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1. WO2012055945 - INDOLE DERIVATIVES AND PROCESS FOR THEIR PREPARATION

Publication Number WO/2012/055945
Publication Date 03.05.2012
International Application No. PCT/EP2011/068820
International Filing Date 27.10.2011
IPC
C07D 209/20 2006.01
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
10with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
20substituted additionally by nitrogen atoms, e.g. tryptophane
A61K 31/405 2006.01
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 25/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 25/28 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
CPC
A61K 31/4045
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
4045Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
A61K 31/405
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 1/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 21/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
21Drugs for disorders of the muscular or neuromuscular system
A61P 21/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
21Drugs for disorders of the muscular or neuromuscular system
02Muscle relaxants, e.g. for tetanus or cramps
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
Applicants
  • MERZ PHARMA GMBH & CO. KGAA [DE]/[DE] (AllExceptUS)
  • ABEL, Ulrich [DE]/[DE] (UsOnly)
Inventors
  • ABEL, Ulrich
Agents
  • JACOBI, Markus
Priority Data
10189377.429.10.2010EP
61/407,92429.10.2010US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) INDOLE DERIVATIVES AND PROCESS FOR THEIR PREPARATION
(FR) DÉRIVÉS D'INDOLE ET PROCÉDÉ POUR LEUR PRÉPARATION
Abstract
(EN)
Substituted indole derivatives of formula (I) wherein the radicals have e. g. the following meaning: R1 is hydrogen, -C1-6-alkyl, R2 is hydrogen, -C1-6-alkyl or cycloC3-12-alkyl; R3 is OR R4 is hydrogen or halogen, R5 is hydrogen, -C1-6-alkyl R6 is hydrogen, -C1-6-alkyl R is hydrogen or -C1-6-alkyl; X is a group -C(O)CH2- or -CH=CH-; R7 is hydrogen are potent inhibitors of Abeta peptide polymerization and can be used for the treatment of e.g. Alzheimers disease or ocular disorders.
(FR)
L'invention porte sur des dérivés d'indole substitués de formule (I) dans laquelle les radicaux ont par exemple la signification suivante : R1 représente l'atome d'hydrogène ou un groupe alkyle en C1-6, R2 représente l'atome d'hydrogène, un groupe alkyle en C1-6 ou un groupe cycloalkyle en C3-12, R3 représente OR, R4 représente l'atome d'hydrogène ou un atome d'halogène, R5 représente l'atome d'hydrogène ou un groupe alkyle en C1-6, R6 représente l'atome d'hydrogène ou un groupe alkyle en C1-6, R représente l'atome d'hydrogène ou un groupe alkyle en C1-6, X représente un groupe -C(O)CH2- ou -CH=CH- et R7 représente l'atome d'hydrogène. Ces dérivés sont des inhibiteurs puissants de la polymérisation du peptide Abêta et peuvent être utilisés pour le traitement par exemple de la maladie d'Alzheimer ou de troubles oculaires.
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