284663-87-2Relevant academic research and scientific papers
Design and synthesis of selective, dual fatty acid binding protein 4 and 5 inhibitors
Kühne, Holger,Obst-Sander, Ulrike,Kuhn, Bernd,Conte, Aurelia,Ceccarelli, Simona M.,Neidhart, Werner,Rudolph, Markus G.,Ottaviani, Giorgio,Gasser, Rodolfo,So, Sung-Sau,Li, Shirley,Zhang, Xiaolei,Gao, Lin,Myers, Michael
, p. 5092 - 5097 (2016/10/05)
Dual inhibition of fatty acid binding proteins 4 and 5 (FABP4 and FABP5) is expected to provide beneficial effects on a number of metabolic parameters such as insulin sensitivity and blood glucose levels and should protect against atherosclerosis. Starting from a FABP4 selective focused screening hit, biostructure information was used to modulate the selectivity profile in the desired way and to design potent dual FABP4/5 inhibitors with good selectivity against FABP3. With very good pharmacokinetic properties and no major safety alerts, compound 12 was identified as a suitable tool compound for further in vivo investigations.
NEW ARYL-QUINOLINE DERIVATIVES
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Page/Page column 71-72; 126, (2013/05/22)
The invention provides novel compounds having the general formula (I), wherein R1, R2, R3, R4 R5, R6 and n are as described herein, compositions including the compounds and methods of using the compounds.
ARYL-QUINOLINE DERIVATIVES
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Paragraph 0464; 0743; 0744, (2013/05/21)
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6 and n are as described herein, compositions including the compounds and methods of using the compounds. The present compounds are useful as fatty-acid binding protein (FABP) 4 and/or 5 inhibitors and may be used for the treatment or prophylaxis of lipodystrophy, type 2 diabetes, dyslipidemia, atherosclerosis, liver diseases involving inflammation, steatosis and/or fibrosis, such as non-alcoholic fatty liver disease, in particular non-alcoholic steatohepatitis, metabolic syndrome, obesity, chronic inflammatory and autoimmune inflammatory diseases.
