Incyte Corp v. Concert Pharmaceuticals Inc

1. Case Identification

• Case #: PGR2021-00006
• Patent #: 10,561,659
• Filed: October 28, 2020
• Petitioner(s): Incyte Corporation
• Patent Owner(s): Concert Pharmaceuticals, Inc.
• Challenged Claims: 1-21

2. Patent Overview

• Title: Methods of Treating Hair Loss with Deuterated Ruxolitinib
• Brief Description: The ’659 patent discloses methods of treating hair loss disorders, such as alopecia areata, by administering specific doses of an octa-deuterated analog of ruxolitinib (referred to as "Compound (I)"). The patent also claims pharmaceutical compositions containing specific amounts of Compound (I).

3. Grounds for Unpatentability

Ground 1: Obviousness over Silverman, Xing, and Ruxolitinib PI - Claims 1-21 are obvious over Silverman in view of Xing and Ruxolitinib Prescribing Information.

• Prior Art Relied Upon: Silverman (Patent 9,249,149), Xing (a 2014 journal article), and Ruxolitinib Prescribing Information (a 2015 Physician’s Desk Reference excerpt).
• Core Argument for this Ground:
  • Prior Art Mapping: Petitioner argued that the combination of references taught all limitations of the challenged claims. Silverman disclosed Compound (I), a deuterated analog of ruxolitinib, and expressly taught its use for treating diseases that are beneficially treated by ruxolitinib. Xing taught that ruxolitinib is highly effective for treating alopecia areata (a hair loss disorder) in humans with oral doses of 20 mg twice daily. The Ruxolitinib Prescribing Information disclosed FDA-approved formulations, oral tablet administration, and established dosing ranges for ruxolitinib (5 mg to 50 mg daily) that encompass the doses claimed in the ’659 patent. Petitioner contended that substituting the known deuterated equivalent from Silverman for ruxolitinib to treat a known indication taught by Xing, using a dosage within the known effective range taught by the Prescribing Information, rendered the claims obvious.
  • Motivation to Combine: A POSITA would combine the references to develop an alternative treatment for alopecia areata with at least equal efficacy to ruxolitinib. Silverman provided the explicit motivation to use Compound (I) for any condition treated by ruxolitinib. Further motivation arose from the well-understood goal of deuteration: to improve a drug's metabolic properties (e.g., longer half-life, improved safety profile) while retaining the parent drug’s therapeutic efficacy.
  • Expectation of Success: A POSITA would have had a high expectation of success. The art taught that deuterium substitution is a minimal structural change not expected to alter a drug’s biochemical potency or selectivity. Therefore, it was predictable that Compound (I) would be effective in treating alopecia areata, just as ruxolitinib was known to be. Success in formulating specific oral tablet dosages was also expected, as this was a routine practice for which the prior art provided extensive guidance.

Ground 2: Obviousness over Silverman, Christiano, and Ni - Claims 1-21 are obvious over Silverman in view of Christiano and Ni.

• Prior Art Relied Upon: Silverman (Patent 9,249,149), Christiano (Patent 9,198,911), and Ni (Application # 2014/0135350).

• Core Argument for this Ground:

  • Prior Art Mapping: This ground presented a similar argument using a different combination of references. As in Ground 1, Silverman disclosed Compound (I). Christiano, like Xing, taught the use of ruxolitinib to treat hair loss disorders, including alopecia areata. Ni disclosed that immediate-release tablets of ruxolitinib phosphate were commercially available in various strengths (5, 10, 15, 20, and 25 mg), reinforcing the known effective dose ranges and oral tablet formulation. Petitioner argued that the combination rendered the claimed subject matter obvious for reasons analogous to Ground 1.
  • Motivation to Combine: The motivation was substantially the same as in Ground 1. Silverman provided the deuterated compound and the rationale for its use. Christiano provided the specific therapeutic target (hair loss). Ni provided further guidance on established, commercially successful dosage forms and strengths. A POSITA would have been motivated to combine these teachings to create a therapy for alopecia areata with the potential benefits of deuteration.
  • Expectation of Success: The expectation of success was similarly high. The structural similarity between Compound (I) and ruxolitinib, combined with Christiano's teaching of ruxolitinib's efficacy and Ni's disclosure of standard oral dosage forms, would lead a POSITA to reasonably expect that Compound (I) would be effective and could be formulated into oral tablets at the claimed doses.

• Additional Grounds: Petitioner also asserted that claim 8 is anticipated by Silverman under 35 U.S.C. §102. Petitioner argued Silverman expressly disclosed a pharmaceutical composition comprising Compound (I) with a pharmaceutically acceptable carrier, at least 95% deuterium incorporation, and within dosage ranges that encompass the claimed 8 mg and 12 mg amounts.

4. Key Claim Construction Positions

• "[A]t least 95% incorporation of deuterium": Petitioner argued that this phrase, as defined in the specification, refers to the isotopic enrichment at each of the eight designated deuterium positions independently. Consequently, a POSITA would understand that a collection of molecules meeting this limitation could contain as little as 66% (0.95^8) of molecules that are fully octa-deuterated. This construction broadens the scope of the claims, making them more susceptible to invalidity challenges.

5. Relief Requested

• Petitioner requests institution of a post-grant review and cancellation of claims 1-21 of Patent 10,561,659 as unpatentable.