Disclosed are small molecule PLK inhibitors that can target the polo box domain (PBD). Inhibitors can have an atomic mass of about 1000 Da or less and a general structure of ##STR00001##
For instance, the inhibitors can include an alkyl benzamido benzoic acid core structure.

Provided herein are brain penetrant histone deacetylase (HDAC) inhibitors useful for treating diseases or disorders associated with HDAC. An exemplary HDAC inhibitor provided herein exhibits a brain-to-plasma ratio of 20:1. Pharmaceutical compositions comprising HDAC inhibitors and methods for treating diseases associated with HDAC are also provided.

Provided are a photosensitive resin composition which has excellent pattern processabilities (high sensitivity and high resolution) and is excellent in chemical resistance and thermal resistance after thermally treated; a heat-resistant resin or heat-resistant resin precursor used for the composition; and a diamine compound which is a raw material of the resin and the precursor. The diamine compound is a diamine compound represented by a general formula (1).

##STR00001##

This invention relates to compounds of Formula (I) wherein Cy.sup.1, L.sup.1, Y, R.sup.1, L.sup.2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions. ##STR00001##

This invention relates to compounds of Formula (I) wherein Cy.sup.1, L.sup.1, Y, R.sup.1, L.sup.2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions. ##STR00001##

The present invention relates to a novel pseudoceramide derivative, a pharmaceutically acceptable salt thereof or a solvate thereof, and a pharmaceutical or cosmetic composition containing the same as an active ingredient. The novel pseudoceramide derivative of the present invention is expected to be very useful for treating or preventing skin diseases by activating cannabinoid receptors. In addition, the novel pseudoceramide derivative, the pharmaceutically acceptable salt thereof or the solvate thereof, of the present invention, has a simple synthesis process compared with a known cannabinoid receptor antagonist so as to reduce processing time and curtail material costs, and thus is economical, and has advantages such as easy emulsification during the formulation of cosmetic products or medical supplies.

The present invention relates to a novel pseudoceramide derivative, a pharmaceutically acceptable salt thereof or a solvate thereof, and a pharmaceutical or cosmetic composition containing the same as an active ingredient. The novel pseudoceramide derivative of the present invention is expected to be very useful for treating or preventing skin diseases by activating cannabinoid receptors. In addition, the novel pseudoceramide derivative, the pharmaceutically acceptable salt thereof or the solvate thereof, of the present invention, has a simple synthesis process compared with a known cannabinoid receptor antagonist so as to reduce processing time and curtail material costs, and thus is economical, and has advantages such as easy emulsification during the formulation of cosmetic products or medical supplies.

The present invention provides a process of producing a trifluoromethoxylated aryl or trifluoromethoxylated heteroaryl having the structure:

##STR00001##

wherein A is an aryl or heteroaryl, each with or without subsutitution; and R.sub.1 is —H, -(alkyl), -(alkenyl), -(alkynyl), -(aryl), -(heteroaryl), -(alkylaryl), -(alkylheteroaryl), —NH-(alkyl), —N(alkyl).sub.7, —NH-(alkenyl), —NH-(alkynyl) —NH-(aryl), —NH-(heteroaryl), —O-(alkyl), —O-(alkenyl), —O-(alkynyl), —O-(aryl), —O-(heteroaryl), —S-(alkyl), —S-(alkenyl), —S-(alkynyl), —S-(aryl), or —S-(heteroaryl), comprising: (a) reacting a compound having the structure:

##STR00002##

with a trifluoromethylating agent in the presence of a base in a first suitable solvent under conditions to produce a compound having the structure:

##STR00003##

and (b) maintaining the compound produced in step (a) in a second suitable solvent under conditions sufficient to produce the trifluoromethoxylated aryl or trifluormethoxylated heteroaryl having the structure:

##STR00004##

The present invention provides a process of producing a trifluoromethoxylated aryl or trifluoromethoxylated heteroaryl having the structure:

##STR00001##

wherein A is an aryl or heteroaryl, each with or without subsutitution; and R.sub.1 is —H, -(alkyl), -(alkenyl), -(alkynyl), -(aryl), -(heteroaryl), -(alkylaryl), -(alkylheteroaryl), —NH-(alkyl), —N(alkyl).sub.7, —NH-(alkenyl), —NH-(alkynyl) —NH-(aryl), —NH-(heteroaryl), —O-(alkyl), —O-(alkenyl), —O-(alkynyl), —O-(aryl), —O-(heteroaryl), —S-(alkyl), —S-(alkenyl), —S-(alkynyl), —S-(aryl), or —S-(heteroaryl), comprising: (a) reacting a compound having the structure:

##STR00002##

with a trifluoromethylating agent in the presence of a base in a first suitable solvent under conditions to produce a compound having the structure:

##STR00003##

and (b) maintaining the compound produced in step (a) in a second suitable solvent under conditions sufficient to produce the trifluoromethoxylated aryl or trifluormethoxylated heteroaryl having the structure:

##STR00004##

The present invention relates to compounds of formula (I) or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein X.sub.1, X.sub.2, X.sub.3, X.sub.4, X.sub.5, W.sub.1, W.sub.2, W.sub.3, and W.sub.4 are as described. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. In one aspect, the invention relates to selective HDAC3 inhibitors useful for protecting β-cells and improving insulin resistance. The selective HDAC3 inhibitors are also useful for promoting cognitive function and enhancing learning and memory formation. Compounds of the invention are useful for treating, alleviating, and/or preventing various conditions, including for example, a metabolic disorder such as type 1 or type 2 diabetes, dyslipidemias, lipodystrophies, liver disease associated with metabolic syndrome, polycystic ovarian syndrome, or obesity; inflammatory disease; neurological disorder; a memory or cognitive function disorder/impairment; an extinction learning disorder; fungal disease or infection; viral disease or infection such as HIV; hematological disease; liver disease; lysosomal storage disease; or neoplastic disease in humans or animals. ##STR00001##