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    SUBSTITUTED BENZAMIDE DERIVATIVES
    51.
    发明专利
    SUBSTITUTED BENZAMIDE DERIVATIVES 未知

    公开(公告)号：SG194840A1

    公开(公告)日：2013-12-30

    申请号：SG2013082656

    申请日：2012-06-06

    Applicant: HOFFMANN LA ROCHE

    Inventor： GALLEY GUIDO ,  NORCROSS ROGER ,  PFLIEGER PHILIPPE ,  TRUSSARDI RENE

    Abstract: The present invention relates to compounds of formula (I) wherein R1 is hydrogen, halogen, cyano, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen or C(O)NH2, or is phenyl optionally substituted by halogen, cyano or lower alkoxy substituted by halogen, or is 2,2-difluorobenzo[d][1,3]dioxol-5-yl, or is 6-(trifluoromethyl)pyrazin-2-yl or 5-(trifluoromethyl)pyrazin-2-yl or is 6-(trifluoromethyl)pyrimidin-4-yl, or is 6- (trifluoromethyl)pyridin-3-yl, or is 5-cyanopyrazin-2-yl or is 2- (trifluoromethyl)pyrimidin-4-yl; n is 1 or 2 R2 is halogen, lower alkyl or cyano and R3 is hydrogen, or R2 is hydrogen and R3 is halogen, lower alkyl or cyano; X is a bond, -NR'-, -CH2NH- or -CHR'-; R' is hydrogen or lower alkyl; Z is a bond, -CH2- or -O-; Ar is phenyl or is heteroaryl, selected from the group consisting of 1H-indazole-3yl, pyridine-2-yl, pyridine-3-yl, pyridine-4-yl, pyrimidine-5-yl, lH-pyrazole-3-yl, 1H- pyrazole-4-yl or lH-pyrazole-5-yl; or to a pharmaceutically suitable acid addition salt thereof, which may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse, metabolic disorders, 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.

    Aminomethyl-2-imidazoles with affinity with the trace amine associated receptors
    53.
    发明专利
    Aminomethyl-2-imidazoles with affinity with the trace amine associated receptors 未知

    公开(公告)号：AU2007312389B2

    公开(公告)日：2012-02-23

    申请号：AU2007312389

    申请日：2007-10-09

    Applicant: HOFFMANN LA ROCHE

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

    IPC: C07D233/64 ,  A61K31/417 ,  A61P25/00 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12

    Abstract: The present invention relates to compounds of Formula (I) and to their pharmaceutically active salts. It has been found that the compounds of formula (I) have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), 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.

    SUBSTITUTED DIBENZO-AZEPINE AND BENZO-DIAZEPINE DERIVATIVES USEFUL AS GAMMA-SECRETASE INHIBITORS
    54.
    发明专利
    SUBSTITUTED DIBENZO-AZEPINE AND BENZO-DIAZEPINE DERIVATIVES USEFUL AS GAMMA-SECRETASE INHIBITORS 未知

    公开(公告)号：CA2541470C

    公开(公告)日：2011-11-29

    申请号：CA2541470

    申请日：2004-09-27

    Applicant: HOFFMANN LA ROCHE

    Inventor： FLOHR ALEXANDER ,  GALLEY GUIDO ,  JAKOB-ROETNE ROLAND ,  KITAS ERIC ARGIRIOS ,  PETERS JENS-UWE ,  WOSTL WOLFGANG

