Patents by Inventor Riccardo Bertini
Riccardo Bertini 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: 9493402Abstract: (R)-2-Arylpropionamide compounds of formula (I), pharmaceutical preparations of the compounds and a process for making the compounds are described. The 2-Arylpropionamides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonuclear leukocytes and monocytes at inflammatory sites. In particular, the invention relates to the R enantiomers of omega-aminoalkylamides of 2-aryl propionic acids, of formula (I), for use as inhibitors of chemotaxis of neutrophils and monocytes induced by the C5a fraction of complement and by other chemotactic proteins whose biological activity is associated with activation of a 7-TD receptor. Selected compounds of formula (I) are dual inhibitors of both the C5a-induced chemotaxis of neutrophils and monocytes and the IL-8-induced chemotaxis of polymorphonuclear leukocytes.Type: GrantFiled: October 15, 2012Date of Patent: November 15, 2016Assignee: DOMPÉ FARMACEUTICI S.P.A.Inventors: Marcello Allegretti, Riccardo Bertini, Valerio Berdini, Cinzia Bizzarri, Maria Candida Cesta, Vito Di Cioccio, Gianfranco Caselli, Francesco Colotta, Carmelo Gandolfi
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Patent number: 9328057Abstract: The compounds of formula (I): where Ar is an aromatic ring and Ra, Rb, are as defined in the description, are useful in therapy as drugs for the treatment of diseases mediated by infiltrations of neutrophils induced by IL-8, such as psoriasis, rheumatoid arthritis, ulcerative cholitis and for the treatment of damages caused by ischemia and reperfusion.Type: GrantFiled: December 3, 2008Date of Patent: May 3, 2016Assignee: DOMPE' FARMACEUTICI S.P.A.Inventors: Marcello Allegretti, Riccardo Bertini, Maria Candida Cesta, Cinzia Bizzarri, Francesco Colotta
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Patent number: 8871784Abstract: Selected 2-arylacetic acids, their derivatives and pharmaceutical compositions that contain these compounds are useful in inhibiting chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from their activation. In particular, 2(ortho)-substituted arylacetic acids or their derivatives, such as amides and sulfonamides, lack cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: GrantFiled: June 30, 2010Date of Patent: October 28, 2014Assignee: Dompe'S.p.A.Inventors: Alessio Moriconi, Marcello Allegretti, Maria Candida Cesta, Riccardo Bertini, Cinzia Bizzarri, Francesco Colotta
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Patent number: 8648110Abstract: Selected 2-arylacetic acids, their derivatives and pharmaceutical compositions that contain these compounds are useful in inhibiting chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from their activation. In particular, 2(ortho)-substituted arylacetic acids or their derivatives, such as amides and sulfonamides, lack cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: GrantFiled: April 22, 2011Date of Patent: February 11, 2014Assignee: Dompe Pha.R.Ma S.p.A.Inventors: Alessio Moriconi, Marcello Allegretti, Maria Candida Cesta, Riccardo Bertini, Cinzia Bizzarri, Francesco Colotta
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Patent number: 8293788Abstract: 4-(trifluoromethanesulfonyloxyphenyl)propionic acid derivatives and pharmaceutical composition containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: GrantFiled: September 15, 2011Date of Patent: October 23, 2012Inventors: Marcello Allegretti, Marla Candida Cesta, Riccardo Bertini, Marco Mosca, Francesco Colotta
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Patent number: 8288368Abstract: (R)-2-Arylpropionamide compounds of formula (I) are described. The process for their preparation and pharmaceutical preparations thereof are also described. The 2-Arylpropionamides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear leukocytes (leukocytes PMN) and of monocytes at the inflammatory sites. In particular, the invention relates to the R enantiomers of omega-aminoalkylamides of 2-aryl propionic acids, of formula (I), for use in the inhibition of the chemotaxis of neutrophils and monocytes induced by the C5a fraction of the complement and by other chemotactic proteins whose biological activity is associated with activation of a 7-TD receptor. Selected compounds of formula (I) are dual inhibitors of both the C5a-induced chemotaxis of neutrophils and monocytes and the IL-8-induced chemotaxis of PMN leukocytes.Type: GrantFiled: February 25, 2002Date of Patent: October 16, 2012Assignee: Dompé Pha.R.Ma S.p.A.Inventors: Marcello Allegretti, Riccardo Bertini, Valerio Berdini, Cinzia Bizzarri, Maria Candida Cesta, Vito Di Cioccio, Gianfranco Caselli, Fracesco Colotta, Carmelo Gandolfi, Janete Peloia Barroso Gandolfi, legal representative, Giulio Agostino Gandolfi, legal representative, Maria Carla Gandolfi, legal representative, Arrigo Aldo Gandolfi, legal representative
