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Use of the enantiomer 1S,2R of milnacipran for the preparation of a medicament
专利权人:
发明人:
드레쥐나우꾸르, 쟝,그로스, 리샤르
申请号:
KR1020057015077
公开号:
KR1011853220000B1
申请日:
2004.02.16
申请国别(地区):
KR
年份:
2012
代理人:
摘要:
The use of a mixture of enantiomers of Milnacipran and/or its metabolites or salts, enriched in the dextrorotatory enantiomer F2695, is claimed in medicines for treating pathological disorders treated by the double inhibition of serotonin and noradrenaline recapture, while limiting the risk of cardiovascular disturbance. ACTIVITY : Antidepressant; Muscular-Gen; Immunomodulator; Analgesic; Antiinflammatory; Uropathic; Antiaddictive. MECHANISM OF ACTION : Serotonin inhibitor; Noradrenaline recapture inhibitor. In tests used to determine the capture of noradrenaline and serotonin and the binding of paroxetine in rats, results showed that F2695 was twice as active as the racemic mixture (F2207) and 25 times as active as the levorotatory enantiomer (F2696) in the capture of noradrenaline, that F2695 was three times as active as F2207 and 12 times as active as F2696 in the capture of serotonin and that F2695 was twice as active as F2207 and 10 times as active as F2696 in binding paroxetine. 본 발명은 심장혈관 장애 및/또는 기관 및/또는 조직 독성의 위험을 제한시키면서, 세로토닌(5-HT) 및 노르아드레날린 (NA) 재흡수의 이중 억제에 의해 조절할 수 있는 질환을 예방 또는 치료하고자 하는 약제의 제조를 위하여 밀나시프란의 공간형태 (1S, 2R) 거울상이성체가 풍부한 거울상 이성체, 및/또는 적어도 하나의 그의 대사물질은 물론 그의 약제학적으로 허용되는 염의 혼합물의 용도에 관한 것이다.
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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