Board of Patent Appeals and Interferences
Patent and Trademark Office (P.T.O.)
*1 EX PARTE RENE HEYMES AND ANDRE LUTZ
Appeal No. 93-1646
November 9, 1993
HEARD: October 5, 1993
Application for Patent filed November 8, 1991, Serial No. 07/789,363, which is a Continuation of Serial No. 07/336,843, filed April 12, 1989 (ABN), which is a Continuation of Serial No. 06/634,148, filed July 24, 1984 (ABN), which is a Division of Serial No. 05/969,208, filed December 13, 1978, now Patent No. 4,476,122, issued October 9, 1984, which is a Division of Serial No. 05/796,315, filed May 12, 1977, now Patent No. 4,202,893, issued May 13, 1980, which is a Continuation-in-Part of Serial No. 05/781,344, filed March 25, 1977 (ABN). Novel Alkyloximes of 7-Amino-Thiazolyl-Acetamiko-Cephalosporanic Acids.
Before Winters, Emery and Garris
Administrative Patent Judges [FN1]
Administrative Patent Judge
This appeal is from the examiner's decision refusing to allow claims 1, 3 through 11 and 17 through 21, which are all of the claims remaining in the application.
Claim 1 is representative:
1. A compound of the formula
wherein R is selected from the group consisting of alkyl of 1 to 5 carbon atoms, cycloalkyl of 3 to 5 carbon atoms and -CH2SR' R' is selected from the group consisting of acyl of an alkanoic acid of 2 to 4 carbon atoms, 1-methyl-tetrazolyl and 2-methyl-1, 3, 4-thiadiazolyl, R1 is a group easily removable by acid hydrolysis or hydrogenolysis, R2 is selected from the group consisting of alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, A is selected from the group consisting of hydrogen, an alkali metal cation, or equivalent of an alkaline earth metal or magnesium, an organic amine base cation and an ester group easily removable by acid hydrolysis or hydrogenolysis and OR2 is in the syn position.
The references relied on by the examiner are:
Ochiai et al. (Ochiai '246) 4,008,246 Feb. 15, 1977
Menard et al. (Menard) 4,011,216 Mar. 8, 1977
Cook et al. (Cook '137) 4,024,137 May 17, 1977
Barth 4,045,436 Aug. 30, 1977
Ochiai et al. (Ochiai '888 4,098,888 Jul. 4, 1978
Takahashi et al. (Takahashi), Chemical Abstracts, "Alkanoyloxyalkyl cephalosporanates", Vol. 78, 111337v (1973).
The issue presented for review is whether the examiner correctly rejected claims 1, 3 through 11 and 17 through 21 under 35 USC 103 as unpatentable over the combined teachings of the above-cited references.
We shall sustain this rejection.
*2 Initially, we note appellants' statement in their main Brief, page 3, that "[a]ll of the claims stand or fall together". Accordingly, for the purposes of this appeal, we shall treat dependent claims 3 through 11 and 17 through 21 as standing or falling together with independent claim 1.
Having reviewed all the references relied on by the examiner, we find that Ochiai '888 and Cook '137 here constitute the closest prior art.
Ochiai '888 discloses a class of compounds which includes a number of the compounds set forth in appealed claim 1. Note particularly compounds having the formula (VII) disclosed by Ochiai '888 in column 1, lines 55 through 68. Also note the relevant definition of R4 (columns 5 and 6) and R5 (columns 7 and 8) and R1 (column 4) in the patent. Ochiai '888 suggests using either the syn or anti isomer of the compounds. Furthermore, the Ochiai '888 patent, like appellants' specification disclosure, relates to cephalosporin-type compounds having antibiotic properties. On these facts, we conclude that the subject matter sought to be patented in claim 1 on appeal would have been prima facie obvious based on Ochiai '888 alone. Generally speaking there is nothing unobvious in choosing "some" among "many" indiscriminately. Some compounds, falling within the scope of a prior art genus, are unpatentable in the absence of a showing of unexpectedly superior results. In re Lemin, 332 F.2d 839, 141 USPQ 814 (CCPA1964); In re Susi, 440 F.2d 442, 169 USPQ 423 (CCPA1971).
The Cook '137 patent further supports the examiner's conclusion of obviousness. That patent discloses cephalosporin-type compounds which have high antibacterial activity against a range of gram-positive and gram-negative organisms and which contain, as an essential feature, an (<<alpha>>??Illegible Text??- etherified oximino) acylamido group. Cook '137 requires that his compounds are syn isomers or exist as a mixture containing at least 75% of the syn isomer. In our judgment, the collective teachings of Ochiai '888 and Cook '137 would have suggested as particularly useful those compounds within the scope of Ochiai's formula (VII) which contain an (<<alpha>>??Illegible Text??-etherified oximino) acylamido group and which are syn isomers.
We therefore find that the examiner established a prima facie case of obviousness of appellants' claimed compounds and that the burden of persuasion shifted to appellants to rebut the prima facie case. This appellants did not do.
