Patents by Inventor Mario Grugni

Mario Grugni 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: 8426625
    Abstract: A compound of general formula (I): in which: R is selected from the group consisting of (C1-C25)alkyl, (C2-C25)alkenyl, aryl, (C7-C10)aralkyl; n and m are each independently an integer of two to eight; p is one or two; A is selected from the group consisting of —B—, —B—(CH2)r—B—, —B—(CH2)r—B—(CH2)z—B—, wherein r and z are an integer from 2 to 8, B is a —NR1— or —N(R2)2+1/pQ?p group, in which R1 is selected from hydrogen, (C1-C4)alkyl, (C1-C4)acyl, tert-butoxycarbonyl, and R2 is selected from hydrogen and (C1-C4)alkyl; Q?p is an anion selected from chloride, bromide, iodide, nitrate, sulphate, hydrogen sulphate, perchlorate, R3COO? wherein R3 has the same meanings as R, independently from one another and R4—O—SO3? wherein R4 is (C2-C14)alkyl with the proviso that, when Q?p is selected from chloride, bromide, iodide, nitrate, sulphate, hydrogen sulphate, perchlorate, R is not (C1-C4)alkyl.
    Type: Grant
    Filed: December 21, 2006
    Date of Patent: April 23, 2013
    Assignee: Cell Therapeutics, Inc.
    Inventors: Alberto Bernareggi, Mario Grugni, Giulio Mariotti, Ernesto Menta, Gianluca Pardi, Paolo Pavesi, Gabriella Pezzoni, Paolo Nicoli, Sergio De Munari
  • Publication number: 20130018096
    Abstract: The present invention relates to the antitumor compound of formula (I) a process for its preparation and pharmaceutical compositions containing it.
    Type: Application
    Filed: September 16, 2009
    Publication date: January 17, 2013
    Inventors: Sergio De Munari, Stefano Di Giovine, Mario Grugni, Paola Nicoli, Alessandro Paganelli, Gianluca Pardi, Gabriella Pezzoni
  • Patent number: 8329853
    Abstract: The invention relates to an improved process for the preparation of poly-?-glutamic acids which comprises the polymerization of tertiary ?-esters of ?-glutamic acid N-carboxy anhydride with appropriate solvents and initiators, followed by acid hydrolysis of the resulting poly-?-glutamic acid-?-ester. The process is particularly advantageous in that it allows one to carefully control the molecular weight of the resulting poly-?-glutamic acid. The invention also relates to poly-?-glutamic acids capped at the amino terminus with carboxylic acids or amino acids and to a process for the preparation thereof.
    Type: Grant
    Filed: December 10, 2010
    Date of Patent: December 11, 2012
    Assignee: Cell Therapeutics, Inc.
    Inventors: Marc McKennon, Giovanni Da Re, Luca Feliciotti, Marco Artico, Gianluca Pardi, Mario Grugni
  • Publication number: 20110196123
    Abstract: The invention relates to an improved process for the preparation of poly-?-glutamic acids which comprises the polymerization of tertiary ?-esters of ?-glutamic acid N-carboxy anhydride with appropriate solvents and initiators, followed by acid hydrolysis of the resulting poly-?-glutamic acid-?-ester. The process is particularly advantageous in that it allows one to carefully control the molecular weight of the resulting poly-?-glutamic acid. The invention also relates to poly-?-glutamic acids capped at the amino terminus with carboxylic acids or amino acids and to a process for the preparation thereof.
    Type: Application
    Filed: December 10, 2010
    Publication date: August 11, 2011
    Applicant: Cell Therapeutics, Inc.
    Inventors: Marc McKENNON, Giovanni Da Re, Luca Feliciotti, Marco Artico, Gianluca Pardi, Mario Grugni
  • Publication number: 20100292322
    Abstract: A compound of general formula (I): in which: R is selected from the group consisting of (C1-C25)alkyl, (C2-C25)alkenyl, aryl, (C7-C10)aralkyl; n and m are each independently an integer of two to eight; p is one or two; A is selected from the group consisting of —B—, —B—(CH2)r—B—, —B—(CH2)r—B—(CH2)z—B—, wherein r and z are an integer from 2 to 8, B is a —NR1— or —N(R2)2+ 1/pQ?p group, in which R1 is selected from hydrogen, (C1-C4)alkyl, (C1-C4)acyl, tert-butoxycarbonyl, and R2 is selected from hydrogen and (C1-C4)alkyl; Q?p is an anion selected from chloride, bromide, iodide, nitrate, sulphate, hydrogen sulphate, perchlorate, R3COO? wherein R3 has the same meanings as R, independently from one another and R4—O—SO3? wherein R4 is (C2-C14)alkyl with the proviso that, when Q?p is selected from chloride, bromide, iodide, nitrate, sulphate, hydrogen sulphate, perchlorate, R is not (C1-C4)alkyl.
