PDF, Patent Landscape Report on Atazanavir - WIPO

CATEGORIES WITH HIGHEST EMPHASISWhen the entire collection is compared by category, and the categories with the highestemphasis within each assignee group is noted, similarities and differences in assigneeemphasis can be noted (Figure 24).The commercial entities are relatively similar in chemical and formulation emphasis, withtheir highest focus on synthesis, and stereospecific synthesis in particular. Most of the drugcandidates for this target (viral protease) are peptide mimetics which must stereospecificallybind to a site on the surface of the target. Commercial focus on this issue is understandablesince the efficacy, cost of goods and reduction of side-effects all rest on the effectiveness ofstereospecific synthesis of a drug with multiple stereoisomeric centers (molecular linkageswhich are required to be in the appropriate orientation, left-handed or right-handed).In the area of combinations, Novartis/BMS places slightly more emphasis on combinationswith other protease inhibitors and reverse transcriptase inhibitors than with integrase. It alsoemphasizes auto-immune indications and cancer but there is little evidence of pursuit ofneurologic or other anti-viral indications.Figure 24. Emphasis on Categories in Drug DevelopmentChemistryCombinationsFormulationsIndicationsCOMPARING TECHNICAL EMPHASIS OF TOP COMPANIESThe categories listed above allowed creation of a matrix (Figure 25) that compares eachcompany for activity in different technical areas. The companies selected for the matrix area sampling (44 of 288) of the full list available in Appendix B, and include those companiesthat have an approved HIV-protease inhibitor drug.30