Key points
- This decision deals with novelty, namely a "counting to two" case, and inventive step of polymorphs.
- Claim 1 of the main request is directed to the citrate salt of the compound SCY-078. Novelty over D6 is at issue.
- The Board: "As set out above, claim 49 of D6 relates both to SCY-078 in its free-base form and to a pharmaceutically acceptable salt thereof. Furthermore, the passage quoted above [column 21, line 54 to column 22, line 21] discloses citrate as a pharmaceutically acceptable salt. The board acknowledges that this disclosure is not made specifically in the context of SCY-078, but rather in relation to all the compounds of the invention of D6. However, since SCY-078 is one of those compounds, the skilled person would already derive directly and unambiguously from this disclosure that citrate also applies to SCY-078. "
- The passage is a list of pharmaceutically acceptable salts and includes citrate.
- Hence, citrate is one selection; a question is whether claim 49 / SCY-078 is a second selection, or at least the embodiment "pharmaceutically acceptable salt" of claim 49.
- "even if one were to accept the respondent's [proprietor's] rather formal approach that, in addition to selecting citrate from the passage quoted above, a pharmaceutically acceptable salt of SCY-078 must be selected from claim 49 instead of the free base of SCY-078, D6 provides a clear technical link between these selections. Accordingly, D6 directly and unambiguously discloses SCY-078 citrate as defined in claim 1 of the main request."
- Claim 1 of the AR recites 10 crystalline forms of the citrate salts, each defined by an XRD pattern. Inventive step is at issue.
- "At the oral proceedings, the appellant [opponent] considered, inter alia, D6 as possible closest prior art. [The opponent] stated that it regarded the pharmaceutically acceptable salt of SCY-078 disclosed in claim 49 as the starting point for assessing inventive step. However, it did not start from the citrate of SCY-078 as disclosed in D6 (see assessment of main request above). To the benefit of the appellant [opponent] [*], it is assumed in the following that this is correct."
- * see below, the selection of "citrate" is considered as the distinguishing feature that provides for inventive step. How this is to be reconciled with the Board's conclusion of lack of novelty of that feature in connection with the Main Request, and with Article 114(1) EPC in that respect, is not entirely clear to me.
- "table 18 of the application as filed shows that the Type A citrate crystal form exhibits superior kinetic solubility in fasted state simulated intestinal fluid (FaSSIF) and in fed state simulated intestinal fluid (FeSSIF) compared with other salts of SCY-078 (hippurate, fumarate, mesylate, phosphate). "
- "none of the documents in the proceedings teaches the use of citrate in order to increase bioavailability of a drug relative to other salt-forming options."
- The claims are held to be inventive.