    Type: Application
    Filed: December 21, 2006
    Publication date: November 18, 2010
    Inventors: Alberto Bernareggi, Mario Grugni, Giulio Mariotti, Ernesto Menta, Gianluca Pardi, Paolo Pavesi, Gabriella Pezzoni, Paolo Nicoli, Sergio De Munari
  • Publication number: 20090036441
    Abstract: 3H-Benzo[e]indol-4,5-dione derivatives with antitumor activity, the processes for the preparation thereof and pharmaceutical compositions containing them.
    Type: Application
    Filed: December 22, 2005
    Publication date: February 5, 2009
    Applicant: Cell Therapeutics Europe S.R.L.
    Inventors: Mario Grugni, Mara Cassin, Gennaro Colella, Sergio De Munari, Gianluca Pardi, Paolo Pavesi
  • Patent number: 7482458
    Abstract: NK3 receptor antagonists of formula (I): are useful in treating inter alia pulmonary disorders, CNS disorders and neurodegenerative disorders.
    Type: Grant
    Filed: March 21, 2006
    Date of Patent: January 27, 2009
    Assignee: SmithKline Beecham Farmaceutica S.p.A.
    Inventors: Carlo Farina, Giuseppe Arnaldo Maria Giardina, Mario Grugni, Luca Francesco Raveglia
  • Publication number: 20080261980
    Abstract: The invention relates to the use of compounds of general formula (I), in which R1, R2 and X are as defined in the description for the preparation of pharmaceutical compositions for the treatment of pathologies in which inhibition of the interaction between HIF-1? and p300 is beneficial, in particular as antiangiogenic medicaments for the therapy of solid tumors.
    Type: Application
    Filed: December 19, 2005
    Publication date: October 23, 2008
    Applicant: Cell Therapeutics, Inc.
    Inventors: Mara Cassin, Gennaro Colella, Sergio De Munari, Mario Grugni
  • Publication number: 20080255099
    Abstract: The invention relates to the use of diketodithiopiperazine antibiotics, in particular chaetocin and gliotoxin, for the preparation of pharmaceutical compositions for antitumor therapy.
    Type: Application
    Filed: December 14, 2005
    Publication date: October 16, 2008
    Applicant: Cell Therapeutics, Inc.
    Inventors: Sergio De Munari, Mario Grugni, Ernesto Menta, Mara Cassin, Gennaro Colella
  • Publication number: 20080051603
    Abstract: The invention relates to an improved process for the preparation of poly-?-glutamic acids which comprises the polymerization of tertiary ?-esters of ?-glutamic acid N-carboxy anhydride with appropriate solvents and initiators, followed by acid hydrolysis of the resulting poly-?-glutamic acid-?-ester. The process is particularly advantageous in that it allows one to carefully control the molecular weight of the resulting poly-?-glutamic acid. The invention also relates to poly-?-glutamic acids capped at the amino terminus with carboxylic acids or amino acids and to a process for the preparation thereof.
    Type: Application
    Filed: June 12, 2007
    Publication date: February 28, 2008
    Applicants: Cell Therapeutics, Inc., Cell Therapeutics Europe S.R.L.
