Abstract: The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.

Abstract: Pharmaceutical compositions in topical or parenteral form containing organic nitrites are effective in treating male impotence and erectile dysfunction through topical or intracavernosal administration to the penis. Methods of treatment utilizing the nitrite-containing compositions are also disclosed, as are certain novel organic nitrite compounds.

Abstract: Nitric esters with pharmacological activity having general formula (I), their pharmaceutical utilisation and process for their preparation.

Abstract: Object of this invention are nitric esters of derivatives of the 2-(2,6-di-halophenylamino)phenylacetic acid, having the following general formula: ##STR1## wherein: A and B are selected from among hydrogen and linear or branched, substituted or non substituted alkyl chains, X is a halogen selected from among chlorine and bromine, Y is selected from among oxygen, NH and NR.sub.1, wherein R.sub.1 is a linear or branched alkyl group, and n is comprised between 1 and 10 as well as their pharmaceutical utilization and process for their preparation.

Abstract: The invention is directed to improved methods for modulating the human sexual response by administering a vasodilator to the circulation by a route of administration that avoids the "first-pass" effect.

Abstract: A method for control, management and inhibition of a preterm labor by providing to a pregnant woman a donor of nitric oxide. Management and inhibition of preterm labor is achieved by administering to a pregnant woman a nitric oxide or donor source in a safe and non-toxic concentration during the preterm labor.

Abstract: A method of treating a patient suffering from a condition requiring vasodilator therapy, comprising long term, continuous adminstration of an organic nitrite to the patient in a dosage form capable of delivering a sufficient therapeutic amount of nitrite to the bloodstream of the patient thereby providing effective vasodilator therapy for at least 24 hours without the development of tolerance in the patient. The method of the invention is useful in treating conditions such as angina, particularly chronic, stable angina pectoris, ischemic diseases and congestive heart failure, and for controlling hypertension and/or impotence in male patients.

Abstract: Allylaminoesters of the formula (I): ##STR1## in which: R.sub.1 is H or low-molecular-weight alkyl,R.sub.2 is low-molecular-weight alkyl, cycloalkyl, or low-molecular-weight phenylcycloalkyl, pyridyl or phenyl, low-molecular-weight phenylalkyl, low-molecular-weight diphenylalkyl, low-molecular-weight phenylalkenyl, in which the phenyl cycle may be mono-, di- or trisubstituted by chlorine atoms, low-molecular-weight alkyl radicals, low-molecular-weight alkoxy, or trifluoromethyl, acetamide or acetyloxy radicals, their racemic forms, their (S) enantiomers and their addition salts. Also, antiallergic drugs containing the same.

Abstract: New organic nitrate compounds, formed by condensing a nitrato alkanoic acid with a sulfur-containing amino acid or peptide, which prevent nitrate tolerance or overcome existing tolerance and which are useful for the treatment of cardiac diseases including circulatory diseases, high blood pressure, cardiac insufficiency and for dilating the peripheral vessels.

Abstract: New organic nitrate compounds, formed by condensing a nitrato alkanoic acid with a sulfur-containing amino acid or peptide followed by the reaction of the resulting product with an amino acid, N-acylamino acid, peptide or an N-acyl peptide to produce a thio ester thereof, which prevent nitrate tolerance or overcome existing tolerance and which are useful for the treatment of cardiac diseases including circulatory diseases, coronary dilation, high blood pressure, cardiac insufficiency and for dilating the peripheral vessels.

Abstract: The present invention provides a novel method of vasodilator therapy for treating a patient suffering from a condition, comprising long term, continuous administration of an organic nitrite to a patient suffering from the condition in a dosage form capable of delivering a sufficient therapeutic amount of nitrite to the blood stream of the patent thereby providing effective vasodilator therapy for at least 24 hours without development of tolerance in the patient. The method of the invention is useful in treating conditions such as, for example, angina, particularly chronic, stable angina pectoris, ischemic diseases, congestive heart failure, for controlling hypertension and/or impotence in male patients.Any conventional drug delivery system can be employed in carrying out the method of the invention. The drug delivery system can take virtually as many different forms as there are dosage forms available for delivery of nitrite to a patient.

Abstract: The invention relates to a nitroglycerin pump spray containing 0.2 to 3.5% by wt. of nitroglycerin and up to 3% by wt. of customary additives such as flavoring agent or antioxidants and a liquid phase consisting of aliphatic C.sub.2 to C.sub.4 alcohols and a vehicle and is characterized in that the liquid phase consists of 10 to 40% by wt. of ethyl alcohol and 90 to 60% by wt. of a neutral oil.

