|European Case Law Identifier:||ECLI:EP:BA:1984:T012882.19840112|
|Date of decision:||12 January 1984|
|Case number:||T 0128/82|
|Language of proceedings:||DE|
|Download and more information:||
|Title of application:||-|
|Applicant name:||Hoffmann-La Roche|
|Headnote:||Where a known compound is for the first time proposed and claimed for use in therapy, the fact that a specific use is disclosed in the specification does not in itself call for a restriction of the purpose-limited product claim to that use.|
|Relevant legal provisions:||
|Keywords:||First medical indication|
Summary of Facts and Submissions
I. European patent application No. 79 100 378.3 filed on 9 February 1979 and published on 22 August 1979 (publication No. 0 003 602) which claimed priority of the earlier Swiss application CH 1404/78 of 10 February 1978 was refused by the decision of the Examining Division 005 of the European Patent Office dated 31 March 1982. The decision was based on claims 1-8 as originally filed reading as follows:
1. Pyrrolidine derivatives having the general formula (FORMULA I) wherein R1 signifies o-methoxybenzoyl, m-methoxybenzyl, p-methoxybenzyl or p-fluorbenzyl as an active pharmaceutical substance.
2. 1-(p-methoxybenzyl)-2-pyrrolidinone as an active pharmaceutical substance.
3. Pyrrolidine derivatives having the general formula I as claimed in claim 1 as active substances combating cerebral insufficiency and increasing intellectual ability.
4. 1-(p-methoxybenzyl)-2-pyrrolidinone as an active substance combating cerebral insufficiency and improving intellectual ability.
5. Medical preparations containing a pyrrolidine derivative having the general formula I as claimed in claim 1.
6. A preparation combating cerebral insufficiency and improving intellectual ability containing a pyrrolidine derivative having the general formula I as claimed in claim 1.
7. Medical preparations containing 1-(p-methoxybenzyl)-2- pyrrolidinone.
8. A preparation combating cerebral insufficiency and improving intellectual ability containing 1-(p-methoxy-benzyl)-2-pyrrolidinone. II.The application was refused on the grounds that it failed to fulfil the requirements of Article 52(4) and Article 54(5) EPC. Claims 1, 2, 5 and 7, it was stated, related to previously known pyrrolidine derivatives, although hitherto their pharmaceutical use had not been described. Under Article 54(5) a subject-matter of this kind could be regarded as novel as long as it was intended for use with a method referred to in Article 52(4) and its use in connection with one such method was not comprised in the state of the art. The subject-matter of the current claims 1, 2, 5 and 7 failed to meet this requirement because it was not limited to the specific therapeutic use of the known compounds as first discovered. The word "a" ("einem" in the German text) used in Article 54(5) EPC, it was stated, should be regarded as having numerical significance. In the circumstances there was no need to go further into the matter of the insufficient support provided by the description for claims 1, 2, 5 and 7.
III. The applicants appealed against this decision by a document received on 26 May 1982 and duly paid the appeal fee. The statement of grounds was filed later on 2 August 1982. In the statement of grounds the appellants submit that in such a case substance claims should be acceptable without a specific statement of purpose limited to the mode(s) of use actually disclosed. The word "einem" in Article 54(5) EPC (German text), they claimed, should not be regarded as having numerical significance but as an indefinite article. The interpretation of Article 54(5) and Article 52(4) EPC as used by the Examining Division had, it was submitted, no basis in the European Patent Convention. There was a serious need for legal protection for the claims not containing a specific statement of indication. If only claims with a statement of purpose limited to the specifically disclosed indication were to be granted, this would in addition give rise to a serious uncertainty in law as to the scope and enforceability of the patent. Moreover, claims 1, 2, 5 and 7 were supported by the description and therefore met the requirements of Article 84 EPC.
IV. The appellants requested that the contested decision be rescinded and that a European patent be granted on the basis of the existing claims 1 to 8 or in the alternative with the scope of existing claims 3, 4, 6 and 8.
V. At the Board's request new claims were submitted on 29 April 1983 and certain additions were made to them in a communication dated 6 June 1983. These read as follows:
1. Pyrrolidine derivatives having the general formula (FORMULA I) wherein R1 signifies o-methoxybenzoyl, m-methoxybenzyl, p-methoxybenzyl or p-fluorbenzyl for use as an active therapeutic substance.
2. 1-(p-methoxybenzyl)-2-pyrrolidinone for use as an active therapeutic substance.
3. Pyrrolidine derivatives having the general formula I as claimed in claim 1 for use as active substances combating cerebral insufficiency and improving intellectual ability.
4. 1-(p-methoxybenzyl)-2-pyrrolidinone for use as an active substance combating cerebral insufficiency and improving intellectual ability.
5. A medical preparation containing a pyrrolidine derivative having the general formula I as claimed in claim 1 and a pharmaceutically inert excipient.
6. A substance combating cerebral insufficiency and improving intellectual ability containing a pyrrolidine derivative having the general formula I as claimed in Claim 1 and a pharmaceutically inert excipient.
