C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 279/22 (2006.01) A01N 1/02 (2006.01) A61B 10/00 (2006.01) A61K 31/16 (2006.01) C07D 241/26 (2006.01) G01N 33/48 (2006.01)
Patent
CA 2140989
Phenyl-substituted alkylcarboguanidides, carrying perfluoroalkyl groups, of the formula I (see formula I) are described where R(A) and R(B) are H, Hal, CN, OR(6), alkyl, O r-perfluoroalkyl or NR(7)R(8); R(6) is hydrogen, (cyclo)alk(en)yl, perfluoroalkyl, phenyl or benzyl; R(7) and R(8) are defined as R(6) ; X is 1 - 3; R(1) is H, alkyl or -O0-1 (CH2) 0-1perfluoroalkyl; R(2) , R(3) , R(4) and R(5) are defined as R(1) , with the condition, however, that R(1) , R(2) , R(3) , R(4) and R(5) are not simultaneously hydrogen and that R(1), R(2) , R(3) , R(4) and R(5) can only be alkyl when at least one of the substituents R(A) or R(B) contains a O r (CH2)a C b F2b+1 group; as are the pharmaceutically tolerated salts thereof. The compounds I are obtained by reacting a compound II (see formula II) where L is a leaving group which can readily be substituted nucleophilically, with guanidine. The compounds I are inhibitors of the cellular sodium/proton antiporter (Na+/H+ exchanger). They are suitable for use in preventive therapy for preventing the genesis of high blood pressure, for example essential hypertension.
Albus Udo
Kleemann Heinz-Werner
Lang Hans-Jochen
Scholz Wolfgang
Schwark Jan-Robert
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Hoechst Aktiengesellschaft
Hoeschst Aktiengesellschaft
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