Kineta, Inc.
[2017] APO 45
•31 August 2017
IP AUSTRALIA
AUSTRALIAN PATENT OFFICE
Kineta, Inc. [2017] APO 45
Patent Application: 2012315953
Title:Anti-viral compounds
Patent Applicant: Kineta, Inc.
Hearing Officer: Dr S.D. Barker – Deputy Commissioner of Patents
Decision Date: 31 August 2017
Hearing Date: Written submissions completed on 17 August 2017
Catchwords: PATENTS – examiner objection – best method of performance – compounds prepared by contractor, but this was not disclosed in the specification – best method not provided
Representation: Patent attorney for the applicant: Griffith Hack
IP AUSTRALIA
AUSTRALIAN PATENT OFFICE
Patent Application: 2012315953
Title:Anti-viral compounds
Patent Applicant: Kineta, Inc.
Date of Decision: 31 August 2017
DECISION
The ground of objection of lack of a best method of performance is properly raised.
I allow the applicant the time remaining for acceptance in order to attempt to overcome the objection.
Pursuant to regulation 13.4 the present application will not lapse until 3 months from the date of this decision.
REASONS FOR DECISION
Patent application 2012315953 was filed by Kineta, Inc. (the applicant) on 27 September 2012. A first examination report issued on 29 July 2016 raising the grounds of clear enough and complete enough disclosure, novelty and inventive step. Amendments were filed on 2 December 2016, and a second examination report issued on 10 January 2017 maintaining the ground of clear enough and complete enough disclosure. A response was filed on 28 March 2017. A third examination report issued on 12 April 2017 raising the objection of failure to disclose a best method of performance. That objection has been maintained in a fourth and fifth report. The applicant has asked to be heard in relation to the outstanding objection. The matter was heard on the basis of written submissions, which were filed on 10 August 2017.
The relevant law
The examination of the present application is governed by the Patents Act 1990 (the Act) as amended by the Intellectual Property Laws Amendment (Raising the Bar) Act 2012 (the Raising the Bar Act). Amendments to sections 40 and 49 of the Act apply to the present case as a consequence of Schedule 1, items 55(1)(e) and 55(4)(b) of the Raising the Bar Act – the application was made before 15 April 2013 but the applicant did not ask for examination of the patent request and specification for the application until 8 February 2016.
The standard of proof that applies to the examination of the present application is the balance of probabilities – I must accept the present application if satisfied on the balance of probabilities that the application complies with the Act.[1] If I am not so satisfied, then I can refuse the application.[2]
[1] Section 49 of the Act as amended.
[2] Explanatory Memorandum, Intellectual Property Laws Amendment (Raising the Bar) Bill 2011 at page 54.
THE SPECIFICATION
The specification as filed states that the field of the invention is:
"Compounds and methods disclosed herein are useful for treating viral infection in vertebrates, including RNA viral infections."[3]
[3] The application at page 1.
The compounds and methods of the specification are directed at enhancing the host's antiviral response:
"The compounds and methods disclosed herein shift the focus of viral drug development away from the targeting of viral proteins to the development of drugs that target and enhance the host's innate antiviral response. Such compounds and methods are likely to be more effective, less susceptible to the emergence of viral resistance, cause fewer side effects and be effective against a range of different viruses."[4]
[4] The application at page 7.
The description then discloses the invention in general terms:
"The RIG-I pathway is intimately involved in regulating the innate immune response to RNA virus infections. RIG-I is a cytosolic pathogen recognition receptor that is essential for triggering immunity to a wide range of RNA viruses. … A high-throughput screening approach was used to identify compounds that modulate the RIG-I pathway, a key regulator of the cellular innate immune response to RNA virus infection. In particular embodiments, validated RIG-I agonist lead compounds were demonstrated to specifically activate interferon regulatory factor-3 (IRF-3). … As discussed below, these compounds represent a new class of potential antiviral therapeutics. Although the disclosure is not bound by a specific mechanism of action of the compounds in vivo, the compounds are selected for their modulation of the RIG-I pathway. … In one embodiment, the disclosure herein relates to a class of compounds of [sic] "represented by the following formula:
"[5]
[5] The application at pages 7 – 9.
Various more specific embodiments are described by reference to the variables. The specification does not include a generic description of how to produce the compounds.
