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Featured researches published by Thomas Wai-Ho Lee.


ACS Medicinal Chemistry Letters | 2016

Discovery of IWP-051, a Novel Orally Bioavailable sGC Stimulator with Once-Daily Dosing Potential in Humans

Takashi Nakai; Nicholas Robert Perl; Timothy C. Barden; Andrew Carvalho; Angelika Fretzen; Peter Germano; G-Yoon Jamie Im; Hong Jin; Charles Kim; Thomas Wai-Ho Lee; Kimberly Long; Joel Moore; Jason Rohde; Renee Sarno; Chrissie Segal; Erik Solberg; Jenny Tobin; Daniel P. Zimmer; Mark G. Currie

In recent years, soluble guanylate cyclase (sGC, EC 4.6.1.2) has emerged as an attractive therapeutic target for treating cardiovascular diseases and diseases associated with fibrosis and end-organ failure. Herein, we describe our design and synthesis of a series of 4-hydroxypyrimidine sGC stimulators starting with an internally discovered lead. Our efforts have led to the discovery of IWP-051, a molecule that achieves good alignment of potency, stability, selectivity, and pharmacodynamic effects while maintaining favorable pharmacokinetic properties with once-daily dosing potential in humans.


Journal of Medicinal Chemistry | 2006

Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.

John M. Regan; Thomas Wai-Ho Lee; Renee M. Zindell; Younes Bekkali; Jörg Bentzien; Thomas A. Gilmore; Abdelhakim Hammach; Thomas M. Kirrane; Alison Kukulka; Daniel Kuzmich; Richard M. Nelson; John R. Proudfoot; Mark Ralph; Josephine Pelletier; Donald Souza; Lijiljana Zuvela-Jelaska; Gerald H. Nabozny; David S. Thomson


Bioorganic & Medicinal Chemistry Letters | 2006

A concise asymmetric route for the synthesis of a novel class of glucocorticoid mimetics containing a trifluoromethyl-substituted alcohol.

Thomas Wai-Ho Lee; John R. Proudfoot; David S. Thomson


Archive | 2009

Azaindazole compounds as CCR1 receptor antagonists

Brian Nicholas Cook; Darren Di Salvo; Christian Harcken; Daniel Kuzmich; Thomas Wai-Ho Lee; Pingrong Liu; John Lord; Can Mao; Jochen Neu; Brian Christopher Raudenbush; Hossein Razavi; Alan David Swinamer


Archive | 2004

1,1,1-trifluoro-4-phenyl-4-methyl-2-(1h-pyrrolo

Younes Bekkali; Rajashekhar Betageri; Michael J. Emmanuel; Abdelhakim Hammach; Christian Harcken; Thomas M. Kirrane; Daniel Kuzmich; Thomas Wai-Ho Lee; Pingrong Liu; Usha R. Patel; Hossein Razavi; Doris Riether; Hidenori Takahashi; David S. Thomson; Ji Wang; Renee M. Zindell; John R. Proudfoot


ACS Medicinal Chemistry Letters | 2014

Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate.

Christian Harcken; Doris Riether; Pingrong Liu; Hossein Razavi; Usha R. Patel; Thomas Wai-Ho Lee; Todd Bosanac; Yancey David Ward; Mark Ralph; Zhidong Chen; Donald Souza; Richard M. Nelson; Alison Kukulka; Tazmeen Fadra-Khan; Ljiljana Zuvela-Jelaska; Mita Patel; David S. Thomson; Gerald H. Nabozny


Archive | 2005

Alpha-trifluoromethyl alcohols or amines as glucocorticoid mimetics

John R. Regan; Thomas Wai-Ho Lee; David S. Thomson; Thomas M. Kirrane; Daniel Kuzmich; John R. Proudfoot; Younes Bekkali; Renee M. Zindell


Archive | 2004

1,1,1-trifluoro-4-phenyl-4-methyl-2-(1h-pyrrolo(2,3-c) pyridin-2-ylmethyl) pentan-2-ol derivatives and related compounds as glucocorticoid ligands for the treatment of inflammatory diseases and diabetes

Younes Bekkali; Rajashekhar Betageri; Michael J. Emmanuel; Abdelhakim Hammach; Christian Harcken; Thomas M. Kirrane; Daniel Kuzmich; Thomas Wai-Ho Lee; Pingrong Liu; Usha R. Patel; Hossein Razavi; Doris Riether; Hidenori Takahashi; David S. Thomson; Jun Wang; Renee M. Zindell; John R. Proudfoot


Archive | 2018

FUSED BICYCLIC SGC STIMULATORS

Glen Robert Rennie; Rajesh R. Iyengar; Thomas Wai-Ho Lee; Takashi Nakai; Ara Mermerian; Lei Jia; G-Yoon Jamie Im; Paul Allan Renhowe; Joon Jung; Peter Germano; Karthik Iyer; Timothy C. Barden; Kim Tang


Archive | 2014

COMPUESTOS HETEROCICLICOS COMO ESTIMULADORES DE SGC

Charles Kim; Nicholas Robert Perl; Joel D. Moore; Takashi Nakai; Thomas Wai-Ho Lee; Jason Rohde

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