Patents Assigned to Pharmaleads
  • Patent number: 11648231
    Abstract: The present invention concerns a pharmaceutically acceptable salt of a compound of the following formula (I): H2N—CH(R1)—CH2S—S—CH2—CH(R2—CONH—CH(R3)—COOR4 (I) and more particularly an acid addition salt thereof, and the compositions comprising the same, for use in the prevention or treatment of trigeminal nerve pain, in particular migraines or trigeminal neuralgia.
    Type: Grant
    Filed: January 25, 2019
    Date of Patent: May 16, 2023
    Assignee: PHARMALEADS
    Inventors: Hervé Poras, Tanja Ouimet, Marie Claude Fournie Zaluski, Bernard Roques, Michel Wurm
  • Patent number: 11090317
    Abstract: The disclosure relates to compounds of formula (I): R1-NH—CH(R2)-P(?O)(OH)—CH2-C(R3)(R4)-CONH—C(R5)(R6)-COOR7, where R1 to R7 are as defined in the claims, for use of same in the treatment and/or prevention of ocular inflammation, and more particularly for improving the process of ocular healing. Thus, the compounds of formula (I) are used, in particular, to prevent neovascularisation, or to prevent or treat an ocular inflammation linked to a keratitis, scleritis, episcleritis, uveitis, cataract, synechia, macular oedema, detachment of the retina, ocular hypertension and degeneration of the optical nerve caused by glaucoma.
    Type: Grant
    Filed: March 9, 2018
    Date of Patent: August 17, 2021
    Assignee: Pharmaleads
    Inventors: Hervé Poras, Michel Wurm, Stéphane Melik Parsadaniantz, Annabelle Reaux-Le Goazigo
  • Publication number: 20210213036
    Abstract: The disclosure relates to compounds of formula (I): R1-NH—CH(R2)-P(?O)(OH)—CH2-C(R3)(R4)-CONH—C(R5)(R6)-COOR7, where R1 to R7 are as defined in the claims, for use of same in the treatment and/or prevention of ocular inflammation, and more particularly for improving the process of ocular healing. Thus, the compounds of formula (I) are used, in particular, to prevent neovascularisation, or to prevent or treat an ocular inflammation linked to a keratitis, scleritis, episcleritis, uveitis, cataract, synechia, macular oedema, detachment of the retina, ocular hypertension and degeneration of the optical nerve caused by glaucoma.
    Type: Application
    Filed: March 9, 2018
    Publication date: July 15, 2021
    Applicant: PHARMALEADS
    Inventors: Hervé PORAS, Michel WURM, Stéphane MELIK PARSADANIANTZ, Annabelle REAUX-LE GOAZIGO
  • Patent number: 10688113
    Abstract: The disclosure relates to a method of treating or preventing eye pain in a subject in need thereof. The method includes administering a compound of formula (I), R1—NH—CH(R2)—P(?O)(OH)—CH2—C(R3)(R4)—CONH—C(R5)(R6)—COOR7, to the subject.
    Type: Grant
    Filed: February 11, 2019
    Date of Patent: June 23, 2020
    Assignee: PHARMALEADS
    Inventors: Hervé Poras, Michel Wurm, Stéphane Melik Parsadaniantz, Annabelle Reaux-Le Goazigo
  • Patent number: 10399936
    Abstract: The present invention relates to an industrial process for the preparation of (5S,10S)-10-benzyl-16-methyl-11,14,18-trioxo-15,17,19-trioxa-2,7,8-trithia-12-azahenicosan-5-aminium (E)-3-carboxyacrylate salt of following formula (I): wherein X is fumarate. This process comprises the following successive key steps: a kinetic resolution, formation of disulfide compound, peptide coupling, and anion exchange reaction to obtain the desired product of formula (I).
