The present invention is directed to a compound of Formula I or Formula III or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: wherein the definitions R.sub.1-R.sub.13 and L.sub.1-L.sub.4 are provided in the disclosure, and wherein R14 is a peptide. The compounds of Formula I may be covalently bonded to a peptide via a linker to provide a compound of Formula III and thereby extend the half-life of the therapeutic compound. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use in the diagnosis or treatment of diseases.

A dehydration catalyst for preparing N-substituted maleimide, which may minimize formation of by-products, is reusable because its activity is not reduced significantly even after being reused several times, and may maintain its reaction activity for a long time, a preparation method thereof, and a method of preparing N-substituted maleimide, are provided.

The present invention relates to compounds that inhibit the activity of Type III deiodinase (DIO3). The present invention further relates to methods for treating or preventing depression, depression associated with other psychiatric or general medical diseases or conditions, condition amenable to treatment with known anti-depressants and cancer, particularly by using the compounds of the invention.

The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related conditions.

A dehydration catalyst for preparing N-substituted maleimide, which may minimize formation of by-products, is reusable because its activity is not reduced significantly even after being reused several times, and may maintain its reaction activity for a long time, a preparation method thereof, and a method of preparing N-substituted maleimide, are provided.

The present invention is directed to a compound of Formula I or Formula III or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: wherein the definitions R.sub.1-R.sub.13 and L.sub.1-L.sub.4 are provided in the disclosure, and wherein R14 is a peptide. The compounds of Formula I may be covalently bonded to a peptide via a linker to provide a compound of Formula III and thereby extend the half-life of the therapeutic compound. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use in the diagnosis or treatment of diseases.

The present invention relates to functionalized Maleimides and Isomaleimides of general Formula (I) and a process for the preparation thereof, involving [3+2] annulation of ?,?-unsaturated aldehydes with carbamoyl alkylates via an enolate pathway to afford highly functionalized compounds of Formula (I);

##STR00001##

The present invention relates to functionalized Maleimides and Isomaleimides of general Formula (I) and a process for the preparation thereof, involving [3+2] annulation of ?,?-unsaturated aldehydes with carbamoyl alkylates via an enolate pathway to afford highly functionalized compounds of Formula (I);

##STR00001##

Disclosed herein are inhibitors of the Notch transcriptional activation complex, and methods for their use in treating or preventing diseases, such as cancer. The inhibitors described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: Formula (I), wherein the substituents are as described.

##STR00001##

Disclosed herein are inhibitors of the Notch transcriptional activation complex, and methods for their use in treating or preventing diseases, such as cancer. The inhibitors described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: Formula (I), wherein the substituents are as described.

##STR00001##