C07C237/00

Selective androgen receptor degrader (SARD) ligands and methods of use thereof

This invention provides novel 3-amino propanamide selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, androgenic alopecia or other 5 hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

NOVEL CYSTOBACTAMIDES

The present invention provides cystobactamides of formula (I) and the use thereof for the treatment or prophylaxis of bacterial infections.

##STR00001##

MODULATORS OF THE INTEGRATED STRESS PATHWAY

Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.

Method for Preparation of N-Acetyl Cysteine Amide and Derivatives Thereof

The present invention includes methods for making and isolating N-acetylcysteine amide, (2R,2R′)-3,3′-disulfanediyl bis(2-acetamidopropanamide, diNACA), intermediates and derivatives thereof comprising: contacting cystine with an alcohol and a chlorinating reagent to form an organic solution containing L-cystine dimethylester dihydrochloride; combining dried or undried L-cystine dimethylester dihydrochloride with a triethylamine, an acetic anhydride, and an acetonitrile to form a di-N-acetylcystine dimethylester; mixing dried di-N-acetylcystine dimethylester with ammonium hydroxide to form a di-N-acetylcystine amide (diNACA); and separating dried di-N-acetylcystine dimethylester into N-acetylcysteine amide with dithiothreitol, triethylamine and an alcohol.

MODULATORS OF THE INTEGRATED STRESS PATHWAY

Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases, disorders and conditions.

Catalyst, production method therefor, and method for producing optically active anti-1, 2-nitroalkanol compound

A catalyst including: neodymium; sodium; and a ligand, which is a compound expressed by Structural Formula (1) below, wherein the neodymium and the ligand form a complex at a molar ratio of 1:2 (neodymium:ligand): ##STR00001##

Process for the preparation of lacosamide

The present invention relates to an improved process for the synthesis of (R)-Lacosamide in which free base of O-methyl-N-benzyl-D-Serinamide is not isolated before acylation. The process avoids the use of column chromatography and chiral resolution for the preparation of different stages of Lacosamide.

Process for the preparation of lacosamide

The present invention relates to an improved process for the synthesis of (R)-Lacosamide in which free base of O-methyl-N-benzyl-D-Serinamide is not isolated before acylation. The process avoids the use of column chromatography and chiral resolution for the preparation of different stages of Lacosamide.

AN IMPROVED PROCESS FOR THE PREPARATION OF LACOSAMIDE

The present invention relates to an improved process for the synthesis of (R)-Lacosamide in which free base of O-methyl-N-benzyl-D-Serinamide is not isolated before acylation. The process avoids the use of column chromatography and chiral resolution for the preparation of different stages of Lacosamide.

Inhibitors of Mcl-1 as Drugs to Overcome Resistance to BRAF Inhibitors and MEK Inhibitors
20180161313 · 2018-06-14 ·

The present invention includes compositions and methods for inhibiting MCL-1, including novel inhibitors of MCL-1, and compositions and methods for treating a subject with cancer that is refractory to one or more MAPK pathway protein inhibitors.