C07D233/22

COMPOUNDS FOR TREATMENT OF CANCER

The present invention relates to a compound of formula XXII and a compound of formula 17ya, which are defined as anywhere in the specification, to a composition comprising the same, and to a method of using thereof in the treatment of various forms of cancer.

MODULARLY ASSEMBLED SMALL MOLECULES FOR THE TREATMENT OF MYOTONIC DYSTROPHY TYPE 1
20180089049 · 2018-03-29 ·

Transcriptomes provide a myriad of potential RNAs that could be the targets of therapeutics or chemical genetic probes of function. Cell permeable small molecules, however, generally do not exploit these targets, owing to the difficulty in the design of high affinity, specific small molecules targeting RNA. As part of a general program to study RNA function using small molecules, we designed bioactive, modularly assembled small molecules that target the non-coding expanded RNA repeat that causes myotonic dystrophy type 1 (DM1), r(CUG).sup.exp. Herein, we present a rigorous study to elucidate features in modularly assembled compounds that afford bioactivity. Different modular assembly scaffolds were investigated including polyamines, -peptides, -peptides, and peptide tertiary amides (PTAs). Based on activity as assessed by improvement of DM1-associated defects, stability against proteases, cellular permeability, and toxicity, we discovered that constrained backbones, namely PTAs, are optimal.

Novel compounds

The present invention is directed to novel retinoid-related orphan receptor gamma (ROR) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR.

Sulfonamide compounds and their use in the modulation retinoid-related orphan receptor

The present invention is directed to novel retinoid-related orphan receptor gamma (ROR) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR.

Sulfonamide compounds and their use in the modulation retinoid-related orphan receptor

The present invention is directed to novel retinoid-related orphan receptor gamma (ROR) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR.

Process for the synthesis of lofexidine
12351558 · 2025-07-08 · ·

The present invention relates to an improved process for the synthesis of lofexidine, or a pharmaceutically acceptable salt thereof, using an aluminium alkoxide as Lewis acid. ##STR00001##

Process for the synthesis of lofexidine
12351558 · 2025-07-08 · ·

The present invention relates to an improved process for the synthesis of lofexidine, or a pharmaceutically acceptable salt thereof, using an aluminium alkoxide as Lewis acid. ##STR00001##

Longer-lived ruthenium olefin metathesis catalysts supported by hemi-labile carbene ligands

Contemplated subject matter disclosed herein relates generally to organometallic olefin metathesis catalysts, and more particularly to longer-lived olefin metathesis catalysts supported by hemi-labile carbene ligands that bear an arm with one or more donor ligands, as well as the use of such catalysts in metathesis reactions of olefins and olefin compounds. The contemplated subject matter has utility in the fields of catalysis, organic synthesis, polymer chemistry, and industrial and fine chemicals chemistry. This contemplated subject matter serves to reduce the cost of olefin metathesis (OM) processes including in olefin metathesis polymerizations, conversion of vegetable oils into chemicals, and processes in the petrochemical industry. This contemplated subject matter reduces the cost of OM processes by providing OM catalysts that are longer-lived and lead to higher turnover numbers, hence requiring less catalyst to convert a given amount of substrate(s). Considering that the OM catalyst is the most expensive part of some OM processes, longer-lived OM catalysts have the benefit of reducing the overall cost of the OM processes.

Longer-lived ruthenium olefin metathesis catalysts supported by hemi-labile carbene ligands

Contemplated subject matter disclosed herein relates generally to organometallic olefin metathesis catalysts, and more particularly to longer-lived olefin metathesis catalysts supported by hemi-labile carbene ligands that bear an arm with one or more donor ligands, as well as the use of such catalysts in metathesis reactions of olefins and olefin compounds. The contemplated subject matter has utility in the fields of catalysis, organic synthesis, polymer chemistry, and industrial and fine chemicals chemistry. This contemplated subject matter serves to reduce the cost of olefin metathesis (OM) processes including in olefin metathesis polymerizations, conversion of vegetable oils into chemicals, and processes in the petrochemical industry. This contemplated subject matter reduces the cost of OM processes by providing OM catalysts that are longer-lived and lead to higher turnover numbers, hence requiring less catalyst to convert a given amount of substrate(s). Considering that the OM catalyst is the most expensive part of some OM processes, longer-lived OM catalysts have the benefit of reducing the overall cost of the OM processes.