PURPOSE: To provide a new compound having powerful and centrally selective acetylcholinesterase-inhibitory activity, thus useful as a medicine for improving brain function or an antidemential agent.
CONSTITUTION: The compound of formula I (R is H, alkyl, alkenyl, etc.; R1-R4 are each H, halogen, alkyl, phenyl, alkoxy, acyl, OH, etc.; n is 1-3; A is alkylene), e.g. 3-(2-(1-benzyl-4-piperizyl)ethyl)-6,7-dimethoxy-1,2-benzoisoxazole. The compound of the formula I can be obtained by acylation between an oxime derivative of formula II (P is either the same as R or a protecting group for acetyl, benzyl, benzyloxycarbonyl, etc.) and a compound of formula W-COOH (W is lower alkyl or phenyl) to form a compound of formula III, which is, in turn, put to ring closure reaction.
| JPH08231428 | SUPERFICIAL LOCAL MEDICINE COMPOSITION |
| WO/2013/087954 | COMPOUNDS THAT INHIBIT BETA AMYLOID PEPTIDE AGGREGATION |
| WO/2013/107291 | THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE |
MURAKAMI OSAMU
TAKEHARA SHUZO
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