BLACKBURN ANTHONY C.,HAN SANGDON,MONTALBAN ANTONIO GARRIDO,PAL BIMAN B.,RUETER JAIMIE KARYN,JONES ROBERT M.
申请号：
NZ61478712
公开号：
NZ614787A
申请日:
2012.02.24
申请国别(地区):
NZ
年份:
2014
代理人:
摘要：
Disclosed are anhydrous crystalline forms of condensed azacycles with pyrazole and pyrazine components, and a process for preparing the compounds by crystallising from acetonitrile and water, and other non-selective solvates. The anhydrous crystalline form 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 pharmaceutical compositions thereof are disclosed which modulate the activity of the cannabinoid CB receptor and are therefore useful in the treatment of CB receptor-mediated disorders, for example, osteoarthritis； pain； hyperalgesia； allodynia； inflammatory hyperalgesia； neuropathic hyperalgesia； acute nociception； osteoporosis； multiple sclerosis-associated spasticity； autoimmune disorders； allergic reactions CNS inflammation for example； atherosclerosis； undesired immune cell activity, and inflammation associated with a disorder selected from: osteoarthritis, anaphylaxis, Behcet&rsquo；s disease, graft rejection, vasculitis, gout, spondylitis, viral disease, bacterial disease, lupus, inflammatory bowel disease, autoimmune hepatitis, and type 1 diabetes mellitus； age-related macular degeneration； cough； leukaemia； lymphoma； CNS rumours； prostate cancer； Alzheimer&rsquo；s disease； stroke-induced damage； dementia； amyotrophic lateral sclerosis； and Parkinson&rsquo；s disease.