    IPC: C07D223/18 ,  A61K31/55 ,  A61K31/5513 ,  A61P25/28 ,  C07D223/16 ,  C07D243/12 ,  C07D243/24 ,  C07D409/12

    Abstract: The present invention relates to compounds of the general formula (I) Wherein R1 is -(CHR~)q-aryl or -(CHR')q-heteroaryl, which are unsubstituted or mono, di- or tri-substituted by lower alkyl, lower alkoxy, CF3 or halogen, or is lower alkyl, lower alkenyl, -(CH2)n-Si(CH3)3, -(CH2)n-O-lower alkyl, -(CH2)n-S-lower alkyl, -(CH2)q-cycloalkyl, -(CH2)n-[CH(OH)]m-(CF2)p-CHqF(3-q), or is -(CH2)n-CR2-CF3, wherein the two R radicals form together with the carbon atom a cycloalkyl ring; R' is hydrogen or lower alkyl; n is 1, 2 or 3; in is 0 or 1; p is 0, 1, 2, 3, 4, 5 or 6; q is 0, 1, 2 or 3; R2 is hydrogen or lower alkyl; R3 is hydrogen, lower alkyl, -CH2CF2CF3, CH2CF3, (CH2)2CF3, CF3, CHF2, CF3, CHF2, CH2F, or is aryl, optionally mono, di or tri-substituted by halogen, or is (CH2)nNR5R6, wherein R5 and R6 are independently from each other hydrogen or lower alkyl; R4 is one of the following groups wherein R7is hydrogen, lower akl, -(CH2)n-CF3 or -(CH2)n-cycloalkyl; R8 is hydrogen, lower alkyl, -C(O)-phenyl, -C(O)-lower alkyl, -C(O)O-(CH2)n- cycloalkyl, -C(O)O-(CH2)n-lower alkyl, -C(O)NH-(CH2)n-lower alkyl or -C(O)NH~(CH2).-CyClOalkYl; R9 is hydrogen, lower alkyl, -(CH2)n-cycloalkyl or -(CH2)n-CF3; and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racernates or diastereomeric mixtures thereof for the treatment of Alzheimer's disease..

    NUEVAS 2-AMINOOXAZOLINAS COMO LIGANDOS TAAR1 PARA TRASTORNOS CNS
    55.
    发明专利
    NUEVAS 2-AMINOOXAZOLINAS COMO LIGANDOS TAAR1 PARA TRASTORNOS CNS 未知

    公开(公告)号：CO6321133A2

    公开(公告)日：2011-09-20

    申请号：CO09072375

    申请日：2009-07-13

    Applicant: HOFFMANN LA ROCHE

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

    IPC: A61K31/421 ,  A61P3/04 ,  A61P3/10 ,  C07D263/28 ,  C07D413/04

    Abstract: La invención se refiere al uso de compuestos de la Fórmulaen la queR1 es hidrógeno, deuterio, tritio, alquilo inferior, alcoxi inferior, alquilo inferior sustituido por halógeno, alcoxi inferior sustituido por halógeno, halógeno, fenilo opcionalmente sustituido por halógeno, o es feniloxi, bencilo, benciloxi, -COO-alquilo inferior, -O-(CH2)o-O-alquilo inferior, NH-cicloalquilo, cicloalquilo o tetrahidropiran-4-iloxi, dichos sustituyentes para n>1 pueden ser iguales o diferentes;X es un enlace, -CHR-, -CHRCHR'-, -OCH2-, -CH2OCHR-, -CH2-CH2CH2-, -SCH2-, -S(O)2CH2-, -CH2SCH2-, -CH2N(R)CH2-, -cicloalquil-CH2- o SiRR' -CH2-;R/R' con independencia entre sí pueden ser hidrógeno, alquilo inferior o alquilo inferior sustituido por halógeno; R2 es hidrógeno, fenilo o alquilo inferior; Y es fenilo, naftilo, tiofenilo, piridinilo, cicloalquilo, 1,2,3,4-tetrahidro-naftalen-2-ilo, 2,3-dihidrobenzo-[1, 4]dioxin-6-ilo o benzo [1, 3]dioxol-5-ilo;n es el número 0, 1, 2 ó 3;o es el número 2 ó 3;o a una sal de adición de ácido farmacéuticamente aceptable para la fabricación de medicamentos destinados al tratamiento de enfermedades relacionadas con la función biológica de los receptores asociados con aminas trazas, dichas enfermedades son: la depresión, los trastornos de ansiedad, el trastorno bipolar, el trastorno de hiperactividad con déficit de atención, los trastornos relacionados con el estrés, los trastornos psicóticos, la esquizofrenia, las enfermedades neurológicas, la enfermedad de Parkinson, los trastornos neurodegenerativos, la enfermedad de Alzheimer, la epilepsia, la migraña, el abuso de sustancias y los trastornos metabólicos, los trastornos de ingestión de comida, la diabetes, las complicaciones diabéticas, la obesidad, la dislipidemia, los trastornos de consumo y asimilación de energía, los trastornos y la malfunción de la temperatura corporal, la homeostasis, los trastornos del sueño y del ritmo circadiano y los trastornos cardiovasculares.

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