| 摘要 |
The present invention relates to processes, and process intermediates useful in the preparation of (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid ((S)-1-hydroxymethyl-2,2-dimethyl-propyl)-amide (Compound 1) and crystalline forms thereof. The compound (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid ((S)-1-hydroxymethyl-2,2-dimethyl-propyl)-amide has been identified as a modulator of the cannabinoid 2 (CB2) receptor and useful in the treatment of CB2 receptor-mediated disorders, for example, pain, disorders of the immune system (such as, autoimmune disorders, type 1 hypersensitivity and allergic response, conditions associated with CNS inflammation, conditions associated with vascular inflammation, and other disorders associated with aberrant or unwanted immune response), bone and joint diseases (such as, osteoporosis and arthritis), eye disease, cough, cancer, and regenerative medicine. The present invention further provides pharmaceutical compositions comprising Compound 1 and the use of the pharmaceutical compositions for the treatment of CB2 receptor-mediated disorders. |
