Abstract: The present invention relates to a new process of synthesis and to some new intermediates for the preparation of steroids with progestogen activity, more particularly, for the preparation of Desogestrel of formula (I). Said process is characterized by the regioselective reduction of the compound of formula (II) to give the intermediate of formula (III).

Abstract: Process for the preparation of compounds active in the treatment of Parkinson's disease, and such compounds, having general formula (VI) wherein R4 may be, independently, a linear, branched or cyclic, saturated or unsaturated C1-8 alkyl radical, such as, for example, the radicals methyl, ethyl, propyl, butyl, isobutyl, tert-butyl, pentyl, cyclopentyl, hexyl, cyclohexyl and octyl. The process utilizes as starting materials the compound of formula (I) wherein R1 represents a linear, branched or cyclic, saturated or unsaturated C1-8 alkyl residue.

Abstract: The present invention provides new process of preparing neuromuscular blocking agents. The process include preparing neuromuscular blocking agents using the compounds of formula I: ##STR1## wherein R.sub.1 is=O and X is halo; and formula II: ##STR2## wherein R, and X are as defined above.

Abstract: The present invention provides a method of preparing thieno[3,2-c]pyridine derivatives of formula I: ##STR1## wherein R.sub.1 is selected from the group consisting of lower alkyl; lower alkylene phenyl; substituted lower alkylene phenyl wherein the phenyl is substituted from 1 to 3 times with lower alkyl, lower alkoxy, lower acyloxy, hydroxy, nitro and halo; lower alkylene naphthyl, lower alkylene thienyl; lower alkylene diphenyl; lower alkylene-hydroxy-phenyl; substituted lower alkylene-hydroxy-phenyl wherein the phenyl is substituted from 1 to 3 times with lower alkyl, lower alkoxy, lower acyloxy, hydroxy, nitro, and halo; lower alkylene-hydroxy-naphthyl; lower alkylene-hydroxy-thienyl; lower alkylene-hydroxy-diphenyl, and R.sub.2 is H or lower alkylene. The method comprises reacting a compound of a formula II: ##STR2## with a cyclic dioxy or cyclic dithio in the presence of catalyst.

Abstract: The present invention provides a method of achieving the time-specific delivery of a pharmaceutically active agent to a patient in need of the therapeutic effects of the pharmaceutically active agent. The method includes administering a pharmaceutical formulation comprising (a) a core including the pharmaceutically active agent to be delivered, and (b) a swellable polymeric coating layer substantially surrounding the core. The swellable polymeric coating layer delays the release of the pharmaceutically active agent from the core for a predetermined period of time dependent upon the thickness of the swellable polymeric coating layer. The swellable polymeric coating layer surrounding the core is provided by a new method which includes alternately (i) wetting the core with a binder solution, and (ii) coating the core with powdered polymeric particles a sufficient number of times to produce a time-specific dosage formulation having the desired thickness of swellable polymeric coating layer.

Abstract: The present invention provides new process of preparing neuromuscular blocking agents. The process include preparing neuromuscular blocking agents using the compounds of formula I: ##STR1## wherein R.sub.1 is .dbd.O and X is halo; and formula II: ##STR2## wherein R.sub.1 and X are as defined above.

Abstract: The present invention provides new process of preparing neuromuscular blocking agents. The process include preparing neuromuscular blocking agents using the compounds of formula I: ##STR1## wherein R.sub.1 is .dbd.O and X is halo; and formula II: ##STR2## wherein R.sub.1 and X are as defined above.

Abstract: A novel, cyclosporin-producing microbe is described. A process for the production of cyclosporin, comprising culturing the novel microbe and recovering the desired form of cyclosporin produced, is described.

Abstract: The invention relates to pharmaceutical compositions for parenteral administration. The compositions comprise an amount of neuromuscular blocking agent effective to produce muscular relaxation, and at least one zwitterionic substance having an isoionic point not greater than 7. The zwitterionic substance is present in an amount of between about 2 and about 30 percent by weight, based on the weight of the composition. The resulting composition has a pH of less than 7.

