3-indoline derivatives useful in the treatment of...

C - Chemistry – Metallurgy – 07 – D

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C07D 401/06 (2006.01) A61K 31/4439 (2006.01) A61K 31/454 (2006.01) A61K 31/496 (2006.01) A61P 25/00 (2006.01) C07D 209/14 (2006.01) C07D 403/06 (2006.01)

Patent

CA 2432473

The present invention relates to the use of a compound having the general formula wherein R1 is acyl, thioacyl, trifluoromethylsulfonyl or R1 is a group R12SO2-, R12OCO- or R12SCO- wherein R12 is C1-6-alkyl, C2-6-alkenyl, C2-6- alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl or aryl, or R1 is a group R13R14NCO,- R13R14NCS-, wherein R13 and R14 are independently hydrogen, C1-6- alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl or aryl, or R13 and R14 together with the N-atom to which they are linked form a pyrrolidinyl, piperidinyl or perhydroazepin group; n is 1-6;X is C, CH or N, and the dotted line emanating from X indicates a bond when X is C and no bond when X is N or CH;R', R'' and R2 are independently selected from hydrogen and C1-6-alkyl;R3-R11 are independently selected from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8- cycloalkyl-C1-6-alkyl, amino, C1-6-alkylamino, di-(C1-6-alkyl)amino, C1-6- alkylcarbonyl, aminocarbonyl, C1-6-alkylaminocarbonyl, di-(C1-6- alkyl)aminocarbonyl, C1-6-alkoxy, C1-6-alkylthio, hydroxy, trifluoromethyl, trifluoromethylsulfonyl and C1-6-alkylsulfonyl; or a pharmaceutically acceptable acid addition salt thereof, for the manufacture of a medicament useful in the treatment of psychiatric and neurologic disorders, in particular psychoses.

La présente invention concerne l'utilisation d'un composé ayant la formule générale dans laquelle R1 est acyle, thioacyle, trifluorométhylsulfonyle ou R1 est un groupe R12SO2-, R12OCO- ou R12SCO- dans lequel R12 est alkyle C1-6, alcényle C2-6, alkynyle C2-6, cycloalkyle C3-8, cycloalkyle C3-8 - alkyle ou aryle C1-6, ou R1 est un groupe R13R14NCO,- R13R14NCS-, dans lequel R13 et R14 sont indépendamment hydrogène, alkyle C1-6, C2-6 alcényle, alkynyle C2-6, cycloalkyl C3-8, cycloalkyle C3-8 alkyle ou aryle C1-6, ou R13 et R14 avec l'atome N auquel ils sont liés forment un groupe pyrrolidinyle, piperidinyle ou perhydroazépine; n est 1-6; X est C, CH ou N, et le pointillé venant de X indique une liaison dans laquelle X est C, et aucun lien si X est N ou CH; R ', R'' et R2 sont indépendamment sélectionné parmi hydrogène et alkyle C1-6;R3-R11 sont indépendamment sélectionnés parmi hydrogène, halogène, cyano, nitro, alkyle C1-6, alcényle C2-6, alkynyle C2-6, cycloalkyle C3-8, cycloalkyle C3-8 - alkyle C1-6, amino, alkyle C1-6 amino, di-(alkyle C1-6 )amino, alkyle C1-6 carbonyle, aminocarbonyle, alkyle C1-6 aminocarbonyle, di-(alkyle C1-6)aminocarbonyle, alcoxy C1-6, alkyle C1-6 thio, hydroxy, trifluorométhyle, trifluorométhylsulfonyle et alkyle C1-6 sulfonyle; ou un sel d'additif acide pharmaceutiquement acceptable de celui-ci. L'invention permet de fabriquer un médicament utile dans le traitement de troubles psychiatriques et neurologiques, et notamment de psychoses.

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