Patents by Inventor Adriano Malabarba

Adriano Malabarba 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).

  • Patent number: 5644025
    Abstract: Tetrapeptides of general formula (I) deriving from dalbaheptide antibiotics ##STR1## wherein: W and Z represent the relative portions of the aglycon of an antibiotic of the dalbaheptide group (aglucodalbaheptides);Y represents a carboxylic group or a functional derivative of said carboxylic group;R and R.sub.0 each independently represent amino or a protected amino group;R.sub.1 represents hydrogen or a protecting group of the carboxylic function;and its salts with acids and bases as well as its inner salts.A process for producing the tetrapeptides of formula (I) from the corresponding dalbaheptides and aglucodalbaheptides.
    Type: Grant
    Filed: February 17, 1995
    Date of Patent: July 1, 1997
    Assignee: Gruppo Lepetit SPA
    Inventors: Adriano Malabarba, Romeo Ciabatti
  • Patent number: 5602229
    Abstract: 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: Grant
    Filed: May 15, 1995
    Date of Patent: February 11, 1997
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Adriano Malabarba, Romeo Ciabatti, J urgen K. Kettenring
  • Patent number: 5521155
    Abstract: 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: Grant
    Filed: February 14, 1995
    Date of Patent: May 28, 1996
    Assignee: Gruppo Lepetit S.p.A
    Inventors: Adriano Malabarba, Giorgio Tarzia
  • Patent number: 5500410
    Abstract: The present invention is directed to new C.sup.63 amide derivatives of teicoplanin wherein the amide moiety is derived from a di- or poly-alkylamine, and to a process for preparing them. The derivatives are prepared by reacting a teicoplanin-like product with an active ester forming reagent such as chloroacetonitrile and then contacting said active ester with the appropriate di- or poly-alkylamine. The amide derivatives of the invention are active against gram positive and gram negative bacteria.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: March 19, 1996
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Adriano Malabarba, Pierfausto Seneci, Jurgen K. Kettenring, Romeo Ciabatti
  • Patent number: 5438117
    Abstract: Hexapeptides of formula (I) deriving from aglucoteicoplanin and their salts with acids and bases as well as their inner salts wherein R is hydrogen or a protecting ##STR1## group of the amino function. The products of formula (I), wherein R is hydrogen, possess antimicrobial activity in particular against coagulase-negative strains and some S. aureus and S. epidermidis strains which have low sensitivity toward teicoplanin. The hexapeptides are produced by reductive cleavage of aglucoteicoplanin with alkali metal borohydrides in the presence of a hydroalcoholic mixture as solvent.
    Type: Grant
    Filed: June 23, 1994
    Date of Patent: August 1, 1995
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Adriano Malabarba, Romeo Ciabatti
  • Patent number: 5198418
    Abstract: The present invention is directed to teicoplanin derivatives in which position 63 of the glycopeptide core is substituted with a substituted alkylamide.
    Type: Grant
    Filed: January 21, 1992
    Date of Patent: March 30, 1993
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Adriano Malabarba, Giorgio Tarzia
  • Patent number: 5194424
    Abstract: C.sup.63 -Amide derivatives of 34-de(acetylglucosaminyl)-34-deoxy-teicoplanin wherein the amide moiety is derived from a di- or poly-amine. The derivatives are prepared by reacting 34-de(acetylglucosaminyl)- 34-deoxy-teicoplanins with an active esters forming reagent such as chloroacetonitrile and then contacting the resulting active esters with the appropriate di- or poly-amine. The amide derivatives which are active against Gram-positive microorganisms, in particular against Group A Streptococci were found to be active also against bacteria which are resistant to glycopeptide antibiotics.
    Type: Grant
    Filed: May 20, 1992
    Date of Patent: March 16, 1993
    Assignee: Gruppo Lepetit SpA
    Inventors: Adriano Malabarba, Jurgen K. Kettenring
  • Patent number: 5164484
    Abstract: The present invention is directed to new de-(acetylglucosaminyl)-di(dehydro)deoxy teicoplanin derivatives which possess antibiotic activity mainly against gram positive bacteria.The new compounds are obtained by chemical modification of a teicoplanin antibiotic substance.
