Patents Assigned to Pharmaleads
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Patent number: 11648231Abstract: 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: GrantFiled: January 25, 2019Date of Patent: May 16, 2023Assignee: PHARMALEADSInventors: Hervé Poras, Tanja Ouimet, Marie Claude Fournie Zaluski, Bernard Roques, Michel Wurm
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Patent number: 11090317Abstract: 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: GrantFiled: March 9, 2018Date of Patent: August 17, 2021Assignee: PharmaleadsInventors: Hervé Poras, Michel Wurm, Stéphane Melik Parsadaniantz, Annabelle Reaux-Le Goazigo
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Publication number: 20210213036Abstract: 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: ApplicationFiled: March 9, 2018Publication date: July 15, 2021Applicant: PHARMALEADSInventors: Hervé PORAS, Michel WURM, Stéphane MELIK PARSADANIANTZ, Annabelle REAUX-LE GOAZIGO
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Patent number: 10688113Abstract: 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: GrantFiled: February 11, 2019Date of Patent: June 23, 2020Assignee: PHARMALEADSInventors: Hervé Poras, Michel Wurm, Stéphane Melik Parsadaniantz, Annabelle Reaux-Le Goazigo
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Patent number: 10399936Abstract: 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: GrantFiled: October 14, 2016Date of Patent: September 3, 2019Assignee: PHARMALEADSInventors: Herve Poras, Loic Lefebvre, Xinjun Zhao, Luca Gamberoni, Sabrina De Rosa, Rosario Velardi
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Publication number: 20190167701Abstract: 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: ApplicationFiled: February 11, 2019Publication date: June 6, 2019Applicant: PHARMALEADSInventors: Hervé PORAS, Michel WURM, Stéphane MELIK PARSADANIANTZ, Annabelle REAUX-LE GOAZIGO
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Publication number: 20180344753Abstract: 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: ApplicationFiled: November 30, 2016Publication date: December 6, 2018Applicant: PHARMALEADSInventors: Hervé PORAS, Michel WURM, Stéphane MELIK PARSADANIANTZ, Annabelle REAUX-LE GOAZIGO
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Patent number: 10131681Abstract: 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 substiType: GrantFiled: February 18, 2014Date of Patent: November 20, 2018Assignee: PHARMALEADSInventors: Bernard Roques, Herve Poras, Marie-Claude Fournie-Zaluski
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Publication number: 20180305308Abstract: 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: ApplicationFiled: October 14, 2015Publication date: October 25, 2018Applicant: PHARMALEADSInventors: Herve PORAS, Loic LEFEBVRE, Xinjun ZHAO, Luca GAMBERONI, Sabrina DE ROSA, Rosario VELARDI
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Publication number: 20160206762Abstract: 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: ApplicationFiled: January 20, 2016Publication date: July 21, 2016Applicants: Institut National de la Sante et de la Recherche Medicale, Pharmaleads, Assistance Publique Hopitaux de Paris, Universite Paris Diderot - Paris 7Inventors: Jean-Baptiste Michel, Francois Rouzet, Dominique Leguludec, Herve Poras, Marie-Claude Fournie-Zaluski, Bernard Roques
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Patent number: 9388129Abstract: 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: GrantFiled: October 23, 2013Date of Patent: July 12, 2016Assignee: PHARMALEADSInventors: Bernard Pierre Roques, Marie-Claude Fournie-Zaluski, Hervé Poras
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Patent number: 9272054Abstract: 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: GrantFiled: December 5, 2011Date of Patent: March 1, 2016Assignees: Institut National de la Sante et de la Recherche Medicale (INSERM), Pharmaleads, Assistance Publique Hopitaux de Paris, Universite Paris Diderot-Paris 7Inventors: Jean-Baptiste Michel, François Rouzet, Dominique Leguludec, Hervé Poras, Marie-Claude Fournie-Zaluski, Bernard Rogues
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Publication number: 20150299116Abstract: 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: ApplicationFiled: October 23, 2013Publication date: October 22, 2015Applicant: PHARMALEADSInventors: Bernard Pierre ROQUES, Marie-Claude FOURNIE-ZALUSKI, Hervé PORAS
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Publication number: 20140161839Abstract: 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 substiType: ApplicationFiled: February 18, 2014Publication date: June 12, 2014Applicant: PHARMALEADSInventors: Bernard Roques, Herve Poras, Marie-Claude Fournie-Zaluski
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Patent number: 8703747Abstract: 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 substiType: GrantFiled: July 22, 2009Date of Patent: April 22, 2014Assignee: PharmaleadsInventors: Bernard Roques, Hervé Poras, Marie-Claude Fournie-Zaluski
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Publication number: 20130243691Abstract: 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: ApplicationFiled: December 5, 2011Publication date: September 19, 2013Applicant: PHARMALEADSInventors: Jean-Baptiste Michel, François Rouzet, Dominique Leguludec, Hervé Poras, Marie-Claude Fournie-Zaluski, Bernard Roques
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Publication number: 20130203097Abstract: 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: ApplicationFiled: July 21, 2011Publication date: August 8, 2013Applicant: PHARMALEADSInventors: Herve Poras, Tanja Ouimet, Marie-Claude Fournie-Zaluski
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Patent number: 8247608Abstract: 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: GrantFiled: October 24, 2006Date of Patent: August 21, 2012Assignee: PharmaleadsInventors: Bernard Roques, Marie-Claude Fournie-Zaluski
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Publication number: 20110071218Abstract: 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: ApplicationFiled: May 13, 2009Publication date: March 24, 2011Applicant: PHARMALEADSInventors: Marie-Claude Fournie-Zaluski, Hervé Poras, Bernard Roques
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Patent number: 7875436Abstract: 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: GrantFiled: May 4, 2005Date of Patent: January 25, 2011Assignee: PharmaleadsInventors: Marie-Claude Fournie-Zaluski, Bernard Pierre Roques