The examples
The specification has the heading "EXAMPLES" on page 38. This section begins with the following text:
"The Examples below describe the antiviral and pharmacological properties of the disclosed compounds. The Examples are included to demonstrate particular embodiments of the disclosure. It should be appreciated by those of ordinary skill in the art that the techniques disclosed in the Examples represent techniques and compositions discovered by the inventors to function well in the practice of the disclosure, and thus can be considered to constitute preferred modes for its practice. However, those of ordinary skill in the art should, in light of the present disclosure, appreciate that many changes can be made in the specific embodiments which are disclosed and still obtain a like or similar result without departing from the spirit and scope of the disclosure."
All that needs to be said about the Examples is that they proceed from the point that various compounds designated KIN1000 and KIN1148 (several others are listed in Table 3) are available and are tested for their biological activity. The Examples do not suggest how any of the compounds can be prepared or obtained.
The claims
10. Claim 1 as proposed to be amended is directed to a compound represented by the formula:
11. For the purposes of this decision it is not necessary to consider the definition of the variables R1, R5, R16, R17 and R18. Later claims are appended to claim 1 and directed to pharmaceutical compositions comprising the compound and methods of treatment comprising administering the composition.
THE GROUND OF OBJECTION
12. The single ground of objection is best method of performance. The latest examination report states:
"Objection 5 of the fourth report is maintained: the present application does not satisfy the requirements of sec 40(2)(aa) requiring a best method of performing the invention be disclosed in the specification as filed.
In your response you have stated that there is no evidence that there were methods known to the applicant at filing that were not included in the specification. However, the specification itself demonstrates that the applicant had the compounds of invention in your possession and tested them for activity. As such it is readily apparent that the applicant has synthesised these compounds (or otherwise obtained them) and has not stated at least one method of doing so, which is the requirement of sec 40(2)(aa) of the Patents Act 1990.
The other points you have raised which discuss decisions of the Federal Court only further support the best method of performing the invention needs to be included in the specification at the filing date. Given that the present specification does not include a worked example or generic scheme showing how the present compounds can be made (or otherwise obtained) the only conclusion that can be drawn is that the application fails to satisfy the requirements of sec 40(2)(aa)."
THE GOLDBERG DECLARATIONS
13. During prosecution of the application the applicant provided two declarations by Dr Goldberg. Dr Goldberg is a Director of Discovery Research at Kineta, Inc., and an internationally recognised expert in medicinal chemistry and drug discovery.[6] Dr Goldberg sets out what he has been told is the definition of common general knowledge (being the well-known words of Emmett J in ICI Chemicals & Polymers Ltd v Lubrizol Corporation Inc[7]), and then goes on to say:
"With the above in mind, it is my experience that compounds of the nature of those claimed in the application can be synthesized as follows:
Step 1: Synthesis of benzo-bisthiazole core can be accomplished as described in the literature:
(a) 2-chloro-5-nitroaniline in the presence of formic acid, followed by disodium sulphide reduction to 1,3-benzothiazol-5-amine; see Kasimogullari, R. et al., Bioorg Med Chem, 17(9), 2009, 3295-3301;
(b) Cyclisation with NBS or bromine in the presence of, for example, 3-(naphthalene-2-yl)prop-1-ene-1,3-dithione; see Elmore, C.S. et al., J Label Comp and Radiopharm, 52(9), 2012, 359-365; and
(c) Alternatively, the last cyclization to the benzo-bisthiazole can be accomplished with thiocyanic acid and bromine, see: Alanine, A, et al., WO 2001097786"[8]
[6] First Goldberg declaration at [1] and [3].
[7] [1999] FCA 345; 45 IPR 577 at [112].
[8] First Goldberg declaration at [7].
14. Prior to the hearing I wrote to the applicant and asked them to address several specific issues coming out of Dr Goldberg's evience:
"While not seeking to limit the submissions you make, from a reading of the file I have identified several questions. The applicant's case relies upon the declarations of Dr Goldberg. To ensure that I properly understand the evidence of Dr Goldberg, it would be helpful if you could include submissions on the following matters.
