Patents by Inventor Ettore Perrone
Ettore Perrone 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: 8114865Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer formula (I).Type: GrantFiled: December 14, 2007Date of Patent: February 14, 2012Assignee: Nerviano Medical Sciences S.R.L.Inventors: Tiziano Bandiera, Andrea Lombardi Borgia, Marcella Nesi, Ettore Perrone, Roberto Bossi, Paolo Polucci
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Publication number: 20110288088Abstract: Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.Type: ApplicationFiled: May 17, 2011Publication date: November 24, 2011Applicant: NERVIANO MEDICAL SCIENCES S.r.I.Inventors: Tiziano BANDIERA, Andrea LOMBARDI BORGIA, Sten Christian ORRENIUS, Ettore PERRONE, Italo BERIA, Daniele FANCELLI, Arturo GALVANI
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Patent number: 7968583Abstract: Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.Type: GrantFiled: December 6, 2006Date of Patent: June 28, 2011Assignee: Nerviano Medical Sciences S.r.l.Inventors: Tiziano Bandiera, Andrea Lombardi Borgia, Sten Christian Orrenius, Ettore Perrone, Italo Beria, Daniele Fancelli, Arturo Galvani
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Publication number: 20100292207Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.Type: ApplicationFiled: July 8, 2008Publication date: November 18, 2010Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
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Publication number: 20100197665Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer formula (I).Type: ApplicationFiled: December 14, 2007Publication date: August 5, 2010Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Tiziano Bandiera, Andrea Lombardi Borgia, Marcella Nesi, Ettore Perrone, Roberto Bossi, Paolo Polucci
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Publication number: 20090163503Abstract: Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.Type: ApplicationFiled: December 6, 2006Publication date: June 25, 2009Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Tiziano Bandiera, Andrea Lombardi Borgia, Sten Christian Orrenius, Ettore Perrone, Italo Beria, Daniele Fancelli, Arturo Galvani
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Publication number: 20090136513Abstract: A compound having formula (I): wherein: R, A, R1 and R2, are as defined in the specification, and pharmaceutical formulas thereof, and methods of use thereof, as Kinase inhibitors.Type: ApplicationFiled: March 2, 2007Publication date: May 28, 2009Applicant: NERVIANO MEDICAL SCIENCES S.R.LInventors: Tiziano Bandiera, Jay Aaron Bertrand, Paolo Pevarello, Ettore Perrone, Andrea Lombardi Borgia, Sten Christian Orrenius, Mauro Angiolini, Daniele Fancelli
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Publication number: 20060074243Abstract: This invention is directed generally to hydroxamic acid and amide compounds (including salts of such compounds), and, more particularly, to aryl- and heteroaryl-arylsulfonylmethyl hydroxamic acids and amides that, inter alia, inhibit protease activity, particularly matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. These compounds generally correspond in structure to Formula I: wherein A1, A2, A3, E1, E2, E3, and E4 are as defined in this patent. This invention also is directed to compositions of such compounds, intermediates for the syntheses of such compounds, methods for making such compounds, and methods for treating conditions associated with MMP activity and/or aggrecanase activity, particularly pathological conditions.Type: ApplicationFiled: November 10, 2005Publication date: April 6, 2006Inventors: Daniel Becker, Yiyuan Chen, John Freskos, Alan Gasiecki, Margaret Grapperhaus, Donald Hansen, Robert Heintz, Darren Kassab, Ish Khanna, Stephen Kolodziej, Sergio Mantegani, Mark Massa, Joseph McDonald, Deborah Mischke, Mark Nagy, Ettore Perrone, Joseph Rico, Michelle Schmidt, Dale Spangler, John Talley, Mahima Trivedi, Thomas Wynn