    Type: Grant
    Filed: October 21, 1991
    Date of Patent: November 17, 1992
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Adriano Malabarba, Pietro Ferrari, Aldo Trani, Giorgio Tarzia
  • Patent number: 5132286
    Abstract: The present invention is directed to the essentially pure preparation of an antibiotic substance arbitrarily designated antibiotic L 17054. This antibiotic substance is obtained from the known antibiotic substance named teicoplanin (formerly teichomycin) by chemical treatment. The new compound and the pharmaceutically acceptable salts possess antimicrobial activity.
    Type: Grant
    Filed: May 17, 1991
    Date of Patent: July 21, 1992
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Adriano Malabarba, Angelo Borghi, Paolo Strazzolini, Bruno Cavalleri, Carolina Coronelli
  • Patent number: 5041534
    Abstract: The present invention is directed to the essentially pure preparation of an antibiotic substance arbitrarily designated antibiotic L 17054. This antibiotic substance is obtained from the known antibiotic substance named teicoplanin (formerly teichomycin) by chemical treatment. The new compound and the pharmaceutically acceptable salts possess antimicrobial activity.
    Type: Grant
    Filed: November 10, 1986
    Date of Patent: August 20, 1991
    Assignee: Merrell Dow Pharmaceuticals
    Inventors: Adriano Malabarba, Paolo Strazzolini, angelo Borghi, Bruno Cavalleri, Carolina Coronelli
  • Patent number: 4954483
    Abstract: The present invention is directed to carboxylic acid esters of deglucoteicoplanin, i.e. of the aglycon moiety of the antibiotic teicoplanin. The compounds of the invention are conveniently prepared either by deglucoteicoplanin or by any of the glycopeptides of the teicoplanin group, such as teicoplanin itself, one of its components, antibiotic L 17054 and antibiotic L 17046.
    Type: Grant
    Filed: September 8, 1988
    Date of Patent: September 4, 1990
    Assignee: Gruppo Lepetit, S.p.A.
    Inventors: Adriano Malabarba, Paolo Strazzolini, Aldo Trani, Ambrogio Magni, Bruno Cavalleri
  • Patent number: 4914187
    Abstract: The present invention is directed to ester derivatives at the carboxylic function of the glycopeptidic antibiotic substance called antibiotic L 17046 with antimicrobial activity mainly against gram-positive bacteria.
    Type: Grant
    Filed: June 23, 1989
    Date of Patent: April 3, 1990
    Assignee: Gruppo Lepetit S.p.A
    Inventors: Adriano Malabarba, Paolo Strazzolini, Ambrogio Magni, Bruno Cavalleri, Aldo Trani
  • Patent number: 4882419
    Abstract: Process for preparing antibiotic L, 17392 by catalytically hydrogenating a deglucoteicoplanin ester of formula ##STR1## wherein A, B and Z represent hydrogen atoms, R represents benzyl or substituted benzyl, wherein the phenyl group is substituted with at least a substituent selected from chloro, bromo, fluoro, nitro, (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy and the like, with the exclusion of the tri-nitro phenyl group, or acid addition salts thereof, to catalytic hydrogenolysis in the presence of a poisoned hydrogenation catalyst at a temperature from 10.degree. C. to 40.degree. C. and a pressure between ambient pressure and 5 atm, in an inert organic solvent preferably in the presence of a mineral acid.
    Type: Grant
    Filed: February 6, 1986
    Date of Patent: November 21, 1989
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Adriano Malabarba, Paolo Strazzolini, Bruno Cavalleri
  • Patent number: 4789661
    Abstract: The present invention is directed to new de-(acetylglucosaminyl-di(dehydro)deoxy teicoplanin derivatives which possess antibiotic activity mainly against gram positive bacteria.The new compounds are obtained by chemical modification of a teicoplanin antibiotic substance.
