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COMBINACION DEL COMPUESTO GLYT1 CON ANTIPSICOTICOS
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
ALBERATI, DANIELA,MOREAU, JEAN-LUC,WETTSTEIN, JOSEPH G.
申请号:
PE0002352013
公开号:
PE11002013A1
申请日:
2011.08.05
申请国别(地区):
PE
年份:
2013
代理人:
摘要:
Referring to a Pharmaceutical Combination comprising an antipsychotic paliperidone and olanzapine, risperidone, quetiapine, Aripiprazole, ziprasidone or and a receptor antagonist (Glycine Transporter GlyT1 Inhibitor) of formula (i), where ar is a heteroaryl 6 members I with 1 to 3 nitrogen ATOMS, optionally substituted by HalogenC1 - C6 alkyl or haloalquilo C1 - C6 r1 is H or c1-c6 alkyl R2 is haloalquilo C1 - C6 R3, R4 and R6 are h, halogen, alkyl or alkoxy C1 - C6 C1 - C6 R5 is c1-c6 alkyl, optionally substituted by Halogen.Compounds of formula (i): Favorites [4 - (3 - 5 - fluoro - trifluoromethyl pyridin-2-yl) piperazin-1-yl] - 5 - [2 - (metanosulfonil 2,2,2-trifluoro-1 - ethoxy methyl) phenyl] - - [4 - methanone, RAC (3 - Chloro - 5 - trifluoromethyl - pyridin-2-yl) piperazin-1-yl] - 5 - [2 - (metanosulfonil 2,2,2-trifluoro-1 - ethoxy methyl) phenyl] - metanon A, RAC - [4 - (5 - bromo - (pyridin-2-yl) piperazin-1-yl] - 5 - [2 - (2,2, - metanosulfonil2 - trifluoro - 1 - methyl - ethoxy) - phenyl] - methanone, among others. Said composition is useful in the treatment of schizophreniaREFERIDA A UNA COMBINACION FARMACEUTICA QUE COMPRENDE UN FARMACO ANTIPSICOTICO TAL COMO OLANZAPINA, RISPERIDONA, PALIPERIDONA, ARIPIPRAZOL, QUETIAPINA O ZIPRASIDONA Y UN ANTAGONISTA DEL RECEPTOR DE GlyT1 (INHIBIDOR DEL TRANSPORTADOR DE GLICINA) DE FORMULA (I), DONDE Ar ES UN HETEROARILO DE 6 MIEMBROS CON 1 A 3 ATOMOS DE NITROGENO, OPCIONALMENTE SUSTITUIDO CON HALOGENO, ALQUILO C1-C6 O HALOALQUILO C1-C6 R1 ES H O ALQUILO C1-C6 R2 ES HALOALQUILO C1-C6 R3, R4 Y R6 SON H, HALOGENO, ALQUILO C1-C6 O ALCOXI C1-C6 R5 ES ALQUILO C1-C6 OPCIONALMENTE SUSTITUIDO CON HALOGENO. SON COMPUESTOS DE FORMULA (I) FAVORITOS: [4-(3-FLUORO-5-TRIFLUOROMETIL-PIRIDIN-2-IL)-PIPERAZIN-1-IL]-[5-METANOSULFONIL-2-(2,2,2-TRIFLUORO-1-METIL-ETOXI)-FENIL]-METANONA, rac-[4-(3-CLORO-5-TRIFLUOROMETIL-PIRIDIN-2-IL)-PIPERAZIN-1-IL]-[5-METANOSULFONIL-2-(2,2,2-TRIFLUORO-1-METIL-ETOXI)-FENIL]-METANONA, rac-[4-(5-BROMO-PIRIDIN-2
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