Bicyclic cb2 cannabinoid receptor ligands

C - Chemistry – Metallurgy – 07 – F

Patent

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C07F 9/09 (2006.01) A61K 31/02 (2006.01) A61K 31/075 (2006.01) A61K 31/12 (2006.01) A61K 31/122 (2006.01) A61K 31/35 (2006.01) C07C 39/08 (2006.01) C07C 39/23 (2006.01) C07C 45/29 (2006.01) C07C 45/54 (2006.01) C07C 45/71 (2006.01) C07C 49/433 (2006.01) C07C 49/657 (2006.01) C07C 49/747 (2006.01) C07C 49/753 (2006.01) C07C 69/025 (2006.01) C07C 69/035 (2006.01) C07C 69/30 (2006.01) C07C 69/40 (2006.01) C07C 69/60 (2006.01) C07C 251/42 (2006.01) C07C 251/44 (2006.01) C07C 255/40 (2006.01) C07F 9/12 (2006.01)

Patent

CA 2474135

The present invention relates to non-classical cannabinoids that are ligands of the peripheral cannabinoid receptor CB2, and to pharmaceutical compositions thereof comprising as an active ingredient novel (+) .alpha.-pinene derivatives, which are useful for prevention and treatment of autoimmune diseases including but not limited to rheumatoid arthritis, multiple sclerosis, systemic lupus erythematosus, myasthenia gravis, diabetes mellitus type I, hepatitis, psoriasis, tissue rejection in organ transplants, malabsorption syndromes such as celiac disease, pulmonary diseases such as asthma and Sjögren's syndrome, inflammation including inflammatory bowel disease, pain including peripheral, visceral, neurophathic inflammatory and referred pain, muscle spasticity, cardiovascular disorders including arrhythmia, hypertension and myocardial ischemia, neurological disorders including stroke, migraine and cluster headaches, neurodegenerative diseases including Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's chorea, prion-associated neurodegeneration, CNS poisoning and certain types of cancer.

L'invention concerne des cannabinoïdes non classiques qui sont des ligands du récepteur cannabinoïde périphérique CB2, et des compositions pharmaceutiques de ces composés, contenant en tant que principe actif de nouveaux dérivés (+) .alpha.-pinène qui sont utiles pour la prévention et le traitement des maladies auto-immunes notamment, mais non exclusivement, l'arthrite rhumatoïde, la sclérose en plaques, le lupus érythémateux disséminé, la myasthénie gravis, le diabète sucré de type I, l'hépatite, le psoriasis, les rejets de tissus lors de greffes d'organes, les syndromes de malabsorption, notamment la maladie coeliaque, les maladies pulmonaires telles que l'asthme et le syndrome de Sjögren, les inflammations, notamment les affections intestinales inflammatoires, les douleurs telles que les douleurs périphériques, viscérales, neuropathiques, inflammatoires et irradiées, la spasticité musculaire, les troubles cardio-vasculaires tels que l'arythmie, l'hypertension et l'ischémie myocardique, les troubles neurologiques tels que les accidents vasculaires cérébraux, les migraines, et les algies vasculaires de la face, les maladies neurodégénératives telles que la maladie de Parkinson, la maladie d'Alzheimer, la sclérose latérale amyotrophique, la chorée de Huntington, les dégénérescences neurologiques associées aux prions, les intoxications du SNC et certains types de cancers.

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