Application of Kirk

• Decision Date: 10 April 1967
• Docket Number: Patent Appeal No. 7522.
• Parties: Application of David Neville KIRK and Vladimir Petrow.
• Court: U.S. Court of Customs and Patent Appeals (CCPA)

376 F.2d 936 (1967)

Application of David Neville KIRK and Vladimir Petrow.

Patent Appeal No. 7522.

United States Court of Customs and Patent Appeals.

March 16, 1967.

Dissenting Opinions April 10, 1967.

Bacon & Thomas, Washington, D. C. (Jesse B. Grove, Jr., Washington, D. C., of counsel), for appellants.

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

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

WORLEY, Chief Judge.

This appeal is from the decision of the Board of Appeals affirming the rejection of claims 11, 25, 26, 28, 29, 39, 41 and 45 in appellants' application¹ entitled "1-Dehydro-6-Methyl Steroid Compounds."

Each claim defines a specific steroid compound, claim 11 relating to a compound of the spirostane series; claims 25, 26, 28, 29 and 45 to compounds of the androstane series; and claims 39 and 41 to compounds of the pregnane series. It is unnecessary to reproduce any claim since the nature of the compounds will become apparent.

The Patent Office rejected all claims for failure of the specification "to comply with 35 U.S.C. §§ 101 and 112." As we view the record, we are concerned with not only the legal adequacy of appellants' disclosure of "how to use" the claimed compounds under 35 U.S.C. § 112,² but also the legal adequacy of assertions of usefulness in the original specification under 35 U.S.C. § 101.³ We are particularly concerned with the applicability of the decision of the Supreme Court in Brenner v. Manson, 383 U.S. 519, 86 S.Ct. 1033, 16 L.Ed.2d 69, to the facts here.⁴

The appropriate starting point for disposition of those issues is appellants' specification, which begins with several general statements as to how the claimed compounds are useful:

It is an object of the present invention to provide a process for the conversion of 3-oxo-?4-6-methyl and 3-oxo-?4:6-6-methyl steroidal derivatives into the corresponding 1-dehydro-derivatives which are a new class of compounds often possessing high biological activity.

The present invention provides new 1-dehydro-derivatives of 3-oxo-?4:6-6-methyl and certain 3-oxo-?4-6-methyl steroids having the formula

(with or without a double bond at the 6:7 position) which 1-dehydro-derivatives are of value on account of their biological properties or as intermediates in the preparation of compounds with useful biological properties as herein indicated or as is apparent to those skilled in the art.

* * * * * *

The invention also provides the following new steroidal 6-methyl-1:4-dien-3-ones and 6-methyl-1:4:6-trien-3-ones which are of value in steroid technology, in the furtherance of steroidal research and in the application of steroidal materials to veterinary or medical practice, whether as tablets, elixirs, injections, implants, or other types of pharmaceutical preparation well known to those skilled in the art. (Emphasis supplied)

The description continues with lists of specific compounds of the cholestane, spirostane, androstane and pregnane steroid series together with a recital of "uses" for the compounds recited in the lists. Two compounds of the spirostane series are disclosed, one of which, 6-hydroxy - 6 - methyl - 25D - spirosta-1:4-dien-3-one, is the subject of claim 11. They are said to be

* * * of value as intermediates in the preparation of 6-methylated aromatic steroid hormones into which intermediates they may be converted by reaction in solution in acetic anhydride with toluene-p-sulphonic acid. (Emphasis supplied)

Eighteen compounds of the androstane series are disclosed. The five recited in the claims are

17ß - Hydroxy-6:17a - dimethylandrosta-1:4:6-trien-3-one Claim 45

17a - Ethynyl - 17ß - hydroxy - 6 - methylandrosta - 1:4:6 - trien - 3 - one Claim 25

17ß - Acetoxy - 4:6a - dimethylandrosta-1:4-dien-3-one Claim 26

9a - Fluoro - 11ß:17ß - dihydroxy - 6a:17a - dimethyl - androsta - 1:4 - dien-3-one Claim 28

17ß - Hydroxy - 6a - methyl - 17a-(prop-l-ynyl) androsta-1:4-dien-3-one Claim 29

They are said to be

* * * of value as intermediates in the preparation of 6-methylated aromatic steroidal hormones, into which they may be converted by reaction in solution in acetic anhydride with toluene-p-sulphonic acid, as intermediates in the preparation of biologically active compounds and in some cases on account of their biological properties. (Emphasis supplied)

Some sixteen compounds of the pregnane series are disclosed, including the two compounds of claims 39 and 41,

6a - Methyl - 16a:17a - isopropylidenedioxy - pregna - 1:4 - diene - 3:20 - dione Claim 39 and

20:20 - Bisethylenedioxy - 6a - methyl-pregna-1:4-dien-3-one Claim 41.

