Abstract: The invention relates to antibacterially active pyrido-benzothiazine derivatives with long-term action, having the following general formula: ##STR1## in which R is ##STR2## Where R.sup.1 is H, C.sub.1 -C.sub.6 alkyl, p-fluorophenyl, m-fluorophenyl, o-fluorophenyl or 2-pyridyl; or ##STR3## where R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 are lower alkyls. The invention also comprises the process for preparing compounds of general formula (I). Said process consists of a synthesis cycle using 2,4-difluoro-3-chloronitrobenzene and thiolactic acid as starting substances.The inventiona also comprises pharmaceutical compositions containing at least one of the compounds of general formula (I) as active principle.
Abstract: A process for producing natural heparan sulphate and dermatan sulphate for mixtures of proteoglycans from the aorta, myocardium and particularly vascularized organs, based on a series of precipitation and purification steps which enable the protein part of the proteoglycan to be eliminated and the two products to be obtained in substantially pure form, without any chemical or enzymatic degradation.When administered orally or parenterally, the heparan sulphate obtained exerts activation effects on antithrombin III and on the fibrinolytic process.The dermatan sulphate obtained exerts an inhibiting effect on Factor Xa and also possesses the property of activating the fibrinolytic effect of heparan sulphate.
Type:
Grant
Filed:
March 10, 1986
Date of Patent:
November 8, 1988
Assignee:
Mediolanum Farmaceutici Srl
Inventors:
Rinaldo Del Bono, Luigi De Ambrosi, Piergiuseppe Pagella, Gianni Ferrari
Abstract: Bio-available iron-protein derivatives having an iron content of from 2% to 20% by weight and a nitrogen content of from 12% to 16% by weight obtained by reacting acetylated globin with an iron compound selected from the group consisting of ferric chloride, iron fructate and iron saccharate, and pharmaceutical compositions for treating and preventing iron deficiency in animals and humans.
Abstract: Pyrido-benzothiazine compounds having anti-microbial activity are prepared by (a) reacting 3-chloro-4-fluoroaniline with potassium thiocyanate and bromine to produce 2-amino-6-fluoro-7-chlorobenzothiazole, (b) reacting 2-amino-6-fluoro-7-chlorobenzothiazole with sodium hydroxide to produce the disulfide of 2-amino-5-fluoro 6-chlorothiophenol, (c) reacting the disulfide with sodium monochloroacetate to produce 7-fluoro-8-chloro-2H-1,4-benzothiazin-3(4H)-one, (d) reducing 7-fluoro-8-chloro-2H-1,4-benzothiazin-3(4H)-one to produce 7-fluoro-8-chloro-3,4-dihydro-2H-1,4-benzothiazone, (e) reacting 7-fluoro-8-chloro-3,4-dihydro-2-H-1,4-benzothiazone with ethyl ethoxymethylenemalonate and cyclyzing the intermediate formed with polyphosphoric acid to produce ethyl 9-fluoro-10-chloro-7-oxo-2,3-dihydro-7H-pyrido[1,2,3 de] [1,4]-benzothiazine-6-carboxylate and (f) hydrolyizing the ethyl carboxylate to produce the corresponding carboxylic acid.
Type:
Grant
Filed:
August 13, 1985
Date of Patent:
May 26, 1987
Assignee:
Mediolanum Farmaceutici S.R.L.
Inventors:
Giuseppe Mascellani, Arnaldo Fravolini, Patrizia Terni
Abstract: Object of the invention is a class of new organic compounds derived from 1,4-benzothiazine through substitution of an hydrogen atom in position 6, 7 or 8 by an oxypropanolammine radical monosubstituted in N and furthermore a series of new phenyl derivatives of 1,4-benzothiazine, obtained as intermediate in the synthesis of oxypropanolammine derivatives, and process for obtained the new compounds in form suitable for the preparation of pharmaceutical compositions having antihypertensive, vasodilating and antiarrhythmic activity.
Abstract: An arterial polysaccharide complex of anionic character consisting of hexosamine glycanmonosulphates (FAPA) derived from the aorta of young mammals and a process for its preparation.
Abstract: 1,2 Benzothiazino[3,4-d]pyrazoles of the following general formula ##STR1## wherein R stands for a linear or branched (C.sub.2-4) alkyl chain bearing a substituent of formula ##STR2## in which the R" radicals may be the same or different and represent hydrogen, (C.sub.2-4)alkyl, (C.sub.4-7) cycloalkyl or, taken together with the adjacent nitrogen atom, may also represent a saturated, 5 to 7 membered heterocyclic ring containing from one to three heteroatoms independently selected from O,N and S, or R may represent the 1-ethyl-pyrrolidine-2-yl-methyl radical, and R' is hydrogen, a halogen atom or a (C.sub.1-4) alkyl radical; methods for their preparation; pharmaceutical compositions containing them. The compounds possess antiinflammatory, antipyretic and analgesic activity.
Abstract: The invention provides 2-(2-thenoylthio)-propionylglycine, a novel compound having liver-protective, mucolytic and bronchial-spasm relieving activity.