934638-01-4

Upstream product

• 99-10-5 3,5-Dihydroxybenzoic acid 
• 2150-44-9 1-carbomethoxy-3,5-dihydroxybenzene 
• 41696-97-3 3,5-dihydroxybenzoyl chloride 
• 29654-55-5 5-(hydroxymethyl)benzene-1,3-diol 
• 17178-10-8 2-methoxy-ethyl p-toluenesulfonyloxy ester 
• 1010413-35-0 methyl 3,5-bis{[2-(methyloxy)ethyl]oxy}benzoate 

Downstream Products

• 1010413-34-9 1-(chloromethyl)-3,5-bis{[2-(methyloxy)ethyl]oxy}benzene 

Relevant academic research and scientific papers

Screening for covalent inhibitors using DNA-display of small molecule libraries functionalized with cysteine reactive moieties

DNA-encoded chemical libraries are increasingly used to identify leads for drug discovery or chemical biology. Despite the resurging interest in covalent inhibitors, libraries are typically designed with synthon filtered out for reactive functionalities that can engage a target through covalent interactions. Herein, we report the synthesis of two libraries containing Michael acceptors to identify cysteine reactive ligands. We developed a simple procedure to discriminate between covalent and high affinity non-covalent inhibitors using DNA display of the library in a microarray format. The methodology was validated with known covalent and high affinity non-covalent kinase inhibitors. Screening of the library revealed novel covalent inhibitors for MEK2 and ERBB2.

1H-INDOLE-2-CARBOXYLIC ACID DERIVATIVES USEFUL AS PPAR MODULATORS

The present invention relates to certain indole derivatives that are modulators of PPAR, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine.

PYRIDAZINONE COMPOUNDS AS CALCILYTICS

Various calcilytic compounds and pharmaceutical compositions containing these compounds are disclosed. Calcilytic compounds are compounds capable of inhibiting calcium receptor activity. Methods for preparing calcilytic compounds, oral bioavailability of calcilytic compounds, and their use as calcium receptor antagonists are also disclosed.