In an effort to rebut the prima facie case of obviousness, appellants rely heavily on In re Magerlein, 602 F.2d 366, 372, 202 USPQ 473, 478 (CCPA1979) where the court concluded that "evidence of an unexpectedly superior activity or property of an end product may, under appropriate circumstances, be considered in the determination of the non-obviousness of the claimed intermediate". Appellants take the position that their end products, i.e., compounds where R1 is hydrogen, have been patented [FN2]; that these end products have unexpectedly superior anti-bacterial activity compared with the closest end products disclosed by Ochiai '888; and that, further to the case law enunciated in Magerlein, the instantly claimed intermediates are likewise patentable. In support of this argument, appellants refer to Rule 132 declarations in the patent files which, in their view, establish the unexpected superiority of the end products. These declarations are: (1) the Penasse declaration dated October 23, 1979 in the file of U.S. Patent No. 4,476,122; (2) the Penasse declaration dated December 29, 1978 in the file of U.S. Patent No. 4,202,893; and (3) the Penasse declaration dated February 9, 1979 in the file of U.S. Patent No. 4, 202,893. Appellants argue that In re Magerlein is "on all fours" with the present situation, and the prima facie case of obviousness has been overcome. See appellants' Brief before the Board, page 7. We disagree.
*3 As stated by the court in Magerlein, 602 F.2d at 373-74, 202 USPQ at 480, "the record establishes that there is no known (or suspected) utility for the claimed intermediates other than as intermediates" and "the record discloses no other properties with respect to which a meaningful comparison of the claimed and prior art intermediates can be made". That is not the case here.
As observed by the Board in Appeal No. 86-3283, see Paper No. 16, page 5 of parent application Serial No. 06/634,148, "unlike the situation in Magerlein, this record does not establish that there is no known utility for the claimed intermediates other than as intermediates". That observation is equally applicable on the present record. We further note the examiner's finding that compounds of the type claimed, 7-acylamino-cephalosporins, are reasonably expected to possess antibiotic properties in their own right and are capable of independent use. We agree with that finding. In so doing, we take official notice of Burger's Medicinal Chemistry, Fourth Edition, Part III, Section 9.1, providing evidence that a large number of 7-acylamino-cephalosporins possess antibiotic properties. A copy of the relevant section of the Burger text is enclosed with this opinion.
Appellants' argument to the contrary, notwithstanding, In re Magerlein is not "on all fours" with the present situation. We have carefully considered the comparative data presented in the above-noted Penasse declarations, relied on by appellants as evidence of non-obviousness. Conspicuous by its absence from this record, however, is a direct comparison of anti-bacterial activity possessed by the instantly claimed compounds in their own right vis-a-vis anti-bacterial activity possessed by the closest prior art compounds. In the absence of such direct comparison, we cannot evaluate the whole story. In our judgment, based on a careful review of the Magerlein case, appellants have the burden of (1) establishing that there is no known (or suspected) utility for the claimed intermediates other than as intermediates; or (2) establishing by way of a direct comparison that the instantly claimed compounds possess unexpectedly superior anti-bacterial activity compared with the closest prior art compounds. This appellants have not done. Instead, they rely on the Penasse declarations to carry the instantly claimed intermediates as well as the final products where R1 is hydrogen, and they pursue the incorrect argument that In re Magerlein is "on all fours". Bear in mind, on the particular facts of this case, the examiner's finding that 7-acylamino cephalosporins of the type claimed are reasonably expected to possess antibiotic properties in their own right and are capable of independent use.
In their Brief before the Board, page 7, appellants characterize the Chantot declaration as follows:
Applicants have submitted a declaration by Dr. Chantot which clearly establishes that the claimed intermediates do not have any use as anti-bacterial agents and only have use as intermediates for the production of patentably distinct final products. Therefore, the present situation falls on all fours with the decision of In re Magerlein and the declaration of Dr. Chantot shows that the claimed trityl intermediates are substantially devoid of anti-bacterial activity as compared to the final products. [emphasis added]
*4 That characterization of the Chantot declaration is factually incorrect. The Chantot declaration is limited to the testing of two compounds, both of which are 3-acetoxymethyl compounds and both of which are outside the scope of compounds defined in appealed claim 1. Dr. Chantot does not provide probative evidence that the claimed intermediates are substantially devoid of antibacterial activity, because the Chantot declaration does not test any claimed compound or compounds.
In conclusion, the burden of persuasion shifted to appellants to rebut the prima facie case of obviousness established by the art of record. On the facts of this case, which are distinguishable from those presented in Magerlein, the Penasse declarations and the Chantot declaration do not serve as adequate rebuttal evidence. Accordingly, the burden of persuasion remains with appellants and we sustain the examiner's § 103 rejection.
The examiner's decision, refusing to allow claim 1 is affirmed. As previously indicated, dependent claims 3 through 11 and 17 through 21 fall together with independent claim 1. Accordingly, the examiner's decision refusing to allow claims 3 through 11 and 17 through 21 is also affirmed.
No time period for taking any subsequent action in connection with this appeal may be extended under 37 CFR 1.136(a). See the final rule notice, 54 F.R. 29548 (July 13, 1989), 1105 O.G. 5 (August 1, 1989).
BOARD OF PATENT APPEALS AND INTERFERENCES
Stephen J. Emery
Bradley R. Garris
Administrative Patent Judges
FN1. Pursuant to a Commissioner's order dated October 4, 1993, this title is being used in lieu of "Examiner-in-Chief."
FN2. See U.S. Patent No. 4,476,122 and U.S. Patent No. 4,202,893.