GlaxoSmithKline

The development of a new drug is both a time-consuming and a cost-intensive process. It takes 12 to 15 years and costs up to 800 million to bring a new drug to the market. As measured by the market capitalization, the pharmaceutical companies play a pivotal role in the global economy. In February 2003 Pfizer was ranked at position five worldwide, with a market capitalization of 163 billion. Ranking third as far as the market capitalization in Europe is concerned was GlaxoSmithKline, with a current value of 101 billion. Novartis was number five in Europe with 82 billion. 

Although no PPARS-specific ligands are currently FDA-approved, GW501516 is a compound being developed jointly by GlaxoSmithKline and Ligand Pharmaceuticals. This compound is currently in Phase II trials for the treatment of dyslipidemia. 

GlaxoWellcome (now GlaxoSmithKline) licensed 4-deoxy-4-guanidino-Neu5Ac2en 12 as a lead drug candidate under the generic name zanamivir and... 

Billich A (2003) S-1360 Shionogi-GlaxoSmithKline. Curr Opin Investig Dmgs 4 206-209 Black LW (1988) DNA packaging in dsDNA bacteriophages. In Calendar R (ed) The bacteriophages. Plenum, NY, pp 321-373... 

However, despite their practical and societal value, vaccines remain only a small component of the global pharmaceutical market ( 5 billion out of 350 billion sales in 2000). The vaccine market is dominated by just four large manufacturers GlaxoSmithKline, Aventis Pasteur, Wyeth, and Merck Co. There is, however, a strong resurgence of interest in vaccines, with a growing cluster of small vaccine companies and biotech hrms, led by Chiron. 

The CHI index is reportedly a relevant parameter in quantitative structure-activity relationship (QSAR) studies [41]. With this approach, log P could be determined in the range -0.45more than 25000 compounds with excellent reproducibility (within 2 index units) and reported in a GlaxoSmithKline database [11]. Two main drawbacks were identified using this approach (i) the assumptions used in Ref [7], i.e. that S is constant for all compounds and that the system dwell volume is excluded in calculations, yield some discrepancies in the resulting log P, and (ii) the set of gradient calibration... 

Microbial, Musculoskeletal, and Proliferative Diseases CEDD, GlaxoSmithKline Pharmaceuticals, Collegeville, PA 19426, USA... 

In the patent literature, Aventis has published a patent application covering hydroxamic acid containing macrocycles (39) with the same general template as the A-formyl-A-hydroxylamine macrocycles described above [114] and GlaxoSmithKline has published an application on macrocyclic PDF inhibitors containing a hydrazide scaffold (40) [115], No data has been published on these inhibitors to date. 

Researchers at GlaxoSmithKline have numerous recent patent applications describing several series of H3 antagonists including the benzazapines (41) [115] and (42) [116], quinolizidines (43) [117], isoindolines (44) [118], and the piperidine amides (45) [119] and (46) [120]. All of these structures were disclosed as functional H3 antagonists. 

GlaxoSmithKline, New Frontiers Science Park (North), Third Avenue, Harlow, Essex, CM19 SA JV, UK... 

GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SGI 2NY, UK... 

The search for an effective non-peptide oxytocin antagonist has become a major goal of a number of pharmaceutical companies because of the poor pharmacokinetic properties and especially the lack of oral bioavailability associated with peptidic antagonists. Early research in this field was dominated by Merck, but in recent years significant research efforts at GlaxoSmithKline and Serono have been published. A number of other companies, notably Sanofi-Aventis, Yamanouchi and Wyeth, have had a major presence in vasopressin receptor research and oxytocin is frequently included in patent claims for the molecules. Occasionally, oxytocin-selective compounds have been reported, usually derived by adaptation of the vasopressin antagonist template. 

A benzodiazepine template was also reported by researchers at GlaxoSmithKline [85]. The lead molecule GW405212, (40), was identified from a 1,296-member library of 1,4-benzodiazepines prepared on Tentagel beads and screened initially in pools of 30 against CHO cells expressing the human oxytocin receptor. It is a highly potent inhibitor of oxytocin binding with a K of 8nM [86]. However, all attempts to improve the pharmacokinetic properties of this molecule were unsuccessful. It appears that the functionality responsible for the oxytocin activity is distributed around the periphery... 

CCR3 GW-766994 GlaxoSmithKline Phase II Asthma, allergic rhinitis 111-113, 125... 

Narendra B. Barn, Ph.D. Project Management and R D Strategy, GlaxoSmithKline, Collegeville, Pennsylvania... 

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