Patents by Inventor Giuseppe Mascellani
Giuseppe Mascellani has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Publication number: 20090149423Abstract: The present invention relates to the use of heparin oligosaccharides having a molecular weight?5050 Da and an anti-factor Xa activity?80 IU/mg, or their sodium salts, for preparing a medicament for the prevention and treatment of osteoporosis and associated pathologies and for preparing a medicament effective for the prevention and treatment of cerebral ischemia and pathologies related thereto whose treatment necessitates drugs able to cross the blood-brain barrier.Type: ApplicationFiled: October 27, 2005Publication date: June 11, 2009Applicant: OPOCRIN S.P.A.Inventors: Pietro Bianchini, Giuseppe Mascellani, Bruna Parma
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Publication number: 20050049222Abstract: The present invention relates to a process for preparing high purity low molecular weight heparins with average molecular weight of between 2000 and 10000 daltons by the stages of forming an intermediate heparin benzethonium salt, from this latter a water soluble heparin ester, and of subjecting said ester to depolymerisation with bases to form said low molecular weight heparins, characterised in that at least said stage of heparin benzethonium salt formation is carried out on an inert adsorbent solid matrix of filtering material, or filter-aid, said low molecular weight heparins being finally subjected to a purification stage by reducing the impurities present with borohydride.Type: ApplicationFiled: August 26, 2004Publication date: March 3, 2005Applicant: OPOCRIN S.p.A.Inventors: Pietro Bianchini, Lino Liverani, Giuseppe Mascellani, Stefania Tiddia
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Patent number: 5547944Abstract: A natural dermatan sulphate with antithrombinic activity in excess of 220 U/mg which comprises an oligosaccharide sequence with a high degree of sulfation, having formula (III) ##STR1## in which: n=integers 1 or 2; R.sub.4 =SO.sub.3, or H; R.sub.6 =H, or SO.sub.3 ; G=glucuronic acid: I--non-sulfated uronic acid, preferably glucuronic acid, is extracted from organs, and subsequently purified in mild operating conditions, at pH 5-7, isolation and fractionation being carried out with macroreticular ion exchange resins, having a particle size of less than 10 .mu..Type: GrantFiled: February 23, 1994Date of Patent: August 20, 1996Assignee: Opocrin S.p.A.Inventors: Giuseppe Mascellani, Pietro Bianchini
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Patent number: 4973580Abstract: Process for the preparation of oligosaccharides by a controlled chemical depolymerization of natural polysaccharides, such as heparins, heparan sulfates, dermatan sulfates, chondroitinsulfates, hyaluronic acid, by a radicalic reaction in an aqueous solution, at a temperature ranging between 20.degree. and 70.degree. C., in the presence of a catalyst selected in the group consisting of Cu++, Fe++, Cr+++, Cr.sub.2 O.sub.7 - as well as the resulting oligosaccharides and their related pharmaceutical compositions. The products exhibit high antithrombotic activity, little or no anticoagulant activity, high fibinolytic activity an antiinflammatory activity.Type: GrantFiled: May 10, 1989Date of Patent: November 27, 1990Assignee: Opocrin S.p.A. Laboratorio FarmacobiologicoInventors: Giuseppe Mascellani, Pietro Bianchini
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Patent number: 4933326Abstract: Heparin fractions which are a mixture of oligosaccharides containing 6-12 monosaccharides are described. The oligosaccharides contain reducing end groups composed of iduronic acid 2-sulfate or glucosamine N, 6-disulfate. The end group monosaccharides contain the reducing anomeric carbons. The SO.sub.3.sup.- /COO.sup.- ratio is essentially the same as in heparin. The method of preparation is a depolymerization initiated by free radicals. One fraction is a heparin fragment with a molecular weight (MWw) of 2,100 daltons (+10%). The compound contains 6-8 monosaccharides, has the same SO.sub.3.sup.- /COO.sup.- ratio as the parent heparin and has platelet anti-aggregating activity, arterial and venous antithrombotic action, fibrinolytic and antiatherosclerotic activity. It exhibits poor anti factor Xa activity and no anticoagulant action.Type: GrantFiled: September 21, 1988Date of Patent: June 12, 1990Assignee: Opocrin S.p.A.Inventors: Pietro Bianchini, Giuseppe Mascellani
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Patent number: 4791195Abstract: Novel oligosaccharide fractions with valuable pharmacological properties are obtained from heparin. They have the same structural characteristics of heparin. The heparin fraction consists of oligosaccharides which contain end groups consisting of iduronic acid 2-sulfate, or glucosamine N, 6-disulfate. Further the oligosaccharides contain and monosaccharide endowed with reducing anomeric carbon, and are constituted by multiples of monosaccharide units.Type: GrantFiled: October 21, 1986Date of Patent: December 13, 1988Assignee: Opocrin A.P.A.Inventors: Pietro Bianchini, Giuseppe Mascellani
