DETAILED ACTION
Notice of Pre-AIA or AIA Status
The present application, filed on or after March 16, 2013, is being examined under the first inventor to file provisions of the AIA .
This is a Final Office Action.
Claims 1-16 are pending and under consideration.
Claim Objections
The objection to claim 14 because of the term “legs” should be singular is withdrawn based on the amendments.
Claims 7-12, 15 and 16 are objected to as being dependent upon a rejected base claim, but would be allowable if rewritten in independent form including all of the limitations of the base claim and any intervening claims.
In the event the determination of the status of the application as subject to AIA 35 U.S.C. 102 and 103 (or as subject to pre-AIA 35 U.S.C. 102 and 103) is incorrect, any correction of the statutory basis for the rejection will not be considered a new ground of rejection if the prior art relied upon, and the rationale supporting the rejection, would be the same under either status.
Claim Rejections - 35 USC § 102/103
The following is a quotation of the appropriate paragraphs of 35 U.S.C. 102 that form the basis for the rejections under this section made in this Office action:
A person shall be entitled to a patent unless –
(a)(1) the claimed invention was patented, described in a printed publication, or in public use, on sale or otherwise available to the public before the effective filing date of the claimed invention.
(a)(2) the claimed invention was described in a patent issued under section 151, or in an application for patent published or deemed published under section 122(b), in which the patent or application, as the case may be, names another inventor and was effectively filed before the effective filing date of the claimed invention.
Claim(s) 1-6, 13 and 14 are rejected under 35 U.S.C. 102(a)(1) and 102(a)(2) as anticipated by or, in the alternative, under 35 U.S.C. 103 as obvious over Nishimura et al. (US 9138434).
The reference teaches the following species:
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352
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, see column 155, compound I-15. The reference further teaches a small genus of salts, see column 7, lines 22-36. The M.P.E.P. states:
2131.02 [R-6] Genus-Species Situations
A GENERIC CHEMICAL FORMULA WILL ANTICIPATE A CLAIMED
SPECIES COVERED BY THE FORMULA WHEN THE SPECIES CAN BE
“AT ONCE ENVISAGED” FROM THE FORMULA
When the compound is not specifically named, but instead it is
necessary to select portions of teachings within a reference and
combine them, e.g., select various substituents from a list of
alternatives given for placement at specific sites on a generic chemical
formula to arrive at a specific composition, anticipation can only be
found if the classes of substituents are sufficiently limited or well
delineated. Ex parte A, 17 USPQ2d 1716 (Bd. Pat. App. & Inter. 1990).
If one of ordinary skill in the art is able to “at once envisage” the
specific compound within the generic chemical formula, the compound
is anticipated. One of ordinary skill in the art must be able to draw the
structural formula or write the name of each of the compounds included in the generic
formula before any of the compounds can be “at once envisaged.” One
may look to the preferred embodiments to determine which
compounds can be anticipated. In re Petering, 301 F.2d 676, 133 USPQ
275 (CCPA 1962).
The reference further teaches that the compound may be isolated or purified according to conventional isolation and purification techniques well-known in the art of the relevant field, such as… crystallizations, recrystallization…”, see column 19, lines 49-56.
The reference further teaches compositions, see column 236, claims 11 and 12.
Thus, said claims are anticipated by or, in the alternative, obvious over Nishimura et al.
Applicant traverses by stating 1) Nishimura only includes a general description of salts, and succinic acid is simply one example of an organic acid described in a broad list of acid addition salts; 2) One of ordinary skill in the art would not have arrived at the succinate salt of compound (B) with a reasonable expectation of success because the chemical arts is unpredictable; and 3) The examples in the specification demonstrate the unexpectedly superior properties and effects of the succinate salt of the present invention compared to other salts.
This is not persuasive.
As noted in the rejection, the list of salts in column 7 is a list of only 26 acids, which is not a broad, see In re Petering cited in the rejection.
Applicant cited the Byrn reference, which is not of record, and therefore, has not been considered.
Indeed, the chemical arts may be unpredictable but making salts of organic compounds is conventional and routine in an organic chemistry lab.
Applicant points to Tables 7, 8 and 10 in the specification where the succinate salt is compared to the hydrochloride, sebacate and adipate salts, with no explanation as to why these particular salts were chosen for comparison. It’s well-known in the chemical arts that HCl salts may be hygroscopic, and ultimately less stable, although many pharmaceutical drugs are HCl salts, see the cited Berge reference below, with succinate being the second highest percentage in Table 2. While adipate (6 carbons) and sebacate (10 carbons) are a closer comparison to succinate (4 carbons) with diacid groups than HCl, glutarate (5 carbons) and malonic (3 carbons) salts are closer in structure. Moreover, if the ratio of components in the salt is critical, then other succinate salts of the same compound should have used for the comparison.
