Apotex Pty Ltd v Warner Chilcott Company, LLC
[2016] APO 29
•23 May 2016
IP AUSTRALIA
AUSTRALIAN PATENT OFFICE
Apotex Pty Ltd v Warner Chilcott Company, LLC [2016] APO 29
Patent Application: 2011218625
Title:Dosage forms of risedronate
Patent Applicant: Warner Chilcott Company, LLC
Opponent: Apotex Pty Ltd
Delegate: K. Wagg
Decision Date: 23 May 2016
Hearing Date: 1 March 2016
Catchwords: PATENTS – Opposition unsuccessful–claims are novel and inventive because the cited prior art teaches away from the opposed claims–Costs awarded against the opponent.
Representation: Patent Applicant: Ben Fitzpatrick of Counsel instructed by David Miles and Bernard Nutt of Pizzeys
Opponent:Craig Smith of Counsel instructed by James Cherry and Sarah Hennebry of Freehills
IP AUSTRALIA
AUSTRALIAN PATENT OFFICE
Patent Application: 2011218625
Title:Dosage forms of risedronate
Patent Applicant: Warner Chilcott Company, LLC
Date of Decision: 23 May 2016
DECISION
The opposition fails.
Subject to appeal, patent applicant number 2011218625 is to proceed to grant.
I award costs according to Schedule 8 against Apotex Pty Ltd.
REASONS FOR DECISION
Patent application number 2011218625 (the opposed application) was filed on 29 August 2011. It is a divisional of application number 2005330654 (the parent application), now withdrawn. The Applicant is Warner Chilcott Company, LLC (the Applicant). The application was examined by the Commissioner and acceptance was advertised on 20 March 2014. On 20 June 2014, Apotex Pty Ltd (the Opponent) filed a Notice of Opposition.
A hearing was held on 1 March 2016 in Canberra to decide the opposition. The Applicant was represented by Ben Fitzpatrick of Counsel instructed by David Miles and Bernard Nutt of Pizzeys. The Opponent was represented by Craig Smith of Counsel instructed by James Cherry and Sarah Hennebry of Freehills.
The request for examination was filed prior to 15 April 2013. As a consequence, substantive amendments of the Patents Act 1990 brought about by the Intellectual Property Laws Amendment (Raising the Bar) Act 2012 do not apply to the present patent application. This includes the amendment to subsection 60 (3A) that allows the Commissioner to refuse a patent application if satisfied on the balance of probabilities that a ground of opposition exists. I also note that any subsequent reference to the Patents Act relates to the Patents Act1990 (the Act), prior to amendment by the Intellectual Property Laws Amendment (Raising the Bar) Act 2012.
Standard of proof
The onus of proof in this opposition proceeding rests with the Opponent, who must demonstrate that it is clear that a valid patent cannot be granted (F.Hoffman-La Roche AG v New England Biolabs Inc [2000] FCA 283 at [67]; 50 IPR 305; Commissioner of Patents v Sherman [2008] FCAFC 182 at [18]; 79 IPR 426).
The opposition
The Statement of Grounds and Particulars identified seven grounds of opposition. At the hearing, the opposition was limited to the grounds of novelty and inventive step.
The parties relied upon evidence by several declarants. Evidence in support is as follows:
Evidence in Support Date of declaration Declarant Annexes Abbreviation 23 October 2014 Robert William Milne RM-1 to RM-3 Milne #1 16 December 2014 Robert William Milne Milne #2 11 December 2014 Brett Antony Mooney BAM-1 to BAM-3 Mooney #1 16 December 2014 Brett Antony Mooney BAM-4 to BAM-8 Mooney #2 17 December 2014 Sarah Catherine Hennebry SCH-1 to SCH-2 Hennebry #1 17 December 2014 Sarah Catherine Hennebry SCH-3 to SCH-33 Hennebry #2
Evidence from the opposition on the parent application 2005330654 has been filed as exhibits annexed to declarations filed on this opposition. I have listed them in the table below.
