Drafting Claims and Patent Specifications for Chemical Inventions: A European Perspective Andrew G. Smith

2 Europe play a different game

Scenario Claims 1. A compound of formula I 2. A compound according to claim 1, or salt thereof, wherein R 1 is CN, NO 2 or halo. 3. A compound according to claim 1, or salt thereof, wherein R 2 is C 1-6 alkyl, CH 2 SH or CH 2 OH. 4. A compound according to claim 1, or salt thereof wherein X is NR 3, R 1 is CN and R 2 is CH 2 CH 3. wherein R 1 is H, CN, NO 2, or halo; R 2 is H, C 1-6 alkyl, CH 2 OH, CH 2 SH or CH 2 NH 2 ; X is CHR 3, S, O or NR 3 ; R 3 is H, C 1 -C 6 alkyl, phenyl or pyridyl; or a salt thereof. wherein R 1 is -H, -CN, CH 3, OH R 2 is -H, -C 1-6 alkyl, -CH 2 OH, -CH 2 SH or -CH 2 NH 2 ; X is CH 2, S, O, N-phenyl, N-pyridyl or N-propyl; or a salt thereof. Prior art Claims 1. A compound of formula I Prior art Examples 3nM 4µM 13mM

4 Article 123 (2) EPC The European patent application or European patent may not be amended in such a way that it contains subject-matter which extends beyond the content of the application as filed. The description, claims and drawings (G 11/91): X The Abstract (Art.85 EPC): X Priority document (T260/85):

5 Assessing Allowability of an Amendment Disclosure test: (T194/84). An amendment is unallowable if the overall change in the content of the application results in the skilled person being presented with information which is not directly and unambiguously derivable from that previously presented in the application as filed, even when account is taken of matter which is implicit to a person skilled in the art. The term "directly" means that the invention including all of its elements must be immediately recognizable (see T 514/88). The term "unambiguously" means that there should not exist the slightest doubt in the mind of the skilled reader that the invention including all of its elements is actually disclosed in the application as filed (see T 383/88).

6 Allowable Amendments Explicit disclosures in the description/claims/drawings. Selection of one preferred feature disclosed in the description. (T234/00). Deleting an originally disclosed meaning from an independent list is allowable provided that said deletions do not result in singling out a particular combination of specific meanings but maintained the remaining subject-matter as a generic group of compounds differing from the original group only by its smaller size. (T615/95 and T948/02)

7 Unallowable Amendments  New (undisclosed) narrower inventions: –Selection Inventions: (Guidelines, C-IV, 9.8) –Selection from two lists, or parameter sub-range. –Undisclosed individual compound.  Intermediate generalisation (Guidelines, C-IV, 9.8, T962/98)  Well-known Equivalents. (Guidelines, C-IV, 9.2, T 673/89 &T 685/90).

8 Fallback Positions – Suggestions Broad claims should be accompanied by narrow claims specifically focused toward embodiments of most interest. One fallback position in the claims for each substituent Multiple dependencies should be used when drafting the claims to increase the disclosure of sub-genera. Provide multiple levels of fall back in the description. Fallback positions should apply for each substituent and for the combination of preferred features X

Claims 1. A compound of formula I 2. A compound according to claim 1, or salt thereof, wherein R 1 is CN, NO 2 or halo. wherein R 1 is H, CN, NO 2, or halo; R 2 is H, C 1-6 alkyl, CH 2 OH, CH 2 SH or CH 2 NH 2 ; X is CHR 3, S, O or NR 3 ; R 3 is H, C 1 -C 6 alkyl, phenyl or pyridyl; or a salt thereof. Preferred claims 4. A compound according to any one of claims 1 to 3, or salt thereof, wherein X is NR A compound according to any one of claims 1 to 4, or salt thereof, wherein R 3 is H or methyl. R 1 is preferably CN, NO 2 or -halo. R 1 is more preferably CN. R 2 is preferably C 1-6 alkyl, CH 2 SH or CH 2 OH. R 2 is more preferably H or C 1-3 alkyl. R 2 is most preferably methyl or ethyl. R 3 is preferably H or methyl. R 3 is more preferably H. X is preferably NR 3. A preferred embodiment is a compound of formula I wherein R 1 is CN, NO 2 or halo and R 2 is C 1-6 alkyl, CH 2 SH or CH 2 OH. A preferred compound of the invention is a compound of formula I wherein R 1 is CN and R 2 is methyl or ethyl. Description 3. A compound according to claim 1 or 2, or salt, thereof, wherein R2 is C 1-6 alkyl, CH 2 SH or CH 2 OH.

Inventive Step - Art. 56 EPC Article 56 EPC defines one of the patentability requirements set in Art. 52(1) EPC, i.e. it provides the legal definition of the term “inventive step” under the EPC. Art. 56 EPC, first sentence, reads: An invention shall be considered as involving an inventive step if, having regard to the state of the art, it is not obvious to a person skilled in the art.

