Aktie Bolaget Astra Apotekarnes Kemiska Fabriker v Willows Francis Pharmaceutical Products Ltd

• Jurisdiction: South Africa
• Judge: De Wet J, Hill J and Hiemstra J
• Judgment Date: 03 August 1959
• Court: Transvaal Provincial Division
• Citation: 1959 (4) SA 1 (T)

De Wet, J.:

On the 18th December, 1947, the appellant filed an application in the Union of South Africa for a patent which will be described later. On the 14th January, 1949, letters patent were duly granted, and the patent is still of full force and effect. On the 28th A January, 1953, the appellant filed an application for leave to amend the specification of the patent, but thereafter applied for leave to vary its application for an amendment, and on the 6th April, 1954, the Commissioner of Patents granted an order allowing the appellant to vary its original application for an amendment. This application was heard later and was opposed by an objector.

B The title of the invention is 'A process for the preparation of local anaesthetics'. The introductory paragraph of the specification reads:

'Compounds having the general formula:

x-acyl-xylidide - 2, 6,

in which x represents a mono - or di-substituted amino group, and particularly such compounds in which the amino group x consists of an alkylamino, dialkylamino, allylamino, cyclohexylamino, or piperidino C group, and salts of such compounds, have been found to constitute valuable local anaesthetics, which have a comparatively low toxicity in comparison to their efficiency. Furthermore, these compounds are very quick-acting, and they may be used without an addition of vaso-constrictors. Solutions of their salts possess an unlimited stability, and they give very stable solutions with adrenaline.'

The consistory clause reads:

D 'The process according to the invention for the preparation of these new compounds consists principally in causing 2, 6 - dimethyl - aniline, or a derivative thereof, to react with an aliphatic halogen-carboxylic acid, or with a derivative of such an acid, and treating the halogen-carboxylic acid xylidide - 2, 6 thus formed with a primary or secondary amino.'

The revised amendments in effect consist of three amendments, each with consequential alterations. These can be summarised as follows:

E (1) By way of disclaimer, to claim the preparation of a single specific compound, viz. N-diethylaminoacetyl-xylidide - 2, 6 (i.e. xylocaine) and its salts instead of a class of compounds, of which the specific compound xylocaine is a member; and to restrict the description and examples given in the specification accordingly.

F (2) By way of correction, explanation or disclaimer, to limit the halogens used in the processes to bromine, chlorine and iodine, and excluding fluorine.

(3) By way of explanation, to include an additional claim, viz. claim 8, claiming the specific compound when prepared by any of the processes claimed in claims 1 - 7, or by an obvious chemical equivalent thereof.

G A great deal of documentary evidence was placed before the Commissioner by the appellant and by the objector (now the respondent). In the result the main issues to be decided by the Commissioner were: (a) whether objectively the proposed amendments fell within the competence of sec. H 36 (3) of the Act; (b) if so, whether the Commissioner had a discretion to refuse the application, and (c) assuming the Commissioner had a discretion, whether, on the evidence, the application should be refused in the exercise of such discretion.

It will be convenient to deal with these amendments separately in the order in which I have placed them.

In regard to the first amendment the Commissioner found that the amendment to restrict the patent to processes for the preparation of the specific compound xylocaine only fell within the competence of

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sec. 36 (3) of Act 37 of 1952. It is conceded by the respondent that this finding is correct, but the Commissioner held that he had a discretion to refuse the amendment and, in the exercise of that discretion, he did refuse to allow it. It is now argued by Mr. Suzman, for the appellant, in the first place that the Act does not confer a discretion upon the Commissioner and, in the alternative, that he did A not exercise a judicial discretion in that he misdirected himself in considering the evidence placed before him. I shall deal with the latter argument first on the assumption that the Commissioner does have a discretion.

The Commissioner's findings appear from the following extracts from his judgment:

B 'The applicant admits that in July, 1947, a few months before the application was made in the Union, and in connection with its application for the patent in the United States, it filed an affidavit by Dr. Goldberg which referred to one of the substances included in the scope of the unamended claims of its specification, but denies that the said substance was not useful for treatment of human beings, and that the inclusion thereof in its claims was in breach of good faith.

