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    • 3. 发明授权
    • 4-Substituted pyrazoles
    • 4-取代的吡唑
    • US4112109A
    • 1978-09-05
    • US766187
    • 1977-02-07
    • Eike MollerKarl Meng, deceasedEgbert WehingerHarald HorstmannFriedel Seuter
    • Eike MollerKarl Meng, deceasedEgbert WehingerHarald HorstmannFriedel Seuter
    • C07D231/20C07D231/28A61K31/415
    • C07D231/20C07D231/28Y10S514/822Y10S514/869
    • 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.
    • 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。
    • 7. 发明授权
    • 1-Substituted pyrazoles
    • 1-取代的吡唑
    • US4113957A
    • 1978-09-12
    • US693971
    • 1976-06-08
    • Eike MollerKarl-August Meng, deceasedEgbert WehingerHarald HorstmannFriedel Seuter
    • Eike MollerKarl-August Meng, deceasedEgbert WehingerHarald HorstmannFriedel Seuter
    • C07D231/20
    • C07D231/20Y10S514/822Y10S514/869
    • Pyrazoles of the formula ##STR1## wherein R is hydrogen, alkyl, trifluoromethyl, aryl, aralkyl or a heterocycle;R.sup.1 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; of (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 substituents 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.