Abstract: Methods of treating atrial arrhythmia include administering an effective amount of at least one antiarrhythmic pharmaceutical agent to a patient in need thereof, such that the at least one antiarrhythmic pharmaceutical agent first enters the heart through the pulmonary vein to the left atrium. Other methods of treating atrial arrhythmia include administering by inhalation an effective amount of at least one antiarrhythmic pharmaceutical agent to a patient in need thereof. An amount of the at least one antiarrhythmic pharmaceutical agent may peak in the coronary sinus of the heart at a time ranging from 10 seconds to 30 minutes from initiation of the administering. Unit doses, aerosols, and kits are also contemplated.

Abstract: Compounds of formula (I) especially where R1 is an optionally substituted alkyl, aralkyl or heterocyclyl-alkyl group, are shown to have activity as sodium channel blockers or as antifolates. Some novel compounds where R1 is an aralkyl or heterocyclyl-alkyl are disclosed.

Abstract: Pentafluorosulfanylbenzoylguanidines, of the formula I and II in which R1 to R4 have the meanings stated 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.

Abstract: The invention provides saponin mixtures and compounds which are isolated from the species Acacia victoriae and methods for their use. These compounds may contain a triterpene moiety, such as acacic or oleanolic acid, to which oligosaccharides and monoterpenoid moieties are attached. The mixtures and compounds have properties related to the regulation of apoptosis and cytotoxicity of cells and exhibit potent anti-tumor effects against a variety of tumor cells.

Abstract: A polypeptide is identified as being functionally included in a signal transduction pathway having a biological effect. Contemplated polypeptides are different from a retinoic acid receptor, a retinoid X receptor, or a cellular retinoic acid binding protein, however bind a retinoid or retinoid metabolite, and binding of the retinoid or retinoid metabolite lead to a modulation of the biological effect. In particularly contemplated methods, a retinoid or retinoid metabolite is administered to a cell or mammal in a concentration effective to modulate the biological effect.

Abstract: A transdermal or topical composition including anticholinergic agents, such as oxybutynin, a urea-containing compound and a carrier system. A method is disclosed for treating a subject for urinary incontinence while reducing the incidences of peak concentrations of drug and undesirable side effects.

Abstract: Disclosed are novel peptides including antiarrhythmic peptides that have improved stability. Further disclosed are compositions that include such peptides and methods of using the compositions particularly as medicaments.

Abstract: An implantable cardiac stimulation device, such as a pacemaker or Implantable Cardioverter Defibrillator, is configured to automatically monitor the effects of antiarrhythmic drugs on cardiac electrical signals within a patient to verify the efficacy of the drugs taken. In one example, an analysis of patient cardiac electrical signals is performed by comparing the cardiac electrical signals with values representative of the effects of different classes of antiarrhythmic drugs. If the implantable device determines that the prescribed antiarrhythmic drugs have not been effective, a warning signal is generated. The warning signal is conveyed directly to the patient via a bedside monitor and to the patient's physician via remote connection to an external programmer device so that both are notified of the drug efficacy problems.

Abstract: A method of treating myocardial damage secondary to myocardial infarction using moxonidine or a physiologically compatible salt thereof. Pharmaceutical preparations containing moxonidine and its physiologically compatible acid addition salts are suitable for use in acute myocardial infarction and/or postmyocardial infarction management. In addition to a beneficial influence, promoting recovery and/or rehabilitation, on the myocardial status following myocardial infarction, moxonidine and its physiologically compatible acid addition salts, especially when used in the management of postmyocardial infarction patients in the chronic stage, also show a preventive effect against the progression of heart failure after myocardial infarction.

Abstract: A composition employing a small amount of the hormone melatonin combined with a magnesium compound is formed into a lozenge or into a timed release tablet to act as an antiarrhythmic agent. As a lozenge to be dissolved in the mouth, it may incorporate magnesium in several forms such as a citrate, as a niacinate, as an aspartate, or as an orotate. The preferred formulations according to the invention alleviate cardiac arrhythmia, as well as the extreme manifestation of this condition known as atrial fibrillation. Magnesium citrate is not only beneficial to the heart muscle but also contributes to a laxative effect that counters the constipating action of the melatonin. As a time release tablet for daytime use, the same ingredients indicated above may be combined in tablet or capsular form, but are accompanied by the addition of agents which stimulate the mind such as tyrosine and phenylalanine. These stimulants serve to counter the sleep-inducing action of the melatonin.

