Biogen Idec International GmbH
[2015] APO 17
•27 April 2015
IP AUSTRALIA
AUSTRALIAN PATENT OFFICE
Biogen Idec International GmbH [2015] APO 17
Patent Number: 752733
Title:Utilisation of Dialkylfumarates
Patentee: Biogen Idec International GmbH
Delegate: Dr M-A. Fam
Decision Date: 27 April 2015
Hearing Date: 8 April 2015, in Canberra
Catchwords: PATENTS – re-examination of patent following request for an extension of term – objection of “whole of contents” novelty – lack of novelty established – claims 18, 23, 24, 25, 26, 27, 42, 47, 48, 49, 50, 51, 64, 67, 68, 69, 74, 75, 76, 77, 78 and 82 are not novel – opportunity to amend
Representation: Patentee: Angus Lang of counsel assisted by Lisa Taliadoros of Jones Day
IP AUSTRALIA
AUSTRALIAN PATENT OFFICE
Patent Number: 752733
Title:Utilisation of Dialkylfumarates
Patentee: Biogen Idec International GmbH
Date of Decision: 27 April 2015
DECISION
Claims 18, 23, 24, 25, 26, 27, 42, 47, 48, 49, 50, 51, 64, 67, 68, 69, 74, 75, 76, 77, 78 and 82 are not novel.
I allow the patentee two months from the date of this decision to propose amendments to overcome this deficiency.
REASONS FOR DECISION
Background
Patent application 11572/00 was filed by Fumapharm AG (Fumapharm) on 29 October 1999. The application was subsequently examined and patent 752733 granted on 16 January 2003. Fumapharm later changed its name to Biogen Idec International GmbH (Biogen). Biogen filed a request for an extension of term for 752733. The request was granted and the term of the patent extended from 29 October 2019 to 29 October 2024.
In considering the extension of term request, the Commissioner determined that there was information relevant to the validity of 752733 and decided to re-examine the patent. A re‑examination report was issued on 23 January 2014 and subsequent reports issued on 2 April 2014 and 30 May 2014. In response to the report issued on 30 May 2014, the patentee requested the opportunity to make oral submissions at a hearing. Another re-examination report issued on 22 August 2014 and the patentee was invited to request an oral hearing. The hearing was held in Canberra on 8 April 2015. Biogen was represented by Angus Lang of counsel and Lisa Taliadoros of Jones Day.
As the patent was granted on 16 January 2003, substantive amendments of the Patents Act 1990 brought about by the Intellectual Property Laws Amendment (Raising the Bar) Act 2012 do not apply, other than expanded grounds for re-examination under section 98. However, the expanded grounds are not relevant in the present case. I also note that any subsequent reference to sections of the Patents Act relate to the Patents Act 1990 prior to amendment by the Raising the Bar Act.
The re-examination
In the re-examination report issued on 22 August 2014, the Examiner indicated that claims 18, 23, 24, 26, 27, 42, 47, 48, 50, 51, 69, 70, 71, 72, 73, 74, 75, 77, 78, 82, 88 and 92 lack novelty (“whole of contents”) in view of AU 21593/99 (D1).
Prior to the hearing, Biogen was invited by letter (dated 29 January 2015) to additionally provide submissions in relation to claims 13, 14, 16, 17, 25, 40, 41, 49, 64, 67, 68, 76 and 91. Biogen was also advised that D1 is no longer considered relevant to claims 70, 71, 72 and 73.
Biogen filed written submissions on 30 March 2015 addressing the relevant claims as identified above.
The subject matter of the specification
The specification relates to pharmaceutical preparations containing dialkyl fumarates. The preparations are used in the treatment of host-versus-graft reactions or graft-versus-host reactions in transplantation medicine, and autoimmune diseases, including psoriasis, psoriatic arthritis, neurodermatitis and enteritis regionalis Crohn.
The specification indicates that both graft rejection and autoimmune diseases are based on medically undesirable reactions or dysregulation of the immune system and in general these conditions are treated by the administration of immunosuppressive agents such as cyclosporine (page 1, paragraph [3]).
The dialkyl fumarates of the present patent (752733) are derivatives of fumaric acid. Fumaric acid has the structure of formula (I) shown below, wherein R1 and R2 both represent hydrogen.
Formula (I)
The dialkyl fumarates of 752733 are compounds of formula (I) wherein R1 and R2, which may be the same or different, independently represent a linear, branched or cyclic, saturated or unsaturated C1-20 alkyl radical which may be optionally substituted with halogen, hydroxy, C1‑4 alkoxy, nitro or cyano.