Annexure Date of declaration Declarant Annexes Abbreviation RM-1 20 December 2012 Robert William Milne RWM-1 to RWM-2 Milne #1A RM-2 26 August 2013 Robert William Milne RWM-3 to RWM-8 Milne #1B RM-3 16 September 2013 Robert William Milne RWM-9 to RWM-10 Milne #1C SCH-1 29 July 2013 Jeffrey David Zajac JDZ-1 to JDZ-9 Zajac SCH-2 11 September 2013 Sarah Catherine Hennebry SCH-49 to SCH-53 Hennebry #1A The Applicant responded with the following Evidence in Answer:
Evidence in Answer Date of declaration Declarant Annexes Abbreviation 18 May 2015 Hans Junginger HJ-1 to HJ-46 Junginger #1 The Opponent then filed the following Evidence in Reply:
Evidence in Reply Date of declaration Declarant Annexes Abbreviation 21 July 2015 Robert William Milne Milne #3 21 July 2015 Brett Antony Mooney BAM-9 to BAM-10 Mooney #3 Further information
The Notice of Opposition was filed on 20 June 2014, so Chapter 5 of the Regulations is amended by the Intellectual Property Legislation Amendments (Raising the Bar) Regulation 2013 (No. 1). As a consequence, the further evidence provisions of the former Reg 5.10(4) are no longer available.
Regulation 5.23 of the Regulations as amended allows the Commissioner discretion to consult documents. Consideration of when this discretion can be exercised occurred in Merial Limited v Bayer Intellectual Property GmbH [2015] APO 16 where the Delegate concluded:
“I conclude that a decision under regulation 5.23 must have regard to the nature of the information and whether the information is likely, if not certain, to change the outcome of the opposition in a significant way.”
The Applicant had sought to bring in the following declaration under the reg 5.23 as they felt some of the Evidence in Reply was new evidence:
Date of declaration Declarant Annexes Abbreviation 18 August 2015 Hans Junginger HJ-47 to HJ-54 Junginger #2
At the beginning of the hearing the matter was discussed. The discussion did not provide me with clear reasons as to why the material would be determinative on any particular ground. It was decided to continue the hearing to see if anything arose that would alter this conclusion.
I have reached the conclusion that the information the Applicant had considered was not Evidence in Reply is not been determinative on any particular ground of opposition. The new information is thus not significant to the opposition. I will not exercise the discretion under reg 5.23.
The specification
The specification relates to oral dosage forms of risedronate, a compound that is known for the treatment of conditions involving abnormal calcium and phosphate metabolism. The specification ends with 39 claims. Claims 1 and 28 are independent.
What is the invention as described
Before commencing to construe the specification, I note what Middleton J said in Eli Lilly and Company Limited v Apotex Pty Ltd [2013] FCA 214, 100 IPR 451 at [139]:
"It is well settled that the Court should, from the outset, approach the task of patent construction with a generous measure of common sense. The Court must place itself in the position of a person skilled in the relevant art, being the subject matter of the patent. From this perspective, the patent is to be read as a whole, in the context of the specification and in light of the prevailing common general knowledge and state of the relevant art at the priority date."
The background to the invention
The Specification begins by introducing bisphosphonates generally by stating on page 1 at lines 26-29 that:
“Bisphosphonates were first developed to complex calcium in hard water to improve detergent performance. Bisphosphonates have since been found to be useful in the treatment and prevention of diseases or conditions characterised by abnormal calcium and phosphate metabolism.”
An example of a disease associated with abnormal calcium and phosphate metabolism is osteoporosis (page 2). Bisphosphonates act by inhibiting resorption of bone tissue (page 2 line 21).
Examples of bisphosphates used in treatment are given on page 2 and these include risedronate and alendronate (line 29).
Patient complaints associated with bisphosphonate are then discussed on page 2 lines 30-33. These include heartburn, esophageal burning, pain and/or difficulty upon swallowing, and/or pain existing behind and/or mid-sternum. The specification then states that:
“In order to avoid potential upper gastrointestinal irritation, patients taking bisphosphonates are instructed to take their medication with a full glass of water, and to remain upright for at least thirty minutes after taking an oral dose of a bisphosphonate.”
