Israel Patent Application No. 176831 to Novartis is titled “COMPRESSED PHARMACEUTICAL TABLETS OR DIRECT COMPRESSION PHARMACEUTICAL TABLETS COMPRISING DPP-IV INHIBITOR CONTAINING PARTICLES AND PROCESSES FOR THEIR PREPARATION ” the patent application is a national phase of PCT/EP/2005/000400. It relates to a pharmaceutical used in the treatment for diabetes known as Vildagliptin (previously LAF237, trade names Galvus, Zomelis,) which is an oral anti-hyperglycemic agent (anti-diabetic drug) of the dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. Vildagliptin inhibits the inactivation of GLP-1 and GIP by DPP-4, allowing GLP-1 and GIP to potentiate the secretion of insulin in the beta cells and suppress glucagon release by the alpha cells of the islets of Langerhans in the pancreas.
Unipharm has opposed the patent issuing and, in an intermediate proceeding, Unipharm (not represented) submitted a disclosure request for:
- The specific testing referred to Appendix E of a the Applicant’s expert witness.
- All other tests relating to all the formulations that were performed where the particle size distribution was examined.
Alternatively, Unipharm requests that the part of the evidence that relates to the evidence submitted in the European Opposition proceeding from Dr Davis’ statement, including Appendix E, be struck.
The patent relates to tablets that are made by direct compaction and which include DPP-IV, (s)-1-[(3-hydroxy-1-adamantyl)amino]acetyl-2-cyanopyrrolidin (Vildagliptin) in free radical form or as a salt, wherein at least 80% of the particles compressed into the tablet are in size range of 10 microns to 250 microns.
In their Statement of Case, Novartis explains that use of direct compression was not obvious to persons of the art wishing to produce vildagliptin formulations, and the distribution and size of the particles affects the character of the tablet in a manner that determines the efficacy of the formulation. The chosen distribution enables tablets to be produced by direct compaction which have high quality, acceptable stability and good physical properties.
With respect to this, Novartis’ expert witness, Dr Davis, explains in his expert opinion as follows:
“There is no prior art suggesting that tablets of vildagliptin can be made using direct compression with this size range or any size range. This particle size range and percentage of the active agent is not disclosed in the prior art. It should be noted that the particle size distribution is important to achieving good physical properties in the tablet (e.g. good hardness). Evidence filed in a technical annex for the corresponding European Patent Application No.15199440.7 (available on-line from the EPO at https://register.epo.org/application?documentId=EZQR8ZQ06757DSU&number=EP15199440&lng=en&npl=false), comparing 88% PSD of 10-250 micron (within the claim) versus 79% PSD of 10-250 micron (outside the claim) shows that the use of a particle size distribution as claimed is important in providing directly compressed tablets with good hardness (Appendix E).”
The Expert witness related to the technical appendixes that were submitted by the Applicant to the European Patent Office which compares tablets that fall within the ambit of claim 1 to those that do not, and this is the basis of the discovery request that Unipharm submitted.
Claims of the Parties
Unipharm’s opposition to this evidence is that Professor Davis relied on test results from tests that he himself did not conduct, and they express wonderment that Novartis did not produce the drug developers to be cross-examined. In response, the Applicants claim that the disclosure process should be allowed in cases where it is proven that the documents in question are relative to the proceeding in general and to the point of contention between the parties, and in this instance the Opposer did not justify his request for disclosure of documents and did not explain how the disclosure would help clarify the question under debate.
Novartis further allege that the request for disclosure is wide and general, in that it relates to all testing and formulations made, where particle size was examined. The Applicant further asserts that Dr Davis referred to Appendix E merely to show that it was published and not as evidence that the data therein is true (!?).
As to Unipharm’s alternative request, Novartis claims that the Opposer did not base this allegation, and that we are referring to an expert opinion based on data provided to him and his relying on the publication is equivalent to any expert relying on a professional publication such as a paper in a scientific journal or a patent application in a relevant field.
