Patents by Inventor Lucio Claudio Rovati

Lucio Claudio Rovati 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: 20240091227
    Abstract: The invention concerns a compound of formula 2-phenyl-6-(1H-imidazol-1-yl)quinazoline or a pharmaceutically acceptable salt thereof for use in the treatment of a neurodegenerative disease.
    Type: Application
    Filed: November 7, 2023
    Publication date: March 21, 2024
    Inventors: Lucio Claudio Rovati, Gianfranco Caselli, Emanuele Sala
  • Patent number: 11718582
    Abstract: The following invention relates to (R)-4-(1-(1-(4-(trifluoromethyl)benzyl) pyrrodiline-2-carboxamide) cyclopropyl benzoic acid (Compound 1) or a salt thereof. Advantageous methods for obtaining the Compound 1 are also described, as well as pharmaceutical compositions containing it (R)-4-(1-(1-(4-(trifluoromethyl)benzyl)pyrrodiline-2-carboxamide) cyclopropyl benzoic acid (Compound 1) or a pharmaceutically acceptable salt thereof is described for use as an EP4 receptor antagonist in the treatment of a pathology that involves the activities of prostaglandin E2 (PGE2) in its pathogenesis.
    Type: Grant
    Filed: July 4, 2019
    Date of Patent: August 8, 2023
    Assignee: ROTTAPHARM BIOTECH S.R.L.
    Inventors: Sabrina Pucci, Francesco Makovec, Lucio Claudio Rovati
  • Publication number: 20230127805
    Abstract: The present invention provides a process for preparing (R)-6-(tert-butoxycarbonyl)-6-azaspiro[2.5]octane-5-carboxylic acid (SM1), said process comprising the step of: iv) converting a compound of formula (VII) into a compound of formula (VIII) using a Wittig reagent in a suitable solvent; v) reacting through the Makosza reaction the compound of Formula (VIII) using bromoform and a suitable base to obtain cyclopropane compound of Formula (IX); and vi) removing bromine atoms in the presence of a reducing agent and a base in an alcoholic solvent thus obtaining (SM1). The invention relates also to a process for the conversion of the compound (SM1) for preparing (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl) benzoic acid (IV) or a salt thereof. The salt is preferably the sodium salt, more preferably the polymorphic form A of sodium (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.
    Type: Application
    Filed: March 19, 2021
    Publication date: April 27, 2023
    Inventors: Lucio Claudio Rovati, Roberto Artusi, Filippo Magaraci, Benedetta Buzzi
  • Publication number: 20230122048
    Abstract: The present invention provides a pharmaceutical combination comprising the EP4 antagonist of Formula (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl)-benzoic acid or a pharmaceutically acceptable salt thereof and at least one immune checkpoint inhibitor, preferably the sodium salt of (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl) benzoic acid. A polymorphic form A of sodium salt of (R)-4-(1-(6-(4-(trifluoromethyl) benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl)benzoate characterized by a powder XRD spectrum with peaks at values of the angle 2? ±0.2° of 4.3, 5.0, 5.8, 6.4, 7.1, 8.3, 8.7, 12.8, 15.3, 15.9 is also described. The combination and the polymorphic form A are described for use in the treatment of tumours.
    Type: Application
    Filed: October 26, 2022
    Publication date: April 20, 2023
    Inventors: Lucio Claudio Rovati, Antonio Giordani, Filippo Magaraci, Giafrano Caselli, Tiziana Piepoll, Daniele Maggioni, Albino Bonazzi
  • Publication number: 20230061118
    Abstract: The invention relates to a N-phenylcarbamoyl compound of Formula (I) or a pharmaceutically acceptable salt thereof for use in the inhibition of at least one of tyrosine kinase selected from Fyn and VEGFR2 in the treatment of diseases and disorders involved with one or both kinases.
    Type: Application
    Filed: December 7, 2020
    Publication date: March 2, 2023
    Inventors: Lucio Claudio Rovati, Gianfranco Caselli, Roberto Artusi, Laura Mennuni, Fabrizio Colace, Stefano Mandelli, Clara Bovino, Filippo Magaraci, Benedetta Buzzi
  • Patent number: 11590114
    Abstract: The present invention provides a pharmaceutical combination comprising the EP4 antagonist of Formula (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl)-benzoic acid or a pharmaceutically acceptable salt thereof and at least one immune checkpoint inhibitor, preferably the sodium salt of (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl) benzoic acid. A polymorphic form A of sodium salt of (R)-4-(1-(6-(4-(trifluoromethyl) benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl)benzoate characterized by a powder XRD spectrum with peaks at values of the angle 2?+0.2° of 4.3, 5.0, 5.8, 6.4, 7.1, 8.3, 8.7, 12.8, 15.3, 15.9 is also described. The combination and the polymorphic form A are described for use in the treatment of tumours.
