Key points
- Claim 1 of the patent is directed to "crystalline micronizate of tiotropium bromide" which is characterized by a certain particle size and a certain water content. The water content is higher than in the closest prior art D9.
- The proprietor submits that (post-filed) experimental reports D23 and D65 demonstrate that the distinguishing feature leads to improved storage stability. The Board concludes that the reports sufficiently demonstrate the advantage.
- The opponent submits that the experimental reports can not be considered because the application as filed contained no reference to improved storage stability.
- The present Board interprets G 2/21, in translation: "it is not a prerequisite that this claimed effect must be expressly mentioned or proven in the application as originally filed."
- The application as filed referred to an "objective of the present invention to provide a process which makes micronized tiotropium bromide available in a form that meets the high requirements placed on an inhaled active ingredient and thereby takes into account the specific properties of tiotropium bromide"
- The Board, in translation:"The application as originally filed therefore focuses on the use of the claimed micronisates as inhalation powders and teaches that a certain particle size range is required for administration by inhalation. Since a certain amount of time necessarily elapses between the production of a drug and its administration, it can be deduced from the application as originally filed that particle size stability (corresponding to the storage stability demonstrated in D23 and D65) is an essential prerequisite for the administration of the drug according to the application."
- "Furthermore, as stated by the respondent [proprietor] at the hearing, it was well known to the person skilled in the art before the priority date of the application that particle size stability is crucial for the administration of a drug by inhalation. As evidence of general specialist knowledge, the respondent referred to documents D1, D16a, D16b and D17."
- The Board reviews these documents.
- The Board: "Based on his above-mentioned specialist knowledge [Fachwissen] regarding the necessary particle sizes/particle size distribution when using inhalation powders for medical administration, the person skilled in the art would recognize, based on the originally filed version of the application, that the tiotropium bromide also has adequate stability due to the disclosed particle sizes and its intended use particle sizes. This stability corresponds to the technical effect of storage stability used by the respondent for the inventive step. The person skilled in the art would therefore draw direct conclusions about the storage stability of this product from the use of the claimed micronisate as an inhalation product described in the originally filed application. Nothing in the originally filed application or general technical knowledge casts reasonable doubt on the achievement of this storage stability by the subject matter of the claim, and no such doubt was expressed by the complainant. Therefore, it can be deduced from the originally filed application that this technical effect is covered by the technical teaching of the application and is embodied by the invention originally disclosed to it."
- "the board recognizes that the technical effect that can be derived from the originally filed application within the meaning of point 2 of the decision formula of G 2/21 is storage stability as such, while the effect shown by D23 and D65 is the improvement of this storage stability compared to the closest prior art cited. In the Board's view, as soon as the above-mentioned criterion of the derivability of a technical effect is met, this also applies to the improvement of this effect. "
- "Therefore, the fact that the technical effect cited by the respondent consists of a storage stability that is improved compared to the closest state of the art does not preclude its consideration in the light of decision G 2/21."
- The Board concludes that the claimed composition is inventive.
3.3 Consideration of the technical effect shown in D23 and D65 in the light of G 2/21
3.3.1 In addition to the points discussed above, it was argued by the appellant that the experimental data in D23 and D65 were subsequently published and that the originally filed application contained no reference to the technical effect of improved storage stability shown in D23 and D65. Therefore, this effect cannot be taken into account in the context of the inventive step.
3.3.2 The question of possible consideration of a technical effect was discussed in the decision of the Enlarged Board of Appeal G 2/21 of March 23, 2023 (OJ EPO 2023, A85).
3.3.3 Point 1 of the decision formula reads as follows:
"Evidence which is submitted by a patent applicant or proprietor to prove a technical effect and which he relies on in order to recognize the inventive step of the claimed subject matter may not be disregarded solely for the reason that this evidence on which the effect is based is based , were not publicly available before the filing date of the patent in dispute and were only filed after that date."
Therefore, according to point 1 of the decision formula, the fact that D23 and D65 are post-published does not in itself exclude the possibility of taking into account this evidence showing the technical effect of improved storage stability (see point 3.2 above).
