Patents by Inventor Gianfranco Caselli

Gianfranco Caselli 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).

  • Publication number: 20110288173
    Abstract: Use of neboglamine, (S)-4-amino-N(4,4-dimethyl-cyclohexyl)glutamic acid (CR 2249) (CAS Registry Number 163000-63-3), the racemic mixture thereof or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for use in the treatment of toxicodependency induced by drugs such as CNS sedatives such as opiates, barbiturates, benzodiazepines, alcohol, stimulants such as amphetamines and cocaine, and hallucinogens such as LSD, mescalin, cannabis (marijuana) or fencyclidine.
    Type: Application
    Filed: July 27, 2011
    Publication date: November 24, 2011
    Applicant: ROTTAPHARM S.P.A.
    Inventors: Francesco MAKOVEC, Gianfranco CASELLI, Lucio Claudio ROVATI, Antonio GIORDANI
  • Publication number: 20110257209
    Abstract: The present invention is directed to novel 6-1H-imidazo-2-aryl and 2-heteroaryl quinazoline and quinoline of formula I, corresponding salts and solvates thereof, to a process for their preparation and to the use of this compounds and corresponding pharmaceutical composition for the treatment of pain and inflammatory related disorders. Compounds of the invention have been proven highly effective in the pharmacological treatment of both inflammatory and neuropathic pain, in addition to striking anti-inflammatory properties. Their effectiveness in interfering with COX-2 and inflammatory cytokines expressions and production, highlights them as interesting compounds also for the treatment of cancer in addition to several inflammatory diseases.
    Type: Application
    Filed: June 27, 2011
    Publication date: October 20, 2011
    Applicant: ROTTAPHARM S.P.A
    Inventors: Antonio GIORDANI, Stefano MANDELLI, Ilario VERPILIO, Simona ZANZOLA, Francesca TARCHINO, Gianfranco CASELLI, Tiziana Piepoli, Silvio MAZZARI, Francesco MAKOVEC, Lucio Claudio ROVATI
  • Patent number: 7994181
    Abstract: The present invention is directed to novel 6-1H-imidazo-2-aryl and 2-heteroaryl quinazoline and quinoline of formula I, corresponding salts and solvates thereof, to a process for their preparation and to the use of this compounds and corresponding pharmaceutical composition for the treatment of pain and inflammatory related disorders. Compounds of the invention have been proven highly effective in the pharmacological treatment of both inflammatory and neuropathic pain, in addition to striking anti-inflammatory properties. Their effectiveness in interfering with COX-2 and inflammatory cytokines expressions and production, highlights them as interesting compounds also for the treatment of cancer in addition to several inflammatory diseases.
    Type: Grant
    Filed: August 3, 2006
    Date of Patent: August 9, 2011
    Assignee: Rottapharm S.p.A.
    Inventors: Antonio Giordani, Stefano Mandelli, Ilario Verpilio, Simona Zanzola, Francesca Tarchino, Gianfranco Caselli, Tiziana Piepoli, Silvio Mazzari, Francesco Makovec, Lucio Claudio Rovati
  • Patent number: 7968558
    Abstract: The present invention concerns novel amidines derivatives of 2-heteroaryl-quinazoline and quinolines of general formula (I), to a process for their preparation, to their pharmaceutical compositions and to the use of these compounds, salts and solvates thereof, along with the corresponding pharmaceutical compositions, for the treatment of pain and inflammatory disorders. Compounds of this invention are extremely potent analgesics, suitable for the treatment of both inflammatory and neuropathic pain. Particularly for the treatment of neuropathic pain the compounds of the invention have been proved largely superior to the standards currently in the clinical use. These compounds are not acting through inhibition of COX or NOS enzymes but are effective in inhibiting inflammatory cytokine production induced by inflammatory stimuli.
    Type: Grant
    Filed: July 31, 2006
    Date of Patent: June 28, 2011
    Assignee: Rottapharm S.p.A.