    Type: Grant
    Filed: April 8, 2020
    Date of Patent: February 28, 2023
    Assignee: ROTTAPHARM BIOTECH S.R.L.
    Inventors: Lucio Claudio Rovati, Antonio Giordani, Filippo Magaraci, Gianfranco Caselli, Tiziana Piepoli, Daniele Maggioni, Albino Bonazzi
  • Publication number: 20230028519
    Abstract: There is described a compound of formula (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)-cyclopropyl)benzoic acid or a pharmaceutically acceptable salt thereof or the form A of its sodium salt for use in the prevention of heterotopic ossification. Preferably such a compound is effective in a specific dose range.
    Type: Application
    Filed: November 27, 2020
    Publication date: January 26, 2023
    Inventors: Lucio Claudio ROVATI, Gianfranco CASELLI, Tiziana PIEPOLI
  • Publication number: 20230000868
    Abstract: The present invention relates to a compound of formula 2-phenyl-6-(1H-imidazol-1-yl) quinazoline (CR4056) or a pharmaceutically acceptable salt thereof for use in the prevention of abuse in an opioid non-addicted subject and other side effects of at least one opioid. The invention also relates to a composition or a pharmaceutical kit comprising a compound of formula 2-phenyl-6-(1Himidazol-1-yl) quinazoline (CR4056) or one of its pharmaceutically acceptable salts and at least one opioid for use in the prevention of abuse in an opioid non-addicted subject and other side effects of at least one opioid.
    Type: Application
    Filed: November 27, 2020
    Publication date: January 5, 2023
    Inventor: Lucio Claudio ROVATI
  • Publication number: 20220257598
    Abstract: The invention concerns a compound of formula 2-phenyl-6-(1H-imidazol-1-yl)quinazoline or a pharmaceutically acceptable salt thereof for use in the treatment of a neurodegenerative disease. The neurodegenerative disease is a disease selected from the group consisting of Alzheimer's disease, Lewy body dementia, frontotemporal dementia, amyotrophic lateral sclerosis, Huntington disease, prion diseases, HIV-associated dementia and any form of cognitive disorders linked to neurodegeneration, preferably Alzheimer's disease.
    Type: Application
    Filed: May 8, 2020
    Publication date: August 18, 2022
    Inventors: Lucio Claudio Rovati, Gianfranco CASELLI, Emanuele SALA
  • Publication number: 20220142996
    Abstract: The present invention provides a pharmaceutical combination comprising the EP4 antagonist of Formula (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl)-benzoic acid or a pharmaceutically acceptable salt thereof and at least one immune checkpoint inhibitor, preferably the sodium salt of (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl) benzoic acid. A polymorphic form A of sodium salt of (R)-4-(1-(6-(4-(trifluoromethyl) benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl)benzoate characterized by a powder XRD spectrum with peaks at values of the angle 2?+0.2° of 4.3, 5.0, 5.8, 6.4, 7.1, 8.3, 8.7, 12.8, 15.3, 15.9 is also described. The combination and the polymorphic form A are described for use in the treatment of tumours.
    Type: Application
    Filed: April 8, 2020
    Publication date: May 12, 2022
    Inventors: Lucio Claudio Rovati, Antonio GIORDANI, Filippo MAGARAACI, Gianfranco CASELLI, Tiziana PIEPOLI, Daniele MAGGIONI, Albino BONAZZI
  • Publication number: 20220041559
    Abstract: The invention relates to new chemical compounds of Formula (I), pharmaceutical compositions containing them, and their use for the pharmacological treatment of a cancer, preferably a glioblastoma.
    Type: Application
    Filed: April 16, 2020
    Publication date: February 10, 2022
    Inventors: Lucio Claudio Rovati, Roberto ARTUSI, Clara BOVINO, Stefano MANDELLI, Fabrizio COLACE, Benedetta BUZZI, Tiziana PIEPOLI
  • Publication number: 20210130290
    Abstract: The following invention relates to (R)-4-(1-(1-(4-(trifluoromethyl)benzyl) pyrrodiline-2-carboxamide) cyclopropyl benzoic acid (Compound 1) or a salt thereof. Advantageous methods for obtaining the Compound 1 are also described, as well as pharmaceutical compositions containing it (R)-4-(1-(1-(4-(trifluoromethyl)benzyl)pyrrodiline-2-carboxamide) cyclopropyl benzoic acid (Compound 1) or a pharmaceutically acceptable salt thereof is described for use as an EP4 receptor antagonist in the treatment of a pathology that involves the activities of prostaglandin E2 (PGE2) in its pathogenesis.
