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BRPI0413536A - derivados de 1-benzoil-piperazina como inibidores da absorção de glicina para o tratamento de psicose - Google Patents

derivados de 1-benzoil-piperazina como inibidores da absorção de glicina para o tratamento de psicose

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Publication number
BRPI0413536A
BRPI0413536A BRPI0413536-9A BRPI0413536A BRPI0413536A BR PI0413536 A BRPI0413536 A BR PI0413536A BR PI0413536 A BRPI0413536 A BR PI0413536A BR PI0413536 A BRPI0413536 A BR PI0413536A
Authority
BR
Brazil
Prior art keywords
alkyl
halogen
substituted
alkoxy
hydrogen
Prior art date
Application number
BRPI0413536-9A
Other languages
English (en)
Inventor
Daniela Alberati-Giani
Synese Jolidon
Robert Narquizian
Roger David Norcross
Emmanuel Pinard
Henri Stalder
Matthias Heinrich Nettekoven
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of BRPI0413536A publication Critical patent/BRPI0413536A/pt
Publication of BRPI0413536B1 publication Critical patent/BRPI0413536B1/pt
Publication of BRPI0413536B8 publication Critical patent/BRPI0413536B8/pt

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    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/10Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms
    • C07D295/104Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
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    • C07D295/16Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
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    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

"DERIVADOS DE 1-BENZOIL-PIPERAZINA COMO INIBIDORES DA ABSORçãO DE GLICINA PARA O TRATAMENTO DE PSICOSE". A invenção se refere a compostos da fórmula em que Ar é arila substituído ou heteroarila de 6 membros não substituído ou substituído, contendo um, dois ou três átomos de nitrogênio e em que os grupos arila ou heteroarila podem ser substituídos por um ou mais substituintes selecionados do grupo que consiste de hidróxi, halogênio, CN, (C~ 1~-C~ 6~)-alquila, (C~ 1~-C~ 6~)-alquila substituído por halogênio, (C~ 1~-C~ 6~)-alcóxi, (C~ 1~-C~ 6~)-alcóxi substituído por halogênio, NR¬ 7¬R¬ 8¬, C(O)R¬ 9¬ OU SO~ 2~R¬ 10¬; R¬ 1¬ é hidrogênio ou (C~ 1~-C~ 6~)-alquila; R¬ 2¬ é halogênio, (C~ 1~-C~ 6~)-alquila, (C~ 2~-C~ 6~)-alquenila, em que um átomo de hidrogênio pode ser substituído por CN, C(O)-R¬ 9¬ ou (C~ 1~-C~ 6~)-alquila ou é (C~ 2~C~ 6~)-alquinila, (C~ 1~-C~ 6~)-alquila substituído por halogênio, -(CH~ 2~)~ n~-(C~ 3~-C~ 7~)-cicloalquila, -(CH~ 2~)~ n~-heterocicloalquila, -C(O)-R¬ 9¬, -(CH~ 2~)~ n~-arila ou -(CH~ 2~)~ n~-heteroarila de 5 ou 6 membros contendo um, dois ou três heteroátomos, selecionados do grupo que consiste de oxigênio, enxofre ou nitrogênio em que arila, cicloalquila, heterocicloalquila e heteroarila são não substituídos ou substituídos por um ou mais substituintes selecionados do grupo que consiste de hidróxi, halogênio, (C~ 1~-C~ 6~)-alquila, (C~ 1~-C~ 6~)-alquila substituído por halogênio ou (C~ 1~-C~ 6~)-alcóxi; R¬ 3¬, R¬ 4¬ e R¬ 6¬ independentemente um dos outros são hidrogênio, hidróxi, halogênio, (C~ 1~-C~ 6~)-alquila ou (C~ 1~-C~ 6~)-alcóxi; R¬ 5¬ é NO~ 2~, CN, C(O)R¬ 9¬, SO~ 2~R¬ 10~ ou NR¬ 11¬R¬ 12¬; R¬ 7¬ e R¬ 8¬ independentemente um dos outros são hidrogênio ou (C~ 1~-C~ 6~)-alquila; R¬ 9¬ é (C~ 1~-C~ 6~)-alquila, (C~ 3~-C~ 6~)-cicloalquila, (C~ 1~-C~ 6~)-alcóxi ou NR¬ 7¬R¬ 8¬; R¬ 10¬ é (C~ 1~-C~ 6~)-alquila, (C~ 3~-C~ 6~)- cicloalquila ou NR¬ 7¬R¬ 8¬; R¬ 11¬ e R¬ 12¬ independentemente um dos outros são hidrogênio ou formam junto com o átomo de N ao qual estão ligados em grupo heteroarila de 5 membros; n é 0, 1 ou 2; e sais de adição ácida farmaceuticamente aceitáveis dos mesmos para o tratamento de psicoses, dor, disfunção neurodegenerativa na memória e no aprendizado,esquizofrenia,demência e outras doenças nas quais os processos cognitivos estão prejudicados, tais como os distúrbios de déficit de atenção ou doença de alzheimer.
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