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Piperidines substituted by aroylamino and heteroaroylamino as inhibitors of GLYT-1
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
KOLCZEWSKI, SABINE,PINARD, EMMANUEL,STALDER, HENRI
申请号:
ES10700563
公开号:
ES2445143T3
申请日:
2010.01.19
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A compound of the general formula wherein R1 is hydrogen, C1-7 alkyl, CD3, - (CH2) n-CHO, - (CH2) nO-C1-7 alkyl, - (CH2) n-OH, - (CH2 ) C3-7 n-cycloalkyl, wherein the cycloalkyl is a saturated or partially saturated ring or is heterocycloalkyl, selected from the group consisting of piperazinyl, pyrrolidinyl, oxetanyl, morpholinyl, piperidinyl or tetrahydropyranyl; R2 is hydrogen, halogen, hydroxy, C1-7 alkyl, C1-7 dialkyl, -OCH2-O-C1-7 alkyl or C1-7 alkoxy; or the piperidine ring together with R2 forms a spiro ring, chosen from 4-aza-spiro [2.5] oct-6-yl; Ar is aryl or heteroaryl, which are optionally substituted by one, two or three substituents chosen from halogen, C1-7 alkyl, C1-7 alkyl substituted by halogen, C1-7 alkoxy substituted by halogen, cycloalkylC3-7, wherein the cycloalkyl is a saturated or partially saturated ring, C1-7 alkoxy, S- C1-7 alkyl, heteroaryl, C3-7 heterocycloalkyl selected from the group consisting of piperazinyl, pyrrolidinyl, oxetanyl, morpholinyl, piperidinyl or tetrahydropyranyl or by phenyl optionally substituted by R ' and R 'is halogen, C1-7 alkyl, C1-7 alkoxy or C1-7 alkoxy substituted by halogen, or is heteroaryl; R is C1-7 alkyl, C3-7 cycloalkyl, wherein the cycloalkyl is a saturated or partially saturated, heterocycloalkyl ring, selected from the group consisting of piperazinyl, pyrrolidinyl, oxetanyl, morpholinyl, piperidinyl or tetrahydropyranyl, or is aryl or heteroaryl, wherein aryl and heteroaryl are optionally substituted by one or two R '; n is the number 0, 1, 2 or 3; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and / or optical isomer.Un compuesto de la fórmula general en la que R1 es hidrógeno, alquilo C1-7, CD3, -(CH2)n-CHO, -(CH2)n-O-alquilo C1-7, -(CH2)n-OH, -(CH2)n-cicloalquilo C3-7, endonde el cicloalquilo es un anillo saturado o parcialmente saturado o es heterocicloalquilo, elegido del grupoconstituido por piperacinilo, pirrolidinilo, oxetanilo,
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