The preparations containing dialkyl fumarates surprisingly permit a positive modulation of the immune system in host-versus-graft reactions, graft-versus-host reactions and other autoimmune diseases (page 6, paragraph [3]).
The specification further indicates that the dialkyl fumarates to be used according to the invention are not the active ingredient per se, but are prodrugs which are converted into the active ingredient following administration (page 11, paragraph [2]). In the case of dimethyl fumarate, this is metabolised to methyl hydrogen fumarate (or monomethyl fumarate). Methyl hydrogen fumarate corresponds to formula (I) wherein one of R1 and R2 is hydrogen and the other is methyl. Figure 1 of the specification shows that oral administration of dimethyl fumarate allows for a fast onset and high initial plasma levels of methyl hydrogen fumarate (monomethyl fumarate) (page 16, paragraph [2]).
The dialkyl fumarates may be used alone or as a mixture of several compounds, optionally in combination with the customary carriers and excipients (page 8, paragraph [4]). In addition, therapy with dialkyl fumarates may be carried out in combination with one or more preparations of the triple drug therapy generally used in organ transplantation or with cyclosporine A alone (page 9, paragraph [3]). In this situation, the preparation administered may contain a combination of the active ingredients.
The specification indicates that therapy with the fumaric acid derivatives according to the invention rarely results in serious side effects (page 15, paragraph [3]).
The claims of the specification
The specification ends with 92 claims. The claims relevant to the re-examination are claims 13, 14, 16, 17, 18, 23, 24, 25, 26, 27, 40, 41, 42, 47, 48, 49, 50, 51, 64, 67, 68, 69, 74, 75, 76, 77, 78, 82, 88, 91 and 92 and these are discussed in detail below. The remaining claims will not be considered further.
Claims construction
The approach to claims construction was considered by Bennett J in H Lundbeck A/S v Alphapharm Pty Ltd [2009] FCAFC 70 at [118]-[120]; 81 IPR 228:
“the end point is that the words in a claim should be read through the eyes of the skilled addressee in the context in which they appear. … While the claims define the monopoly claimed in the words of the patentee’s choosing, the specification should be read as a whole … It is not permissible to read into a claim an additional integer or limitation to vary or qualify the claim by reference to the body of the specification … However, terms in the claim which are unclear may be defined or clarified by reference to the body of the specification …”
Biogen’s submissions addressed the claims in groups and it is convenient to adopt the same grouping here.
Pharmaceutical preparation claims 13, 14, 16, 17, 40 and 41
Claim 13 is independent and is as follows (emphasis added):
“13. Pharmaceutical preparation in the form of micro-tablets or micro-pellets consisting of one or more dialkyl fumarates of the formula
wherein R1 and R2, which may be the same or different, independently represent a linear, branched or cyclic, saturated or unsaturated C1-20 alkyl radical which may be optionally substituted with halogen, hydroxy, C1-4 alkoxy, nitro or cyano, and optionally suitable carriers and excipients for use in transplantation medicine or for the therapy of autoimmune diseases or psoriasis, psoriatic arthritis, neurodermatitis or enteritis regionalis Crohn.”
Dependent claims 16 and 17 define further features of the preparation as indicated below (emphasis added):
“16. A preparation according to any one of claims 13 to 15 comprising dimethyl fumarate, diethyl fumarate or methylethyl fumarate.
17. A preparation according to any one of claims 13 to 16 comprising an amount of the active ingredient corresponding to 10 to 300 mg of fumaric acid.”
Dependent claim 14 defines additional features of the preparation and dependent claims 40 and 41 are directed to the pharmaceutical preparation of claim 13 “when used” in transplantation medicine or therapy.
“Consisting of”
Biogen submitted that “consist of” should be given its ordinary meaning, namely “to be made up or composed of” (Macquarie Dictionary, 5th Edition). Thus, “consisting of” in claim 13 should be construed in an exhaustive sense, i.e. the claim does not permit the presence in the pharmaceutical preparations of material amounts of fumaric acid derivatives that are not dialkyl fumarates.
It was further submitted that the context of claim 13 makes it clear that “consisting of” is used in an exhaustive sense, through the use of the words “one or more dialkyl fumarates of the formula” and the setting out of the detailed chemical formula to define the class of compounds permitted. Additionally, if the wording of the claim is intended to be read inclusively, i.e. permitting the presence of other active ingredients such as alkyl hydrogen fumarates, there would be no need to refer to optional carriers or excipients, as these could have been included without requiring specific reference in the claim.
Biogen acknowledged that all of the challenged claims encompass preparations that contain impurities or breakdown products of dialkyl fumarates, including alkyl hydrogen fumarates. However, these are present in concentrations that are not therapeutically effective, and are formed during the manufacture or shelf-life of the product.
