Abstract: A method of preventing, treating, terminating and protecting against cardiac arrhythmias, such as atrial, supraventricular and ventricular ectopy, tachycardia, flutter or fibrillation, including atrial, supraventricular and ventricular arrhythmias resulting from myocardial ischemic injury in a patient in need thereof, comprising administration of a selective I.sub.Ks antagonist and a beta-adrenergic receptor blocking agent, administered in combined therapy either simultaneously, separately or sequentially is presented. Additionally, a pharmaceutical preparation comprising a selective I.sub.Ks antagonist and a beta-adrenergic receptor blocking agent, wherein these compounds are administered simultaneously, separately or sequentially is presented.

Abstract: Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro)(mercapto)alk(oxy)yl, E is O or S; Y is --?CR(3).sub.2 !.sub.n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO.sub.2 or alk(yl)oxy, are described.The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.

Abstract: The present invention provides a preventive or therapeutic agent for tissue injury caused by active oxygens and free radicals, having for its effective component .gamma.-L-glutamyl-L-cysteine ester derivative indicated in the following general formula: ##STR1## wherein, R is a straight chain, branched or cyclical hydrocarbon group having 1-10 carbon atoms, or a straight chain or branched hydrocarbon group having 1-5 carbons substituted with an aromatic group, or its oxidized dimerThis compound has the effect of elevating glutathione levels in tissue and biochemically substitute for glutathione thereby performing preventive or therapeutic effects against ischemia-reperfusion tissue injury in the heart, liver and other organs, arrhythmia, as well as lung injury caused by active oxygens and free radicals.

Abstract: N.sup.6 -(epoxynorborn-2-yl)adenosines are Al adenosine receptor agonists that are useful for controlling atrial fibrillation, ventricular rate in atrial flutter, supraventricular tachyarrhythmia, inhibiting A--V- nodal transmission in supraventricular tachycardia, and for normalizing ventricular rhythm and hemodynamics.

Abstract: Alkyl-benzoylguanidines of the formula I ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 have the meanings given, and physiologically acceptable salts thereof show antiarrhythmic properties and act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.

Abstract: Disclosed are 14-aminosteroid compounds, including pharmaceutically acceptable acid salts and esters thereof, useful in treating individuals afflicted with congestive heart failure, which compounds have the general formula: ##STR1## wherein R.sub.3 is a deoxy or oxygen-substituted monosaccharide sugar residue and R.sub.1, R.sub.2 and R.sub.4 are various other substituents as defined herein.

Abstract: Benzoylguanidines of the formula I ##STR1## wherein R.sup.1 and R.sup.2 have the meanings indicated herein, and their physiologically acceptable salts, show anti-arrhythmic properties and act as inhibitors of the cellular NA.sup.+ /H.sup.+ antiporter.

Abstract: Substituted benzenesulfonylureas and -thioureas--processes for their preparation and their use as pharmaceuticalsBenzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro)(mercapto)alk(oxy)yl, E is O or S; Y is --?CR(3).sub.2 !.sub.n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO.sub.2 or alk(yl)oxy, are described.The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.

Abstract: 3,4,5-Substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic and medicament containing themBenzoylguanidines of the formula I ##STR1## where R(1) is R(4)--SO.sub.m or R(5)R(6)N--SO.sub.2 --, where R(4) and R(5) are alk(en)yl, --C.sub.n H.sub.2n --R(7), and where R(7) is cycloalkyl or phenyl, where R(5) is also H, R(6) is H or C.sub.1 --C.sub.4 --alkyl,R(2) is hydrogen, (cyclo)-alk(en)(yn)yl, aryl and hetaryl,R(3) is defined as R(2)and their pharmaceutically tolerable salts are described.

Abstract: A method for the concomitant treatment of ischemia and arrhythmia in mammalian species which includes administering a combination of a potassium channel opener having little or no effect on action potential duration in the heart and a class III antiarrhythmic compound.

Abstract: A method is described for obtaining an extract from the flowers of Salvia officinalis. The extraction process is performed preferably at a temperature of less than 50.degree. C. A preferred extraction agent is supercritical CO.sub.2. The extract thus obtained can be processed, if desired, with the addition of suitable thinners or fillers, in order to obtain a medicament. Medicaments containing the extract of Salvia officinalis flowers can be used to control high blood-pressure, circulatory problems and incomplete cicatrization of wounds.