    Type: Grant
    Filed: October 14, 2016
    Date of Patent: September 3, 2019
    Assignee: PHARMALEADS
    Inventors: Herve Poras, Loic Lefebvre, Xinjun Zhao, Luca Gamberoni, Sabrina De Rosa, Rosario Velardi
  • Publication number: 20190167701
    Abstract: The disclosure relates to a method of treating or preventing eye pain in a subject in need thereof. The method includes administering a compound of formula (I), R1—NH—CH(R2)—P(?O)(OH)—CH2—C(R3)(R4)—CONH—C(R5)(R6)—COOR7, to the subject.
    Type: Application
    Filed: February 11, 2019
    Publication date: June 6, 2019
    Applicant: PHARMALEADS
    Inventors: Hervé PORAS, Michel WURM, Stéphane MELIK PARSADANIANTZ, Annabelle REAUX-LE GOAZIGO
  • Publication number: 20180344753
    Abstract: The disclosure relates to formula (I) compounds R1-NH—CH(R2)-P(=0)(OH)—CH2-C(R3)(R4)-CONH—C(R5)(R6)-COOR7 for the use thereof in treating and/or preventing eye pain.
    Type: Application
    Filed: November 30, 2016
    Publication date: December 6, 2018
    Applicant: PHARMALEADS
    Inventors: Hervé PORAS, Michel WURM, Stéphane MELIK PARSADANIANTZ, Annabelle REAUX-LE GOAZIGO
  • Patent number: 10131681
    Abstract: The present invention relates to a compound of the following general formula (I): R1—NH—CH(R2)—P(?O)(OR3)—CH2—C(R4)(R5)—CONH—CH(R6)—COOR7 (I) or a pharmaceutically acceptable salt of the latter, an isomer or a mixture of isomers in any proportions, especially a mixture of enantiomers, and in particular a racemic mixture, for which R1 represents a —C(?O)—O—C(R8)(R9)—OC(?O)—R10 group; R2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle; R3 represents a hydrogen atom or a —C(R12)(R13)—OC(?O)—R14 group; R4 and R5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R4 represents a hydrogen atom and R5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle; R6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substi
    Type: Grant
    Filed: February 18, 2014
    Date of Patent: November 20, 2018
    Assignee: PHARMALEADS
    Inventors: Bernard Roques, Herve Poras, Marie-Claude Fournie-Zaluski
  • Publication number: 20180305308
    Abstract: The present invention relates to an industrial process for the preparation of (5S,10S)-10-benzyl-16-methyl-11,14,18-trioxo-15,17,19-trioxa-2,7,8-trithia-12-azahenicosan-5-aminium (E)-3-carboxyacrylate salt of following formula (I): wherein X is fumarate. This process comprises the following successive key steps: a kinetic resolution, formation of disulfide compound, peptide coupling, and anion exchange reaction to obtain the desired product of formula (I).
    Type: Application
    Filed: October 14, 2015
    Publication date: October 25, 2018
    Applicant: PHARMALEADS
    Inventors: Herve PORAS, Loic LEFEBVRE, Xinjun ZHAO, Luca GAMBERONI, Sabrina DE ROSA, Rosario VELARDI
  • Publication number: 20160206762
    Abstract: The present invention is directed to the use of an irreversible ligand of a serine protease selected from the group consisting of leukocyte elastase, thrombin, tissue plasminogen activator (t-PA) and plasmin for the molecular imaging of said serine protease and the diagnosis of pathophysiological conditions associated with said serine protease activity.
    Type: Application
    Filed: January 20, 2016
    Publication date: July 21, 2016
    Applicants: Institut National de la Sante et de la Recherche Medicale, Pharmaleads, Assistance Publique Hopitaux de Paris, Universite Paris Diderot - Paris 7
    Inventors: Jean-Baptiste Michel, Francois Rouzet, Dominique Leguludec, Herve Poras, Marie-Claude Fournie-Zaluski, Bernard Roques
  • Patent number: 9388129
    Abstract: Mixed inhibitors of aminopeptidase N and neprilysin are disclosed. Pharmaceutical compositions containing at least one of these compounds, used alone or in combination with morphine and derivatives thereof, endocannabinoids and inhibitors of endocannabinoid metabolism, GABA derivatives such as gabapentin or pregabalin, duloxetine or methadone, can be used as an analgesic, anxiolytic, antidepressant or anti-inflammatory.