It was submitted that claim 13 does not encompass preparations that contain alkyl hydrogen fumarates in therapeutically effective amounts, or wherein the alkyl hydrogen fumarate is an active ingredient. However, preparations containing “de minimus” or impurity amounts of the substance fall within the scope of the claim.
As indicated above, the plain meaning of the term “consist of” is “to be made up or composed of” (Macquarie Dictionary).
The courts have also given some consideration to the term, albeit in the context of construing the words “comprising” or “comprise”. In Asahi Kasei Kogyo Kabushiki Kaisha v W R Grace & Co (1991) 22 IPR 491 at 514 – 515, Heerey J held that in the context of that case “comprise” meant “consists of” and that the word was used in an exhaustive sense rather than an inclusive sense.
In General Clutch Corporation v Sbriggs Pty Ltd (1997) 38 IPR 359 at 376, Lindgren J concluded:
“In my opinion, the words “spring clutch comprising” signify that what is claimed is a device which possesses the four functional elements to which I referred earlier, and which consists of, is made up of, is composed of, or is constituted by, the integers described in claim 1, and no more.” (emphasis in original)
In Fresenius Medical Care Australia Pty Limited v Gambro Pty Limited [2005] FCAFC 220; (2006) 67 IPR 230 at [56] – [64], the Full Court considered whether “comprise” means “consists only of” or “includes”. The Full Court held that in this context “comprise” had an inclusive meaning, and was not intended to mean and does not mean “consists only of”.
It therefore appears that the natural meaning of “consists of” is “consists only of”, i.e. the term is used in an exhaustive sense.
However, noting Biogen’s submissions that the preparation naturally contains impurities or breakdown products, in practice “consisting of” in the present context does not mean the preparation is purely dialkyl fumarates. It seems reasonable to adopt this construction, considering that the words are read through the eyes of the skilled addressee (H Lundbeck A/S v Alphapharm Pty Ltd supra).
Claim 13 is thus considered to define a pharmaceutical preparation consisting of one or more dialkyl fumarates, and optionally carriers or excipients. The preparation does not contain other components, apart from non-therapeutically effective amounts of impurities or breakdown products of the dialkyl fumarates, which have formed during manufacture or shelf-life of the preparation.
“Comprising”
The plain meaning of the term “comprise” or “comprising” is “to include; contain”, “to consist of; be composed of” (Macquarie Dictionary, 6th Edition). As indicated above, the courts have considered the term to be used in either an exhaustive sense or an inclusive sense, depending on the context.
Dependent claims 16 and 17 define a preparation comprising a particular fumarate or comprising an amount of active ingredient. Biogen submitted that as these claims are dependent, they narrow the features defined by claim 13 and therefore “comprising” is used in an exhaustive sense.
This seems an appropriate approach and in the context of these claims “comprising” is given an exhaustive meaning.
“Active ingredient”
Dependent claim 17 defines a preparation wherein the amount of active ingredient present corresponds to 10 to 300 mg of fumaric acid. The specification at page 11, paragraph [2] indicates that the dialkyl fumarates are not the active ingredient per se, but a prodrug (that is converted to the alkyl hydrogen fumarate). As there is no antecedent for the “active ingredient” in claims 13 to 16, the question arises as to whether this term refers to the dialkyl fumarate or the alkyl hydrogen fumarate.
Biogen submitted that the statement on page 11 does not preclude the dialkyl fumarate from being an active ingredient. I note that this submission is supported by the fact that the specification, when referring to the dialkyl fumarates, indicates that the amounts to be used are selected such that the preparations contain the active ingredient in certain amounts (page 8, paragraph [4]).
Therefore, in the context of claim 17, the term “active ingredient” is construed to mean the dialkyl fumarate.
Conclusion on construction of claims 13, 14, 16, 17, 40 and 41
Claim 13 is considered to define a pharmaceutical preparation consisting of one or more dialkyl fumarates, and optionally carriers or excipients. The preparation does not contain other components, apart from non-therapeutically effective amounts of impurities or breakdown products of the dialkyl fumarates, which have formed during manufacture or shelf-life of the preparation. A similar construction applies to dependent claims 14, 16, 17, 40 and 41.
Use claims 18, 23, 24, 25, 26 and 27 and “when used” claims 69, 74, 75, 76, 77 and 78
Claims 18 and 69 are independent and are as follows:
“18. The use of one or more dialkyl fumarates for preparing a pharmaceutical preparation in the form of micro-tablets or micro-pellets for the therapy of psoriasis, psoriatic arthritis, neurodermatitis or enteritis regionalis Crohn, or autoimmune diseases selected from the group consisting of polyarthritis, multiple sclerosis, juvenile-onset diabetes, Hashimoto’s thyroiditis, Grave’s disease, systemic Lupus erythematodes (SLE), Sjogren’s syndrome, pernicious anaemia and chronic active (lupoid) hepatitis.
