公开(公告)号：US4117143A

公开(公告)日：1978-09-26

申请号：US766684

申请日：1977-02-08

申请人： Eike Moller ,  Karl-August Meng, deceased ,  Egbert Wehinger ,  Harald Horstmann ,  Friedel Seuter

发明人： Eike Moller ,  Karl-August Meng, deceased ,  Egbert Wehinger ,  Harald Horstmann ,  Friedel Seuter

IPC分类号： C07D231/20 ,  A61K31/415 ,  A61K31/445

CPC分类号： C07D231/20 ,  Y10S514/822 ,  Y10S514/869

摘要： Pyrazoles of the formula ##STR1## wherein R is hydrogen, alkyl, trifluoromethyl, aryl, aralkyl or a heterocycle;R.sup.2 is hydrogen, alkyl, aryl or aralkyl;R.sup.3 is an unsubstituted or substituted carboacyl or sulphonyl moiety;X is (a) methylene; (b) ethylene; (c) ethylene wherein 1 hydrogen atom on one or both of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms; (d) ethylene, or ethylene wherein 1 hydrogen atom on one or both of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms, linked to R.sup.2 via an oxygen or sulphur atom; (e) propenyl; or (f) propenyl wherein a hydrogen atom on 1, 2 or 3 of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms; said propenyl moiety being linked to the N.sup.1 atom via a methylene moiety; andR.sup.2 is aryl unsubstituted or substituted by 1 or 2 of the same or different substituents selected from the group consisting of alkyl, alkenyl, alkoxy, halo, trifluoromethyl, trifluoromethoxy, cycloalkyl, cycloalkenyl, mono- or di-alkylamino, nitro, cyano, unsubstituted or substituted carboxamido, unsubstituted or substituted sulphonamido and SO.sub.n -alkyl wherein n is 0 to 2, or aryl having 2 substitutents which together form a branched or unbranched, saturated or unsaturated 5- to 7-membered isocyclic or heterocyclic ring, said heterocyclic ring containing 1 or 2 oxygen or sulphur atoms, or pyridyl;Are useful for their diuretic, saluretic, antihypertensive and antithrombotic properties.

公开(公告)号：US4112109A

公开(公告)日：1978-09-05

申请号：US766187

申请日：1977-02-07

申请人： Eike Moller ,  Karl Meng, deceased ,  Egbert Wehinger ,  Harald Horstmann ,  Friedel Seuter

发明人： Eike Moller ,  Karl Meng, deceased ,  Egbert Wehinger ,  Harald Horstmann ,  Friedel Seuter

IPC分类号： C07D231/20 ,  C07D231/28 ,  A61K31/415

CPC分类号： C07D231/20 ,  C07D231/28 ,  Y10S514/822 ,  Y10S514/869

摘要： Pyrazoles of the formula ##STR1## wherein R is hydrogen, alkyl, aryl, aralkyl, trifluoromethyl or a heterocycle;R.sup.1 is aryl or aralkyl unsubstituted or substituted by halo, trifluoromethyl, alkyl, alkoxy or nitro; or a halo-substituted alkylthio moiety;R.sup.2 is lower alkyl; phenyl; or benzyl;R.sup.3 is aryl unsubstituted or substituted by alkyl, alkenyl, alkoxy, halo, trifluoromethyl, trifluoromethoxy, mono- or di-alkylamino, nitro, cyano, carboxamido, sulphonamido or SO.sub.n -alkyl; phenyl having fused thereto a 5- to 7-membered isocyclic or heterocyclic ring, said heterocyclic ring having 1 or 2 oxygen or sulphur heteroatoms; or pyridyl; andR.sup.4 is unsubstituted or substituted carboacyl or sulphonyl;Are useful for their diuretic, saluretic, antihypertensive and antithrombotic properties.

摘要翻译： 其中R为氢，烷基，芳基，芳烷基，三氟甲基或杂环的吡唑类化合物。 R 1为未取代或被卤素，三氟甲基，烷基，烷氧基或硝基取代的芳基或芳烷基; 或卤素取代的烷硫基部分; R2是低级烷基; 苯基; 或苄基; R 3为未取代的或被烷基，烯基，烷氧基，卤素，三氟甲基，三氟甲氧基，单 - 或二 - 烷基氨基，硝基，氰基，甲酰氨基，磺酰氨基或SO-烷基取代的芳基; 与5至7元环或杂环稠合的苯基，所述杂环具有1或2个氧或硫杂原子; 或吡啶基; 并且R 4是未取代的或取代的碳酰基或磺酰基; 有用于他们的DIYTIC，SALURETIC，ANTIHYPERTENSIVE和抗生素属性。