The specification continues with further issues with bisphosphonate administration. Importantly, that oral doses of bisphosphonates are poorly absorbed (page 3 line 3). The specification then discusses other approaches to this issue of absorption, such as modifying the permeability of the intestinal mucosa, and tells the reader that the use of EDTA has been proposed but previously thought impossible in the light of the effects of EDTA on mucosal integrity and the high amount required (page 3).
The specification then states that the primary site of absorption is the small intestine (page 3 line 20). The specification then introduces the drug risedronate and alendronate as being approved by a number of regulatory agencies for the treatment of various bone pathologies (page 3, lines 29-30) but then further states a possible reason for the low absorption (at page 3 lines 30-33):
“…interactions between bisphosphonate and foods and minerals (especially cations like calcium, magnesium, aluminium, and iron-containing foods or supplements) cause less of the bisphosphonate to be available for absorption”.
The specification goes on to state that (page 3, line 34 to page 4 line 9):
“.. it was [previously] demonstrated that administration of risedronate within 30 minutes of a meal reduced the amount absorbed by 50% compared to administration in the fasting state. In order to reduce this food effect, the labelling of oral bisphosphonate products instructs patients to take their medication at least thirty minutes … before the first food of the day, and are instructed to take their calcium suppliments at another time of the day, or on a day when they are not taking an oral dose of a bisphosphonate. These dosing instructions can seem complex and inconvenient to the patient, which can lead to poor patient compliance.”
There was agreement in the submissions and in evidence from both parties that risedronate in the previously FDA approved oral dose forms has:
- gastrointestinal side effects;
- is poorly absorbed; and
- patients are instructed to take it on an empty stomach because of poor absorption.
The aim of the invention
The aim of the inventive can be gleaned from the specification at lines 10-13:
“There is an ongoing need to develop an oral dosage form of a bisphosphonate which can be taken with or without food or beverages (i.e. has pharmaceutically effective absorption regardless of food or beverage intake), at the preference of the patient, and which does not produce upper gastrointestinal irritation”.
The nature of the invention
At lines 14 through to lines 25 on page 3 the specification states:
“It has been found that a pharmaceutical composition containing risedronate, a sufficient amount of chelating agent to bind the ions and minerals in food, and a means for effecting delayed release of risedronate and the chelating agent in the small intesting is useful in providing an oral dosage form which provides immediate release of risedronate to the small intestine, as well as pharmaceutically effecting absorption of risedronate when administered with or without food or beverages.
The summary of the invention on page 4 breaks it down to a pharmaceutical composition comprising three features:
1.from about 1 mg to about 250 mg risedronate;
2.from about 10 mg to about 970 mg of a chelating agent; and
3.a delayed release mechanism to immediately release the risedronate and the chelating agent in the small intestine; wherein such composition is a tablet size of no greater than one gram.
The Claims
The correct approach to the construction of claims was discussed by Bennett J in H Lundbeck A/S v Alphapharm Pty Ltd [2009] FCAFC 70, 81 IPR 228 at [118] – [120]:
"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 … terms in the claim which are unclear may be defined or clarified by reference to the body of the specification"
Claim 1 and 28 are the independent claims. Claim 1 reads:
“1. An oral dosage form comprising:
(a) about 35 mg of a risedronate salt;
(b) about 100 mg of EDTA or a pharmaceutically acceptable salt thereof; and
(c) a delayed release mechanism to deliver the risedronate salt and EDTA or pharmaceutically acceptable salt thereof to the lower gastrointestinal tract.”Claim 28 reads:
“28. An oral dosage form comprising:
(a) about 150 mg of a bisphosphonate selected from the group consisting of a risedronate and salt thereof;
(b) from about 55 mg to about 500 mg of ethylenendiaminetetraacetic acid (EDTA) or a pharmaceutically acceptable salt thereof; and
(c) a delayed release mechanism to deliver the risedronate and the EDTA in the lower gastrointestinal tract.”Claims 2-27 are dependent on claim 1 and claims 29-39 are dependent on claim 28. These claims introduce various limitations.
