Patents by Inventor Francesco Makovec

Francesco Makovec 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).

  • 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
  • Patent number: 7824710
    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: Grant
    Filed: February 23, 2007
    Date of Patent: November 2, 2010
    Assignee: Rottapharm S.p.A.
    Inventors: Antonio Giordani, Antonino Santoro, Paolo Senin, Matteo Ghirri, Francesco Makovec, Paola Gilotta, Walter Peris, Lucio Claudio Rovati
  • 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: 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
  • Patent number: 7737180
    Abstract: Use of neboglamine, (S)-4-amino-N-(4,4-dimethylcyclohexyl)glutamic acid (CR 2249) (CAS Registry Number 163000-63-3), of the racemate thereof or of a pharmaceutically acceptable salt thereof for the preparation of a medicament for the treatment of schizophrenia.
    Type: Grant
    Filed: May 23, 2005
    Date of Patent: June 15, 2010
    Assignee: Rottapharm S.p.A.
    Inventors: Francesco Makovec, Lucio Claudio Rovati
  • Publication number: 20100120802
    Abstract: Heterocyclic amidines with anti-inflammatory and analgesic activity that inhibit nitrogen oxide production, of formula (I): in which: G1 and G2 are hydrogen, halogen, hydroxyl, C1-C4 alkoxy, C1-C4 alkyl, and an amidino substituent of formula Q, provided that, for each compound of formula (I), only one of the two substituents G1 or G2 is an amidino substituent of formula Q: and in which the substituents W, Y and X are combined to form 9- or 10-membered bicyclic heteroaromatic derivatives containing up to 2 hetero atoms in the same ring; and Z is an aryl or heteroaryl group, a linear or branched C1-C6 alkyl or alkenyl chain, a C1-C4 alkyl-aryl group or a C1-C4 alkyl-heteroaryl group.
    Type: Application
    Filed: January 15, 2010
    Publication date: May 13, 2010
    Inventors: Francesco MAKOVEC, Antonio Giordani, Roberto Artusi, Stefano Mandelli, Ilario Verpiliq, Simona Zanzola, Lucio Claudio Rovati
  • Patent number: 7674809
    Abstract: Heterocyclic amidines with anti-inflammatory and analgesic activity that inhibit nitrogen oxide production, of formula (I): in which: G1 and G2 are hydrogen, halogen, hydroxyl, C1-C4 alkoxy, C1-C4 alkyl, and an amidino substituent of formula Q, provided that, for each compound of formula (I), only one of the two substituents G1 or G2 is an amidino substituent of formula Q: and in which the substituents W, Y and X are combined to form 9- or 10-membered bicyclic heteroaromatic derivatives containing up to 2 hetero atoms in the same ring; and Z is an aryl or heteroaryl group, a linear or branched C1-C6 alkyl or alkenyl chain, a C1-C4 alkyl-aryl group or a C1-C4 alkyl-heteroaryl group.
    Type: Grant
    Filed: March 1, 2005
    Date of Patent: March 9, 2010
    Assignee: Rottapharm S.p.A.
    Inventors: Francesco Makovec, Antonio Giordani, Roberto Artusi, Stefano Mandelli, Ilario Verpilio, Simona Zanzola, Lucio Claudio Rovati
  • Patent number: 7662994
    Abstract: The present invention describes a novel method for the purification of dexloxiglumide by crystallization from isopropyl ether which permits the production, in a reproducible manner, of a product with morphological and particle-size characteristics such as to favor its use in the preparation of oral pharmaceutical forms on an industrial scale.
    Type: Grant
    Filed: June 21, 2004
    Date of Patent: February 16, 2010
    Assignee: Rottapharm S.p.A.
    Inventors: Francesco Makovec, 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: 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: 20090253664
    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: Application
    Filed: July 31, 2006
    Publication date: October 8, 2009
    Inventors: Francesco Makovec, Massimo Maria D'Amato, Antonio Giordani, 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: 7560591
    Abstract: Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta p
    Type: Grant
    Filed: April 30, 2008
    Date of Patent: July 14, 2009
    Assignee: Rotta Research Laboratorium S.p.A.
