Abstract: 4-(isoxazolyl)-thiazole-2-oxamic acids, esters and salts thereof; method for preparing them and intermediate compounds useful for their preparation.Said compounds possess antiallergic and antianaphylactic activity and may be used in the pharmaceutical field.Compositions for pharmaceutical use containing said compounds as the active ingredients are also described.
Type:
Grant
Filed:
March 13, 1986
Date of Patent:
August 23, 1988
Assignee:
Zambon S.p.A.
Inventors:
Angelo Carenzi, Dario Chiarino, Davide Della Bella, Giancarlo Grancini
Abstract: A process is described for preparing alpha-haloalkyl-aryl-ketones, comprising reacting a substantially anhydrous strong acid with a ketal of formula ##STR1## in which Ar, R, R.sub.1, R.sub.2 and X have the meanings given in the description.
Abstract: The compounds of formula ##STR1## wherein the group ##STR2## represents the residue of a natural amino acid selected from the group consisting of glycine, alanine, beta-alanine, phenylalanine, isoleucine, methionine, proline, aspartic acid and arginine; R represents a hydrogen atom or a C.sub.1 -C.sub.4 alkyl; and their acid-addition salts with pharmaceutically acceptable organic or inorganic acids; are useful in the preventive and curative treatment of pathologic syndromes due to the lowering of glutathione (GSH) levels.
Type:
Grant
Filed:
August 11, 1986
Date of Patent:
August 2, 1988
Assignee:
Zambon S.p.A.
Inventors:
Alberto Pilotto, Mario Portelli, Angelo Carenzi, Davide Della Bella
Abstract: A process is described for the preparation of cis-5-fluoro-2-methyl-1-(4-methylthiobenzylidene)-indene-3-acetic acid that consists in reacting a lower alkyl ester of 5-fluoro-2-methylindene-3-acetic acid with a substantially equimolecular amount of 4-methylthio-benzaldehyde in a solid-liquid two-phase system in which the solid phase is a potassium alcoholate or hydroxide and the liquid phase is a solution of the reagents in an organic solvent inert in the reaction conditions, in the presence of a phase transfer catalyst and at a temperature comprised between -20.degree. and +20.degree. C.
Abstract: Replacement with fluorine of the primary hydroxy group of 1-phenyl-2-amino-1,3-propanediol compounds wherein the secondary hydroxy group and the amino group have been suitably protected.The reaction is carried out with an inorganic fluoride in a polyglycol.New oxazoline compounds particularly useful in said process.
Abstract: Compounds of formula ##STR1## wherein Ar represents an optionally substituted aryl group;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, equal to or different from each other, represent hydroxy, O.sup.- M.sup.+, OR.sub.3 or ##STR2## R.sub.3 represents a C.sub.1 -C.sub.24 alkyl, a C.sub.3 -C.sub.6 cycloalkyl, a phenyl or a benzyl;M.sup.+ represents the cation of an alkaline metal;R.sub.4 and R.sub.5, equal to or different from each other, represent a hydrogen atom, a C.sub.1 -C.sub.4 alkyl, a C.sub.5 -C.sub.6 cycloalkyl, a (CH.sub.2).sub.n --CH.sub.2 OH group with n=1, 2 or 3, or R.sub.4 and R.sub.5 together are a group (CH.sub.2).sub.m with m=4 or 5, a group --CH.sub.2 --CH.sub.2 --R.sub.6 --CH.sub.2 --CH.sub.2 -- in which R.sub.6 is an oxygen atom, an N--H or N--(C.sub.1 -C.sub.
Abstract: Bis-(2-ammonium-2-hydroxymethyl-1,3-propanediol)(2R-cis)-(3-methyloxiranyl) -phosphonate showing high bioavailability and tolerability is disclosed, as well as a method for preparing same from (2R-cis)-(3-methyloxiranyl)-phosphoric acid, or a salt thereof, and 2-amino-2-hydroxymethyl-1,3-propanediol, or a salt thereof. Pharmaceutical compositions containing the novel bis-phosphonate; useful for clinical forms of urinary and respiratory infections, are also disclosed.
Type:
Grant
Filed:
January 23, 1986
Date of Patent:
February 23, 1988
Assignee:
Zambon S.p.A.
Inventors:
Dario Chiarino, Davide Della Bella, Vittorio Ferrari
Abstract: A new enantioselective process is described for preparing optically active alpha-arylalkanoic acids by:(a) halogenation on the aliphatic carbon atom alpha to the ketal group, of ketals of formula ##STR1## in which Ar represents an aryl, optionally substituted;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, represents a hydroxy, a O.sup.- M.sup.+, OR.sub.3 or NR.sub.4 R.sub.5 group; the carbon atoms indicated by an asterisk both simultaneously are in (R) or (S) configuration.This reaction is diastereoselective, so that a misture of alpha-haloketals is obtained in which one of the two epimers prevails, and generally strongly prevails, over the other.(b) rearrangement of the haloketals of formula ##STR2## in which X is Cl, Br or I to alpha-arylalkanoic acids in a single stage or in two successive stages, by way of esters of formula ##STR3## The compounds (A) and (C) are all new compounds. The rearrangement step (b) may be performed under new, inventive conditions.