7. A medical preparation containing 1-(p-methoxybenzyl)-2- pyrrolidinone and a pharmaceutically inert excipient.
8. A substance combating cerebral insufficiency and improving intellectual ability containing 1-(p-methoxybenzyl)- 2-pyrrolidinone and a pharmaceutically inert excipient. Claims 1 to 4 differ from the claims as rejected by the Examining Division in that their formulation has been improved to take account of the wording of Article 54(5) EPC, and claims 5 to 8 in the addition of a statement to the effect that the preparation contains a pharmaceutically inert excipient.
Reasons for the Decision
1. The appeal complies with Articles 106-108 EPC and Rule 64 EPC and is therefore admissible.
2. The subject-matter of the claims does not go beyond the content of the application in the version originally filed. Use of the compounds listed in claim 1 as active pharmaceutical substances and medical preparations was originally widely disclosed (cf. page 1, lines 7-10; page 2, lines 3-9 and page 5, lines 26-29, as also original claims 1, 2, 5, 7, 9 and 11).
3. The applicants have imparted to experts the new teaching that it is possible to use pyrrolidine derivatives having the formula I and not previously described as being pharmaco-dynamically active as active therapeutic substances, suitable especially for combating cerebral insufficiency and improving intellectual ability. However, the pyrrolidine derivatives on which the claimed substances are based are known in the art. Chemical Abstracts 63, 16256e (1965) describes inter-alia 1-(o-methoxybenzoyl)-2-pyrrolidinone, while FR-A-2 294 698 makes mention, on page 3, lines 30 to 37, of 1-(p-fluorbenzyl)-2-pyrrolidinone and, in the Table on page 13, of 1-(p-menthoxybenzyl)-2-pyrrolidinone and 1-(m-methoxybenzyl) -2-pyrrolidinone. However, their use in any method covered by Article 52(4) EPC is not conventional. Under Article 54(5) EPC such subject-matter must be regarded as novel.
4. It must also be affirmed, in agreement with the decision of the Examining Division, that an inventive step has been achieved. Although 1-(3, 4,5-trimethoxybenzoyl)-2-pyrrolidinone was already known from Chemical Abstracts 87, 39272m and 68145e (1977) as a substance improving learning and memory ability the only representative of the subject-matter of the application which also carries a substituted benzoyl group on the nitrogen atom of the pyrrolidinone nucleus, namely 1-(-o-methoxybenzoyl)- 2-pyrrolidinone, differs from this known compound in that it contains only a single methoxy group instead of three. Moreover, this methoxy group is linked to the 2-(or ortho-) position of the benzoyl residue. Given these structural differences it was impossible for a person skilled in the art to foresee that the compounds covered by the application, including this 1-(o-methoxybenzoyl)-2-pyrrolidinone, would bring about an improvement in learning and memory ability. Nor was it obvious that they would have any therapeutic activity.
5. The existing claims come under two different headings: claims 1 to 4 are purpose-limited substance claims and claims 5 to 8 are preparation claims. The patentability of both types of claims as such is not disputed in substance by the Examining Division.
6. However, the reasons adduced by the Examining Division can no longer be regarded as applying to the present claims 5 and 7. Article 54(5) EPC relates to substances or compounds already known in the art, which the compounds covered by claims 5 and 7 are not. The only question that, therefore, still has to be considered is whether the broad version of claims 1 and 2 is allowable having regard to Article 54(5) EPC.
7. The question involved here has been discussed in depth in the patent literature. Besides those advocating the widest possible statement of purpose there are also those who urge that the statement of purpose should be limited. A summary of the main arguments on either side is to be found, for example, in GAUMONT - Revue trimestrielle de droit commercial et de droit économique 1980, pages 441-455, a publication from which the applicants quote on several occasions.
8. The first question needing clarification is whether the European Patent Convention offers a basis for a limited statement of therapeutic purpose susceptible of narrow interpretation. In the opinion of the Board of Appeal the Convention neither prohibits nor requires an unlimited statement of purpose. Neither Article 54(5) nor Article 52(4) clearly stipulates the scope of statements of purpose for the surgical or therapeutic method referred to.