69. One or more dialkyl fumarates in a preparation in the form of micro-tablets or micro-pellets when used for the therapy of psoriasis, psoriatic arthritis, neurodermatitis or enteritis regionalis Crohn or autoimmune diseases selected from the group consisting of polyarthritis, multiple sclerosis, juvenile-onset diabetes, Hashimoto’s thyroiditis, Grave’s disease, systemic Lupus erythematodes (SLE), Sjogren’s syndrome, pernicious anaemia and chronic active (lupoid) hepatitis.”
Claims 23, 24, 25, 26 and 27 are dependent on claim 18 and define additional features of the preparation. Similarly, claims 74, 75, 76, 77 and 78 are dependent on claim 69 and also define further features of the preparation.
Biogen stated that during the re-examination, the reasoning relied on by the Examiner in relation to these claims is that they “are not restricted to using a preparation free of alkyl hydrogen fumarates”, i.e. the use of alkyl hydrogen fumarates is not excluded from the scope of the claims.
Biogen submitted that claim 18 refers to “The use of one or more dialkyl fumarates” and that these words suggest that the use of other kinds of fumaric acids is not included. If this were otherwise, there would have been no need to refer to “one or more” dialkyl fumarates being used, as these words would be redundant. It was further stated that the purpose and effect of these words is to state the nature of the fumaric acid derivatives that may be used as the active ingredients in the preparation of the claim.
Biogen indicated that this construction is supported by parts of the specification that refer to the use of dialkyl fumarates alone or in mixtures of dialkyl fumarates, in combination with carriers and excipients, or in combination with other drugs customarily used in triple drug therapy or cyclosporine A alone (page 8, paragraph [4] and page 9, paragraph [3]). It was submitted that the specification clearly points to a limited number of compounds that the dialkyl fumarates can be combined with.
Biogen submitted that similar reasoning applies to dependent claims 23, 24, 25, 26 and 27, and claim 69 and its dependent claims 74, 75, 76, 77 and 78. In particular, it was stated that claim 69 does not encompass cases in which the preparation is made using fumaric acid derivatives other than those specifically referred to in the claim.
The reference in claims 18 and 69 to “one or more dialkyl fumarates”, using a plain meaning of the words, is taken to define either a single dialkyl fumarate or a mixture of dialkyl fumarates. The wording of the claims does not suggest that other components cannot be present when making the preparation. This is consistent with the specification, which indicates that carriers and excipients may also be present (page 8, paragraph [4]). Similarly, components that are therapeutically active may be included in the preparation, for example cyclosporine A (page 9, paragraph [3]).
I also note that there is no indication that the preparation is precluded from containing alkyl hydrogen fumarates. There is no suggestion that the presence of these substances would be deleterious. In the case of methyl hydrogen fumarate (monomethyl fumarate), this is not unexpected, given that this compound is the active ingredient derived from dimethyl fumarate (page 11, paragraph [2] and Figure 1) and medicaments containing it are known (page 6, paragraph [5]).
Conclusion on construction of claims 18, 23, 24, 25, 26, 27, 69, 74, 75, 76, 77 and 78
Claim 18 is considered to define the use of a single dialkyl fumarate or a mixture of dialkyl fumarates for preparing a pharmaceutical preparation for the therapy of certain diseases, wherein other components may be present when preparing the preparation. A similar construction applies to dependent claims 23, 24, 25, 26 and 27.
Similarly, claim 69 and its dependent claims 74, 75, 76, 77 and 78 are considered to define a single dialkyl fumarate or a mixture of dialkyl fumarates in a preparation when used for the therapy of the listed diseases, wherein other components may be present in the preparation.
Method claims 42, 47, 48, 49, 50, 51, 64, 67 and 68
Claims 42 and 64 are independent and are as follows (emphasis added):
“42. A method for the therapy of psoriasis, psoriatic arthritis, neurodermatitis or enteritis regionalis Crohn or autoimmune diseases selected from the group consisting of polyarthritis, multiple sclerosis, juvenile-onset diabetes, Hashimoto’s thyroiditis, Grave’s disease, systemic Lupus erythematodes (SLE), Sjogren’s syndrome, pernicious anaemia and chronic active (lupoid) hepatitis comprising administering to a patient in need of such treatment a preparation in the form of micro-tablets or micro-pellets comprising one or more dialkyl fumarates optionally together with a suitable carrier and/or excipient.
