US 2001/0020042 A1 · Fluorophenyl-substituted alkenylcarboxylic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament containing them

Abstract

This invention relates to fluorophenyl-substituted alkenylcarboxylic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament containing them. An embodiment of the invention embraces compounds of the formula I: 1 and the pharmaceutically tolerated salts thereof. The disclosed compounds are valuable inhibitors of the cellular sodium/proton exchanger (Na+/H+ exchanger). They are therefore outstandingly suitable for the treatment of all diseases attributable to increased Na+/H+ exchange.

Claims19

Dependent claims

A compound of the formula I:

10
in which:
R(6) is hydrogen, (C1-C8)-alkyl, (C3-C8)-cycloalkyl or phenyl, the phenyl group being unsubstituted or substituted by 1 - 3 substituents selected from the group consisting of F, Cl, CF3, methyl, methoxy and NR(9)-R(10);
R(9) and R(10) are hydrogen, (C1-C4)-alkyl or (C1-C4) -perfluoroalkyl;
R(7) is independently defined in the same way as R(6);
and
R(1), R(2), R(3), R(4) and R(5) independently of one another are hydrogen or F, wherein at least one of the radicals R(1), R(2), R(3), R(4) and R(5) is fluorine;
or a pharmaceutically tolerated salt thereof.

5 more elements

Dependencies are inferred from the claim text.

Facts

Application

09/778,899Filed 8 Feb 2001

Priority

DE 195 18 796.222 May 1995

Published

6 Sep 2001

Term ends

Not estimatedThe source records don’t support an estimate.

Classification15 codes

C07C 279/22
Containing any of the groups [IMAGE cpc-sch-C07C-0971.gif], X being a hetero atom, Y being any atom, e.g. acylguanidines: y being a hydrogen or a…
A61P 1/16
Drugs for disorders of the alimentary tract or the digestive system: for liver or gallbladder disorders, e.g. hepatoprotective agents,…
A61P 3/08
Drugs for disorders of the metabolism: for glucose homeostasis
A61P 9/00
Drugs for disorders of the cardiovascular system

Family

Application08/651,196Continuation · filed 20 May 1996

Application08/947,517Continuation · filed 29 Sep 1997

Application09/244,177Continuation · filed 4 Feb 1999

Application09/413,478Continuation · filed 6 Oct 1999

Application09/778,899Continuation · filed 8 Feb 2001

US 2001/0020042 A1This patent

From the US filing history. Foreign family members aren’t listed.

Fluorophenyl-substituted alkenylcarboxylic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament containing them

Life of this patent

Fluorophenyl-substituted alkenylcarboxylic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament containing them

Life of this patent

Abstract

Claims19