Dual nk1/nk3 antagonists against schizophrenia

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 213/75 (2006.01) A61K 31/44 (2006.01) A61K 31/4436 (2006.01) A61K 31/4439 (2006.01) A61K 31/444 (2006.01) A61P 25/18 (2006.01) C07D 409/04 (2006.01)

Patent

CA 2575894

The present invention relates to the use of compounds of the general formula (I) wherein R1 is lower alkyl or halogen; R2 is hydrogen or halogen; R3- (CHR')nOH, phenyl, optionally substituted by -(CHR')nOH, or is a saturated, partial saturated or aromatic 5-or 6-membered heterocyclic ring with one heteroatom, selected from the group consisting of-N(R4)-, -N=, formula (II), - S- or -S(O)2, and which rings are optionally substituted by - (CHR~)nOH; R~ is independently from ~n~ hydrogen or - (CH2)nOH; R4 is hydrogen, -S(O2)-lower alkyl or -C(O)-lower alkyl; X is -O-, -CH2O-, -S- or a bond; n is 1 or 2; or to pharmaceutically active acid-addition salts thereof, for the preparation of medicaments for the treatment of schizophrenia.

Cette invention a pour objet le recours à des compositions de formule générale (I) où R1 est un alkyle ou un halogène plus faible ; R2est un hydrogène ou un halogène; R3 -(CHR')nOH, est optionnellement substitué par -(CHR')nOH, est saturé, partiellement saturé ou est un anneau aromatique hétérocyclique à 5 ou 6 membres avec un seul hétéroatome, sélectionnées parmi les compositions N(R4)-, -N=, de formule (II), -S- ou -S(O)2, et dont les anneaux sont optionnellement substitués par - (CHR~)nOH; où R~ est indépendant de ~n~ hydrogène ou de - (CH2)nOH; où R4 est un hydrogène, -S(O2)- est un alkyle inférieur ou -C(O)-un alkyle inférieur; X est -O-, -CH2O-, -S- ou un maillon; n est 1 ou 2; ou par des sels d~adjonction d~acide pharmaceutiquement actifs présents dans ces compositions permettant de préparer les médicaments nécessaires au traitement de la schizophrénie.

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