83097-87-4

Upstream product

• 372-31-6 ethyl 4,4,4-trifluoroacetoacetate 
• 100-51-6 benzyl alcohol 
• 83643-84-9 methyl 4,4,4-trifluoroacetoacetate 

Downstream Products

• 87962-73-0 Benzyl 4-acetyl-5-methyl-3-trifluoromethylpyrrole-2-carboxylate 
• 852613-23-1 4-(3-cyano-phenyl)-2-hydroxy-5-oxo-2-trifluoromethyl-1,2,3,4,5,6,7,8-octahydro-quinoline-3-carboxylic acid benzyl ester 
• 874179-67-6 4-(3-chloro-phenyl)-2-hydroxy-6-methyl-2-trifluoromethyl-1,2,3,4-tetrahydro-pyridine-3,5-dicarboxylic acid 3-benzyl ester 5-(2-cyano-ethyl) ester 
• 314776-25-5 5-benzyl 3-(2-cyanoethyl) 4-(3-chlorophenyl)-2-methyl-6-trifluoromethyl-1,4-dihydropyridine-3,5-dicarboxylate 
• 852613-33-3 4-(3-cyano-phenyl)-5-oxo-2-trifluoromethyl-1,4,5,6,7,8-hexahydro-quinoline-3-carboxylic acid benzyl ester 
• 87973-35-1 Benzyl 4-ethyl-5-methyl-3-trifluoromethylpyrrole-2-carboxylate 
• 87962-74-1 Benzyl 5-acetoxymethyl-4-ethyl-3-trifluoromethylpyrrole-2-carboxylate 

Relevant academic research and scientific papers

NEW ANALOGS AS ANDROGEN RECEPTOR AND GLUCOCORTICOID RECEPTOR MODULATORS

The present invention relates to novel dihydropyridine derivatives of formula (I): as modulators of nuclear receptors selected from androgen receptor and glucocorticoid receptor, to processes for their preparation, to pharmaceutical compositions comprising said compounds and to the use of said for manufacturing a medicament for the treatment of pathological conditions or diseases that can improve by modulation of androgen receptor and/or glucocorticoid receptor, selected from cancer, metastasizing cancers, benign prostate hyperplasia, polycystic ovary syndrome (PCOS), hair loss, hirsutism, acne, hypogonadism, muscle wasting diseases, cachexia, Cushing's syndrome, anti-psychotic drug induced weight gain, obesity, post-traumatic stress disorder and alcoholism.

PYRAZOLE AMIDE DERIVATIVE

The present invention relates to a novel compound having a function of inhibiting RORγ activity. The present invention also relates to pharmaceutical composition comprising the compound, a use of the compound in treating or preventing autoimmune diseases, inflammatory diseases, metabolic diseases, or cancer diseases.

Structure-activity relationship study of 1,4-dihydropyridine derivatives blocking N-type calcium channels

Cilnidipine is a 1,4-dihydropyridine derived L/N-type calcium channel dual blocker possessing neuroprotective and analgesic effects which are related to its N-type calcium channel inhibitory activity. In order to find specific N-type calcium channel blockers with the least effects on cardiovascular system, we performed structure-activity relationship study on APJ2708, which is a derivative of cilnidipine, and found a promising N-type calcium channel blocker 21b possessing analgesic effect in vivo with a 1600-fold lower activity against L-type calcium channels than that of cilnidipine.

Alternative esters in the synthesis of ZD0947

Alternatives to the original iso-borneol and allyl esters were investigated in the synthesis of ZD0947 (1). Homologous allylic esters were prepared in higher yields and were more readily purified than for the existing route, but offered no further benefits later in the synthesis. However, the PNB-substituted ester series provided crystalline intermediates, higher yields and simplified isolations through-out, and utilised a heterogeneous hydrogenation, thus reducing the residual catalyst levels.