News | July 15, 1998

Irori Patents Combinatorial Chemistry System

By Angelo DePalma

Irori (La Jolla, CA) has received two U.S. patents (Nos. 5,751,629 and 5,741,462) for its direct sorting combinatorial chemistry technology, which combines the advantages of two well-known chemical synthesis approaches ("parallel" and "split and pool") with a radiofrequency (RF) tagging device. This combination provides a rapid, economical means to generate large numbers of unique chemical compounds.

"These two patents, with several more pending, represent a strong patent portfolio for our core technology," said John Lillig, vice president of research and development at Irori. "This technology is the foundation of our highly successful AccuTag line of combinatorial chemistry systems, in use at over 50 pharmaceutical and biotechnology companies worldwide. It is also the focus of our two recent alliances with Bristol-Myers Squibb and Rhone-Poulenc Rorer, in which we're developing customized systems for the rapid development of their drug discovery efforts."

Directed sorting technology uses microreactors and RF tagging to produce discrete compounds, rather than mixtures. A single compound is synthesized in each microreactor, while the RF tag records the sorting process that occurs between chemical synthesis steps. Radiofrequency tagging of microreactors also provides convenient and positive identification of compounds for archival purposes. Using this technology, compounds can be sorted at a rate of more than 1, 000 per hour for the rapid generation of libraries of thousands of compounds.

"Not only has this technology been important to the advancement of combinatorial chemistry, but it can also be used in a multiplicity of applications such as isolation and purification, as well as analytical sample tracking, chemical compound archiving, high throughput screening and the capture and detection of macromolecules," Lillig added. "We will be looking to license the technology for any applications outside of our combinatorial chemistry focus."

Directed Sorting and Radiofrequency Tagging

Directed sorting, enabled by RF tagging, sets Irori's instruments apart from other combinatorial systems.

Fig. 1: Directed sorting diagram.

Directed sorting (Figure 1) is made possible by splitting and pooling RF tagged microreactors rather than individual solid phase resin beads. During the first directed sorting step each microreactor is assigned to one specific compound. This assignment is maintained during all subsequent "directed sorting" and synthesis steps and assures that:

  • Every desired compound is synthesized
  • Only one copy of each compound is synthesized
  • All compounds are present as discrete entities (no mixtures)

Fig. 2: RF tag diagram.

Each microreactor contains a miniature radiofrequency (RF) tag that is a unique label used to identify it during the sorting processes that occur between chemical synthesis steps (Figure 2). The glass-encased RF tag (Figure 3) provides a unique ID for each microreactor and therefore each compound. This unique ID allows each microreactor to be identified during the combinatorial "directed sorting" process.

Fig. 3: Glass-encased RF tag.

Irori has formed collaborations with Bristol-Myers Squibb and Rhone-Poulenc Rorer (custom combinatorial chemistry systems), DuPont Merck and Hewlett Packard (drug discovery).

For more information: Richard K. Brown, VP of marketing and sales, Irori, 11149 North Torrey Pines Rd., La Jolla, California 92037. Tel: 619-546-1300, ext. 125.