Abstract: This invention relates to substituted benzenesulfonylureas and -thioureas, processes for their preparation, their use as a medicament or diagnostic, and medicament containing them.Substituted benzenesulfonylureas and -thioureas 1 ##STR1## exhibit effects on the cardiovascular system.

Abstract: An oligosaccharide containing about 20 monosaccharide units is provided. This oligosaccharide designated (M.sub.9 G).sub.2 is a copolymer .beta.-D-(1.fwdarw.4) connected mannuronopyranose units and an .alpha.-L-(1.fwdarw.4) connected guluronic acid unit at a ratio of 9:1. In addition, 40-60% of the carboxylic functional groups are esterified with propanol, 2-propanol or methanol, and substantially all of the C.sub.2 carbons and about 50% of the C.sub.3 positions of the residues are sulfated, such that the resulting compound contains about 7-13% organic sulfur. The compounds are used for the prevention and therapy of thrombosis-induced ischemic vascular diseases of the heart and the central nervous system, for treating acute thrombosis-induced brain infarction and in coronary ischemia-induced angina, and for treating hyperlipoproteinemia and lowering the relative amount of cholesterol.

Abstract: The present invention provides for the use of Tripterygium wilfordii Hook F extracts and purified components thereof in the treatment of inflammation or an immune disorder with concomitant lack of steroidal effect. Extracts of this plant (T2) bound to the glucocorticoid receptor and competitively inhibited glucocorticoid mediated cellular processes, such as dexamethasone binding to the glucocorticoid receptor, glucocorticoid mediated activation of target genes, dexamethasone dependent cellular growth, with concomitant inhibition of cyclooxygenase-2 induction and inflammatory processes such as the production of prostaglandin E.sub.2. The T2 extract components triptolide and tripdiolide were effective inhibitors. The particular advantage provided by the methods herein is the treatment or prevention of inflammation and the concomitant lack of steroidal agonist effects and NSAID side effects. Conditions treatable by the present methods include inflammation and immune disorders including autoimmune disease.

Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds of structure: ##STR1## wherein each R.sup.1 is independently one of alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl;each R.sup.2 and R.sup.3 is independently one of hydrogen, alkyl, aryl or arylalkyl;Y is a bond, or is one of --(CH.sub.2).sub.p --, cycloalkyl, aryl or C.sub.2-10 heterocycle; andm, n and p are each independently 1 to 10.

Abstract: A method of treatment or prophylaxis of angina in mammals, such as humans, which comprises the administration to the sufferer of an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, or a solvate of any of the foregoing: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, A and B are herein defined.

Abstract: Benzodiazepine analogs have been found to be useful in treating cardiac abnormalities.

Abstract: Benzo-(1,5)-diazepine derivatives with an amide or urea function in the 3-position are useful in the treatment of arrhythmia.

Abstract: The present invention relates to a method of using zatebradine by intravenous (IV) injection to retard or eliminate arrhythmias due to abnormal spontaneous activity in subendocardial Purkinje fibers. More specifically, the present invention relates to the use of zatebradine to reduce intracellular Na.sup.+ activity in Purkinje fibers and block I.sub.f current. Arrhythmias due to abnormal spontaneous activity in subendocardial Purkinje fibers occur 24 hours after occlusion of the left anterior descending (LAD) coronary artery in canine heart. These Purkinje fibers in the infarcted hearts are depolarized and have elevated intracellular Na.sup.+ activity. The major current underlying normal automaticity in these fibers is the I.sub.f current. Zatebradine reduces intracellular Na.sup.+ activity in Purkinje fibers by 4 mM. In vivo, 0.25-1.0 mg/kg intravenous injections of zatebradine slow ventricular rhythms by 24%. Although zatebradine also slows sinus nodal rate, it precipitates a more severe arrhythmia.

Abstract: Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro) (mercapto) alk (oxy) yl, E is O or S; Y is --[CR(3).sub.2 ]n-, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO.sub.2 or alk(yl)oxy, are described.The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.

Abstract: The present invention relates to the treatment and prevention of conditions wherein protein Kinase C inhibition is indicated.

Abstract: The invention relates to the use of an N-substituted heterocyclic derivative and its pharmaceutically acceptable salts for the treatment or prevention of cardiac arrhythmia.