Abstract: It is described an effervescent composition consisting of:Ibuprofen 9-17% w/wArginine 17-33% w/wSodium or potassium bicarbonate 20-35% w/wSodium bitartrate 25-40% w/wSuch composition is useful for pharmaceutical preparations in the form of effervescent tablets or granulates.
Type:
Grant
Filed:
November 6, 1986
Date of Patent:
August 25, 1987
Assignee:
Zambon S.p.A.
Inventors:
Annibale Gazzaniga, Valter Gianesello, Federico Stroppolo, Luigi Vigano'
Abstract: A process is described for the preparation of alpha-hydroxyl-alkanoic acids of formula ##STR1## which are known anti-inflammatory agents or intermediates for known pharmaceutical products. The process consists essentially in the rearrangement of phenolates of formula ##STR2## wherein Ar is an unsubstituted or substituted phenyl or naphthyl, in aqueous environment or in an organic medium, at temperatures comprised within the range of from 0.degree. to 100.degree. C. and within short times, followed by either acid or alkaline hydrolysis.
Type:
Grant
Filed:
February 1, 1985
Date of Patent:
February 10, 1987
Assignee:
Zambon S.p.A
Inventors:
Claudio Giordano, Fulvio Uggeri, Francesco Minisci
Abstract: N-substituted derivatives of 1-(4'-alkylthiophenyl)-2-amino-1,3-propanediol, their salts with pharmaceutically acceptable organic and inorganic acids, processes for preparing them, pharmaceutical compositions containing them and intermediates useful in the preparation thereof.The novel derivatives according to this invention are endowed with calcium antagonist activity and are useful as antiarrhythmic and vasodilating agents.
Type:
Grant
Filed:
August 1, 1984
Date of Patent:
January 20, 1987
Assignee:
Zambon S.p.A.
Inventors:
Dario Chiarino, Angelo Carenzi, Davide Della Bella, Mario Fantucci
Abstract: N-substituted derivatives of 1-(4'-alkylsulfonylphenyl)-2-amino-1,3-propanediol, their salts with pharmaceutically acceptable organic and inorganic acids, processes for preparing them, pharmaceutical compositions containing them and intermediates useful in the preparation thereof.The novel derivatives according to this invention are endowed with local anesthetic activity.
Type:
Grant
Filed:
August 3, 1984
Date of Patent:
December 30, 1986
Assignee:
Zambon S.p.A.
Inventors:
Dario Chiarino, Angelo Carenzi, Davide Della Bella, Mario Fantucci
Abstract: Process for the preparation of pharmacologically active compounds containing a sulfoxide group by oxidation of a thioether with hypochlorite in an alkaline medium at a pH higher than 10 and at a temperature comprised between 0.degree. and 40.degree. C.
Abstract: Alpha-alkyl-alkanoic acids are prepared by heating at boiling temperature a mixture of an alpha-halogen-alkyl-arylketone in a saturated aliphatic diol or in a mixture of saturated aliphatic diols in the presence of a Broensted's acid and by successively alkalifying the reaction mixture.
Abstract: A process is disclosed for the preparation of optically active alpha-arylalkanoic acids, consisting in the rearrangement of optically active alpha-(haloalkyl)-aryl-ketals and in submitting to hydrolysis the so-obtained esters of alpha-arylalkanoic acids.The rearrangement reaction is carried out under neutral or slightly alkaline conditions in a polar protic medium.
Abstract: A process is disclosed for the preparation of optically active alpha-arylalkanoic acids, consisting in the rearrangement of optically active (alpha-haloalkyl)-aryl-ketals and in submitting to hydrolysis the thus obtained esters of alpha-arylalkanoic acids. The rearrangement reaction is carried out under neutral or alightly alkaline conditions, in an aprotic dipolar diluent and in the presence of a protic substance having a high dielectric constant.
Abstract: New imidazole compounds of the formula ##STR1## their salts and analgesic, antipyretic and antiinflammatory pharmaceutical composition containing them. New intermediates useful in the preparation of said imidazole compounds.Process for preparing the new imidazole compounds as well as some new intermediates for the preparation thereof.
Type:
Grant
Filed:
March 20, 1984
Date of Patent:
December 24, 1985
Assignee:
Zambon S.p.A.
Inventors:
Angelo Carenzi, Dario Chiarino, Davide Della Bella, Viviana Frigeni, Carlo Veneziani
Abstract: Alpha substituted alkylarylketals of formula: ##STR1## wherein Ar is an aromatic radical having from 3 to 20 C atoms,X is halogen, OR.sub.3 (wherein R.sub.3 is H, acyl or aroyl), OSO.sub.2 CH.sub.3 or OSO.sub.2 C.sub.6 H.sub.4 --CH.sub.3,R is H or alkyl having from 1 to 3 C atoms,Y is --CH.sub.2 --C(R.sub.1).dbd.C(R.sub.2)--CH.sub.2 --(wherein, in turn, R.sub.1 and R.sub.2 are H or methyl).The products of formula I are useful for preparing alpha-aryl-alkanoic acids.
Abstract: Rearrangement of alpha-halo-alkylarylketals in neutral or weakly alkaline conditions and in the presence of a polar-protic medium and subsequent hydrolysis of the thus obtained esters, in the same reaction medium, to afford the corresponding alpha-arylalkanoic acids or their salts which are particularly useful as anti-inflammatory, analgesic and antipyretic agents.