In response, Unipharm claims that the Applicant’s expert, Professor Davis, did not merely testify that the document was included in the file wrapper of the European Patent Application, but also reached conclusions in his expert opinion that were based thereon. As far as anything connected to the scope of the disclosure, Unipharm focuses their request and asks to receive the documents relating to the experimentation with the particle distributions and efficacy of formulations made with the specific distributions.
Unipharm claims that the documents will reveal that the tests conducted, if indeed conducted, do not provide sufficient instruction to persons of the art to produce the invention successfully without additional experimentation and thus the patent application should be rejected as not enabled under Section 12 of the Israel Patent Law 1967.
Discussion and Ruling
There is no doubt that the Commissioner of Patents can request disclosure and access to documents in opposition proceedings. The disclosure is efficient in that it provides documents to the Patent Office that are not covered by Section 18 of the Law (Duty of Disclosure) and which can help clarify if an application is patent worthy. However, disclosure is performed in a manner to prevent the Applicant going on an illegal fishing expedition in the Applicant’s filing cabinets.
The considerations to be weighed up prior to giving a disclosure order are detailed in Opposition to 60312 Biotechnology General Corp vs. Genentech Inc and in Opposition to 143977 AstraZeneca AB vs. Unipharm ltd, and these are the stage of the opposition reached; the amount of documents and their content; the weight of the claim that the Applicants are attempting to prove with the documents asked disclosure of, their evidential weight, the possibility of the Applicant to obtain the documents themselves, and the burden it will cause the opposing party.
In these rulings it was also determined that disclosure could damage the property rights of the opposing party by forcing revelation of trade-secrets. However, the possibility of such damage being caused does not remove the authority of the Patent Office to demand such a disclosure, but obliges consideration of the legitimate property rights of the party when applying that authority.
In the opinion of Commissioner Alon Ofir, Novartis is correct that the experimental results will have no effect on the average person of the art’s ability to implement the invention. The answer to this question is found in what is revealed and not in what is not revealed in the patent application.
Nevertheless, Unipharm is correct with regard to everything related to the tests described in Appendix E, since the Applicant himself relied upon this in his statement. In this regard the Commissioner does not accept that this evidence can be considered as external evidence that their Expert Witness relied on. The document was prepared by Novartis themselves, with data they control, and their expert witness relied on it in his Opinion.
The particle size distribution is claimed by Novartis themselves as being a central element of their invention, and the claims of the Application itself limits the requested patent to one wherein 80% of the particles are in the 10 micron to 250 micron range. The Applicants themselves state in their Statement of Case, that the choice of particle size and distribution is what enables the fabrication of tablets of an acceptable quality by direct compression. Their Expert Witness finds support for this claim in Appendix E which compares tablets having this particle distribution with tablets that do not.
In these circumstances, one should consider the documents as relating to the central question being debated by the parties. Thus the documents relating to Appendix E are ruled relevant and Novartis are required to provide not just those relied upon but other documents summarizing experiments done with the intention of producing Appendix E, even if not included therein.
Novartis is given 30 days to produce an Affidavit of Disclosure with the relevant documents describing test results obtained in the experimentation leading to Appendix E, whether or not included in the Appendix, but relating to the hardness of tablets made from different particle distribution.
As an after-note, the Opposer is chastised for using language that does not show respect for the proceedings which was inappropriate.
No costs are awarded.
Ruling on Interim Proceeding regarding disclosure, by Commissioner Ofir Alon, 3 January 2018.
In court proceedings in the United States there is wide discovery and the parties effectively go on fishing expeditions with trawlers and haul up everything and then have to wade through the bycatch. This is not the case in Israel. One can ask for specific documents, but have to justify the request. Thus I have used the term disclosure and not discovery.
In this instance, Unipharm is not-represented, or to be more accurate Dr Zebulun Tomer is representing himself. No doubt if he runs into trouble he will call on his attorney Adi Levit to represent them. It is unlikely that the inappropriate language lost Unipharm a costs award as, since they have not used legal counsel, they are not entitled to costs anyway.
We strongly discourage industrialists to represent themselves in Opposition proceedings. The Tomers, however, have so much experience of killing pharma patent applications that there are very few lawyers that have handled so many cases.