Patents by Inventor Sergio Mantegani
Sergio Mantegani 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: 9701686Abstract: Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.Type: GrantFiled: July 29, 2015Date of Patent: July 11, 2017Assignee: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Teresa Disingrini, Sergio Mantegani, Mario Varasi
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Publication number: 20150329552Abstract: Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.Type: ApplicationFiled: July 29, 2015Publication date: November 19, 2015Applicant: NERVIANO MEDICAL SCIENCES S.r.l.Inventors: Teresa Disingrini, Sergio Mantegani, Mario Varasi
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Patent number: 9127015Abstract: Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.Type: GrantFiled: November 24, 2010Date of Patent: September 8, 2015Assignee: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Teresa Disingrini, Sergio Mantegani, Mario Varasi
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Patent number: 8309578Abstract: Bicyclic pyrazole and isoxazole 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 mediated by HSP90 protein, like cancer and neurodegenerative disorders.Type: GrantFiled: November 19, 2009Date of Patent: November 13, 2012Assignee: Nerviano Medical Sciences S.r.l.Inventors: Sergio Mantegani, Maria Gabriella Brasca, Francesco Casuscelli, Ron Ferguson, Helena Posteri, Carlo Visco, Elena Casale, Fabio Zuccotto
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Publication number: 20120277214Abstract: Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.Type: ApplicationFiled: November 24, 2010Publication date: November 1, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Teresa Disingrini, Sergio Mantegani, Mario Varasi
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Publication number: 20110294790Abstract: Bicyclic pyrazole and isoxazole 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 mediated by HSP90 protein, like cancer and neurodegenerative disorders.Type: ApplicationFiled: November 19, 2009Publication date: December 1, 2011Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Sergio Mantegani, Maria Gabriella Brasca, Francesco Casuscelli, Ron Ferguson, Helena Posteri, Carlo Visco, Elena Casale, Fabio Zuccotto
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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: 20050032869Abstract: Pyrazolyl-indole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, 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 disregulated protein kinase activity, like cancer.Type: ApplicationFiled: July 1, 2004Publication date: February 10, 2005Applicant: Pharmacia Italia S.p.A.Inventors: Daniela Berta, Barbara Forte, Sergio Mantegani, Mario Varasi, Paola Vianello
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Publication number: 20040204477Abstract: A compound of formula (I) is provided which is able to interact with &bgr;-catenin/TCF-4 binding site, having a structure essentially equivalent to a pharmacophore (IA), as herein described.Type: ApplicationFiled: May 24, 2004Publication date: October 14, 2004Inventors: Juergen Moll, Stefan Knapp, Claudio Dalvit, Jean-Yves Trosset, Michael Sundstrom, Sergio Mantegani
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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: 6407122Abstract: The present invention relates to amino-benzothiazole compounds of formula (I) wherein X, Y, Z and R1 are as defined in the specification, their pharmaceutically acceptable salts, processes for their preparation, pharmaceutical composition comprising such compounds and their use as neuroprotective agents.Type: GrantFiled: June 1, 2000Date of Patent: June 18, 2002Assignee: Pharmacia & Upjohn S.p.A.Inventors: Sergio Mantegani, Paolo Cremonesi, Mario Varasi, Carmela Speciale
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Patent number: 6316451Abstract: A compound of formula (1) wherein R1 is hydrogen, hydroxy, a group of formula OR5 wherein R5 is C1-C6 alkyl, C2-C6 alkenyl or C3-C8 cycloalkyl, halogen, amino which may be unsubstituted or mono or disubstituted by C1-C6 alkyl, C2-C6 alkenyl, aralkyl, acyl or trifluoroacetyl; R2 is hydrogen, hydroxy, a group NR6R7 wherein R6 and R7 independently represent hydrogen, an optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C3-C8 cycloalkyl or, taken together with the nitrogen atom, represent an optionally substituted C3-C8 heterocyclic ring; R3 is hydrogen, hydroxy, R4 is a 2-substituted thiazolyl or imidazolyl system and the pharmaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.Type: GrantFiled: September 26, 2000Date of Patent: November 13, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Sergio Mantegani, Gabriella Traquandi, Tiziano Bandiera, Jacqueline Lansen, Mario Varasi
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Patent number: 6284896Abstract: There are provided compounds of formula (I), wherein R1 is a hydrogen, chlorine or bromine atom or a methyl, methylthio, hydroxy, cyano or carboxamido group; R2 is C1-C3 alkyl or an alkyl group; R3 and R4 are independently a hydrogen atom, a C1-C5 alkyl group, a C3-C5 alkenyl group, a C5-C6 cycloalkyl C1-C3 alkyl group, a phenyl-C3-C5 alkenyl or phenyl group: which groups are optionally substituted by C1-C3 alkyl, C1-C3 alkoxy, triflouromethyl, hydroxy or amino group; or a group of formula (a), wherein R6 is hydrogen atom or a C1-C3 alkyl group and R7 is a phenyl group, a substituted phenyl group as described above or a heterocyclic ring, R5 is a hydrogen or bromine atom or an organic residue and R is H or an organic residue, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmaceutical compositions comprising them are also provided.Type: GrantFiled: December 29, 1997Date of Patent: September 4, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Sergio Mantegani, Tiziano Bandiera, Enzo Brambilla, Carla Caccia, Nicola Carfagna
