Abstract: Organic salts of physostigmine derivatives, having the following general mula: ##STR1## in which R is a linear or branched C.sub.2 -C.sub.12 alkyl or a cycloalkyl or an aryl, and X.sub.- is the anion of an organic acid, the process for their preparation and their pharmaceutical use for acetylcholinesterase inhibition purposes.
Type:
Grant
Filed:
March 28, 1988
Date of Patent:
December 18, 1990
Assignee:
Mediolanum Farmaceutici S.r.l. Consiglio Nazionale Delle Ricerch
Inventors:
Carlo Meroni, Stefano Maiorana, Mario Brufani, Massimo Pomponi, Riccardo Bernardi, Pier L. Rugarli, Pier G. Pagella
Abstract: Pyrido-benzothiazine derivatives having the following general formula: ##STR1## in which R is H or a C.sub.1 -C.sub.6 alkyl or a C.sub.1 -C.sub.6 fluoroalkyl, and R.sub.1 is N-alkyl-3-pyrrolidinalkylamine with C.sub.1 to C.sub.6 alkyls or ##STR2## where R.sub.2 is a S.sub.1 -C.sub.6 alkyl or a C.sub.2 -C.sub.6 alkenyl or an arylalkyl group, possibly substituted by halogen, hydroxy or keto-groups, both in the racemic form and in the optically active form.The invention also comprises the process for the preparation of derivatives of formula (I) starting from 2.4-difluoro-3-chloronitrobenzene.Said derivatives possess a high antibacterial acitvity as well as a high bioavailability to tissues; the invention also refers to pharmaceutical compositions containing them as active components.
Type:
Grant
Filed:
September 30, 1988
Date of Patent:
May 8, 1990
Assignee:
Mediolanum farmaceutici, S.r.l.
Inventors:
Patrizia Terni, Stefano Maiorana, Antonio Papagni, Piergiuseppe Pagella
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.