DEUTSCHE GOLD-UND SILBER-SCHEID. v. Commissioner of Patents

Decision Date08 February 1966
Docket NumberCiv. A. No. 3012-63.
Citation148 USPQ 412,251 F. Supp. 624
PartiesDEUTSCHE GOLD-UND SILBER-SCHEIDEANSTALT VORMALS ROESSLER, Plaintiff, v. COMMISSIONER OF PATENTS, Defendant.
CourtU.S. District Court — District of Columbia

Jennings Bailey, Jr., Hugo Huettig, Jr., Bailey, Stephens & Huettig, Washington, D. C., for plaintiff.

Raymond E. Martin, Solicitor's Office, U. S. Patent Office, Washington, D. C., for defendant.

JACKSON, District Judge.

This is a civil action under 35 U.S.C. § 145 in which plaintiff, assignee of Schuler et al. patent application Serial No. 56,702, entitled "Thiophenylpyridyl Amine, Chlorothiophenyl-Pyridyl Amine, Their Salts and Preparation", seeks an adjudication that it is entitled to receive a patent for the invention specified in Claims 1 and 2 of said application.

Claim 1 of the application reads as follows:

1. A thiophenylpyridyl amine compound selected from the group consisting of compounds of the formula
wherein X is selected from the group consisting of H and chlorine, their hydrochlorides and their sulfates.

Claim 2 is directed to the specific thiophenylpyridyl amine compound of claim 1 wherein X is hydrogen. This chemical species is also identified as 1-azaphenothiazine. Claim 3, directed to a process for production of the compounds of Claim 1, was withdrawn from this action prior to trial.

Plaintiff's application Serial No. 56,702, filed September 19, 1960, is a division of parent application Serial No. 537,896 (now U. S. Patent No. 2,974,139), filed September 30, 1955. During prosecution of the parent application priority under 35 U.S.C. § 119 of a German application filed October 2, 1954 was claimed. Although priority of the original German application was not claimed for the divisional application in suit, it is nevertheless entitled under 35 U.S.C. §§ 120, 121 "to the benefit of the filing date of the original application" which, according to 35 U.S.C. § 119, is October 2, 1954, the original German filing date, which is also the date of invention for the invention of the divisional case under 35 U.S.C. § 104.

Defendant contends that the claimed subject matter, and particularly 1-azaphenothiazine, is unpatentable under 35 U.S.C. § 103 since "the differences between the subject matter sought to be patented and the prior art are such that the subject matter as a whole would have been obvious at the time the invention was made (October 2, 1954) to a person having ordinary skill in the art to which said subject matter pertains."

Although other references were relied upon by the Patent Office in rejecting process claims which are not now before the Court, the four references relied upon by defendant in rejecting product Claims 1 and 2 are as follows:

The Chemical Abstracts Index discloses the names and structural formulas of various chemical compounds without any indication as to their properties or utilities. The parties agree that this reference discloses substituted 3-azaphenothiazines. Defendant also contends that the references disclose the structural formula of unsubstituted 3-azaphenothiazine, which is a ring position isomer of plaintiff's claimed 1-aza compound. However, no literature reference is provided in the index for the unsubstituted 3-azaphenothiazine, which indicates clearly that the structural formula of this 3-aza isomer is listed in Chemical Abstracts only for indexing purposes. The reference also discloses the structural formulas of 1-, 2-, and 3-azaphenoxazines. The 1-aza compound is the oxygen analogue of plaintiff's claimed 1-azaphenothiazine, with oxygen substituted in place of sulfur.

The Petrow et al. article discloses the synthesis of 3-azaphenothiazines as well as the fact that "biological examination of these new azaphenothiazines * * * did not reveal any outstanding activity". In discussing the process of preparation analogous to that which plaintiff used for synthesis of its claimed 1-aza isomer, Petrow et al. said that "we were not able to convert any of these diphenylamine analogues into the azaphenothiazines by the known standard methods." Lastly, the reference article states that two substituted 3-azaphenothiazines were "too insoluble to give results of value", when tested for "therapeutic activity".

Takahashi et al. disclose substituted 2-azaphenothiazines by name, but both parties agree that, according to the system of nomenclature commonly used in the United States, these reference compounds are really substituted 4-azaphenothiazines. Takahashi et al. likewise do not indicate any therapeutic activity, effects, properties or utilities for their substituted 4-aza compounds.

Rath discloses in Example 15 of his patent the compound 1,9-diazaphenothiazine, which is the diaza analogue of plaintiff's 1-monoaza compound. Rath is the only one of the four references relied upon by the defendant which provides some indication of therapeutic utility for the disclosed compounds, which are said "to be distinguished by relatively low toxicity and valuable physiological effects based on their capacity of stabilizing the vegetative and central nervous system, accompanied by essentially reduced side effects".

