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).
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Patent number: 8426625Abstract: 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: GrantFiled: December 21, 2006Date of Patent: April 23, 2013Assignee: Cell Therapeutics, Inc.Inventors: Alberto Bernareggi, Mario Grugni, Giulio Mariotti, Ernesto Menta, Gianluca Pardi, Paolo Pavesi, Gabriella Pezzoni, Paolo Nicoli, Sergio De Munari
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Publication number: 20130018096Abstract: The present invention relates to the antitumor compound of formula (I) a process for its preparation and pharmaceutical compositions containing it.Type: ApplicationFiled: September 16, 2009Publication date: January 17, 2013Inventors: Sergio De Munari, Stefano Di Giovine, Mario Grugni, Paola Nicoli, Alessandro Paganelli, Gianluca Pardi, Gabriella Pezzoni
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Patent number: 8329853Abstract: 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: GrantFiled: December 10, 2010Date of Patent: December 11, 2012Assignee: Cell Therapeutics, Inc.Inventors: Marc McKennon, Giovanni Da Re, Luca Feliciotti, Marco Artico, Gianluca Pardi, Mario Grugni
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Publication number: 20110196123Abstract: 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: ApplicationFiled: December 10, 2010Publication date: August 11, 2011Applicant: Cell Therapeutics, Inc.Inventors: Marc McKENNON, Giovanni Da Re, Luca Feliciotti, Marco Artico, Gianluca Pardi, Mario Grugni
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Publication number: 20100292322Abstract: 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: ApplicationFiled: December 21, 2006Publication date: November 18, 2010Inventors: Alberto Bernareggi, Mario Grugni, Giulio Mariotti, Ernesto Menta, Gianluca Pardi, Paolo Pavesi, Gabriella Pezzoni, Paolo Nicoli, Sergio De Munari
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Publication number: 20090036441Abstract: 3H-Benzo[e]indol-4,5-dione derivatives with antitumor activity, the processes for the preparation thereof and pharmaceutical compositions containing them.Type: ApplicationFiled: December 22, 2005Publication date: February 5, 2009Applicant: Cell Therapeutics Europe S.R.L.Inventors: Mario Grugni, Mara Cassin, Gennaro Colella, Sergio De Munari, Gianluca Pardi, Paolo Pavesi
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Patent number: 7482458Abstract: NK3 receptor antagonists of formula (I): are useful in treating inter alia pulmonary disorders, CNS disorders and neurodegenerative disorders.Type: GrantFiled: March 21, 2006Date of Patent: January 27, 2009Assignee: SmithKline Beecham Farmaceutica S.p.A.Inventors: Carlo Farina, Giuseppe Arnaldo Maria Giardina, Mario Grugni, Luca Francesco Raveglia
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Publication number: 20080261980Abstract: 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: ApplicationFiled: December 19, 2005Publication date: October 23, 2008Applicant: Cell Therapeutics, Inc.Inventors: Mara Cassin, Gennaro Colella, Sergio De Munari, Mario Grugni
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Publication number: 20080255099Abstract: The invention relates to the use of diketodithiopiperazine antibiotics, in particular chaetocin and gliotoxin, for the preparation of pharmaceutical compositions for antitumor therapy.Type: ApplicationFiled: December 14, 2005Publication date: October 16, 2008Applicant: Cell Therapeutics, Inc.Inventors: Sergio De Munari, Mario Grugni, Ernesto Menta, Mara Cassin, Gennaro Colella
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Publication number: 20080051603Abstract: 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: ApplicationFiled: June 12, 2007Publication date: February 28, 2008Applicants: Cell Therapeutics, Inc., Cell Therapeutics Europe S.R.L.Inventors: Marc McKennon, Giovanni Da Re, Luca Feliciotti, Marco Artico, Gianluca Pardi, Mario Grugni
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Publication number: 20070197546Abstract: 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, halogType: ApplicationFiled: March 27, 2007Publication date: August 23, 2007Inventors: Giuseppe Giardina, Mario Grugni, Davide Graziani, Luca Raveglia
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Publication number: 20070015766Abstract: 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: ApplicationFiled: June 26, 2006Publication date: January 18, 2007Inventors: Carlo Farina, Stefania Gagliardi, Giuseppe Giardina, Mario Grugni, Marisa Martinelli, Guy Marguerite Marie Gerard Nadler
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Publication number: 20060235026Abstract: 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, carboxyType: ApplicationFiled: June 21, 2006Publication date: October 19, 2006Inventors: Carlo Farina, Giuseppe Giardina, Mario Grugni, Guy Gerard Nadler
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Publication number: 20060223819Abstract: 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: ApplicationFiled: June 21, 2006Publication date: October 5, 2006Inventors: Carlo Farina, Stefania Gagliardi, Giuseppe Giardina, Mario Grugni, Marisa Martinelli, Guy Marguerite Nadler
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Patent number: 7115633Abstract: 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 byType: GrantFiled: May 1, 2001Date of Patent: October 3, 2006Assignee: GlaxoSmithKline S.p.A.Inventors: Daniela Barlocco, Giorgio Cignarella, Giuseppe Giardina, Mario Grugni, Silvano Ronzoni
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Publication number: 20060205735Abstract: 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, haloType: ApplicationFiled: May 4, 2006Publication date: September 14, 2006Inventors: Giuseppe Maria Glardina, Mario Grugni, Davide Graziani, Luca Raveglia
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Publication number: 20060160846Abstract: NK3 receptor antagonists of formula (I): are useful in treating inter alia pulmonary disorders, CNS disorders and neurodegenerative disorders.Type: ApplicationFiled: March 21, 2006Publication date: July 20, 2006Inventors: Carlo Farina, Giuseppe Giardina, Mario Grugni, Luca Raveglia
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Publication number: 20060161004Abstract: 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: ApplicationFiled: January 13, 2006Publication date: July 20, 2006Inventors: Carlo Farina, Giuseppe Giardina, Mario Grugni, Guy Marguerite Nadler
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Publication number: 20060122387Abstract: 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: ApplicationFiled: June 12, 2003Publication date: June 8, 2006Inventors: Ernesto Menta, Giovanni Da Re, Mario Grugni
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Patent number: 6969724Abstract: 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 C1-6alkylType: GrantFiled: December 19, 2002Date of Patent: November 29, 2005Assignee: SmithKline Beecham-SpAInventors: Daniela Barlocco, Giorgio Cignarella, Giuseppe Arnaldo Maria Giardina, Mario Grugni, Silvano Ronzoni