Patents Assigned to Rottapharm S.p.A.
  • Patent number: 9623108
    Abstract: Formulation for oral administration, in the form of tablets or of powder for extemporaneous use, able to exert a beneficial effect on the cardiovascular system and having eulipidaemic activity, cholesterol-lowering and triglyceride-lowering activity, antioxidant activity, and a protective action on the vasal endothelium, comprising berberine in combination with a policosanol and/or red yeast and preferably containing an antioxidant, such as astaxanthin and/or folic acid.
    Type: Grant
    Filed: March 29, 2007
    Date of Patent: April 18, 2017
    Assignee: ROTTAPHARM S.p.A.
    Inventors: Paolo Senin, Ivo Setnikar, Luigi Angelo Rovati
  • Patent number: 9174966
    Abstract: The present invention relates to the solid state of 6-(1H-imidazol-1-yl)-2-phenylquinazoline (I) and therefore to novel crystalline forms of the base and of pharmaceutically acceptable salts and solvates thereof, and also to methods for preparing them, to the respective pharmaceutical formulations and to their therapeutic use. Compound (I) may be obtained as the free base in five different crystalline forms, three polymorphic forms and two hydrates. Some pharmaceutically acceptable salts of (I) that have physicochemical characteristics acceptable for pharmaceutical development were obtained, and the respective polymorphic forms and/or hydrates were characterized.
    Type: Grant
    Filed: June 4, 2010
    Date of Patent: November 3, 2015
    Assignee: ROTTAPHARM S.P.A.
    Inventors: Antonio Giordani, Stefano Mandelli, Francesca Porta, Matteo Ghirri, Lucio Claudio Rovati
  • Patent number: 9062129
    Abstract: New ester derivatives of hyaluronic acid with hydroxy-cinnamic acid, their rheological and anti-radical properties are used as protective agents in dermatology.
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: June 23, 2015
    Assignee: ROTTAPHARM S.p.A.
    Inventor: Lucio Claudio Rovati
  • Publication number: 20140243373
    Abstract: There is described a group of novel cyclic amine derivative compounds having an EP4 receptor agonistic activity. Specifically, the compounds according to the invention are provided with analgesic, antinflammatory, antiglaucoma activity, and also with anti-osteoporosis and antiulcerative activity. The present invention therefore relates to novel cyclic amine derivative compounds, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as pain, glaucoma, ulcerative colitis and osteoporosis.
    Type: Application
    Filed: July 4, 2011
    Publication date: August 28, 2014
    Applicant: Rottapharm S.P.A.
    Inventors: Manuela Borriello, Sabrina Pucci, Luigi Piero Stasi, Lucio Rovati
  • Patent number: 8809306
    Abstract: The invention relates to the combination of Andolast, a calcium-activated potassium channel opener and glucocorticoids for the treatment of patients suffering for airway diseases. Pharmaceutical compositions comprising Andoalst and glucocorticoids are also disclosed.
    Type: Grant
    Filed: July 31, 2006
    Date of Patent: August 19, 2014
    Assignee: Rottapharm S.p.A.
    Inventors: Francesco Makovec, Massimo Maria D'Amato, Antonio Giordani, Lucio Claudio Rovati
  • Patent number: 8633208
    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: Grant
    Filed: June 20, 2008
    Date of Patent: January 21, 2014
    Assignee: Rottapharm S.p.A
    Inventors: Antonio Giordani, Marco Lanza, Gianfranco Caselli, Stefano Mandelli, Simona Zanzola, Francesco Makovec, Lucio Claudio Rovati
  • Publication number: 20130310400
    Abstract: The invention concerns a spiro-amino compound of Formula (I), wherein A is selected from a 5- or 6-membered aromatic ring and a 5- or 6-membered heteroaromatic ring containing 1 to 3 nitrogen atom; X is a substituent selected from the group consisting of (C1-C3)alkyl and halogen, Y is a substituent selected from the group consisting of halogen and trifluoromethyl or a pharmaceutically acceptable salt thereof for use in the treatment of pathologies which require an antagonist of the NK1 receptor.
    Type: Application
    Filed: February 2, 2012
    Publication date: November 21, 2013
    Applicant: ROTTAPHARM S.P.A.
