The present disclosure relates to prodrugs of 7-chlorokynurenic acid. In certain embodiments, the prodrugs include those having the structure of any one of formula (I)-(VIII), wherein R.sup.1-R.sup.13, monomer 1, monomer 2, and linker are defined herein. Also provided are methods of preparing and using these prodrugs.

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The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril, inter alia via nitro 5 compounds. It further relates to new intermediate compounds and their use for said new chemical synthesis route, as well as a new catalyst ligand.

The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril, inter alia via nitro 5 compounds. It further relates to new intermediate compounds and their use for said new chemical synthesis route, as well as a new catalyst ligand.

Provided are new crystalline forms A, B, C, D and E of sacubitril sodium salt and a method for preparation thereof, pharmaceutical compositions thereof, and application thereof in preparing drugs for enkephalinase-related diseases.

A method for producing a compound of formula (I) or a pharmaceutically acceptable salt, solvate, tautomer or stereoisomer, such as compound 1 and compound 2 is disclosed. The method proceeds through an O-allylated tyrosine-based compound, such as compound 3 and preferably comprises [3,3] sigmatropic Claisen rearrangement and olefin cross metathesis reactions. In addition, a pharmaceutical composition comprising a compound of formula (I) a tumor necrosis factor (TNF) related apoptosis inducing ligand (TRAIL) and a pharmaceutically acceptable carrier or excipient is disclosed.

A method for producing a compound of formula (I) or a pharmaceutically acceptable salt, solvate, tautomer or stereoisomer, such as compound 1 and compound 2 is disclosed. The method proceeds through an O-allylated tyrosine-based compound, such as compound 3 and preferably comprises [3,3] sigmatropic Claisen rearrangement and olefin cross metathesis reactions. In addition, a pharmaceutical composition comprising a compound of formula (I) a tumor necrosis factor (TNF) related apoptosis inducing ligand (TRAIL) and a pharmaceutically acceptable carrier or excipient is disclosed.

A method for producing a compound of formula (I) or a pharmaceutically acceptable salt, solvate, tautomer or stereoisomer, such as compound 1 and compound 2 is disclosed. The method proceeds through an O-allylated tyrosine-based compound, such as compound 3 and preferably comprises [3,3] sigmatropic Claisen rearrangement and olefin cross metathesis reactions. In addition, a pharmaceutical composition comprising a compound of formula (I) a tumor necrosis factor (TNF) related apoptosis inducing ligand (TRAIL) and a pharmaceutically acceptable carrier or excipient is disclosed.

Cinnamoyl amino acid compounds and a use thereof, which relate to the fields of medicinal chemistry and pharmacotherapeutics, and specifically relate to cinnamoyl amino acid compounds having inducible nitric oxide synthase (iNOS) inhibitory activity or a pharmaceutically acceptable salt thereof, a pharmaceutical composition including the compounds, and a medical use thereof, particularly an application thereof in the prevention and treatment of neurodegenerative diseases related to nerve cell damage, including ischemic stroke, Parkinson's disease, and so on.

Cinnamoyl amino acid compounds and a use thereof, which relate to the fields of medicinal chemistry and pharmacotherapeutics, and specifically relate to cinnamoyl amino acid compounds having inducible nitric oxide synthase (iNOS) inhibitory activity or a pharmaceutically acceptable salt thereof, a pharmaceutical composition including the compounds, and a medical use thereof, particularly an application thereof in the prevention and treatment of neurodegenerative diseases related to nerve cell damage, including ischemic stroke, Parkinson's disease, and so on.

Embodiments of screening methods for determining test agents effective for modifying the appearance of pigmented skin are provided. The screening method may comprise the steps of contacting a cell, a cell culture, or bulk cells with the test agent, wherein the cell, the cell culture, or the bulk cells comprise ADR1 receptors, and determining based on the binding interaction of the test agent with the ADR1 receptors whether the test agent is an effective ADR1 receptor antagonist suitable for modifying the appearance of pigmented skin, wherein a test agent is considered to be an effective ADR1 receptor antagonist when it defines a half maximal inhibitory concentration of less than about 1000 ppm.