1240112-40-6

Upstream product

• 15861-24-2 1H-indole-5-carbonitrile 
• 98-09-9 benzenesulfonyl chloride 
• 144340-21-6 1-benzenesulfonyl-1H-indole-5-carbonitrile 
• 74-88-4 methyl iodide 

Downstream Products

• 36798-24-0 2-methyl-1H-indole-5-carbonitrile 
• 1401726-51-9 1-benzenesulfonyl-2-methyl-1H-indole-5-carbaldehyde 
• 36798-25-1 5-Aminomethyl-2-methylindol 
• 1401726-53-1 (S)-2-methylpropane-2-sulfinic acid [(S)-1-(1-benzenesulfonyl-2-methyl-1H-indol-5-yl)-2,2,2-trifluoroethyl]amide 

Relevant academic research and scientific papers

Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083)

The AAA-ATPase p97 plays vital roles in mechanisms of protein homeostasis, including ubiquitin-proteasome system (UPS) mediated protein degradation, endoplasmic reticulum-associated degradation (ERAD), and autophagy. Herein we describe our lead optimization efforts focused on in vitro potency, ADME, and pharmaceutical properties that led to the discovery of a potent, ATP-competitive, D2-selective, and orally bioavailable p97 inhibitor 71, CB-5083. Treatment of tumor cells with 71 leads to significant accumulation of markers associated with inhibition of UPS and ERAD functions, which induces irresolvable proteotoxic stress and cell death. In tumor bearing mice, oral administration of 71 causes rapid accumulation of markers of the unfolded protein response (UPR) and subsequently induces apoptosis leading to sustained antitumor activity in in vivo xenograft models of both solid and hematological tumors. 71 has been taken into phase 1 clinical trials in patients with multiple myeloma and solid tumors.

Positive allosteric modulators of nicotinic acetylcholine receptor

The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.

NOVEL COMPOUNDS EFFECTIVE AS XANTHINE OXIDASE INHIBITORS, METHOD FOR PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME

The present invention relates to novel compounds which are effective as an inhibitor for xanthine oxidase, a process for preparing the same, and a pharmaceutical composition comprising a therapeutically effective amount of the same.