64. A method of treating host-versus-graft reactions or graft-versus-host reactions in transplantation medicine or in the therapy psoriasis, psoriatic arthritis, neurodermatitis or enteritis regionalis Crohn or autoimmune diseases comprising administering to a patient in need of such treatment a pharmaceutical preparation comprising one or more dialkyl fumarates of the formula
wherein R1 and R2, which may be the same or different, independently represent a linear, branched or cyclic, saturated or unsaturated C1-20 alkyl radical which may be optionally substituted with halogen, hydroxy, C1-4 alkoxy, nitro or cyano, and optionally suitable carriers and excipients.”
Claims 47, 48, 49, 50 and 51 are dependent on claim 42 and define additional features of the preparation. Similarly, claims 67 and 68 are dependent on claim 64 and also define further features of the preparation.
Biogen submitted that even on the construction put forward in the re-examination reports and the letter dated 29 January 2015, the claims are novel in view of D1.
The letter dated 29 January 2015 indicated that claim 64 is considered to define a method of treating host-versus-graft reactions or graft-versus-host reactions in the context of transplantation medicine, or psoriasis, psoriatic arthritis, neurodermatitis or enteritis regionalis Crohn, or autoimmune diseases. This aspect of the claim construction is not in dispute.
In the re-examination reports, the reasoning relied on by the Examiner in relation to this group of claims is that they “are not restricted to using a preparation free of alkyl hydrogen fumarates”, i.e. the use of alkyl hydrogen fumarates is not excluded from the scope of the claims.
Biogen submitted that the dialkyl fumarates of the preparation of claims 42 and 64, and their dependent claims, can be combined with only a limited number of compounds, namely cyclosporine A or substances used in triple drug therapy.
“Comprising”
Claims 42 and 64 both define methods “comprising administering to a patient in need of such treatment a (pharmaceutical) preparation in the form of micro-tablets or micro-pellets comprising one or more dialkyl fumarates” optionally together with suitable carriers and/or excipients.
When asked whether “comprising” is used in an exclusive sense or an inclusive sense, Biogen reiterated that even if the word is used inclusively, D1 is not novelty destroying for these claims.
As previously indicated, the courts have considered “comprising” to be used in either an exhaustive sense or an inclusive sense, depending on the context.
The first occurrence of the term “comprising” in claims 42 and 64 relates to the “method for the therapy” or “method of treating” aspect of the claims. The specification indicates that such therapy or treatment can involve steps in addition to the administration of the dialkyl fumarates, for example parallel administration of separate preparations of drugs used in combination therapy (page 9, paragraph [3] to page 10, paragraph [1]), or alternating dialkyl fumarate therapy with cyclosporine therapy (page 10, paragraph [2]). This is consistent with the use of “comprising” in an inclusive sense, i.e. the therapy or treatment is not limited to one that involves only the step of administering the dialkyl fumarates.
The second occurrence of the term “comprising” in claims 42 and 64 relates to the preparation aspect. Assuming a consistent use of language within these claims would suggest that the second occurrence of “comprising” is also used in an inclusive sense. Conversely, as Biogen submitted previously, if the preparation is intended to permit the presence of other ingredients, there would be no need to refer to optional carriers or excipients, as these could have been included without requiring specific reference in the claim.
As discussed previously, the specification indicates that other components may be present in the preparation, such as cyclosporine A (page 9, paragraph [3]). This is consistent with the use of “comprising” in an inclusive sense, i.e. the preparation may contain other components in addition to dialkyl fumarates.
Conclusion on construction of claims 42, 47, 48, 49, 50, 51, 64, 67 and 68
Claims 42 and 64 are considered to define methods of therapy or treatment wherein the therapy or treatment is not limited to one that involves only the step of administering the dialkyl fumarates. The preparation administered during the therapy or treatment may contain other components in addition to the dialkyl fumarates.
Omnibus claims 82, 88, 91 and 92
The omnibus claims are as follows (emphasis added):
“82. The use of one or more dialkyl fumarates for preparing a pharmaceutical preparation in the form of micro-tablets or micro-pellets for the therapy of psoriasis, psoriatic arthritis, neurodermatitis or enteritis regionalis Crohn or autoimmune diseases selected from the group consisting of polyarthritis, multiple sclerosis, juvenile-onset diabetes, Hashimoto’s thyroiditis, Grave’s disease, systemic Lupus erythematodes (SLE), Sjogren’s syndrome, pernicious anaemia and chronic active (lupoid) hepatitis, said one or more dialkyl fumarates being substantially as hereinbefore described with reference to any one of the examples.
