Accounts in Drug Discovery : case studies in medicinal chemistry / [edited by] Joel Barrish, Percy Carter, Peter Cheng, Robert Zahler.

• The Discovery of the Dipeptidyl Peptidase-4 (DPP4) Inhibitor Onglyza™: From Concept to Market / Jeffrey A. Robl and Lawrence G. Hamann -- The Discovery of Vorapaxar (SCH 530348), a Thrombin Receptor (Protease Activated Receptor-1) Antagonist with Potent Antiplatelet Effects / Samuel Chackalamannil -- The Discovery of Piragliatin, a Glucokinase Activator / Ramakanth Sarabu, Jefferson W. Tilley and Joseph Grimsby -- The Discovery of OSI-906, a Small-molecule Inhibitor of the Insulin-like Growth Factor-1 and Insulin Receptors / Mark J. Mulvihill and Elizabeth Buck -- The Genesis of the Antibody Conjugate Gemtuzumab Ozogamicin (Mylotarg®) for Acute Myeloid Leukemia / Philip R. Hamann -- Novel Androgen Receptor Antagonists for the Treatment of Prostate Cancer / Ashvinikumar V. Gavai, William R. Foster, Aaron Balog and Gregory D. Vite -- The Discovery of UK-390957: the Challenge of Targeting a Short Half-life, Rapid Tmax SSRI / Mark D. Andrews and Donald S. Middleton -- The Discovery of the Long-acting PDE5 Inhibitor PF-489791 for the Treatment of Pulmonary Hypertension / Andrew S. Bell and Michael J. Palmer -- From HTS to Market: the Discovery and Development of Maraviroc, a CCR5 Antagonist for the Treatment of HIV / Chris Barber and David Pryde -- The Discovery of GS-9131, an Amidate Prodrug of a Novel Nucleoside Phosphonate HIV Reverse Transcriptase Inhibitor / Richard Mackman -- 2′-F-2′-C-Methyl Nucleosides and Nucleotides for the Treatment of Hepatitis C Virus: from Discovery to the Clinic / Michael J. Sofia, Phillip A. Furman and William T. Symonds -- A Case History on the Challenges of Central Nervous System and Dual Pharmacology Drug Discovery / Paul V. Fish, Anthony Harrison, Florian Wakenhut and Gavin A. Whitlock -- The Discovery of TRPV1 Antagonists: Turning up the Heat / Mark H. Norman -- Uncoupling Neuroprotection from Immunosuppression: the Discovery of ILS-920 / Edmund I. Graziani -- Identification of α7 Nicotinic Acetylcholine Receptor Agonists for their Assessment in Improving Cognition in Schizophrenia / Bruce N. Rogers, E. Jon Jacobsen, Christopher J. O’Donnell, Christopher L. Shaffer, Daniel P. Walker and Donn G. Wishka. 

• Accounts in Drug Discovery describes recent case studies in medicinal chemistry with a particular emphasis on how the inevitable problems that arise during any project can be surmounted or overcome. The Editors cover a wide range of therapeutic areas and medicinal chemistry strategies, including lead optimization starting from high throughput screening "hits" as well as rational, structure-based design. The chapters include "follow-ons" and "next generation" compounds that aim to improve upon first generation agents. This volume surveys the range of challenges commonly faced by medicinal chemistry researchers, including the optimization of metabolism and pharmacokinetics, toxicology, pharmaceutics and pharmacology, including proof of concept in the clinic for novel biological targets. The case studies include medicinal chemistry stories on recently approved and marketed drugs, but also chronicle "near-misses", i.e., exemplary compounds that may have proceeded well into the clinic but for various reasons did not result in a successful registration. As the vast majority of projects fail prior to registration, much can be learned from such narratives. By sharing a wide range of drug discovery experiences and information across the community of medicinal chemists in both industry and academia, we believe that these accounts will provide insights into the art of medicinal chemistry as it is currently practiced and will help to serve the needs of active medicinal chemists. 

Ämnesord

Farmaceutisk kemi  (sao)

Drug development  -- Case studies. (LCSH)

Pharmaceutical chemistry  -- Case studies. (LCSH)

Pharmaceutical chemistry  (LCSH)

Genre

Case studies.  (fast)

Electronic books. 

Indexterm och SAB-rubrik

Vd Farmakologi

Klassifikation

615.19 (DDC)

Vd (kssb/8)