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Patent number: 6087371Abstract: Ergoline derivative having formula (I) wherein R.sub.1 is hydrogen atom or C.sub.1-4 alkyl group; R.sub.2 is hydrogen, chlorine, or bromine atom, methyl or C.sub.1-4 alkylthio group; n is 0, 1 or 2; the substituent at position 8 is in .alpha. or .beta. configuration; Het represents an aromatic 5-membered heterocyclic ring, said ring having three heteroatoms which are the same or different and which are selected from the group consisting of sulfur, oxygen and nitrogen atom and X is hydrogen, chlorine or bromine or fluorine atom, or a pharmaceutically acceptable acid addition salt thereof are active at the Central Nervous System level. A process for their preparation is also described, as are pharmaceutical compositions containing them.Type: GrantFiled: August 17, 1998Date of Patent: July 11, 2000Assignee: Pharmacia & Upjohn S.p.A.Inventors: Sergio Mantegani, Tiziano Bandiera, Maurizio Meroni, Mario Varasi, Carla Caccia
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Patent number: 6060483Abstract: The present invention provides the new use in the treatment of neurodegenerative diseases with ergoline derivatives of formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a linear or branched C.sub.1 -C.sub.5 alkyl or C.sub.2 -C.sub.5 alkenyl group optionally substituted with a C.sub.3 -C.sub.7 cycloalkyl, a hydroxy group or a R.sub.3 -substituted phenyl group wherein R.sub.3 is a hydroxy or a hydroxymethyl group; R.sub.2 represents a hydrogen atom or a linear or branched C.sub.1 -C.sub.5 alkyl or a C.sub.2 -C.sub.5 alkenyl group optionally substituted with a hydroxy group, or a R.sub.3 -substituted phenyl group wherein R.sub.3 is as above defined, or with a C.sub.1 -C.sub.5 alkoxy group; the symbols--at positions 2,3 and 8, 9 independently denote a single or double chemical bond and Z represents a group (CH.sub.2).sub.n OH, wherein n is 0 or an integer from 1 to 3, or a group C(R.sub.4).sub.2 OH wherein R.sub.4 is a C.sub.1 -C.sub.Type: GrantFiled: December 28, 1998Date of Patent: May 9, 2000Assignee: Pharmacia & Upjohn S.p.A.Inventors: Sergio Mantegani, Enzo Brambilla, Nicola Carfagna, Mario Varasi
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Patent number: 5968955Abstract: A Disubstituted piperidine compounds of formula (I), wherein R.sub.1 is hydrogen; bromo; chloro; a linear or branched C.sub.1 -C.sub.5 alkyl group; a linear or branched C.sub.1 -C.sub.5 alkoxy group; or an optionally substituted phenyl group; R.sub.2 is hydrogen, a linear or branched C.sub.1 -C.sub.5 alkyl group or an optionally substituted phenyl group; X is CH.sub.2, C.dbd.O, CHOH or C.dbd.NOH; R.sub.3 is hydrogen or a linear or branched C.sub.1 -C.sub.5 alkyl group; Y is a (CH.sub.2).sub.n group in which n is an integer from 0 to 4, CHOH, C.dbd.O or CH-A wherein A is an optionally substituted phenyl group; A is an optionally substituted phenyl group; W is hydrogen or hydroxy; stereoisomers thereof and their pharmaceutically acceptable salts. The compounds possess selective neuroprotective activity and are useful in the treatment of an acute or a degenerative CNS disease. A process is described for preparing the compounds and pharmaceutical compositions containing them.Type: GrantFiled: March 31, 1998Date of Patent: October 19, 1999Assignee: Pharmacia & Upjohn S.p.A.Inventors: Sergio Mantegani, Tiziano Bandiera, Manuela Villa, Mario Varasi, Carmela Speciale
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Patent number: 5430031Abstract: The present invention provides compounds of the formula (I) ##STR1## wherein A, R.sub.1, R.sub.2 and R.sub.3 are defined as in the specification, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmacetical compositions comprising them are also provided.Type: GrantFiled: December 20, 1993Date of Patent: July 4, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Sergio Mantegani, Enzo Brambilla, Carla Caccia, Nicola Carfagna
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Patent number: 5210194Abstract: Ergoline derivatives of the formula I: ##STR1## wherein R represents hydrogen or C.sub.1 -C.sub.4 alkyl; R.sub.1 represents hydrogen, chlorine, bromine or methyl; either R.sub.2 and R.sub.3 both represent hydrogen or together represent a chemical bond; R.sub.4 represents a C.sub.1 -C.sub.4 hydrocarbon group; each of R.sub.5, R.sub.6, R.sub.8 and R.sub.9 independently represents hydrogen or C.sub.1 -C.sub.4 alkyl; R.sub.7 represents hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or C.sub.3 -C.sub.7 cycloalkyl and n is 0, 1 or 2; are prepared by reaction between compounds of the formulae II and III: ##STR2## and subsequent cyclization of the resultant compounds. The compounds of the formula I are known useful anxiolytic, antipsychotic and anti-parkinson agents.Type: GrantFiled: September 25, 1991Date of Patent: May 11, 1993Assignee: Farmitalia Carlo Erba S.r.l. An Italian Body CorporateInventors: Sergio Mantegani, Gabriella Traquandi, Tiziano Bandiera, Enzo Brambilla
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Patent number: 4920099Type: GrantFiled: October 29, 1987Date of Patent: April 24, 1990Assignee: Farmitalie Carlo Erba S.p.A.Inventors: Laura Chiodini, Mauro Gobbini, Sergio Mantegani, Daniela Ruggieri, Aldemio Temperilli, Gabriella Traquandi, Patrizia Ferrari