1208984-79-5Relevant articles and documents
CARBOCYCLIC GLYT1 RECEPTOR ANTAGONISTS
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Page/Page column 22, (2011/04/14)
The present invention relates to the use of a compound of general formula (I) wherein R1/R2 are independently from each other hydrogen, lower alkyl, -CH2)o-cycloalkyl for o being 0 or 1, or are benzyl or heterocycloalkyl; or R1 and R2 are together with the N-atom to which they are attached a ring containing -(CH2)3-, -(CH2)4-, -(CH2)5-, -(CH2)2-O-(CH2)2-, -(CH2)2-S-(CH2)2-, -(CH2)2-NR-(CH2)2-, -(CH2)2-C(O)-(CH2)2-, -(CH2)2-CF2-(CH2)2-, -CH2-CHR-(CH2)2, -CHR-(CH2)3, CHR-(CH2)2-CHR-, or is the ring 2,6-diaza-spiro[3.3]heptane-2-carboxylic acid tert-butyl ester and R is hydroxy, halogen, cycloalkyl, or C(O)O-lower alkyl; X is -(CH2)4-, -(CH2)3-, -(CH2)2- or -CH2-; R3 is S-lower alkyl, CF3, OCHF2, lower alkoxy, lower alkyl, phenyl, cycloalkyl or halogen; R4 is CF3, lower alkoxy, lower alkyl, halogen and n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers thereof for the manufacture of a medicament for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.
TETRAHYDRO-PYRAN DERIVATIVES
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Page/Page column 8, (2011/08/08)
The present invention relates to a compound of formula I wherein R1/R2 are independently from each other hydrogen, (CR2)o-cycloalkyl, optionally substituted by lower alkyl or hydroxy, or are lower alkyl or heterocycloalkyl, and o is 0 or 1; andR may be the same or different and is hydrogen or lower alkyl; orR1 and R2 may form together with the N atom to which they are attached a heterocycloalkyl group, selected from the group consisting of pyrrolidinyl, piperidinyl, 3-aza-bicyclo[3.1.0]hex-3-yl or 2-aza-bicyclo[3.1.0]hex-2-yl, which are optionally substituted by hydroxy;R3 is S-lower alkyl, lower alkyl, lower alkoxy or cycloalkyl;R3′ is hydrogen, lower alkyl substituted by halogen, lower alkyl or lower alkoxyR4 is lower alkyl substituted by halogen, lower alkyl or lower alkoxy;X is —O— or —CH2—;X′ is —O— or —CH2—; with the proviso that one of X or X′ is always —O— and the other is —CH2—; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. It has been found that the compounds of formula I are good inhibitors of the glycine transporter 1 (GlyT-1) and therefore they may be used for the treatment of schizophrenia.
GlyT1 RECEPTOR ANTAGONISTS
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Page/Page column 8, (2010/03/31)
The present invention relates to a compound of formula I wherein R1, R2, X, Ar1 and Ar2 are as defined herein and to pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to their correspond
