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    PYRAZOLE CARBOXAMIDE DERIVATIVES AS TAAR MODULATORS FOR USE IN THE TREATMENT OF SEVERAL DISORDERS, SUCH AS DEPRESSION, DIABETES AND PARKINSON'S DISEASE
    42.
    发明专利
    PYRAZOLE CARBOXAMIDE DERIVATIVES AS TAAR MODULATORS FOR USE IN THE TREATMENT OF SEVERAL DISORDERS, SUCH AS DEPRESSION, DIABETES AND PARKINSON'S DISEASE 未知

    公开(公告)号：SG11201501958QA

    公开(公告)日：2015-04-29

    申请号：SG11201501958Q

    申请日：2013-09-11

    Applicant: HOFFMANN LA ROCHE

    Inventor： GALLEY GUIDO ,  NORCROSS ROGER ,  PFLIEGER PHILIPPE

    IPC: C07D403/12 ,  A61K31/4155 ,  A61K31/454 ,  A61K31/5377 ,  A61P25/00 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

    Abstract: The present invention relates to compounds of formula wherein R1 is phenyl, optionally substituted by halogen, lower alkyl, lower cycloalkyl, lower alkoxy, cyano, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, lower alkoxy substituted by halogen or lower alkoxy substituted by hydroxy; or is pyridine-2, 3 or 4-yl, optionally substituted by halogen, lower alkyl, lower cycloalkyl, cyano, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, lower alkoxy, lower alkoxy substituted by halogen or lower alkoxy substituted by hydroxyl; or is pyrimidin-2, 4 or 5-yl, optionally substituted by halogen, lower alkyl, lower cycloalkyl, lower alkyl substituted by hydroxy or lower alkyl substituted by halogen; or is pyrazin-2-yl, optionally substituted by halogen, lower alkyl, lower cycloalkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy or cyano; or is 2,2-difluorobenzo[d][1,3]dioxol-5-yl, or is thiazolyl, optionally substituted by lower alkyl substituted by halogen; R2 is hydrogen or lower alkyl; R3 is hydrogen, amino or lower alkyl; Z is a bond, —CH2— or —O—; or to a pharmaceutically suitable acid addition salt thereof. It has now been found that the compounds of formulas 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.

    2-aminooxazolinas como ligandos de TAAR1
    44.
    发明专利
    2-aminooxazolinas como ligandos de TAAR1 未知

    公开(公告)号：ES2525229T3

    公开(公告)日：2014-12-19

    申请号：ES08708678

    申请日：2008-02-05

    Applicant: HOFFMANN LA ROCHE

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

    IPC: C07D263/28 ,  A61K31/421 ,  A61K31/422 ,  A61P25/00 ,  C07D413/06

    Abstract: Un compuesto de la fórmula**Fórmula** en la que C1-7 R1 es arilo o heteroarilo, dichos grupos arilo y heteroarilo pueden estar sin sustituir o sustituidos de una a tres veces por sustituyentes elegidos entre el grupo formado por cicloalquilo, fenilo, feniloxi, bencilo, benciloxi, halógeno, alquilo C1-7, alcoxi C1-7, heteroarilo, piperidin-1-ilo o por alquilo C1-7 sustituido por halógeno, o es arilo o heteroarilo, en los que por lo menos un átomo de hidrógeno se ha reemplazado por deuterio o tritio; R2 es hidrógeno, alquilo C1-7 o es bencilo sin sustituir o sustituido por alcoxi C1-7 o halógeno; o R1 y R2 junto con el átomo de N al que están unidos forman un 2,3-dihidroindol-1-ilo o 3,4-dihidro-quinolin-1-ilo; R3 es hidrógeno o alquilo C1-7; o las sales de adición de ácido farmacéuticamente idóneas del mismo.

    Heterocyclic amine derivatives
    45.
    发明专利
    Heterocyclic amine derivatives 未知

    公开(公告)号：NZ616150A

    公开(公告)日：2014-09-26

    申请号：NZ61615012

    申请日：2012-03-21

    Applicant: HOFFMANN LA ROCHE

    Inventor： GALLEY GUIDO ,  NORCROSS ROGER ,  PFLIEGER PHILIPPE

    IPC: C07D207/09 ,  A61K31/4025 ,  A61K31/4462 ,  A61K31/5375 ,  A61K31/5377 ,  C07D211/26 ,  C07D265/30 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