88. A method for the therapy of psoriasis, psoriatic arthritis, neurodermatitis or enteritis regionalis Crohn or autoimmune diseases selected from the group consisting of polyarthritis, multiple sclerosis, juvenile-onset diabetes, Hashimoto’s thyroiditis, Grave’s disease, systemic Lupus erythematodes (SLE), Sjogren’s syndrome, pernicious anaemia and chronic active (lupoid) hepatitis comprising administering to a patient in need of such treatment a preparation in the form of micro-tablets or micro-pellets comprising one or more dialkyl fumarates optionally together with a suitable carrier and/or excipient, said one or more dialkyl fumarates being substantially as hereinbefore described with reference to any one of the examples.
91. A method of treating host-versus-graft reactions or graft-versus-host reactions in transplantation medicine or in the therapy of autoimmune diseases comprising administering to a patient in need of such treatment a pharmaceutical preparation in the form of micro-tablets or micro-pellets comprising one or more dialkyl fumarates of the formula
wherein R1 and R2, which may be the same or different, independently represent a linear, branched or cyclic, saturated or unsaturated C1-20 alkyl radical which may be optionally substituted with halogen, hydroxy, C1-4 alkoxy, nitro or cyano, and optionally suitable carriers and excipients, said one or more dialkyl fumarates being substantially as hereinbefore described with reference to any one of the examples.
92. One or more dialkyl fumarates in the form of micro-tablets or pellets when used for the therapy of psoriasis, psoriatic arthritis, neurodermatitis or enteritis regionalis Crohn or autoimmune diseases selected from the group consisting of polyarthritis, multiple sclerosis, juvenile-onset diabetes, Hashimoto’s thyroiditis, Grave’s disease, systemic Lupus erythematodes (SLE), Sjogren’s syndrome, pernicious anaemia and chronic active (lupoid) hepatitis, said one or more dialkyl fumarates being substantially as hereinbefore described with reference to any one of the examples.”
Claims 82 and 88 are the omnibus “version” of claims 18 and 42 respectively. Therefore the conclusions on the construction of claims 18 and 42 apply equally to the corresponding omnibus version.
Claim 91 is considered to be the omnibus version of claim 64. Although claim 91 only refers to “autoimmune diseases”, this term encompasses psoriasis, psoriatic arthritis, neurodermatitis and enteritis regionalis Crohn (page 9, paragraph [1]). Thus, the conclusions on the construction of claim 64 also apply to claim 91.
Claim 92 is similar to “when used” claim 69 discussed previously. However, claim 92 defines “one or more dialkyl fumarates in the form of micro-tablets or pellets”, whereas claim 69 defines “one or more dialkyl fumarates in a preparation in the form of micro-tablets or micro-pellets” (emphasis added).
As indicated above, the plain meaning of the words “one or more dialkyl fumarates” is taken to mean a single dialkyl fumarate or a mixture of dialkyl fumarates. The question then arises as to whether other components are included in the micro-tablets and pellets of claim 92, in addition to the dialkyl fumarates. However, given that the dialkyl fumarate is “substantially as hereinbefore described with reference to any one of the examples”, it is appropriate to consider what limitation this phrase places on the scope of claim 92 and the other omnibus claims.
In the re-examination reports and the letter of 29 January 2015, it was submitted that the reference to the examples is used only to define the dialkyl fumarate per se, namely dimethyl fumarate, and not to define other features of the preparation containing it.
Biogen submitted that the omnibus claims must be construed narrowly and encompass only those embodiments shown in each of the examples, subject to variations that the skilled addressee would consider minor. It was further stated that the claims must be construed as confined to pharmaceutical preparations described in the examples, subject to any “minor variations”. Thus, the claims do not encompass the use of fumaric acid derivatives other than dialkyl fumarates, as the addition of an active ingredient other than a dialkyl fumarate could not be considered a minor variation.
When queried on the interpretation of the omnibus claims, Biogen submitted that all aspects of the dialkyl fumarate are as described in the examples and not just the chemical structure. As all the examples refer to the same dialkyl fumarate, namely dimethyl fumarate, the omnibus claims must incorporate the manner in which the compound is formulated (noting that the examples describe different formulations).
Biogen further submitted that if the reference to a single chemical compound had been intended, i.e. dimethyl fumarate, then the claims would have been drafted accordingly, similar to claim 16.
In construing the omnibus claims, it is necessary to consider the context of “said one or more dialkyl fumarates”.
Claim 82 refers to “The use of one or more dialkyl fumarates for preparing a pharmaceutical preparation in the form of micro-tablets or micro-pellets”. The dialkyl fumarate is an ingredient for making the preparation and in this context is considered to refer to the compound per se. The dialkyl fumarate per se that is described in the examples is dimethyl fumarate. Thus, claim 82 defines the use of dimethyl fumarate for preparing a pharmaceutical preparation for the therapy of the specified disorders.