    Inventors: Antonio Giordani, Stefano Mandelli, Simona Zanzola, Francesca Tarchino, Gianfranco Caselli, Teresa Simonetta Fiorentino, Silvio Mazzari, Francesco Makovec, Lucio Claudio Rovati
  • Publication number: 20110118289
    Abstract: The present invention is directed to 6-(1H-imidazo-1-yl)-2-aryl and 2-heteroaryl quinazoline and quinolines derivatives, compounds of formula (I), their pharmaceutical acceptable salts and solvates and corresponding pharmaceutical compositions, that acts as Monoamine Oxidase (MAO) inhibitors and Imidazoline Receptor ligands: wherein: X is independently selected from —CH group or a nitrogen atom (—N), W is independently selected from an aryl group, an heteroaryl group, or a benzocondensed heteroaryl group such as 1,3-benzodioxole, benzofuran, 2,3-dihydrobenzofuran, benzothiophene, 2,3-dihydrobenzothiophene, indole, 2,3-dihydroindole, benzimidazole, benzoxazole, benzothiazole, 2H-3,4-dihydrobenzopyran, [1,4]-benzodioxine, 2,3-dihydro-[1,4]-benzodioxine (1,4-benzodioxan). R1 is independently selected from hydrogen (—H), C1-C4 alkyl, hydroxymethyl (—CH2OH), aminomethyl (—CH2NH2), alkylaminomethyl [CH2NH(R2)], or di-alkylaminomethyl [CH2N(R2)2], trifluoromethyl (—CF3).
    Type: Application
    Filed: June 20, 2008
    Publication date: May 19, 2011
    Applicant: ROTTAPHARM S.P.A.
    Inventors: Antonio Giordani, Marco Lanza, Gianfranco Caselli, Stefano Mandelli, Simona Zanzola, Francesco Makovec, Lucio Claudio Rovati
  • Patent number: 7906551
    Abstract: This invention relates to 3-substituted-1,5-diaryl-2-alkyl-pyrroles of Formula I, pharmaceutical compositions containing them, and to their use for the pharmacological treatment of pain and COX-2 over-activation associated disorders. Compounds of this invention are new pyrrole derivatives bearing in position -3 of the pyrrole ring, several variously functionalized, not aliphatic, side chains which confer to the compounds a relevant COX-2 potency and selectivity along with a remarkable oral efficacy. Phenyl rings in position -1 and -5 are variously substituted, but compounds of particular interest are those substituted in position -5 with 4-methylsulphonyl-phenyl or with 4-aminosulphonyl-phenyl groups.
    Type: Grant
    Filed: August 3, 2006
    Date of Patent: March 15, 2011
    Assignee: Rottapharm S.p.A.
    Inventors: Andrea Cappelli, Maurizio Anzini, Mariangela Biava, Francesco Makovec, Antonio Giordani, Gianfranco Caselli, Lucio Claudio Rovati
  • Publication number: 20110045033
    Abstract: The invention relates to the combination of the cholecystokinin-2 (CCK-2) receptor antagonist Itriglumide and proton pump inhibitors (PPIs) for the treatment of patients suffering from gastrointestinal and related disorders.
    Type: Application
    Filed: November 1, 2010
    Publication date: February 24, 2011
    Applicant: ROTTAPHARM S.p.A.
    Inventors: Lucio Claudio ROVATI, Gianfranco CASELLI, Massimo Maria D'AMATO, Antonio GIORDANI, Francesco MAKOVEC
  • Publication number: 20110003861
    Abstract: 2-aryl and 2-heteroaryl 4h-1-benzopyran-4-one-6-amidino derivatives of formula (I) useful as pharmacological agents for the treatment of arthritis, cancer and related pain.
    Type: Application
    Filed: March 6, 2008
    Publication date: January 6, 2011
    Applicant: ROTTAPHARM S.P.A.
    Inventors: Antonio Giordani, Ilario Verpilio, Sabrina Pucci, Roberto Artusi, Gianfranco Caselli, Marco Lanza, Laura Mennuni, Francesco Makovec, Lucio Claudio Rovati
  • Patent number: 7846921
    Abstract: The invention relates to a method for relieving or ameliorating symptoms of gastroesophageal reflux disease by administering a medicament that includes the cholecystokin-2 (CCK-2) receptor antagonist itriglumide and a proton pump inhibitor (PPI).
    Type: Grant
    Filed: July 24, 2006
    Date of Patent: December 7, 2010
    Assignee: Rottapharm, S.p.A.
    Inventors: Lucio Claudio Rovati, Gianfranco Caselli, Massimo Maria D'Amato, Antonio Giordani, Francesco Makovec
  • Publication number: 20100197962
    Abstract: Use of neboglamine, (S)-4-amino-N(4,4-dimethyl-cyclohexyl)glutamic acid (CR 2249) (CAS Registry Number 163000-63-3), the racemic mixture thereof or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for use in the treatment of toxicodependency induced by drugs such as CNS sedatives such as opiates, barbiturates, benzodiazepines, alcohol, stimulants such as amphetamines and cocaine, and hallucinogens such as LSD, mescalin, cannabis (marijuana) or fencyclidine.
