95333-16-7

Upstream product

• 111-34-2 -butyl vinyl ether 
• 133720-60-2 7-bromobenzo(b)furan 
• 181819-95-4 1-(benzofuran-7-yl)ethan-1-ol 
• 52951-09-4 benzofuran-7-carbonitrile 
• 75-16-1 methylmagnesium bromide 
• 253429-15-1 1-bromo-2-(2,2-diethoxyethoxy)benzene 
• 95-56-7 2-hydroxybromobenzene 

Relevant academic research and scientific papers

1,3-disubstituted ketene compound and application thereof

The invention relates to a 1,3-disubstituted ketene compound with a structure as shown in a formula (I) and application thereof. The compound mainly activates a PPAR (Peroxisome Proliferators-Activated Receptor) alpha, and also has excitation activity for PPPA delta and PPPA gamma. The 1,3-disubstituted ketene compound can be used for treating various diseases related to the PPAR regulation abnormality, such as NASH (nonalcoholic steatohepatitis), and particularly treating nonalcoholic hepatitis, also has potentials for treating diabetes, obesity, fibrotic diseases, cardiovascular diseases (comprising a heart failure, atherosclerosis and the like), kidney diseases (comprising chronic nephrosis, a kidney failure and the like), brain degenerative diseases (comprising the alzheimer disease and the like) and the like, and has higher application value. The formula is shown in the description.

Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles

Replacing the naphthalene C-unit of the anti-tuberculosis drug bedaquiline with a range of bicyclic heterocycles of widely differing lipophilicity gave analogs with a 4.5-fold range in clogP values. The biological results for these compounds indicate on average a lower clogP limit of about 5.0 in this series for retention of potent inhibitory activity (MIC90s) against M.tb in culture. Some of the compounds also showed a significant reduction in inhibition of hERG channel potassium current compared with bedaquiline, but there was no common structural feature that distinguished these.

ANTIBACTERIAL COMPOUNDS AND USES THEREOF

The present invention relates to compounds of formula (I) including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of tuberculosis.

NOVEL TRICYCLIC CALCIUM SENSING RECEPTOR ANTAGONISTS

Novel tricyclic compounds of Formula (I) and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing osteoporosis and similar conditions. The compounds are effective as calcium sensing receptor antagonists. Pharmaceutical compositions and methods of treatment are also included.

NOVEL TRICYCLIC CALCIUM SENSING RECEPTOR ANTAGONISTS FOR THE TREATMENT OF OSTEOPOROSIS

Novel tricyclic compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing osteoporosis and similar conditions. The compounds are effective as calcium sensing receptor antagonists. Pharmaceutical compositions and methods of treatment are also included.

CONFORMATIONAL ANALYSIS OF ORGANIC CARBONYL COMPOUNDS. PART 4. A (1)H AND (13)C NUCLEAR MAGNETIC RESONANCE STUDY OF FORMYL AND ACETYL DERIVATIVES OF BENZOFURAN

A conformational study of formyl and acetyl derivatives of benzofuran provides evidence that in the case of 2- and 7-derivatives the E,Z-conformational mixture is solvent dependent, the Z-form prevailing in solvents with higher polarity.The presence of the same substituents in the 3- and 4-position gives compounds with predominantly Z-conformation and no change is caused by solvents.These results show an interestingly different behaviour by carbonyl derivatives of benzofuran with respect to the same benzothiophene derivatives.The conformational analysis was carried out by the n.m.r. method by employing (1)H and (13)C chemical shifts, long-range proton-proton coupling constants, and lanthanide-induced shifts (LIS) simulation.For the derivatives substituted in position 7, the LIS method is not a suitable approach for the determination of the conformer populations since, in solution, a chelate is formed where bonding of Eu to the oxygen atoms of the carbonyl and of the heterocyclic ring stabilizes the Z-form.A quantitative approach for determining the relative conformer populations of benzofuran-7-carbaldehyde was set up by statistical manipulation of long-range proton-proton coupling constants, proton chemical shifts, and the classical of dielectrics.