    Type: Grant
    Filed: October 23, 2013
    Date of Patent: July 12, 2016
    Assignee: PHARMALEADS
    Inventors: Bernard Pierre Roques, Marie-Claude Fournie-Zaluski, Hervé Poras
  • Patent number: 9272054
    Abstract: The present invention is directed to the use of an irreversible ligand of a serine protease selected from the group consisting of leukocyte elastase, thrombin, tissue plasminogen activator (t-PA) and plasmin for the molecular imaging of said serine protease and the diagnosis of pathophysiological conditions associated with said serine protease activity.
    Type: Grant
    Filed: December 5, 2011
    Date of Patent: March 1, 2016
    Assignees: Institut National de la Sante et de la Recherche Medicale (INSERM), Pharmaleads, Assistance Publique Hopitaux de Paris, Universite Paris Diderot-Paris 7
    Inventors: Jean-Baptiste Michel, François Rouzet, Dominique Leguludec, Hervé Poras, Marie-Claude Fournie-Zaluski, Bernard Rogues
  • Publication number: 20150299116
    Abstract: Mixed inhibitors of aminopeptidase N and neprilysin are disclosed. Pharmaceutical compositions containing at least one of these compounds, used alone or in combination with morphine and derivatives thereof, endocannabinoids and inhibitors of endocannabinoid metabolism, GABA derivatives such as gabapentin or pregabalin, duloxetine or methadone, can be used as an analgesic, anxiolytic, antidepressant or anti-inflammatory.
    Type: Application
    Filed: October 23, 2013
    Publication date: October 22, 2015
    Applicant: PHARMALEADS
    Inventors: Bernard Pierre ROQUES, Marie-Claude FOURNIE-ZALUSKI, Hervé PORAS
  • Publication number: 20140161839
    Abstract: The present invention relates to a compound of the following general formula (I): R1—NH—CH(R2)—P(?O)(OR3)—CH2—C(R4)(R5)—CONH—CH(R6)—COOR7 (I) or a pharmaceutically acceptable salt of the latter, an isomer or a mixture of isomers in any proportions, especially a mixture of enantiomers, and in particular a racemic mixture, for which R1 represents a —C(?O)—O—C(R8)(R9)—OC(?O)—R10 group; R2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle; R3 represents a hydrogen atom or a —C(R12)(R13)—OC(?O)—R14 group; R4 and R5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R4 represents a hydrogen atom and R5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle; R6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substi
    Type: Application
    Filed: February 18, 2014
    Publication date: June 12, 2014
    Applicant: PHARMALEADS
    Inventors: Bernard Roques, Herve Poras, Marie-Claude Fournie-Zaluski
  • Patent number: 8703747
    Abstract: The present invention relates to a compound of the following general formula (I): R1—NH—CH(R2)—P(?O)(OR3)—CH2—C(R4)(R5)—CONH—CH(R6)—COOR7 (I) or a pharmaceutically acceptable salt of the latter, an isomer or a mixture of isomers in any proportions, especially a mixture of enantiomers, and in particular a racemic mixture, for which R1 represents a —C(?O)—O—C(R8)(R9)—OC(?O)—R10 group; R2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle; R3 represents a hydrogen atom or a —C(R12)(R13)—OC(?O)—R14 group; R4 and R5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R4 represents a hydrogen atom and R5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle; R6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substi
    Type: Grant
    Filed: July 22, 2009
    Date of Patent: April 22, 2014
    Assignee: Pharmaleads
    Inventors: Bernard Roques, Hervé Poras, Marie-Claude Fournie-Zaluski
  • Publication number: 20130243691
    Abstract: The present invention is directed to the use of an irreversible ligand of a serine protease selected from the group consisting of leukocyte elastase, thrombin, tissue plasminogen activator (t-PA) and plasmin for the molecular imaging of said serine protease and the diagnosis of pathophysiological conditions associated with said serine protease activity.