    Type: Grant
    Filed: July 17, 1987
    Date of Patent: December 6, 1988
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Adriano Malabarba, Aldo Trani, Pietro Ferrari, Giorgio Tarzia
  • Patent number: 4699977
    Abstract: The present invention is directed to a new antibiotic substance arbitrarily denominated antibiotic L 17046. This antibiotic substance is obtained from the known antibiotic substance called teicoplanin (formerly teichomycin) by chemical treatment. The new compound possesses antimicrobial activity expecially against gram-positive bacteria.
    Type: Grant
    Filed: November 10, 1986
    Date of Patent: October 13, 1987
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Adriano Malabarba, Angelo Borghi, Paolo Strazzolini, Bruno Cavalleri, Carolina Coronelli
  • Patent number: 4698418
    Abstract: This invention relates to a process for converting a teicoplanin-like compound into antibiotic L 17046 characterized in that a teicoplanin-like compound selected from teicoplanin complex, any further purified preparation thereof, teicoplanin factor A.sub.2, teicoplanin factor A.sub.3, each of the main components of teicoplanin factor A.sub.2, antibiotic L 17054 and a mixture of two or more of the above substances in any proportion is submitted to hydrolysis with a strong acid in the presence of a polar aprotic organic solvent selected from ethers, ketones and mixtures thereof that a room temperature are liquid.
    Type: Grant
    Filed: September 20, 1985
    Date of Patent: October 6, 1987
    Assignee: Gruppo Lepetit, S.p.A.
    Inventors: Adriano Malabarba, Bruno Cavalleri
  • Patent number: 4684644
    Abstract: The present invention is directed to a class of basic monocarboxyamide derivatives of actagardine. Actagardine (INN) is an antibiotic substance produced by actinoplanes strains such as Actinoplanes Sp. ATCC 31048 and Actinoplanes Sp. ATCC 31049 which are described in U.S. Pat. No. 4,022,884. Actagardine shows antimicrobial in vitro and in vivo activity against gram-positive organisms. Its complete chemical structure is not yet known but there is only information on its chemical functions and main fragments. In particular, it has been found that actagardine has two carboxylic functions and a primary amino function and can therefore be represented as follows: ##STR1## The compounds of the invention are monoamide derivatives at one of the carboxy functions of actagardine.
    Type: Grant
    Filed: March 21, 1986
    Date of Patent: August 4, 1987
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Adriano Malabarba, Bruno Cavalleri
  • Patent number: 4661470
    Abstract: The present invention is directed to ester derivatives at the carboxylic function of the glycopeptidic antibiotic substance called antibiotic L 17046 with antimicrobial activity mainly against gram-positive bacteria.
    Type: Grant
    Filed: November 12, 1985
    Date of Patent: April 28, 1987
    Assignee: Gruppo Lepetit S.P.A.
    Inventors: Adriano Malabarba, Ambrogio Magni, Paolo Strazzolini, Bruno Cavalleri, Aldo Trani
  • Patent number: 4650855
    Abstract: The present invention is directed to a new antibiotic substance arbitrarily denominated antibiotic L 17046. This antibiotic substance is obtained from the known antibiotic substance called teicoplanin (formerly teichomycin) by chemical treatment. The new compound possesses antimicrobial activity especially against gram-positive bacteria.
    Type: Grant
    Filed: March 19, 1984
    Date of Patent: March 17, 1987
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Adriano Malabarba, Paolo Strazzolini, Angelo Borghi, Bruno Cavalleri, Carolina Coronelli
  • Patent number: 4645827
    Abstract: The present invention is directed to the essentially pure preparation of an antibiotic substance arbitrarily designated antibiotic L 17054. This antibiotic substance is obtained from the known antibiotic substance named teicoplanin (formerly teichomycin) by chemical treatment. The new compound and the pharmaceutically acceptable salts possess antimicrobial activity.
    Type: Grant
    Filed: March 19, 1984
    Date of Patent: February 24, 1987
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Adriano Malabarba, Paolo Strazzolini, Angelo Borghi, Bruno Cavalleri, Carolina Coronelli