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.

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.

Abstract: The present invention relates to a method for the industrial preparation of ((2S)-3-([1,1?-biphenyl]-4-yl)-2-((((R)-1-aminoethyl)(hydroxy)phosphoryl)methyl)propanoyl)-L-alanine acid of following formula (E): from (S)-1-phenylethylamine via a multi-step synthesis. The present invention pertains to a method for the industrial preparation of the disodium salt of ((2S)-3-([1,1?-biphenyl]-4-yl)-2-((hydroxy((1R)-1-(((1-(isobutyryloxy)ethoxy)carbonyl)amino)ethyl)phosphoryl)methyl)propanoyl)-L-alanine of following formula (I): in two additional steps from the compound (E) such as defined above. The present invention also pertains to a method for diastereoisomeric enrichment of the intermediates of the method for the industrial preparation of the compound of formula (E) of the present invention.

Abstract: The present invention relates to a compound of following formula (I): H—CO—N(OH)—CH2—CH(R1)—CO—NH—(CH2)n—CH(R2)—(CH2)m—CO—R3??(I) as well as a pharmaceutically acceptable salt and/or solvate thereof. The present invention also pertains to a pharmaceutical composition comprising at least one compound of formula (I) and at least one pharmaceutically acceptable excipient. The present invention also relates to the use of a compound of formula (I), or a pharmaceutically acceptable salt and/or solvate thereof, or a composition comprising it, as analgesic, anxiolytic, antidepressant or anti-inflammatory.

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.

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.

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.

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.

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).

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.

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.

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

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).

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.

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.

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.

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.

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

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

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.