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Publication number: 20120004264Abstract: 4-(trifluoromethanesulfonyloxyphenyl)propionic acid derivatives and pharmaceutical composition containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: ApplicationFiled: September 15, 2011Publication date: January 5, 2012Applicant: Dompé pha.r.ma S.p.A.Inventors: Marcello Allegretti, Marla Candida Cesta, Riccardo Bertini, Marco Mosca, Francesco Colotta
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Patent number: 8063242Abstract: (R) and (S) 2-Aryl-propionic acids, and pharmaceutical compositions that contain them, are useful in inhibiting chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The acids are used for the prevention and treatment of pathologies deriving from said activation. In particular, the (R) enantiomers of said acids are lacking cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrofil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bollous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: GrantFiled: November 19, 2002Date of Patent: November 22, 2011Assignee: Dompe PHA.R.MA S.p.A.Inventors: Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Maria Candida Cesta, Francesco Colotta
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Patent number: 8039656Abstract: 4-(trifluoromethanesulfonyloxyphenyl)propionic acid derivatives and pharmaceutical composition containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: GrantFiled: March 21, 2005Date of Patent: October 18, 2011Inventors: Marcello Allegretti, Maria Candida Cesta, Riccardo Bertini, Marco Mosca, Francesco Colotta
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Patent number: 8026367Abstract: The present invention relates to selected (R)-arylalkylamino derivatives of formula (I), in which R, R1 and Ar are as defined in the claims. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.Type: GrantFiled: November 24, 2006Date of Patent: September 27, 2011Assignee: Dompe PHA.R.MA S.p.A.Inventors: Marcello Allegretti, Alessio Moriconi, Andrea Aramini, Maria Candida Cesta, Andrea Beccari, Riccardo Bertini
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Publication number: 20110195967Abstract: Selected 2-arylacetic acids, their derivatives and pharmaceutical compositions that contain these compounds are useful in inhibiting chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from their activation. In particular, 2(ortho)-substituted arylacetic acids or their derivatives, such as amides and sulfonamides, lack cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: ApplicationFiled: April 22, 2011Publication date: August 11, 2011Applicant: DOMPE PHA.R.MA S.P.A.Inventors: Alessio MORICONI, Marcello ALLEGRETTI, Maria Candida CESTA, Riccardo BERTINI, Cinzia BIZZARRI, Francesco COLOTTA
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Patent number: 7939521Abstract: The present invention relates to selected (R)-2-phenyl-propionamides and (R)-2-phenyl-sulfonamides with a hydrogen bond acceptor atom/group in a well defined position in the chemical space. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.Type: GrantFiled: December 13, 2005Date of Patent: May 10, 2011Assignee: DompePHA.R.MA S.p.A.Inventors: Marcello Allegretti, Riccardo Bertini, Andrea Beccari, Alessio Moriconi, Andrea Aramini, Cinzia Bizzarri, Francesco Colotta
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Patent number: 7868046Abstract: The present invention relates to novel (2R)-2-phenylpropanamides bearing a 4-sulfonylamino substituent on the 4 position of the phenyl group and to pharmaceutical compositions containing them, which are used as inhibitors of the chemotaxis of polymorphonucleate and mononucleate cells, and which are useful in the treatment of various ELR+CXC chemokine-mediated disorders. In particular, the compounds of the invention are useful in the treatment and control of specific CXCR2 dependent pathologies such as BOS, COPD, angiogenesis and melanoma.Type: GrantFiled: December 15, 2009Date of Patent: January 11, 2011Assignee: Dompe' Pha.r.ma S.p.A.Inventors: Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Maria Candida Cesta, Andrea Aramini, Alessio Moriconi
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Publication number: 20100267726Abstract: Selected 2-arylacetic acids, their derivatives and pharmaceutical compositions that contain these compounds are useful in inhibiting chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. In particular, 2(ortho)-substituted arylacetic acids or their derivatives, such as amides and sulfonamides, lack cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: ApplicationFiled: June 30, 2010Publication date: October 21, 2010Applicant: DOMPE PHA.R.MA S.P.A.Inventors: Alessio MORICONI, Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Maria Candida Cesta, Francesco Colotta