    Inventors: Marc McKennon, Giovanni Da Re, Luca Feliciotti, Marco Artico, Gianluca Pardi, Mario Grugni
  • Publication number: 20070197546
    Abstract: A compound, or a solvate or a salt thereof, of formula (I): wherein, Ar is an optionally substituted aryl or a C5-7 cycloalkdienyl group, or a C5-7 cycloalkyl group or an optionally substituted single or fused ring aromatic heterocyclic group,; R is C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, optionally substituted phenyl or phenyl C1-6 alkyl, an optionally substituted five-membered heteroaromatic ring comprising up to four heteroatoms selected from O and N, hydroxy C1-6 alkyl, amino C1-6 alkyl, C1-6 alkylaminoalkyl, di C1-6 alkylaminoalkyl, C1-6 acylaminoalkyl, C1-6 alkoxyalkyl, C1-6 alkylcarbonyl, carboxy, C1-6 alkoxycarbonyl, C1-6 alkoxycarbonyl C1-6 alkyl, aminocarbonyl, C1-6 alkylaminocarbonyl, di C1-6 alkylaminocarbonyl, halogeno C1-6 alkyl; or R is a group —(CH2)p— wherein p is 2 or 3 which group forms a ring with a carbon atom of Ar; R1 represents hydrogen or up to four optional substituents selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halog
    Type: Application
    Filed: March 27, 2007
    Publication date: August 23, 2007
    Inventors: Giuseppe Giardina, Mario Grugni, Davide Graziani, Luca Raveglia
  • Publication number: 20070015766
    Abstract: Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: wherein: R1 is H or alkyl; R2 is aryl, cycloalkyl or heteroaryl; R3 is H or C1-3 alkyl, optionally substituted by one or more fluorines; R4 is H, R8NR9R10, R11R13 or R11R12R13; or R5 is branched or linear alkyl, cycloalkyl, aryl, arylalkyl, or a single or fused ring aromatic heterocyclic group; a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and the use of such compounds and composition in medicine.
    Type: Application
    Filed: June 26, 2006
    Publication date: January 18, 2007
    Inventors: Carlo Farina, Stefania Gagliardi, Giuseppe Giardina, Mario Grugni, Marisa Martinelli, Guy Marguerite Marie Gerard Nadler
  • Publication number: 20060235026
    Abstract: Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: wherein: R1 is H or C1-6 alkyl; R2 is aryl or C3-7 cycloalkyl or heteroaryl; R3 is H or C1-3 alkyl, optionally substituted by one or more fluorines; R4 is R8R9; R8 is a single bond, C1-6 alkyl, or aryl; R9 is H, COO R10, or NR11R12; R10 is H or C1-6 alkyl; R11 and R12 are independently selected from H and C1-6 alkyl; R5 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, aryl, or a single or fused ring aromatic heterocyclic group; R6 represents H or up to three substituents independently selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, amino or mono- or di-C1-6 alkylamino; R7 is H or halo; a is 1-6; and any of R2, R5, R8, R10, R11 and R12 may optionally be substituted one or more times by halo, hydroxy, amino, cyano, nitro, carboxy
    Type: Application
    Filed: June 21, 2006
    Publication date: October 19, 2006
    Inventors: Carlo Farina, Giuseppe Giardina, Mario Grugni, Guy Gerard Nadler
  • Publication number: 20060223819
    Abstract: Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.
    Type: Application
    Filed: June 21, 2006
    Publication date: October 5, 2006
    Inventors: Carlo Farina, Stefania Gagliardi, Giuseppe Giardina, Mario Grugni, Marisa Martinelli, Guy Marguerite Nadler
  • Patent number: 7115633
    Abstract: Compounds of formula (I) or a derivative thereof, wherein; R is C1-6alkyl, C3-7cycloalkyl, C1-6alkoxy, hydroxy, halo, C1-6alkenyl, C1-6alkynyl, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aminoC1-6alkyl, (C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl; R1 is hydrogen or R; R2 is hydroxy, C1-6alkoxy, amino, C1-6alkylamino, di(C1-6alkyl)amino; R3 is hydrogen or C1-6alkyl; R4 and R5 are each independently selected from the list consisting of perhaloC1-6alkyl, hydrogen, halo, C1-6alkyl, C1-6alkoxy, hydroxy, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aminoC1-6alkyl, (C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl, and COX wherein X may be hydroxy, C1-6alkoxy, C1-6alkyl, amino, C1-6alkylamino, or di(C1-6alkyl)amino; with the proviso that, when R3 is hydrogen, then R4 and R5 are not both hydrogen; and wherein any alkyl group or the alkyl moiety of any group containing such a moiety may be substituted one or more times by
    Type: Grant
    Filed: May 1, 2001
    Date of Patent: October 3, 2006
    Assignee: GlaxoSmithKline S.p.A.
