Phenyl-substituted alkylcarboguanidides carrying perfluoroalkyl groups, a process for their preparation, their use as a medicament or a diagnostic agent, and a medicament containing them

US5567734A · kind A · utility

Assignee

• Hoechst GmbH · DE

Inventors

• Jan-Robert Schwark · Frankfurt am Main, DE
• Heinz-Werner Kleemann · Bischofsheim, DE
• Hans-Jochen Lang · Hofheim, DE
• Andreas Weichert · Egelsbach, DE
• Wolfgang Scholz · Beverly, US
• Udo Albus · Florstadt, DE

Key dates

• Filing date: Jan 23, 1995
• Grant date: Oct 22, 1996
• Expiry date: Jan 23, 2015

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C279/22
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Phenyl-substituted alkylcarboguanidides carrying perfluoroalkyl groups, of the formula I ##STR1## are described where R(A) and R(B) are H, Hal, CN, OR(6), alkyl, O.sub.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 --O.sub.0-1 (CH.sub.2)O.sub.0-1 perfluoroalkyl; 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.sub.r (CH.sub.2).sub.a C.sub.b F.sub.2b+1 group; as are the pharmaceutically acceptable salts thereof. Methods of preparation of compounds of formula I are also described.