Hoffmann-la Roche Inc.

Roche Palo Alto LLC

Richard Hugh Philip Porter

Georg Jaeschke

Eric Vieira

Sabine Kolczewski

Bernd Buettelmann

Simona Maria Ceccarelli

Patrick Schnider

Paul Spurr

Anthony P D W Ford

Yu Zhong

The present invention relates to imidazole derivatives of formula I wherein R, R, Rand Rare described hereinabove. These compounds can be used in the treatment or prevention of mGluR5 receptor mediated disorders. These compounds are useful, inter alia, in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer' disease, cognititve disorders and memory deficits, as well as chronic and acute pain.

Imidazole derivatives

The present invention relates to diazole derivatives of the general formula wherein A, E, R, Rand Rare as defined in application and pharmaceutical compositions containing them. The invention also relates to use of such compounds for the treatment of diseases mediated by the metabotropic glutamate receptors (mGluR), such as anxiety, chronic and acute pain, protection against liver damage, urinary incontinence, obesity, Fragile-X and autism, Alzheimer's disease, epilepsy, schizophrenia, ischemia, Huntington's chorea, amyotrophic lateral sclerosis (ALS), dementia caused by AIDs, and Parkinson's disease.

Diazole derivatives

The present invention relates to process for the preparation of an imidazole derivative of formula I, wherein R, R, Rand Rare described hereinabove. These compounds can be used in the treatment or prevention of mGluR5 receptor mediated disorders. These compounds are useful, inter alia, in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer' disease, cognitive disorders and memory deficits, as well as chronic and acute pain.

The present invention relates to imidazole derivatives of formula I wherein R, R, R, R, X, Y and R are described hereinabove, or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition comprising the imidazole derivatives of formula I, a process for preparing a compound of formula I, and a method of treating or preventing acute and/or chronic neurological disorder comprising administering to a patient in need of such treatment and/or prevention a therapeutically effective amount of said pharmaceutical composition. These disorders include Alzheimer's disease. These disorders also include mild cognitive impairment.

The present invention is concerned with novel pyrazine 2-carboxyamide derivatives of formula (I) wherein R, Rand Rare as defined in the specification. These compounds are useful for the treatment of CNS disorders.

Pyrazine-2-carboxyamide derivatives

The present invention is concerned with novel thiazole 4-carboxyamide derivatives of the general formula (I) and with methods for the preparation thereof, which compounds are useful as metabotropic glutamate receptor antagonists: wherein Rto Rare as defined in the specification.

Thiazole-4-carboxyamide derivatives

The present invention relates to imidazole derivatives of formula I wherein R, R, Rand Rare described hereinabove. These compounds can be used in the treatment or prevention of mGluR5 receptor mediated disorders. These compounds are useful, inter alia, in the treatment of genitourinary diseases.

The present invention relates to heterocyclic derivatives of formula I wherein R, Rand Rare as defined in the description and claims, which compounds are metabotropic glutamate receptor 5 antagonists.

Naphthyridin derivatives

The invention relates to compounds of formula I: wherein Rto Rare as defined in the specification, to processes for their preparation, to pharmaceutical compositions containing them, and to methods for treating CNS disorders.

Pyridine-2-carboxyamide derivatives

The present invention relates to imidazole derivatives of formula I wherein R, R, Rand Rare described hereinbelow. These compounds can be used in the treatment or prevention of mGluR5 receptor mediated disorders. These compounds are useful, inter alia, in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer' disease, cognitive disorders and memory deficits, as well as chronic and acute pain.

The present invention relates to imidazole derivatives of the general formula wherein R, R, Rand Rare described hereinbelow. These compounds can be used in the treatment or prevention of mGluR5 receptor mediated disorders. These compounds are useful, interalia, in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer's disease, cognitive disorders and memory deficits, as well as chronic and acute pain.

Heteroaryl-substituted imidazole derivatives

The present invention provides 4-[1-Aryl-imidazol-4-ylethynyl]-2-alkyl-pyridine and 1-heteroaryl-imidazol-4-ylethynyl]-2-alkyl-pyridine derivatives and pharmaceutically acceptable salts thereof for the treatment or prevention of disorders mediated in full or in part by metabotropic glutamate receptor 5. These disorders include, e.g. acute, traumatic and chronic degenerative processes of the nervous system, such as Alzheimer's disease, senile dementia, Parkinson's disease, Huntington's chorea, amyotrophic lateral sclerosis and multiple sclerosis, psychiatric diseases, such as schizophrenia and anxiety, depression, pain and drug dependency.

The present invention relates to imidazole derivatives of the general formula wherein R, R, Rand Rare as defined hereinabove. This invention also relates to the compound's pharmaceutically acceptable salt and processes for the preparation thereof. These compounds can be used for the manufacture of pharmaceutical compositions for the treatment and prevention of mGluR5 receptor mediated disorders. These compounds are useful, inter alia, in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer's disease, cognitive disorders and memory deficit disorders, as well as chronic and acute pain.

Growing community of inventors

Reinach, Switzerland

Richard Hugh Philip Porter