    Inventors: Francesco Makovec, Simona Zanzola, Roberto Artusi, Lucio Claudio Rovati
  • Publication number: 20080207764
    Abstract: Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta p
    Type: Application
    Filed: April 30, 2008
    Publication date: August 28, 2008
    Applicant: ROTTA RESEARCH LABORATORIUM S.p.A.
    Inventors: Francesco Makovec, Simona Zanzola, Roberto Artusi, Lucio Claudio Rovati
  • 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: 20070293574
    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: June 14, 2006
    Publication date: December 20, 2007
    Applicant: ROTTAPHARM S.p.A.
    Inventors: Francesco MAKOVEC, Massimo Maria D'Amato, Antonio Giordani, Lucio Claudio Rovati
  • Patent number: 7294648
    Abstract: Anthranylic compounds having anti-CCK activity of general formula (I) in which, n is a whole number lying between 0 and 7; R1 is chosen independently from the groups (II), in which X1 is chosen independently from, S, O, NR2 and X2 is a group chosen from: H, C1-C4 alkyl, F, Cl, CF3, OCH3, OC2H5, CN; R2 is chosen from H or CH3; R3 is chosen from H, CH3, F, Cl, CF3, OCH3; R4 is chosen from the groups: H, —S—(CH2)m-R5, —SO2—(CH2)m-R5 (n different from 0), a branched alkyl group, a cyclo alkyl, a cyclo alkenyl, the group 1 or 2 adamantile, a phenyl group optionally substituted; R5 is chosen from the groups: H, linear or branched alkyl, cyclo alkyl, the group 1 or 2 adamantile, a suitably substituted phenyl group
    Type: Grant
    Filed: July 23, 2003
    Date of Patent: November 13, 2007
    Assignee: Rottapharm S.p.A.
    Inventors: Francesco Makovec, Antonio Varnavas, Lucia Lassiani, Lucio Claudio Rovati
  • Publication number: 20070249715
    Abstract: Use of neboglamine, (S)-4-amino-N-(4,4-dimethylcyclohexyl)glutamic acid (CR 2249) (CAS Registry Number 163000-63-3), of the racemate thereof or of a pharmaceutically acceptable salt thereof for the preparation of a medicament for the treatment of schizophrenia.
    Type: Application
    Filed: May 23, 2005
    Publication date: October 25, 2007
    Applicant: ROTTAPHARM, S.P.A.
    Inventors: Francesco Makovec, Lucio Rovati
  • Publication number: 20070244170
    Abstract: Compounds which may be represented by the general formula (I) shown below and in which: R1 is a group independently selected from among: CHO, —COOH, —CH2OH R2 is hydrogen or a linear or branched C1-C6 alkyl group R3 is hydrogen or a halogen group selected from among Cl and Br R4 is a linear or branched C3-C5 alkyl group and the pharmaceutically acceptable salts thereof such as the sodium or potassium salt. The compounds exhibit potent and selective All antagonist activity and are useful for the treatment of any disorders in which elevated synthesis of All or overexpression of the AT1 receptor may play a primary pathological role, as in the case of arterial hypertension, congestive cardiac insufficiency, platelet aggregation and disorders associated therewith such as for example myocardial and cerebral infarction, renal ischaemia, venous and arterial thrombosis, peripheral vasculopathy, pulmonary hypertension, diabetes mellitus, diabetic neuropathy, glaucoma and diabetic retinopathy.
    Type: Application
    Filed: April 27, 2005
    Publication date: October 18, 2007
    Inventors: Francesco Makovec, Roberto Artusi, Antonio Giordani, Simona Zanzola, Lucio Rovati
  • Publication number: 20070149586
    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: February 23, 2007
    Publication date: June 28, 2007
    Applicant: ROTTAPHARM S.P.A.
    Inventors: Antonio Giordani, Antonino Santoro, Paolo Senin, Matteo Ghirri, Francesco Makovec, PaoLa Gilotta, Walter Peris, Lucio Claudio Rovati