Both claim 1 and claim 28 are for oral administration and they differ in the amounts of risedronate and EDTA. Evidence showed that 35 mg of risedronate would be a weekly dose (Zagac at paragraph 29) and 150 mg would be a monthly dose.
The delayed release feature is taken to mean that the risedronate and EDTA is held in the formulation until it reaches the small intestine. This is different to a slow release or instantaneous release.
The Person Skilled in the Art
It is well established that many of the issues in an opposition are answered by reference to the person skilled in the art (PSA):
"He is the person to whom the patent is addressed and who must construe it. He is the person whose knowledge will determine whether a patent is novel. He is the person who will judge whether a patent is obvious."
(Root Quality Pty Ltd v Root Control Technologies Pty Ltd [2000] FCA 980 at [70])The PSA is an artificial construct that is used as a tool of analysis, and there is a danger in trying to identify them as an actual person or persons:
"The notional person is not an avatar for expert witnesses whose testimony is accepted by the court. It is a pale shadow of a real person – a tool of analysis which guides the court in determining, by reference to expert and other evidence, whether an invention as claimed does not involve an inventive step."
AstraZeneca AB v Apotex Pty Ltd [2015] HCA 30 at [23]Our understanding of the person skilled in the art is based on evidence from persons with knowledge of the art as to the things that they know and do, and what they understand to be commonly known and done. The weighting and evaluating of this evidence to decide the characteristics of the person skilled in the art is part of the normal work of a delegate of the Commissioner.
The parties agreed that the person skilled in the art would be a team which includes knowledge and skill of the following fields:
·Medical practice-providing knowledge of bisphosphonates including risedronate for the treatment of metabolic bone disorders
·Pharmacokinetics-providing knowledge of drug absorption
·Formulation science-providing knowledge of formulating pharmaceuticals to meet pharmacokinetic requirements.
Novelty
It is a requirement of subsection 18(1) of the Patents Act (the Act) that the invention, so far as claimed in any claim, is novel. Subsection 7(1) states that an invention is taken to be novel unless it is not novel in the light of the prior art. A citation is part of the prior art base for the purposes of novelty if it was published before the priority date of the claim.
It is well established that the general test for lack of novelty is the reverse infringement test. The classic formulation of this test is that given by Aickin J in Meyers Taylor Pty Ltd v Vicarr Industries Ltd [1977] HCA 19 at [20], 137 CLR 228 at 235:
"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 as claimed (see Nicaro Holdings Pty Ltd v Martin Engineering Co (1990) 91 ALR 513 at 517). 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).
Australian courts have often cited with approval the words of the UK Court of Appeal in The General Tire & Rubber Company v The Firestone Tyre and Rubber Company Limited [1972] RPC 457 (the General Tire case) at 485 – 486:
"If the prior inventor's publication contains a clear description of, or clear instructions to do or make, something that would infringe the patentee’s claim if carried out after the grant of the patentee's patent, the patentee's claim will have been shown to lack the necessary novelty, that is to say, it will have been anticipated. The prior inventor, however, and the patentee may have approached the same device from different starting points and may for this reason, or it may be for other reasons, have so described their devices that it cannot be immediately discerned from a reading of the language which they have respectively used that they have discovered in truth the same device; but if carrying out the directions contained in the prior inventor's publication will inevitably result in something being made or done which, if the patentee's patent were valid, would constitute an infringement of the patentee's claim, this circumstance demonstrates that the patentee's claim has in fact been anticipated.
If, on the other hand, the prior publication contains a direction which is capable of being carried out in a manner which would infringe the patentee's claim, but would be at least as likely to be carried out in a way which would not do so, the patentee's claim will not have been anticipated, although it may fail on the ground of obviousness. To anticipate the patentee's claim the prior publication must contain clear and unmistakeable directions to do what the patentee claims to have invented: Flour Oxidizing Co. Ltd. v. Carr & Co. Ltd. (1908) 25 R.P.C. 428 at 457, line 34, approved in B.T.H. Co. Ltd. v. Metropolitan Vickers Electrical Co. Ltd. (1928) 45 R.P.C. 1 at 24, line 1). A signpost, however clear, upon the road to the patentee's invention will not suffice. The prior inventor must be clearly shown to have planted his flag at the precise destination before the patentee."