Abstract: The present invention provides a method for isolating cyclosporin by adsorption chromatography. The method comprises the steps of: (a) loading a crude solution containing a cyclosporin onto adsorption chromatography column containing an adsorption resin, (b) eluting the cyclosporin from the adsorption chromatography column, and (c) collecting the eluted cyclosporin. The step of eluting the cyclosporin is carried out by passing an eluting solvent through the column, which comprises a hydrophilic component and a lipophilic component, wherein the cyclosporin is separately eluted from other compounds by providing a hydrophilic/lipophilic balance in the eluting solvent that selectively desorbs the cyclosporin from the column.

Abstract: Liquid bioadhesive microemulsions or liposomic dispersions containing proteinic substances, especially calcitonin, that allow the systemic, local or topical administration of drugs by transmucosal route are described. This type of administration shows some considerable advantages of activity, tolerability, dosage individualization and drug stability. The compositions contain proteinic substances, and a polyoxyethylene-polyoxypropylene thermosetting copolymer. At body temperature the viscosity of the compositions is increased and provides increase residence time at the administration site.

Abstract: A liquid pharmaceutical composition which can be administered as a foam by means of suitable supplying devices, without necessity of gas propeller, said composition consisting of:a) one or more natural or synthetic ionic or non ionic, acid, basic or neutral surfactants;b) a solvent or a solvent mixture;c) an active ingredient or a combination of active ingredients;d) optionally mucoadhesive or thermosetting polymers;e) optional adjuvants or excipients.

Abstract: N-(5-thioxo-L-prolyl)-L-cysteine and derivatives thereof, having interesting mucolytic-expectorant, antioxidant (radical-scavenger), antielastase, antiemphysema, immunostimulating and hepatoprotective activities and a low toxicity are described, as well as processes for the preparation thereof and pharmaceutical formulations for the use in therapy.

Abstract: 3-L-(5-thioxo-L-prolyl)thiazolidine-4-carboxylic acid and the derivatives thereof have valuable immunostimulating, antioxidant, antiradical and antiageing properties. They are prepared by thionating the corresponding 3-L-pyroglutamyl-L-thiazolidine-4-carboxylic acid derivatives or by condensing 5-thioxo-L-proline with the corresponding L-thiazolidine-4-carboxylic acid derivatives.

Abstract: Processes for the preparation of bromocriptine tablets or capsules wherein the active ingredient is protected by inclusion in an excipient or by separated granulation of the excipients and mixing granulate with a mixture of the active ingredient and a excipient having low moisture content.

Abstract: Ester or amide derivatives of 3-pyroglutamylthiazolidine-4-carboxylic acid exhibit interesting immunostimulating, antitoxic, antiinflammatory, antioxidental, antiageing properties.

Abstract: New N-(2-cycloalkylamino)ethyl-substituted benzamides having a powerful stimulating activity on gastric motility and with a low central anti-dopaminergic activity are described. The synthesis and the pharmaceutical preparation for therapeutical use are also described.

Abstract: 3-L-pyroglutamoyl-thiazolidine-4-carboxylic acid, prepared starting from an activated ester of L-pyroglutamic acid from pyroglutamoyl chloride and L-thiazolidine-4-carboxylic acid, exhibits interesting immunostimulant, antitoxic, antiinflammatory, antioxidant and anti-aging properties.

Abstract: 1,4-Dihydropiridine derivatives having the formula ##STR1## wherein R is methyl, ethyl or isopropyl, are endowed with a hypotensive, vasodilator and Ca.sup.++ -antagonistic activity.

Abstract: A pharmaceutical composition containing .alpha.-dihydroergocryptine, or a salt thereof, is used in combination with pharmaceutically acceptable carrier means or excipient for the treatment of Parkinson's disease, depression or cephalalgias is disclosed. A method for administering the composition to a patient is also provided.