Abstract: The present invention provides pharmaceutical compositions effective against angina-like heart and circulatory diseases containing at least one nitroxyalkylamine derivative of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom, a lower-alkyl radical, a C.sub.3 -C.sub.8 -cycloalkyl or C.sub.3 -C.sub.8 -cycloalkenyl radical, an aminocarbonyl, C.sub.1 -C.sub.6 -mono- or di-alkylaminocarbonyl radical, R.sup.2 is a hydrogen atom, a lower-alkyl radical or a C.sub.3 -C.sub.8 -cycloalkyl or cycloalkenyl radical or R.sup.2, together with R.sup.1 and the nitrogen atom to which they are attached, form a heteroaliphatic ring containing up to 6 carbon atoms, A is a valency bond or a straight-chained or branched lower-alkylene radical, in which a --CH.sub.2 -- group can be replaced by a cycloalkylene radical, B is a lower-alkylene radical, in which a --CH.sub.2 -- group can be replaced by a cycloalkylene radical and X is an --NR.sup.3 --CO-- or --CO--NR.sup.3 -- radical, in which R.sup.

Abstract: Nitroglycerin injection that is free of the customary organic solvents and has an extended shelf life of at least 1 year, consisting essentially of water, lactose, and nitroglycerin. Sodium chloride or dextrose may be added during manufacture or upon diluting with an infusion. Commercially safe manufacture and stable dispersion are assured by mixing lactose adsorbate, containing nitroglycerin, with water at high shear so that no nitroglycerin droplets coalesce. Stability is maintained by filtering and filling operations using nonreactive, nonleaching, nonadsorptive materials.

Abstract: The present invention relates to a nitroglycerin spray prepared by filling a solution comprising nitroglycerin, ethanol and water and having a pH of about 2.4 to about 6.7 into a liquid-pressurized container.

Abstract: Novel external medications comprise, as essential components, the following three components (A) to (C):(A) an .alpha.-monoglyceryl ether represented by the following formula (I): ##STR1## wherein R means an alkyl or alkenyl group having 10 - 24 carbon atoms; (B) a physiologically active material; and(C) an oily material.The external medications have extremely high skin occlusive properties and significantly-improved absorptivity of phosiologically active materials. Therefore, a smaller amount of the medications compared with the conventional ones can give sufficient pharmacological effects and thus side effects can be reduced. The external medications may contain physiologically active materials such as drugs, growth hormones and the like, which are expected to show pharmacological effects upon their percutaneous absorption.

Abstract: Nitroglycerin injection that is free of the customary organic solvents and has an extended shelf life of at least 1 year, consisting essentially of water, lactose, and nitroglycerin. Sodium chloride or dextrose may be added during manufacture or upon diluting with an infusion. Commerically safe manufacture and stable dispersion are assured by mixing lactose adsorbate, containing nitroglycerin, with water at high shear so that no nitroglycerin droplets coalesce. Stability is maintained by filtering and filling operations using nonreactive, nonleaching, nonadsorptive materials.

Abstract: The present invention provides compounds of the general formula: ##STR1## wherein Ar is a substituted or unsubstituted aromatic or heteroaromatic radical, A is a straight-chained or branched alkylene chain containing up to 8 carbon atoms, a --CH.sub.2 -- group of which can be replaced by a cycloalkylene radical containing 3 to 7 carbon atoms, B is a straight-chained mono- or bicyclic, optionally branched, saturated or unsaturated alkylene chain containing up to 12 carbon atoms, a --CH.sub.2 -- group of which can be replaced by a cycloalkylene radical containing 3 to 7 carbon atoms and/or up to two --CH.sub.2 -- groups of which can be replaced by an oxygen or a sulphur atom or by an --S(.dbd.O) or --S(.dbd.O).sub.2 group, X is a valency bond, an oxygen atom or an --NR.sup.1 group, in which R.sup.1 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated alkyl or nitroxyalkyl radical containing up to 6 carbon atoms or R.sup.1, together with the nitrogen atom of the --NR.sup.

Abstract: A method, composition, and article for use in transdermal or percutaneous administration to humans of systemically active medicaments in the form of a solution in benzyl alcohol.

