796844-14-9

Upstream product

• 121-33-5 vanillin 
• 140690-56-8 2,4-bis(trifluoromethyl)benzyl bromide 

Downstream Products

• 1264751-86-1 (5Z)-5-[(4-{[2,4-bis(trifluoromethyl)benzyl]oxy}-3-methoxyphenyl)methylidene]-4-{[2-(1-methylpyrrolidin-2-yl)ethyl]amino}-1,3-thiazol-2(5H)-one 
• 2306388-57-6 (E)-3-(4-((2,4-bis(trifluoromethyl)benzyl)oxy)-3-methoxyphenyl)-2-cyanoacrylic acid 

Relevant academic research and scientific papers

Identification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation

A series of (E)-3-(4-((2,4-bis(trifluoromethyl)benzyl)oxy)-3-methoxyphenyl)-2-cyanoacrylamide derivatives were designed and synthesized as new estrogen-related receptor α (ERRα) degraders based on the proteolysis targeting chimera (PROTAC) concept. One of the representative compounds 6c is capable of specifically degrading ERRα protein by >80% at a relatively low concentration of 30 nM, becoming one of the most potent and selective ERRα degraders to date. Compound 6c could be utilized as a new powerful research tool for further biological investigation of ERRα.

Compound for targeted ubiquitination degradation of ERRalpha protein and pharmaceutical composition and application thereof

The invention provides a compound with a structure shown as a formula (I), which has the effects of inhibiting ERRalpha protein activity and degrading ERRalpha protein activity, has relatively strongsubtype selectivity and can also effectively inhibit tri

PHENYL [A]INDOLE[2,3-G]QUINOLIZINE COMPOUNDS, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION, AND APPLICATIONS THEREOF

The present invention relates to phenyl [a]indole[2,3-g]quinolizine compounds represented by formula (I), a preparation method therefor, a pharmaceutical composition, and applications thereof. Specific applications are applications in the preparation of d

PROPHYLACTIC OR THERAPEUTIC AGENT FOR CANCER

A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof has a superior activity as an estrogen-related receptor-α modulator, and is useful as a prophylactic or therapeutic agent for cancer.

PHARMACEUTICAL COMPOSITIONS

Compounds for use in compositions and methods for modulating the activity of nuclear receptors are provided. In particular, compounds for use in compositions and methods for modulating the estrogen related receptors are provided. In one embodiment, the compounds provided herein are ERR modulators. In another embodiment, the compounds provided herein are agonists, partial agonists, antagonists. or inverse agonists of ERR or ERR?. In certain embodiments, the compounds of the invention, as described above in the Summary of the Invention, are compounds of formula (I).

3-PHENYL-N- ((1, 3, 4) THIADIAZOL-2-YL) -ACRYLAMIDE DERIVATIVES AND RELATED COMPOUNDS AS MODULATORS OF ESTROGEN-RELATED RECEPTORS FOR THE TREATMENT OF E.G. CANCER, RHEUMATOID ARTHRITIS OR NEUROLOGICAL DISORDERS

Compounds of formula (I) are provided as well as compositions and methods of using compounds of formula (I) for modulating the activity of the estrogen-related receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder related to the activity of the estrogen-related receptor. Considering the wide range of activity of the nuclear hormone receptor ERRα, the compounds described herein which are capable of modulating ERRα activity, are useful for treating a range of disease states including cancer, diabetes, obesity, hyperlipidermia, arthritis, atherosclerosis, osteoporosis, anxiety, depression, Parkinson’s disease and Alzheimer’s disease. Formula (I). The substituents are defined in the claims.

Identification of a selective inverse agonist for the orphan nuclear receptor estrogen-related receptor α

The estrogen-related receptor α (ERRα) is an orphan receptor belonging to the nuclear receptor superfamily. The physiological role of ERRα has yet to be established primarily because of lack of a natural ligand. Herein, we describe the discovery of the fi