United States Patent and Trademark Office allows a patent application within ‘Esau’ patent family

Regulus Therapeutics Inc., founded by Alnylam Pharmaceuticals, Inc. (Nasdaq: ALNY), and Isis Pharmaceuticals, Inc. (Nasdaq: ISIS), announced today that the United States Patent and Trademark Office (USPTO) has allowed a patent application within the ‘Esau’ patent family (US Application Serial No. 10/909,125). The Esau patent estate, which is owned exclusively by Regulus, represents one of the earliest filings in the microRNA intellectual property landscape, and is fundamental to the discovery, development, and commercialization of microRNA therapeutics.

“Regulus is advancing a new class of innovative medicines based on microRNAs. Indeed, microRNA therapeutics represent a new frontier of pharmaceutical research where an entire pathway of human disease can be targeted,” said Kleanthis G. Xanthopoulos, Ph.D., President and Chief Executive Officer of Regulus Therapeutics. “This Notice of Allowance is the first in the Esau series, and we expect many more patents covering microRNA therapeutics to issue from this important and early patent family.”

The currently allowed claims describe methods of inhibiting miR-122, a liver-specific microRNA that has been shown to facilitate replication of hepatitis C virus (HCV) infection (Jopling et al. (2005) Science 309, 1577-81). Specifically, the claims encompass methods of inhibiting miR-122 in a cell using a broad class of anti-miRs with sugar modifications at each nucleoside, such as 2’-MOE or bicyclic nucleic acid modifications, and with or without the addition of conjugate groups. Regulus holds exclusive rights to additional patents covering miR-122 antagonists and their use as HCV therapeutics, including the ‘Tuschl III’ patent claiming the sequences of miR-122 and its complement (U.S. Patent No. 7,232,806), and the Sarnow patent pertaining to the use of anti-miR-122 to inhibit HCV replication (US Patent No. 7,307,067).

“The Regulus miR-122 program is focused on developing a therapeutic oligonucleotide that antagonizes miR-122, a microRNA that has been shown to be essential for HCV replication,” said Peter Linsley, Chief Scientific Officer of Regulus Therapeutics. “We are very pleased by the decision of the USPTO to allow the current claims of the Esau ‘125 application, as it will strengthen our continued advancement of this important program.”

Following a Notice of Allowance, the process resulting in final issuance of a patent involves several administrative steps that are typically completed within a year.