In one aspect, the disclosure relates to methods for preparation of intermediates useful for the preparation of aryl-cycloheptene scaffolds. In a further aspect, the disclosed methods pertain to the preparation of compounds comprising an aryl-cycloheptene structure. The disclosed methods utilize abundant starting materials and simple reaction sequences that can be used to modularly and scalably assemble common such cores. In various aspects, the present disclosure pertains to compounds prepared using the disclosed methods. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I): ##STR00001##
or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q.sub.1, Q.sub.2, Z, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.

Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I): ##STR00001##
or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q.sub.1, Q.sub.2, Z, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.

A platform drug delivery system and a method of improving the delivery of low solubility pharmaceuticals utilizing crystal engineering and Theanine dissolution resulting in enhanced bioactivity, dissolution rate, and solid state stability.

A platform drug delivery system and a method of improving the delivery of low solubility pharmaceuticals utilizing crystal engineering and Theanine dissolution resulting in enhanced bioactivity, dissolution rate, and solid state stability.

The present invention provides an improved process for the preparation of 3-(4-chlorophenyl)-3-cyanopropanoic acid (compound (A)) and further its transformation to Baclofen (I). The process comprises reaction of compound (II) with Glyoxylic acid to obtain 3-(4-chlorophenyl)-3-cyanoacrylic acid (III); followed by the ‘in-situ’ reduction of (III) in the presence of a reducing agent to provide the compound (A).

Alternatively, the compound (A) is obtained by the process comprising reacting 2-(4-chlorophenyl)acetonitrile (II) with haloacetic acid (IV) in the presence of a base.

The compound 3-(4-chlorophenyl)-3-cyanopropanoic acid (A) undergoes hydrogenation in the presence of a metal catalyst and ammonia solution to provide Baclofen (I).

The present invention provides an improved process for the preparation of 3-(4-chlorophenyl)-3-cyanopropanoic acid (compound (A)) and further its transformation to Baclofen (I). The process comprises reaction of compound (II) with Glyoxylic acid to obtain 3-(4-chlorophenyl)-3-cyanoacrylic acid (III); followed by the ‘in-situ’ reduction of (III) in the presence of a reducing agent to provide the compound (A).

Alternatively, the compound (A) is obtained by the process comprising reacting 2-(4-chlorophenyl)acetonitrile (II) with haloacetic acid (IV) in the presence of a base.

The compound 3-(4-chlorophenyl)-3-cyanopropanoic acid (A) undergoes hydrogenation in the presence of a metal catalyst and ammonia solution to provide Baclofen (I).

The present invention relates to a novel cathode buffer layer material, and an organic or organic/inorganic hybrid photoelectric device comprising same, and, if a novel compound of the present invention is applied to a cathode buffer layer of an organic photoelectric device such as organic solar cells, organic photodiode, colloidal quantum dot solar cell, and perovskite solar cell, a surface property of an electron transfer layer is improved via a high dipole moment of the novel compound, an electron can be easily extracted from a photoactive layer to a cathode electrode, and series resistance and leakage current can be reduced, thereby having a useful industrial effect, as performance of the organic or organic/inorganic hybrid photoelectric device being manufactured, such as an organic solar cell, organic photodiode, colloidal quantum dot solar cell, and perovskite solar cell, can be significantly improved.

The present invention relates to a novel cathode buffer layer material, and an organic or organic/inorganic hybrid photoelectric device comprising same, and, if a novel compound of the present invention is applied to a cathode buffer layer of an organic photoelectric device such as organic solar cells, organic photodiode, colloidal quantum dot solar cell, and perovskite solar cell, a surface property of an electron transfer layer is improved via a high dipole moment of the novel compound, an electron can be easily extracted from a photoactive layer to a cathode electrode, and series resistance and leakage current can be reduced, thereby having a useful industrial effect, as performance of the organic or organic/inorganic hybrid photoelectric device being manufactured, such as an organic solar cell, organic photodiode, colloidal quantum dot solar cell, and perovskite solar cell, can be significantly improved.

Photostabilizing compounds are provided. In particular, the photostabilizing compounds may be heterocyclic or homocyclic. Topical compositions comprising these compounds are also provided. In particular, these topical compositions may further comprise photoactive compounds. Methods for stabilizing photoactive compounds are also provided. These methods comprise mixing the photoactive compounds with photostabilizing compounds.