发明名称 SESQUITERPENES, THEIR PREPARATION AND THEIR USE AS INHIBITORS ACTING ON THE GABA-BENZODIAZEPINE RECEPTOR
摘要 Sesquiterpenes of formula (I), wherein each of <IMG> and <IMG> is a single bond or one is a single bond aud the other is a double bond; A, together with <IMG>, <IMG> and tho 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 ? obtained from the fungal strain Acremonium strictum X06/15/458, and pharmaceutically and ceterenarily 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 strsin X06115/458 (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 sesquiterpenes into a pharmaceutically or veterinarily acceptable salt thereof.
申请公布号 CA2151251(A1) 申请公布日期 1994.07.07
申请号 CA19932151251 申请日期 1993.12.22
申请人 XENOVA LIMITED 发明人 RENNO, DIDIER VINCENT;O'BEIRNE, GERARD BERNARD;COPP, BRENT RAYMOND
分类号 A61K31/35;A61P21/02;A61P25/08;A61P25/20;A61P43/00;C07D493/06;C07D493/16;C12P17/18;C12R1/645;(IPC1-7):C12P17/18;C12N1/14 主分类号 A61K31/35
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