Heterocyclyl-condensed benzoylguanidines, their production and use as inhibitors of the cellular Na+/H+-antiporter

US6028069A · kind A · utility

Assignee

• MERCK PATENT GESELLSCHAFT MIT BESHRANK TER HAFTUNG · DE

Inventors

• Manfred Baumgarth
• Rolf Gericke · Seeheim-Jugenheim, DE
• Klaus-Otto Minck · Ober-Ramstadt, DE
• Norbert Beier · Reinheim, DE

Key dates

• Filing date: Mar 30, 1999
• Grant date: Feb 22, 2000
• Expiry date: Mar 30, 2019

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D333/68
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Cyclic sulphones of formula (I) are disclosed, in which: R.sup.1 and R.sup.2 each independently of one another stand for H, A, CF.sub.3, CH.sub.2 F, CHF.sub.2, C.sub.2 F.sub.5, Hal, OH, OA, NH.sub.2, NHA, NA.sub.2, NO.sub.2 or CN; X stands for CR.sup.4 R.sup.5, C.dbd.Z, O, S, NH, NA or NR.sup.3 ; Y stands for CR.sup.6 R.sup.7, C.dbd.Z, O, NH, NA, or NR.sup.3 ; Z stands for O, S, NH, NA, NOH, NOA, CH.sub.2, CHA or CA.sub.2 ; R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently of one another stand for H, A, R.sup.3, Hal, OH, OA, SH, SA, NH.sub.2, NHA or NA.sub.2, or alternatively, R.sup.5 and R.sup.6 or R.sup.7 and R.sup.8 can together represent a bond, only one such bond being present in each molecule; R.sup.4 and R.sup.5 together can also stand for O--(CH.sub.2).sub.2 --O or O--(CH.sub.2).sub.3 --O; R.sup.8 and R.sup.9 each independently of one another stand for H or A; A stands for alkyl with 1-6 C atoms; Hal stands for F, Cl, Br or I; and R.sup.3 stands for phenyl or benzyl which is unsubstituted or single-, double- or triple-substituted by A, OA, NH.sub.2, NHA, NA.sub.2, F, Cl, Br and/or CF.sub.3 ; and n is 0 or 1. Also disclosed are the physiologically tolerable salts of t…