Société des Usines Chimiques Rhone-Poulenc et al. v. Jules R. Gilbert Limited et al.

RHONE-POULENC and CIBA, S.A.,

APPELLANTS; June 24

HALL J.:-This is an action for alleged infringement by the respondents of claim 18 of Canadian Patent no. 474637 granted to the appellant Soci6t6 des Usines Chimiques Rhone-Poulenc on June 19, 1951, for an invention entitled "Substituted Diamines". -Claim 18 is, in substance, for processes which, among others, include several particular chemical reactions, any one of which might be a step in a process for the synthesis of a substance which has become known by the generic name tripelennamine.

The first named appellant sues as owner of the patent and the appellant Ciba as exclusive licensee under it. Their claim is that claim 18 of the patent has been infringed by the respondent, Gilbert Surgical Supply Co. Ltd. and by the other respondents. It is conceded that if claim 18 of the patent is valid the respondents have infringed.

The issues were narrowed in the Exchequer Court' by an agreement as to facts providing that for the purposes of the action the parties agreed:

on June 22, 1943, to substances which were also known on the said date, though the said methods had never at the said date been applied to the said substances except by the inventor named in the said patent.

RIONE- 2. That the substance referred to in paragraphs 6 and 7 of the reamended Statement of Defence was not manufactured in Canada and was imported from outside Canada.

R.

That none of the defendants has any knowledge as to the process by which the said substance was prepared or produced.

Hall J.

Tripelennamine is one of a group of drugs which have been found to be useful in blocking the effects of histamine in the body and which have become known as anti-histamines.

The specification in Canadian Patent No. 474637 is, in part, as follows:

TO ALL WHOM IT MAY CONCERN:

BE IT KNOWN THAT I, RAYMOND JACQUES HORCLOIS, of 31 Rue du Chalet, Malakoff (Seine), France, a citizen of France, having made an invention entitled: "IMPROVEMENTS IN OR RELATING TO SUBSTITUTED DIAMINES", the following is a full, clear and exact disclosure of the nature of the same invention and of the best mode of realizing the advantages thereof:- The present invention relates to new chemical compounds and to processes of producing the same. More particularly, this invention is concerned with new substituted diamines.

It is the main object of the present invention to provide new tertiary diamines having exceptionally powerful anti-histaminic action. It is a further object of this invention to provide processes for the production of these new diamines.

The new therapeutically active ditertiary diamines of the present invention conform to the general formula:where "Het" represents a monocyclic, heterocyclic nucleus, for example, pyridine, piperidine, furane, tetrahydrofurane, thiazole and pyrimidine, R represents a radical selected from the class consisting of aralkyl, aryl and monocyclic heterocyclic groups and aryl substituted in the nucleus by a member of the class consisting of alkyl and alkoxy groups, and R is a lower alkylene group having at least two carbon atoms. Substances in this class possess an exceptionally powerful antihistaminic action. and includes details set out in the reasons of Thurlow J. not necessary to repeat here. Thirteen examples are given in the specification but only those numbered I, IX and XIII represent separate methods of preparing tripelennamine, example XIII being the method involved in claim 18. The disclosure portion of the specification concludes:

It will be understood that, without departing from the spirit of the SociT invention or the scope of the claims, various modifications may be made CUISNES in the specific expedients described. The latter are illustrative only and not RHONEoffered in a restricting sense, it being desired that only such limitations shall be placed thereon as may be required by the state of the prior art. Claim 18, the claim in question in this action, reads:

JULESR. 18. A process as defined in claim 8 in which R is phenyl.

Reference to claim 8 brings in successive references to claim HallJ. 7 and claim 3 the result of which, on the references being incorporated, is that claim 18 reads:

A process for the preparation of new therapeutically valuable tertiary diamines being compounds of the general formula

R-N where Het is pyridine, R is phenyl and R, is -CHC and their salts, by reacting a secondary tertiary diamine of the formula

/CH:with a compound of the formula pyridine-X where X is a halogen atom.

The validity of claim 18 was challenged on a number of grounds, all of which were dealt with by Thurlow J. in his comprehensive reasons now under review. In my view only one of these grounds needs to be considered. If this ground is valid, as I think it is, that concludes the matter adversely to the appellants. This ground has two aspects which are interrelated, the first aspect being that claim 18 is too broad in its terms in respect of utility and for the reasons given in Hoechst Pharmaceuticals of Canada Limited and Farbwerke Hoechst Aktiengesellschaft Vormals Meister Lucius & Bruning v. Gilbert & Company, Gilbert Surgical Supply Co. Limited, Jules R. Gilbert Limited is invalid. In Hoechst Thurlow J. is quoted with approval at p. 193 as follows:

As a matter of interpretation however it is in my opinion clear that the claim refers to every mathematically conceivable sulphonyl urea of [1966] S.C.R. 189, 32 Fox Pat.

S.C.R.

[19681 the class for I can see no basis upon which anyone who might contrive to make a substance of the class, however inconceivable the preparation USINES of such a substance may have been at the time of the drafting of the CHIMIQUES claim, could successfully maintain that his substance was not within the RHONEclass. But even if the claim were read as referring only to those members of the class which as a matter of chemistry or even of commercial manufacture could conceivably be made, I see no reason to doubt that it R.

would refer to a class many thousands strong.

al.

ofIt is obvious and conceded by appellant that claim 18 H of the patent in suit covers at least twelve different substances, namely the alpha, beta and gamma isomers and their four hydrohalide salts. On the other hand, it is equally clear that the beta and gamma isomers are not shown to be therapeutically valuable anti-histamines, the effective antihisme, tripelennamine, being the alpha isomer. It is also established that at least one of the hydrohalide salts cannot be safely used as oral medication, namely the hydrofluoride. This is sufficient to bring the case within the principle of the decision Re May & Baker Ltd. v. Boots Pure Drugs Co. Ltd. , which is referred to by Thurlow J. and was applied by this Court in Commissioner of Patents v. Ciba. This principle is stated as follows in that case by Martland J. at p. 381:

Although the two named thiazoles were of considerable therapeutic value, there was no evidence that this was true of any other derivatives covered by the claims, and accordingly the patent was bad for want of subject-matter, since the claims covered substances which were not useful. As this is sufficient to dispose of the case, I prefer to express no opinion as to the consequence of having claimed, in addition to the substances obtained by the process described in claim 18, the salts of those substances. Similarly, I prefer to express no opinion as to whether the rare radioactive halogen element atastatine is to be considered as included in claim 18 in addition to the four usual halogens. I also prefer to express no opinion as to whether the claim should be read as implying that the alpha isomer may be prepared by the process described otherwise than by using alpha material in the reaction.

(1950), 67 R.P.C. 23; (1949), 66 R.P.C. 8; (1948), 65 R.P.C. 255. 4 [1959] S.C.R. 378, 19 Fox Pat.