PYRAZOL-5-ONES

摘要

1429141 Pyrazolin-5-ones BAYER AG 16 April 1974 [17 April 1973 19 Dec 1973] 16507/74 Heading C2C The invention comprises compounds of formula (including tautomers thereof, especially when R is amino), wherein R is H, amino, alkyl, alkenyl, CF 3 or Ph; R1 is H, alkyl, alkenyl or an optionally substituted aryl or aralkyl radical; R2 is an alkyl group; and R3 is a pyridyl radical or an aryl radical carrying 1 or 2 identical or different substituents, which are selected from halogen, CF 3 , alkyl, alkenyl, and alkoxy radicals, or carrying one mono- or di-alkylamino, CF 3 O, nitro, nitrile, carbamoyl, alkyl- or dialkylcarbamoyl, sulphamyl, or alkyl- or dialkylsulphamyl radical, or a group -B, -CO.B or -SO 2 .B (in which B is a saturated ring containing a nitrogen atom in the 1-position) or a -SO n alkyl group (in which n=0, 1 or 2), optionally together with 1 or 2 substituents selected from alkyl, alkenyl, alkoxy, halogen and CF 3 , or carrying none or 1 only of these substituents and a fused branched or unbranched, saturated or unsaturated 5-, 6- or 7- membered ring optionally containing 1 or 2 oxygen or sulphur atoms. In examples, these compounds are prepared by (a) reacting R2R3CHNHNH 2 with an appropriate ring-forming co-reactant, (2) replacing a compound in which R is halogen, by amino, (3) hydrolysing a compound in which R is (e.g.) NHCO 2 Et, or (4) introducing the R2R3CH group by N1-substitution. Therapeutic compositions having diuretic, saluretic, antihypertensive and antithrombotic activity comprise compounds of the above formula, and may be administered orally, parenterally, rectally, topically, or by spray.