The Opponent relied on a single document:
BR 0106601-3 A (LIBBS PHARMCEUTICAL COMPANY LTDA.) 21 December 2001 (BR ‘601)
BR’601 was filed in evidence as RWM-9. It was published before the priority date of the opposed applicant and therefore is part of the prior art base.
Disclosure of BR ‘601
BR ‘601 is entitled:
“Pharmaceutical composition containing bisphosphonate for the treatment of diseases related to calcium and/or phosphate metabolism, its use in the preparation of medication to treat diseases related to calcium and/or phosphate metabolism, and method for treating diseases related to calcium and/or phosphate metabolism”
The document introduces bisphosphonates and mentions risedronate as an example of one on page 2. It then discusses the issue of bioavailability stating that the low bioavailability:
“…necessitates the use of high doses of the drugs in relation to the quantity actually absorbed by the body, with the disadvantage of undesirable exposure of the body to the excess quantity of the drug, the cost involved in the overdose, and the size of the dosage unit.”
On page 3 of the document then introduces the use of chelating agents in the context of the low absorption of bisphosphonates:
“Among the various solutions present in the current state of the art, in terms of scientific evidence, the use of chelating agents stands out.”
The document then mentions an article on EDTA but notes that that article concludes that EDTA would not be effective because it requires a high dose of 100 mg/kg of body weight.
The document then states the following:
“This invention solves the problem encountered in the current state of the art in presenting an innovative technique in which the chelating agent becomes available only in the small intestine, which is the principal site of bisphosphonate absorption.
The purpose of targeting the release of chelating agents into the small intestine is to eliminate the interaction of these agents with the contents of the stomach.
Without limiting the scope of the invention at this point it is of particular interest to approach the possible mechanisms involved in increasing the absorption of bisphosphonate by the action of chelating agents a) reduction of the formation/solubilisation of insoluble complexes of bivalent ions with bisphosphonates, and b) increase in permeability of the intestinal mucosa. Both mechanisms appear to derive from the ability of chelating agents to sequester bivalent ions such as calcium and magnesium and to form highly stable complexes.”The document then states that the contents of the stomach also contains calcium and magnesium ions and this calcium and magnesium consumes the chelating agent and compromises absorption by concluding that:
“This being the case, release of chelating agent only into the small intestine permits a reduction in the dosage administered for the desired result, which is increased absorption of the bisphosphonate.”
The document goes on to state that there are at least three ways the cores of the composition can be made, with one of them being:
“bisphosphonate and chelating agent are contained in a single same core”
Example of BR ‘601
BR ‘601 only provides the PSA with one worked example. This example uses sodium alendronate, which is another bisphosphonate drug related to risedronate. The example produces cores of sodium alendronate and EDTA and then coats them with an enteric coating to provide a multigranular product with an enteric coating. This enteric coating provides for the delayed release.
The cores are made on a large scale using 6.0 kg of sodium aldendronate and 6 kg disodium EDTA. An individual dose unit is not produced.
In Junginger #1 at paragraph 101 the declarant tells me that:
“Because the molecular weight of disodium EDTA dehydrate is about 372 g/mol, whereas the form of alendronate specified (sodium alendronate trihydrate … has a molecular weight of about 325 g/mol, there are fewer moles of EDTA than moles of alendronate.”
Risdronate in BR ‘601
The current claims require that the bisphosphonate be risedronate. The disclosure of BR ‘601 is directed towards bisphosphonates generally. On page 5 it provides a general formula of bisphosphonates and provides examples. Risedronate is noted on page 6, first line.
In Milne #1C at paragraph 12 the declarant reads these as suitable bisphosphonates and notes that the more commonly known bisphosphonates alendronate, ibandronate and risedronate are specifically mentioned and also notices them in claim 11.
Given that risedronate was noticeable to the declarant and in light of the general nature of the disclosure about bisphosphonates, I consider that the use of risedronate in the formulation of BR ‘601 is clear to the person skilled in the art.
