PURPOSE: To obtain a new (thio)morpholine derivative which is useful as a prophylactic agent for hyperlipemia, hyperglycemia and obesity, further hypertension and osteoporosis.
CONSTITUTION: A morpholine or thiomorpholine derivative of formula I [R1 to R5 are H, 1-5C alkyl, 1-5C alkoxy, halogen, OH, CF3; R6 is H, 1-5C alkyl; A is O, S; B is a bond, O, S; m is 1 to 5; X is N, CH; Y is NH, O, S; Z is H, formula II (R7 is H, 1-5C alkyl; n is 1 to 5)] or its salts, for example, 5-{4-[2-(2-(3-chlorophenyl)morpholino)propoxyl]benzyl}thiazolidine-2,4-dione. The compound of the formula I where B is O or S is obtained by detritylation of a compound of the formula (IV) where Z1 is trityl, resulting from the reaction of a compound of the formula (II) with a compound of the formula (III) (B1 is O, S; Z1 is formula II other than R7 is H, trityl).
FUJITA TAKESHI
AIZAWA YUICHI
KANAI TSUTOMU
SANO HIROMI
HORIKOSHI HIROYOSHI
FUJIWARA TOSHIHIKO