Sesquiterpenes, their preparation and their use as...

Details Sesquiterpenes, their preparation and their use as... Sesquiterpenes, their preparation and their use as...

C - Chemistry, Metallurgy

12

P

C12P 17/18 (2006.01) A61K 31/35 (2006.01) C07D 493/06 (2006.01) C07D 493/16 (2006.01) C12N 1/14 (2006.01)

Patent

CA 2151251

Sesquiterpenes of formula (I), wherein each of Image and Image is a single bond or one is a single bond aud the other is a double bond; A, together with Image , Image 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.

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