Dosage in BR ‘601
The claims require that the dosage of risedronate be either about 35 mg or about 150 mg and the chelating agent be EDTA in an amount of about 100 mg and from about 55 mg to about 500 mg.
Junginger states in Junginger #1 at paragraph 100 that:
“…there is no disclosure of a 35 mg or 150 mg dose of risedronate in BR ‘601, nor is there a disclosure of any dose of risedronate added to any dose of EDTA, let alone 100 mg.”
BR ‘601 teaches broad ranges for the dosage of bisphosphonate. These ranges do encompass the dosages of the opposed application. On page 7, second last paragraph, BR ‘601 states:
“…the compositions for this use include an effective quantity of the pharmaceutical compositions described above (for example, between 1 and 150 mg of bisphosphonate for each ingestion, or about 0.01 to 2.15 mg per kg of body weight), at regular intervals (for example, daily or weekly).”
This range is again repeated in the first paragraph of page 8.
The dosage of EDTA used BR ‘601 was discussed at length in the evidence, the document itself states on page 6:
“the proportion between the quantities of chelating agent and bisphosphonate is greater than 10% mol/mol, particularly higher than 50% mol/mol. It is preferable but not exclusively preferable for the daily intake of chelating agent, particularly EDTA, not to exceed about 175 mg.”
Junginger #1 states that BR ‘601 does not disclose an EDTA ratio greater than 100%.
In Zajac at paragraph 29 I am told that once a week administration of 35 mg of risedronate was available in Australia in 2002. It was discussed in the hearing that 150 mg would correspond to a monthly dose. The main driver for decreasing the frequency of administration was to improve patient compliance (Zajac at paragraph 30).
Given this information from Zajac I am then faced with the following question:
Would the person skilled in the art use the standard weekly dose or a monthly dose of risedronate in the composition of BR ‘601?
In response to this question BR ‘601 states on page 4:
“…with this invention we obtain an effective treatment with a small quantity of bisphosphonate compared to the current treatment by its association with a chelating agent, and in lower quantities than those already studied in the state of the art.” (my emphasis)
In view of the above passage, BR ‘601 directs the reader to use a small quantity of bisphosphonate compared to the current treatment and in lower quantities than those studied. Given that 35 mg and 150 mg of risedronate are the current treatment (Zajac, paragraph 29), BR ‘601 teaches the reader to use amounts less than these and therefore below the scope of the current claims.
In this case the bullet has struck below the target and is not fatal; the anticipation lacks the “accuracy of a sniper” (ICI Chemicals & Polymers Ltd v The Lubrizol Corporation Inc [2000] FCA 1349 at [51]).
Consequently, BR ‘601 does not provide clear and unmistakable directions to the claims of the opposed application and this ground of opposition is unsuccessful.
Inventive step
It is a requirement of subsection 18(1) of the Act that the invention, so far as claimed in any claim, involves an inventive step. Subsection 7(2) states that an invention is taken to involve an inventive step unless it would have been obvious to a person skilled in the art in the light of the common general knowledge, considered alone or together with the prior art. A document is prior art for this purpose if "a skilled person mentioned in subsection (2) could, before the priority date of the relevant claim, be reasonably expected to have ascertained, understood, regarded [the document] as relevant" (subsection 7(3)).
The test for whether an invention is obvious is to ask whether it would have been a matter of routine to proceed to the claimed invention. In Wellcome Foundation Ltd v V.R. Laboratories (Aust.) Pty Ltd [1981] HCA 12 at [45], 148 CLR 262 at 286 Aickin J stated:
"The test is whether the hypothetical addressee faced with the same problem would have taken as a matter of routine whatever steps might have led from the prior art to the invention, whether they be the steps of the inventor or not."
The High Court in Aktiebolaget Hassle v Alphapharm Pty Ltd [2002] HCA 59, 212 CLR 411 approved this approach.
In the current case the problem lies with the immediate release forms of risedronate which were available in Australia at the priority in daily and weekly dosages, with the weekly dose being 35 mg (Zajac, at paragraph 29).
