Application of Petering

Citation133 USPQ 275,301 F.2d 676
Decision Date13 April 1962
Docket NumberPatent Appeal No. 6750.
PartiesApplication of Harold G. PETERING and Harry H. Fall.
CourtUnited States Court of Customs and Patent Appeals

George T. Johannesen, Kalamazoo, Mich. (Eugene O. Retter, Washington, D. C., of counsel), for appellants.

Clarence W. Moore, Washington, D. C. (Raymond E. Martin, Washington, D. C., of counsel), for the Commissioner of Patents.

Before WORLEY, Chief Judge, and RICH, MARTIN, and SMITH, Judges, and Judge JOSEPH R. JACKSON, Retired.

MARTIN, Judge.

This is an appeal from a decision of the Board of Appeals of the United States Patent Office which affirmed the examiner's rejection of claims 1, 2, 4, 5, 7, and 10-12 of appellants' application for a patent on "Isoalloxazines." Eighteen claims stand allowed by the examiner. The application was filed September 7, 1954.

The following appealed claims are representative:1

"1. Compounds represented by the formula:
wherein R is an -monohydroxyalkyl group containing from two to six carbon atoms inclusive, R3 and R4 are members selected from the group consisting of lower-alkyl, lower-alkoxy, amino and a polymethylene group linked to the aromatic ring to form a carbocyclic ring having six carbon atoms, R2 and R5 are members selected from the group consisting of hydrogen, lower-alkyl, lower-alkoxy and amino, and wherein R2, R3, R4 and R5 when taken together include not more than one amino group.
"2. Compounds represented by the formula:
wherein R is an -monohydroxyalkyl group containing from two to six carbon atoms inclusive and R3 and R4 are lower-alkyl.
"10. 6, 7-Dimethyl-9-ß-monohydroxyethyl-isoalloxazine.
"11. 6, 7-Diethyl-9-ß-monohydroxyethyl-isoalloxazine.
"12. 6-Ethyl-7-methyl-9-ß-monohydroxyethyl-isoalloxazine."

Claims 4, 5 and 7 are subgeneric to claim 2. In claim 4, R3 and R4 are methyl, CH3. In claim 5, R3 and R4 are ethyl, C2H5. In claim 7, R is -CH2CH2OH. Otherwise, claims 4, 5 and 7 are identical with claim 2.2

The allowed product claims are subgeneric to claim 1 in that R2 and R5 are hydrogen while at least one of the R3 and R4 groups is amino or alkoxy. Certain claims to a process of producing the claimed compounds have also been allowed.

The reference relied on by the examiner and the board is:

Karrer 2,155,555 April 25, 1939.

As the claims indicate, this application relates to a group of isoalloxazines and to a method of preparing them. The issue is whether the subject matter of the appealed claims is patentable in view of the Karrer patent.

The only relevant part of the application concerning utility of the claimed compounds is as follows:3

"These new and novel compounds possess antimetabolite activity; for example, they are competitively active riboflavin antagonists."

The Karrer patent is entitled "Iso-Alloxazine Derivatives and Process for the Manufacture of Same." The Karrer process is not the same as appellants' process. Karrer's isoalloxazines are expressed by the following generic formula:

wherein X, Y, Z, P and R' represent either hydrogen or alkyl radicals, R a side chain containing an OH group * * *".

Karrer discloses that R may be "for instance -CH2OH, -CH2CH2OH, -CH2CH(OH)CH2OH, -CH2CH(OH)CH(OH)-CH(OH)CH2OH, or -CH2 (CHOH)4-CH2OH." Also disclosed are eight specific isoalloxazines all encompassed by the generic formula. We tabulate these as follows:

                  X        Y        Z         P        R'              R
                  H        H        H         H        H        -CH2CH(OH)CH2OH
                  H        CH3      CH3       H        H        -CH2CH(OH)CH2OH
                  H        H        H         H        H        -CH2CH2OH
                  H        H        H         H        H        -CH2(CHOH)3CH2OH
                  H        CH3      CH3       H        H        -CH2(CHOH)3CH2OH
                  H        CH3      H         H        H        -CH2(CHOH)4CH2OH4
                  H        CH3      CH3       H        H        -d,l'-ribityl5
                  H        CH3      H         H        H        -d,l'-ribityl
                

There are three portions of the Karrer patent which relate to utility. First, shortly after setting forth his generic formula, supra, Karrer states:

"* * * Neither alloxazine and its derivatives substituted in the benzene ring, nor N-methyliso-alloxazine possess any vitamin action, whereas the new compounds very decidedly influence the growth."