    Type: Application
    Filed: October 3, 2006
    Publication date: August 5, 2010
    Applicant: ROTTAPHARM S.P.A.
    Inventors: Francesco Makovec, Gianfranco Caselli, Lucio Claudio Rovati, Antonio Giordani
  • Publication number: 20100197670
    Abstract: Amidine, thiourea and guanidine derivatives of appropriately substituted 2-aminobenzothiazoles, 2-amino-3,1-4H-benzothiazines and 3-amino-1,4-3H-benzothiazines, as understood from formula (I), the related pharmaceutically acceptable salts and solvates thereof: and the use of the products and the corresponding pharmaceutical formulations for the treatment of neurodegenerative pathologies such as cerebral ischemia, neurodegeneration induced by cranial trauma, Alzheimer's disease, Multiple Sclerosis and Amyotrophic Lateral Sclerosis.
    Type: Application
    Filed: September 22, 2008
    Publication date: August 5, 2010
    Inventors: Maurizio Anzini, Antonio Giordani, Francesco Makovec, Andrea Cappelli, Salvatore Vomero, Gianfranco Caselli, Lucio Claudio Rovati
  • Publication number: 20090264500
    Abstract: This invention relates to 3-substituted-1,5-diaryl-2-alkyl-pyrroles of Formula I, pharmaceutical compositions containing them, and to their use for the pharmacological treatment of pain and COX-2 over-activation associated disorders. Compounds of this invention are new pyrrole derivatives bearing in position-3 of the pyrrole ring, several variously functionalized, not aliphatic, side chains which confer to the compounds a relevant COX-2 potency and selectivity along with a remarkable oral efficacy. Phenyl rings in position-1 and -5 are variously substituted, but compounds of particular interest are those substituted in position-5 with 4-methylsulphonyl-phenyl or with 4-aminosulphonyl-phenyl groups.
    Type: Application
    Filed: August 3, 2006
    Publication date: October 22, 2009
    Inventors: Andrea Cappelli, Maurizio Anzini, Mariangela Biava, Francesco Makovec, Antonio Giordani, Gianfranco Caselli, Lucio Claudio Rovati
  • Publication number: 20090264451
    Abstract: The present invention is directed to novel 6-1H-imidazo-2-aryl and 2-heteroaryl quinazoline and quinoline of formula I, corresponding salts and solvates thereof, to a process for their preparation and to the use of this compounds and corresponding pharmaceutical composition for the treatment of pain and inflammatory related disorders. Compounds of the invention have been proven highly effective in the pharmacological treatment of both inflammatory and neuropathic pain, in addition to striking anti-inflammatory properties. Their effectiveness in interfering with COX-2 and inflammatory cytokines expressions and production, highlights them as interesting compounds also for the treatment of cancer in addition to several inflammatory diseases.
    Type: Application
    Filed: August 3, 2006
    Publication date: October 22, 2009
    Applicant: ROTTAPHARM S.p.A.
    Inventors: Antonio Giordani, Stefano Mandelli, Ilario Verpilio, Simona Zanzola, Francesca Tarchino, Gianfranco Caselli, Tiziana Piepoli, Silvio Mazzari, Francesco Makovec, Lucio Claudio Rovati
  • Publication number: 20090227609
    Abstract: The present invention concerns novel amidines derivatives of 2-heteroaryl-quinazoline and quinolines of general formula (I), to a process for their preparation, to their pharmaceutical compositions and to the use of these compounds, salts and solvates thereof, along with the corresponding pharmaceutical compositions, for the treatment of pain and inflammatory disorders. Compounds of this invention are extremely potent analgesics, suitable for the treatment of both inflammatory and neuropathic pain. Particularly for the treatment of neuropathic pain the compounds of the invention have been proved largely superior to the standards currently in the clinical use. These compounds are not acting through inhibition of COX or NOS enzymes but are effective in inhibiting inflammatory cytokine production induced by inflammatory stimuli.
    Type: Application
    Filed: July 31, 2006
    Publication date: September 10, 2009
    Applicant: Rottapharm S.p.A.
