PREFACE

The Annual Report in Medicinal Chemistry is dedicated to furthering genuine

interest in learning, chronicling, and sharing information about the discov-

ery of compounds and the methods that lead to new therapeutic advances.

ARMC’s tradition is to provide disease-based reviews and highlight emerg-

ing technologies of interest to medicinal chemists.

A distinguishing feature ofARMC is its knowledgeable section editors in

the field who evaluate invited reviews for scientific rigor. The current

volume contains 28 chapters in 8 sections. The first five sections have a ther-

apeutic focus. Their topics include CNS diseases (edited by Albert J.

Robichaud); cardiovascular and metabolic diseases (edited by Robert L.

Dow); inflammatory, pulmonary, and gastrointestinal diseases (edited by

David S. Weinstein); oncology (edited by Shelli R. McAlpine); and infec-

tious diseases (edited by John Primeau). Sections VI and VII review impor-

tant topics in biology (edited by John A. Lowe) and new technologies for

drug optimization (edited by Peter R. Bernstein). The last section deals with

case histories and drugs approved by the FDA in the previous year (edited by

Joanne Bronson).

The format for Volume 48 follows our previous issue.We continue with

the personal essays, written by MEDI hall of famers, which express the per-

sonal stories and scientific careers of “drug hunters,” as well as a chapter list-

ing new chemical entities that have entered Phase III. The volume opens

with essays by Ashit K. Ganguly, Christopher A. Lipinski, and Malcolm

MacCoss. In section VII, a chapter whose subject matter was jointly devel-

oped by IUPAC andMEDI, we collate and define many terms that are con-

sidered to be essential components of the medicinal chemist’s expanded

repertoire. In the current volume, the last section has been consolidated with

new title, “Case histories and NCE,” which includes case histories for the

two recently approved cancer drugs, crizotinib and vemurafenib.

This would not have been possible without our panel of section editors, to

whom I am indeed very grateful. I would like to thank the authors of this vol-

ume for their hard work, patience, dedication, and scholarship in the lengthy

process of writing, editing, and making last-minute edits and revisions to their

contributions. Further, I extend my sincere thanks to the following reviewers

who have provided independent edits to the manuscripts: Michael Bishop,

George Chang, Margaret Chu-Moyer, Michael Clarke, Andrew Combs,

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xviii Preface

Chris Cox, Kevin Currie, Michael Dillon, Gene Dubowchik, Carolyn

Dzierba, Gary Flynn, William Greenlee, Randall Halcomb, Nicholas Lodge,

MaryMader, Paul Orenstein, Anandan Palani, Paul Renhowe, Paul Roethle,

Greg Roth, Joachim Rudolf, David Sperandio, James Taylor, Bingwei Yang,

and Will Watkins. Additionally, I would like to thank Rachel Sumi for edi-

torial help with personal essays.

Finally, I would like to thank Andy Stamford, whowas the section editor

for the cardiovascular and metabolic diseases for Volumes 40–47, for his

dedication to identifying the most relevant topics of interest to the medicinal

chemists and his editorial expertise.

I hope the material provided in this volume will serve as a precious

resource on important aspects of medicinal chemistry, and, in this way,

maintain the tradition of excellence that ARMC has brought to us for more

than four decades. I am excited about our new initiatives; I look forward to

hearing from you about them and welcome your suggestions for

future content.

MANOJ C. DESAI, Ph.D.

Gilead Sciences, Inc.

Foster City, CA