Application of Lund

• Decision Date: 11 May 1967
• Docket Number: Patent Appeal No. 7713.
• Citation: 376 F.2d 982,153 USPQ 625
• Parties: Application of Frantz LUND and Wagn Ole Godtfredsen.
• Court: U.S. Court of Customs and Patent Appeals (CCPA)

153 USPQ 625, 376 F.2d 982 (1967)

Application of Frantz LUND and Wagn Ole Godtfredsen.

Patent Appeal No. 7713.

United States Court of Customs and Patent Appeals.

May 11, 1967.

Lawrence S. Levinson, Westfield, N. J. (N. Dale Sayre, Robert Alpher, New York City, Merle J. Smith, Scotch Plains, N. J., of counsel), for appellants.

Joseph Schimmel, Washington, D. C. (Jack E. Armore, Washington, D. C., of counsel), for the Commissioner of Patents.

Before RICH, Acting Chief Judge, MARTIN, SMITH and ALMOND, Judges, and WILLIAM H. KIRKPATRICK.^*

KIRKPATRICK, Judge.

This is an appeal from the decision of the Board of Appeals affirming the examiner's rejection of claims 2-4, 15 and 16 in appellants' application¹ entitled "Substituted Dihydrobenzothiadiazines."

The subject matter of the application relates to certain 3-substituted-6-trifluoromethyl-7-sulfamyl-3, 4-dihydro-1, 2, 4-benzothiadiazine-1, 1-dioxides of the formula

As set forth in the claims, the "R" group at position 3 of the benzothiadiazine nucleus is the only variable,² defined in claim 15 as "Aralkyl," in claim 16 as "mononuclear aralkyl," in claim 2 as "Phenyl (lower alkyl)", in claim 3 as "benzyl" and in claim 4 as "phenethyl."

Appellants prepare the claimed compounds by reacting a,a,a-trifluoro-m-toluidene,

with excess chlorosulfonic acid in the presence of an alkali metal chloride to yield 5-trifluoromethylaniline-2,4-disulfonyl chloride. That compound is treated with aqueous ammonia to yield 5-trifluoromethyl-2,4-disulfamylaniline,

The latter derivative, in turn, is reacted with an aldehyde of the formula RCHO, where R is as defined above, to yield the claimed compounds. To obtain the 3-benzyl compound of claim 3, for example, phenylacetaldehyde is reacted with 5-trifluoromethyl-2,4-disulfamylaniline.

According to appellants, the claimed compounds exert "strongly saluretic sodium expelling and diuretic water expelling effects" and are useful in the treatment of heart conditions and hypertension. The record shows that the compounds of the claims are generally more active than the corresponding 3-unsubstituted or 3-aliphatically substituted compounds, with the specific compounds of claims 3 and 4 having greatest activity.

With that background information concerning appellants' invention in mind, we turn to the issues presented to us by the decision of the board and appellants' reasons of appeal. As those issues are quite diverse in nature, we shall discuss each separately.

The 35 U.S.C. § 112 Rejection

The examiner rejected claims 15 and 16 as "failing to properly define the invention in accordance with the requirements of 35 U.S.C. 112." He was of the view that the expressions "aralkyl" and "mononuclear aralkyl," which are employed in those claims to define the substituent in the 3-position of the molecule, are "beyond the scope of the disclosure" in appellants' specification, having found that the disclosure was not "sufficiently representative to support the breadth of the claims." The board agreed.

Appellants disagree with that position, and contend that the following portion of their specification, which describes the aldehyde reactants employed to introduce the 3-substituent, provides sufficient support for claims 15 and 16:

* * * Among the suitable aldehyde reactants may be mentioned: aralkanals, particularly mononuclear ar (lower alkanals), such as phenylacet-aldehyde, a-phenylpropionaldehyde, ß-phenylpropionaldehyde, ß-phenyl-n-butyraldehyde, o, m, and p-tolylacetaldehyde and 6-phenylcaproaldehyde; * * * and diarylalkanals, particularly mononuclear diaryl lower alkanals, such as diphenylacetaldehyde, ß, ß-diphenylpropionaldehyde, and a-phenyl-ß-phenylpropionaldehyde. * * (Emphasis added).

We note, as did the board, that the alkyl radicals provided by the above aldehydes all fall within a limited range, none exceeding five carbon atoms, and that the aryl radicals provided by the above aldehydes are all phenyl or hydrocarbon substituted phenyl.

Appellants have not defined the intended scope of the terms "aralkyl" and "mononuclear aralkyl" in their specification. Under the circumstances, we must give those terms their broadest possible meaning in determining just what appellants are claiming as the subject matter which they regard as their invention.³ See In re Sus, 306 F.2d 494, 49 CCPA 1301.

