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European Patent Office Appeal Board Rules in Favor of Alnylama?s Kreutzer-Limmer Patent

^{Published on 2010-05-19 06:07:24 - Market Wire}
 

CAMBRIDGE, Mass.--([ BUSINESS WIRE ])--Alnylam Pharmaceuticals, Inc. (Nasdaq: ALNY), a leading RNAi therapeutics company, announced today that the Board of Appeals of the European Patent Office (EPO) has ruled that claims of the Kreutzer-Limmer a™945 (EP 1214945) patent meet needed requirements under European patent law. The a™945 patent comprises broad claims covering the length and certain structural requirements for siRNAs that are important for advancement of RNAi therapeutics.

"Alnylam has leveraged its unparalleled intellectual property estate to enable the field with freedom to operate for RNAi therapeutics as evidenced by more than 25 licensing agreements yielding over $700 million in realized cash funding, and we expect this to continue in the future."

The a™945 patent is one of a number of patents in the Kreutzer-Limmer estate. Other distinct patents in the family include EP 1550719, or a™719, which covers siRNAs comprising 15-21 nucleotides in length stabilized by chemical linkages. In addition, patents from the Kreutzer-Limmer patent family have been granted in other countries, including Germany (DE 10080167 and DE 10066235) with claims covering siRNAs with lengths of 15-49 nucleotides. Many additional patents from the Kreutzer-Limmer patent family are pending in the U.S., Japan, and other countries.

aWe are very pleased with the outcome of the EPO proceedings today for the Kreutzer-Limmer a™945 patent,a said Barry Greene, President and Chief Operating Officer of Alnylam. aAlnylam has leveraged its unparalleled intellectual property estate to enable the field with freedom to operate for RNAi therapeutics as evidenced by more than 25 licensing agreements yielding over $700 million in realized cash funding, and we expect this to continue in the future.a

aWe are gratified with the EPO ruling today in relation to our early discoveries in the RNAi field,a said Roland Kreutzer, Ph.D., Head of Rochea™s Center of Excellence for RNA Therapeutics in Kulmbach, Germany, and an inventor on the Kreutzer-Limmer patent series. aWe are very excited about the progress being made in the field of RNAi research and are absolutely committed to advancing RNAi therapeutics to patients. Clearly, a strong IP estate is critical for the success of such an endeavor, and Alnylam and its partners, such as Roche, uniquely enjoy this benefit.a

The claims of the a™945 patent as maintained cover methods, medicaments and uses of siRNAs with a double-stranded structure (dsRNA) consisting of 15 to 49 nucleotides.

About Alnylam Intellectual Property (IP)

Alnylama™s IP position is comprised of fundamental, chemistry, and target IP that the company believes is necessary for the development and commercialization of RNAi therapeutics. In aggregate, Alnylam owns or has in-licensed over 1,800 active patent cases, of which over 700 have issued or been granted worldwide, and over 300 have issued or been granted in the U.S., Europe, or Japan, the worlda™s largest pharmaceutical markets.

Alnylama™s IP estate includes issued, allowed, or granted fundamental patents in many of the worlda™s major pharmaceutical markets that claim the broad structural and functional properties of RNAi therapeutic products. These include, but are not limited to:

• the Crooke Patents (U.S. Patent Nos. 5,898,031, 6,107,094, 7,432,249, 7,432,250, 7,629,321 and EP 0928290) issued in over 15 countries and licensed exclusively from Isis Pharmaceuticals, Inc. to Alnylam for RNAi therapeutics, which cover compositions, methods, and uses of modified oligonucleotides, including double stranded RNAs, to inactivate a target mRNA mediated by a double stranded RNase, such as aRISC,a which is the cellular enzyme complex that mediates RNAi;
• the Glover a™375 patent (EP 1230375), granted in July 2005, licensed exclusively to Alnylam from Cancer Research Technologies, Ltd., and currently under appeal, which covers therapeutic uses of double-stranded RNA expressed from endogenous templates or expression vectors to mediate RNA interference in mammalian cells;
• the Kreutzer-Limmer I a™719 patent (EP 1550719), owned by Alnylam and where the company has received a notification of aintent to granta™, which covers siRNAs comprising 15-21 nucleotides in length stabilized by chemical linkages;
• the Kreutzer-Limmer I a™235 patent (DE 10066235), granted in January 2008 and owned by Alnylam, which covers methods, uses, and medicaments of siRNAs, with a length between 15 and 49 nucleotides, expressed through a vector;
• the Kreutzer-Limmer I a™945 patent (EP 1214945) granted in June 2005 and owned by Alnylam, which covers compositions, methods, and uses of siRNAs with a length between 15 and 49 nucleotides;
• the Kreutzer-Limmer II a™061 patent (EP 1352061), granted in May 2006 and owned by Alnylam, which covers therapeutic compositions, methods, and uses of siRNA and derivatives directed toward approximately 130 disease targets;
• the Tuschl I patent (EP 1309726), granted in December 2009, and exclusively licensed to Alnylam from the Max Planck Society, the Massachusetts Institute of Technology, and Whitehead Institute, which covers methods for using certain dsRNAs for RNAi;
• the Tuschl II a™704 patent (U.S. Patent No. 7,056,704) issued in June 2006 and exclusively licensed to Alnylam from the Max Planck Society, which broadly covers methods of making siRNAs to silence any and all disease target genes;
• the Tuschl II a™196 patent (U.S. Patent No. 7,078,196) issued in July 2006 and exclusively licensed to Alnylam from the Max Planck Society, which broadly covers methods of making siRNAs with or without chemical modifications;
• the Tuschl II a™044 patent (EP 1407044), granted in January 2008 and exclusively licensed to Alnylam from the Max Planck Society, which broadly covers compositions, methods, and uses of siRNAs;
• the Tuschl II patent (JP 4 095 895) granted in May 2008 in Japan and exclusively licensed to Alnylam from the Max Planck Society, which broadly covers compositions, methods, uses, and systems of siRNAs;
• the Tuschl II patent (JP Application No. 2006-317758) granted in March 2010 in Japan and exclusively licensed to Alnylam from the Max Planck Society, which broadly covers compositions, methods, uses, and systems of siRNAs;
• the Tuschl II patent (Application No. 01820900.9) in China which received an intent to grant in April 2009 and exclusively licensed to Alnylam from the Max Planck Society, which broadly covers compositions, methods, uses, and systems for siRNAs;
• the Kay & McCaffrey patent (AU patent application no. 2002326410) granted in February 2009 in Australia and exclusively licensed to Alnylam from Stanford University, which broadly covers methods and composition for RNAi therapeutics including siRNAs and shRNAs; and,
• many divisional and continuing patent applications pending of the aforementioned issued or granted patents and additional patent applications pending, including patents and patent applications covering inventions by Crooke, Fire & Mello (U.S. Patent No. 6,506,559), Kreutzer & Limmer, Glover, Li & Kirby, Pachuk, Tuschl, Hannon, Giordano, and Kay & McCaffrey, amongst others.

In addition to fundamental patents, Alnylam is the exclusive licensee in the field of RNAi therapeutics for more than 175 issued chemistry patents owned or controlled by Isis Pharmaceuticals, Inc. broadly covering chemical modifications, including motifs and patterns of modifications of oligonucleotides, including RNAi therapeutics. These patents include:

• 2a™-Ribose modifications of oligonucleotides (Cook, U.S. Patent Nos. 5,670,633; 6,005,087; 6,531,584; and 7,138,517);
• chemical conjugates of oligonucleotides (Manoharan, U.S. Patent No. 6,153,737);
• overhang, blunt-end, and nucleotide pairing design motifs (Woppmann et al., UK 2417727 and U.S. Patent Application No. 10/560,336), which is owned by Alnylam; and,
• chemically modified siRNAs of any length with phosphorothioate and 2a™-O-alkyl modifications (Manoharan II, EP Application No. 04 718 537).

In addition to fundamental and chemistry patents, Alnylam is also the exclusive licensee in the field of RNAi therapeutics for certain delivery patents, including those owned and controlled by Tekmira Pharmaceuticals Corporation, broadly covering delivery of oligonucleotides, including RNAi therapeutics, with liposomal formulations. These patents include:

• formulations of oligonucleotides, including siRNAs, in cationic liposomes (Wheeler, U.S. Patent Nos. 5,976,567 and 6,815,432; and Semple, U.S. Patent No. 6,858,225); and,
• chemically modified siRNAs with adrug-likea properties for in vivo delivery (Soutschek and Manoharan, U.S. patent application 10/916,185 /Allowed).

