Application of Ruschig

Citation343 F.2d 965
Decision Date22 April 1965
Docket NumberPatent Appeal No. 7254.
PartiesApplication of Heinrich RUSCHIG, Walter Aumüller, Gerhard Korger, Hans Wagner, Josef Scholz and Alfred Bänder.
CourtUnited States Court of Customs and Patent Appeals

George E. Frost, Chicago, Ill., Henry W. Koster, New York City, Eugene Retter, John Kekich, Kalamazoo, Mich., for appellants.

Clarence W. Moore, Washington, D. C. (Joseph Schimmel, Washington, D. C., of counsel), for the Commissioner of Patents.

Before WORLEY, Chief Judge, and RICH, MARTIN, SMITH, and ALMOND, Judges.

RICH, Judge.

This appeal is from the decision of the Patent Office Board of Appeals affirming the examiner's rejection of claims 1-6 and 8-13 of application serial No. 601,107, filed July 31, 1956, for a patent on "New Benzene Sulfonyl Ureas and Process for their Preparation." All appealed claims are directed to compounds. The appeal from the examiner to the board was on claims 1-13 but in his answer before the board the examiner said, "upon reconsideration claim 7 is deemed allowable."

The board's opinion recites the fact that there were other claims, 17 and 19-25, referred to as the "non-elected" claims herein, "directed to the process of lowering blood sugar in the treatment of diabetes by the oral administration of, and to pharmaceutical tablets containing, compounds recited in substantially the same manner as in compound claims 1, 2, 3 and 13" (our emphasis) but that the examiner required restriction as between those claims and the claims here on appeal, as a result of which "A divisional application containing claims 17 and 19 to 25 as claims 1 to 8 thereof has been filed and is pending."1 We see no relevancy of these facts to the issue of the patentability of the claims to the compounds before us but recite them because the board, possibly the examiner, and certainly the solicitor for the Patent Office seem to have had them in mind in stating their reasons for rejection, as will appear.

The Invention

The invention here is more than the making of new compounds in the abstract. The field of endeavor in which the claimed invention is found is the production of an oral medication for the control of diabetes mellitus, the common type of diabetes long treated by daily injections of insulin. As is well known, a characteristic of the disease is an abnormal amount of sugar in the blood due to insulin deficiency.

The obvious practical disadvantages of the hypodermically injected insulin gave rise to research to discover and develop an oral medication to take its place and as a result of this research of recent years a few such oral pharmaceuticals have become available. One of them is sold under the trademark "Orinase," which has the descriptive name tolbutamide2 and is N-(4-methyl-benzenesulfonyl)-N'-n-butyl urea. Another one developed later and approved for marketing by the Federal Food and Drug Administration in November 1958, is sold under the trademark "Diabinese," which has the descriptive name chlorpropamide and is N-(4-chloro-benzenesulfonyl)-N'-n-propyl urea. This compound is the subject matter of claim 13 on appeal of the application at bar where it is designated "N-(P-chloro-benzenesulfonyl)-N'-propylurea," the graphic formula of which is

We have marked the "4" position of the chlorine, which is also the para or "p" position. It is interesting to compare this with allowed claim 7, which reads:

7. The compound of the formula

It will be useful in this discussion to bear in mind the basic nomenclature of such compounds as the above. They are of the general class of sulfonyl ureas. The sulfonyl group is the -SO2-. Urea is NH2-CO-NH2 and these compounds are substituted ureas. It will be noted that urea has two N (nitrogen) atoms and to distinguish them in substitution products they are conventionally referred to as N and N'. We will hereafter refer to the nitrogen atom bearing the sulfonyl group as N. In the above claims it will be seen that one of the H (hydrogen) atoms attached to N has been replaced or substituted by the chlorobenzene-sulfonyl group. In claim 13, above, one of the hydrogens attached to N' has been substituted by the propyl group -C3H7, an alkyl group having 3 carbon atoms. In claim 7 the same H has been substituted by a cycloalkylalkyl radical, cyclohexymethyl, -CH2- or methylene attached to the hexagon containing "H" representing a cyclohexyl or -C6H11 ring, not to be confused with the benzene ring. Thus there is always the urea group -NH-CO-NH-, preceded by the benzene-sulfonyl group, on the ring of which there may be one or more additional substituents like C1-, and followed by an N'-substituent.

Claims 7 and 13, above, are two of ten species claims in the application, the other claims being generic (claims 1 and 2) or subgeneric (claims 8 and 9). Of the broad claims the board selected claim 2 for purposes of its analysis of the patentability issue. It reads:

2. Benzenesulphonylureas of the formula wherein R is chlorine and R2 is alkyl of 2 to 7 carbon atoms.

Claim 1 is the broadest, generic to all species claimed but still defining a limited class, and it reads:

1. Compounds selected from the group consisting of (1) benzenesulphonyl ureas of the formula

wherein R is selected from the group consisting of hydrogen, chlorine, bromine, methyl and methoxy, R1 is selected from the group consisting of chlorine and bromine and R2 is of 2 to 7 carbon atoms selected from the group consisting of alkyl-, alkenyl-, cycloalkyl- and cycloalkylalkyl atoms sic and (2) non-toxic basic addition salts thereof.3

The board put some emphasis on the fact that the claims on appeal define compounds "without limitation," which we presume adverts to the lack of any reference in these compound claims to a use for them, though it would not seem that reference to a use in a compound claim would in law be a "limitation," on the question of patentability, a point we need not go into. See In re Thuau, 135 F.2d 344, 30 CCPA 979, and In re Jones, 149 F.2d 501, 32 CCPA 1020. Perhaps the board's observation was stimulated by the following statement in the concluding paragraph of the examiner's answer before the board:

The claims are directed to compounds and not to the use of these compounds in any particular manner. Appellants do not, however, recognize the necessity for this conjunction of utility and product in the claims presented but seek a patent on the compounds per se. Emphasis ours.