1. The method of preparation that comes to Dr Goldberg's mind has one step to prepare the benzo-bisthiazole nucleus. Are there are further steps to link the nucleus to the amide side chain, but these are regarded as straight forward after the nucleus has been prepared? Or is it envisaged that the amide side chain is already present during the synthesis? Put another way, does Dr Goldberg consider there should be a step 2?
2. Sub step (a) is the formation of a 1,3-benzothiazol-5-amine from 2-chloro-5-nitroaniline following the method of Kasimogullari. The article is relevant to the reduction of the nitro to an amine, but is it also relevant to the formation of the benzothiazole nucleus?
3. Sub step (b) is the formation of the second thiazole ring. Presumably Dr Goldberg is implying that the amine is first reacted with benzoylisothiocyanate and then cyclised using NBS following the method of Elmore. The desired cyclisation product (as set out in claim 1) is the bent isomer (analogous to compound 8b in the article) which is the minor product compared to the straight isomer (analogous to compound 8 in the article). Is Dr Goldberg asserting that in the case of the present application the major isomer would be the bent isomer, or that the desired compound is the minor isomer? Would the person skilled in the art understand the specification to be instructing them to follow a process where the desired compound is the minor product?
4. Sub step (c) is the formation of the second thiazole ring in a different way, following the method of Alanine. This method involves the use of thiocyanic acid. Dr Goldberg does not indicate which page(s) of this lengthy document he considers are relevant. Since it is not immediately obvious to me which pages are relevant, it would help if you could identify them.
5. On the assumption that KIN1000 is likely to be the compound of most interest, it is not apparent to me how any of the methods identified by Dr Goldberg could produce this compound. In KIN1000 R18 is methyl and R1 is 3-bromophenyl. In particular, my question relates to the introduction of the methyl group into the R18 position - although this may be resolved by your answer to question 2."
15. Dr Goldberg helpfully provided a response to these questions, which was filed on 17 August 2017. That response established that:
- the side chain is introduced in a subsequent step;
- the Kasimogullari article is only relevant to the reduction of the nitro group;
- the bent isomer is expected to be the only isomer due to the electron donating capabilities of the "para" nitrogen atom;
- the Alanine methodology is relevant to cyclisation using bromine (example 403 on page 122 is referred to); and
- the key compound is KIN1148, which has no methyl group.
16. I conclude from Dr Goldberg's evidence that he understands how to prepare the compounds. I infer that Dr Goldberg considers that a person skilled in the art would have had the same understanding. This leads to two important questions – what did Dr Goldberg understand to be the method of preparing the compounds, and would a person skilled in the art have understood the same thing. I am unsure what Dr Goldberg understood to be the method of preparation of the compounds. For instance, I do not understand how to prepare the first thiazole ring by reaction of 2-chloro-5-nitroaniline with formic acid. I accept that Dr Goldberg is able to supply this missing information due to his expertise, but I am not prepared to draw the inference that an uninventive person skilled in the art would be able to do the same. I am satisfied that the person skilled in the art would not have appreciated how to prepare the compounds from a reading of the specification in the light of the common general knowledge.
APPLICANT SUBMISSIONS
17. The applicant's submissions dated 10 August 2017 provide important information that helps to understand the unusual facts of this case:
"the inventors postulated that the RIG-I pathway, being intimately involved in regulating the innate immune response to RNA virus infections could be a target for therapy. They conducted a high-throughput screening program using a small screening library purchased from Life Chemicals Inc ( – Cat. No. F0725-0022). This library contained a number of compounds which the inventors thought capable of modulating the RIG-I pathway. The inventors identified an initial lead compound and on the basis of its chemical structure designed on paper a variety of different amide variations. They then retained the services of Life Chemicals Inc to synthesize these designed compounds for them. The Applicant did not instruct Life Chemicals Inc to synthesize the compounds in any particular way nor indeed direct Life Chemicals Inc to do anything other than supply, for a fee for service, the putative antiviral compounds. These compounds were synthesized by Life Chemicals Inc and supplied to the Applicant for testing for antiviral activity. The results of the testing are disclosed in the specification in the worked examples. … Life Chemicals Inc are the only body that could supply the details of how the claimed compounds were synthesized.