Abstract: A novel oral dosage to be delivered to the stomach comprising a safe and effective amount of an active ingredient selected from the group consisting of emepronium bromidebromide, doxycycline, and other tetracyclines/antibiotics, iron preparations, quinidine, nonsteroidal anti-inflammatory drugs, alprenolol, ascorbic acid, captopril, theophylline, zidovoudine (AZT), bisphosphonates and mixtures thereof and pharmaceutically-acceptable excipients, wherein said oral dosage form is a generally oval form and film coated to facilitate rapid esophageal transit and avoid irritation in the mouth, buccal cavity, pharynx, and esophagus.

Abstract: The subject invention involves compounds having the structure: wherein each R1 is independently alkyl, aryl, or heterocycle; each R2-R7 is independently hydrogen or other substituent; B is nil and n is 0-3, or B is ethenyl and n is 0-1; and pharmaceutically acceptable forms thereof. The subject invention also involves pharmaceutical compositions containing such compounds, and methods for treating or preventing diseases or disorders using such compounds.

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: 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.

Abstract: The present invention relates to dried preparations containing a class III antiarrhythmic compound in the form of a crystalline or amorphous salt or any combination thereof, where the counterion is selected from pharmaceutically acceptable water-soluble organic or inorganic acids. The present invention also relates to frozen preparations containing a class III antiarrhythmic compound in the form of a salt solution, where the counterion is selected from pharmaceutically acceptable water-soluble organic or inorganic acids. Preferred preparations contain a salt of the compound 3,7-diazabicyclo[3.3.1]-nonane-3-carboxylic acid, 7-[(2S)-3-(4-cyanophenoxy)-2-hydroxypropyl]-1,1-dimethylethyl ester (Compound A). Further aspects of the present invention include salts of Compound A per se, processes for preparing the preparations, as well as use of the preparations for prophylaxis and/or treatment of cardiac arrhytmia.

Abstract: 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.

Abstract: The subject invention pertains to novel enantiomerically pure compounds, and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns a method of making and purifying the compounds. The isolated enantiomerically purified compounds, and compositions of these compounds, exhibit unexpectedly distinct and advantageous characteristics, such as a markedly superior ability to reduce or inhibit ventricular premature beats, as compared to racemic mixtures of the compounds.

Abstract: The invention relates to compounds of formula (I), wherein the symbols have the meanings indicated in the specification. The inventive compounds exhibit dramatic antiarrhythmic proprieties and contain a cardioprotective compound. They can preventively inhibit or strongly reduce pathophysiologic processes upon occurrence of ischemic injuries, especially ischemic cardiac arrhythmia. Said compounds also exhibit a strong inhibiting effect on cellular proliferation.

Abstract: The invention relates to compounds of formula (I), wherein the symbols have the meanings indicated in the specification. The inventive compounds exhibit dramatic antiarrhythmic proprieties and contain a cardioprotective compound. They can preventively inhibit or strongly reduce pathophysiologic processes upon occurrence of ischemic injuries, especially ischemic cardiac arrhythmia. Said compounds also exhibit a strong inhibiting effect on cellular proliferation.

Abstract: Methods, formulations and kits are described for resuscitating a patient suffering from cardiac arrest, for enhancing the efficacy of cardiopulmonary resuscitation, for treating post-resuscitation hypotension, and for reducing the incidence of ventricular arrhythmias and myocardial dysfunction in a patient following cardiopulmonary resuscitation. Prior methods and agents often cause inotropic or chronotropic effects, which can lead to undesirable post-resuscitation myocardial dysfunction. The invention comprises administering a therapeutically effective amount of an &agr;2-receptor agonist that does not cross the blood-brain barrier, such as &agr;-methylnorepinephrine, to enhance cardiopulmonary resuscitation.

Abstract: The subject invention pertains to novel enantiomerically pure compounds, and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns a method of making and purifying the compounds. The enantiomerically purified compounds, and compositions of these compounds, exhibit unexpectedly distinct and advantageous characteristics, such as a markedly superior ability to reduce or inhibit ventricular premature beats, as compared to racemic mixtures of the compounds.

Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.