We confess a failure to grasp what the examiner intended by that observation, made as part of his insistence that the compounds are unpatentable because they would be obvious from the prior art, under 35 U.S.C. § 103, unless it be that in his view applicants are entitled only to claims for a process of treating diabetes. Would a statement in the claims of what the compounds are useful for convert them into claims to compounds which are any less obvious? It is the compounds the examiner says are obvious, not the claims, and it is compounds which the claims define.

To return to our consideration of the place of this invention in the useful arts, these compounds, as here defined in generic and specific claims, have been discovered to have a particular utility which is extensively described in the specification and further expounded in five of the nine affidavits of record.

The claimed compounds fall into the general class of sulfonylureas, which the Patent Office admits may number in the millions. Those singled out here for patenting have been discovered by appellants, as a result of their systematic, extensive, and presumably expensive research, to possess the ability to lower the level of blood sugar (known as hypoglycemic activity), for which reason they are useful in treating diabetes, but particularly because of other desirable properties they possess in connection with such use. We quote relevant passages from the specification:

As has been demonstrated by experiments on animals and in clinical tests, the products of the invention produce a substantial lowering of the blood sugar level. They may be used as such or in the form of their salts, or in the presence of substances that cause salt formation. * * * These salts have the same blood sugar lowering properties. * * * The compounds can be made up, inter alia, into preparations suitable for oral administration and lowering the blood sugar in the treatment of diabetes.
* * * * * *
In animal tests the action on the blood sugar level has been demonstrated, for example, on mice, rats, guinea pigs, rabbits, cats and dogs.
* * * * * *
The testing of the compounds on dogs has the advantage that the resorption conditions in the alimentary canal are similar to those of human beings, and that the blood sugar level exhibits smaller individual variations than in rabbits. * * *
* * * * *
As compared with compounds of similar constitution of the sulphanilyl series the compounds of the present invention are distinguished, on one hand, in that they are more resistant to external oxidising influences, such as atmospheric oxygen, which is of importance to their shelf-life and handling, and, on the other, in that they have no bacteriostatic action.
Furthermore, the new compounds do not produce the secondary effects of sulphonamides on the blood (Heinz bodies) or on the thyroid gland, nor the digestive disturbances caused by action on the bacterial flora of the alimentary tract. * *

Together with these general statements there are included two tables, the first giving the specific blood sugar level reduction produced in rabbits by ten specific compounds here claimed, the second showing the lowering of blood sugar in the dog at various periods after administration, the showing being that the hypoglycemic activity of the compounds of species claims 3 and 5, at least, is long lasting. To illustrate, the figures for N - (4-chloro-benzenesulfonyl) - N' - n-butyl-urea, the claim 3 compound, are:

                  % sugar level lowering .......... 27  40  40
...

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42 cases
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    • United States Courts of Appeals. United States Court of Appeals (District of Columbia)
    • May 8, 1968
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    ...reference containing them, to create hindsight anticipations with the guidance of an applicant's disclosures." In re Ruschig, 52 C.C.P.A. 1238, 343 F.2d 965, 974 (1965); see also Eli Lilly & Co. v. Zenith Goldline Pharms., Inc., 364 F.Supp.2d 820, 900 (D.Ind.2005). Apotex's case for anticip......
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    ...inspection of the dials thereof.")) Focusing on this issue, the United States Court of Customs and Patent Appeals in In re Ruschig, 343 F.2d 965, 994, 52 CCPA 1238 (1965) found that the possibility of 48 compounds resulting from the unguided teachings of the prior art was too broad a class ......
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    ...would be obvious to modify Lyle's glass, a "103 rejection" must be reversed. Id. at 875, 143 USPQ at 259. In In re Ruschig, 343 F.2d 965, 52 CCPA 1238, 145 USPQ 274 (CCPA 1965) the court again observed that the invention "indeed, is a 'conjunction of utility and product', though claimed as ......
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    • United States
    • Albany Law Review Vol. 74 No. 1, September 2010
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    ...a "return to a practical standard of invention" that emphasizes the phrase "useful arts" rather than "science"). (188) See In re Ruschig, 343 F.2d 965, 970 (C.C.P.A. 1965) ("[I]s it not also evident that a patent system must be related to the world of commerce rather than to the realm of ph......
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    ...56 Id. at 536 ("[W]hat now seems without 'use' may tomorrow command the grateful attention of the public."). 57 Id. (citing In re Ruschig, 343 F.2d 965, 970 (C.C.P.A. 1965)). 58 Id. at 534 ("Such a patent may confer power to block off whole areas of scientific development, without compensat......
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    ...273 (1976). [9]Ex Parte Murphy, 200 USPQ 801 (Bd. App. 1977). [10]383 U.S. 519 (1966). [11]Id. at 536 (quoting Application of Ruschig), 343 F.2d 965, 970 (2nd Cir. 1965). [12]35U.S.C.A. § 102(b). [13]See Egbert v. Lippmann, 104 U.S. 333 (1881). [14]Id. at 339, Miller, J., dissenting. [15]TP......

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