C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 333/38 (2006.01) A61K 31/381 (2006.01) A61K 31/4025 (2006.01) A61K 31/4178 (2006.01) A61K 31/4436 (2006.01) A61K 31/4535 (2006.01) C07D 409/04 (2006.01) C07D 409/12 (2006.01)
Patent
CA 2146707
The invention relates to heteroaroylguanidines of the Formula I (see formula I) in which the substituents HA and R(1) to R(5) have the meanings given in claim 1. These compounds exhibit very good antiarrhythmic properties, as are important for treating diseases which occur, for example, in association with symptoms of oxygen deficiency. As a consequence of their pharmacological properties, the compounds are outstandingly suitable for use as antiarrhythmic pharmaceuticals possessing a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris, in connection with which they also inhibit or strongly reduce, in a preventive manner, the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the elicitation of ischemically induced cardiac arrhythmias. On account of their protective effects against pathological hypoxic, and ischemic situations, the compounds of the formula I according to the invention can, as a consequence of inhibiting the cellular Na+/H+ exchange mechanism, be used as pharmaceuticals for treating all acute or chronic damage elicited by ischemia, or diseases induced primarily or secondarily thereby. This is the case with regard to their use as pharmaceuticals for surgical interventions, for example in organ transplantations, where the compounds can be used both for protecting the organs in the donor prior to and during removal, for protecting organs which have been removed, for example when they are being treated with or stored in physiological bathing fluids, and when transferring the organs into the recipient. The compounds are likewise valuable protective pharmaceuticals to be used when carrying out angioplastic surgical interventions, for example on the heart or on peripheral vessels. In conformity with their ability to protect against ischemically induced damage, the compounds are also suitable for use as pharmaceuticals for the treatment of ischemias of the nervous system, in particular of the CNS, in connection with which they are suitable, for example, for the treatment of stroke or cerebral edema. Over and above this, the compounds of the formula I according to the invention are also suitable for use in the treatment of forms of shock, such as, for example, allergic, cardiogenic, hypovolemic and bacterial shock.
Albus Udo
Kleemann Heinz-Werner
Lang Hans-Jochen
Scholz Wolfgang
Schwark Jan-Robert
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Hoechst Aktiengesellschaft
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