Abstract: The present invention relates to novel, antiarrhythmically active phenoxyalkylamine derivatives possessing a double point of attack. More particularly, the present invention relates to new phenoxyalkylamine derivatives of the formula (1) wherein R1 and R2, independently from each other, mean hydrogen, halogen or C1-4 alkyl group; R3, R4 and R5, independently from each other, stand for hydrogen or C1-4 alkyl group; R6 represents hydrogen, C1-4 alkyl or benzyl group; R7 means nitro group or amino group optionally monosubstituted by C1-4 alkyl, benzoyl, C1-4 alkylcarbonyl, C1-4 alkylsulfonyl, C1-4 alkylcarbamoyl or C1-4 alkylthiocarbamoyl group; both n and m are 0 or 1, with the proviso that R2 is different from hydrogen, when R1 is hydrogen, as well as stereoisomers or mixtures of stereoisomers thereof, acid addition salts thereof and hydrates, prodrugs and metabolites of all these compounds.

Abstract: The present invention provides a bilayer structure for encapsulating multiple containment units. These containment units can attach or contain therapeutic or diagnostic agents that can be released through the bilayer structure. A suitable example of such a containment unit is a unilamellar or multilamellar vesicle.

Abstract: A method of treating or preventing supraventricular tachyarrhythmias is disclosed which comprises the use of a compound which selectively blocks the ultra-rapidly-activating delayed rectifier K+ current (IKur) of the human atrium.

Abstract: This application discloses a method of treating or preventing atrial arrhythmias which utilizes compounds which are blockers of the ultra-rapidly-activating delayed rectifier K+ current (IKur) of the human atrium in a use-dependent and/or rate dependent manner, and which provide the selective block preferentially at fast heart rates so that the effect is realized or maximized when required.

Abstract: Disclosed are compositions including an adenosine analog, wherein the composition comprises a dosage form suitable for oral (co)administration. Also disclosed are compositions including adenosine analogs, wherein the composition is in a dosage form including a pill, capsule, lozenge, or tablet, and compositions including adenosine analogs, wherein the composition is in a dosage form comprising a liquid. Additionally disclosed are methods of administering the inventive composition, and kits including the inventive compositions.

Abstract: The invention relates to the substantially pure dofetilide polymorphs P162, P162a and P143, and to processes for the preparation of, compositions containing and to the uses of, such polymorphs.

Abstract: Compounds of formula (I): ##STR1## where the substituents are as defined herein, and salts thereof, are matrix metalloprotease inhibitors.

Abstract: Chromans of formula I ##STR1## with the meanings of R(A), R(B) and R(1) to R(8) stated in the specification are suitable for producing a medicament for blocking the K.sup.+ channel that is opened by cyclic adenosine monophosphate (cAMP); also for producing medicaments for inhibiting gastric acid secretion; for the treatment of ulcers of the stomach and the intestinal region, in particular the duodenum, for the treatment of reflux esophagitis, for the treatment of diarrheal disorders, for the treatment and prevention of all types of arrhythmias, including atrial, ventricular and supraventricular arrhythmias, for controlling reentry arrhythmias and for preventing sudden heart death as a result of ventricular fibrillation.

Abstract: Compounds of the formula I ##STR1## and the pharmaceutically tolerated salts thereof, are described. A process for their preparation and their use as medicaments in cardiovascular diseases are also described.

Abstract: Compositions and methods for treatment and prevention of hypertrophy, hypertension, congestive heart failure, ischemic heart disease, ischemia-related conditions, such as ischemia reperfusion injury and cellular dysfunction, are described. The methods are directed to administering pharmaceutical compositions containing at least one compound selected from pyridoxal-5'-phosphate, pyridoxine, pyridoxal, and pyridoxamine.

Abstract: Phenyl-substituted alkenylcarboguanidides carrying perfluoroalkyl groups, a process for their preparation, their use as a medicament or diagnostic agent, and also a medicament containing them.Phenyl-substituted alkenylcarboguanidides carrying perfluoroalkyl groups, of the formula I ##STR1## in which the substituents have the meanings stated in the description, and their pharmaceutically suitable salts, are described. They are obtained by reacting a compound II ##STR2## with guanidine, in which R(1) to R(5) and R(A), R(B), R(C) and R(D) have the stated meaning, and L is a leaving group which easily undergoes nucleophilic substitution. Compounds I are excellent cardiovascular therapeutic agents.

