Patents Assigned to Gruppo Lepetit S.p.A.
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Patent number: 6573366Abstract: A process for purifying human Interleukin-1 receptor antagonist (IL-1ra), obtained by fermenting a strain of recombinant E. coli, which comprises: a) loading the mixture to be purified, which has been buffered at a pH value lower than 6.2 and optionally diluted to reduce its ionic strength at a low value, onto a cationic exchange matrix and eluting said matrix with an aqueous buffered solution having a pH value from about 7.5 to 9.0 and a low ionic strength; and b) applying the eluate from the cationic exchange step, containing the desired IL-1ra protein, directly onto an anionic exchange matrix and eluting with an aqueous buffered solution having a pH value within the above range 7.5 to 9.0 and an increased ionic strength.Type: GrantFiled: May 9, 2000Date of Patent: June 3, 2003Assignee: Gruppo Lepetit S.p.A.Inventors: Dino Zanette, Edoardo Giacomo Sarubbi, Adolfo Soffientini
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Patent number: 6228851Abstract: Process for preparing the compound 11&bgr;-21-dihydroxy-2′-methyl-5′&bgr;H-pregna-1,4-dieno[17,16-d]oxazoline-3,20-dione of formula (I): which comprises adsorbing said compound, contained into an aqueous solution resulting from fermentation broths or process streams, on an adsorbent polymeric resin having a styrenic or acrylic matrix and subsequently desorbing the said compound by eluting the resin with suitable mixture of water with a water-miscible organic solvent.Type: GrantFiled: August 7, 1998Date of Patent: May 8, 2001Assignee: Gruppo Lepetit S.p.A.Inventor: Luigi Forte
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Patent number: 6159746Abstract: Solid phase immunoassay for detecting specific inhibitors of proteolytic enzymes in biological fluids, which comprises: a) contacting a tubulin peptide covalently linked to a support with a solution containing a proteolytic activity together with a protease inhibitor, b) detecting the inhibitor activity against the selected proteases by contacting the support with a solution containing a labelled monoclonal antibody which specifically recognises the free end of the tubulin peptide linked to the support.Type: GrantFiled: September 23, 1996Date of Patent: December 12, 2000Assignee: Gruppo Lepetit S.p.A.Inventors: Khalid Islam, Lucia Carrano, Maurizio Denaro
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Patent number: 6133254Abstract: Use of a compound of formula (I) wherein R represents hydrogen or chlorine, for preparing an immunosuppressive medicament.Type: GrantFiled: October 26, 1998Date of Patent: October 17, 2000Assignee: Gruppo Lepetit, S.p.A.Inventor: Khalid Islam
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Patent number: 6103895Abstract: A process for preparing the compound (11.beta.,16.beta.)-21-(acetyloxy)-11-hydroxy-2'-methyl-5'H-pregna-1,4-die no[17,16-d]oxazole-3,20-dione (INN deflazacort) which comprises reacting (11.beta.,16.beta.)-11,21 -dihydroxy-2'-methyl-5'H-pregna-1,4-dieno[17,16-d]oxazole-3,20-dione with acetic anhydride in a suitable organic solvent in the presence of a basic catalyst and water.Type: GrantFiled: June 5, 1998Date of Patent: August 15, 2000Assignee: Gruppo Lepetit S.p.A.Inventors: Luigi Forte, Calogero Cancellieri
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Patent number: 6040297Abstract: 5,5'-Pyrophosphates of non-naturally occurring nucleosides selected from 1-(1-thyminyl)-3-azido-2, 3-dideoxy-D-riboside, 1(5-fluoro-1-uracilyl)-2, 3-dideoxy-D-riboside, 1-(1-uracilyl)-3-azido-2, 3-dideoxy-D-riboside, 1-(9-guaninyl)-2, 3-dideoxy-D-riboside, 1-(9-hypoxanthinyl)-2, 3-dideoxy-D-riboside, 1-(1-cytosinyl)-2, 3-dideoxy-D-riboside, and 1-(9-adeninyl)-2, 3-dideoxy-D-riboside, are described as well as their manufacture and use as therapeutic agents against tumors and retroviral infections including HIV infections. The compounds may be administered as the active ingredients of pharmaceutical compositions or as prodrugs encapsulated within biological carriers, e.g. transformed erythrocytes, for targeting to specific cell populations responsible for the development of the noted pathological disorders.Type: GrantFiled: January 14, 1997Date of Patent: March 21, 2000Assignees: Biosearch Italia, S.p.A., Gruppo Lepetit, S.p.A.Inventors: Antonio De Flora, Umberto Benatti, Marco Giovine
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Patent number: 5882900Abstract: A method for increasing both total antibiotic yield the selective production of factor A of the GE 2270 antibiotics consisting in the addition of vitamin B.sub.12 or its analogs having vitamin B.sub.12 --like activity to the fermentation media of Planobispora rosea ATCC 53773 or any antibiotic GE 2270 producing mutant or variant thereof.Type: GrantFiled: September 30, 1997Date of Patent: March 16, 1999Assignee: Gruppo Lepetit S.p.A.Inventors: Angelo Michele Rizzo, Luciano Gastaldo