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Publication number: 20040167182Abstract: This invention is directed generally to hydroxamic acid and amide compounds (including salts of such compounds), and, more particularly, to aryl- and heteroaryl-arylsulfonylmethyl hydroxamic acids and amides that, inter alia, inhibit protease activity, particularly matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity.Type: ApplicationFiled: June 25, 2003Publication date: August 26, 2004Inventors: Daniel P. Becker, Yiyuan Chen, John N. Freskos, Alan F. Gasiecki, Margaret L. Grapperhaus, Donald W. Hansen, Robert M. Heintz, Darren J. Kassab, Ish K. Khanna, Stephen A. Kolodziej, Sergio Mantegani, Mark A. Massa, Joseph J. McDonald, Deborah A. Mischke, Mark A. Nagy, Ettore Perrone, Joseph G. Rico, Michelle A. Schmidt, Dale P. Spangler, John J. Talley, Mahima Trivedi, Thomas A. Wynn
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Patent number: 6765003Abstract: Compounds which are 3-arylsulfonyl-2-methyl propanoic acid derivatives of formula (I): wherein X is HO—NH— or HO—, R1 is selected from phenyl, 4-chlorophenyl, 4-florophenyl, 4-cyanophenyl, benzamido (i.e., —NH—CO-Ph) and benzamido substituted on the terminal phenyl ring by C1-C4 alkyl, fluoro, chloro, cyano or C1-4 alkoxy; R2 is selected from (a) —S—Ar or —S—CH2—Ar wherein Ar is an aromatic moiety; (b) —O—Ar wherein Ar is as defined above; (c) —S-Het or —S—CH2-Het wherein Het is a heterocyclic ring; and (d) 2,5-dioxo-1-imidazolidinyl or 2,4-dioxo-1-imidazolinyl; and the pharmaceutically acceptable salts thereof; have potent and selective inhibitory activity against matrix metalloproteinases (MMPs) and can thus be used in the treatment and prevention of diseases mediated by MMPs.Type: GrantFiled: April 9, 2002Date of Patent: July 20, 2004Assignee: Pharmacia Italia, SpAInventors: Sergio Mantegani, Francesca Abrate, Pierluigi Bissolino, Paolo Cremonesi, Ettore Perrone, Daniela Jabes
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Patent number: 6482827Abstract: A compound, which is an amine derivative of formula (I) wherein W is —CNHOH or —COOH: R1 and R2 are each hydrogen or an organic residue, R3 is an organic group, Q is a secondary or tertiary acyclic or cyclic amido group, and the pharmaceutically acceptable salts, solvates and hydrates thereof, are inhibitors of matrix metalloproteinases (MMPs) and of the release of tumor necrosis factor-alpha (TNF) from cells. They are therefore useful in the prevention, control and treatment of diseases in which MMPs or TNF are involved, especially tumoral and inflammatory diseases. Processes for their preparation and pharmaceutical compositions containing them are also described.Type: GrantFiled: March 10, 1999Date of Patent: November 19, 2002Assignee: Pharmacia & Upjohn S.p.A.Inventors: Marco Alpegiani, Pierluigi Bissolino, Francesca Abrate, Ettore Perrone, Riccardo Corigli, Daniela Jabes
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Publication number: 20010011085Abstract: The present invention relates to cephem-derivatives and to a process for their preparation, having proper substituents at C-2 position, i.e. heterocyclylthio or acyloxy group. They are potent protease inhibitors, in particular human leucocyte elastase (HLE) inhibitors.Type: ApplicationFiled: August 14, 1997Publication date: August 2, 2001Inventors: MARCO ALPEGIANI, PIERLUIGI BISSOLINO, MASSIMILIANO PALLADINO, ETTORE PERRONE