Second, regarding the last compound in our table, supra, Karrer states:

"* * * In the biological test it has the same influence on the growth as vitamin B2 (lactoflavine)."

Finally, the two claims of Karrer are pertinent with regard to utility and are as follows:

"1. The 7-methyl-9-d,l\'-ribityl-iso-alloxazine, the new compound crystallizing in yellow needles melting at 275° C., dissolving in water with yellow colouring and having an influence on the weight increase of test animals characteristic for vitamin B2.
"2. The compounds of the formula
wherein Y is an alkyl radical, R1 is selected from the group consisting of hydrogen and alkyl radicals, and R is a hydroxylated side chain, the compounds dissolving in water with yellow coloring, being very sensitive to light and having an influence upon the weight increase of test animals chacteristic of vitamin B2."

The examiner rejected the appealed claims "as lacking invention over Karrer who discloses generically the claimed compounds and sets forth specifically a homolog."6 The examiner considered the third compound in our table supra, to be a "homolog of the claims," and stated:

"* * * Applicants have failed to submit a verified affidavit as required by the Examiner showing unusual or unforeseen properties to overcome prior art homologs. * *"

As authority for this requirement, In re Hass et al., 141 F.2d 122, 31 CCPA 895, and In re Henze, 181 F.2d 196, 37 CCPA 1009, were cited. In response to appellants' alleged argument that "the patent teaches that the compounds claimed have utility directly opposite to the compounds instantly claimed and that no showing over the prior art homologs is necessary,7 the examiner expressed the opinion that the first statement from Karrer that his "new compounds very decidely influence the growth" was broad enough to include retarding growth as well as promoting growth, and that the other pertinent statements in Karrer relate only to specific compounds and not to all of the compounds encompassed by the Karrer disclosure. The examiner stated:8

"* * * The choosing of certain compounds falling within the sphere taught by Karrer and determining that these compounds have antimetabolite activity i. e. prevent growth is not invention. It represents that which is taught by Karrer when he disclosed that his compounds influence the growth."

The board affirmed the examiner's rejection generally. In response to appellants' argument that the Karrer general formula is broad and that many choices must be made to arrive at appellants' compounds, the board related Karrer's specific examples to his generic formula, supra, and came to the conclusion that the "formula is not as broad and the range of selection not as great as appellants would make it appear." Relative to the issue between appellants and the examiner as to the differences in properties between Karrer's compounds and appellants' compounds, the board stated:

"* * * It is not clear that Karrer intends the possession of vitamin activity to refer to all compounds of the class or all those disclosed since the statement is explicitly made only with respect to some of them but we are not convinced that the ascertainment of the property referred to could make such obvious compounds unobvious as compounds."

Appellants urge that the Patent Office has "clearly erred in holding the claimed compounds to be obvious and unpatentable" and asks that we reverse "their action in so doing."

First we will consider the statements of Karrer relating to the properties of the compounds disclosed in his patent. It is noted that the board expressed doubt on this issue. It is our opinion that no portion of that patent teaches any relevant property for any of those compounds, specific or generic, other than, in the words of the examiner, a "positive vitamin like activity." In view of this record, we do not believe Karrer teaches one skilled in this art that any compound encompassed by his disclosure has or might have a negative influence on growth. It may be that the phrase in Karrer, "the new compounds very decidedly influence the growth," when taken out of context, includes both a positive and a negative influence on growth, but this phrase occurs in the same sentence, as set forth supra, with a reference to "any vitamin action." We are unable to accept the suggestion that "any vitamin action" includes an anti-vitamin action. In our opinion, Karrer contemplated and was discussing only a positive "vitamin action" and indeed only a positive vitamin B2 action when he stated that his "new compounds very decidedly influence the growth."

The solicitor urges us to consider the following dictionary definition of "antimetabolite":9

"Antimetabolite: A substance having a molecular structure similar to but a pharmacologic effect antagonistic to a metabolite (i. e. a vitamin or a hormone). The mechanism of antagonism is considered to be a competition between antimetabolite for a specific protein in an organism."
The solicitor states:
"This definition would suggest to skilled workers in the art that one or more compounds coming within the general formula of Karrer, such as one of the compounds produced in his specific examples, or one differing slightly therefrom, would act as antimetabolites."

First, we again point out that we believe Karrer intended to include and did include all of his compounds, specific and generic, when he stated, "the new compounds very decidedly influence the growth." Second, there is no evidence whatever in the record other than in appellants' own specification that any compound "coming within the general formula of Karrer" is known to act or would obviously act as an antimetabolite. Finally, it...

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