Abstract: This invention provides novel indenone derivatives, their pharmaceutical formulations and their use for the inhibition of leukocyte adherence to cells.

Abstract: Compounds of the formula ##STR1## where T is ##STR2## and R(A), R(B), R(C), R(D), R(E), R(F), x and y have the meanings indicated in the claims, and their pharmaceutically acceptable salts are effective inhibitors of the cellular sodium-proton antiporter (Na.sup.+ /H.sup.+ exchanger). These compounds are therefore outstandingly suitable for treatment of all illnesses which are to be attributed to increased Na.sup.+ /H.sup.+ exchange.

Abstract: Benzoylguanidines of the formula I ##STR1## in which: R(1) to R(4) have the meanings given in the claims, are antiarrhythmic pharmaceuticals, having a cardioprotective component, which are also valuable for the prevention of ischemically induced damage, in particular in association with the triggering of ischemically induced cardiac arrhythmias. As a consequence of inhibiting the cellular Na.sup.+ /H.sup.+ exchange mechanism, they are used for treating acute or chronic damage triggered by ischemia. In addition to this, they are notable for their strong inhibitory effect on the proliferation of cells. They are suitable for preventing the genesis of high blood pressure.

Abstract: Adenosine and xanthine deriviatives, and compositions comprising those compounds, are potent selective agonists of adenosine receptors. The derivatives and compositions are used to treat conditions, including certain cardiac arrhythmias.

Abstract: This invention relates to substituted benzenesulfonylureas and -thioureas, processes for their preparation and use of pharmaceutical preparations based on these compounds, and medicaments containing them.Substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## exhibit effects on the cardiovascular system.

Abstract: Substantially single enantiomer (R or S) verapamil, or a pharmaceutically-acceptable salt thereof provides an improved treatment for patients having a condition susceptible to treatment with racemic verapamil and who are disposed to constipation.

Abstract: The invention is directed to a method useful in the treatment of preterm labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery.

Abstract: Substituted Indanylidineacetylguanidines, process for their preparation, their use as medicaments or diagnostic and medicaments containing them:Indanylidineacetylguanidines I ##STR1## and their pharmaceutically acceptable salts wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and X have the meanings given in the claims, are effective inhibitors of the cellular sodium/proton antiport (Na.sup.+ /H.sup.+ exchanger), which, in numerous diseases (essential hypertension, atherosclerosis, diabetes and the like) is also increased in those cells which are readily accessible for measurements, such as, for example, in erythrocytes, platelets or leukocytes. They are also advantageous for the preparation of a medicament for the treatment or prophylaxis of disorders of lipid metabolism.

Abstract: Compounds of the formula I ##STR1## are described in which at least one of the substituents R(1), R(2), R(3), R(4) and R(5) is a nitrogen-containing heterocyclic radical. They are outstanding cardiovascular therapeutic agents. They are obtained by reaction of a compound II ##STR2## with guanidine.

Abstract: A microcapsule contains a pharmaceutically effective amorphous water-soluble 2-piperazinone-1-acetic acid compound or salt thereof and a polymer binder and a method of preparing said microcapsule. The microcapsule is produced by dispersing in an aqueous phase a dispersion of the amorphous water-soluble 2-piperazinone-1-acetic acid compound or salt thereof in a solution of a polymer in an organic solvent to give an s/o/w type emulsion and subjecting the emulsion to in-water drying. The sustained-release microcapsule entraps 2-piperazinone-1-acetic acid compound or the salt thereof, as a drug, in high concentration, and in reducing the initial release of the drug, thereby reducing undesirable side effects of the drug.

Abstract: Carnitine, aminocarnitine and cysteic acid serve as carriers to bring pharmaceutically active compounds to desired sites in the body, e.g. skeletal muscle or the heart. The pharmaceutically active compound can be a protease inhibitor, a cardioactive drug for combating arrythmia, etc. The linkage is chemical through one or more alcohol, carboxyl or amine groups using reagents such as glutaraldehyde, dicarboxylic acid anhydrides and acid halides and carbodiimides. Carnitine derivatives are also incorporated into liposomes which are then used as carriers of active pharmaceutical agents.

