Patent classifications
A61K31/67
Aminophosphinic derivatives that can be used in the treatment of pain
The present invention relates to a compound of the following general formula (I): R.sub.1NHCH(R.sub.2)P(O)(OR.sub.3)CH.sub.2C(R.sub.4)(R.sub.5)CONHCH(R.sub.6)COOR.sub.7 (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 R.sub.1 represents a C(O)OC(R.sup.8)(R.sup.9)OC(O)R.sup.10 group; R.sub.2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle; R.sub.3 represents a hydrogen atom or a C(R.sup.12)(R.sup.13)OC(O)R.sup.14 group; R.sub.4 and R.sub.5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R.sub.4 represents a hydrogen atom and R.sub.5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle; R.sub.6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substituted; and R.sub.7 represents a hydrogen atom or a benzyl, alkyl, heteroaryl, alkylheteroaryl, CHMe-COOR.sup.18, CHR.sup.19OC(O)R.sup.20 and CHR.sup.19OC(O)OR.sup.20 group. The present invention also relates to the use of these compounds as a medicinal product, and in particular for the treatment of pain, more advantageously neuropathic and neuroinflammatory pain, to their method of synthesis and also to the compositions containing them.
PHOSPHINIC PEPTIDE DERIVATIVES FOR USE AS MMP-12 INHIBITORS
This invention relates to compounds that are selective inhibitors of Matrix Metalloprotease-12 (MMP-12), to cosmetic and pharmaceutical compositions containing them, and to their use in the prevention and/or treatment of ailments associated with MMP-12. Formula (I).
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PHOSPHINIC PEPTIDE DERIVATIVES FOR USE AS MMP-12 INHIBITORS
This invention relates to compounds that are selective inhibitors of Matrix Metalloprotease-12 (MMP-12), to cosmetic and pharmaceutical compositions containing them, and to their use in the prevention and/or treatment of ailments associated with MMP-12. Formula (I).
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TC-PTP INHIBITORS AS APC ACTIVATORS FOR IMMUNOTHERAPY
The invention encompasses the novel class of compounds represented by the Formula (I) below, which are inhibitors of the TC-PTP enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown above and methods of treating or preventing TC-PTP mediated diseases, including cancer, via their use in the activation of antigen-presenting cells, like dendritic cells, for applications in the immunotherapeutic treatment of diseases.
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TC-PTP INHIBITORS AS APC ACTIVATORS FOR IMMUNOTHERAPY
The invention encompasses the novel class of compounds represented by the Formula (I) below, which are inhibitors of the TC-PTP enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown above and methods of treating or preventing TC-PTP mediated diseases, including cancer, via their use in the activation of antigen-presenting cells, like dendritic cells, for applications in the immunotherapeutic treatment of diseases.
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TC-PTP INHIBITORS AS APC ACTIVATORS FOR IMMUNOTHERAPY
The invention encompasses the novel class of compounds represented by the Formula (I) below, which are inhibitors of the TC-PTP enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown above and methods of treating or preventing TC-PTP mediated diseases, including cancer, via their use in the activation of antigen-presenting cells, like dendritic cells, for applications in the immunotherapeutic treatment of diseases.
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Predictive biomarker for hypoxia-activated prodrug therapy
CYP2W1 levels are predictive of the probability that a cancer patient will respond favorably to cancer therapy involving administration of a hypoxia-activated achiral phosphoramidate mustards.
Predictive biomarker for hypoxia-activated prodrug therapy
CYP2W1 levels are predictive of the probability that a cancer patient will respond favorably to cancer therapy involving administration of a hypoxia-activated achiral phosphoramidate mustards.
Silicone-based composition for skin treatment
The present embodiments may relate to topically delivered compounded medications for the treatment of scar tissue, skin disorders, and/or other ailments. In one aspect, a transdermal cream or gel may provide for the effective administration of multiple medications simultaneously. Preferably, a silicone-based gel may be provided as a base composition and may have a non-zero percentage of silicone or silicone variant. The silicone-based gel may comprise cyclopentasiloxane, polysilicone-11, dimethicone, and C30-45 alkyl cetearyl dimethicone crosspolymer, and include several active ingredients, such as glucocorticoids, antihistamines, and nerve depressants. The silicone-based gel may include a combination of fluticasone, loratadine, and gabapentin. The concentrations of fluticasone and loratadine may be relatively low, while that of gabapentin moderately high. The silicone-based gel may also have one or more local anesthetics, such as prilocaine and/or lidocaine. The silicone-based gel may include additional active ingredients, such as NSAIDs, anticonvulsants, antidepressants, muscle relaxants, and/or other active ingredients.
Method of treating presbyopia using dithiol compounds and their derivatives
Dithiol compounds and derivatives thereof are disclosed. The agents are useful for treating ocular disease, especially presbyopia and cataract.