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1. WO1994029272 - 1-SUBSTITUTED ISATIN AND OXINDOLE DERIVATIVES AS INHIBITORS OF ACETYLCHOLINESTERASE

Publication Number WO/1994/029272
Publication Date 22.12.1994
International Application No. PCT/SE1994/000448
International Filing Date 13.05.1994
Chapter 2 Demand Filed 09.01.1995
IPC
C07D 209/34 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
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
32Oxygen atoms
34in position 2
C07D 209/38 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
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
32Oxygen atoms
38in positions 2 and 3, e.g. isatin
C07D 491/10 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
02in which the condensed system contains two hetero rings
10Spiro-condensed systems
CPC
C07D 209/34
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
32Oxygen atoms
34in position 2
C07D 209/38
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
32Oxygen atoms
38in positions 2 and 3, e.g. isatin
C07D 491/10
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
02in which the condensed system contains two hetero rings
10Spiro-condensed systems
Applicants
  • ASTRA AKTIEBOLAG [SE]/[SE] (AllExceptUS)
  • BOAR, Bernard, Robin [GB]/[GB] (UsOnly)
  • O'SHEA, Dennis, Mark [AU]/[GB] (UsOnly)
  • TOMLINSON, Ian, David [GB]/[GB] (UsOnly)
Inventors
  • BOAR, Bernard, Robin
  • O'SHEA, Dennis, Mark
  • TOMLINSON, Ian, David
Agents
  • FREDRIKSSON, Gunilla
Priority Data
9302080-816.06.1993SE
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) 1-SUBSTITUTED ISATIN AND OXINDOLE DERIVATIVES AS INHIBITORS OF ACETYLCHOLINESTERASE
(FR) DERIVES DE L'ISATINE A SUBSTITUTION 1 ET DE L'OXINDOLE UTILES COMME INHIBITEURS DE L'ACETYLCHOLINESTERASE
Abstract
(EN)
The present invention relates to novel compounds having general formula (1) wherein n is 3, 4, 5, 6 or 7; X represents one or more substituents independently selected from hydrogen, lower alkyl, aryl, lower alkoxy, halogen, trifluoromethyl, nitro, -NHCOR where R is lower alkyl or aryl, -NR1R2 where R1 and R2 are independently hydrogen or lower alkyl or together form a ring, or cycloalkyl, cycloalkenyl or bicycloalkyl either optionally further substituted by lower alkyl; Y is (a) or (b) where R3 and R4 are independently hydrogen, lower alkyl, lower alkoxy or together form a cyclic acetal; Z is lower alkyl; and W represents one or more substituents independently selected from hydrogen, lower alkyl, lower alkoxy or halogen; stereo and optical isomers and racemates thereof where such isomers exist, as well as pharmaceutically acceptable acid addition salts thereof and solvates thereof having therapeutic activity, intermediates for their preparation, processes for their preparation, pharmaceutical formulations containing said compounds and medicinal use of said compounds.
(FR)
La présente invention se rapporte à de nouveaux composés ayant la formule générale (I) dans laquelle n vaut 3, 4, 5, 6 ou 7; X représente un ou plusieurs substituants sélectionnés indépendamment parmi hydrogène, alkyle inférieur, aryle, alcoxy inférieur, halogène, trifluorométhyle, nitro, -NHCOR où R représente alkyle inférieur ou aryle, -NR1R2 où R1 et R2 représentent indépendamment hydrogène ou alkyle inférieur ou forment un anneau, ou cycloalkyle, cycloalcényle ou bicycloalkyle, l'un et l'autre éventuellement également substitués par alkyle inférieur; Y représente (a) ou (b) où R3 et R4 représentent indépendamment hydrogène, alkyle inférieur, alcoxy inférieur ou forment un acétal cyclique; Z représente alkyle inférieur; et W représente un ou plusieurs substituants indépendamment sélectionnés parmi hydrogène, alkyle inférieur, alcoxy inférieur ou halogène; l'invention se rapporte également à des stéréo-isomères et à des isomères optiques et des racémates de ces composés dans lesquels ces isomères existent, ainsi qu'à des sels d'addition d'acide pharmaceutiquement acceptables de ceux-ci et à des solvates de ceux-ci ayant une activité thérapeutique, à leurs intermédiaires de préparation, à leurs procédés de préparation, aux formulations pharmaceutiques contenant ces composés et à l'utilisation médicinale de ces composés.
Also published as
FI956074
NO19955074
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