In claims 88, 91 and 92, the context of the words “one or more dialkyl fumarates” is such that the dialkyl fumarate defined by these claims is already in the form of micro-tablets or (micro)-pellets. Thus, the claims are considered to define methods or uses of dimethyl fumarate, wherein the compound is formulated as described with reference to the examples.
Conclusion on construction of claims 82, 88, 91 and 92
Claim 82 is considered to define a use wherein the dialkyl fumarate is dimethyl fumarate. Claims 88, 91 and 92 are considered to define methods or uses wherein the dialkyl fumarate is dimethyl fumarate and the compounds is formulated as described with reference to the examples.
Novelty
Under subsection 7(1), an invention is taken to be novel unless it is not novel in the light of the prior art base. Information in a document forms part of the prior art base for the purposes of novelty if it was published before the priority date of a claim, or the information was contained in a specification published after the priority date of the claim under consideration and, if that information is, or were to be, the subject of a claim of the specification, that claim has, or would have, a priority date earlier than that of the claim under consideration (referred to as “whole of contents” novelty).
It is well established that the general test for anticipation is the reverse infringement test. The classic formulation of this test is that given by Aicken J in Meyers Taylor Pty Ltd v Vicarr Industries Ltd [1977] HCA 19 at [20]; 137 CLR 228:
“The basic test for anticipation or want of novelty is the same as that for infringement and generally one can properly ask oneself whether the alleged anticipation would, if the patent were valid, constitute an infringement”.
This test is satisfied if the alleged anticipation discloses all the essential features of the invention claimed (Nicaro Holdings Pty Limited v Martin Engineering Company [1990] FCA 40 at [19]; 16 IPR 545). In order to meet this requirement, the prior art “must contain clear and unmistakeable directions to do what the patentee claims to have invented” (The General Tire & Rubber Company v The Firestone Tyre and Rubber Company Limited [1972] RPC 457 at 486).
In addition, in order to raise a “whole of contents” objection, it must be possible to draft a notional claim (assuming there is not an actual claim to the relevant subject matter) that is fairly based on the disclosure of the prior specification relied upon (Danisco A/S v Novozymes A/S (No 2) [2011] FCA 282; (2011) 91 IPR 209 at [178]).
AU 21593/99 (D1)
AU 21593/99 (D1) was published on 7 October 1999. This is after the priority date of the present claims (19 November 1998), however D1 contains information having an earlier priority date (31 March 1998). Consequently, D1 forms part of the prior art base as a “whole of contents” citation.
Biogen stated that if the claims are construed according to its submissions, then it follows that the claimed invention is novel in the light of D1. Biogen submitted that it is clear in this regard that D1 discloses the use of alkyl hydrogen fumarates as an essential part of the preparation.
Biogen further stated that even if the claims are construed so as to permit alkyl hydrogen fumarates to be included in the preparation as optional active ingredients in conjunction with the dialkyl fumarates, D1 does not provide a sufficiently clear disclosure for novelty purposes. It was submitted that D1 does not provide clear and unmistakeable directions to use a preparation that would necessarily fall within the scope of the present claims, since the use of dialkyl fumarates is expressed to be optional in D1. Biogen submitted that the information contained in D1 is not and could not be the subject of a valid claim which anticipates the present claims. In particular, D1 does not disclose a pharmaceutical preparation using one or more dialkyl fumarates as the sole active ingredient. Biogen indicated that the “information” disclosed in D1 is of a pharmaceutical composition that contains one or more alkyl hydrogen fumarates as the active ingredient, optionally in combination with a dialkyl fumarate.
Disclosure of D1
D1 relates to the use of alkyl hydrogen fumarates, either alone or in combination with a dialkyl fumarate, for preparing a pharmaceutical composition in the form of micro-tablets for treating psoriasis, psoriatic arthritis, neurodermatitis and enteritis regionalis Crohn (page 1, paragraph [1]).
The specification further indicates that the compositions may be in the form of micro-tablets or micro-pellets, wherein the total weight of the active ingredients is from 100 to 300 mg (page 3, paragraphs [1] and [3]). Thus, for example, the composition may contain 30.0 mg to 35.0 mg of dimethyl fumarate and 70 to 90 mg of methyl hydrogen fumarate (page 3, paragraph [4]), however other amounts are also contemplated (page 3, paragraph [5] and claim 5). It is noted, for example, that a composition containing 30.0 mg of dimethyl fumarate and 70 mg of methyl hydrogen fumarate corresponds to 86 mg of fumaric acid.