3.3.4 Point 2 of the decision formula of decision G 2/21 reads as follows:
"A patent applicant or patent holder may rely on a technical effect to prove inventive step if the person skilled in the art, based on general knowledge and on the basis of the application as originally filed, would conclude that this effect is covered by the technical teaching and of the same invention as originally disclosed."
3.3.5 Since decision G 2/21 was issued, the above-mentioned considerations must therefore be taken into account as decisive for the question of whether a technical effect can be recognized in the context of the examination of inventive step. According to the wording of point 2 of the decision formula, the examination of whether such an effect can be derived from the application in the originally filed version or can be inferred from it must be based on two criteria, namely "covered by the technical teaching" and "originally from the same disclosed invention "embodies". The fact that the technical teaching of the application as originally filed is important is evident from the reasons for the decision, for example points 71 and 93.
3.3.6 In point 71, the Enlarged Board of Appeal stated that it took the previous jurisprudence of the Boards of Appeal as a common basis that the core issue was what the skilled person - based on the general knowledge on the filing date of the application in the originally filed version - should do - understand as technical teaching of the claimed invention.
3.3.7 As explained above, the respondent in the present case relies on the technical effect of improved storage stability demonstrated using D23 and D65. The assessment of whether this technical effect can be taken into account when examining inventive step must therefore be made from the perspective of the person skilled in the art, who, using his general specialist knowledge, starts from the application as originally filed.
From this specific perspective of the person skilled in the art, it must be assessed whether the technical effect mentioned can be derived as "covered by the technical teaching and embodied by the same originally disclosed invention".
3.3.8 In the Board's view, derivability as being "covered by the technical teaching" and "embodied by the same originally disclosed invention" are two criteria that must be fulfilled cumulatively.
3.3.9 In this context, the Chamber is of the opinion that point 93 of the reasons for the decision in G 2/21 is of particular importance. This is as follows:
"The relevant standard for relying on a claimed technical effect in assessing whether the claimed subject matter involves an inventive step is what the person skilled in the art would understand to be the technical teaching of the claimed invention, based on common general knowledge on the filing date of the originally filed application . The technical effect claimed - even at a later point in time - must be covered by this technical teaching and embody the same invention, because such an effect does not change the nature of the invention claimed.
3.3.10 It follows from these statements by the Enlarged Board of Appeal that a technical effect can only be asserted at a later point in time, ie after the filing date, in the proceedings. In order for a technical effect to be recognized in the context of the assessment of inventive step, it is not a prerequisite that this claimed effect must be expressly mentioned or proven in the application as originally filed. Rather, a technical effect proven by subsequently published evidence within the meaning of point 2 of the decision formula of G 2/21 can be recognized if it is included in the technical teaching of the originally filed application and can be derived from the same originally disclosed invention. This in turn means that with regard to this technical effect, the nature of the claimed invention is not changed compared to this originally disclosed invention.
3.3.11 In this context, as stated by the respondent in the oral hearing, the following passages of the application in the originally filed version are of particular importance:
On page 1, line 22 to page 2, line 2 it is disclosed that tiotropium bromide is a highly effective anticholinergic and may have therapeutic benefit in the treatment of asthma or chronic obstructive pulmonary disease. It should be noted that the application of tiotropium bromide is preferably carried out by inhalation and that with regard to the inhalation application of tiotropium bromide it is necessary to provide the active ingredient in micronized form. The active ingredient preferably has an average particle size of 0.5 mym to 10 mym, preferably from 1 mym to 6 mym, particularly preferably from 1.5 mym to 5 mym.
According to page 2, lines 14 to 18 it is
"...objective of the present invention to provide a process which makes micronized tiotropium bromide available in a form that meets the high requirements placed on an inhaled active ingredient and thereby takes into account the specific properties of tiotropium bromide."
According to page 6, lines 28 to 30, another aspect of the present invention is one
"Inhalation powder characterized by a content of tiotropium bromide micronisate according to the invention."
Finally, page 7, lines 5 to 8 reveals:
"Accordingly, the present invention aims at inhalation powder containing at least about 0.03%, preferably less than 5%, particularly preferably less than 3%
of the tiotropium bromide micronisate obtainable by the process described above..."
