abstract |
NEW MATERIAL: A thiadiazole derivative of formula I [wherein R 1 is phenyl (which may be substituted with methyl, methoxyl or CF 3 ); R 2 is H or an alkyl; R 3 is formula II (wherein A 1 is an alkyl; R 4 and R 5 are each H or an alkyl; or they together with the N may form a five- or six-membered heterocycle), formula III, formula IV, formula V or the like; and R 2 , R 3 and the N may form formula VI (wherein R 6 is methyl or ethyl)], an inorganic salt thereof or an organic acid addition salt thereof. n EXAMPLE: 2-(3-Dimethylaminopropylamino)-5-(2,4,6-trimethylphenyl)-1,3,4- thiadiazole. n USE: An agonist for a muscarine receptor and a remedy against degeneration syndromes, especially disturbances in memory and senile dementia, occasioned by aging. n PREPARATION: A 2-halogeno-1,3,4-thiadiazole of formula VII (wherein X is Cl or Br) is reacted with a compound of the formula: NHR' 2 R' 3 (wherein R' 2 and R' 3 are each R 2 or R 3 , and either of them is a protective group when they are H atoms simultaneously) to obtain a compound of formula I, which is optionally converted into a medicinally acceptable salt. n COPYRIGHT: (C)1990,JPO |