Abstract: The present invention provides new aminopropanol derivatives of the general formula: ##STR1## wherein A is a direct bond, a straight-chained or branched alkylene chain containing up to 3 carbon atoms or a --CO--CH.sub.2 -- group; X is a direct bond or a carbonyl group; B is a straight-chained or branched, saturated or unsaturated alkylene chain containing up to 12 carbon atoms, in which one or two --CH.sub.2 -- groups can also be replaced by a saturated or unsaturated alkylene ring containing 3 to 7 carbon atoms and/or by an oxygen or sulphur atom or an --S(.dbd.O)-- or --S(.dbd.O).sub.2 -- group, n is 1, 2 or 3; R.sub.1 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated alkyl radical containing up to 6 carbon atoms or a --B--(ONO.sub.2).sub.n group, in which B and n have the same meanings as above, or when A is a --CO--CH.sub.2 -- group and X is a direct bond, R.sub.

Abstract: A device for the controlled release and delivery of a pharmacologically active agent, comprising a vinyl gel layer and a pharmacologically active agent uniformly dispersed in the layer in a pharmacologically effective amount, the vinyl layer comprising a polyvinyl chloride resin, a primary plasticizer for the polyvinyl chloride resin, and an organic, nonvolatile gel forming additive in an amount sufficient to form a gel.

Abstract: Pharmaceutical preparations comprised of a pharmaceutically active ingredient and a carrier which comprises a percutaneous penetration enhancer comprised of 2-ethyl-1, 3-hexanediol alone or in combination with oleic acid is disclosed. The 2-ethyl-1, 3-hexanediol may be present in an amount in the range of about 50% to 100% based on the weight of the carrier. The oleic acid may be used in combination with 2-ethyl-1, 3-hexanediol in an amount of about 1 to 40% based on the weight of the carrier to provide a synergistic effect with respect to percutaneous penetration enhancement. The compound 2-ethyl-1, 3-hexanediol as used alone and/or in combination with the oleic acid has been found to significantly enhance the delivery of a drug, to a patient, from a transdermal delivery system.

Abstract: A device for the controlled release and delivery of a pharmacologically active agent, comprising a vinyl gel layer and a pharmacologically active agent uniformly dispersed in the layer in a pharmacologically effective amount, the vinyl layer comprising an emulsion polymerized polyvinyl chloride resin, a primary plasticizer for the polyvinyl chloride resin, and an organic, nonvolatile gel forming additive in an amount sufficient to form a gel.

Abstract: A pressure-sensitive adhesive tape for delivering nitroglycerin to skin, the tape comprising a backing with a layer of inert pressure-sensitive adhesive attached thereto, said pressure-sensitive adhesive layer comprising a pressure-sensitive adhesive polymer, skin penetration-enhancing ingredients and a relatively high concentration of nitroglycerin. The tape is useful for systemic treatment of angina pectoris, control of hypertension and treatment of congestive heart failure.

Abstract: Detonatable organic nitrates which are blended with excipients in drug mixtures for use as vasodialators such as nitroglycerine/lactose are rendered nondetonatable when burned in smoldering fires by the incorporation therewith of minor amounts of alkaline solid material such as magnesium carbonate and hydroxide.

Abstract: A high flux transdermal nitroglycerin therapeutic system is disclosed which is capable of delivering nitroglycerin through intact human skin at rates of 40 .mu.g/cm.sup.2 hr and preferably in the range of 50-150 .mu.g/cm.sup.2 hr. Ethanol delivered at a rate of from 250-500 .mu.g/cm.sup.2 hr is employed as a permeation enhancer for the nitroglycerin and a rate controlling membrane formed from ethylene vinyl acetate having a vinyl acetate content greater than 11% and preferably between 12-18% provides the appropriate rate control for both the drug and the permeation enhancer. This system is suitable for use in treatment of angina pectoris and congestive heart failure.

Abstract: A gel or gel preparation of improved stability and shelf life having an action on the coronary arteries comprising nitroesters, an oil base and finely disperse silica, wherein the finely disperse silica contains hydrophilic and hydrophobic, finely disperse silica is disclosed. A method for making the gel preparation is also disclosed.

Abstract: A trinitroglycerol-containing substantially disaccharide-free polymeric diffusion matrix is provided for the transdermal systemic delivery of trinitroglycerol through the skin of a patient. The polymeric diffusion matrix contains sufficient trinitroglycerol to be released over a prolonged period of time and comprises a first lower molecular weight, partially hydrolyzed polyvinylalcohol component, a second higher molecular weight, essentially fully hydrolyzed polyvinylalcohol component, and glycerol.