Anthony C. BLACKBURN,Sangdon HAN,Robert M. JONES,Anthony GARRIDO MONTALBAN,Biman B. PAL,Jaimie Karyn RUETER
申请号：
MX2013009760
公开号：
MX346533B
申请日:
2012.02.24
申请国别(地区):
MX
年份:
2017
代理人:
摘要：
The present invention relates to crystalline forms of (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)- 1a,2,5.5a-tetrahydro- 1 H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid ((S)- 1 - hydroxymcthyl-2.2-dimcthyl-propyl)-amidc (Compound 1) and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor and are therefore useful in t 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 rumors； prostate cancer； Alzheimer's disease； stroke-induced damage； dementia； amyotrophic lateral sclerosis； and Parkinson's disease.La presente invención se refiere a formas cristalinas de ((S)-1-hidroximetil-1,2-dimetil-propil)-amida de ácido (1aS,5aS)-2-(4-oxi-pirazin-2-il)-1a,2,5,5a-tetrahidro-1H-2,3-diaz a-ciclopropa[a}pentalen-4- carboxílico y composiciones farmacéutica de la misma que modulan la actividad del receptor canabinoide CB2 y por lo tanto son útiles en el tratamiento de desórdenes mediados por receptor CB2, por ejemplo, osteoartritis； dolor； hiperalgesia； alodinia； hiperalgesia inflamatoria； hiperalgesia neuropática, nocicepción aguda； osteoporosis； espasticidad asociada con esclerosis múltiple； desórdenes autoinmunes； reacciones alérgicas inflamación de CNS por ejemplo； aterosclerosis； actividad celular inmune no deseada, e inflamación asociada con un desorden seleccionado de: osteoartritis, anafilaxis, enfermedad d
