Patents Assigned to Polifarma S.p.A.
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Patent number: 6339160Abstract: Objects of the present invention are compounds of a peptido-mimetic character having the capacity of acting as inhibitors of metalloproteinases produced by venom of snake, and of other metalloproteinases of human origin which have been put in relation with various pathologies in man, including tumoral growth and metastatization, aterosclerosis, multiple sclerosis, Alzheimer's disease, osteoporosis, hypertension, rheumatoid arthritis and other inflammatory diseases. Object of the present invention is also the procedure for the production of diethylester of (1)-phosphotryptophan, as an initial product necessary to synthesize all compounds mentioned above.Type: GrantFiled: May 9, 2000Date of Patent: January 15, 2002Assignees: Polifarma S.p.A., Consiglio Nazionale Delle RicercheInventors: Vincenzo Politi, Enrico Gavuzzo, Carlo Gallina, Giovanni Di Stazio, Silvana D'Alessio, Antonio Sella, Cinzia Piazza, Cesare Giordano, Barbara Gorini, Gabriella Panini, Mario Paglialunga Paradisi, Maurizio Cirilli, Giorgio Pochetti, Fernando Mazza
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Patent number: 6057297Abstract: Peptidomimetic compounds capable of inhibiting zinc-dependent metalloproteinases to treat pathological conditions associated with activation of endogenous metalloproteinases in mammals.Type: GrantFiled: March 18, 1998Date of Patent: May 2, 2000Assignee: Polifarma S.p.A.Inventors: Vincenzo Politi, Silvana D'Alessio, Giovanni Di Stazio, Giovanna De Luca, Mario Materazzi
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Patent number: 5962459Abstract: Uridine is a therapeutic agent active as a growth promoter for treatment of neuron degenerative diseases deriving from pathological ageing or selective destruction, in particular Uridine shows the same biological effects as NGF, when added at low doses to the culture medium, so that uridine may replace NGF as therapeutic agent in neural diseases and it may be also associated with other growth factors that allow differentiation of neurons, or with anti-cancer and anti-virus drugs that cause neuron damage. In addition uridine shows important trophic properties on various types of cultured cells, stimulating cell reproduction when used at rather high dose levels.Type: GrantFiled: May 23, 1997Date of Patent: October 5, 1999Assignee: Polifarma S.p.A.Inventors: Cinzia Piazza, Vincenzo Politi, Mario Materazzi, deceased
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Patent number: 5846755Abstract: A method for determining the therapeutic potential of peptidomimetic compounds as inhibitors of zinc-dependent metalloproteinase activity associated with pathological conditions of humans and animals.Type: GrantFiled: August 6, 1996Date of Patent: December 8, 1998Assignee: Polifarma S.p.A.Inventors: Vencenzo Politi, Silvana D'Alessio, Giovanni Di Stazio, Giovanna De Luca, Mario Materazzi
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Patent number: 5736518Abstract: Compounds of general formula A--B--C in which: A is a monovalent radical of a L-ring molecule; B is a bivalent radical of a L-.alpha.-aminoacid; and C is a monovalent radical of a L-aromatic molecule. The compounds show an anti-hypertensive, analgesic, immuno-modulating and antiinflammatory activity, they are resistant to enzyme hydrolysis and they can be used for the preparation of drugs for oral administration.Type: GrantFiled: December 15, 1995Date of Patent: April 7, 1998Assignee: Polifarma S.p.A.Inventors: Vincenzo Politi, Giovanni Di Stazio, Andrea Margonelli, Giovanna De Luca
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Patent number: 5504071Abstract: Compounds of general formula A--B--C in which: A is a monovalent radical of a laevorotatory ring molecule; B is a bivalent radical of a laevorotatory .alpha.-aminoacid; and C is a monovalent radical of a laevorotatory aromatic molecule. The compounds show an anti-hypertensive, analgesic, immuno-modulating and antiinflammatory activity, they are resistant to enzyme hydrolysis and they can be used for the preparation of drugs for oral administration.Type: GrantFiled: September 26, 1994Date of Patent: April 2, 1996Assignee: Polifarma S.p.A.Inventors: Vincenzo Politi, Giovanni Di Stazio, Andrea Margonelli, Giovanna De Luca
