Heterocycle-substituted 3-alkyl azetidine derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 403/10 (2006.01) A61K 31/41 (2006.01) A61K 31/4245 (2006.01) A61P 25/00 (2006.01) C07D 413/10 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2630040

Compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB 1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB 1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), and non- alcoholic steatohepatitis (NASH). (see formula I)

La présente invention concerne des composés atypiques de formule structurelle (I) qui sont des antagonistes et/ou des antagonistes inverses du récepteur Cannabinoide-1 (CB1) et qui sont utiles dans le traitement, la prévention et la suppression de maladies facilitées par le récepteur CB1. Les composés de la présente invention sont utiles comme médicaments agissant centralement dans le traitement de la psychose, des déficits de la mémoire, des désordres cognitifs, de la maladie d'Alzheimer, de la migraine, de la neuropathie, des désordres neuro-inflammatoires y compris la sclérose en plaques et le syndrome Guillain-Barre et les séquelles inflammatoires d'une encéphalite virale, d'accidents cérébro-vasculaires et de traumatismes crâniens, de désordres dus à l'anxiété, du stress, de l'épilepsie, de la maladie de Parkinson, des désordres moteurs et de la schizophrénie. Ces composés sont également utiles dans le traitement de désordres découlant de la toxicomanie, le traitement de l'obésité ou autres désordres alimentaires ainsi que dans le traitement de l'asthme, de la constipation, de la pseudo-obstruction intestinale chronique, de la cirrhose du foie, de la stéatose hépatique non alcoolique (NAFLD) et de la stéatohépatite non alcoolique (NASH).

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