A Broad Outline Of A Genus's Perimeter Is Insufficient For Written Description Of The Members Of The Genus

• Published date: 24 April 2023
• Subject Matter: Intellectual Property, Patent
• Law Firm: Oblon, McClelland, Maier & Neustadt, L.L.P
• Author: Ms Marina I. Miller

The Regents of the University of Minnesota ("Minnesota") appealed from a final decision of the U.S. PTO Patent Trial and Appeal Board ("the Board") holding that the claims of U.S. Patent 8,815,830 were unpatentable as anticipated. The Court of Appeals for the Federal Circuit ("the Court") affirmed.

Gilead Sciences, Inc. ("Gilead") filed an IPR petition challenging the claims of the '830 patent directed to phosphoramidate prodrugs of nucleoside derivatives that prevent viruses from reproducing or cancerous tumors from growing. Representative claim 1 reads:

1. A compound of formula I

wherein

R1 is guanine, cytosine, thymine, 3-deazaadenine, or uracil, optionally substituted by 1, 2, or 3 U; wherein each U is independently halo, hydroxy, (C1-C6)alkyl, (C3-C6)cycloalkyl, (C1-C6)alkoxy, (C3-C6)cycloalkyloxy, (C1-C6)alkanoyl, (C1-C6)alkanoyloxy, trifluoromethyl, hydroxy(C1-C6)alkyl, -(CH2)1-4P(=O)(ORw)2, aryl, aryl(C1-C6)alkyl, or NRxRy;
R2 is halo;
R6 and R7 are independently H or (C1-C6)alkyl; R3 is hydroxy;
R4 is hydrogen, (C1-C6)alkyl, (C3-C6)cycloalkyl, aryl, aryl(C1-C6)alkyl, or 2-cyanoethyl;
R5 is an amino acid;
X is oxy, thio, or methylene;
each Rw is independently hydrogen or (C1-C6)alkyl; Rx and Ry are each independently hydrogen, (C1-C6)alkyl, (C3-C6)cycloalkyl, phenyl, benzyl, phenethyl, or (C1-C6)alkanoyl; or Rx and Ry together with the nitrogen to which they are attached are pyrrolidino, piperidino or morpholino;
wherein any (C1-C6)alkyl of R1, R4-R7, Rw, Rx, and Ry is optionally substituted with one or more halo, hydroxy, (C1-C6)alkoxy, (C3-C6)cycloalkyloxy, (C1-C6)alkanoyl, (C1-C6)alkanoyloxy, trifluoromethyl, azido, cyano, oxo (=O), (C1-C6)alkyl, (C3-C6)cycloalkyl, (C3-C6)cycloalkyl(C1-C6)alkyl, (C1-C6)alkyl-S-(C1-C6)alkyl-, aryl, heteroaryl, alkyl(C1-C6)alkyl, or heteroaryl(C1-C6)alkyl, or NRajRak; wherein each Raj and Rak is independently hydrogen, (C1-C6)alkyl, (C3-C6)cycloalkyl, phenyl, benzyl, or phenethyl; and
wherein any aryl or heteroaryl may optionally be substituted with one or more substituents selected from the group consisting of halo, hydroxy, (C1-C6)alkyl, (C3-C6)cycloalkyl, (C1-C6)alkoxy, (C3-C6)cycloalkyloxy, (C1-C6)alkanoyl, (C1-C6)alkanoyloxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, and amino; or
a pharmaceutically acceptable salt thereof.

Sofosbuvir falls within the claimed genus and is an FDA-approved drug marketed by Gilead for treating chronic hepatitis C infections. If the '830 patent were found to be valid, it...