Intellectual Asset Estate
Intellectual property:
We believe Regulus has established an unparalleled patent position in the field of microRNA therapeutics. The Regulus portfolio includes early fundamental patent filings in the field of microRNA, as well as more than 900 patents and patent applications (over 600 issued) pertaining to modifications of oligonucleotides for therapeutic applications. Additional patent rights are directed to specific microRNA compositions and therapeutic methods of use. The combination of these different types of patent rights allows Regulus to build multiple layers of patent protection for each therapeutic target.
Fundamental Intellectual Property
Regulus has exclusive rights to patent filings stemming from early and pioneering discoveries that are broadly applicable to microRNA therapeutics, such as the identification of microRNA sequences.
- A fundamental and very early piece of IP is the Tuschl III patent series, based on the discovery of more than 100 naturally occurring mammalian microRNAs by Dr. Tuschl and colleagues at the Max Planck Institute, to which Regulus has exclusive therapeutic rights. The first patents from the Tuschl III series claiming miR-122 and antisense sequences, have been granted by the US, Japan and Australia patent offices (US Patent No. 7,232,806).
- Regulus also has access on a non-exclusive basis to IP stemming from the discovery by Dr. Tuschl of additional novel microRNAs, during his research activities at The Rockefeller University.
Other fundamental patent filings relate to drug design motifs that are optimal for microRNA drug product activity. Additional IP is created as Regulus applies its technical expertise and know-how to the optimization of microRNA compounds and identifies new drug design motifs.
- Various designs of microRNA modulators, including 2'-MOE anti-miRs, are included in the 'Esau' patent series, owned by Regulus, which is one of the earliest filings in the microRNA IP landscape.
- The cholesterol-conjugated anti-miR design is captured in the 'antagomir' patent family, owned by Alnylam and exclusively licensed to Regulus for microRNA therapeutics (US Patent No. 7,582,744).
- Additional microRNA drug design motifs having various combinations of modifications, such as 2'-MOE, 2'-fluoro and bicyclic nucleic acid modifications are claimed in Regulus' pending patent applications.
Intellectual Property Specific to microRNA compositions and function
The Regulus patent estate includes claims to specific microRNA compositions that are optimized for therapeutic use. As Regulus know-how is applied to the development of microRNA modulators with improved potency, new IP is generated for each of these microRNA compositions.
Regulus internal drug discovery efforts and external collaborator activities lead to the establishment of IP related to methods of use of microRNA modulators for specific therapeutic indications. Examples of method of use patent filings are in the therapeutic areas of metabolism, oncology, virology, inflammation, and immune response.
For example, Regulus exclusively controls the patent rights pertaining to the use of miR-122 antagonists for the treatment of HCV, which originated from Dr. Peter Sarnow's discovery that antagonism of miR-122 affects HCV replication (US Patent No. 7,307,067).
Chemical Modification Intellectual Property
Regulus utilizes a comprehensive and versatile toolbox of oligonucleotide modifications, many of which are protected by patents owned by Isis or Alnylam. Regulus has been granted exclusive rights to Isis' and Alnylam's vast chemical modification IP estates, for microRNA applications. These rights grant Regulus access to a portfolio of over 900 patents and patent applications, including over 600 issued patents, owned by Isis and Alnylam and pertaining to chemical modifications of oligonucleotides for therapeutic applications.
Representative examples of chemical modification IP include patents covering 2'-MOE modifications, bicyclic nucleic acid modifications, and oligonucleotide conjugates.
