1.
Bioorg Med Chem Lett
; 17(15): 4228-31, 2007 Aug 01.
Article
in English
| MEDLINE
| ID: mdl-17532633
ABSTRACT
The discovery and optimization of a novel class of potent CCR3 antagonists is described. Details of synthesis and SAR are given together with some ADME properties of selected compounds. An optimal balance between activities, physicochemical properties, and in vitro metabolic stability was reached by the proper choice of substituents.
Subject(s)
Piperidines/pharmacology , Receptors, Chemokine/antagonists & inhibitors , Humans , Piperidines/chemical synthesis , Piperidines/chemistry , Receptors, CCR3 , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 16(7): 1834-9, 2006 Apr 01.
Article
in English
| MEDLINE
| ID: mdl-16439121
ABSTRACT
SAR around 4,6-diaminopyrimidine derivatives allowed the discovery of the first potent dual M(3) antagonists and PDE4 inhibitors. Various chemical modulations around that scaffold led to the discovery of ucb-101333-3 which is characterized by the most interesting profile on both targets.