US 2002/0173500 A1 · Substituted heterocyclo-norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics, and medicaments comprising them

Abstract

Substituted heterocyclo-norbornylaminoderivatives having: a) an exo-configuration nitrogen and an endo-fused five-membered ring or six-membered ring of the formula (I) or b) an exo-configuration nitrogen and an exo-fused five-membered ring or six-membered ring of the formula (Ia), 1 wherein Rn, Het, A, B and T have the meanings given in the claims. These compounds have a variety of uses. They can be used as antihypertensives, for the reduction or prevention of is chemically induced damage, as pharmaceuticals for surgical interventions, for the treatment of ischemia of the nervous system, including stroke and cerebral edema, for the treatment of ischemia due to shock and disturbed respiratory drive, for the treatment of snoring, as a laxative, as an agent against ectoparasites, for the prevention of gallstone formation, as an antiatherosclerotic, as an agent against diabetic late complications, cancers, fibrotic disorders, endothelial dysfunction, organ hypertrophy, and organ hyperplasia. The compounds of the invention are inhibitors of the cellular sodium-proton antiporter. Additonally, the compounds of the invention influence the serum lipoproteins and can therefore be used for the prophylaxis and the regression of atherosclerotic changes.

Claims34

Dependent claims

A substituted heterocyclo-norbornylamino derivative having an exo-configuration nitrogen and endo-fused five-membered or six-membered ring of the formula I or having an exo-configuration nitrogen and exo-fused five-membered or six-membered ring of the formula Ia,

45
wherein:
A is (C1-C4)-alkylene;
T is (C1-C4)-alkyl or H;
B is a saturated or unsaturated carbon five-membered or six-membered ring, which is unsubstituted or is substituted by 1-3 substituents chosen from oxo, hydroxyl, (C1-C4)-alkoxy, and (C1-C4)-alkyl;
Het is a 5- or 6-membered, saturated or unsaturated, heterocycle that contains up to four identical or different heteroatoms chosen from O, S, N, and Se;
R is OH, F, Cl, Br, I, CN, NO2, phenyl, CO2R1, (C1-C4)-alkyl, (C1-C4)-alkoxy, amino, (C1-C4)-alkylamino, di(C1-C4)-alkylamino, or amino-(C1-C4)) -alkyl,
wherein the alkyl radicals are unsubstituted or are completely or partly substituted by fluorine;
R1 is H or (C1-C4)-alkyl, which is unsubstituted or completely or partly substituted by fluorine;
n is 0, 1, 2, 3 or 4,
wherein, if n=2, 3 or 4, the substituents R are chosen independently of one another;
or a pharmaceutically tolerable salt or trifluoracetate thereof.

9 more elements

Dependencies are inferred from the claim text.

Substituted heterocyclo-norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics, and medicaments comprising them

Life of this patent

Substituted heterocyclo-norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics, and medicaments comprising them

Life of this patent

Abstract

Claims34