The terms "aralkyl" and "mononuclear aralkyl" are broad terms, but are not objectionable for that reason alone if those terms are supported by the specification and properly define the subject matter described therein. Consonant with the purpose behind section 112, the invention claimed should be no broader than the invention set forth in the written description contained in the specification.

We think the terms "aralkyl" and "mononuclear aralkyl" as used here are broader than the invention described in the specification. Manifestly, the terms "aryl" and "alkyl" encompass far more than the phenyl groups and carbon chains of less than five carbon atoms, respectively, which appellants have set forth in their specification. The term "aryl," for example, is broad enough to include multi-ring compounds, mention of which we do not find in appellants' specification. Similarly, the term "alkyl" is sufficiently broad to include radicals derived from paraffin hydrocarbons of a chain length far greater than five carbon atoms. In their specification, appellants themselves characterize the aldehydes they employ to synthesize the present compounds as "lower alkanals." As we stated in In re Cavallito, 282 F.2d 363, 48 CCPA 720:

* * * Moreover, the selection of the examples and other exemplary material used as the disclosure to support a claim must be adequately representative of the area covered by it. In some instances a limited disclosure which is typical of various areas covered by a claim may be of greater value in determining the patentable characteristics of the claimed compounds than a more extensive disclosure would be if related only to a limited portion of the area.

Thus it seems to us that one skilled in the art would learn from the specification that certain aryl or alkyl radicals would be suitable for the purposes of the invention, not that any aryl radical or alkyl radical would be so suitable. In re Sus, supra. There is no question but that the disputed terms — though they are the same as the terms used in the specification — are so broad that they embrace subject matter not described to be appellants' actual invention by means of adequate representative examples. See also In re Holmen, 347 F.2d 852, 52 CCPA 1626; In re Cavallito, 306 F.2d 505, 49 CCPA 1335.

We affirm the rejection of claims 15 and 16 under section 112.

The Rejection on Margerison

The issue presented by the Patent Office rejection of claims 2-4, 15 and 16 as "unpatentable over" the Margerison patent is one which, insofar as we are aware, has never been before this court in the present context.

The Margerison patent 3,095,446, issued June 25, 1963, on an application filed May 12, 1959, relates to processes for the preparation of certain 7-sulfamyl-3, 4-dihydro-1, 2, 4-benzothiadiazine-1, 1-dioxides of the general formula

The generic formula of Margerison reproduced above includes within its scope the compounds of appellants' claims, and a hindsight selection from the column-long list of appropriate substituents disclosed by Margerison⁴ yields the compounds of appellants' narrowest claims, claims 3 and 4. One of the processes disclosed by the Margerison patent for preparing the compounds appears identical to appellants' process in all material respects. The compounds so disclosed are said to be useful as diuretic agents to relieve excess water and/or salt retention, or to relieve states of hypertension.

The examiner noted that the Margerison patent specification states that it is "a continuation-in-part application of our application Serial No. 763,806, filed September 29, 1958 (now abandoned)." (Emphasis added). The '806 application reproduced in the record before us discloses several closely related processes for preparing compounds having a generic formula which, for purposes here, may be said to be identical to that disclosed in the issued patent. A comparison of the generic disclosure and the nature of the substituents on the benzothiadiazine nucleus as disclosed in the Margerison patent with the abandoned application reveals them, in the words of the board, "to be strikingly parallel." Thus, in both the Margerison patent and abandoned application, R2' and R2" may be hydrogen; and R3 and R1 may be, among many other things, trifluoromethyl and benzyl or 2-phenylethyl, respectively. It seems to be generally agreed between appellants and the Patent Office that the appellants' process for preparing the compounds is not described in the '806 application.⁵

While the examiner rejected all claims as "unpatentable over" the Margerison patent, it seems clear from his Answer that he at least⁶ does not rely on anything described above as being disclosed either in the Margerison patent or in the abandoned application for evidence that appellants are not the first inventors of the presently claimed subject matter. Rather, the examiner turned to Example 2 of the abandoned '806 application, which discloses the preparation of 6-chloro-7-sulfamyl-3,4-dihydro-2-H 1, 2, 4-benzothiadiazine by first reacting 5-chloro-4-sulfamyl-aniline-2-sulfonyl chloride with paraformaldehyde to form 5-chloro-4-sulfamyl-N- chloromethylaniline-2-sulfonyl chloride, and then reacting the latter compound with ammonia to yield the desired product. The last paragraph of Example 2 was particularly relied upon by the examiner. It reads:

Other sulfamyl-aniline-2-sulfonyl chlorides, aldehydes or amines may be used in the above process; for example, 5-methyl-4-sulfamyl-aniline-2-sulfonyl chloride, 5-trifluoromethyl-4-sul- famyl-aniline-2-sulfonyl choride or 5-chloro-4- (N-methyl-sulfamyl)-

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