    Type: Application
    Filed: December 5, 2011
    Publication date: September 19, 2013
    Applicant: PHARMALEADS
    Inventors: Jean-Baptiste Michel, François Rouzet, Dominique Leguludec, Hervé Poras, Marie-Claude Fournie-Zaluski, Bernard Roques
  • Publication number: 20130203097
    Abstract: The present disclosure includes the use of an R—(X)n-Fluo-Rep-(Gly)m-Z—NH2 peptide for detecting and assaying the activity of the major surface protease of Legionella pneumophilia. This disclosure also includes a method for detecting and quantifying Legionella pneumophilia in any medium likely to be contaminated with the bacterium, for example a domestic hot water supply and cooling tower circuits.
    Type: Application
    Filed: July 21, 2011
    Publication date: August 8, 2013
    Applicant: PHARMALEADS
    Inventors: Herve Poras, Tanja Ouimet, Marie-Claude Fournie-Zaluski
  • Patent number: 8247608
    Abstract: The invention relates to novel compounds of formula (I): H2N—CH(R1)—CH2—S—S—CH2—CH(R2)—CONH—R5, wherein R1 is a hydrocarbon chain, phenyl or benzyl radical, methylene radical substituted by a 5 or 6 atom heterocycle; R2 is a phenyl or benzyl radical, a 5 or 6 atom aromatic heterocycle, methylene group substituted by a 5 or 6 atom heterocycle; R5 is a CH(R3)—COOR4 radical, wherein R3 is hydrogen, an OH or OR group, a saturated hydrocarbon group, a phenyl or benzyl radical and OR4 is hydrophile ester, or 5 or 6 membered heterocycle comprising several heteroatoms selected from a group consisting of nitrogen, sulphur and oxygen, with at least two nitrogene atoms, wherein said heterocycle is substitutable by an alkyl C1-C6, phenyl or benzyl radical.
    Type: Grant
    Filed: October 24, 2006
    Date of Patent: August 21, 2012
    Assignee: Pharmaleads
    Inventors: Bernard Roques, Marie-Claude Fournie-Zaluski
  • Publication number: 20110071218
    Abstract: The disclosure relates to novel compounds of the formula (I) R1NH—CH(R2)CH2—S—S—CH2—C(R3)(R4)—CONH—C(R5)(R6)—COOR7, in which R1 is a (acyloxy)alkyl carbamate-C(O)—O—C(R8)(R9)—OC(O)—R10 group; R2 is a hydrocarbon chain, a methylene radical substituted by a heterocycle, R4 is a hydrogen atom and R3 is a phenyl or benzyl radical, a heteroaryl, a methylene group substituted by a heterocycle or R3 and R4 form together a saturated cycle; R5 and R6 are hydrogen, a hydrocarbon chain, a phenyl or benzyl radical or R5 and R6 form together a saturated cycle; R7 is hydrogen, a phenyl or benzyl radical, a group of the formula CR12(R13)C(O)OR14 or OCR12(R13)OC(O)R14 or OCR12(R13)OC(O)OR14. The disclosure also relates to the use of these compounds as a drug, and to a pharmaceutical composition containing said compounds and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: May 13, 2009
    Publication date: March 24, 2011
    Applicant: PHARMALEADS
    Inventors: Marie-Claude Fournie-Zaluski, Hervé Poras, Bernard Roques
  • Patent number: 7875436
    Abstract: A peptide substrate selectively recognisable by a botulinum toxin A, BoNT/A containing a Nop-(Z)-Pya fragment in the peptide structure thereof, wherein Z is an aminoacid chain, preferably RA and the fragment is cleaved by the toxin.
    Type: Grant
    Filed: May 4, 2005
    Date of Patent: January 25, 2011
    Assignee: Pharmaleads
    Inventors: Marie-Claude Fournie-Zaluski, Bernard Pierre Roques