| 摘要 |
<p>1-Aryl-4-arylsulphonyl-3-aminopropoxy -1H-pyrazole derivs. of formula (I) and their salts are new: (where R1 is H, halogen, 1-3C alkyl or alkoxy or CF3- gp. in meta or para position; R2, R3, R4 are H, halogen, 1-3C alkyl or alkoxy or CF3-; R5, R6 are each H or lower alkyl or together, and with the N atom to which they are attached, form a 5- or 6-membered heterocycle (piperidine or pyrrolidine) opt. contg. another heteroatom such as O (morpholine). (I) have hypolipaemic and hypocholesterolaemic properties. Suitable daily doses are 0.3-0.15 g, split up into two or three doses per 24 hrs. Even in amounts far greater than this (20-30 mg/kg) (I), eg. 4-gamma-(p-chlorophenylsulphonyl)-3-dimethylaminopropoxy-1-phenyl- -1H-pyrazole (I') affects neither the CNS nor the cardiac/circulatory and respiratory system, and is non-ulcerogenic. (I) are of low toxicity e.g. LD50 for mice is 125 mg/kg i.p. and 670 mg/kg p.o.</p> |