C Dr. Goldberg's affidavit (exh. H.G.B.1) and the paper read by him to the Pharmacological Department at Stockholm (exh. H.B.G.2) are put in by Mr. Bouly in his affidavit of 28th November, 1954.

According to Dr. Goldberg the subcutaneous injection of the substance mentioned in example 2 of the specification, produced a 'strong smarting sensation' which excluded the further testing of the substance in man. In his paper he said the substance caused 'intensive smarting and heavy pain lasting for several days' even though a minimal quantity was injected.

D There is evidence to show that the substance mentioned by Dr. Goldberg and included in applicant's specification, is a valuable anaesthetic when its use is restricted to purely surface application.

There is a conflict of view between the experts as to whether, having regard to the harmful results following the use of the compound subcutaneously, the applicant acted bona fide or justifiably in describing it, in company with the other compounds covered by the specification (which may be used subcutaneously) in the following terms:

E 'Compounds having the general formula

x-acyl-xylidide 2, 6, . . . and salts of such compounds, have been found to constitute valuable local anaesthetics which have a comparatively low toxicity in comparison to their efficiency. Furthermore, these compounds are very quick-acting and they may be used without vaso-constrictors. Solutions of their salts possess an unlimited stability and they give very stable solutions with adrenaline.'

Dr. Goldberg, who made his affidavit of the 16th July, 1947 (exh. F H.G.B.1) at the applicant's request in support of its United States Patent application, therein expressed the view that - 'It is a prerequisite for clinical use of a substance as a local anaesthetic, that the substance shall lack irritating or tissue damaging properties. I have given particular attention to this question.'

The applicant was aware of this comment.

No evidence was directed to a comparison as to width of claims and other features between the American and Union specifications, but even G in the absence of such evidence it is observed by comparison that the former does not incorporate the example 2 of the latter, which applicant now seeks to expunge, and which the applicant admits is the preparation to which Dr. Goldberg refers in his affidavit.

It is also admitted that the substance in question is included in the general formula claimed in the specification. There is no explanation why it was specifically included in the Union specification as a H preferred embodiment in example 2, whilst deliberately omitted from the United States specification - presumably because of Dr. Goldberg's criticism. The applicant does not explain its incorporation as being due to a mistake or inadvertence. On the contrary Dr. Sjögren now seeks to justify rather than excuse the applicant's conduct in this regard, by stating that the reference in the opening paragraph of the specification relating to the general formula did not mean that 'all' or even 'the' compounds within that category have the properties claimed.

I cannot agree with that negation of the clear meaning of the words used. No exception or qualification is implied by the general statement 'compounds

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having the formula . . . have been found to constitute valuable local anaesthetics. . . .'

Moreover, even as an excuse it is entirely without substance, because of the mention by Dr. Goldberg of the harmful consequences of the use of the very compound included as example 2 in the specification.

A further explanation offered by Dr. Sjögren is to say that this A compound was 'later found to be a good surface anaesthetic'.

Dr. Edlund in his affidavit of 7th June, 1955, and in his last affidavit of 3rd October, 1956 (accompanied by various publications) supports the view that the compound is a good surface anaesthetic. He, however, made his tests years after the Union patent was applied for - presumably for purposes of this case.

It seems to me, therefore, that the inclusion of the compound in the B generality of the applicant's introductory premise and the listing of it as example No. 2 without any limitation as to its method of use, was either mala fide, reckless or covetous.

The evidence clearly reveals, and it is admitted by applicant, that the compounds covered by employment of the formula mentioned are almost unlimited. The evidence on the opponent's behalf, based upon calculations, is that the number of compounds falling within the general formula of the specification is 'immense, and indeed astronomical' and C that the ambit of the invention is 'so wide that the total number of substances included within their scope is counted in millions'.

In para. 3 of his affidavit of 3rd October, 1956, Dr. Sjögren admits that 'if account were taken of all the theoretically possible compounds having the...