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Patent number: 5869449Abstract: The present invention is directed to novel 38-decarboxy-38-hydroxymethyl derivatives of teicoplanin antiobiotics and a process for preparing them which includes submitted the corresponding lower alkyl ester precursor to a reduction reaction in the presence of an alkali metal borohydride. The compounds of the invention show an improved antibacterial activity against some clinical isolates of Staphylococci somewhat resistant to teicoplanin.The teicoplanin derivatives of the present invention are represented by the following formula: ##STR1## wherein: X represents hydroxymethyl;R represents hydrogen or --N?(C.sub.9 -C.sub.12)aliphatic acyl!-.beta.-D-2-deoxy-2-aminoglucopyranosyl;R.sub.1 represents hydrogen or N-acetyl-.beta.-D-2-deoxy-2-aminoglucopyranosyl;R.sub.2 represents hydrogen of alpha-D-mannopyranosyl;R.sub.3 represents hydrogen or a protecting group of the amino function; and the acid addition salts thereof; with the proviso that R.sub.1 represents hydrogen only when R and R.sub.Type: GrantFiled: June 10, 1997Date of Patent: February 9, 1999Assignee: Gruppo Lepetit S.P.A.Inventors: Adriano Malabarba, Romeo Ciabatti
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Patent number: 5854036Abstract: The present invention concerns novel compounds obtained by fermenting a microorganism of the genus Memnonoiella or Stachybotrys, which compounds are inhibitors of the enzyme inositol monophosphatase (EC 3.1.3.25). The present invention also relates to the use of these novel compounds in treating manic depression and pharmaceutical formulations comprising said compounds as active ingredient; a further object is the use of these compounds in an analytical method for detecting inositol monophosphatase.Type: GrantFiled: September 10, 1996Date of Patent: December 29, 1998Assignee: Gruppo Lepetit S.p.A.Inventors: Stefania Stefanelli, Federica Sponga, Khalid Islam, Maurizio Denaro, Pietro Ferrari
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Patent number: 5843890Abstract: The present invention is directed to new antibiotic substances denominated antibiotic GE 2270 factors B.sub.1, B.sub.2, C.sub.1, C.sub.2, D.sub.1, D.sub.2, E and T, the addition salts thereof, the pharmaceutical compositions thereof and their use as medicaments, particularly in the treatment of infectious diseases involving microorganisms susceptible to them and their use as animal growth promoters.Type: GrantFiled: June 5, 1995Date of Patent: December 1, 1998Assignee: Gruppo Lepetit S.p.A.Inventors: Enrico Selva, Paolo Tavecchia, Ermenegildo Restelli, Pietro Ferrari, Maurizio Denaro
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Patent number: 5786350Abstract: Rifamycin antibiotic derivatives of formulae (I) and (Ia) bearing at the position 36 a substituent selected from (C.sub.1 -C.sub.8)alkyl, halo, hydroxy, (C.sub.1 -C.sub.4)acyloxy, (C.sub.1-C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkylamino, di(C.sub.1-C.sub.4)alkylamino and substituted 4-oxo-3-pyridinyl carbonyloxy of formula (1) obtained by reacting rifamycin with suitably substituted malonic acid. The compounds of the invention are antimicrobial agents mainly active against gram positive bacteria and fastidious gram negative bacteria showing the considerable antimicrobial activity against the rifamypicin resistant microbial strains.Type: GrantFiled: January 31, 1997Date of Patent: July 28, 1998Assignee: Gruppo Lepetit S.p.A.Inventors: Emilio Occelli, Sergio Lociuro, Romeo Ciabatti, Maurizio Denaro
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Patent number: 5752941Abstract: The invention relates to central venous polyurethane catheters with a thin hydrophilic coating loaded with an antibiotic of the ramoplanin group or any mixture thereof and their use in preventing catheter related infections. These catheters are useful to prevent bacterial adherence and colonization and, therefore, to lower the risk of vascular infections in catheterized patients. The method of preparing the catheter of the invention consists in incubating polyurethane catheters coated with a hydrophilic film in an aqueous solution of the selected antibiotic.Type: GrantFiled: August 2, 1996Date of Patent: May 19, 1998Assignee: Gruppo Lepetit S.p.A.Inventors: Gabriella Romano', Beth P. Goldstein, Rosamund Jean Williams, Maurizio Denaro
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Patent number: 5750509Abstract: The present invention is directed to novel antibiotic A 40926 derivatives characterized by having a carboxy, (C.sub.1 -C.sub.4) alkoxy-carbonyl, aminocarbonyl, (C.sub.1 -C.sub.4) alkylaminocarbonyl, di (C.sub.4 -C.sub.4)alkylaminocarbonyl or hydroxymethyl substituent on the N-acylaminoglucuronyl moiety and a hydroxy or a polyamine substituent in position 63 of the molecule. The compounds of the invention show high in vitro activity against glycopeptide resistant Enterococci and Staphylococci.Type: GrantFiled: April 30, 1996Date of Patent: May 12, 1998Assignee: Gruppo Lepetit S.p.A.Inventors: Adriano Malabarba, Romeo Ciabatti, Gianbattista Panzone, Alessandra Maria Marazzi