3.3.12 The application as originally filed therefore focuses on the use of the claimed micronisates as inhalation powders and teaches that a certain particle size range is required for administration by inhalation. Since a certain amount of time necessarily elapses between the production of a drug and its administration, it can be deduced from the application as originally filed that particle size stability (corresponding to the storage stability demonstrated in D23 and D65) is an essential prerequisite for the administration of the drug according to the application.
3.3.13 Furthermore, as stated by the respondent at the hearing, it was well known to the person skilled in the art before the priority date of the application that particle size stability is crucial for the administration of a drug by inhalation. As evidence of general specialist knowledge, the respondent referred to documents D1, D16a, D16b and D17.
D1 is a review article published in 1998 and concerns dry powder formulations for pulmonary delivery. The maximum particle size is stated to be 5 mym for deposition in the central airways and 2 to 3 mym for deposition in the periphery/depth of the lung. Larger particles are retained by the protective devices of the lungs, while particles smaller than 0.5 mym are exhaled (D1, page 395, left column, lines 1 to 5).
D1 therefore shows that it was well known to those skilled in the art that particle size is a crucial factor for the inhalation administration of a drug.
D16a is an excerpt from a book published in 2001 entitled "Particulate interactions in dry powder formulations for inhalation". Section 3.6.1 (page 86, first sentence) states that the deposition properties and effectiveness of an aerosol largely depend on particle size. The same book (D16b; page 136, section 5.1) states that it is generally accepted that drug particles must have an aerodynamic diameter between 1 and 5 mym for the drug to reach the lower respiratory tract.
D17 is a US Food and Drug Administration (FDA) document entitled "Guidance for Industry" and concerns metered dose inhaler (MDI) and dry powder inhaler (DPI) drugs Products"). This document teaches that particle size distribution (among other things) is critical and that maintaining it during the shelf life period is probably the biggest challenge (lines 103 to 105). It is also noted that the particle size distribution of a drug in the formulation should be determined and monitored at the initial dose and the final dose (lines 792 to 974).
3.3.14 Based on his above-mentioned specialist knowledge regarding the necessary particle sizes/particle size distribution when using inhalation powders for medical administration, the person skilled in the art would recognize, based on the originally filed version of the application, that the tiotropium bromide also has adequate stability due to the disclosed particle sizes and its intended use particle sizes. This stability corresponds to the technical effect of storage stability used by the respondent for the inventive step. The person skilled in the art would therefore draw direct conclusions about the storage stability of this product from the use of the claimed micronisate as an inhalation product described in the originally filed application. There is nothing in the originally filed application or general technical knowledge that casts reasonable doubt on the achievement of this storage stability by the subject matter of the claim, and no such doubt was expressed by the complainant. It can therefore be deduced from the originally filed application that this technical effect is covered by the technical teaching of the application and is embodied by the invention originally disclosed to it.
3.3.15 Here, the board recognizes that the technical effect that can be derived from the originally filed application within the meaning of point 2 of the decision formula of G 2/21 is storage stability as such, while the effect shown by D23 and D65 is the improvement of this storage stability compared to the closest prior art cited.
3.3.16 In the Chamber's view, as soon as the above-mentioned criterion of the derivability of a technical effect is met, this also applies to the improvement of this effect. Specifically, even if the skilled person has no inventive skills, he will strive for further developments or technical improvements in any area of technology. If a specific technical effect, such as storage stability in the present case, can be derived from the originally filed application for the skilled person in the sense of the decision formula, point 2 of decision G 2/21, its improvement must also be viewed as implicitly derivable.
3.3.17 Therefore, the fact that the technical effect cited by the respondent consists of a storage stability that is improved compared to the closest state of the art does not preclude its consideration in the light of decision G 2/21.
3.3.18 Consequently, the technical effect of improved storage stability shown in subsequent documents D23 and D65 does not change the nature of the invention claimed.
3.3.19 The improved storage stability shown in D23 and D65 can therefore be taken into account in the light of decision G 2/21.
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