Abstract: The use of 3-benzoyl-3,7-diazabicyclo[3.3.1]nonane compounds of the general formula I ##STR1## in which R.sup.1 is an alkyl group having 1-6 carbon atoms or a cycloalkylalkyl group having 4-7 carbon atoms,R.sup.2 and R.sup.3 are each individually lower alkyl or together form an alkylene chain having 3-6 carbon atoms,R.sup.4 is hydrogen, halogen, cyano, nitro, trifluoromethyl or a R.sup.6 --SO.sub.2 -- group, in which R.sup.6 is fluorine or lower alkyl, andR.sup.5 is hydrogen, halogen, trifluoromethyl or nitro, or their physiologically acceptable acid addition salts for the treatment of cardiac arrhythmias in larger mammals, including humans.

Abstract: The use of lidocaine or other Class I cardiac antiarrhythmic compound in the management of preterm labor and the stoppage of labor preparatory to cesarian delivery, is disclosed. The electrophysiological effects of lidocaine on the sodium, calcium and potassium channels of freshly dissociated myocytes from late-pregnant rat uteri with the tight-seal patch-clamp method are presented. Dose-response relations on the sodium and calcium currents, and effects on the availability relation for sodium current are also presented. Also disclosed are the effects of chronic administration of lidocaine on the duration of pregnancy.

Abstract: For short-term therapy of transient functional cardiovascular symptoms, borderline active dosage forms of beta blockers are used which produce in the body only the borderline active concentrations of active ingredient which produce no significant changes in the physiological values in the cardiovascular system under resting conditions for the respective specific beta blocker used and significantly reduce adrenergically induced transient stimulation effects. Oral, transdermal, or topical dosage forms are particularly advantageous. A differentiated therapy of functional symptoms which does not exist with the customary dosage forms of beta blockers designed for long-term therapies is possible. Both the quality of life and the risk-benefit ratio of the beta blockers are improved. The duration of the therapy also does not have to be extended beyond the symptomatically required scale since no rebound danger exists after withdrawal.

Abstract: A method of treatment or prophylaxis of angina in mammals, such as humans, which comprises the administration to the sufferer of an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, or a solvate of any of the foregoing: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, A and B are herein defined.

Abstract: The invention describes a method for normalizing a cardiac inotropic irregularity, via administering an effective amount of 12(R)HETE. Also described are therapeutic compositions which combine a cardiac glycoside and 12(R)HETE.

Abstract: A process for producing microcapsules with an adhesive coating layer which comprises forming a slurry of microcapsules in a medium selected from water, one or more organic solvents or a mixture thereof by a coacervation method, adding powders of a pharmaceutically acceptable inorganic compound which is insoluble in the medium to the slurry, so that the inorganic compound adheres to substantially the overall surface of the adhesive coating layer, and separating the microcapsules from the medium.

Abstract: Compounds of the formula: ##STR1## are useful for treating conditions modulated by .alpha..sub.1 -adrenergic receptors.

Abstract: Compounds of the formula: ##STR1## are useful for treating conditions modulated by .alpha..sub.1 -adrenergic receptors.

Abstract: Imidazobenzo-(1,5)-diazepine derivatives with an amide or urea function in the 3-position are useful in the treatment of arrhythmia.

Abstract: Benzodiazepine derivatives with an amide or urea function in the 3-position are useful in the treatment of arrhythmia.

Abstract: Benzodiazepine analogs have been found to be useful in treating cardiac abnormalities.

Abstract: Methods of treatment of the human or animal body are provided to combat conditions responsive to lithium and/or C.sub.18-22 polyunsaturated fatty acid therapy, including conditions associated with essential lithium deficiency, and also transfer of lipid-enveloped viruses between humans or animals or between cells within a human or animal body. The methods include administration of an effective amount of a lithium salt of a C.sub.18-22 polyunsaturated fatty acid. Devices for combatting transmission of viral diseases including lithium salts of a C.sub.18-22 polyunsaturated fatty acid are also provided.

Abstract: This invention relates to the treatment of tachyarrhythmias of supraventricular origin. This condition may safely be treated by nasal administration of a composition comprising propranolol dissolved in a pharmaceutically acceptable, aqueous-based carrier. A total dose of up to 20 mg of propranolol may be administered at one time.