As stated in Dr Goldberg's 1st declaration and accepted by the Examiner, the ability to synthesize the claimed compounds based upon common general knowledge is not in question. … As stated in Dr Goldberg's 2nd declaration the Applicant believes they provided all the information regarding the compounds sufficient to satisfy the written description and enablement requirements in jurisdictions like the USA and Europe."
18. I consider that two arguments are apparent in the applicant's submissions. First, a person skilled in the art would have appreciated how the compounds would be prepared, so a best method is implicitly disclosed. Second, the applicant has not withheld anything as it did not actually prepare the compounds. I will consider both arguments
CONSIDERATION
19. The ground of best method of performance does not often arise as the subject of a hearing. However, the fact that it does not commonly arise does not mean that it is of little or no importance.
The law
20. Section 40(2) relevantly reads:
A complete specification must …
(aa) disclose the best method known to the applicant of performing the invention;
21. Prior to the changes introduced by the RTB, this requirement was found in paragraph (a) of section 40(2):
A complete specification must:
describe the invention fully, including the best method known to the applicant of performing the invention;
22. In Expo-Net Danmark A/S v Buono-Net Australia Pty Ltd (No 2) (Expo-Net)[9] Bennett J stated:
"it must be established that there was a better method known to the applicant at the date of filing the patent than the one described in the specification. This is clearly a subjective question."[10]
and
"To that end it is necessary first to understand what the invention is. Indeed, this is perhaps the first question that needs to be answered".[11]
[9] [2011] FCA 710.
[10] Expo-Net at [15].
[11] Expo-Net at [16].
23. Her Honour went on to recite the approach adopted by the Supreme Court of South Africa Transvaal Provincial Division Harms in Enka BV v E I Dupont De Nemours & Co,[12] and stated that it was a useful analysis:
"(a) the method which the patentee failed to disclose is a method of performing the invention;
(b) the method is in fact a better method of performing the invention than the method disclosed in the specification;
(c) the method was known to the patentee at the time when the application for the patent was lodged at the Patent Office;
(d) the method is not disclosed in the specification; and(e) the patentee knew that the method was better than the method(s) described in the specification."[13][12] (1987) BP 13 (TPD).
[13] Expo-Net at [16].
24. To put it another way, it is necessary to determine what method is disclosed in the specification, and then to ask whether there is any evidence that the applicant was aware of a better method of performing the invention.
25. The construction of the specification is a task undertaken through the eyes of the person skilled in the art. The person skilled in the art is a person having "a practical interest in the subject matter",[14] but is "incapable of a scintilla of invention."[15]
[14] Catnic Components Limited v Hill & Smith Limited [1982] RPC 183 at 242.
[15] Technograph Printed Circuits Ltd v Mills & Rockly (Electronics) Ltd [1972] RPC 346 at 355.
26. What is required to provide a best method of performance depends on the facts of the case:
"It can be accepted that there are cases where the claim is to a product or class of products and the best method requirement is satisfied by a description of the best embodiment known to the patentee at the relevant time. It can also be accepted that there are cases where the claim is to a product and there is no requirement to provide a method of using that product. It is also the case that there is no requirement actually to have carried out the best method and that a prediction will suffice. However, it is necessary to understand the invention itself. … The nature of the invention will determine what is 'best' in the circumstances."[16]
[16] Les Laboratoires Servier v Apotex Pty Ltd [2016] FCAFC 27; 117 IPR 415 (Servier) at [129].
27. It is not necessary for the specification to describe those things that a person would understand and be able to supply from a reading of the specification.[17]
[17] CCOM Pty Ltd v Jeijing Pty Ltd [1993] FCA 1168; 27 IPR 577 at 614-615.
28. The Court in Servier carried out a detailed consideration of the relevant authorities. Of particular assistance for the present case is their discussion of the Illinois Tool Works case:[18]
"The question was whether, where the claim was to an article, the patentee was obliged to describe a method by which such an article could be made; where the claim was to an article having a certain shape, did the requirement to include the best method of performing the invention require disclosure of the method by which it was to be formed? Justice Graham concluded that there was no obligation to describe how the article was made, accepting the argument that in the case of a claim to an article which is directed to the shape of the article, the method of performance means the production of an article in the shape described irrespective of how it may in fact have been made. The patentee had described the formation of a cup with the wedges shown and the evidence was that it was the conception of the shape that was the invention. That is, the decision can be understood in the context of the nature of the claimed invention and the description that was given in the specification."[19]
[18] Illinois Tool Works Inc v Autobars Co (Services) Ltd [1974] RPC 337.