    Inventors: Daniela Barlocco, Giorgio Cignarella, Giuseppe Giardina, Mario Grugni, Silvano Ronzoni
  • Publication number: 20060205735
    Abstract: A compound, or a solvate or a salt thereof, of formula (I): wherein, Ar is an optionally substituted aryl or a C5-7 cycloalkdienyl group, or a C5-7 cycloalkyl group or an optionally substituted single or fused ring aromatic heterocyclic group; R is C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, optionally substituted phenyl or phenyl C1-6 alkyl, an optionally substituted five-membered heteroaromatic ring comprising up to four heteroatoms selected from O and N, hydroxy C1-6 alkyl, amino C1-6 alkyl, C1-6 alkylaminoalkyl, di C1-6 alkylaminoalkyl, C1-6 acylaminoalkyl, C1-6 alkoxyalkyl, C1-6 alkylcarbonyl, carboxy, C1-6 alkoxycarbonyl, C1-6 alkoxycarbonyl C1-6 alkyl, aminocarbonyl, C1-6 alkylaminocarbonyl, di C1-6 alkylaminocarbonyl, halogeno C1-6 alkyl; or R is a group —(CH2)p— wherein p is 2 or 3 which group forms a ring with a carbon atom of Ar; R1 represents hydrogen or up to four optional substituents selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halo
    Type: Application
    Filed: May 4, 2006
    Publication date: September 14, 2006
    Inventors: Giuseppe Maria Glardina, Mario Grugni, Davide Graziani, Luca Raveglia
  • Publication number: 20060160846
    Abstract: NK3 receptor antagonists of formula (I): are useful in treating inter alia pulmonary disorders, CNS disorders and neurodegenerative disorders.
    Type: Application
    Filed: March 21, 2006
    Publication date: July 20, 2006
    Inventors: Carlo Farina, Giuseppe Giardina, Mario Grugni, Luca Raveglia
  • Publication number: 20060161004
    Abstract: Certain compounds of formula (I): or a pharmaceutically acceptable salt or hydrate thereof, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.
    Type: Application
    Filed: January 13, 2006
    Publication date: July 20, 2006
    Inventors: Carlo Farina, Giuseppe Giardina, Mario Grugni, Guy Marguerite Nadler
  • Publication number: 20060122387
    Abstract: The compounds of formula (I) wherein A and R1-R5 are as defined in the description, are inhibitors of Vascular Endothelial Growth Factor and are useful as angiogenesis inhibitors and antiproliferative agents.
    Type: Application
    Filed: June 12, 2003
    Publication date: June 8, 2006
    Inventors: Ernesto Menta, Giovanni Da Re, Mario Grugni
  • Patent number: 6969724
    Abstract: Compounds of formula I, or a salt thereof or a hydrate thereof, as follows: wherein X and Y are selected independently from hydrogen and aryl, which aryl is unsubstituted or substituted one or more times by hydroxy, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aryl, heterocyclyl, amino, C1-6alkylamino, di(C1-6alkyl)amino, arylC1-6alkoxy, C1-6alkyl, C1-6alkoxy or halo, which alkyl or alkoxy groups are unsubstituted or substituted one or more times by halo; m and n are independently 0 to 3, provided that m and n are not both 0; A represents a single bond or is —(CRpa Rpb)p— wherein p is 1-3 and Rpa and Rpb are selected independently from hydrogen, C1-6alkyl, C1-6alkoxy and halo, which alkyl or alkoxy groups are independently substituted one or more times by halo; B represents a C4-8 saturated or unsaturated ring, which ring is unsubstituted or substituted one or more times by C1-6alkyl, C1-6alkoxy, aryl, aryloxy, hydroxy, oxo, halo, amino, C1-6alkylamino, di(C1-6 alkyl)amino, and C1-6alkylamido, which C1-6alkyl
    Type: Grant
    Filed: December 19, 2002
    Date of Patent: November 29, 2005
    Assignee: SmithKline Beecham-SpA
    Inventors: Daniela Barlocco, Giorgio Cignarella, Giuseppe Arnaldo Maria Giardina, Mario Grugni, Silvano Ronzoni