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Patent number: 6194451Abstract: A compound of formula (I), wherein W is —NHOH or —OH, R1 is either free or protected hydroxymethyl or mercaptomethyl or derivatives thereof, R2 is free or protected hydroxy, R3 and R4 is an organic group, R5 is hydrogen or methyl, or R4 and R5, together with the nitrogen atom to which they are attached, constitute an azaheterocyclyl group, and the solvates, hydrates and pharmaceutically acceptable salts thereof, can inhibit matrix metalloproteinases and the release of tumour necrosis factor (TNF). Processes for producing the compound, intermediates involved in the processes, and pharmaceutical compositions containing the compound are also described.Type: GrantFiled: July 30, 1999Date of Patent: February 27, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Marco Alpegiani, Massimiliano Palladino, Riccardo Corigli, Daniela Jabes, Ettore Perrone, Maria Francesca Abrate, Pierluigi Bissolino, Marina Lombroso
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Patent number: 5777104Abstract: The present invention relates to the use of known cephem derivatives of the formula: ##STR1## wherein n is zero, one or two; R.sup.1 is hydrogen or an organic radical, R.sup.2 represents halo or an organic radical or R.sup.1 and R.sup.2 taken together with the C-2 carbon atom of the cephem nucleus constitute a carbocyclic or heterocyclyl group; R.sup.3 represents R.sup.2 as defined above or an organic radical, R.sup.4 is either R.sup.1 or an organic group, R.sup.5 is either R.sup.1 as defined above or halo or C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio or C.sub.1 -C.sub.6 acylamino;R.sup.6 is R.sup.2 as defined above or an organic group,or a pharmaceutically acceptable salts thereof.Type: GrantFiled: March 8, 1995Date of Patent: July 7, 1998Assignee: Pharmacia & Upjohn S.p.A.Inventors: Marco Alpegiani, Pierluigi Bissolino, Ettore Perrone, Enrico Pesenti
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Patent number: 5587373Abstract: The present invention provides cephalosporin sulphones of formula (I) and the pharmaceutically and veterinarily acceptable salts thereof: ##STR1## wherein n is one or two: A and B are both or each independently hydrogen or an organic radical;R.sup.1 represents halogen, A, OA, --S(O).sub.m A wherein m is 0-2, --OC(O)A, --OS(O).sub.2 A, --NHC(O)A or --NH--Z wherein Z is a mono, di- or tripeptide and A is as defined above;R.sup.2 represents a halogen, A, --S(O).sub.m A, --O--A, --C(O)A, --C(O)OA, --CH.sub.2 --OA, --CH.sub.2 S(O).sub.m A, --CH.sub.2 OC(O)A, --CH.sub.2 O--Z, --CH.sub.2 SC(O) A, --CH.sub.2 --N(A)A, --CH.sub.2 N.sup.+ (A)(A')A", --CH.sub.2 NH--C(O)A or --CH.sub.2 NH--Z wherein A and Z are as defined above.The compounds of formula (I) and their salts are elastase inhibitors.Type: GrantFiled: November 4, 1994Date of Patent: December 24, 1996Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Marco Alpegiani, Pierluigi Bissolino, Ettore Perrone
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Patent number: 5585372Abstract: The present invention provides compounds of formula (I) and pharmaceutically or veterinarily salts thereof; ##STR1## wherein R.sub.1 is hydrogen or halogen or an organic group; R.sub.2 is hydrogen or an optionally substituted C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.14 aralkyl group;R.sub.3 is hydrogen or halogen, or an organic groupR.sub.4 is hydrogen or a group defined as R.sub.2 above or R.sub.4 taken together with R.sub.3 constitutes a C.sub.2 -C.sub.6 alkanediyl or an alkanediyl radical optionally substituted by methyl or phenyland X is either oxygen or sulphur or NR.sub.6, wherein R.sub.6 is either hydrogen or a group as defined for R.sub.2. A process for their preparation by cyclization of appropriate intermediates is also described.The compounds of formula I and the pharmaceutically and veterinarily acceptable salts thereof are elastase inhibitors.Type: GrantFiled: January 20, 1995Date of Patent: December 17, 1996Assignee: Pharmacia S.p.A.Inventors: Marco Alpegiani, Pierluigi Bissolino, Ettore Perrone, Vincenzo Rizzo
