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    • 5. 发明授权
    • 3,5-substituted aminobenzoylguanidines, their use as a medicament or
diagnostic and medicament containing them
    • 3,5-取代的氨基苯甲酰基胍,它们用作药物或诊断剂以及含有它们的药物
    • US5516805A
    • 1996-05-14
    • US450225
    • 1995-05-25
    • Hans-Jochen LangHeinrich EnglertAndreas WeichertHeinz-Werner KleemannWolfgang ScholzUdo Albus
    • Hans-Jochen LangHeinrich EnglertAndreas WeichertHeinz-Werner KleemannWolfgang ScholzUdo Albus
    • A61K31/165A61K31/155A61K49/00A61P1/04A61P9/00A61P9/10A61P35/00A61P43/00C07C279/22C07C311/16
    • C07C279/22
    • 3,5-Substituted aminobenzoylguanidines, process for their preparation, their use as a medicament or diagnostic and medicament containing themThere are described benzoylguanidines of the formula I ##STR1## where one of the substituents R(1), R(2), R(3) or R(4) is: an amino group ##STR2## where R(5), R(6)=inter alia, H or alkyl, or alternatively R(5) and R(6), together with the nitrogen atom, are a 5-7-membered ring, and the other substituents R(1), R(2), R(3) and R(4) in each case are: H, Hal, CN, CF.sub.3, NO.sub.2, CF.sub.3 --O--, C.sub.m F.sub.2m+1 --CH.sub.2 --O--, R(11)--C.sub.q H.sub.2q --X.sub.p --, X=O or NR(12), R(11)=H, (cyclo)alkyl, phenyl, and where R(1) and R(4) are not simultaneously hydrogen.The compounds I have very good antiarrhythmic and cardio-protective properties, but no undesired salidiuretic properties. They additionally exhibit protective properties against is chemically induced damage in vivo and in vitro in different organs and gastroprotective properties as a result of inhibition of gastric acid secretion. Moreover, they are distinguished by inhibitory action on the proliferation of cells.
    • 3,5-取代的氨基苯甲酰胍,其制备方法,它们作为药物或诊断剂的用途和含有它们的药物描述了式I(I)的苯甲酰胍,其中取代基R(1),R(2 ),R(3)或R(4)是:氨基,其中R(5),R(6)=特别是H或烷基,或者R(5)和R(6) 与氮原子一起为5-7元环,其他取代基R(1),R(2),R(3)和R(4)分别为:H,Hal,CN,CF 3, NO2,CF3-O-,CmF2m + 1-CH2-O-,R(11)-CqH2q-Xp-,X = O或NR(12),R(11)= H,(环)烷基,苯基和 其中R(1)和R(4)不同时为氢。 化合物I具有非常好的抗心律失常和心脏保护作用,但没有不希望的耐盐性。 它们另外表现出防止由于抑制胃酸分泌而导致的体内和体外在不同器官和胃保护性质中的化学诱导的损伤的保护性。 此外,它们通过对细胞增殖的抑制作用来区分。