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Use what preparation as the crystalline form and preparation method of the condensed azacyclo- of Cannibinoid receptor modulators
专利权人:
艾尼納製藥公司;Arena Pharmaceuticals, Inc.;艾尼纳制药公司
发明人:
A.C.布莱克本,A.C.布萊克本,韩相敦,韓相敦,R.M.琼斯,R.M.瓊斯,安东尼奥.加利多.蒙塔尔班,安東尼奧.加利多.蒙塔爾班,B.B.帕尔,B.B.帕爾,J.K.鲁特,J.K.魯特
申请号:
MOJ003666
公开号:
MOJ003666B
申请日:
2019.04.29
申请国别(地区):
MO
年份:
2019
代理人:
摘要:
The present invention relates to (1aS, 5aS) -2- (4- oxygen-pyrazine -2- base) -1a, 2,5,5a- tetrahydro -1H-2, the crystalline form and its pharmaceutical composition of 3- diaza-cyclopropyl simultaneously [a] pentalene -4- formic acid ((S) -1- hydroxymethyl -2,2- Dimethyl-propyl)-amide (compound 1)The crystalline form and composition adjust the activity of Cannabined receptor and therefore available what treats the receptor-mediated illness of CB2,The receptor-mediated illness of CB2 for example,Osteoarthritis; Pain; Hyperalgia; Allodynia; Inflammatory hyperalgesia; Neuropathic hyperalgesia; Acute nociception; Osteoporosis; Spasticity related with multiple sclerosis; Autoimmune conditions; Allergic response; CNS inflammation,Such as atherosclerosis; Undesirable immunocyte activity,And inflammation related with illness selected from the following: osteoarthritis,Allergic reaction,Behcet's disease,Transplant rejection,Vasculitis,Gout,Spondylitis,Viral disease,Bacteriosis,Lupus,Inflammatory bowel disease,Oneself immunity hepatitis and type 1 diabetes; Age-related macular degeneration; Cough; Leukaemia; Lymthoma; Cns tumor; Prostate cancer; Alzheimer disease; The damage of stroke induction; It is dull-witted; Amyotrophic lateral sclerosis; And Parkinson's disease.本發明涉及(1aS,5aS)‑2‑(4‑氧‑吡嗪‑2‑基)‑1a,2,5,5a‑四氫‑1H‑2,3‑二氮雜‑環丙并[a]并環戊二烯‑4‑甲酸((S)‑1‑羥基甲基‑2,2‑二甲基‑丙基)‑酰胺(化合物1)的晶形及其藥物組合物,所述晶形和組合物調節大麻素受體的活性並因此可用於治療CB2受體介導的病症,所述CB2受體介導的病症例如,骨關節炎;疼痛;痛覺過敏;異常性疼痛;炎性痛覺過敏;神經性痛覺過敏;急性傷害感受;骨質疏鬆症;與多發性硬化症有關的痙攣狀態;自身免疫性病症;變應性應答;CNS炎症,例如動脈粥樣硬化;不期望的免疫細胞活動,以及與選自以下的病症有關的炎症:骨關節炎、過敏性反應、貝切特氏病、移植排異、血管炎、痛風、脊椎炎、病毒性疾病、細菌性疾病、狼瘡、炎性腸病、自身免疫性肝炎和1型糖尿病;年齡相關性黃斑變性;咳嗽;白血病;淋巴瘤;CNS腫瘤;前列腺癌;阿爾茨海默病;卒中誘導的損傷;痴呆;肌萎縮性側索硬化;以及帕金森病。
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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