)-C(=O)-; Y is hydrogen, C1-C3 alkyl, C1-C3 alkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substituted 6-membered monocyclic heteroaryl ring.
(FR) Cette invention concerne des composés de formule (I) ayant une activité d'inhibition de la protéine checkpoint kinase 1 (CHK1). Dans la formule (I) selon l'invention, R1, R2, R5 et R6 sont indépendamment choisis parmi un atome d'hydrogène, un groupe hydroxy, méthyle, trifluorométhyle, hydroxyméthyle, méthoxy, trifluorométhoxy, méthylamino et diméthylamino; R3, et R4 sont indépendamment choisis parmi un atome d'hydrogène, un groupe hydroxy, alkyle C1-C3, fluoroalkyle C1-C3, hydroxyalkyle C1C3, alcoxy C1-C3, fluoroalcoxy C1-C3, hydroxyalcoxy C1-C3, -N(R11)-R12, -Alk-N(R11)-R12, -O-Alk-N(R11)-R12, -C(=O)OH, carboxyalkyle C1-C3, ou -C(=O)-NH-R13 ; Alk est un radical alkylène C1-C6 divalent à chaîne droite ou ramifiée; R7 et R8 sont indépendamment choisis parmi un atome d'hydrogène, un groupe hydroxy, ou alcoxy C1-C3; X est un radical alkylène C1-C3 divalent à chaîne droite, éventuellement substitué sur un ou plusieurs carbones par R9 et/ou R10 ; W est choisi parmi -C(=O)-N(-R16)- ou -N(-R17)-C(=O)-; Y est un atome d'hydrogène, un groupe alkyle C1-C3, alcoxy C1-C3, ou halogéno; et Q est choisi parmi un groupe phényle éventuellement substitué, cyclohexyle éventuellement substitué, ou un cycle hétéroaryle monocyclique de 6 chaînons éventuellement substitué.
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