Thus, the 102/103 rejection is maintained for the reasons noted above.
Claim Rejections - 35 USC § 103
The following is a quotation of 35 U.S.C. 103(a) which forms the basis for all obviousness rejections set forth in this Office action:
(a) A patent may not be obtained though the invention is not identically disclosed or described as set forth in section 102 of this title, if 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 to a person having ordinary skill in the art to which said subject matter pertains. Patentability shall not be negatived by the manner in which the invention was made.
The factual inquiries set forth in Graham v. John Deere Co., 383 U.S. 1, 148 USPQ 459 (1966), that are applied for establishing a background for determining obviousness under 35 U.S.C. 103(a) are summarized as follows:
1. Determining the scope and contents of the prior art.
2. Ascertaining the differences between the prior art and the claims at issue.
3. Resolving the level of ordinary skill in the pertinent art.
4. Considering objective evidence present in the application indicating obviousness or nonobviousness.
This application currently names joint inventors. In considering patentability of the claims under 35 U.S.C. 103(a), the examiner presumes that the subject matter of the various claims was commonly owned at the time any inventions covered therein were made absent any evidence to the contrary. Applicant is advised of the obligation under 37 CFR 1.56 to point out the inventor and invention dates of each claim that was not commonly owned at the time a later invention was made in order for the examiner to consider the applicability of 35 U.S.C. 103(c) and potential 35 U.S.C. 102(e), (f) or (g) prior art under 35 U.S.C. 103(a).
Claims 1-6, 13 and 14 are rejected under AIA 35 U.S.C. 103(a) as being unpatentable over Nishimura et al. (US 9138434) in view of Berge et al. (Journal of Pharmaceutical Sciences, 1977, 66(1), 1-19), Kath et al. (US 6844349) and Ku et al. (US 20070149552).
The 102/13 rejection above is incorporated here.
Succinate salts are an entirely conventional drug form as evidence by Berge et al. that teach succinate salts as an FDA-approved salts, see page 2, Table I.
Moreover, the ‘349 patent and ‘552 publication teach that succinate salts of APIs may form highly crystalline salts, see column 2, lines 49-53, and page 2, paragraph 0019. Furthermore, it would be obvious to make a crystalline salt to facilitate the purification of the compound by crystallization or recrystallization.
Routine optimization would provide salts in different ratios. Generally, differences in concentration or temperature will not support the patentability of subject matter encompassed by the prior art unless there is evidence indicating such concentration or temperature is critical. "Where the general conditions of a claim are disclosed in the prior art, it is not inventive to discover the optimum or workable ranges by routine experimentation." In re Aller, 220 F.2d 454, 105 USPQ 233, 235 (CCPA 1955). The adjustment of particular conventional working conditions (e.g., determining result effective amounts of the solvents taught by the cited references), is deemed merely a matter of judicious selection and routine optimization which is well within the purview of the skilled artisan. Accordingly, this type of modification would have been well within the purview of the skilled artisan and no more than an effort to optimize results.
Therefore, claims 1-6, 13 and 14 are obvious over Nishimura et al. in view of Berge et al., Kath et al. and Ku et al.
Applicant traverses by stating, “Nishimura does not disclose the sesquisuccinate salt (A-1) or monosuccinate salt (A-2).”
Indeed, which is why the present rejection is a 103 rejection.
Applicant further states, “Berge teaches a succinate salt as one example of an FDA-approved commercially marketed salt among a list of FDA-approved commercially marketed salts. In addition, there is no disclosure in Berge regarding any advantages or benefits of a succinate salt. In fact, Berge teaches that monoprotic hydrochloride is the most frequent choice of available anionic salt- forming radicals (42.98%). Further, there is no disclosure in Berge regarding any properties or effects of a succinate salt.”
