Genesis Pharmaceuticals (Cambridge, MA) -- Combinatorial Chemistry ???

merlin merlin at neuro.usc.edu
Mon Oct 10 05:39:52 EST 1994


Does anyone have any clue, reference, citations, papers describing the
combinatorial chemistry technology invented by Genesis Pharmaceuticals?

According to Biotechnology 12:446-449 (12 May 1994):

  "Sphinx [Pharmaceuticals (Durham, NC)] purchased Genesis [Pharmaceuticals
   (Cambridge, MA)] through a stock exchange valued at roughtly $3.8 million.
   It then sold Genesis' combinatorial chemistry technology to Lilly for
   about $50 million, more than 13 times the amount it paid for this
   technology."

  "Sphinx's nonpeptide compounds ... are of molecular weights under 500 to
   assure oral bioavailability, and they require minimal, if any, additional
   modification, says the firm.  Sphinx constructs its compounds by carrying
   out a multistep organic synthesis procedure.  This synthesis is conducted
   on a solid support by first introducing a 'scaffold' molecule and then
   introducing functional groups important for target recognition, with
   these functional groups--up to three or four at a time--placed around
   the scaffold in numerous variations.  After one round of combinatorial
   chemistry on a first scaffold, Sphinx adds a second scaffold and conducts
   an additional round of combinatorial chemistry.  Using two such rounds of
   construction, Sphinx can turn 10 functional groups and 10 scaffolds into
   1 million structurally unique molecules.  Moreover, removal of the final
   compound from the solid support generates a soluable entity for testing."

I couldn't find any references to this technology in medline.  Could someone
provide more detailed information (published papers, published patents, etc)
describing this apparently novel combinatorial chemistry synthesis technique.

Thanks, AJ

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