Lexicon Pharmaceuticals

H.C. Kolb etaU US Patent 6,642,390 (November 4, 2003) Assignee Lexicon Pharmaceuticals, Inc. 

In addition to possible applications for the development of cancer drugs, deoxycytidine kinase (dCK) inhibitors also hold promise for the treatment of immune disorders. Drug discovery efforts aimed at inhibiting deoxycytidine kinase have been reported by Lexicon Pharmaceuticals. They disclosed an HTS assay for the discovery of dCK inhibitors.30... 

A study by researchers at Lexicon Genomics (now Lexicon Pharmaceuticals) looked at the targets for the top 100 prescription drugs and found that for the targets where knockout models could be generated (most of them) in 85% of the cases the knockouts produced phenotypes that were informative for the therapeutic indication involved. Not only Lexicon but also National Institutes of Health NIH) has now embarked on projects aimed at knocking out most if not all of the genes found in mouse. ... 

Researchers at Lexicon Pharmaceuticals found that limonene aziridines could be efficiently prepared from the corresponding limonene oxides using the Blum aziridine synthesis. Epoxide 32 was opened with sodium azide to produce the regioisomeric azido-alcohols 33 and 34 in an approximate 1 1 ratio. The secondary azide was reductively cyclized with triphenylphosphine at ambient temperature, whereas the tertiary azide required heating to effect the same transformation. In this way, the desired aziridines 35 and 36 were prepared in good yield on multigram scale. 

Lexicon Pharmaceuticals, Corporate Headquarters, The Woodlands, TX 77381, (3) Thus Therapeutics, Inc, San Diego, CA 92121, (4) ActiveSight, San Diego 92121... 

The coordination of this entire complex process is the province of project management, the objective of which is to ensure that all the necessary parts and components of a project mate up. This discipline in its modem form was first developed for the Polaris missile project in the 1960s. Its major tool that is familiar to pharmaceutical scientists is the network or PERT (Program Evaluation Review Technique) chart, as illustrated in Figure 1.2. This chart is a tool that allows one to see and coordinate the relationships between the different components of a project. One outcome of the development of such a network is identification of the rate-limiting steps, which, in aggregate, comprise the critical path (see Table 1.3 for a lexicon of the terms used in project management). 

Unacceptable starting materials used in research must be replaced by those which meet the regulatory quality and safety criteria. Reference to standard volumes of pharmaceutical ingredients and excipients should be made to decide whether a certain ingredient can be used. Standards are described in the pharmacopoeias of relevant countries, the "Handbook of Pharmaceutical Excipients" or its Swiss anchestor the "Katalog pharmazeutischer Hilfsstoffe". Fiedler s "Lexikon der Hilfsstoffe" (Lexicon of Excipients) provides many useful informations about the safety and about applications for excipients. (For references see Annex B to the registration requirements chapter.)... 

Lexikon der Hilfsstoffe fuer Pharmazie, Kosmetik und angrenzende Gebiete. (Lexicon of excipients for pharmaceuticals, cosmetics and related areas) Editio Cantor, Aulendorf/Germany, 1989... 

Pharmaceutical Company Directory, Worldwide http //www.pharma-lexicon.com/pharmaceutical-companies.php... 

Medi-lexicon (formerly pharmalexicon). URL http //www. pharma-lexicon.com/. A dictionary of medical, pharmaceutical, biomedical and healthcare terms, acronyms, and abbreviations. 

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