Patents Assigned to Rottapharm S.p.A.
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Patent number: 9623108Abstract: 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: GrantFiled: March 29, 2007Date of Patent: April 18, 2017Assignee: ROTTAPHARM S.p.A.Inventors: Paolo Senin, Ivo Setnikar, Luigi Angelo Rovati
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Patent number: 9174966Abstract: 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: GrantFiled: June 4, 2010Date of Patent: November 3, 2015Assignee: ROTTAPHARM S.P.A.Inventors: Antonio Giordani, Stefano Mandelli, Francesca Porta, Matteo Ghirri, Lucio Claudio Rovati
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Patent number: 9062129Abstract: New ester derivatives of hyaluronic acid with hydroxy-cinnamic acid, their rheological and anti-radical properties are used as protective agents in dermatology.Type: GrantFiled: May 10, 2012Date of Patent: June 23, 2015Assignee: ROTTAPHARM S.p.A.Inventor: Lucio Claudio Rovati
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Publication number: 20140243373Abstract: 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: ApplicationFiled: July 4, 2011Publication date: August 28, 2014Applicant: Rottapharm S.P.A.Inventors: Manuela Borriello, Sabrina Pucci, Luigi Piero Stasi, Lucio Rovati
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Patent number: 8809306Abstract: 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: GrantFiled: July 31, 2006Date of Patent: August 19, 2014Assignee: Rottapharm S.p.A.Inventors: Francesco Makovec, Massimo Maria D'Amato, Antonio Giordani, Lucio Claudio Rovati
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Patent number: 8633208Abstract: 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: GrantFiled: June 20, 2008Date of Patent: January 21, 2014Assignee: Rottapharm S.p.AInventors: Antonio Giordani, Marco Lanza, Gianfranco Caselli, Stefano Mandelli, Simona Zanzola, Francesco Makovec, Lucio Claudio Rovati
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Publication number: 20130310400Abstract: 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: ApplicationFiled: February 2, 2012Publication date: November 21, 2013Applicant: ROTTAPHARM S.P.A.Inventors: Luigi Piero Stasi, Lucio Rovati
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Publication number: 20130165494Abstract: 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: ApplicationFiled: September 7, 2011Publication date: June 27, 2013Applicant: Rottapharm S.p.A.Inventors: Antonio Giordani, Mariangela Biava, Maurizio Anzini, Vicenzo Calderone, Lucio Claudio Rovati
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Patent number: 8420634Abstract: 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: GrantFiled: September 22, 2008Date of Patent: April 16, 2013Assignee: Rottapharm S.p.A.Inventors: Maurizio Anzini, Antonio Giordani, Francesco Makovec, Andrea Cappelli, Salvatore Vomero, Gianfranco Caselli, Lucio Claudio Rovati
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Patent number: 8372866Abstract: 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: GrantFiled: March 6, 2008Date of Patent: February 12, 2013Assignee: Rottapharm S.p.A.Inventors: Antonio Giordani, Sabrina Pucci, Roberto Artusi, Gianfranco Caselli, Marco Lanza, Laura Mennuni, Francesco Makovec, Lucio Claudio Rovati, Stefania Mazza
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Publication number: 20120289478Abstract: New ester derivatives of hyaluronic acid with hydroxy-cinnamic acid, their rheological and anti-radical properties are used as protective agents in dermatology.Type: ApplicationFiled: May 10, 2012Publication date: November 15, 2012Applicant: ROTTAPHARM S.p.A.Inventor: Lucio Claudio ROVATI
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Patent number: 8258185Abstract: 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: GrantFiled: July 27, 2011Date of Patent: September 4, 2012Assignee: Rottapharm S.p.A.Inventors: Francesco Makovec, Gianfranco Caselli, Lucio Claudio Rovati, Antonio Giordani
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Patent number: 8193353Abstract: 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: GrantFiled: June 27, 2011Date of Patent: June 5, 2012Assignee: Rottapharm S.p.AInventors: Antonio Giordani, Stefano Mandelli, Ilario Verpilio, Simona Zanzola, Francesca Tarchino, Gianfranco Caselli, Tiziana Piepoli, Silvio Mazzari, Francesco Makovec, Lucio Claudio Rovati
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Publication number: 20110288173Abstract: 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: ApplicationFiled: July 27, 2011Publication date: November 24, 2011Applicant: ROTTAPHARM S.P.A.Inventors: Francesco MAKOVEC, Gianfranco CASELLI, Lucio Claudio ROVATI, Antonio GIORDANI
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Publication number: 20110257209Abstract: 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: ApplicationFiled: June 27, 2011Publication date: October 20, 2011Applicant: ROTTAPHARM S.P.AInventors: Antonio GIORDANI, Stefano MANDELLI, Ilario VERPILIO, Simona ZANZOLA, Francesca TARCHINO, Gianfranco CASELLI, Tiziana Piepoli, Silvio MAZZARI, Francesco MAKOVEC, Lucio Claudio ROVATI
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Patent number: 7994181Abstract: 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: GrantFiled: August 3, 2006Date of Patent: August 9, 2011Assignee: 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
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Patent number: 7968558Abstract: 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: GrantFiled: July 31, 2006Date of Patent: June 28, 2011Assignee: 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
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Publication number: 20110118289Abstract: 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: ApplicationFiled: June 20, 2008Publication date: May 19, 2011Applicant: ROTTAPHARM S.P.A.Inventors: Antonio Giordani, Marco Lanza, Gianfranco Caselli, Stefano Mandelli, Simona Zanzola, Francesco Makovec, Lucio Claudio Rovati
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Publication number: 20110086896Abstract: 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: ApplicationFiled: September 24, 2010Publication date: April 14, 2011Applicant: Rottapharm S.p.A.Inventors: Antonio GIORDANI, Antonino SANTORO, Paolo SENIN, Matteo GHIRRI, Francesco MAKOVEC, Paola GILOTTA, Walter PERIS, Lucio Claudio ROVATI
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Publication number: 20110065797Abstract: 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: ApplicationFiled: November 19, 2010Publication date: March 17, 2011Applicant: ROTTAPHARM S.P.AInventors: Francesco MAKOVEC, Massimo Maria D'AMATO, Antonio GIORDANI, Lucio Claudio ROVATI