CABINET CHAILLOT

T0852/20 - Post-published experimental data

Post-published experimental data, G2/21, Inventive step, skilled person

The appeal by the opponent ("appellant") lies from the opposition division's decision to reject the opposition filed against European patent No. 2 955 180.
Claim 1 of the patent relates to a crystalline polymorph Form 1 of compound I. Compound I will be referred to hereinafter as vemurafenib.
In the impugned decision, with regard to the assessment of inventive step, the opposition division referred to "post-published experimental data" filed by the respondent during the examination phase. The opposition division relied on these data for formulating the objective technical problem, namely that of providing an improved form of vemurafenib with the aim of overcoming known solubility issues. According to the opposition division, the post-published experimental data were "meaningful, since they represent experimental evidence in support of an alleged improved solubility already mentioned in the application."
The appellant did not dispute that the experimental data demonstrated increased water solubility and bioavailability achieved by Form 1 of vemurafenib compared with Form 2; however, it contested that the post-published experimental data could be used as the sole basis to demonstrate this effect, since this effect was not derivable from the application as filed.
According to G 2/21, "a patent applicant or proprietor may rely upon a technical effect for inventive step if the skilled person, having the common general knowledge in mind, and based on the application as originally filed, would derive said effect as being encompassed by the technical teaching and embodied by the same originally disclosed invention."
The question to be answered in the present case is thus whether the effect relied upon by the respondent and demonstrated in the post-published experimental data, namely the increased water solubility and bioavailability, can be derived by the skilled person, having the common general knowledge in mind and based on the application as filed, as being encompassed by the technical teaching and embodied by the same originally disclosed invention.
In the board's view, this question has to be answered in the negative.
The purported technical effect of increased water solubility and bioavailability of Form 1 (a crystalline form) of vemurafenib in comparison with Form 2 (another crystalline form) is not disclosed in the application as filed. The application refers to certain compounds in crystalline form not having an increased dissolution rate, but a low dissolution rate, and as a result having poor bioavailability. The application teaches that it is desired to formulate vemurafenib so that it may stably exist primarily in amorphous form. Lastly, the application teaches how to provide vemurafenib in a composition, form, or formulation in which it has improved water solubility and/or bioavailability as compared with vemurafenib in a crystalline form or in a primarily crystalline form. The vemurafenib mentioned as having improved water solubility and/or bioavailability as compared with vemurafenib in a crystalline form can only be amorphous vemurafenib. These passages of the application as filed thus teach the purported technical effect for amorphous vemurafenib in comparison with crystalline forms. Therefore, if anything, the skilled person would derive from the application as filed that amorphous forms are more soluble and bioavailable than crystalline forms. By no means could the skilled person derive from the application as filed that one particular crystalline form, namely the claimed Form 1, has good solubility and bioavailability, let alone solubility and bioavailability that is better than that of another crystalline form (Form 2). It follows that, based on the application as filed, and having the common general knowledge in mind, the skilled person would not have derived the purported technical effect, i.e. the increased water solubility and bioavailability of Form 1 of vemurafenib over Form 2, as being encompassed by the technical teaching of the application as filed, let alone that the skilled person would have derived it as being embodied by the same originally disclosed invention. Therefore, it cannot be taken into account for formulating the objective technical problem, in accordance with G 2/21.
In the absence of a technical affect achieved by the distinguishing feature of claim 1 of the main request, the objective technical problem is to provide an alternative crystalline form of vemurafenib.
The subject-matter of claim 1 of the main request lacks an inventive step in view of D1 in combination with the common general knowledge.
The patent is revoked.

 

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