Abstract: A system for controlled release, site-specific delivery of therapeutic agents, particularly myocardial agents such as antiarrhythmic agents, comprises a biocompatible polymeric matrix with an incorporated therapeutic agent for direct placement at the epicardium. Advantageously, the dosage form can be fabricated in such a manner as to tailor the release characteristics as required by the nature of the physical condition desired to be treated. In a specific illustrative embodiment, lidocaine, an antiarrhythmic depressant, is incorporated in polyurethane by a unique method which permits drug-loading of the polymeric matrix from about 5% up to 40% by weight, with about 25% to 30% in a preferred embodiment. A novel FeCl.sub.3 catalyst causes the polyurethane to polymerize despite the presence of drug in the polymeric matrix mixture.

Abstract: Benzoylguanidines of the formula I ##STR1## are described where R(1) is R(4)--SO.sub.m or R(5)R(6)N--SO.sub.z --, where R(4) and R(5) are alk(en)yl or --C.sub.n H.sub.2n --R(7), and where R(7) is a cycloalkyl or phenyl, where R(5) also has the meaning of H, and R(6) is H or C.sub.1 -C.sub.4 -alkyl, R(2) is hydrogen, halogen, alkyl, O--(CH.sub.2).sub.m C.sub.p F.sub.2p+1, --X--R(10), where X is O, S or NR(11), R(10) is H, (cyclo)alkyl(methyl) or --C.sub.n H.sub.2n --R(12) where R(12) is phenyl, and R(3) is defined, inter alia, as R(1), and their pharmaceutically tolerable salts.The compounds I are obtained by reaction of compounds of the formula II ##STR2## with guanidine, in which L is a leaving group which can be easily nucleophilically substituted.

Abstract: Optically pure (S) metoprolol, which is substantially free of the (R) enantiomer, is a potent beta-blocker for treating myocardial infarction and for relieving the symptoms of angina pectoris, cardiac arrhythmia and hypertension in individuals. A method is disclosed utilizing the optically pure (S) configurational enantiomer of metoprolol for treating cardiovascular disorders while reducing undesirable side effects associated with the administration of beta-blockers.

Abstract: A diltiazem pellet formulation for oral administration comprises a core of diltiazem or a pharmaceutically acceptable salt thereof in association with an organic acid, and a multi-layer membrane surrounding the core and containing a major proportion of a pharmaceutically acceptable film-forming, water insoluble synthetic polymer and a minor proportion of a pharmaceutically acceptable film-forming, water soluble synthetic polymer. The number of layers in the membrane and the ratio of the water soluble to water insoluble polymer being effective to permit release of diltiazem from the pellet at a rate allowing controlled absorption thereof over a twelve hour period following oral administration. The pellet has a dissolution rate in vitro which when measured in a dissolution apparatus (Paddle) according to U.S. Pharmacopoeia XXI in 0.05 M KC1 at pH 7.0 results in not more than 35% of the total diltiazem being released after 2 hours of measurement.

Abstract: New aryloxy-alkylamine derivatives of the general formula I ##STR1## in which A signifies a benzene or thiophene ring, R and R.sub.1, independently of one another, each hydrogen, alkyl, halogen, CF.sub.3 or alkoxy, R.sub.2 alkyl, cycloalkyl, alkenyl, alkynyl, alkaryl or saturated or unsaturated aliphatic or aromatic acyl, R.sub.3 and R.sub.4 in each case hydrogen, alkyl, alkenyl, alkynyl or cycloalkyl with, in each case, up to 8 C-atoms, whereby R.sub.3 and R.sub.4 can be the same or different but are not simultaneously hydrogen or R.sub.3 and R.sub.4, together with the nitrogen atom connecting them, form a 5- to 7-membered saturated ring or a saturated heterocyclic ring which can possibly contain an oxygen or nitrogen atom as a further heteroatom in the ring, whereby an additional nitrogen atom can be substituted by an alkyl radical with up to 3 C-atoms, and their acid-addition salts possess interesting pharmaceutical properties and are especially suitable as anti-arrhythmics.

Abstract: An antihypertensive, antianginal, antiarrhythmic and antiglaucomic pharamaceutical preparation consists of an active principle, namely 3-methyl-5-[2-(3-tert.butylamino-2-hydroxypropoxy-phenoxymethyl]-1,2,4-oxa diazole hydrochloride of the following formula: ##STR1## and a pharmaceutically acceptable diluent.

