PURPOSE: To provide a new compd. having properties of an antagonistic material to melatonin recepter of very strong in vitro and in vivo.
CONSTITUTION: This new compd. is expressed by the formula I (where R is H or OR4 (R4 is alkyl, cycloalkyl, phenyl, etc.); R1 is H, CO-O-R4 (R5 is H, or alkyl); R2 is H, and R'2 is alkyl; R3 is C(=O)-(CH2)n-R6 (n is 0-3; R6 is H, alkyl, alkene, cycloalkyl, pyrrolidine, piperidine, piperazine, homopiperidine, homopiperazine, morpholine, thiomorpholine or the group of the formula II (X is O or S; n' is 0-3; R7 is alkyl, cycloalkyl or phenyl)) such as N-[2-(1-naphtyl) ethyl]cyclopropane carboxyamide. The compd. of the formula I (wherein R is H, OH and alkoxy group, R3 is C(=O)-(CH2)n-R6) is obtained by reacting the compds. of the formula III (R' is H, OH or alkoxy) with the acid halides of the formula IV (Hal is halogen).
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