Search

Your search keyword '"Briceno SW"' showing total 2 results
Start Over Author "Briceno SW"
2 results on '"Briceno SW"'

1. Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis.

Author

Santella JB 3rd, Gardner DS, Duncia JV, Wu H, Dhar M, Cavallaro C, Tebben AJ, Carter PH, Barrish JC, Yarde M, Briceno SW, Cvijic ME, Grafstrom RR, Liu R, Patel SR, Watson AJ, Yang G, Rose AV, Vickery RD, Caceres-Cortes J, Caporuscio C, Camac DM, Khan JA, An Y, Foster WR, Davies P, and Hynes J Jr

Subjects
Animals, Biological Availability, Clinical Trials, Phase II as Topic, Hep G2 Cells, Humans, Male, Microsomes, Liver metabolism, Models, Molecular, Piperidines metabolism, Piperidines pharmacokinetics, Piperidines therapeutic use, Pregnane X Receptor, Protein Conformation, Receptors, CCR1 chemistry, Receptors, CCR1 metabolism, Receptors, Steroid metabolism, Species Specificity, Urea metabolism, Urea pharmacokinetics, Urea pharmacology, Urea therapeutic use, Valine metabolism, Valine pharmacokinetics, Valine pharmacology, Valine therapeutic use, Arthritis, Rheumatoid drug therapy, Drug Discovery, Piperidines pharmacology, Receptors, CCR1 antagonists & inhibitors, Urea analogs & derivatives, Valine analogs & derivatives
Abstract

High-affinity, functionally potent, urea-based antagonists of CCR1 have been discovered. Modulation of PXR transactivation has revealed the selective and orally bioavailable CCR1 antagonist BMS-817399 (29), which entered clinical trials for the treatment of rheumatoid arthritis.

Published
2014
Full Text
View/download PDF

2. The discovery of BMS-457, a potent and selective CCR1 antagonist.

Author

Gardner DS, Santella JB 3rd, Duncia JV, Carter PH, Dhar TG, Wu H, Guo W, Cavallaro C, Van Kirk K, Yarde M, Briceno SW, Grafstrom RR, Liu R, Patel SR, Tebben AJ, Camac D, Khan J, Watson A, Yang G, Rose A, Foster WR, Cvijic ME, Davies P, and Hynes J Jr

Subjects
Dose-Response Relationship, Drug, Humans, Molecular Structure, Piperidines chemical synthesis, Piperidines chemistry, Structure-Activity Relationship, Drug Discovery, Piperidines pharmacology, Receptors, CCR1 antagonists & inhibitors
Abstract

A series of compounds which exhibited good human CCR1 binding and functional potency was modified resulting in the discovery of a novel series of high affinity, functionally potent antagonists of the CCR1 receptor. Issues of PXR activity, ion-channel potency, and poor metabolic stability were addressed by the addition of a hydroxyl group to an otherwise lipophilic area in the molecule resulting in the discovery of preclinical candidate BMS-457 for the treatment of rheumatoid arthritis., (Copyright © 2013 Elsevier Ltd. All rights reserved.)

Published
2013
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results