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Patent number: 5447951Abstract: 3-indolepyruvic acid is an active agent in preventing cerebral damage caused by stress and ageing and induced by an excessive presence in the blood of glucocorticoids, secreted by the adrenal gland.Type: GrantFiled: January 10, 1994Date of Patent: September 5, 1995Assignee: Polifarma S.p.A.Inventors: Vincenzo Politi, Mario Materazzi, Giovanni Di Stazio, Giovanna De Luca
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Patent number: 5210215Abstract: 3-indolepyruvic acid derivatives substituted on the benzene moiety show good antagonizing activity on excitatory aminoacids and on free radicals, for which reason they are therapeutic agents in cerebral and peripheral degenerative pathologies. Their method of production by passage through the corresponding substituted triptophane.Type: GrantFiled: September 18, 1990Date of Patent: May 11, 1993Assignee: Polifarma S.p.A.Inventors: Vincenzo Politi, Giovanna De Luca, Giovanni Di Stazio, Mario Materazzi
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Patent number: 5190948Abstract: Uridine is used to treat the peripheral complications of diabetes, such as neuropathy, retinopathy and vasculopathy, thanks to its characteristics of promotor of glycogen endocellular biosynthesis. 40 diabetic patients were treated for six months with uridine or with placebo in a double-blind clinical teat.Type: GrantFiled: May 22, 1991Date of Patent: March 2, 1993Assignee: Polifarma S.p.A.Inventors: Mario Materazzi, Vincenzo Politi, Giovanni Di Stazio, Giovanna De Luca
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Patent number: 5143903Abstract: Compounds of peptide nature presenting a sequence of three aminoacids, in particular with PYR and TRP as terminal groups, are found to be active as immunomodulating agents.Type: GrantFiled: September 14, 1990Date of Patent: September 1, 1992Assignee: Polifarma S.p.A.Inventors: Vincenzo Polita, Giovanna De Luca, Giovanni Di Stazio, Mario Materazzi
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Patent number: 5091172Abstract: A description is given of the cosmetic use of 3-indolepyruvic acid for the protection of the skin from damage caused by oxygen, by the sun and by aging.Type: GrantFiled: August 6, 1990Date of Patent: February 25, 1992Assignee: Polifarma S.p.A.Inventors: Vincenzo Politi, Giovanna De Luca, Giovanni Di Stazio, Mario Materazzi
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Patent number: 5075329Abstract: Indolepyruvic acid shows an inhibitory activity with respect to the degenerative action by oxygen free radical which are responsible for a number of pathologic conditions in various peripheral tissues. The compound can find application in miocardiopathies, inflammations, circulatory shock, arteriosclerosis, and cardiac ischemia.Type: GrantFiled: August 17, 1989Date of Patent: December 24, 1991Assignee: Polifarma, S.p.A.Inventors: Vincenzo Politi, Giovanni DiStazio, Giovanna DeLuca, Mario Materazzi
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Patent number: 5051404Abstract: Tripeptides having hypotensive activity, defined by the following general formula:A--B--C--OZ (I)wherein:A represents a residue of L-pyroglutamic acid, L-proline of L-proline bearing a substituent on its amino group ##STR1## wherein R.sub.1 is an acyl with a number of carbon atoms in straight chain not higher than 9, a benzyloxycarbonyl group or an alkyloxycarbonyl group;B is an .alpha.-aminoacide residue derived from one of the natural aminoacids;C is a residue of L-tryptophan (Trp), of L-phenylalanine (Phe) or of L-tyrosine (Tyr);Z is a hydrogen atom or an alkyl group with a number of carbon atoms in straight chain not higher than 9.Type: GrantFiled: September 20, 1988Date of Patent: September 24, 1991Assignees: Eniricerche, S.p.A., Polifarma, S.p.A.Inventors: Alessandro Sisto, Antonio S. Verdini, Antonino Virdia, Giovanna De Luca, Giovanni Di Stazio, Vincenzo Politi