Problem Solution Approach To assess inventive step of the invention claimed, the Boards normally apply the “problem and solution approach” (Guidelines, C-IV, 11.5). This consists essentially of: Identifying the closest prior art Comparing the claimed invention with the closest prior art Assessing the technical effect achieved by the claimed invention when compared with the closest prior art. Defining the technical problem to be solved as the object of the invention to achieve this effect Examining whether or not a skilled person, having regard to the state of the art would have obviously suggested the claimed technical features as a solution to the problem posed.

Structural non-obviousness T467/94 and T643/96 established that when considering the modification of pharmaceutically active compounds it is essential to appreciate that prima facie small modifications, electronically of sterically, to an existing nucleus can have a dramatic effect on activity “when deciding upon inventive step in relation to pharmacologically active compounds it is not essential whether a particular substructure of a compound could be replaced by another known isoteric one, but whether information was available on the impact of such a replacement on the pharmacological activity of the specific group of compounds concerned.” Prior Art

Experimental Data Article 56 Applicant has to provide experimental data to demonstrate or make it at least plausible that the invention indeed works, i.e. that a problem had been solved and not merely put forward at the filing date of the application (T 0792/00, T 1329/04) If inventive step depends on improved effect: the improved effect must be implied or at least related to an effect disclosed in the original application (T 0893/02 ) advantage must at least be plausible over whole scope; often comparative data needed with regard to the closest prior art (T 0603/05) Late filed evidence will not help if evidence is the first disclosure going beyond mere speculation (T 1306/04, T 1329/04, T 0861/08)

Selection of Comparator U.S. “…proving a reason to select a compound as a lead compound depends on more than just structural similarity, but also knowledge in the art of the functional properties and limitations of the prior art compounds.” Takeda & Lilly v Zenith EPO “The crucial criteria are that the ‘closest prior art’ is normally a prior art document disclosing subject-matter conceived for the same purpose as the claimed invention and additionally having the most relevant technical features in common, i.e. requiring the minimum of structural modifications (T0730/96, T 606/89, etc.)” 3nM 4µM 13mM

Art. 83 EPC Art. 83 EPC defines a requirement of the European patent application namely it defines how an invention must be disclosed in the European patent application: “The European patent application shall disclose the invention in a manner sufficiently clear and complete for it to be carried out by a person skilled in the art” Although not explicitly stated in Art. 83 EPC, according to the Case Law of the Board of Appeal, a European patent application is deemed to be in accordance with Art. 83 EPC, if the invention as claimed fulfils the requirements of Art. 83 EPC.

Technical Effect in Claim If a technical effect is expressed in the claim as a functional feature of the subject matter claimed, it must be examined under Art. 83 EPC if the disclosure of the invention is sufficiently clear and complete to allow the skilled person to carry out the invention as claimed, i.e. It needs to be examined if the skilled person is enabled to achieve the claimed effect without undue burden over the whole scope claimed. “...as the effect is part of the claim, it appears... that only an objection for insufficiency can be raised under certain circumstances; these circumstances being that the application as filed would not contain sufficient information on the relevant criteria for finding appropriate alternatives over the claimed range with reasonable effort.” (T 5/06, point 7)

Art 56 Vs Art 83 For Art. 56 or 83 EPC it follows that, depending on the wording of the claim, the non-achievement of a technical effect underlying the problem purportedly solved, has different consequences, depending on the circumstances: if the effect is not expressed in a claim but is part of the problem to be solved, there is a problem of inventive step If the effect is expressed in a claim, there is a problem of sufficient disclosure (G1/03, point 2.5)

Late Filed Evidence Guidelines C-VI, referring to Articles 56 and 83 Under certain circumstances later filed examples or new effects may be taken into account as evidence in support of the patentability, e.g. additional example to demonstrate that on the basis of the information given in application the invention can be applied over the whole field claimed, or as evidence for inventive step, provided that the new effect is implied or at least related to an effect disclosed in the original application (see also T 0893/02 re. Art 56 ) No Help if: Art 56 - Evidence is the first disclosure going beyond mere speculation (T 1306/04, T 1329/04, T 0861/08) Art 83 - Effect is not made at least plausible in application per se (T 0609/02)

Guidelines C IV-7.4: “… it is an accepted principle in most patent systems that two patents cannot be granted to the same applicant for one invention. It is permissible to allow an applicant to proceed with two applications having the same description where the claims are quite distinct in scope and directed to different inventions.” Guidelines C VI-9.1.6: “… parent and divisional applications may not claim the same subject matter…. This means not only that they must not contain claims of substantially identical scope, but also that one application must not claim the subject matter claimed in the other, even in different words. The difference between the claimed subject matter of the two applications must be clearly distinguishable.” 19 Double Patenting