[19] Servier at [131].
29. It is clear that I need to consider three matters:
1. what is the invention for which a best method must be provided;
2. what method is described in the specification; and
3. was the applicant aware of a better method?
30. I will address each of these matters in turn.
What is the nature of the invention?
31. The invention lies in the identification of new compounds that are useful for the treatment of viral infections. The compounds are new, in that they were not previously known to science. However, the utility of the compounds lies in their ability to enhance the antiviral response of a patient. Does the invention lie in the compounds or in their use?
32. I do not believe that this is a case like the Illinois Tool Works case. It cannot fairly be said that the invention is simply the conception of the shape (or structure) of the molecule. Until the applicant was in possession of the compounds, as distinct from merely conceiving their structure, it was not able to do the work to determine whether or not it had solved the problem. It is clear that the invention lies in the compounds and the fact that they can be made. In order for the public to have the full benefit of the invention they must be able to prepare the compounds and then use them for their beneficial properties. The invention must lie in both the compounds and their use.
33. What the applicant did was to contract the work of preparing the compounds to a commercial supplier. The applicant did not provide any instruction how the work was to be done, and did not provide any supervision or guidance of the work. It was left solely to the contractor to work out how to prepare the compounds. While this work was critical to the success of the invention, I will proceed on the basis that the contractor should not be regarded as an inventor.[20]
[20] The relevant law is set out in University of Western Australia v Gray (No 20) [2008] FCA 498, (2008) 246 ALR 603.
What does the specification disclose?
34. The specification discloses the structure of the compounds.
35. The applicant contends that the specification discloses the best method between pages 7 and 30:
"The best method known to the Applicant at the time of filing the application is provided in the specification between page 7, paragraph [0028] and page 30, paragraph [0119]. Applicant submits that all of the information required by a person skilled in the art to make the claimed compounds is contained within this section of the specification combined with their common general knowledge."[21]
[21] Response dated 22 June 2017.
36. The key part of this statement is the reference to the common general knowledge. It is the assertion of the applicant that a person skilled in the art, seeing the structure of the compounds, would readily understand how the compounds would be produced. This point is most clearly made in the following submission:
"if a person skilled in the art could look at a novel chemical structure in [a] patent specification and without issue know how to go about synthesizing that chemical entity then the specification is sufficient."[22]
[22] Response dated 25 July 2017.
37. The applicant submitted that the person skilled in the art would have a basic understanding of synthesis:
"Finally, the Applicant submits that, in the case of pharmaceutical chemistry, it must be assumed that the reader, being a skilled addressee, must have a basic understanding of synthesis. Thus, to suggest that a patent specification does not satisfy the requirements of section 40(2)(aa) simply because the reader is not directed towards a generic scheme is, with all due respect, absurd and as stated in the Manual of Practice and Procedure section 2.11.2.2.6 'if possible, a specification should be construed so as not to lead to a foolish result or one which the patentee could not have contemplated' (Henrikson v Tallon (1965) RPC 434). To expect the patentee to include in the specification every possible permutation or methodology that might be used by the skilled addressee otherwise the specification would not contain the best method would be absurd."[23]
[23] Response dated 22 June 2017.
38. I have already discussed Dr Goldberg's evidence in relation to this point. I concluded that a person skilled in the art would not have appreciated how to prepare any of the compounds from a reading of the specification in the light of the common general knowledge.
Did the applicant know anything better?
39. There is evidence from Dr Goldberg that the applicant did not know of anything beyond what is disclosed in the specification. In his declaration of July 2017 he states:
"I find nothing 'missing' in the application. All of the information the inventors and applicant had to hand at the time the priority document and application were filed was incorporated into the specification of the application."[24]
"There was no information 'withheld' by the Applicant. Any information such as techniques that could be used for synthesis of the novel compounds were well known and did not need to be provided to satisfy the requirements of enablement or written description. I was not aware of a 'new', 'novel' or 'better' way of synthesizing the claimed compounds than the currently known techniques as referred to in my first declaration."[25]
[24] Second Goldberg declaration at [3].
