| abstract |
NEW MATERIAL:The clathrate compound consisting of the acylated indole derivative of formula I (R is H, lower alkyl or lower acyl; n is 1 or 2) and cyclodextrin. n USE: Preventive and remedy for cardiovascular infarction, post-operative thrombosis, thrombosis in the vessel after surgical operation, and arteriosclerosis. It has blood platelet coagulation inhibiting activity. It has low individual variation in absorption, sure effect, and increased absorptivity, and can be easily converted to drug preparation. n PROCESS: The clathrate compound can be prepared by contacting the acylated indole derivative [e.g. 3-benzoyl-1-(hydroxy-2-propyl)-2-methylindole] with cyclodextrin in the presence of water. Th compound of formula I wherein n is 1 is obtained e.g. by dehydrogenating the compound of formula II (R' is lower alkyl or lower acyl) and if necessary hydrolyzing the product. n COPYRIGHT: (C)1982,JPO&Japio |