Pre-Meeting AIPLA Mid-Winter Meeting January 22, 2012 Las Vegas Sumiko Kobayashi Patent Attorney

1. IP High Court Case ReviewFinding of Invention Disclosed in Cited Prior Art in Finding Non-Inventive Step Pre-Meeting AIPLA Mid-Winter Meeting January 22, 2012 Las Vegas Sumiko Kobayashi Patent Attorney 1

2. 1. This is Particulars of Decision Case: Heisei 21 (Gyo-Ke) 10180 Case to Seek Rescission of Trial Decision Rendered: August 18, 2010 Contents of Judgment: The trial decision dated February 25, 2009 rendered by JPO in Invalidation Trial Case No. 2008-800062 is rescinded. 2

3. 2. Patent claim • [Claim 6] A solid pharmaceutical composition for the treatment and prevention of diseases involving bone resorption, comprising 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid monosodium salt trihydrate as an active ingredient. Hereinafter, 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid monosodium salt trihydrate is referred to as “Alendronate-Na-3H2O”. 3

4. 3. Logic of Ease of Inventionin JPO decision Main Cited Invention • Alendronate-Na-3H2O is disclosed in Exhibit A-7 (“A-7”) • Difference between Present Invention and A-7 is Solid Pharmaceutical. Sub-Cited Invention • Using a pharmaceutical active ingredient in a solid formulation was known. Formulating Pharmaceutical in A-7 into solid formulation was easy. 4

5. 4. Exhibit A-7 5

6. 4. Exhibit A-7

7. 4. Exhibit A-7 7

8. The Reason for Finding Alendronate-Na-3H2O in A-7in JPO decision Reasonable assumption of presence of Alendronate-Na-3H2O • The A-7 is on drug analysis for a person to carry out experiment on pharmaceutical dosage forms containing 4-amino-l-hydroxybutane-l,l-diphosphonic acid monosodium salt trihydrate (MK0217) (“Alendronate-Na-3H2O”) as a new inhibitor of bone resorption, with an assay technique.

9. The Reason for Finding Alendronate-Na-3H2O in A-7in JPO decision Reasonable assumption of presence of Alendronate-Na-3H2O • The article is based on the reasonable premise Alendronate-Na-3H2Ois known as a new inhibitor of bone resorption. • The article does not merely state a hope or hypothesis but reports the actual experiment. • The analysis is reproducible and applicable to Alendronate-Na-3H2O.

10. The Reason for Finding Alendronate-Na-3H2O in A-7in JPO decision Reasonable assumption of presence of Alendronate-Na-3H2O • Specific conditions for derivatization of Alendronate-Na-3H2O in A-7, specific conditions of high performance liquid chromatography (HPLC)are described. • It is hard to assume that the speaker would present only the assay method for a drug ingredient none of the participants knew.

11. The Reason for Finding Alendronate-Na-3H2O in A-7in JPO decision As to the Knowledge of Process for Producing Alendronate-Na-3H2O • Trial decision gave a conclusion that Any process of producing Alendronate-Na-3H2Ois not described in the A-7 document, those skilled in the art would be able to understand, when they reviewed the A-7 document, prior to the priority date that they could easily produce it.

12. The Reason for Finding Alendronate-Na-3H2O in A-7in JPO decision Knowledge of Process for Producing Alendronate-Na-3H2O • Step 1: In Example 5, 5-amino-l-hydroxybutane-l,l-diphosphonic acid –Na could be obtained by addition of NaOH solution. • Step 2: In Example 5, the bisphosphonic acid sodium salt is obtained as the crystalline solid by neutralizing followed by crystallization from the aqueous solution

13. The Reason for Finding Alendronate-Na-3H2O in A-7in JPO decision Knowledge of Process for Producing Alendronate-Na-3H2O • it is conventional to crystallize from an aqueous solution. It was well known that crystal water is sequentially split off upon heating • it is natural for those skilled in the art to assume that the trihydrate would be obtained by crystallizing Alendronate-Na from the aqueous solution, since it is described in the A-7 Alendronate-Na-3H2O exists.

14. The Reason for Finding Alendronate-Na-3H2O in A-7in JPO decision Knowledge of Process for Producing Alendronate-Na-3H2O • If the hydration number of Alendronate-Na obtained by crystallization from the aqueous solution exceeds 3, the trihydrate would readily be obtained by appropriate heating or the like thereby to reduce the hydration number. • In fact, the trihydrate is obtained by drying under such drying conditions as used in A-6 or A-10, which are ordinary conditions as drying conditions.

15. Judgment • Article 29, Paragraph 1 of the Patent Act stipulates "an inventor … may not be entitled to obtain a patent for the invention described in a distributed publication …prior to the filing of the patent application"

16. Judgment • In order to state that "a product invention" is described in "a publication," it goes without saying that the elements of the product invention are required to be disclosed in the publication. • It is required that a person skilled in the art upon reading the publication enables to easily embody the invention even without creative ability including deliberation, trial and error, etc. but based on common technical knowledge as of the filing date.

17. Reason for Judgment • In organic compounds, trial and error experimentation is required to a considerable extent to give the hydrate crystals of an organic compound having a desired number of hydration, for the following reason. • Crystal structure of an organic compound is extremely complicated as compared to the crystal structure of an inorganic compound; for this reason, the binding modes have so many different types in the hydrate crystal of an organic compound(Expert Opinions)

18. Reason for Judgment • The Technical Matter found in JPO decision based on A-5 is not common technical knowledge while it can be said known technology. • A-6 and A-10 are those prepared and filed after the priority date; therefore they are not common technical knowledge.

19. Note • Common technical knowledge found in a separate IP High Court case is process for separating optical isomer from its racemic body. • In the case above, an optical isomer was found to be disclosed in a Cited Document where its racemic body is written.

20. Lesson Liability of Mistake by Examiner or Judges • Reading part of the invention at issue on Cited Document • A Novel Compound written by Famous author or Author of Famous Company is trusted to be present. • It is enough for a person skilled in the art to be able to produce the novel compound in Cited Document easily. What should be found is not “easily” but “readily”.

21. Lesson Cause for Liable Mistakes • Read below for [Human being is happy upon any achievement. Even Success in Constructing the Invention by gathering parts found in Cited Documents can make human happy.] • In the Patent System, it is necessary to explain the reasons for the examiner only when rejecting the application. Success in explanation gives professional satisfaction. Thus, the system is liable to ferment further a motivation to construct the invention by gathering parts found in different Cited Documents.

22. Lesson • (i) Then what we can do. • (ii) Knowing the nature of the examiners or the judges, the applicant or the patentee and the attorneys therefor should be much more carefully prepare the argument on patentability or validity than present so that you would be able to save costs.

23. Any Questions ? Sumiko Kobayashi Abe, Ikubo & Katayama sumiko@aiklaw.co.jp 23