In our past newsletter (Newsletter ’21 No. 2), we posted an article about the Supreme Court decision that states the criteria for an unexpected advantageous effect.

 

 

In this article, we will introduce how to allege an unexpected advantageous effect in determination of inventive step, with reference to one of the recent court decisions.

The court decision introduced below was also dealt with by the Trial and Appeal Practitioner Study Group (2021) hosted by the JPO Appellate Board. As a side note, the Trial and Appeal Practitioner Study Group is a study group that deliberates on trial decisions and judgements, comprising corporate in-house personnel undertaking IP-related issues, patent and trademark attorneys, lawyers, and chief trial examiner and administrative judges of the JPO.

 

 

 

In the court decision as follows, it was examined whether there was an unexpected advantageous effect, as one of the issues.

The plaintiff is a patentee of a patent whose invention is entitled “USE OF MOMETASONE FUROATE FOR TREATING AIRWAY PASSAGE AND LUNG DISEASES”, which will be talked about in this article (Japanese Patent No. 3480736). The defendant filed a request for a trial for patent invalidation (Invalidation No. 2015-800166) against the subject patent. A trial decision of invalidation was rendered, and the plaintiff filed a litigation cancelling this trial decision. The following descriptions are extractions from the text of the court decision. The author of this article has made some modifications to the text as appropriate to enhance the readers’ understanding.

 

 

 

[Claim 1] A medicament for treating allergic or seasonal allergic rhinitis comprising an aqueous suspension of mometasone furoate to be administered intranasally once a day.

[Claim 2] The medicament of Claim 1, wherein the once-a-day dose is 100 to 200 micrograms, and the absolute bioavailability of unchanged mometasone furoate is less than about 1%.

 

 

 

The effects recognized in the trial decision are as follows:

–    Effect A: Once-a-day intranasal administration of mometasone furoate is therapeutically effective against allergic rhinitis relative to placebo.

–    Effect B: Compared to oral solution, oral suspension and nasal spray suspension have lower systemic absorption of mometasone furoate, and there is an effect that mometasone furoate itself exists in plasma below the limit of quantification.

–    Effect C: There are no systemic side effects due to suppression of hypothalamic-pituitary-adrenal (HPA) function compared to placebo.

 

 

 

Exhibit Ko #1 describes an aqueous suspension for intranasal administration containing mometasone furoate monohydrate for treating inflammatory conditions.

Exhibit Ko #2 describes that (1) based on an assumption that mometasone furoate has a topical anti-inflammatory activity to skin, therapeutic effect of intranasal inhalation against allergic rhinitis can be expected, and mometasone furoate is used for treating allergic rhinitis by means of intranasal inhalation, and (2) mometasone furoate is a synthetic corticosteroid that has a topical anti-inflammatory activity, and, on the other hand, exhibits a potential capability to suppress hypothalamic-pituitary-adrenal (HPA) function only at the minimum.

Furthermore, it was recognized by a person skilled in the art, as a common technical knowledge, that (1) while mometasone furoate exhibits very strong topical anti-inflammation effect, it is weak in terms of side effects (systemic action, skin atrophy) and has a large deviation between principal action and side effects, (2) mometasone furoate has a safe and quick therapeutic effect against skin disease even for children with once-a-day administration, (3) topical active steroid having a value verified in treatment for skin disease is also effective for treating airway disease, including rhinitis.

It was known that, as of the priority date of the subject patent, when topical steroid therapy was used for allergic disease of mucosa of the respiratory organs including nose, some arrangements were provided to steroid formulations in order to deliver steroid to the respiratory tract mucosa over a long period of time, by making the steroid into a suspension and making the suspension viscous to prevent the effects on the whole body. Exhibit Ko #1 also discloses an aqueous suspension provided with the similar arrangements.

 

 

 

The court has made a decision on each of the effects.

–    With Respect to Effects A and C

It is recognized that a person skilled in the art as of the priority date of the subject patent could have predicted, from common technical knowledge as well as the aforementioned descriptions of Exhibit Ko #1 and Exhibit Ko #2, that with respect to aqueous suspension of mometasone furoate, which is weak in terms of side effects, for intranasal administration, even if pharmacokinetics differed between topical application to skin and intranasal topical administration, once-a-day intranasal administration had therapeutic effect against allergic rhinitis, systemic absorption was low, and bioavailability was good. (snip) A person skilled in the art as of the priority date of the subject patent would have predicted an effect that, with respect to the structure of the subject invention, “once-a-day intranasal administration of mometasone furoate is therapeutically effective against allergic rhinitis relative to placebo, and bioavailability of mometasone furoate is low, there is substantial absence of absorption systemically into the bloodstream of mometasone furoate, and there are no systemic side effects. With respect to the figure “bioavailability is less than about 1%”, there is no evidence that sufficiently proves the figure this much is prominent beyond what was predictable based on common technical knowledge as of the priority date of the subject patent.

 

Although the plaintiff alleges that the subject invention is an invention focused on an unknown nature concerning the structure of mometasone furoate (the furoate part), which has been identified later, and possesses an inventive step, there is no description related to this aspect in the specification of the subject patent, …the fact that the nature of the furoate part has been identified later does not affect the determination of inventive step of the subject invention.

 

–    With Respect to Effect B

In view of the descriptions in the specification of the subject patent “it is sought to find corticosteroid that is therapeutically effective and shows low bioavailability and low systemic side effects when intranasally administered.” and “the present invention provides the use of mometasone furoate aqueous suspension for formulating a medicament to effectively treat nasal cavities against allergic rhinitis with once-a-day administration. Here, there is substantial absence of absorption systemically into the bloodstream of mometasone furoate.”, numerical values for the oral solution and oral suspension and the comparisons to them indicated in the specification of the subject patent cannot be deemed to be described as effects that the structure of the subject invention possesses. Therefore, comparisons to the oral solution and oral suspension should not be recognized as an effect as described in Effect B.

 

 

 

In the specification of the subject patent, comparisons only to placebo were described, and there was no description of to what degree effects of the subject Invention is superior compared to other medicaments of the same kind that were publicly known at the reference date for determining inventive step. Taking these into consideration, an unexpected advantageous effect was not acknowledged in the subject invention.

In alleging an advantageous effect, it is likely that a comparison of the effect to placebo or to other effects for different purposes keeps the effect away from being acknowledged as an advantageous effect. Thus, it is important to demonstrate that the subject invention is more advantageous than effects expected in relation to the use of the invention. Besides, it should be kept in mind that the specification should describe such effects as much as possible. In preparation for the subsequent examinations, it is considered also important to collect, in advance, the academic documents, etc. that support the advantageous effect of the subject invention.

 

The plaintiff made an allegation based on the matter (nature of furoate), which has been identified after the priority date, but there was no description regarding this aspect in the specification of the subject patent, and the allegation was not taken into consideration in determining inventive step of the subject invention.

It is highly probable that alleging afterwards an effect based on post-filing information is not accepted in determining inventive step. Thus, it should be noted that you should describe information and effects that may contribute to inventive step as much as possible in the specification at the time of filing.

 

In order to effectively demonstrate an advantageous effect, what you should do first is to enhance the content of your specification. And when actually alleging the effect, you should make the most appropriate allegation based on the description of the specification. Please consult with our firm, and we will thoroughly go over the content of your specification, and the academic documents, etc. that are considered beneficial to your allegation, carefully study the technical significance of the matters specifying the invention, and provide you with suggestions on how to allege an unexpected advantageous effect in the most efficient way.

 

 

Edited by Yusuke Tsuji