They are alleged to be

* * * of value as intermediates in the preparation of compounds with valuable biological properties such as progestational properties or properties associated with the adreno-cortical hormones or as intermediates in the preparation of compounds with useful biological properties. (Emphasis supplied)

Appellants' arguments are, in the main, two-fold. They first contend that the specification is adequate to comply with § 101 and § 112 because it discloses that the claimed compounds "have present and useful biological activity of the nature known for analogous steroidal compounds," and that "one skilled in the art would know how to use the compounds of the claims to take advantage of their presently-existing biological activity." The second argument is that the specification adequately discloses that the compounds "have use as intermediates in the production of aromatic steroidal hormones and other biologically useful compounds," and that the examiner has admitted one skilled in the art would know how to use the claimed compounds as intermediates for that purpose. The respective arguments present somewhat different considerations, and will be discussed separately.

I. The Asserted "Therapeutic" or "Biological" Activity

In his final rejection, the examiner stated:

All the claims are again rejected as lacking adequate utility. The disclosure fails to indicate to one skilled in the art how one is to use the novel compounds of this invention. The therapeutic properties are stated in such general terms i. e., "useful biological properties", that it fails to convey any useful information to one skilled in the art and further fails to state which of the claimed compounds have a therapeutic activity. * * *

In response, appellants submitted argument that the rejection "is not warranted," and also submitted an affidavit of one of the applicants, a Dr. Petrow, which appellants summarized in a letter accompanying the affidavit and substantially reiterate in their brief here:

Attached hereto is an affirmation of Vladimir Petrow which shows that one skilled in the art would be able to determine the biological uses of the claimed compounds by routine tests. The Petrow affirmation specifically shows that * * * the steroid of (Claim 25) in the well-known McPhail modification of the Clauberg Assay possesses progestational activity on oral administration. The natural hormone, progesterone, on the other hand shows no response on oral administration in the same test. Accordingly, it is quite evident that the compound of claim 25 is a valuable oral progestational agent. This affirmation, accordingly, is proof of the fact that one skilled in the art would have no difficulty in determining whether or not the 1-dehydro derivatives of the pregnane series, as claimed, have value biologically as progestational agents. (Emphasis supplied)

In addition, the Petrow affirmation * * * discloses the determination of the anabolic activity of * * * the compound of claim 26. It is shown by standard test procedure that this compound does have anabolic activity and that, in addition, it has a much higher anabolic/androgenic ratio than that of testosterone propionate, a well-known anabolic agent. * * *

Further * * * the oral progestational activity of * * * the compound of claim 39, is set forth by virtue of well-known test procedure. This pregnane derivative is shown to be approximately 4 times as active progestationally on oral administration as * * a well-known oral progestational agent. * * * by means of other tests the compound of claim 39 has been found to have valuable anti-inflammatory activity greater than that of either cortisone acetate or hydrocortisone. By virtue of a further standard test procedure the gluco corticoid activity of the compound of claim 39 has been shown to be more than 10 times that of cortisone and hydrocortisone acetates.

The affirmation of Dr. Petrow not only shows that the compounds claimed do have biological activity as asserted in the specification, but that the nature of such biological activity can be readily determined by those skilled in the art by reason of standard test procedures.⁵

Appellants' affidavit and argument went for naught, the examiner responding that

* * * the final rejection of all the claims in the case as lacking an adequate disclosure of utility is deemed sound and adhered to. * * *

In his Answer before the board, the examiner rejected the claims

* * * as failing to comply with 35 U.S.C. 101 and 112 in that the specification fails to teach those skilled in the art how to use the invention. * * *

After reviewing the various passages of appellants' specification relating to the uses of the claimed compounds and "how to use" them, he concluded:

* * * nowhere is there found a specific allegation of utility for any compound within the scope of the claims. Thus the specification does not describe the manner in such full, clear, concise and exact terms as to enable one skilled in the steroid art to use the compounds of the instant invention. * * * Appellants have not listed one specific use for their claimed steroids and as those skilled in the art know steroids are susceptible to hundreds of uses. What appellants are really saying to those in

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