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Patent number: 5747295Abstract: The present invention is directed to new antibiotic substances denominated antibiotic GE 2270 factors B.sub.1, B.sub.2, C.sub.1, C.sub.2, D.sub.1, D.sub.2, E and T, the addition salts thereof, the pharmaceutical compositions thereof and their use as medicaments, particularly in the treatment of infectious diseases involving microorganisms susceptible to them and their use as animal growth promoters.Type: GrantFiled: June 2, 1995Date of Patent: May 5, 1998Assignee: Gruppo Lepetit S.p.A.Inventors: Enrico Selva, Paolo Tavecchia, Ermenegildo Restelli, Pietro Ferrari, Maurizio Denaro
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Patent number: 5648456Abstract: Pentapeptide antibiotics of the formula ##STR1## wherein W, Z, X.sub.1, X.sub.2 and T represent the relative portions of an antibiotic of the dalbaheptide group (glyccpeptide antibiotics), Y represents a carboxyacid group, a functional derivative of said carboxyacid group or a hydroxymethyl group. The invention includes the salts of the above represented pentapeptide antibiotics with acids or bases as well as their inner salts.The compounds are obtained by reductive cleavage of the peptidic bond between the second and the third aminoacid of the seven aminoacid chain of dalbaheptides (glycopeptide antibiotics). The inventions concerns also the reductive cleavage process which implies using an alkali metal borohydride as the reagent. The compounds show antibacterial activity against staphylococcal and streptococcal strains.Type: GrantFiled: May 31, 1995Date of Patent: July 15, 1997Assignee: Gruppo Lepetit S.p.A.Inventors: Adriano Malabarba, Romeo Ciabatti, Jurgen Kurt Kettenring
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Patent number: 5610143Abstract: The present invention is directed to new antibiotic substances denominated antibiotics GE 37468 A, B and C, their addition salts with bases, the pharmaceutical compositions thereof and their use as medicaments, particularly in the treatment of infectious diseases involving microorganisms susceptible to them.The compounds of the invention are also active as growth promotant agents in animals, such as poultry, swine, ruminants, etc.Type: GrantFiled: June 21, 1995Date of Patent: March 11, 1997Assignee: Gruppo Lepetit S.p.A.Inventors: Sergio Stella, Nicoletta Montanini, Francis J. LeMonnier, Luigi Colombo, Enrico Selva, Maurizio Denaro
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Patent number: 5602229Abstract: Pentapeptide antibiotics of the formula ##STR1## wherein W, Z, X.sub.1, X.sub.2 and T represent the relative portions of an antibiotic of the dalbaheptide group (glycopeptide antibiotics), Y represents a carboxyacid group, a functional derivative of a carboxyacid group or a hydroxymethyl group. The invention includes the salts of the above represented pentapeptide antibiotics with acids or bases as well as their inner salts.Type: GrantFiled: May 15, 1995Date of Patent: February 11, 1997Assignee: Gruppo Lepetit S.p.A.Inventors: Adriano Malabarba, Romeo Ciabatti, J urgen K. Kettenring
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Patent number: 5594102Abstract: The present invention is directed to a chemical process for preparing antibiotic L 17392 (deglucoteicoplanin) and its salts with bases and acids by submitting a teicoplanin compound or a teicoplanin-like compound to controlled strong acid hydrolysis in the presence of an organic aprotic solvent, and a purification thereof.Type: GrantFiled: May 30, 1995Date of Patent: January 14, 1997Assignee: Gruppo Lepetit S.p.AInventors: Giambattista Panzone, Anacleto Gianantonio
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Patent number: 5567676Abstract: The present invention concerns new antiobiotic substances demoninated de-acyl antibiotics A40926, de-acyl antibiotic A 40926P and antibiotic A 40926 amino glucronyl aglycon, and the use of these substances in the treatment of infectious diseases involving microorganisms susceptible to it.Type: GrantFiled: June 1, 1995Date of Patent: October 22, 1996Assignee: Gruppo Lepetit S.p.AInventors: Enrico Selva, Grazia Beretta, Angelo Borghi, Maurizio Denaro
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Patent number: 5521155Abstract: The present invention is directed to an amide derivative of the glycopeptide, teicoplanin. This compound is an antibiotic that is active against gram positive bacteria. This compound is produced by subjecting teicoplanin to an amidation reaction.Type: GrantFiled: February 14, 1995Date of Patent: May 28, 1996Assignee: Gruppo Lepetit S.p.AInventors: Adriano Malabarba, Giorgio Tarzia