Abstract: Compounds of formula (I) and pharmacologically acceptable salts thereof wherein: n is 1 to 3, R is an alkyl, R.sub.1 is hydrogen or alkyl, R.sub.2 is alkyl, R.sub.3 is an alkyl; b) alkyl substituted with an aryl, heteroaryl or cycloalkyl; c) alkyl substituted with one to eight fluorine atoms; d) cycloalkyl; e) alkenyl; f) alkyl substituted with one to three hydroxy, acyloxy or alkoxy substituents, and where the sum of carbons in R.sub.2 and R.sub.3 is greater than five br where R.sub.2 and R.sub.3 with the nitrogen atom form a saturated heterocyclic group having one nitrogen and form 4-8 carbon atoms or a 4-substituted piperazine group in which the 4-substituent can be alkyl, aryl, benzyl, or heteroaryl, and X is hydrogen, hydroxy, alkoxy, alkyl, carbon trifluoride or a halogen, or compounds of formula (I') and pharmacologically acceptable salts thereof wherein: n is 1 to 3, R is an alkyl, R.sub.1 is hydrogen or alkyl, R.sub.2 is an alkyl, R.sub.

Abstract: Substituted benzoylguanidines, process for their preparation, their use as a pharmaceutical or diagnostic, and pharmaceutical containing them.Described are benzoylguanidines of the formula I ##STR1## where R(1) to R(3) are H, Hal, (cyclo)alkyl, N.sub.3, CN or OH, alkyloxy, phenyl, phenoxy or benzoyl, and their pharmacologically acceptable salts, but with the exception of the compounds benzoylguanidine, 4-chlorobenzoylguanidine, 3,4-dichlorobenzoylguanidine and 3- or 4-methylbenzoylguanidine.They are obtained by reacting a compound II ##STR2## with guanidine, L being a leaving group.

Abstract: A method of altering the concentration of cholesterol constituents in human blood is provided. A daidzein material is administered to a human to increase the concentration of HDL-cholesterol and to decrease the level of LDL-cholesterol in the blood. The daidzein material may be administered in a pharmaceutical composition, or in a dietary supplement, including soy protein based dietary supplements. Utilization of daidzein to increase the concentration of HDL cholesterol and to decrease the concentration of LDL-cholesterol in the blood reduces the risk of atherosclerosis and vascular disease by providing more health beneficial HDL-cholesterol and reducing the level of atherosclerosis-inducing LDL-cholesterol.

Abstract: Ortho-substituted benzoic acid derivatives of the formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 have the given meanings, and Q is guanidyl, and also their physiologically harmless salts, exhibit antiarrhythmic properties and act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter. In addition, the compounds of the formula I, in which R.sup.1 to R.sup.3 and also Q have the given meanings, are suitable for use as valuable intermediates for the preparation of medicaments, in particular of inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.

Abstract: Medicated plasters composed of a flexible support and a pressure-sensitive adhesive layer laminated thereon, in which said pressure-sensitive adhesive layer has an exposed surface with pH of 7 or higher and contains one of the following three components:i) a basic physiologically active agent and an acidic substance,ii) a salt of a basic physiologically active agent and a basic substance, andiii) a basic physiologically active agent and a salt of a basic physiologically active agent.

Abstract: Methods of preventing tissue damage associated with decreased blood flow in a human by administering AICA riboside or a prodrug thereof in an amount which provides a blood plasma concentration of between 1 .mu.g/ml and 20 .mu.g/ml of AICA riboside for a time sufficient to reduce the risk of said tissue damage in said human. Methods of preventing an adverse clinical outcome, such as an adverse cardiovascular and/or cerebrovascular event, in a patient at risk for such outcome by administering AICA riboside or a prodrug thereof in an amount which provides a blood plasma concentration of between 1 .mu.g/ml and 20 .mu.g/ml of AICA riboside for a time sufficient to reduce the risk for said patient.

Abstract: Atrial arrhythmias, a major contributor to cardiovascular morbidity, are believed to be influenced by autonomic nervous system tone. The main purpose of this invention was to highlight new findings that have emerged in the study of effects of autonomic nervous system tone on atrial arrhythmias, and its interaction with class III antiarrhythmic drug effects. This invention evaluates the significance of sympathetic and parasympathetic activation by determining the effects of autonomic nervous system using a vagal and stellar ganglions stimulation, and by using autonomic nervous system neurotransmitters infusion (norepinephrine, acetylcholine).