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Crystalline forms and processes for the preparation of condensed azacycles ( cannabinoid receptor modulators)
专利权人:
ARENA PHARMACEUTICALS INC.
发明人:
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’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’s disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis; and Parkinson’s disease.
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http://www.ckcest.cn/home/
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