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: 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: 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: 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
  • 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
  • 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
  • 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
  • Patent number: 7906501
    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: Grant
    Filed: April 27, 2005
    Date of Patent: March 15, 2011
    Assignee: Rottapharm S.p.A.
    Inventors: Francesco Makovec, Roberto Artusi, Antonio Giordani, Simona Zanzola, 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: 7863330
    Abstract: Combination of dexloxiglumide and a proton pump inhibitor (PPI) for the treatment of patients suffering from functional dyspepsia and gastroesophageal reflux disease (GERD) is disclosed.
    Type: Grant
    Filed: June 14, 2006
    Date of Patent: January 4, 2011
    Assignee: Rottapharm S.p.A.
    Inventors: Francesco Makovec, Massimo Maria D'Amato, Antonio Giordani, Lucio Claudio Rovati