329932-20-9Relevant academic research and scientific papers
1, 2, 3-TRIAZOLE DERIVATIVES FOR USE AS STEAROYL-COA DESATURASE INHIBITORS
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Page/Page column 45, (2009/06/27)
The present invention relates to substituted triazole compounds of the formula (I) and pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds for modulating SCD activity.
From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: The discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis
Santella III, Joseph B.,Gardner, Daniel S.,Yao, Wenqing,Shi, Chongsheng,Reddy, Prabhakar,Tebben, Andrew J.,DeLucca, George V.,Wacker, Dean A.,Watson, Paul S.,Welch, Patricia K.,Wadman, Eric A.,Davies, Paul,Solomon, Kimberly A.,Graden, Dani M.,Yeleswaram, Swamy,Mandlekar, Sandhya,Kariv, Ilona,Decicco, Carl P.,Ko, Soo S.,Carter, Percy H.,Duncia, John V.
, p. 576 - 585 (2008/09/19)
Conformational analysis of trans-1,2-disubstituted cyclohexane CCR3 antagonist 2 revealed that the cyclohexane linker could be replaced by an acyclic syn-α-methyl-β-hydroxypropyl linker. Synthesis and biological evaluation of mono- and disubstituted propyl linkers support this conformational correlation. It was also found that the α-methyl group to the urea lowered protein binding and that the β-hydroxyl group lowered affinity for CYP2D6. Ab initio calculations show that the α-methyl group governs the spatial orientation of three key functionalities within the molecule. α-Methyl-β-hydroxypropyl urea 31 with a chemotaxis IC50 = 38 pM for eosinophils was chosen to enter clinical development for the treatment of asthma.
ARYLUREA DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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Page/Page column 31-32, (2008/06/13)
A compound of formula (I), wherein substituents are as given above, useful in the treatment of a disease mediated by the action of CCR3, in particular inflammatory or obstructive airway diseases.
N-UREIDOALKYL-PIPERIDINES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY.
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Page 25, (2010/11/30)
The present application describes N-ureidoalkyl piperidines as modulators of chemokine receptors, or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
