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1. WO2007045867 - 3 -AMINOINDOLE COMPOUNDS AS CRTH2 RECEPTOR LIGANDS

Publication Number WO/2007/045867
Publication Date 26.04.2007
International Application No. PCT/GB2006/003872
International Filing Date 18.10.2006
IPC
C07D 209/40 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
30with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
40Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
A61K 31/405 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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403condensed with carbocyclic rings, e.g. carbazole
404Indoles, e.g. pindolol
405Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
A61P 29/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
CPC
C07D 209/40
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
30with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
40Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
Applicants
  • ARGENTA DISCOVERY LIMITED [GB]/[GB] (AllExceptUS)
  • RAY, Nicholas, Charles [GB]/[GB] (UsOnly)
  • HYND, George (UsOnly)
  • ARIENZO, Rosa [IT]/[GB] (UsOnly)
  • FINCH, Harry [GB]/[GB] (UsOnly)
Inventors
  • RAY, Nicholas, Charles
  • HYND, George
  • ARIENZO, Rosa
  • FINCH, Harry
Agents
  • GILL JENNINGS & EVERY LLP
Priority Data
0521275.819.10.2005GB
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) 3 -AMINOINDOLE COMPOUNDS AS CRTH2 RECEPTOR LIGANDS
(FR) COMPOSES 3-AMINOINDOLE UTILISES EN TANT QUE LIGANDS DU RECEPTEUR CRTH2
Abstract
(EN) Compounds of formula [I] are CRTH2 antagonists, useful in the treatment o conditions having an inflammatory component: in which: R1, R2, R3 and R4 are independently hydrogen, (C1-C6) alky!, (C1-C6) haloalkyl, halo, -S(O)nR10, -NR11SO2R10, -SO2N(R11)2, -N(R11)2, -NR11C(O)R10, -C(O)N(R11)2, -CO2R11, -C(O)R10, CN or a group OR12; wherein each R10 is independently (C1-C6) alkyl, (C1-C6) haloalkyl, cycloalkyl, aryl, or heteroaryl; R11 is independently hydrogen, (C1-C6)alkyl, (C1-C6) haloalkyl, cycloalkyl, aryl, or heteroaryl; R12 is hydrogen, (C1-C6) alkyl, (C1-C6) haloalkyl, cycloalkyl, or a group -SO2R10, wherein n is O 1 or 2; R5 and R6 are independently hydrogen, (C1-C6) alkyl or (C1-C6) haloalkyl, or R5 and R6 together with the atom to which they are attached form a cycloalkyl group; R7 is hydrogen, (C1-C6) alkyl, or (C1-C6) haloalkyl; R8 is aryl, heteroaryl, aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused- heterocycloalkyl or aryl-fused-cycloalkyl; and R9 is hydrogen, (C1-C6) alkyl, (C1-C6) haloalkyl, or cycloalkyl.
(FR) La présente invention a trait à des composés de formule (I), qui sont des antagonistes du récepteur CRTH2 et sont utiles pour traiter les troubles à composante inflammatoire. Dans ladite formule, R1, R2, R3 et R4 sont indépendamment l’hydrogène, un alkyle en C1 à C6, un halogénoalkyle en C1 à C6, un groupe halogéno, -S(O)nR10, -NR11SO2R10, -SO2N(R11)2, -N(R11)2, -NR11C(O)R10, -C(O)N(R11)2, -CO2R11, -C(O)R10, CN ou un groupe OR12 ;chaque R10 est indépendamment un alkyle en C1 à C6, un halogénoalkyle en C1 à C6, un cycloalkyle, un aryle, ou un hétéroaryle ; R11 est indépendamment l’hydrogène, un alkyle en C1 à C6, un halogénoalkyle en C1 à C6, un cycloalkyle, un aryle, ou un hétéroaryle ; R12 est l’hydrogène, un alkyle en C1 à C6, un halogénoalkyle en C1 à C6, un cycloalkyle ou un groupe -SO2R10, n valant O, 1 ou 2 ; R5 et R6 sont indépendamment l’hydrogène, un alkyle en C1 à C6 ou un halogénoalkyle en C1 à C6, ou bien R5 et R6 forment conjointement, avec l’atome auquel il sont liés, un groupe cycloalkyle ; R7 l’hydrogène, un alkyle en C1 à C6 ou un halogénoalkyle en C1 à C6 ; R8 est un aryle, un hétéroaryle, un hétérocycloalkyle fusionné avec un aryle, un cycloalkyle fusionné avec un hétéroaryle, un hétérocycloalkyle fusionné avec un hétéroaryle ou encore un cycloalkyle fusionné avec un aryle ; enfin R9 est l’hydrogène, un alkyle en C1 à C6, un halogénoalkyle en C1 à C6, ou un cycloalkyle.
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