The micro-tablets or micro-pellets have a size of 300 to 2000 µm (page 4, paragraph [2]), may be encapsulated in gelatinous capsules (page 4, paragraph [3]) and may be provided with a coating resistant to gastric acid (enteric coating) (page 4, paragraph [3]).
I note that there is no preparative example of a composition containing a dialkyl fumarate and an alkyl hydrogen fumarate. D1 does refer to Fumaderm forte, which contains dimethyl fumarate and monoethyl fumarate (ethyl hydrogen fumarate), that is prepared in accordance to example 4 of EP 0 312 697 B1 (page 5, paragraph [4] to page 6, paragraph [1]). However, this preparation is not in the form of micro-tablets or micro-pellets (11.5 mm in diameter). Nevertheless, I am satisfied that having read D1, the skilled addressee would consider that it contains clear and unmistakeable directions to prepare a composition containing both a dialkyl fumarate and an alkyl hydrogen fumarate in the form of micro-tablets or micro-pellets.
As D1 is a “whole of contents” citation, I must further consider whether it is possible to draft a notional claim (assuming there is not an actual claim to the relevant subject matter) that is fairly based on the information disclosed in this document.
In practice, if the information disclosed is sufficient to support a novelty objection, it should follow that the information is sufficiently disclosed to allow the drafting of a valid claim, i.e. one that is fairly based. If I ask whether a valid claim could be drafted based on the information in D1 identified above, I am satisfied that this is the case.
I will now consider the novelty of the claims in view of the disclosure of D1.
Pharmaceutical preparation claims 13, 14, 16, 17, 40 and 41
D1 does not disclose a pharmaceutical preparation consisting of one or more dialkyl fumarates, and optionally carriers or excipients. Furthermore, the compositions of D1 contain alkyl hydrogen fumarates in amounts that are therapeutically effective. In contrast, the preparations of claims 13, 14, 16, 17, 40 and 41 do not contain alkyl hydrogen fumarates, other than in non‑therapeutically effective amounts that are breakdown products of the dialkyl fumarates formed during manufacture or shelf-life of the preparation. Claims 13, 14, 16, 17, 40 and 41 are therefore novel in light of D1.
Use claims 18, 23, 24, 25, 26 and 27 and “when used” claims 69, 74, 75, 76, 77 and 78
D1 discloses the use of alkyl hydrogen fumarates in combination with dialkyl fumarates for the preparation of compositions in the form of micro-tablets or micro-pellets, for the treatment of psoriasis, psoriatic arthritis, neurodermatitis and enteritis regionalis Crohn. As previously indicated, claims 18 and 69 permit the presence of other components in the preparation. Claims 18 and 69 therefore lack novelty in view of D1. The features of dependent claims 23, 24, 25, 26, 27, 74, 75, 76, 77 and 78 are disclosed in D1 as outlined above. Consequently these claims also lack novelty.
Method claims 42, 47, 48, 49, 50, 51, 64, 67 and 68
As previously indicated, claims 42 and 64 define methods of therapy or treatment, wherein the preparation administered during the therapy or treatment may contain other components in addition to the dialkyl fumarates. These claims lack novelty based on the disclosure of D1 as outlined above. Similarly, the features of dependent claims 47, 48, 49, 50, 51, 67 and 68 are described in D1 and consequently these claims lack novelty.
Omnibus claims 82, 88, 91 and 92
As indicated above, claim 82 permits the presence of other components in the preparation, and the claim is limited only in so far as the dialkyl fumarate is dimethyl fumarate. D1 discloses the use of dimethyl fumarate to prepare compositions in the form of micro-tablets or micro-pellets for the treatment of psoriasis, psoriatic arthritis, neurodermatitis and enteritis regionalis Crohn. Claim 82 is therefore not novel in view of D1.
Claims 88, 91 and 92 define methods or uses wherein the dialkyl fumarate is dimethyl fumarate and the compound is formulated as described with reference to the examples. D1 does not disclose such formulations and consequently claims 88, 91 and 92 are novel in light of this document.
Conclusion on novelty
Claims 18, 23, 24, 25, 26, 27, 42, 47, 48, 49, 50, 51, 64, 67, 68, 69, 74, 75, 76, 77, 78 and 82 are not novel in view of D1.
Conclusion
The “whole of contents” novelty objection was validly raised in the re-examination report. Claims 18, 23, 24, 25, 26, 27, 42, 47, 48, 49, 50, 51, 64, 67, 68, 69, 74, 75, 76, 77, 78 and 82 are not novel in view of D1. As this matter may be overcome by amendment, I allow Biogen a period of two months from the date of this decision to propose amendments.
Dr M-A. Fam
Delegate of the Commissioner of Patents
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