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Patent number: 4684647Abstract: A new class of antimicrobial pyrido-benzothiazine compounds and processes for their preparation are described.Type: GrantFiled: October 24, 1986Date of Patent: August 4, 1987Assignee: Mediolanum Farmaceutici S.R.L.Inventors: Giuseppe Mascellani, Arnaldo Fravolini, Patrizia Terni
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Patent number: 4668784Abstract: 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: GrantFiled: August 13, 1985Date of Patent: May 26, 1987Assignee: Mediolanum Farmaceutici S.R.L.Inventors: Giuseppe Mascellani, Arnaldo Fravolini, Patrizia Terni
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Patent number: 4515809Abstract: Derivatives of benzoylphenoxyalkanoic acids corresponding to the formula: ##STR1## wherein: X represents for example a halogen, R.sup.1 and R.sup.2 represent for example alkyl groups, R represents for example an aminoacid; and the salts thereof are new products showing antilipaemic and anticholesterolemic pharmacological activity.Type: GrantFiled: April 20, 1981Date of Patent: May 7, 1985Assignee: Alfa Farmaceutici S.p.A.Inventors: Valerio Borzatta, Manlio Cristofori, Mauro Morotti, Giuseppe Mascellani
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Patent number: 4378373Abstract: Derivatives of benzoylphenoxyalkanoic acids corresponding to the formula: ##STR1## wherein: X represents for example a halogen, R.sup.1 and R.sup.2 represent for example alkyl groups, R represents for example an aminoacid; and the salts thereof are new products showing antilipaemic and anticholesterolemic pharmacological activity.Type: GrantFiled: April 20, 1981Date of Patent: March 29, 1983Assignee: Alfa Farmaceutici S.p.A.Inventors: Valerio Borzatta, Manlio Cristofori, Mauro Morotti, Giuseppe Mascellani
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Patent number: 4296125Abstract: Derivatives of benzoylphenoxyalkanoic acids corresponding to the formula: ##STR1## wherein: X represents for example a halogen, R.sup.1 and R.sup.2 represent for example alkyl groups, R represents for example an aminoacid; and the salts thereof are new products showing antilipaemic and anticholesterolemic pharmacological activity.Type: GrantFiled: February 21, 1980Date of Patent: October 20, 1981Assignee: Alpha Farmaceutici S.p.A.Inventors: Valerio Borzatta, Manlio Cristofori, Mauro Morotti, Giuseppe Mascellani
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Patent number: 4200573Abstract: New compounds being derivatives of 3-carboxyrifamycin S and SV are prepared by oxidation of cyanohydrin of 3-formylrifamycin S to 3-(cyanocarbonyl)rifamycin S, condensation with a compound of formula HR (an alcohol, an amine or an substituted hydrazine) and, optionally, reduction of the derivative of 3-carboxyrifamycin S so obtained to the corresponding SV form. Alternatively 3-(cyanocarbonyl)rifamycin S may be converted to the SV form before condensing with the compound HR.Type: GrantFiled: December 11, 1978Date of Patent: April 29, 1980Assignee: Alfa Farmaceutici, S.p.A.Inventors: Mario Brufani, Egidio Marchi, Pierfranco Bellomo, Giuseppe Mascellani
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Patent number: 4168375Abstract: A process for the recovery of cephalosporin C from an aqueous medium, including the steps of treating the medium with a sulphonyl chloride of formula R--SO.sub.2 Cl, in which R is a substituted or unsubstituted alkyl group having from 4 to 10 carbon atoms, or a substituted or unsubstituted aryl group, to convert the cephalosporin C to the corresponding sulphonamide and extracting the sulphonamide with an essentially water immiscible solvent. The sulphonyl chloride may be toluene-p-sulphonyl chloride, p-isopropylbenzenesulphonyl chloride or .beta.-naphthalenesulphonyl chloride. The molar ratio of sulphonyl chloride to cephalosporin C present in the aqueous medium is from 3 to 10. The temperature of the reaction of sulphonyl chloride with cephalosporin C is maintained in the range from 10.degree. to 20.degree. C. The water immiscible solvent is selected from ethyl acetate, n-butanol and methylisobutylketone. The pH of the reaction medium is maintained at a value of from 7.5 to 9.5 by means of a buffering agent.Type: GrantFiled: February 11, 1975Date of Patent: September 18, 1979Assignee: Alfa Farmaceutici, S.p.A.Inventors: Renato Andrisano, Giuseppe Mascellani, Guido Guerra
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Patent number: 3931161Abstract: Novel cephalosporin derivatives, for example N-acetoacetylcephalosporin C, N-decanoylcephalosporin C, N-dodecanoylcephalosporin C and N-hendecenoylcephalosporin C, are useful as readily-recoverable intermediates in the isolation of cephalosporin C value from fermentation broths and in the preparation of 7-aminocephalosporanic acid. They are prepared by treating an aqueous solution containing cephalosporin C, such as a fermentation broth, with diketene or an acid chloride such as decanoyl chloride, dodecanoyl chloride or hendecenoyl chloride, followed by solvent extraction. They are converted into 7-aminocephalosporanic acid by successively forming the silyl di-ester, halogenating to the imino-halide, converting the imino-ether and hydrolysing to 7-ACA.Type: GrantFiled: March 6, 1973Date of Patent: January 6, 1976Assignee: Alfa Farmaceutici S.p.A.Inventors: Carlo Buitar, Giuseppe Mascellani, Guido Guerra