    Inventors: Luigi Piero Stasi, Lucio Rovati
  • Publication number: 20130165494
    Abstract: 1,5-diaryl-2-alkylpyrrole-3-substituted nitro esters, of Formula (I) are provided. Such compounds are potent and selective COX-2 inhibitors which are able to release NO in concentrations that make it possible to counteract the side effects due to selective COX-2 inhibition, without giving rise to hypotensive effects. Formula (I) includes compounds wherein the groups R? and R? are: —H, —F, —Cl, —Br, —CH3, —CF3, —OCH3, —SCH3, R1 is methyl, ethyl, trifluoromethyl, hydroxymethyl, methoxymethyl and the substituent in position ?3 of the pyrrole ring is a chain, where the groups X, Y, Z, W and R2 are: X is a carbonyl or a group —(CHR3)—, Y is an oxygen atom or the group —NR3— and Z is a carbonyl or a group —(CHR3)—, or a [—CH(COOH)—] group, or a group —(NR3)—, W is an aliphatic chain substituted with one or two (—O—NO2) groups, R2 is: —H, —OH, —OCH3, or —NHR3. R3 is: —H, —CH3, —CH2CH3, [—CH2(CH3)2]. R?? is methylsulphonyl or sulphonamido.
    Type: Application
    Filed: September 7, 2011
    Publication date: June 27, 2013
    Applicant: Rottapharm S.p.A.
    Inventors: Antonio Giordani, Mariangela Biava, Maurizio Anzini, Vicenzo Calderone, Lucio Claudio Rovati
  • Patent number: 8420634
    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: Grant
    Filed: September 22, 2008
    Date of Patent: April 16, 2013
    Assignee: Rottapharm S.p.A.
    Inventors: Maurizio Anzini, Antonio Giordani, Francesco Makovec, Andrea Cappelli, Salvatore Vomero, Gianfranco Caselli, Lucio Claudio Rovati
  • Patent number: 8372866
    Abstract: 2-aryl and 2-heteroaryl 4h-1-benzopyran-4-one-6-amidino derivatives formula (I) useful as pharmacological agents for the treatment of arthritis, cancer and related pain.
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: February 12, 2013
    Assignee: Rottapharm S.p.A.
    Inventors: Antonio Giordani, Sabrina Pucci, Roberto Artusi, Gianfranco Caselli, Marco Lanza, Laura Mennuni, Francesco Makovec, Lucio Claudio Rovati, Stefania Mazza
  • Publication number: 20120289478
    Abstract: New ester derivatives of hyaluronic acid with hydroxy-cinnamic acid, their rheological and anti-radical properties are used as protective agents in dermatology.
    Type: Application
    Filed: May 10, 2012
    Publication date: November 15, 2012
    Applicant: ROTTAPHARM S.p.A.
    Inventor: Lucio Claudio ROVATI
  • Patent number: 8258185
    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: Grant
    Filed: July 27, 2011
    Date of Patent: September 4, 2012
    Assignee: Rottapharm S.p.A.
    Inventors: Francesco Makovec, Gianfranco Caselli, Lucio Claudio Rovati, Antonio Giordani
  • Patent number: 8193353
    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: June 27, 2011
    Date of Patent: June 5, 2012
    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
  • 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
  • Publication number: 20110086896
    Abstract: Described is a new crystalline Form A of Andolast disodium salt, triclinic, displaying a thermal event at 98-112° C. and melting with decomposition at about 400° C. (DSC). Andolast disodium Form A is a not hygroscopic solid, surprisingly stable to several humidity conditions in a temperature range acceptable for ordinary storage conditions. In addition its stability allows both chemical manufacturing and pharmaceutical manufacturing process consistency and reproducibility under conditions more viable and less expensive when compared to those used for highly hygroscopic solids.
    Type: Application
    Filed: September 24, 2010
    Publication date: April 14, 2011
    Applicant: Rottapharm S.p.A.
    Inventors: Antonio GIORDANI, Antonino SANTORO, Paolo SENIN, Matteo GHIRRI, Francesco MAKOVEC, Paola GILOTTA, Walter PERIS, Lucio Claudio ROVATI
  • Publication number: 20110065797
    Abstract: Cholecystokinin-1 (CCK1) receptor antagonists and the combination of CCK1 receptor antagonists and proton pump inhibitors (PPI) for the treatment of patients suffering from gastrointestinal or related disorders that have failed to completely respond to conventional acid suppression therapy.
    Type: Application
    Filed: November 19, 2010
    Publication date: March 17, 2011
    Applicant: ROTTAPHARM S.P.A
    Inventors: Francesco MAKOVEC, Massimo Maria D'AMATO, Antonio GIORDANI, Lucio Claudio ROVATI