Alnylam is also contributing on a royalty-free/non-profit basis its technology and more than 1,500 issued or pending patents from its RNAi patent estate to Pool for Open Innovation against Tropical Disease initiated by GlaxoSmithKline in 2009. The patent pool was formed to aid in the discovery and development of new medicines for the treatment of 16 neglected tropical diseases (NTD), as defined by the U.S. Food and Drug Administration, in the worlda™s least developed countries. In January 2010, BIO Ventures for Global Health (BVGH) was chosen as administrator of patent pool. In this role, BVGH will organize disease-specific meetings that identify the gaps in expertise and intellectual property that currently exist in product development for NTDs, and will help global health researchers work with industry to fill these gaps to create medicines for NTDs faster and more efficiently.

About RNA Interference (RNAi)

RNAi (RNA interference) is a revolution in biology, representing a breakthrough in understanding how genes are turned on and off in cells, and a completely new approach to drug discovery and development. Its discovery has been heralded as aa major scientific breakthrough that happens once every decade or so,a and represents one of the most promising and rapidly advancing frontiers in biology and drug discovery today which was awarded the 2006 Nobel Prize for Physiology or Medicine. RNAi is a natural process of gene silencing that occurs in organisms ranging from plants to mammals. By harnessing the natural biological process of RNAi occurring in our cells, the creation of a major new class of medicines, known as RNAi therapeutics, is on the horizon. Small interfering RNAs (siRNAs), the molecules that mediate RNAi and comprise Alnylama™s RNAi therapeutic platform, target the cause of diseases by potently silencing specific mRNAs, thereby preventing disease-causing proteins from being made. RNAi therapeutics have the potential to treat disease and help patients in a fundamentally new way.

About Alnylam Pharmaceuticals

Alnylam is a biopharmaceutical company developing novel therapeutics based on RNA interference, or RNAi. The company is applying its therapeutic expertise in RNAi to address significant medical needs, many of which cannot effectively be addressed with small molecules or antibodies, the current major classes of drugs. Alnylam is leading the translation of RNAi as a new class of innovative medicines with peer-reviewed research efforts published in the worlda™s top scientific journals including Nature, Nature Medicine, and Cell. The company is leveraging these capabilities to build a broad pipeline of RNAi therapeutics for the treatment of a wide range of disease areas, including respiratory syncytial virus (RSV), liver cancers, TTR-mediated amyloidosis (ATTR), hypercholesterolemia, and Huntingtona™s disease. In addition, Alnylam formed Alnylam Biotherapeutics, a division of the company focused on the development of RNAi technologies for application in manufacturing processes for biotherapeutic products, including recombinant proteins and monoclonal antibodies. The companya™s leadership position in fundamental patents, technology, and know-how relating to RNAi has enabled it to form major alliances with leading companies including Medtronic, Novartis, Biogen Idec, Roche, Takeda, Kyowa Hakko Kirin, and Cubist. Alnylam and Isis are joint owners of Regulus Therapeutics Inc., a company focused on the discovery, development, and commercialization of microRNA-based therapeutics. Founded in 2002, Alnylam maintains headquarters in Cambridge, Massachusetts. For more information, please visit [ www.alnylam.com ].

Alnylam Forward-Looking Statement

Various statements in this release concerning Alnylama™s future expectations, plans and prospects, constitute forward-looking statements for the purposes of the safe harbor provisions under The Private Securities Litigation Reform Act of 1995. Actual results may differ materially from those indicated by these forward-looking statements as a result of various important factors, including the companya™s ability to successfully research and develop products and to successfully prosecute and enforce its patents around the world, as well as those risks more fully discussed in the aRisk Factorsa section of its most recent quarterly report on Form 10-Q on file with the Securities and Exchange Commission. In addition, any forward-looking statements represent Alnylama™s views only as of today and should not be relied upon as representing its views as of any subsequent date. Alnylam does not assume any obligation to update any forward-looking statements.