[25] Second Goldberg declaration at [5].
40. I accept that the applicant contracted the task of preparing the compounds to a contractor, and was not informed how the compounds were prepared. What the applicant knew was that the compounds could be purchased from the contractor. The applicant did not include this information in the specification.
Does this satisfy the best method requirement?
41. The applicant submits that it did not know how the contractor had produced the compounds, so it has not withheld anything within its knowledge. Is this enough? It is useful to remember the purpose of the best method requirement, as explained in the reported cases:
"It is settled law that a patentee must act towards the public uberrima fide [in utmost good faith], and must give the best information in his power as to how to carry out the invention. He is therefore bound to tell the public all the steps that can advantageously be taken in carrying out the invention."[26]
[26] Vidal Dyes Syndicate Ltd v Levenstein Ltd (1912) 29 RPC 245 at 269.
"The Act is intending to protect the public against a patentee who deliberately keeps to himself something novel and not previously published which he knows of or has found out gives the best results, with a view to getting the benefit of a monopoly without giving the public the corresponding consideration of knowledge of the best method of performing the invention."[27]
"The requirement is to ensure good faith on the part of the patentee, and to protect the public against a patentee who deliberately keeps to himself something novel and not previously published which he knows of or has found out gives the best results, with a view to getting the benefit of monopoly without giving to the public the corresponding consideration of knowledge of the best method of performing the invention."[28]
"to allow the public the full benefit of that invention when the monopoly expires".[29]
[27] American Cyanamid Company v Ethicon Limited [1979] RPC 215 at 269.
[28] Firebelt Pty Ltd v Brambles Australia Ltd [2000] FCA 1689; 51 IPR 531 at [48].
[29] Servier at [108].
42. In the present case the public does not know anything. The applicant knew that the compounds could be purchased from Life Chemicals Inc. Life Chemicals Inc knew how to prepare the compounds. The applicant has not disclosed that the only method known to it (and thus the best method known to it) was to purchase the compounds from Life Chemicals Inc.
43. This is similar to the discussion in American Cyanamid Company (Dann's) Patent[30] where Lord Morris of Borth-y-Gest referred to the case of Sturz v De La Rue[31] as authority for the proposition that where a compound (used as a starting material) was not generally known in the trade but could be imported, then "mention should be made of that circumstance" in the specification. The patentee did not have an obligation to also make that compound available.
[30] [1971] RPC 425 at 443.
[31] (1828) 5 Russ 322.
44. It follows that I am satisfied that the applicant was aware that the compounds could be obtained from Life Chemicals Inc, and that information should have been included in the specification. The applicant has not provided a best method of performance. Any other conclusion would allow an applicant to obtain a patent for these novel substances without providing any information as to how to obtain the substance. This would be the antithesis of the quid pro quo at the heart of the patent system.
45. If the specification were amended so that the claims were solely directed to the use of the compounds that would not overcome the problem. While the authorities state that it is not necessary to disclose how starting materials for a process are to be obtained,[32] this is only the situation when the starting material is not the invention.
[32] For instance, see Blanco-White, Patents for Inventions, 4th ed, 1974, para 4-516.
CONCLUSION
46. The applicant was required to provide a best method of performing the invention in relation to the preparation of the novel compounds. The specification does not set out any method of preparing the compounds, and no method is apparent when the specification is read in the light of the common general knowledge. The applicant was aware that the compounds could be obtained from a commercial supplier. I am satisfied that the specification does not comply with section 40(2)(aa) as it does not disclose the best method known to the applicant. The ground of objection is properly raised.
47. The requirement of section 40(2)(aa) is closely related to the requirement of section 40(2)(a). I have found that the specification does not disclose any method of preparing the compounds, and no such method would have been understood by a person skilled in the art. In the light of this conclusion I cannot see that the specification complies with section 40(2)(a). When considering any amendments, the Examiner will consider the applicability of both section 40(2)(a) and 40(2)(aa).
48. I will allow the applicant the time remaining for acceptance in order to attempt to overcome the objection.
49. Pursuant to regulation 13.4 the present application will not lapse until 3 months from the date of this decision.
Dr S.D. Barker
Deputy Commissioner of Patents
6
5
0