1803599-76-9

Upstream product

• 100-39-0 benzyl bromide 
• 142253-55-2 1-(t-butyloxycarbonyl)-azetidine-3-carboxylic acid 

Relevant academic research and scientific papers

Discovery of Novel Azetidine Amides as Potent Small-Molecule STAT3 Inhibitors

We optimized our previously reported proline-based STAT3 inhibitors into an exciting new series of (R)-azetidine-2-carboxamide analogues that have sub-micromolar potencies. 5a, 5o, and 8i have STAT3-inhibitory potencies (IC50) of 0.55, 0.38, and 0.34 μM, respectively, compared to potencies greater than 18 μM against STAT1 or STAT5 activity. Further modifications derived analogues, including 7e, 7f, 7g, and 9k, that addressed cell membrane permeability and other physicochemical issues. Isothermal titration calorimetry analysis confirmed high-affinity binding to STAT3, with KD of 880 nM (7g) and 960 nM (9k). 7g and 9k inhibited constitutive STAT3 phosphorylation and DNA-binding activity in human breast cancer, MDA-MB-231 or MDA-MB-468 cells. Furthermore, treatment of breast cancer cells with 7e, 7f, 7g, or 9k inhibited viable cells, with an EC50 of 0.9-1.9 μM, cell growth, and colony survival, and induced apoptosis while having relatively weaker effects on normal breast epithelial, MCF-10A or breast cancer, MCF-7 cells that do not harbor constitutively active STAT3.

Oleanolic acid and δ - oleanolic acid derivative and medical application thereof (by machine translation)

The invention discloses a derivative of a pentacyclic triterpene novel AMPK agonist oleanolic acid and δ - oleanolic acid and a medical application thereof, in particular to a compound shown in formula I or formula II. A pharmaceutically acceptable salt or ester or solvate thereof, which can be used to prepare AMPK agonists with enhanced AMPK phosphorylation level activity and to the preparation of drugs for preventing or treating AMPK mediated diseases. The novel pentacyclic triterpene compound has remarkable AMPK agonist activity, and the activity is remarkably superior to the recognized AMPK agonist AICICAR, and meanwhile, the novel pentacyclic triterpene compound has pharmacokinetic properties such as better oral bioavailability and very good safety. (by machine translation)

2-ARYLSULFONAMIDO-N-ARYLACETAMIDE DERIVATIZED STAT3 INHIBITORS

The present disclosure provides pharmaceutical compositions comprising 2-arylsulfonamido-N-arylacetamide derivatized Stat3 inhibitors and certain pharmaceutically acceptable salts thereof, and methods of their use.

COMPOUNDS, COMPOSITIONS AND METHODS OF INCREASING CFTR ACTIVITY

The present disclosure features compounds such as those having the Formulae (I) and (II), which can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells. The present disclosure also features methods of treating a condition associated with decreased CFTR activity or a condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of a disclosed compound, such as a compound of Formula (I) or (II).

METHODS OF TREATING PULMONARY DISEASES AND DISORDERS

The present disclosure features disclosed method of treating disorders such as COPD, bronchitis and/or asthma using disclosed compounds, optionally together with one or more additional active agents. Contemplated methods include administrating orally or by inhalation to a patient one or more disclosed compounds.

COMPOUNDS, COMPOSITIONS, AND METHODS FOR INCREASING CFTR ACTIVITY

The present disclosure is directed to disclosed compounds that increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells.