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    NUEVAS 2-AMINOOXAZOLINAS COMO LIGANDOS DE TAAR1
    72.
    发明专利
    NUEVAS 2-AMINOOXAZOLINAS COMO LIGANDOS DE TAAR1 未知

    公开(公告)号：PE17832008A1

    公开(公告)日：2008-12-18

    申请号：PE0003152008

    申请日：2008-02-13

    Applicant: HOFFMANN LA ROCHE

    Inventor： GALLEY GUIDO ,  ZBINDEN KATRIN GROEBKE ,  NORCROSS ROGER ,  STALDER HENRI

    IPC: A61K31/421 ,  A61K31/422 ,  C07D263/28

    CPC classification number: C07D263/28 ,  C07D413/06

    Abstract: SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE R1 ES ARILO, HETEROARILO SUSTITUIDO O NO POR CICLOALQUILO, FENILO, FENILOXI, BENCILO, ENTRE OTROS; R2 ES H, ALQUILO INFERIOR, BENCILO SUSTITUIDO O NO POR ALCOXI, HALOGENO, ENTRE OTROS; R3 ES H, ALQUILO INFERIOR. SON COMPUESTOS PREFERIDOS: (R)-4-[(ETIL-FENIL-AMINO)-METIL]-4,5-DIHIDRO-OXAZOL-2-ILAMINA; (R)-4-[(ISOPROPIL-FENIL-AMINO)METIL]-4,5-DIHIDRO-OXAZOL-2-ILAMINA; (S)-4-{[(3,4-DICLORO-FENIL)-METIL-AMINO]-METIL}-4,5-DIHIDRO-OXAZOL-2-ILAMINA; ENTRE OTROS. REFERIDA TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS TIENEN AFINIDAD CON LOS RECEPTORES ASOCIADOS CON LAS AMINAS TRAZAS (TAAR) EN ESPECIAL CON TAAR1 UTILES EN EL TRATAMINETO DE DEPRESION, ANSIEDAD, TRASTORNO BIPOLAR, ENTRE OTROS

    76.
    发明专利
    未知

    公开(公告)号：NO20083356L

    公开(公告)日：2008-10-21

    申请号：NO20083356

    申请日：2008-07-31

    Applicant: HOFFMANN LA ROCHE

    Inventor： GALLEY GUIDO ,  ZBINDEN KATRIN GROEBKE ,  NORCROSS ROGER ,  STALDER HENRI ,  HOENER MARIUS

    IPC: C07D233/54

    Abstract: The present invention relates to methods for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, Ar, R1, R1′, R2, and n are as defined in the specification and to their pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms. The invention also relates to novel compounds of formula I, compositions containing them, and methods for their preparation.

    2-IMIDAZOLES SUSTITUIDOS
    77.
    发明专利
    2-IMIDAZOLES SUSTITUIDOS 未知

    公开(公告)号：PE20080930A1

    公开(公告)日：2008-07-19

    申请号：PE2007001499

    申请日：2007-10-31

    Applicant: HOFFMANN LA ROCHE

    Inventor： GALLEY GUIDO ,  ZBINDEN KATRIN GROEBKE ,  NORCROSS ROGER ,  STALDER HENRI

    IPC: A61K31/4164 ,  A61K31/4178 ,  A61K31/4709 ,  A61K31/5375 ,  A61K31/538 ,  A61P25/00 ,  C07D401/06 ,  C07D403/06 ,  C07D413/06

    Abstract: SE REFIERE A COMPUESTOS 2-IMIDAZOLES SUSTITUIDOS DE FORMULA (I) DONDE R1 ES H O ALQUILO INFERIOR(C1-C7); R2 ES H O ALQUILO INFERIOR(C1-C7); R3 ES H, HALOGENO, ALCOXI INFERIOR(C1-C7), ENTRE OTROS; X ES -CH2-, -CH- U -O-; Y ES UN ENLACE, -CH2- O -CH-; Z ES -CH2- O -CH-; m ES DE 0 A 2; n ES DE 0 A 2. SON COMPUESTOS PREFERIDOS: 1-(1H-IMIDAZOL-2-ILMETIL)-2,3-DIHIDRO-1H-INDOL, 5-BROMO-1-(1H-IMIDAZOL-2-ILMETIL)-2,3-DIHIDRO-1H-INDOL, 7-ETIL-1-(1H-IMIDAZOL-2-ILMETIL)-2,3-DIHIDRO-1H-INDOL, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS TIENEN AFINIDAD CON LOS RECEPTORES ASOCIADOS CON LAS AMINAS TRAZAS (TAAR) SIENDO UTILES EN EL TRATAMIENTO DE DEPRESION, TRASTORNOS DE ANSIEDAD, TRASTORNO BIPOLAR, ESQUIZOFRENIA, ENFERMEDAD DE PARKINSON

    4-IMIDAZOLINES AS TAAR'S LIGANDS
    80.
    发明专利
    4-IMIDAZOLINES AS TAAR'S LIGANDS 未知

    公开(公告)号：CA2671838A1

    公开(公告)日：2008-06-26

    申请号：CA2671838

    申请日：2007-12-10

    Applicant: HOFFMANN LA ROCHE

    Inventor： STALDER HENRI ,  NORCROSS ROGER ,  GALLEY GUIDO ,  GROEBKE ZBINDEN KATRIN

    IPC: C07D233/64 ,  A61K31/415 ,  A61P9/00 ,  A61P25/00

    Abstract: The invention relates to compounds of formula (I) wherein R is hydrogen, lower alkyl or amino; X-R1 is -CH2 -, -CH(lower alkoxy)- or -CH(OH)- and Y-R 2 is -CH2, -CH(lower alkyl)-, -CH(lower alkoxy)- -O-, -S-, -S(O)-, -S(O)2 -, -CH(phenyl)- or -C(lower alkyl)2 -; or X-R1 is -NH- and Y-R2 is -CH2, -CH(l ower alkyl)-, -CH(lower alkoxy)-, -CH(phenyl)- or -C(lower alkyl)2 -; Ar is phenyl, napthyl or benzofuranyl, which rings are unsubstituted or substitute d by one or more substituents, selected from the group consisting of lower a lkyl, lower alkyl substituted by halogen, halogen, lower alkoxy, lower alkox y substituted by halogen, hydroxy, amino, di-alkylamino, morpholinyl, phenyl , benzyl or by O-benzyl; or to pharmaceutically suitable acid addition salts . It has been found that the compounds of formula (I) have a good affinity t o the trace amine associated receptors (TAARs), especially for TAAR1. The co mpounds may be used for the treatment of depression, anxiety disorders, bipo lar disorder, attention deficit hyperactivity disorder (ADHD), stress-relate d disorders, psychotic disorders such as schizophrenia, neurological disease s such as Parkinson's disease, neurodegenerative disorders such as Alzheimer 's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesit y, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and cir cadian rhythm, and cardiovascular disorders.

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