    Abstract: The disclosure relates to compounds of formula I wherein the various unspecified groups are as described in the specification. The disclosure also relates to the process to synthesise it and the use of these compounds to treat 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. Example compounds include: (RS)-5-Chloro-N-(5-(morpholin-2-yl)pyridin-2-yl)pyridin-2-amine (RS)-5-Bromo-N-(5-(morpholin-2-yl)pyridin-2-yl)pyridin-2-amine (RS)-5-Cyclopropyl-N-(5-(morpholin-2-yl)pyridin-2-yl)pyrimidin-2-amine [(RS)-1-(5-Bromo-pyridin-2-yl)-2,2,2-trifluoro-ethyl]-((RS)-4-pyrrolidin-3-yl-phenyI)-amine (5-Bromo-pyridin-2-ylmethyl)-((S)-4-morpholin-2-yl-phenyl)-amine (6-Methoxy-pyridin-2-ylmethyl)-((S)-4-morpholin-2-yl-phenyl)-amine (4-Methyl-benzyl)-((S)-4-morpholin-2-yl-phenyl)-amine 4-[((S)-4-Morpholin-2-y l-phenylamino)-methyl]-benzonitrile ((S)-4-Morpholin-2-yl-phenyl)-(4-trifluoromethyl-benzyl)-amine ((S)-4-Morpholin-2-yl-phenyl)-(4-trifluoromethoxy-benzyl)-amine.

    SUBSTITUTED BENZAMIDE DERIVATIVES
    46.
    发明专利
    SUBSTITUTED BENZAMIDE DERIVATIVES 未知

    公开(公告)号：ZA201308401B

    公开(公告)日：2014-08-27

    申请号：ZA201308401

    申请日：2013-11-07

    Applicant: HOFFMANN LA ROCHE

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

    IPC: A61K20060101 ,  A61P20060101 ,  C07D20060101

    Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, X, Z, Ar, and n are as described in the claims, Ar is phenyl or heteroaryl, selected from the group consisting of 1H-indazole-3yl, pyridine-2-yl, pyridine-3-yl, pyridine-4-yl, pyrimidine-5-yl, 1H-pyrazole-3-yl, 1H-pyrazole-4-yl and 1H-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.

    49.
    发明专利
    未知

    公开(公告)号：BRPI0806940A2

    公开(公告)日：2014-05-06

    申请号：BRPI0806940

    申请日：2008-01-23

    Applicant: HOFFMANN LA ROCHE

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

    IPC: C07D263/28 ,  A61K31/421 ,  A61K31/422 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P25/00 ,  C07D413/04

    Abstract: The invention relates to compounds of formula I wherein X, Y, R1, R2, and n are as defined herein or to a pharmaceutically suitable acid addition salt thereof. The invention also relates to pharmaceutical compositions containing such compounds and methods for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases include depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and 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.

    DERIVADOS DE BENZAMIDA SUSTITUIDA
    50.
    发明专利
    DERIVADOS DE BENZAMIDA SUSTITUIDA 未知

    公开(公告)号：ECSP13013073A

    公开(公告)日：2014-01-31

    申请号：ECSP13013073

    申请日：2013-12-10

    Applicant: HOFFMANN LA ROCHE

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

    IPC: C07D265/30 ,  A61K31/4245 ,  A61P25/00 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14

    Abstract: La presente invención se refiere a compuestos de la fórmulaen la que:R1 es hidrógeno, halógeno, ciano, alquilo inferior, alquilo inferior sustituido por halógeno, alcoxi inferior, alcoxi inferior sustituido por halógeno o C(O)NH2,o es fenilo opcionalmente sustituido por halógeno, ciano o alcoxi inferior sustituido por halógeno, o es 2,2-difluorbenzo[d][1,3]dioxol-5-ilo, o es 6-(trifluormetil)-pirazin-2-ilo o 5-(trifluormetil)pirazin-2-ilo o es 6-(trifluormetil)pirimidin-4-ilo, o es 6-(trifluormetil)-piridin-3-ilo, o es 5-cianopirazin-2-ilo o es 2-(tri-fluormetil)pirimidin-4-ilo;n es el número 1 ó 2R2 es halógeno, alquilo inferior o ciano y R3 es hidrógeno, oR2 es hidrógeno y R3 es halógeno, alquilo inferior o ciano;X es un enlace, -NR'-, -CH2NH- o -CHR'-;R' es hidrógeno o alquilo inferior; Z es un enlace, -CH2- u -O-;Ar es fenilo o es heteroarilo elegido entre el grupo formado por 1H-indazol-3-ilo, piridin-2-ilo, piridin-3-ilo, piridin-4-ilo, pirimidin-5-ilo, 1H-pirazol-3-ilo, 1H-pirazol-4-ilo y 1H-pirazol-5-ilo;o una sal de adición de ácido farmacéuticamente apropiada de los mismos; que pueden utilizarse para el tratamiento de la depresión, los trastornos de ansiedad, el trastorno bipolar, el trastorno de hiperactividad con déficit de atención (ADHD), 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, la hipertensión, el abuso de sustancias, 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 malfunción de la homeostasis de la temperatura corporal, los trastornos del sueño y del ritmo circadiano y los trastornos cardiovasculares.

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