    Type: Application
    Filed: July 4, 2019
    Publication date: May 6, 2021
    Inventors: Sabrina PUCCI, Francesco MAKOVEC, Lucio Claudio ROVATI
  • Patent number: 9631029
    Abstract: The present invention relates to an antibody, recombinant or synthetic antigen-binding fragments thereof able to recognize and bind an epitope comprised in the spacer domain of ADAMTS-5, nucleic acid and expression vector encoding the same, method of production and uses thereof.
    Type: Grant
    Filed: April 12, 2013
    Date of Patent: April 25, 2017
    Assignee: ROTTAPHARM BIOTECH S.R.L.
    Inventors: Riccardo Chiusaroli, Michela Visintin, Gianfranco Caselli, Lucio Claudio Rovati
  • Publication number: 20160244529
    Abstract: The present invention relates to an antibody, recombinant or synthetic antigen-binding fragments thereof able to recognise and bind an epitope comprised in the TrkA amino acid sequence, medical uses thereof and a pharmaceutical composition comprising at least one of the above antibody, recombinant or synthetic antigen-binding fragments thereof.
    Type: Application
    Filed: May 12, 2016
    Publication date: August 25, 2016
    Inventors: Lucio Claudio ROVATI, Michela VISINTIN, Gianfranco CASELLI, Gabriele UGOLINI
  • Patent number: 9365654
    Abstract: The present invention relates to an antibody, recombinant or synthetic antigen-binding fragments thereof able to recognize and bind an epitope comprised in the TrkA amino acid sequence, medical uses thereof and a pharmaceutical composition comprising at least one of the above antibody, recombinant or synthetic antigen-binding fragments thereof.
    Type: Grant
    Filed: May 15, 2013
    Date of Patent: June 14, 2016
    Assignee: ROTTAPHARM BIOTECH S.R.L.
    Inventors: Lucio Claudio Rovati, Michela Visintin, Gianfranco Caselli, Gabriele Ugolini
  • Patent number: 9248115
    Abstract: The invention relates to the use of a silibinin component for the production of a medicament that is adapted for parenteral administration for the treatment of viral hepatitis, preferably of hepatitis B or C, in particular for the reduction of the virus load. The medicament preferably contains no silidianin and/or no silichristin and/or no isosilibinin.
    Type: Grant
    Filed: April 26, 2013
    Date of Patent: February 2, 2016
    Assignee: MADAUS GMBH
    Inventors: Lucio Claudio Rovati, Massimo Maria D'Amato, Ulrich Mengs, Ralf-Torsten Pohl, Peter Ferenci
  • Patent number: 9174977
    Abstract: The present invention provides compounds of formula (I) including stereoisomers or a racemate or a mixture or a pharmaceutically acceptable salt thereof: wherein X is NH, or O; Q is 5-6 membered heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; A is phenyl or a 5-6 heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; B may assume different meanings from A and is phenyl or a 5-6 membered heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; and processes for their preparation, pharmaceutical compositions containing them and their use as dual antagonists of the Orexin 1 and Orexin 2 receptors.
    Type: Grant
    Filed: March 18, 2013
    Date of Patent: November 3, 2015
    Assignee: Rottapharm Biotech S.R.L.
    Inventors: Luigi Piero Stasi, Lucio Claudio 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: 9162979
    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: Grant
    Filed: September 7, 2011
    Date of Patent: October 20, 2015
    Assignee: ROTTAPHARM BIOTECH S.R.L.
    Inventors: Antonio Giordani, Mariangela Biava, Maurizio Anzini, Vincenzo Calderone, Lucio Claudio Rovati
  • Patent number: 9062033
    Abstract: The invention relates to a novel compound of formula (I) or a stereoisomer, or a racemate or a mixture or a pharmaceutically acceptable salt thereof: wherein: R is phenyl or a 5- or 6-membered heteroaryl ring containing 1 to 3 heteroatoms selected from S, N and O, such rings may be optionally substituted with n groups Q; Q is selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN, SO2CH3 or a group —O[(CR1R2]pQ1; or Q may be a group Q2; Q1 is phenyl, which may be optionally substituted with n substituents selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN, or a group Q2; or corresponds to 2,2-difluoro-benzo[d][1,3]dioxol-4-yl; Q2 is a 5- or 6-membered heteroaryl containing at least one nitrogen atom, which may optionally substituted with n substituents selected from a group consisting of: C1 C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; P is a 6-membered heteroaryl or a 8-1 1 membered bicyclic heteroaryl group, which
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: June 23, 2015
    Assignee: Rottapharm Biotech S.R.L.
    Inventors: Luigi Piero Stasi, Lucio Claudio Rovati, Roberto Artusi, Fabrizio Colace, Stefano Mandelli, Lorenzo Perugini