Abstract: The invention relates to inclusion complexes of 3-morpholino-sydnonimine or its salts or its tautomer isomer, process for the preparation thereof and pharmaceutical compositions containing the same.The inclusion complex of 3-morpholino-sydnonimine or its salt formed with cyclodextrin derivative is prepared bya) reacting the 3-morpholino-sydnonimine or its salt in an aqueous medium with a cyclodextrin derivative and the complex is isolated from the solution by dehydratation, orb) high energy milling of 3-morpholino-sydnonimine or its salt and a cyclodextrin derivative.

Abstract: The present invention is directed to a new class of piperidinyl medicinal agents which are useful as antithrombotic agents and as serotonin 5HT.sub.2 antagonists.

Abstract: Novel diarylamidines, and compositions and methods for treating cardiac arrhythmias in mammals utilizing the novel and related known diarylamidines of formula I, II, III and IV ##STR1##

Abstract: Substituted imidazolyl-alkyl-piperazine and diazepine derivatives and the pharmaceutically acceptable salts thereof are useful for treating mammals having any of a variety of disease states. These disease states include: 1) diseases treated by direct neuronal protection, including focal and global ischemia, spinal injuries, and head trauma, and neurological diseases including Alzheimer's and Huntington's chorea; 2) uraemic and hyponatraemic encephalopathy; 3) diseases treated by diuresis; 4) diseases treated by calcium channel antagonism, including cardiovascular diseases (i.e. hypertension, angina, stable and unstable angina, Prinzmetal angina, arrhythmia, thrombosis, embolism, and congestive heart failure including chronic or acute cardiac failure), diseases characterized by ischemia of lower legs due to peripheral vascular disease (e.g., intermittent claudication), diseases characterized by spasms of smooth muscle (i.e.

Abstract: A method of arrhythmia with an effective amount of dicentrine or other alkaloids extracted from Lindera oldhammii (megaphylla) Hemsl.

Abstract: A controlled release formulation of a calcium channel blocker for oral administration contains non-pareil seeds loaded with a calcium channel blocker, particularly diltiazem, nifedipine, or verapamil, and then microencapsulated in ethylcellulose by phase separation techniques. The resultant microcapsules provide an approximately zero order release rate, preferably over 12 to 16 hours. These microcapsules may be filled into gelatin capsules.

Abstract: A diltiazem pellet formulation for oral administration comprises a core of diltiazem or a pharmaceutically acceptable salt thereof in association with an organic acid, and a multi-layer membrane surrounding the core and containing a major proportion of a pharmaceutically acceptable film-forming, water insoluble synthetic polymer and a minor proportion of a pharmaceutically acceptable film-forming, water soluble synthetic polymer. The number of layers in the membrane and the ratio of the water soluble to water insoluble polymer being effective to permit release of diltiazem from the pellet at a rate allowing controlled absorption thereof over a twelve hour period following oral administration. The pellet has a dissolution rate in vitro which when measured in a dissolution apparatus (Paddle) according to U.S. Pharmacopoeia XXI in 0.05 M KCl at pH 7.0 results in not more than 35% of the total diltiazem being released after 2 hours of measurement.

Abstract: This invention relates to aminoethylthiophene derivatives and more particularly 2-and 3-aminoethylthiophene derivatives which are useful as antiarrhythmic agents, their methods of use as antiarrhythmic agents, and novel intermediate compounds useful for preparation of the aminoethylthiophene derivatives of the invention.

Abstract: New soft .beta.-adrenergic blocking agents, useful in the treatment or prevention of cardiovascular disorders and in the treatment of glaucoma, have the formula ##STR1## wherein n is an integer from 0 to 10; R is C.sub.6 -C.sub.12 cycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkenyl-C.sub.p H.sub.2p -- or C.sub.6 -C.sub.12 cycloalkenyl-C.sub.p H.sub.2p -- (wherein p is 0, 1, 2 or 3), or together with the adjacent ##STR2## group represents a variety of other complex ester groupings; R.sub.1 is C.sub.1 -C.sub.7 alkyl; and Ar is a divalent radical containing at least one aromatic nucleus. The corresponding pharmaceutically acceptable acid addition salts are also described.