The problem identified by the Opponent’s declarant Zajac at paragraphs 16-19 are also found in the specification:
- Risedronate is poorly absorbed (page 3, line 1)
- Risedronate could not be taken with food (page 3, lines 33 to page 4, line 9)
- Risedronate causes upper gastrointestinal (esophageal) irritation (page 2, lines 30-33)
The Applicant sought the limit the problem to the issue of food. However, the food issue is linked to the issue of absorption (Junginger #1, paragraph 13). I therefore accept that all three points identified above were a problem known to the PSA and is the problem addressed by the opposed application.
The Opponent argued that the document, BR ‘601 (cited above under novelty), deprived the current claims of inventive step when combined with common general knowledge of risedronate and enteric coatings.
The threshold question to cite BR ‘601 for inventive step is whether it would have been ascertained, understood and regarded as relevant by the PSA.
In regards to whether it would be understood, it is clear that pharmaceutical formulations are often the subject of patents and this is reflected by the evidence of the declarants who clearly understood patents. In view of this I accept that BR ‘601 would have been understood.
The Opponent provided evidence in Hennebry #1A of a search conducted by the declarant using keywords of “bisphosphonates” and “medication” in the Thomson Innovation database. This search gave 9 results and BR ‘601 was the seventh. The Applicant did not challenge this evidence. In view of this I accept that BR ‘601 would have been ascertained.
The relevance of the title of BR ‘601 to the current problem is clear. It discusses bisphosphonate compositions and the problem of poor absorption (page 2), the contents of the stomach (page 3) and “discomfort caused when the acid form of the bisphosphonate comes into contact directly with the gastroesophageal mucosa” (page 4, last line).
In view of this I accept that BR ‘601 would be ascertained, understood and regarded as relevant.
BR’601 provides a bisphosphonate composition with a chelating agent and a delayed release system (see page 3).
I accept that the references to risedronate in BR ‘601 (see above paragraphs 53-55) give direction to use risedronate as the bisphosphonate in the formulation of the example. The example does also use EDTA as the chelating agent. However, the dosages are not specified.
I also accept the evidence in Zajac at paragraph 29 on the dosage forms available in Australia of risedronate included a weekly dose of 35 mg. I consider that this would also be common general knowledge because it was available on the market and would be known the PSA given that the PSA includes knowledge of medical practice (see paragraph 36 above).
In Mooney #2 he states that if he was seeking to add EDTA to a formulation of risedronate he would start with the weekly dose (paragraph 100) but this is in light of the common general knowledge alone and not when he is combining it with the teaching of BR ‘601.
Working with the disclosure of BR ‘601 and the CGK of the dosage of risedronate would the person skilled in the art be directly led as a matter of routine to use the current dose of risedronate in a formulation of BR ‘601?
Because BR ‘601 optimises absorption, the dosage required is lower. As I mentioned above BR ‘601 has the following passages on page 4:
“…with this invention we obtain an effective treatment with a small quantity of bisphosphonate compared to the current treatment by its association with a chelating agent, and in lower quantities than those already studied in the state of the art.” (my emphasis)”
Therefore in order to arrive at the current claims, the person skilled in the art would have to disregard the above passage, or identify that a current dose of 35 mg could be given in the formulation of BR ‘601.
I do not have evidence before me that demonstrates that it would be a matter of routine to do something that BR ‘601 teaches away from, and use the standard dose of risedronate.
The evidence focuses on the effect of food, with Milne #1C saying at paragraph 36:
“the dosage form discussed in the Brazilian patent application could also provide pharmaceutically effective absorption, even in the presence of food.”
On the other hand, Junginger #1 at paragraph 92 says that there is no mention of “fed or fasted state” or “food studies”.
I do not need to decide this point, since the evidence of Milne does not give me reasons why the PSA would use the dose of 35 mg or 150 mg in view of BR ‘601.
In view of this this ground of opposition is unsuccessful.
Conclusion
The opposition is not successful. Subject to appeal, patent applicant number 2011218625 is to proceed to grant.
Costs
The parties submitted that costs should follow the event. I see no reason to depart from that result. Costs are awarded against the Opponent.
K. Wagg
Delegate of the Commissioner of Patents
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