Conflicting Case Law T587/98 No express or implicit provision in the EPC which prohibits the presence in a divisional of a claim which is related to a claim in the parent such that the parent claim includes all the features of the divisional claim combined with an additional feature. T307/03 Suggested that double patenting objections could be raised in the situation where one claim completely encompassed the other and where there were partially overlapping claims. To avoid this objection of double patenting the Applicants would have had to confine the subject matter of the Divisional to subject matter not already claimed in the Parent. 20

T 587/98 Vs. T 307/03 21 Claims of Parent represented by solid line Claims of Divisional represented by dotted line

EPO Policy Double patenting is only an issue if the subject matter of a claim in the application/patent is identical to the subject matter of a claim in the related application, i.e. both related to the same invention.  No requirement that the wording is identical Another way to look at it:  If claim X lacks novelty over claim Y, and claim Y lacks novelty over claim X, then an objection of double patenting can be raised. 22

Examples 23 Feature A Feature B Feature C Feature D Independent claim 1 Dependent claim 2 Granted parent Feature A Feature B Feature C Feature D Independent claim 1 Pending Divisional Object to double patenting? Yes – Claim 2 (parent) and claim 1 (divisional) relate to indentical subject matter.

Examples 24 Feature A Feature B Feature C Independent claim 1 Granted parent Feature A Feature B Feature C Feature D Independent claim 1 Pending Divisional Object to double patenting? No – Claim 1 of the parent is broader than and fully encompasses claim 1 of the divisional, but the subject-matter of the two claims is not identical.

Examples 25 Feature A Feature B Feature C Feature D Independent claim 1 Granted parent Feature A Feature B Feature C Feature E Independent claim 1 Pending Divisional Object to double patenting? No – Feature E distinguishes the divisional from the parent Feature D distinguishes the parent from the divisional

26 Europe play a different game Added subject matter Obviousness / Inventive Step Double patenting How will the law be applied on a national level?

Backup slides 27 Double Patenting Detail

28 T 587/98 - Claims Parent Claim 1: A data storage device comprising: - Substrate; - First dielectric layer; - Magneto-optic layer; and - Second dielectric layer. Divisional Claim 1 claims 4 alternatives one of which is : A data storage device comprising: - Substrate; - Dielectric layer; and - Magneto-optic layer.

T 587/98 – Exam Division Exam Division refused divisional application because the subject matter claimed in the divisional and that claimed in the parent overlapped and in the overlap region the same subject matter was claimed twice Exam Division based its refusal on the Guidelines in combination with Art. 125 EPC: CIV-7.4 – “…it is an accepted principle in most patent systems that two patents cannot be granted to the same applicant for one invention.” Art. 125 – In the absence of procedural provisions in this Convention, the European Patent Office shall take into account the principles of procedural law generally recognised in the Contracting States. 29

T 587/98 – Appeal Art. 125 does not provide basis for a prohibition on double patenting: Institution of divisional applications defined in the convention is self-contained and complete Prohibition of “conflicting” claims would be a matter of substantive law rather than a matter of procedure No express or implicit provision in the EPC which prohibits the presence in a divisional of a claim which is related to a claim in the parent such that the parent claim includes all the features of the divisional claim combined with an additional feature 30

T 307/03 - Claims Parent: Claim 1: Double metal cyanide (DMC) complex comprising: - up to 10 wt% of a crystalline DMC component; - at least 90 wt% of a DMC component which is amorphous to X-rays and comprises a water-soluble aliphatic alcohol as complexing agent. Claim 3: Complex as in claim 1 having a surface area of less than 30m 2 /g. Divisional: Claim 1 of 2 nd Auxiliary Request: Catalyst having a surface area of less than 30m 2 /g and comprising: - up to 10 wt% of a highly crystalline DMC compound; - at least 90 wt% of a substantially amorphous DMC complex which is prepared in the presence of a water-soluble alcohol as a complexing agent. 31

T 307/03 - Appeal Board acknowledges that the EPC does not contain any specific provisions relating to double patenting Board does not regard this as decisive: double patenting is expensive. Legislator cannot be expected to have made provisions to regulate what will on the grounds of economics alone be a very rare occurrence Nevertheless, Board concludes the principle of prohibition of double patenting can be found in Art. 60 EPC: The right to a European patent shall belong to the inventor or his successor in title. From this it is to be deduced that the inventor has a right to the grant of one and only one patent 32

T 307/03 - Appeal Double patenting objection can be raised in respect of 2 nd Aux. Request To avoid this objection of double patenting the Applicants would have had to confine the subject matter of the Divisional to subject matter not already claimed in the Parent 33

Case Law T1391/07 “....in the case in which the scopes of protection conferred by the respective subject-matters overlap only partially with each other as there is no manifest objective reason to deny the legitimate interest of the applicant in obtaining a protection different from – although partially overlapping with - that of the parent already granted.” T877/06 Followed reasoning of T1391/07 34