摘要:
Substituted benzenesulfonylureas and -thioureas of the formula I in which R1, R2, E, X, Y and Z have the meanings described herein, show effects on the autonomous nervous system. The invention relates to the use of the compounds of the formula I in the treatment and prophylaxis of dysfunctions of the autonomous nervous system, in particular of vagal dysfunctions, for example in the case of cardiovascular diseases. The invention also relates to the use of compounds of the formula I in combination with beta-receptor blockers and to products and pharmaceutical preparations which comprise at least one compound of the formula I and at least one beta-receptor blocker, and to novel compounds.
摘要:
The present invention relates to cinnamoylaminoalkyl-substituted benzenesulfonamide derivatives of formula I in which A(1), A(2), A(3), R(1), R(2), R(3), R(4), X, Y, and Z have the meanings indicated in the claims. Compounds of formula I are valuable pharmaceutical active compounds which exhibit, for example, an inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency or cardiomyopathies, or for the prevention of sudden cardiac death, or for improving decreased contractility of the heart. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, and pharmaceutical preparations comprising them.
摘要:
Novel 2,5-substituted benzolsulfonyl ureas and thioureas of formula (I) as illustrated in the disclosure. The compounds are useful active ingredients for medicaments. The compounds of formula (I) act as inhibitors on ATP-sensitive potassium canals and are suitable for the treatment of cardiovascular disorders, especially the treatment of arrhythmias, prevention of sudden death from heart disease or affect diminished contractility of the heart. The invention also relates to methods for producing compounds of formula (I), the use thereof and pharmaceutical preparations containing said compounds.
摘要:
The present invention relates to piperidinesulfonylureas and piperidinesulfonylthioureas of formula I, in which A, X, R(1), R(2) and R(3) have the meanings indicated in the claims. The compounds of formula I are valuable active pharmaceutical ingredients which show in particular an inhibiting effect on ATP-sensitive potassium channels of the cardiac muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency, cardiomyopathies or reduced contractility of the heart or for the prevention of sudden cardiac death. The invention further relates to processes for preparing the compounds of formula I, their use and pharmaceutical compositions comprising them.
摘要:
One embodiment of the present invention relates to acylaminoalkyl-substituted benzenesulfonamide derivatives of the formula (I), in which A, R(1), R(2), X, Y, and Z have the meanings indicated in the specification, and to pharmaceutically tolerable salts thereof. The compounds of the invention are valuable pharmaceutically active compounds that have, for example, an inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the vagal cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency, cardiomyopathies, decreased contractility of the heart or vagal dysfunction of the heart, or for the prevention of sudden cardiac death. The invention furthermore relates to processes for the preparation of the compounds of the formula (I) and pharmaceutically tolerable salts thereof, their use, and pharmaceutical preparations comprising them.
摘要:
One embodiment of the present invention relates to heteroarylacryloylaminoalkyl-substituted benzenesulfonamide derivatives of the formula (I), in which R(1), R(2), R(3), R(4), Het, X, Y and Z have the meanings indicated in the specification, and to pharmaceutically tolerable salts thereof. The compounds of the invention are valuable pharmaceutically active compounds that have, for example, an at inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the vagal cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency, cardiomyopathies, decreased contractility of the heart, or vagal dysfunction of the heart, or for the prevention of sudden cardiac death. The invention furthermore relates to processes for the preparation of the compounds of the formula (I) and pharmaceutically tolerable salts thereof, their use, and pharmaceutical preparations comprising them.
摘要:
The present invention provides a process for identifying substances that modulate the activity of hyperpolarization-activated cation channels, and the use of this process.
摘要:
The present invention provides a process for identifying substances that modulate the activity of hyperpolarization-activated cation channels, and the use of this process.
摘要:
Sulfur-containing heterocyclic bradykinin antagonists, process for their preparation, and their use Compounds of the formula (I) ##STR1## in which one of the radicals X.sub.1, X.sub.2 or X.sub.3 is C--O--R.sup.2 and the other X.sub.1, X.sub.2, and X.sub.3, in each case, and X.sub.4, are then, identically or differently, N or CR.sup.1 ; R.sup.1 and R.sup.3 are, identically or differently, H, halogen, (C.sub.1 -C.sub.6)-alkyl, O--R.sup.6, S--R.sup.6, NHR.sup.6, (C.sub.6 -C.sub.12)-aryl, (C.sub.6 -C.sub.12)-aryl-(C.sub.1 -C.sub.3)-alkyl, C(O)--OR.sup.6, C(O)--H, (C.sub.2 -C.sub.5)-alkenyl, NO.sub.2, SO.sub.3 R.sup.7, CN or C(O)--NHR.sup.8, where alkyl, aryl and alkenyl can optionally be substituted.
摘要:
The invention relates to the use of non-peptide bradykinin antagonists for the production of pharmaceuticals for the prevention and treatment of Alzheimer's disease. Suitable Compounds are non-peptide bradykinin antagonists which inhibit the actions of the Alzheimer's protein amyloid (.beta./A4) in isolated endothelial cells, such as for example, fused heterobicyclic fluoroalkyl derivatives.