    Inventors: Antonio Giordani, Stefano Mandelli, Simona Zanzola, Francesca Tarchino, Gianfranco Caselli, Teresa Simonetta Fiorentino, Silvio Mazzari, Francesco Makovec, Lucio Claudio Rovati
  • Patent number: 7482371
    Abstract: The invention relates to the use of a pharmaceutically active derivative of N-phenylbenzamide of Formula (I) or of a pharmaceutically acceptable salt thereof, for preparing a medicament for the therapeutic treatment of Chronic Obstructive Pulmonary Disease (COPD). Compounds of Formula (I): wherein R1 is cyano, nitro, halogen, hydroxy, C1-C4 alkyl, methoxy or tetrazol-5-yl group, R2 is hydrogen, hydroxy or methoxy, R3 is a tetrazol-5-yl group or hydrogen, R4 and R5 are hydrogen if R3 is tetrazol-5-yl group, or R4 and R5 are independently selected from the group consisting of carboxy, methoxycarbonyl, ethoxycarbonyl and carbamoyl if R3 is hydrogen, and R6 is hydrogen or methyl.
    Type: Grant
    Filed: August 19, 2005
    Date of Patent: January 27, 2009
    Assignee: Rottapharm S.p.A.
    Inventors: Lucio Claudio Rovati, Antonio Giordani, Gianfranco Caselli
  • Publication number: 20080194877
    Abstract: Mucositis is the result of a complex process of interactive biologic phenomena that take place in both the epitelium and the submucosa, often leading to severe pain and increased risk of dangerous syste f48 mic infections. Mucositis is often a side effect during chemotherapy and radiation therapy. The benzamidine derivatives herein described are particularly effective for treating and preventing mucositis since they are acting simultaneously at the several phases that characterize this disease.
    Type: Application
    Filed: March 16, 2006
    Publication date: August 14, 2008
    Applicant: ROTTAPHARM S.p.A.
    Inventors: Ornella Letari, Massimo Maria D'Amato, Simona Zanzola, Roberto Artusi, Lucio Claudio Rovati, Gianfranco Caselli, Antonio Giordani
  • Publication number: 20080045522
    Abstract: (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: Application
    Filed: August 13, 2007
    Publication date: February 21, 2008
    Applicant: Dompe pha.r.ma S.p.A.
    Inventors: Marcello ALLEGRETTI, Riccardo Bertini, Valerio Berdini, Cinzia Bizzarri, Maria Cesta, Vito Di Cioccio, Gianfranco Caselli, Francesco Colotta, Carmelo Gandolfi, Janete Gandolfi, Giulio Gandolfi, Maria Gandolfi, Arrigo Gandolfi
  • Publication number: 20080004303
    Abstract: The invention relates to the combination of the cholecystokinin-2 (CCK-2) receptor antagonist Itriglumide and proton pump inhibitors (PPIs) for the treatment of patients suffering from gastrointestinal and related disorders.
    Type: Application
    Filed: July 29, 2005
    Publication date: January 3, 2008
    Applicant: ROTTAPHARM S.P.A.
    Inventors: Lucio Rovati, Gianfranco Caselli, Massimo D'Amato, Antonio Giordani, Francesco Makovec
  • Publication number: 20060052427
    Abstract: The invention relates to the use of a pharmaceutically active derivative of N-phenylbenzamide of Formula (I) or of a pharmaceutically acceptable salt thereof, for preparing a medicament for the therapeutic treatment of Chronic Obstructive Pulmonary Disease (COPD). Compounds of Formula (I): wherein R1 is cyano, nitro, halogen, hydroxy, C1-C4 alkyl, methoxy or tetrazol-5-yl group, R2 is hydrogen, hydroxy or methoxy, R3 is a tetrazol-5-yl group or hydrogen, R4 and R5 are hydrogen if R3 is tetrazol-5-yl group, or R4 and R5 are independently selected from the group consisting of carboxy, methoxycarbonyl, ethoxycarbonyl and carbamoyl if R3 is hydrogen, and R6 is hydrogen or methyl.
    Type: Application
    Filed: August 19, 2005
    Publication date: March 9, 2006
    Inventors: Lucio Rovati, Antonio Giordani, Gianfranco Caselli
  • Patent number: 6887903
    Abstract: The compounds of formula 1 wherein R and R2 are as defined in the disclosure, are useful in the prevention and treatment of tissue damage due to exacerbated recruitment of polymorphonuclear neutrophils (PMN leukocytes) at the inflammatory sites.
    Type: Grant
    Filed: October 14, 1999
    Date of Patent: May 3, 2005
    Assignee: Dompe S.p.A.
    Inventors: Riccardo Bertini, Cinzia Bizzarri, Vilma Sabbatini, Gianfranco Caselli, Marcello Allegretti, Maria Candida Cesta, Carmelo Gandolfi, Marco Mantovanini, Francesco Colotta, Stefano Porzio