申请人:Bayer Aktiengesellschaft
公开号:US03952008A1
公开(公告)日:1976-04-20
1-Substituted pyrazole-5-ones of the formula ##SPC1## And pharmaceutically acceptable, nontoxic salts thereof, Wherein R is hydrogen or amino; R.sup.1 is hydrogen, alkyl, alkenyl, unsubstituted or substituted aryl or unsubstituted or substituted aralky; X is A. ethylene, ethylene wherein 1 hydrogen atom on one of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms, ethylene wherein 1 hydrogen atom on each of the two carbon atoms is substituted by alkyl of 1 to 4 carbon atoms or said ethylene which is linked to R.sup.2 via an oxygen or sulphur atom; B. propenyl, propenyl wherein 1 hydrogen atom on one, two or three of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms, said propenyl being linked to the N.sup.1 atom of the pyrazol ring via its methylene moiety; or C. methylene; provided that when X is methylene, R.sup.1 is not hydrogen if R is amino; R.sup.2 is aryl unsubstituted or substituted by: A. 1 or 2 of the same or different substituents selected from the group consisting of halogen, trifluoromethyl, alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 8 carbon atoms and lower alkoxy; B. cycloalkyl of 5, 6 or 7 carbon atoms or cycloalkenyl of 5, 6 or 7 carbon atoms; C. alkylamino, dialkylamino, cyano, trifluoromethoxy, nitro, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, or said carbamoyl wherein the nitrogen atom is a member of a heterocyclic ring, sulphamyl, alkylsulphamyl, dialkylsulphamyl, or said sulphamyl wherein the nitrogen is a member of a heterocyclic ring, or --SO.sub.n alkyl wherein n is 0, 1 or 2; D. alkylamino, dialkylamino, cyano, trifluoromethoxy, nitro, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, or said carbamoyl wherein the nitrogen atom is a member of a heterocyclic ring, sulphamyl, alkylsulphamyl, dialkylsulphamyl or said sulphamyl wherein the nitrogen is a member of a heterocyclic ring, or --SO.sub.n alkyl wherein n is 0, 1 or 2, and 1 or 2 of the same or different substituents selected from the group consisting of alkyl, alkenyl, alkoxy, halogen, and trifluoromethyl; or E. a fused, saturated or unsaturated 5-, 6-, or 7-membered ring or said ring containing 1 or 2 oxygen or sulphur atoms; Are useful for their diuretic, saluretic, antihypertensive and antithrombotic effects.
式为## SPC1 ##的1-取代吡唑-5-酮及其药学上可接受的、无毒的盐,其中R为氢或氨基;R.sup.1为氢、烷基、烯基、未取代或取代的芳基或未取代或取代的芳基烷基;X为A.乙烯,其中一个碳原子上的1个氢原子被1-4个碳原子的烷基取代,两个碳原子上的每个氢原子都被1-4个碳原子的烷基取代,或通过氧或硫原子与R.sup.2连接的乙烯;B.丙烯基,其中一个、两个或三个碳原子上的1个氢原子被1-4个碳原子的烷基取代,该丙烯基通过其亚甲基部分与吡唑环的N.sup.1原子连接;或C.亚甲基;但当X为亚甲基时,若R为氨基,则R.sup.1不为氢;R.sup.2为未取代或取代的芳基,该芳基被以下1种或2种相同或不同的取代基取代:A.卤素、三氟甲基、1-8个碳原子的烷基、2-8个碳原子的烯基和较低的烷氧基中的1种或2种;B.5、6或7个碳原子的环烷基或5、6或7个碳原子的环烯基;C.烷基氨基、二烷基氨基、氰基、三氟甲氧基、硝基、氨基甲酰基、烷基氨甲酰基、二烷基氨甲酰基或其中的氮原子是杂环环的羧酰基,磺酰氨基、烷基磺酰氨基、二烷基磺酰氨基或其中的磺酰氨基是杂环环的,或--SO.sub.n烷基,其中n为0、1或2;D.烷基氨基、二烷基氨基、氰基、三氟甲氧基、硝基、氨基甲酰基、烷基氨甲酰基、二烷基氨甲酰基或其中的氮原子是杂环环的羧酰基,磺酰氨基、烷基磺酰氨基、二烷基磺酰氨基或其中的磺酰氨基是杂环环的,或--SO.sub.n烷基,其中n为0、1或2,以及来自以下群组中1种或2种相同或不同的取代基:烷基、烯基、烷氧基、卤素和三氟甲基;或E.融合的、饱和的或不饱和的5、6或7元环,或含有1或2个氧或硫原子的环,具有利尿、盐利尿、降压和抗血栓作用。