Application of Anthony

• Decision Date: 11 September 1969
• Docket Number: Patent Appeal No. 8166.
• Citation: 162 USPQ 594,414 F.2d 1383
• Parties: Application of William C. ANTHONY.
• Court: U.S. Court of Customs and Patent Appeals (CCPA)

162 USPQ 594, 414 F.2d 1383 (1969)

Application of William C. ANTHONY.

Patent Appeal No. 8166.

United States Court of Customs and Patent Appeals.

September 11, 1969.

COPYRIGHT MATERIAL OMITTED

Joseph K. Andonian, Kalamazoo, Mich., attorney of record, for appellant; Eugene O. Retter, Kalamazoo, Mich., of counsel.

Joseph Schimmel, Washington, D. C., for the Commissioner of Patents; Leroy B. Randall, Washington, D. C., of counsel.

Before RICH, Acting Chief Judge, HOLTZOFF and McLAUGHLIN, Judges, sitting by designation, ALMOND and BALDWIN, Associate Judges.

BALDWIN, Judge.

This appeal is from a decision of the Patent Office Board of Appeals affirming the examiner's rejections of claims 1-12¹ "for lack of utility under 35 U.S.C. 101" and of claims 1-6, 11, and 12 as obvious under 25 U.S.C. § 103 in view of certain prior art.

The invention relates to particular chemical compounds, the d- and 1- isomers of a-ethyltryptamine (hereafter denoted by its generic name, etryptamine); therapeutic compositions containing certain amounts of one of the two pure isomers or their racemic mixture in combination with a pharmaceutical carrier; and methods of using those compositions in treating mental depression in humans. Claims 1 and 7 are representative:

1. A therapeutic composition comprising: as the primary active ingredient, from about 5 to about 300 mg. of a compound selected from the group consisting of a-ethyltryptamine and physiologically acceptable acid addition salts thereof, dispersed in a pharmaceutical carrier.

7. A method for treating mental depression which comprises: administering, in unit dosage form, a composition containing from about 5 to about 300 mg. of a compound selected from the group consisting of a-ethyltryptamine and the physiologically acceptable acid addition salts thereof, dispersed in a pharmaceutical carrier to a depressed subject.

Inasmuch as the issues are quite diverse, we shall treat them separately.

The Section 103 Rejection

The references are:

British specification (Young), 807, 876, January 21, 1959.

Snyder, J. Am. Chem. Soc., Vol. 69, pages 3140-3142 (1947).

Karrer, Organic Chemistry, 2nd Ed., pages 92-102 (1946).

Appellant has acknowledged, both below and here, that Young and Snyder each disclose the racemic mixture of etryptamine per se to be known to the art. Young, for example, discloses a process for preparing various indoles including, inter alia, 3-beta-aminobutylindole, another name for etryptamine. The indole compounds in general are said to be useful "as pharmaceutical products and also as intermediates in the manufacture of compounds of pharmacological utility, particularly of 5-hydroxytryptamine." Snyder, on the other hand, discloses techniques for the preparation of various derivatives of tryptamine including, among other things, the acetate of etryptamine. The various derivatives of tryptamine disclosed by Snyder are said to be "of interest * * * because of the physiological activity of the parent base."

The examiner rejected claims 1-6, 11 and 12 as obvious in view of either Young or Snyder alone or considered with Karrer. In the examiner's view, Young and Snyder state that etryptamine is "useful as a pharmaceutical product" and that the acetates of tetryptamine are of interest "because of their physiological activity." Under those circumstances, it would be a routine matter, the examiner thought, for one of ordinary skill in the art to prepare therapeutic compositions containing a pharmaceutical carrier and the racemic mixture of etryptamine or, in light of Karrer's discussion of separating optical isomers of a racemic mixture, to isolate the individual isomers and prepare therapeutic compositions containing them. The board agreed.

