发明授权
- 专利标题: Crystalline forms and processes for the preparation of cannabinoid receptor modulators
- 专利标题(中): 用于制备大麻素受体调节剂的结晶形式和方法
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申请号: US14001133申请日: 2012-02-24
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公开(公告)号: US09458136B2公开(公告)日: 2016-10-04
- 发明人: Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter
- 申请人: Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter
- 申请人地址: US CA San Diego
- 专利权人: Arena Pharmaceuticals, Inc.
- 当前专利权人: Arena Pharmaceuticals, Inc.
- 当前专利权人地址: US CA San Diego
- 代理机构: Fish & Richardson P.C.
- 代理商 Lyle W. Spruce
- 国际申请: PCT/US2012/026506 WO 20120224
- 国际公布: WO2012/116276 WO 20120830
- 主分类号: A61K31/4965
- IPC分类号: A61K31/4965 ; C07D403/04 ; A61K31/497
摘要:
The present invention relates to crystalline forms 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 that modulate the activity of the cannabinoid CB2 receptor and are therefore useful in the treatment of CB2 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; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis; and Parkinson's disease.
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