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Patent number: 5580865Abstract: The present invention provides cephalosporin sulphones or formula (I), and pharmaceutically or veterinarily acceptable salts thereof; ##STR1## wherein n is zero, one or two; R.sub.1 is hydrogen, halogen or an optionally substituted C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio or C.sub.1 -C.sub.4 carboxamido group;R.sub.2 is hydrogen or an optionally substituted C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.2 -C.sub.5 alkenyl or C.sub.3 -C.sub.6 cycloalkyl group;R.sub.3 is hydrogen or acetoxymethyl, methoxymethyl, methyl or an optionally substituted heterocyclylthiomethyl group;R.sub.4 is an optionally substituted C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.6 alkenyl, aryl(C.sub.1 -C.sub.8)alkyl or heterocyclyl(C.sub.1 -C.sub.8)alkyl group; andR.sub.5 is an optionally substituted C.sub.6 -C.sub.10 aryl or a heterocyclyl group.The compounds of formula I and the pharmaceutically and veterinarily acceptable salts thereof are elastase inhibitors.Type: GrantFiled: April 5, 1993Date of Patent: December 3, 1996Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Marco Alpegiani, Pierluigi Bissolino, Ettore Perrone, Vincenzo Rizzo
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Patent number: 5480880Abstract: The invention provides compounds of the general formula I ##STR1## wherein R.sub.1 is a hydrogen atom, a negative charge or an ester residue; R is:a) --(CH.sub.2).sub.n --A--CO.sub.2 H, --(CH.sub.2)n--A--SO.sub.3 H or --(CH.sub.2).sub.n --A--PO.sub.3 H.sub.2, wherein n is either zero, one or two and A is a group --CH.dbd.CH-- (either E or Z), --OCH.sub.2 --, --SCH.sub.2 -- or --CHOH--;b) --(CH.sub.2).sub.n --PO.sub.3 H.sub.2, --(CH.sub.2).sub.n SO.sub.2 NHCN, --(CH.sub.2).sub.n NHSO.sub.3 H, --(CH.sub.2).sub.n CONHSO.sub.2 CH.sub.3 or --(CH.sub.2).sub.n CONHSO.sub.2 CF.sub.3, wherein n is as defined above;c) --(CH.sub.2 S).sub.m --W--(CH.sub.2).sub.n Z, wherein W is an arylene group or a heterocyclediyl group, m is 0 or 1, n is as above defined, and Z represents CO.sub.2 H, PO.sub.3 H.sub.2, SO.sub.2 NHCN, NHSO.sub.3 H, CONHSO.sub.2 CH.sub.3 or CONHSO.sub.2 CF.sub.3 ;d) ##STR2## wherein Y is O or NH and X is NH, N--OH or N--O--(CH.sub.2).sub.n+1 COOH wherein n is as defined above; ore) --(CH.sub.2 S).sub.Type: GrantFiled: April 9, 1993Date of Patent: January 2, 1996Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Giuseppina Visentin, Franco Zarini, Daniela Jabes, Ettore Perrone, Costantino della Bruna, Marco Alpegiani
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Patent number: 5416208Abstract: Antibacterial penems of formula (I), where R represents a hydrogen atom or a hydroxy protecting group, are prepared by reacting a .beta.-lactam of formula (II) with an oxalyl halide in an inert solvent in the presence of an organic or inorganic base or an acid scavenger to produce a compound of formula (III), wherein X is a halogen atom, treating the resultant compound of formula (III) with a 1,3-dioxolen-2-one of formula (IV), wherein Y is a hydroxy group, in the presence of molecular sieves or an organic or inorganic base to produce a compound of formula (V), and cyclizing the compound of formula (V) in the presence of a trialkylphosphite to provide the penems of formula (I).Type: GrantFiled: February 22, 1994Date of Patent: May 16, 1995Assignee: Farmitalia Carlo Erba S r lInventors: Ettore Perrone, Marco Alpegiani, Franco Zarini, Giuseppe Mazzini, Giovanni Franceschi
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Patent number: 5360904Abstract: A process for preparing penem esters by reacting ##STR1## wherein R.sub.1 is a hydroxy protecting group and X is a C.sub.1 -C.sub.10 alkyl or aryl group, with ##STR2## wherein R.sub.2 is hydrogen or a C.sub.1 -C.sub.6 alkyl group in the presence of an anhydrous organic solvent, condensing the product with ##STR3## wherein X is a halogen atom or a --OCOOR.sub.3 group and then cyclizing.Type: GrantFiled: September 21, 1992Date of Patent: November 1, 1994Assignee: Farmitalia Carlo Erba S r lInventors: Angelo Bedeschi, Walter Cabri, Marcello Marchi, Ettore Perrone