9. It is a generally recognised rule of international law that when interpreting international treaties ancillary use may be made of material relating to their genesis. Under Article 32 of the Vienna Convention on the Law of Treaties of 23 May 1969 (Extracts published in this O.J., p. 192), recourse may be had to supplementary means of interpretation, particularly the preparatory work for a treaty and the circumstances in which it was concluded, in order to confirm the meaning arrived at by application of Article 31 or to determine the meaning when application of Article 31(a) leaves the meaning ambiguous or obscure, or (b) produces a meaning which is obviously nonsensical or unreasonable. Although because it only came into force in 1980 the Vienna Convention cannot be applied directly to the interpretation of the European Patent Convention, it is generally accepted that Articles 31 and 32 merely codified international law as it already existed (cf. Lord Diplock, Fothergill vs. Monarch Airlines (1981) A.C. 251 and GRUR Int. 1983, 205-212 (Bruchhausen). Recourse to the travaux préparatoires for Article 54(5) EPC would in fact seem obvious. This article creates substantive patent law that does not go back to the Strasbourg Convention on the Unification of Certain Points of Substantive Law on Patents for Invention of 27 November 1963, and is also not modelled on concepts existing in the national patent laws of most countries represented at the Munich Diplomatic Conference of 1973. In addition to the general concept of novelty (Article 54(1)-(4) EPC) this article also introduces, in respect of substances and compounds used in surgical and therapeutic treatment and in diagnostic processes carried out on humans and animals (hereinafter referred to briefly as "therapy"), a special concept of novelty unknown in other technical fields. This article was based on the French form of patent for medical preparations applying at the time of the Munich Diplomatic Conference. However, the history of Article 54(5) EPC does not reveal any uniform idea on the part of the negotiating States as to the breadth of the claim to be allowed for pharmaceutical inventions. The protection of inventions relating to therapy has under the EPC been incorporated in the general substantive patent law (Part II Substantive Patent Law, Chapter I - Patentability - Articles 52-57) and has thus been separately regulated, making it impossible clearly to decide which elements of the French form of protection for medical preparations it was intended to include in the EPC. On the other hand, the protection afforded by a French medical preparation patent was not restricted to a given pharmaceutical application (such as the combating of a certain disease). It is therefore impossible to derive from the travaux préparatoires any arguments in favour of limiting claim scope.
10. Whatever the case may be, the practice of the European Patent Office hitherto has shown that substance and medical preparation claims for therapeutically active compounds not limited to specific indications are allowed, even though as a rule only certain specific activities are stipulated. This practice usually always concerns new compounds. It does not derive from the Convention that compounds which although previously known are still patentable under Article 54(5) are in principle to be treated differently. If an inventor is granted absolute protection in respect of a new chemical compound for use in therapy, the principle of equal treatment would require that an inventor who for the first time makes a known compound available for therapy should be correspondinlyg rewarded for his service with a purpose-limited substance claim under Article 54(5) EPC to cover the whole field of therapy. Any other treatment would only be justified were Article 54(5) EPC absolutely to forbid a broad protective scope. The fact that Article 54(5) EPC does not contain any requirement that protection should be broad is of itself no reason for refusing to grant such protection. As a general rule the usual practice as it relates to new compounds should be followed.
11. It is the conviction of the Board of Appeal that the word "a" ("einem" in the German text) used in Article 54(5) EPC should not be regarded as having numerical significance. This conclusion is based on the fact that the paragraph concerned expressly refers to Article 52(4) EPC in which there is mention of three different groups of methods - surgical, therapeutical and diagnostic - all of which are in the plural. Were the word "a" ("einem" in the German text) meant as having numerical significance, the effect would be to make the patenting of substances or compounds suitable for use in more than one of these three groups of methods impossible. If only limited protection were to be allowed for a substance, this would, moreover, produce a situation that could not be justified, namely one in which substances or compounds with several specific therapeutic actions could not be dealt with in a single patent application.
12. The Examining Division has, in addition, advanced the view that the description fails to support claims 1, 2, 5 and 7 from the point of view of Article 84 EPC. It says that the description only discloses a quite specific therapeutic effect on the part of compounds having the formula I and that the fact that compounds acccording to the invention are suitable for a given therapeutic application does not mean that they are also usable for all and any therapeutic purposes. In the Board's view, however, this is not the point at issue. The mere fact that there are not instructions concerning all and any possible specific therapeutic applications does not justify limiting the scope to the therapeutic application actually mentioned. This would not be in accord with the general practice of the European Patent Office concerning therapeutically active compounds.
13. Attention is also drawn to the following points: Under Article 54(5) EPC a compound which is known but not used therapeutically is to be regarded as novel. Novelty, however, is not only destroyed by the fact that the same specific therapeutic effect is already known in the art, but suffers also from the disclosure of any other specific therapeutic application. The disclosure of any specific effect, therefore, always has the same consequences as far as novelty is concerned; which in turn makes it fair to regard as admissible a broad statement of purpose covering all and any specific indications.
14. To summarise: in the present case Article 54(5) EPC permits a purpose-limited substance claim stating a general therapeutic purpose. This does not rule out the conceivability of other cases in which because, for example, of insufficient inventive step, the state of the art could make it necessary to limit the scope of application. In the circumstances it is unnecessary to discuss the alternative application.
15. No application has been made for reimbursement of the appeal fee in accordance with Rule 67 EPC, nor would the circumstances of the case justify it.
For these reasons, it is decided that:
1. The decision of the Examining Division 005 of 31 March 1982 is set aside.
2. The matter is referred back to the previous instance with the order that a European patent be granted on the basis of claims 1 to 8 as filed on 29 April 1983 and a suitably amended description. In addition "(Chemical Abstracts 63, 16256e (1965) and FR-A-2 294 698)" should be inserted on page 1, line 7 of the specification, and the words "and a pharmaceutically inert excipient" should be added at the end of each of claims 5 to 8.