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Patent number: 7776909Abstract: Selected 2-arylacetic acids, their derivatives and pharmaceutical compositions that contain these compounds are useful in inhibiting chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2-membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. In particular, 2(ortho)-substituted arylacetic acids or their derivatives, such as amides and sulfonamides, lack cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: GrantFiled: February 4, 2004Date of Patent: August 17, 2010Assignee: Dompe Pha.R.Ma S.p.A.Inventors: Alessio Moriconi, Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Maria Candida Cesta, Francesco Colotta
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Publication number: 20100152256Abstract: The present invention relates to novel (2R)-2-phenylpropanamides bearing a 4-sulfonylamino substituent on the 4 position of the phenyl group and to pharmaceutical compositions containing them, which are used as inhibitors of the chemotaxis of polymorphonucleate and mononucleate cells, and which are useful in the treatment of various ELR+CXC chemokine-mediated disorders. In particular, the compounds of the invention are useful in the treatment and control of specific CXCR2 dependent pathologies such as BOS, COPD, angiogenesis and melanoma.Type: ApplicationFiled: December 15, 2009Publication date: June 17, 2010Inventors: Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Maria Candida Cesta, Andrea Aramini, Alessio Moriconi
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Patent number: 7737139Abstract: Selected sulfonic acids, their derivatives and pharmaceutical compositions containing such compounds are useful in inhibiting the chernotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, the selected sulfonic acids and their derivativas are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrofil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: GrantFiled: March 11, 2004Date of Patent: June 15, 2010Assignee: Dompe PHA.R.MA S.p.A.Inventors: Marcello Allegretti, Andrea Aramini, Maria Candida Cesta, Riccardo Bertini, Cinzia Bizzarri, Francesco Colotta
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Patent number: 7705050Abstract: N-(2-aryl-propionyl)-amides of formula (I) are described. The process for their preparation and pharmaceutical preparations thereof are also described. The amides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear neutrophils (leukocytes PMN) at the inflammatory sites. In particular, the invention relates to the R enantiomers of N-(2-aryl-propionyl)amides of formula (I) for use in the inhibition of the chemotaxis of neutrophils induced by IL-8. The compounds of the invention are used in the treatment of psoriasis, ulcerative cholitis, glomerular nephritis, acute respiratory insufficiency, idiopathic fibrosis, and rheumatoid arthritis.Type: GrantFiled: February 6, 2001Date of Patent: April 27, 2010Inventors: Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Vilma Sabbatini, Ginfranco Caselli, Maria Candida Cesta, Carmelo Gandolfi, Janete Peloia Barroso Gandolfi, legal representative, Giulio Agostino Gandolfi, legal representative, Maria Carla Gandolfi, legal representative, Arrigo Aldo Gandolfi, legal representative, Francesco Colotta
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Patent number: 7674806Abstract: Amidines and derivatives thereof of formula (I) are described. The process for their preparation and pharmaceutical compositions thereof are also described. The amidines of the invention are useful in the inhibition of chemotaxis of neutrophils induced by IL-8. The compounds of the invention are used in the treatement of psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: GrantFiled: September 16, 2004Date of Patent: March 9, 2010Inventors: Marcello Allegretti, Maria Candida Cesta, Giuseppe Nano, Riccardo Bertini, Cinzia Bizzarri, Francesco Colotta
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Patent number: 7652169Abstract: The present invention relates to novel (2R)-2-phenylpropanamides bearing a 4-sulfonylamino substituent on the 4 position of the phenyl group and to pharmaceutical compositions containing them, which are used as inhibitors of the chemotaxis of polymorphonucleate and mononucleate cells, and which are useful in the treatment of various ELR+CXC chemokine-mediated disorders. In particular, the compounds of the invention are useful in the treatment and control of specific CXCR2 dependent pathologies such as BOS, COPD, angiogenesis and melanoma.Type: GrantFiled: May 17, 2007Date of Patent: January 26, 2010Assignee: Dompe' Pha. R. Ma S.p.A.Inventors: Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Maria Candida Cesta, Andrea Aramini, Alessio Moriconi