None of the references broadly or specifically disclose plaintiff's claimed 1-azaphenothiazines, and it is undisputed that, according to the record in this case, the compounds were new at the time of the invention, October 2, 1954.

Defendant contends that the four references, when combined, suggest at least the structural formula, if not the pharmacological properties and utilities of plaintiff's claimed unsubstituted 1-aza isomer.

Plaintiff accordingly bases its case on the existence of unexpected beneficial properties in the claimed compounds which serve to overcome any presumption that the compounds themselves were obvious due to the fact that their structural formulas were obvious in view of the prior art references at the time of the invention.

In this regard divisional application Serial No. 56,702 in suit contains the following utility disclosures:

"The new compounds can be directly used as medicaments, such as, for example, as vermicides, furthermore they are valuable intermediates for the production of pharmaceuticals, such as in the production of the N9-dimethyl amino isopropyl thiophenyl pyridyl amine, by reaction with dimethyl amino isopropyl chloride as described in copending application Serial No. 537,896, filed September 30, 1955, now U. S. patent No. 2,974,139, of which this application is a division".

Parent application Serial No. 537,896, the disclosures of which are incorporated by reference in the divisional application, contains the following additional utility disclosures:

"the new compounds according to the invention are valuable intermediates for the production of pharmaceuticals and can also be directly used as medicaments, for example, as vermicides, sedatives, narcotics, anti-allergy compounds and sympathomimetic compounds".

With regard to the direct utility of plaintiff's claimed compounds as vermicides (anthelmintics), plaintiff introduced evidence which shows that the claimed 1-azaphenothiazine possesses more than one hundred times the anthelmintic effect on ascaris worms of unsubstituted 4-azaphenothiazine, the structural formula of which is suggested by Takahashi et al. The evidence also shows that the unsubstituted 2 and 3-azaphenothiazines have essentially the same anthelmintic activity as the 1-aza ring position isomer of Claim 2 and that the 1-aza compound is the least toxic of the four ring isomers.

Defendant attacks plaintiff's evidence of relative anthelmintic activity of the four isomers on the ground that the tests were conducted in vitro rather than in vivo, i. e., that the compounds were tested on ascaris worms in solution rather than in the intestines of living animals. In view of the facts that the claimed 1-aza isomer was equal or greatly superior in anthelmintic activity to the other three unsubstituted isomers according to the in vitro test, that this test was shown to be internationally used and recognized, that the 1-aza compound proved to be the least toxic of the four isomers in toxicity tests on mice, and that the claimed 1-aza isomer is effective as an anthelmintic agent in living animals according to University Veterinary Department tests, the Court is of the opinion that it is reasonable to conclude that the 1-aza isomer would also be equal or superior as a vermicide to the other three isomers in in vivo tests as well as in in vitro tests. More importantly, none of the prior art references relied upon by defendant contains the slightest suggestion that any azaphenothiazine would have sufficient anthelmintic activity to be effectively useful as a vermicide. When the prior art does not contain the slightest suggestion that the properties of a claimed compound would make it useful for a certain advantageous purpose, then the utility itself is unobvious, and it is unnecessary for an applicant to prove by comparative tests that his compound is more useful for the certain purpose than closely related prior art compounds. See E. I. Du Pont de Nemours and Company v. Ladd, 117 U.S. App.D.C. 246, 328 F.2d 547 (1964); In re De Lajarte, 337 F.2d 870, 52 CCPA 826 (1964).

When the inherent existence of a certain beneficial utility in a claimed compound is itself unobvious, a requirement that an applicant must additionally show that his compound is unexpectedly more useful in comparison with prior art compounds would amount...

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7 cases
  • Commissioner of Patents v. DEUTSCHE GOLD-UND-SILBER-S., ETC.
    • United States
    • U.S. Court of Appeals — District of Columbia Circuit
    • May 8, 1968
    ...that Court's conclusion that the claimed compound would be "equal or superior as a vermicide" when compared with the prior art isomers. 251 F.Supp. at 628. Furthermore, the District Court found that none of the prior art references relied upon suggested that the azaphenothiazines (the claim......
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    ...invalidity of an unexpired American patent cited as a reference against his application. In Deutsche Gold und Silber-Scheideanstalt, etc. v. Commissioner of Patents, 251 F.Supp. 624 (D.C.1966), the Court held that the plaintiff "not only has the statutory burden of proof under 35 U.S.C. § 2......
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