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2. 发明申请

WO1994014814A1 SESQUITERPENES, THEIR PREPARATION AND THEIR USE AS INHIBITORS ACTING ON THE GABA-BENZODIAZEPINE RECEPTOR 审中-公开
标题翻译： SESQUITERPENES，它们的制备及其作为抑制剂对GABA-苯二氮酮受体的作用
公开(公告)号：WO1994014814A1
公开(公告)日：1994-07-07
申请号：PCT/GB1993002632
申请日：1993-12-22
申请人： XENOVA LIMITED , RENNO, Didier, Vincent , O'BEIRNE, Gerard, Bernard , COPP, Brent, Raymond
发明人： XENOVA LIMITED
IPC分类号： C07D493/06
CPC分类号： C07D493/06 , C12P17/181
摘要： Sesquiterpenes of formula (I), wherein each of - &cir& _- &cir& _- &cir& _- &cir& _- &cir& _ and - &cir& _- &cir& _- &cir& _- &cir& _- &cir& _ is a single bond or one is a single bond and the other is a double bond; A, together with - &cir& _- &cir& _- &cir& _- &cir& _- &cir& _, - &cir& _- &cir& _- &cir& _- &cir& _- &cir& _ and the carbon atoms to which it is attached forms a ring selected from: (a); (b) wherein R is H or OH; (c); and (d); and Y is a double bond or, when A is a ring (a) as defined above Y is either a double bond or forms, together with the carbon atoms to which it is attached, an epoxide linkage &cir& NOt o &cir& NOt &cir& NOt obtainable from the fungal strain Acremonium strictum X06/15/458, and pharmaceutically and veterinarily acceptable salts thereof, are inhibitors of the binding of benzodiazepine to the GABA-benzodiazepine-Cl ionophore receptor complex. These compounds are prepared by (i) fermenting, in a source of carbon, nitrogen and inorganic salts, fungal strain X06/15/458 (IMI 354451) or a mutant thereof which produces the said sesquiterpenes, (ii) isolating the sesquiterpenes from the fermentation medium; and (iii) if desired, converting the said sesquiterpene into a pharmaceutically or veterinarily acceptable salt thereof.
摘要翻译：式（I）的倍半萜类化合物，其中每种化合物的单键或一种是单键或单一键债券，另一方是双重债券; A，连同 - ＆cir＆_-＆cir＆_-＆cir＆_-＆cir＆_-＆cir＆_， - ＆cir＆_-＆cir＆_-＆cir＆_-＆cir＆_-＆cir＆_及其所附的碳原子形成一个选自以下的环：（一个）; （b）其中R是H或OH; （C）; 和（d）; 并且Y是双键，或者当A是如上所定义的环（a）时，Y是双键或与其所连接的碳原子一起形成环氧键和可以被取代的环氧键来自真菌菌株Acremonium strictum X06 / 15/458及其药学上和兽医学上可接受的盐是苯并二氮杂与GABA-苯并二氮杂-Cl离子载体受体复合物结合的抑制剂。这些化合物通过以下方法制备：（i）在碳源，氮源和无机盐源中发酵生产所述倍半萜的真菌菌株X06 / 15/458（IMI 354451）或其突变体，（ii）从倍半萜烯中分离倍半萜烯发酵培养基; 和（iii）如果需要，将所述倍半萜烯转化为其药学上或兽医学上可接受的盐。

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