摘要:
The present invention relates to heteroaryl-substituted carboxamides of the formula I, in which Het, A, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
摘要:
TRPC ion channels are non-selective channels widely expressed in human tissues. These channels are involved in numerous physiological functions and are putative targets for the development of novel medicines. There is a need to gain a better understanding of TRPC ion channels in cells and beyond. The present invention provides a pharmacological tool compound that allows to study TRPC ion channels due to its discriminating inhibition of TRPC subfamilies. In the present invention, norgestimate is shown to selectively inhibit TRPC3, TRPC6 and TRPC7.
摘要:
Pentafluorosulfany0lphenyl-substituted benzoylguanidines, process for their preparation, theie use as medicament or diagnostic aed, and medicament comprising them Pentafluorosulfany0lphenyl-substituted benzoylguanidines of the formulae I and II in which R1, R1′, R2, R2′, R3, R3′, R4 and X have the meanings indicated in the claims, are suitable as antiarrhythmic medicaments with a cardioprotective component for the prophylaxis of infarction and treatment of infarction and for the treatment of angina pectoris. They also inhibit preventively the pathophysiological processes associated with the development of ischemia-induced damage, especially in the triggering of ischemia-induced cardiac arrhythmias.
摘要:
The present invention relates to the novel isoindolone derivatives of the formula I in which R1 to R6 have the meanings stated in the claims. The inventive compounds are suitable as antiarrhythmic medicaments with a cardioprotective component for infarction prophylaxis and infarction treatment and for the treatment of angina pectoris. They also inhibit in a preventive manner the pathophysiological processes associated with the development of ischemia-induced damage, in particular in the triggering of ischemia-induced cardiac arrhythmias and of heart failure.
摘要:
Ortho, meta-substituted bisaryl compounds, processes for their preparation, their use as medicaments, and pharmaceutical preparations including their use as antiarrhythmic active compounds, for example, for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters. Compounds of the invention include compounds of the formula I
摘要:
Pentafluorosulfanylbenzoylguanidines of formula I wherein R1 to R4 have the meanings stated in the claims, are suitable, for example, as antiarrhythmic medicaments with a cardioprotective component for the prophylaxis of infarction and treatment of infarction and for the treatment of angina pectoris. They also inhibit preventively the pathophysiological processes associated with the development of ischemia-induced damage, especially in the triggering of ischemia-induced cardiac arrhythmias.
摘要:
This invention encompasses anthranilamides with heteroarylsulfonyl side chain, process for their preparation, their use as medicament or diagnostic aid, and pharmaceutical preparations containing them. Compounds of formula I, in which R1 to R7 have the meanings stated in the claims, act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. They are therefore suitable as novel antiarrhythmic ingredients, such as for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutter.
摘要:
Pentafluorosulfanylphenyl-substituted benzoylguanidines of the formulae I and II in which R1, R1′, R2, R2′, R3, R3′, R4 and X have the meanings indicated in the claims, are suitable as antiarrhythmic medicaments with a cardioprotective component for the prophylaxis of infarction and treatment of infarction and for the treatment of angina pectoris. They also inhibit preventively the pathophysiological processes associated with the development of ischemia-induced damage, especially in the triggering of ischemia-induced cardiac arrhythmias.
摘要:
The present invention relates to 3-guanidinocarbonyl-1-heteroaryl-indole derivatives, pharmaceutical compositions comprising such derivatives, methods of treatment comprising administering such derivatives, and processes for their preparation.
摘要:
Benzoylguanidines of the formula (I) in which R1 to R4 have the meanings given in the specification and claims are suitable as antiarrhythmic medicaments having a cardioprotective component for infarct prophylaxis and infarct treatment and for the treatment of angina pectoris. The compounds of the invention also preventively inhibit the pathophysiological processes in the formation of ischemically induced damage, in particular in the triggering of ischemically induced cardiac arrhythmias.