With respect to claims 11 and 12, directed to the d- and 1- isomers of etryptamine per se, appellant acknowledges here that those claims are unpatentable on the record since "under existing law a stereoisomer is not patentable over its known racemic mixture unless it possesses unexpected properties not possessed by the racemic mixture."² He asks this court to remand the case to the Patent Office for consideration of new evidence in the form of an affidavit of one Stucki, filed after the board's decision, which appellant apparently believes now shows that the d- and 1- isomers have different, perhaps unexpected, properties. The board refused to consider the affidavit because, in its view, appellant had neither proceeded in accordance with the governing Rules of Practice of the Patent Office nor timely filed that document. We agree with the board's stated reasons for refusing to consider the affidavit, and appellant does not ask us to consider it in the first instance here. Cf. In re Pantzer, 341 F.2d 121, 52 CCPA 1135 (1965). Inasmuch as appellant seemingly was aware of the necessity for such evidence early in the prosecution, and the affidavit does not appear to be in response to any new ground of rejection under § 103 advanced for the first time by the board,³ appellant's request for remand is denied, although he perhaps is not without further recourse.⁴ The rejection of claims 11 and 12 under § 103 is affirmed.

Insofar as the rejection of claims 1-6 is concerned, appellant argues that the two prior art references employed by the Patent Office do not suggest any general or specific therapeutic use for any specific compound, and are so vague as not to provide any meaningful teaching by which the claimed compositions are rendered obvious to one of ordinary skill in the art. The board's reliance on In re Rosicky, 276 F.2d 656, 47 CCPA 859 (1960) in support of its position is misplaced, appellant says, because there composition claims similar in form to those here were held unpatentable over a group of prior art compounds, including the active ingredients of the claims, which, in contrast to the present case, were disclosed to have the very same specific pharmaceutical utility as did the active compounds of the claimed compositions. It was in those circumstances the court held that the mere formulation of pharmaceutical compositions containing certain amounts of the active ingredients of the prior art and a pharmaceutical carrier would be obvious to one of ordinary skill in the art.

We agree with appellant. Snyder's disclosure that the "derivatives" of tryptamine are merely "of interest" because "of the physiological activity of the parent base" is no indication at all that etryptamine itself necessarily has some nebulous "physiological activity" of the parent base (tryptamine) in fact, much less what specific activity that would be. Similarly, Young's disclosure that many widely divergent indoles which can be prepared by his process are useful as "pharmaceutical products" is no clear suggestion that etryptamine itself necessarily has such utility, whatever that may be.⁵ In our view, absent a disclosure by Young or Snyder of specific therapeutic or pharmaceutical uses for etryptamine, the addition of a pharmaceutical carrier to that compound and the determination of suitable unit dosage forms is not obvious. We do not think it is reasonable to assume, as the Patent Office seemingly has, that researches would as a matter of course incorporate chemical compounds in specific amounts into pharmaceutically acceptable carriers and dosage unit forms unless they had some reasonably specific pharmaceutical use in mind. The recitation in the claims of certain amounts of active ingredient in combination with the carrier provides some further measure of distinction over the art, inasmuch as the references do not suggest the use of any particular amounts of etryptamine. Cf. In re Wiggins, 397 F.2d 356, 55 CCPA 1356 (1968).

The rejection of claims 1-6 under § 103 is reversed.

The Section 101 Rejection

This issue — which relates in general to the safety and concomitant usefulness of appellant's compositions and process in treatment of mental depression in humans — appears to be one of first impression. The following background information will facilitate an understanding of our resolution of that issue.

Appellant's present specification sets forth the usefulness of his compositions as follows:

In extensive clinical studies on compositions containing a representative a-ethyltryptamine salt, both its clinical effectiveness and safety have been demonstrated in the treatment of mental depressions of the endogenous, organic, involutional and reactive types, as well as in undefined psychosomatic disorders characterized by a depressive phase. Significant success has also been obtained in treating angina pectoris, rheumatoid arthritis and other conditions.⁶

In the clinical investigations conducted with a-ethyltryptamine acetate no evidence of liver toxicity has been observed, in contradistinction to experience with certain of the hydrazine compounds. An extremely low incidence of agranulocytosis has been as- sociated with its use, but investigators have reported its safety generally to be one of its outstanding characteristics. Of particular importance clinically is the rapid reversibility of activity, effects being dissipated in 24-48 hours after cessation of therapy. This factor, coupled with the early onset of the desired psychic energization or mood enhancement which follows initiation of therapy, provides a high degree of positive control. Following is a summary of results obtained in the treatment of some of the clinical conditions in which the present compositions have proved significantly effective:

                Clinical        Investigators    Number of     Percent
                Condition         Reporting      Patients      Benefit
                Endogenous
                  depression         21            141           82%
                Reactive
                  depression         12             47           74%
                Unclassified
                  depressions        20            207           66%
                *      *      *      *      *      *      *      *
                                                 Emphasis supplied
                

As corroborating evidence of the...