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Patent number: 4960759Abstract: Disorders due to an altered balance of dopamine release by the cerebral dopaminergic system, such as schizophrenia and Parkinson's disease, can be treated by administration of uridine which is a specific agent for the protection of the cholecystokinin level in the brain tissue.Type: GrantFiled: June 19, 1989Date of Patent: October 2, 1990Assignee: Polifarma S.P.A.Inventors: Giovanna De Luca, Giovanni Di Stazio, Mario Materazzi, Vincenzo Politi
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Patent number: 4808728Abstract: Tryptophan and esters thereof, and other indoleaminoacids, can be easily transformed into respective alpha-ketoacids through a coupling reaction with aromatic aldehydes, in the presence of a dehydrating agent.Type: GrantFiled: March 2, 1987Date of Patent: February 28, 1989Assignee: Polifarma S.p.A.Inventors: Giovanna De Luca, Giovanni Di Stazio, Andrea Margonelli, Mario Materazzi, Vincenzo Politi
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Patent number: 4748155Abstract: Pharmacologically active tripeptides, with at least a retro-inverted peptidic bond, definable by means of the following general formulae: ##STR1## their pharmaceutically acceptable salts, esters or alkyl amides, whereinR.sub.1 represents a hydrogen atom, an alkyl group with a maximum of 7 carbon atoms, an aryl, hydroxyalkyl or hydroxyarylalkyl, guanidylalkyl, amino-alkyl, alkyl-oxy-alkyl, acylamino-alkyl, imidazolylalkyl, indolyl-alkyl, mercapto alkyl, alkylmercaptoalkyl, carbamoyl-alkyl, carboxyalkyl, alkyl-carbamoylalkyl or alkyloxy-carbonylalkyl group;R.sub.2 represents a ##STR2## group, Z is an OH, OR.sub.3, NH.sub.2, NHR.sub.3 group, whereinR.sub.3 represents an alkyl group with a number of carbon atoms comprised within the range of from 1 to 10.Type: GrantFiled: March 10, 1986Date of Patent: May 31, 1988Assignees: Eniricerche S.p.A., Polifarma S.p.A.Inventors: Alessandro Sisto, Antonio S. Verdini, Antonio Virdia, Giovanna De Luca, Giovanni Di Stazio, Vincenzo Politi
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Patent number: 4713368Abstract: Peptido-mimetic compounds of hypotensive action definable by the general formula: ##STR1## in which: X represents the pyroglutamic acid residue or a ##STR2## residue where R.sub.2 represents a hydrogen atom, an alkyloxycarbonyl, an arylalkyloxycarbonyl or an acyl group with from 1 to 7 carbon atoms in the linear chain,R.sub.1 represents the aromatic residue of L-phenylalanine, L-tyrosine or L-tryptophan, andZ represents a hydroxyl, hydroxyalkyl, amino or alkylamino group, and their salts and alkyl amides or esters.Type: GrantFiled: July 17, 1986Date of Patent: December 15, 1987Assignees: Eniricerche S.p.A., Polifarma S.p.A.Inventors: Alessandro Sisto, Antonio S. Verdini, Antonino Virdia, Giovanna De Luca, Giovanni Di Stazio, Vincenzo Politi
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Patent number: 4619916Abstract: Thirteen new tripeptides made from levorotatory amino acids are described, corresponding to the formulap--GLU--X--TRPX is a specific amino acid different from p-GLU and TRP, as well as a process for the preparation of these compounds, pharmaceutical formulations containing them and the use of these formulations as hypotensive and analgesic agents.Type: GrantFiled: December 7, 1984Date of Patent: October 28, 1986Assignee: Polifarma S.p.A.Inventors: Giovanni Di Stazio, Vincenzo Politi, Andrea Margonelli, Giovanna De Luca, Mario Materazzi
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Patent number: 4551471Abstract: The process for the biosynthesis of 3-indolpyruvic acid involves the reaction of tryptophan with purified enzyme aspartate aminotransferase obtained from the mytochondria of slaughterhouse animals. When administered orally in rats, 3-indolpyruvic acid leads to a considerable increase in cerebral serotonin levels, and so may be used in all the pathological conditions of the central nervous system involving deficiencies of this neurotransmitter, such as depressions, insomnia, lack of appetite, neuroendocrin imbalances, etc.Type: GrantFiled: October 7, 1983Date of Patent: November 5, 1985Assignee: Polifarma S.p.A.Inventors: Giovanna De Luca, Giovanni Di Stazio, Vincenzo Politi, Mario Materazzi