36
Jurisdiction
Patent/
Application
No.
Title
Expiration
DescriptionofClaims
UnitedStates ...........
7,015,315
GAPPED
OLIGONUCLEOTIDES
2023
Covers 2’-O-alkyl-O-alkyl gapmer
oligonucleotides.
BicyclicNucleosideGapmerOligonucleotides
In addition, we have pursuedpatent claims to antisense drugdesignmotifs incorporating bicyclic nucleoside analogs, which
include lockednucleic acids, or LNAs. In June 2011, theEuropeanPatentOffice, or EPO, grantedour claims drawn to short gapmer
oligonucleotides, 10 to14nucleotides in length, withbicyclic nucleosides, which includes locked nucleic acids, in thewings for the
treatment of cardiovascular ormetabolic disorders. Santaris has opposed this grantedpatent andwe intend tovigorouslydefendour
patent in these proceedings. We have also successfully obtained issuedpatent claims coveringgapmer antisense drugdesignmotifs
that incorporate our cEtmodifiednucleosides. The followingpatents are some examples of our issuedpatents and allowedpatent
applications in this category:
Jurisdiction
Patent/
Application
No.
Title
Expiration
DescriptionofClaims
Europe...................
EP2021472
COMPOUNDSAND
METHODSFOR
MODULATINGGENE
EXPRESSION
2027
Short gapmer oligonucleotides, 10 to14
nucleotides in length, withbicyclic
nucleosides, which includes cEt locked
nucleic acids, in thewings for the treatment
of cardiovascular ormetabolic disorders
UnitedStates .........
7,750,131
6-MODIFIEDBICYCLIC
NUCLEICACIDANALOGS
2027
Covers cEt containinggapmer compounds
Europe...................
EP2092065
ANTISENSECOMPOUNDS
2027
Gapmer compounds havingwings comprised
of 2’-MOE andbicyclic nucleosides
TherapeuticMethods of Treatment andAntisenseDrugSequences
In addition toour broad core patents, we alsoownhundreds of patents, worldwide, with claims to antisense sequences and
compounds directed toparticular therapeutically important targets ormethods of achieving clinical endpoints using these antisense
compounds. Target patentsmay also include claims reciting the specific nucleic acid sequences utilized byour products, independent
of chemicalmodifications andmotifs. In addition, our product specific patents typically include claims combining specific nucleic
acid sequenceswithnucleosidemodifications andmotifs. In thisway, we seekpatent claims narrowly tailored toprotect our products
specifically, in addition to the broader core antisense patents described above.
ApoB100andKYNAMRO
In2008, we obtainedpatent claims in theUnitedStates drawn to the use of both single-stranded anddouble-stranded
antisense drugs complementary to any site of themRNAof human apoB, regardless of chemistryor antisensemechanismof action.
The patent provides broadprotectionof the Isis-Genzyme apoB franchise, includingKYNAMRO andpotential future follow-on
compounds. Similar claims granted inAustralia and Japan in 2009 and2010, respectively. We andGenzyme obtained issued claims
to the specific antisense sequence and chemical compositionofKYNAMRO in theUnitedStates, Australia, SouthAfrica, India and
theEuropeanUnion. The issuedU.S. claims shouldprotectKYNAMRO fromgeneric competition in theUnitedStates until at least
2025. We are alsopursuing additional patent applications designed toprotect KYNAMRO in these andother jurisdictions including
Canada and Japan. The table below lists the key issuedpatent claims designed toprotectKYNAMRO in the applicable jurisdiction:
