Patents

            COMMISSIONER'S DECISION

 

INSUFFICIENT DISCLOSURE S.36(1): Undisclosed Subject Matter Claimed.

 

The decision affirmed that some claims are too wide in covering whole

classes of substances which were obviously untried and untested. In

addition, while claims for benzothiadiazines (claimed in other patents

by the applicant and others) mixed with hypotensive agents may be

inventive, there was no disclosure of such invention as required by

S.36(1). Other objections that the claims were not patentably

different from subject matter lost in conflict, and that there is lack

of invention, were reversed. The disclosure does not reveal any

unexpected synergism, nor does it give adequate details of the

operation, use or effect of such a composition.

 

FINAL ACTION: Affirmed in-part.

 

     ********************************

 

On March 9, 1960, CIBA Limited filed an application for

patent, serial no. 794,095, Class 167 - 213, for 3:4-Dehydro-

1:2:4-Benzo-thiadiazine-1:1-Dioxides and a Process for

Their Manufacture. The inventors were George De Stevens and

Lincoln H. Werner, assignors to Ciba. After numerous actions

the examiner rejected the application on January 8, 1973.

The applicant subsequently requested a review of the rejection

by the Commissioner of Patents, and a Hearing before the

Patent Appeal Board. The Hearing took place on play 8, 1974,

at which time Mr. George Seaby represented the applicant.

 

The application contains 240 claims, of which 180 are for a

process of "combining" certain benzothiadiazines with a hypo-

tensive agent. The remaining 60 claims are for the mixtures so

produced. The product claims are made dependent upon the

process claims. Though claims 22 and 188 will be adequate to

illustrate the nature of the invention, the chemical complexities

of which need not concern us, claim 1 is also reproduced to

indicate the breadth of the invention claimed. It would be no

exaggeration to say that tens of thousands of compounds are

encompassed by the claims.

 

   Cl. 22 Process for the manufacture of a pharmaceutical prepara-

tion consisting of combining a compound of the formula

 

                           (see formula 1)

 

in which R4 stands for a bromine or fluorine atom, a methoxy

or methyl group, or an alkali metal salt thereof together

with a hypotensive agent.

 

   Cl.188 Pharmaceutical preparations whenever prepared or produced

by the process of any one of claims 22, 23 and 24, or by

any process which is an obvious equivalent thereof.

 

   Cl. 1 Process for the manufacture of a pharmaceutical preparation

consisting of combining a compound of the formula

 

                   (see formula 2)

 

in which each of the groups R1, R3, R5 and R6 is hydrogen, an

alkyl or an acyl group, R2 represents hydrogen, or an aliphatic

hydrocarbon radical, a cycloaliphatic radical, a cyclo-

aliphatic-alkyl radical, an aryl radical, an araliphatic

radical, a heterocyclic or heterocyclic-alkyl radical, the

heterocyclic radical of these latter being monocyclic and con-

taining one oxygen, nitrogen or sulfur atom in the ring, all

these radicals being either unsubstituted or substituted by

halogen atoms, free, esterified or etherified hydroxyl or

mercapto groups, nitro, amino, acylamino, monoalkyl-, dialkyl-

or N,N-alkylene-amino groups, whose alkylene radical may be

interrupted by a hetero-atom, carboxyl groups, sulfamyl or

alkyl groups, and R4 stands for an unsubstituted or halogen-

substituted alkyl radical, an esterified or etherified hydro-

xyl group or a halogen atom, with the proviso, that whenever

R4 is chloro, at least one of the groups R1, R2, R3, R5 and R6

stands for one of the above organic radicals, or a salt thereof,

together with a hypotensive agent.

 

The prior prosecution of this application has been both long and involved.

Because of its complexity, it will be more appropriate to summarize the

objections made, rather than to quote directly from the actions and

responses themselves:

 

1. The admixtures claimed are not inventively different. or

patentably distinguishable from subject matter the applicant lost in

conflict proceedings involving other applications of the applicant.

 

2. There is no invention in mixing the new compounds, which

have hypotensive properties, with other known hypotensive compounds.

Such admixtures would be obvious to one skilled in the art.

 

3. There has not been any proper disclosure of an invention.

 

4. The admixtures claimed are not patentably different from claims

made elsewhere by the applicant to the new compounds themselves. In

utilizing this argument the examiner relied extensively upon the

decision of the Supreme Court of Canada in Commissioner of Patents v.

Farbwerke Hoechst (1964) S.C.R. 49, which, he contends, stand for the

proposition that if a chemical compound has already been patented, claims

to that compound in admixture with other ingredients are not patentable

where no additional invention subsists in and has been disclosed for

that admixture.

 

5. The claims are too broad, covering a class of indefinite size,

so large that an assertion as to the properties and usefulness of the

substances are unfounded and unwarranted.

 

6. Section 41 is applicable, and requires that the products be

claimed by way of the chemical process by which they were manufactured,

rather than by the step of admixing them with the hypertensive agents.

 

There are many similarities between the rejection made in this case

and that in the case of copending application 081,556 of the same inventors

and applicant, both of which were heard by the Board at the same time.

In a decision dated August 2, 1974, the Commissioner sustained the re-

jection of application 081556. There are however, some differences

between the rejections. In the present application, for example, process-

type claims are present, and the composition claims are made dependent upon

the process-type claims, so that in form at least Section 41 of the Patent

 

Act has been complied with. In addition, of course, the scope

of the claims is much broader, since R2 is the chloromethyl radical

in 081556.

 

From the claims quoted above, it will be apparent that the invention

of the applicant is a composition consisting of particular benzo-

thiadiazines mixed with a hypotensive agent. The precise chemical

structure of the benzothiadiazine is immaterial to what must be

decided, and the compounds will hereinafter be referred to as

"benzothiadiazine." The "process" merely calls for "combining" (or

mixing) the benzothiadiazine" with a hypotensive agent. No

particular procedural steps are disclosed or claimed for preparing the

composition, and all that is involved is the common expedient of

mixing two ingredients together. Divorced from any invention in the

product, the "process" would be unpatentable. As for the benzothiadiazines,

they possess duretic and other properties which make them useful

medicinally.

 

First to be considered is the objection that subject matter in the claims was

lost by CIBA during conflict proceedings, and now appears in Canadian

Patent 681760 to Bristol-Myers and C.P. 719693 to Abbot Laboratories.

We have found that the broad claims of the application encompass and

some of the specific compositions do in fact appear in those patents.

As one example, claims 30, 89 and 190 of this application cover the

same subject matter as C.P. 681760 (Bristol-Myers). Both of the patents

had been involved in conflict proceedings with application 771510

(now patent 697915) filed by George de Stevens and Lincoln H.Werner

and assigned to CIBA. They were also in conflict with another CIBA

application, now patent 696,976, which stands in the name of another

inventor, E.A. Jack. In his response the applicant argues firstly

that since this particular application was not part of the conflict,

the outcome of the conflict has no bearing on it; and secondly that

his rights to the matter now being claimed were not settled by the

conflict. With the first argument we would disagree, but we are

persuaded by the second. When it has been determined that an inventor

is not the first inventor of subject matter as the result of

conflict proceedings involving one of his applications, he should

not be able to claim it in another of his applications. Section 28(1)

(a) would preclude this. In this instance, however, we have not been

able to ascertain from the evidence with certainty that the conflict

resolved priority against the applicant on the subject matter claimed

here. On this point we find the applicants submissions persuasive,

and consequently are satisfied this objection should not be pursued

further.

 

Similarly we do not think there is anything to be gained in maintaining that

the admixtures claimed are not in fact inventive. Evidence to that

effect was introduced with the amendment of September 8, 1969.

(This, it may be noted, is more than nine years after the application

was filed). Similarly the issuance of Canadian patents 681760, 696976,

697915 and 719693 (referred to previously) testify to that fact that

mixtures of the benzothiadiazine with hypertensive agents amount to

invention. The applicants submission provides many instances of products

on the market based upon the invention, and adequate evidence as to its

patentability.

 

It is when we consider the adequacy of the disclosure, however, that

we believe the application must fail. All thirty-one pages of the

disclosure and all the examples describe the benzothiadiazines, a process

for preparing them by chemical reduction of a C=N double bond and

subsequent acylation, and tabletting with binders. The sole

reference to using them with hypotensive agents appears in the last

sentence of the paragraph bridging pages 6 and 7, which is quoted

below (underlining added):

 

The new compounds may be used as medicaments in the form

of pharmaceutical preparations which contain the

compounds in admixture with a pharmaceutical organic or

inorganic, solid or liquid carrier suitable for enteral,

e.g. oral, or parenteral administration. For making up

the preparations there may be employed substances which do not

react with the new compounds, such as water, gelatine,

lactose, starches, magnesium stearate, talc, vegetable oils,

benzyl alcohols, gums, polyalkylene glycols, petroleum jelly,

cholesterol or any other known carrier for medicaments. The

pharmaceutical preparations may be in solid form, for

example, as tablets, dragees or capsules, or in liquid form

as solutions, suspensions or emulsions. If desired, they

may be sterilized and/or contain auxiliary substances, such

as preserving agents, stabilisers, wetting or emulsifying

agents, salts for varying and osmotic pressure or buffers.

The may also contain other therapeutically useful substances,

for example hypotensive agents, such as Rauwolfia or

Veratrum alkaloids, e.g. reserpine, rescinnamine, deserpidine,

germine or protoveratrine, synthetic hypotensive agents,

e.g. hydralazine, or ganglionic blockers, such as chlorisondamine.

 

While it may be possible for a single sentence to provide sufficient

disclosure to warrant claims to some inventions, we do not think

that can be the case here. There is no indication in it of any unex-

pected synergism, or adequate details about the operation, use of effect

of the invention. Clearly Section 36(1) is not satisfied. In Radio

Corporation of America v. Raytheon Manufacturing (1956-1960) Ex. C.R. 98

at 108, it was stated, for example, that:

It is a cardinal principle of patent law that an inventor

may not validly claim what he has not described. In the

patent law jargon it is said that the disclosures of the

specification must support the claims. If they do not, the

claims are invalid. Moreover, there is a statutory duty of

disclosure and description that must be complied with if a

claim for an invention is to stand. Section 35 of the Patent

Act, 1935, provides, in part:

"35. (1) The applicant shall in the specification

correctly and fully describe the invention and its opera-

tion or use as contemplated by the inventor, and set forth

clearly the various steps in a process, or the method of

constructing, making, compounding or using a machine,

manufacture or composition of matter, in such full, clear,

concise and exact terms as to enable any person skilled in

the art or science to which it appertains, or with which it

is most closely connected, to make, construct, compound

or use it. In the case of a machine he shall explain the

principle thereof and the best mode in which he has contemplated

the application of that principle. In the case of a process he

shall explain the necessary sequence, if any, of the various

steps, so as to distinguish the invention from other

inventions. He shall particularly indicate and distinctly

claim the part, improvement or combination which he claims

as his invention.

(2) The specification shall end with a claim or claims

stating distinctly and in explicit terms the things or combin-

ations which the applicant regards as new and in which he

claims an exclusive property or privilege."

 

In Minerals Separation North American Corporation v. Noranda

Mines Limited (1947) Ex. C.R. 306 I had occasion to consider

the duties of disclosure required of an inventor in consider-

ation of the grant of a valid monopoly in respect of his

invention. At page 316, I said:

 

"Two things must be described in the disclosures of a specific-

ation, one being the invention, and the other the operation or

use of the invention as contemplated by the inventor, and with

respect to each the description must be correct and full. The

purpose underlying this requirement is that when the period

of monopoly has expired the public will be able, having only

the specification, to make the same successful use of the

invention as the inventor could at the time of his application.

The description must be correct; this means that it must be

both clear and accurate. It must be free from avoidable obscurity

or ambiguity and be as simple and distinct as the difficulty of

description permits. It must not contain erroneous or misleading

statements calculated to deceive or mislead the persons to whom

the specification is addressed and render it difficult for them

without trial and experiment to comprehend in what manner the

invention is to be performed. It must not, for example, direct

the use of alternative methods of putting it into effect if only

one is practicable, even if persons skilled in the art would be

likely to choose the practical method.

 

The description of the invention must also be full; this mews

that its ambit must be defined, for nothing that has not been

described may be validly claimed. The description must also

give all information that is necessary for successful operation

or use of the invention, without leaving such result to the

chance of successful experiment, and if warnings are required in

order to avert failure such warnings must be given. Moreover, the invent

must act uberrima fide and give all information known to him

that will enable the invention to be carried out to is best

effect as contemplated by him."

 

and I cited the cases from which this statement was abstracted.

The statutory requirement then in effect was section 14 of

The Patent Act, Statutes of Canada, 1923, Chapter 23, and

I made the statement that it merely puts the requirements of

the law, as laid down in the cases, into statutory form.

While my judgment in the Minerals Separation case (supra)

was reversed, the statement I have cited has not been

challenged. And it is applicable in a case to which section 35

of The Patent Act, 1935, applies: vide Di Fiore v. Tardi,

(1952) Ex. C.R. 149 at 154. The onus of disclosure that the

section places on an inventor is a heavy and exacting one. (under-

lining added)

The same theme was developed in French's Complex Ore v Electrolytic

Zinc 1930 S.C.R. 462, Smith Incubator v. Sealing 1937 S.C.R. 251,

Minerals Separation v. Noranda Mines 1947 Ex. C.R. 306 at 316,

Gilbert v. Sandoz (1971) 64 C.P.R. 7 at 42-45, and Rhone-Poulenc and CIBA

v. Gilbert 1966 Ex. C.R.59 & 1967 S.C.R. 45.

 

As for the evidence now presented that invention is in fact present,

we would refer to the statement of the President of the Exchequer Court

in Riddell v Patrick Harrison 1956-60 Ex. C.R. 213 at 225:

...what has to be considered in a patent case is the in-

vention as described in the specification and defined in

the claims rather than that described in the evidence."

 

That it would have been easily possible to provide a full disclosure

of the invention when this application was filed is demonstrated by the

disclosures of Canadian patents 719693 and 681760 (cf supra), or even

by CIBA's own patents 696976 and 697915. The contract between those

disclosures and that in this application accentuates the inadequacies

in the latter.

 

We have already indicated the scope of the broad claims illustrated

previously by claim 1. There is more than adequate precedent in

Boehringer Sohn v. Bell Craig 1962 Ex. C.R. 201 and 1962 S.C.R. 410;

Farbwerke Hoechst v. Commissioner of Patents 1966 Ex. C.R. 91 and 1966

S.C.R. 606; Burton Parsons v. Hewlett-Packard 7 C.P.R. (2d) 1973 198

and 10 C.P.R. (2d) 126; Rh“ne-Poulenc & CIBA v. Gilbert 1966 Ex. C.R. 59

and 1967 S.C.R. 45 and Hoechst v Gilbert 1965 Ex.C.R. 710 1966 S.C.R. 189

to warrant rejecting the broad claims, such as claims 1-44 inclusive

and 181-195 inclusive.

 

As was said in the latter case (in the Exchequer Court):

... the proposition that all or substantially all of the

limitless number of substances which could be produced

by these processes as defined have value as oral

antidiabetic medicines, when it is apparent from the

mere size of the class that most of its members could

never have been made or tested by anyone, is so

preposterous as to require little in the way of evidence

to dispel any presumption of its truth. Presumed or

not the proposition shocks ones credulity.

 

We see little value in developing the objection based on Section 41.

That issue is beclouded in this instance by such questions as what

invention has been disclosed, what invention has actually been made,

the grant of the four patents mentioned previously which were not put

under Section 41, the form of the claims in this application, and

whether the term "combining" properly defines a process. Since we

believe the patentability of the claims has been fully decided by

Section 36 and the inadequacies of the disclosure, we recommend that

objections based on Section 41 should not form part of the reasons for

a refusal by the Commissioner.

 

We note that the claims overlap patents already granted to CIBA, and

also in some instances to the inventors of this application, such as

Canadian Patents 697915, Nov. 17, 1964 and 696976, Nov. 3, 1964. They

also overlap patents issued to competitors (e. g. 719693 and 681960),

and application 081556 of the applicant). These suggest questions

of extension of monopoly, double patenting, and Section 63(2).

Again, however, we see no need to explore those issues.

 

For the reasons indicated above, the Board is of the opinion

that all of the claims should be refused.

 

Gordon A. Asher,

Chairman,

Patent Appeal Board.

 

I concur with the findings of the Patent Appeal Board. The claims

are refused. The applicant has six months within which to appeal

this decision as provided in Section 44 of the Patent Act.

 

Decision accordingly,

A.M. Laidlaw,

Commissioner of Patents.

Dated at Hull, Quebec

this 13th. day of

August, 1974.

 

Agent for Applicant

Marks & Clerks

Ottawa, Canada