528861-46-3

Upstream product

• 109384-19-2 t-butyl 4-hydroxy piperidine-1-carboxylate 
• 3769-41-3 3-Benzyloxyphenol 
• 108-46-3 recorcinol 
• 1008774-50-2 tert-butyl 4-(3-(benzyloxy)phenoxy)piperidine-1-carboxylate 

Downstream Products

• 1304787-64-1 tert-butyl 4-(3-(2,2,2-trifluoroethoxy)phenoxy)piperidine-1-carboxylate 

Relevant academic research and scientific papers

INDOLE DERIVATIVES AS HISTONE DEMETHYLASE INHIBITORS

The present application relates to compounds of formula (I), wherein A, R, R1, and R2 are as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy.

Discovery of Novel Selective Acetyl-CoA Carboxylase (ACC) 1 Inhibitors

We initiated our structure-activity relationship (SAR) studies for selective ACC1 inhibitors from 1a as a lead compound. SAR studies of bicyclic scaffolds revealed many potent and selective ACC1 inhibitors represented by 1f; however most of them had physicochemical issues, particularly low aqueous solubility and potent CYP inhibition. To address these two issues and improve the druglikeness of this chemical series, we converted the bicyclic scaffold into a monocyclic framework. Ultimately, this lead us to discover a novel monocyclic derivative 1q as a selective ACC1 inhibitor, which showed highly potent and selective ACC1 inhibition as well as acceptable solubility and CYP inhibition profiles. Since compound 1q displayed favorable bioavailability in mouse cassette dosing testing, we conducted in vivo PD studies of this compound. Oral administration of 1q significantly reduced the concentration of malonyl-CoA in HCT-116 xenograft tumors at doses of more than 30 mg/kg. Accordingly, our novel series of selective ACC1 inhibitors represents a set of useful orally available research tools, as well as potential therapeutic agents for cancer and fatty acid related diseases.

BICYCLIC COMPOUND

Provided is a bicyclic compound having an acetyl-CoA carboxylase inhibitory action. A compound represented by the formula: wherein each symbol is as described in the DESCRIPTION, or a salt thereof has an acetyl-CoA carboxylase inhibitory action, is useful for the prophylaxis or treatment of cancer, inflammatory diseases and the like, and has superior efficacy.

IMIDAZOLES AS HISTONE DEMETHYLASE INHIBITORS

The present invention relates to imidazole derivatives, wherein A, R, R1, and R2 are as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy.

AMINE DERIVATIVE

The present invention provide a compound of the formula: wherein X and X' are the same or different and each represents a hydrogen atom, etc.; R1 and R2 are the same or different and each represents a hydrogen atom, etc.; R3/su