Hoffmann-la Roche Inc.

Vernalis Research Limited

F. Hoffmann-la Roche Ag

Henri Stalder

Roger David Norcross

Guido Galley

Katrin Groebke Zbinden

Emmanuel Pinard

Matthias Heinrich Nettekoven

Synese Jolidon

Robert Narquizian

Sabine Kolczewski

Andre Szente

Hans P Marki

Romano Derungs

Daniela Alberati-Giani

Marius Hoener

Annick Goergler

Philippe Guerry

Patrizio Mattei

Hans G Richter

Stephan Roever

Paul Hebeisen

Simona Maria Ceccarelli

Raffaello Masciadri

Jean-Luc Specklin

David Reginald Adams

Howard Langham Mansell

Pierre-Charles Wyss

Jonathan Richard Anthony Roffey

Jonathan Mark Bentley

James Edward Paul Davidson

Claire Elizabeth Dawson

Ingrid Heinze-Krauss

Urs Weiss

Robert Mark Pratt

George P Yiannikouros

Ashley Roger George

Rudolf L Then

Jacques Mizrahi

Valeri Runtz

Hans-Peter Marty

Kerry Wilkinson

Roger Norcross

The present invention relates to a compound of formula I wherein R, R, and Ar are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. These compounds and their pharmaceutical compositions are useful in the treatment of neurological and neuropsychiatric disorders.

Piperidine derivatives

The invention relates to compounds of formula I wherein

2-aminooxazolines as TAAR1 ligands

The present invention relates to amino-4-methyl imidazoles and pharmaceutically-acceptable salts thereof. The compound 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.

Aminomethyl-4-imidazoles

The invention relates to imidazole derivatives which have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The invention also relates to a pharmaceutically-suitable acid-addition salt of the above compound. The invention further relates to a composition comprising an imidazole derivative as described above, or a pharmaceutically-suitable acid-addition salt thereof, and to processes for preparing such compounds.

Imidazole derivatives

The present invention relates to compounds of formula I whereinR, R, R, Ar, n and o are as defined herein and to their pharmaceutically acceptable active salts. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful 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-azetidinemethaneamines and 2-pyrrolidinemethaneamines as TAAR-ligands

The invention relates to the use of compounds of formula I wherein the substituents are described in the description and claims for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease. The invention also relates to some compounds of formula I and pharmaceutical compositions containing them.

Amines or amino alcohols as GLYT1 inhibitors

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 whereinR, Ar, R, R, R, and n are as defined in the specificationand 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.

Methods for treating CNS disorders with 4-imidazole derivatives

The invention relates to a compound of formula wherein The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of CNS disorders.

TAAR1 ligands

The invention relates to compounds of formula whereinR, R, and Rare as defined herein and to a pharmaceutically suitable acid addition salts thereof for the treatment of CNS disorders.

The present invention relates a method 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

Method for the treatment of CNS disorders with substituted 2-imidazoles or imidazole derivatives

The present invention relates to compounds of formula I, wherein The invention relates also to a pharmaceutically-acceptable acid-addition salt of such a compound, processes for making the compound, and a composition comprising such a compound.

2-imidazoles

The present invention relates to a compound of formula I, wherein The invention relates also to a pharmaceutically-acceptable acid-addition salt of such a compound, methods for making the compound, and a composition comprising such a compound. It has been found that the compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1.

Substituted 4-imidazoles

The present invention relates to compounds of formula I wherein The invention relates also to processes for preparing such compounds, compositions comprising such a compound or a pharmaceutically-acceptable acid addition salt thereof, and a method of treating a disease or disorder in a patient comprising administering such a compound, or pharmaceutically-acceptable acid addition salt thereof, to a patient in need of such treatment.

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Basel, Switzerland

Henri Stalder