This is not persuasive. The factual situation is thus similar as in Pfizer, Inc. v. Apotex, Inc. 82 USPQ2d 1321 which was directed to the amlodipine besylate drug. At the time of the invention, amlodipine was known as was the use of besylate anions. While the amlodipine besylate had the same therapeutic use, Pfizer discovered that the besylate (benzene sulphonate) form had a superior properties. Pfizer’s argument that the results of forming amlodipine besylate would have been unpredictable, and therefore were nonobvious, was unpersuasive. The court rejected the notion that unpredictability could be equated with nonobviousness here, because there were only a finite number (53) of pharmaceutically acceptable salts to be tested for improved properties (e.g., non-stickiness, and improved stability) while at the same time having good solubility, and non-hygroscopicity. The court found that one of ordinary skill in the art looking to improve amlodipine would have looked to forming a salt of the compound with the group of potential salt-formers being a group of 53 anions already known to form pharmaceutically acceptable salts, which would be an acceptable number to provide ‘‘a reasonable expectation of success.’’ Indeed, the Court decision quoted unrefuted testimony that “part and parcel of pharmaceutically accepted[] was to look in pharmacopoeias and compendia” to find an anion having “precedence for use within the pharmaceutical industry” and that it “It would be logical to try” salts from the known list (page 1331). That other drugs which used the besylate salt did not have the same therapeutic use as amlodipine was called “unimportant, if not actually irrelevant” (page 1332). The Court further noted that “upon making a new acid addition salt, it was routine in the art to verify the expected physicochemical characteristics of each salt”, so that if “one skilled in the art would have had a reasonable expectation of success at the time the invention was made” one “merely had to verify that expectation” and learn of these properties (page 1335). Moreover, the Court found this “analogous to the optimization of a range or other variable within the claims that flows from the “normal desire of scientists or artisans to improve upon what is already generally known.” In re Peterson, 315 F.3d 1325, 1330 (Fed. Cir. 2003)…”
Applicant notes, “Kath and Ku merely disclose a succinate salt of a completely structurally different compound from the Compound (B) of the present invention. In addition, while there may be a general description of properties or effects of the succinate salts in Kath or Kur, neither Kath nor Ku describe the effects of the succinate salts as a practical example. In fact, Kath is directed to E-2-Methoxy-N-(3-{4-[3-methyl-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quinazolin-6-yl}- allyl)-acetamide and the method of treating hyperproliferative diseases. Ku is directed to triazolopyrimidine compounds and the treatment of cancer.”
The Kath and Ku reference were provided to show that succinate salts of APIs may form highly crystalline salts, see column 2, lines 49-53, and page 2, paragraph 0019.
Applicant further notes, “In addition, as discussed above, the salts disclosed in Berge include a hydrochloride, which is used in the Comparative Examples of the present specification. As can be seen from Tables 7, 8 and 10, the hydrochloride salt does not possess the properties or effects of the succinate salt of the present invention, i.e., the succinate salt of the present invention is unexpectedly physically and chemically stable. Thus, the succinate salts of present invention provides unexpectedly superior properties or effects.”
As noted above, Tables 7, 8 and 10 in the specification, where the succinate salt is compared to the hydrochloride, sebacate and adipate salts, does not provide an explanation as to why these particular salts were chosen for comparison. It’s well-known in the chemical arts that HCl salts may be hygroscopic, and ultimately less stable, although many pharmaceutical drugs are HCl salts, see the cited Berge reference below, with succinate being the second highest percentage in Table 2. While adipate (6 carbons) and sebacate (10 carbons) are a closer comparison to succinate (4 carbons) with diacid groups than HCl, glutarate (5 carbons) and malonic (3 carbons) salts are closer in structure. Moreover, if the ratio of components in the salt is critical, then other succinate salts of the same compound should have used for the comparison.
Thus, the rejection is maintained.
Double Patenting
The nonstatutory double patenting rejection is based on a judicially created doctrine grounded in public policy (a policy reflected in the statute) so as to prevent the unjustified or improper timewise extension of the “right to exclude” granted by a patent and to prevent possible harassment by multiple assignees. A nonstatutory double patenting rejection is appropriate where the claims at issue are not identical, but at least one examined application claim is not patentably distinct from the reference claim(s) because the examined application claim is either anticipated by, or would have been obvious over, the reference claim(s). See, e.g., In re Berg, 140 F.3d 1428, 46 USPQ2d 1226 (Fed. Cir. 1998); In re Goodman, 11 F.3d 1046, 29 USPQ2d 2010 (Fed. Cir. 1993); In re Longi, 759 F.2d 887, 225 USPQ 645 (Fed. Cir. 1985); In re Van Ornum, 686 F.2d 937, 214 USPQ 761 (CCPA 1982); In re Vogel, 422 F.2d 438, 164 USPQ 619 (CCPA 1970); and In re Thorington, 418 F.2d 528, 163 USPQ 644 (CCPA 1969).
A timely filed terminal disclaimer in compliance with 37 CFR 1.321(c) or 1.321(d) may be used to overcome an actual or provisional rejection based on a nonstatutory double patenting ground provided the reference application or patent either is shown to be commonly owned with this application, or claims an invention made as a result of activities undertaken within the scope of a joint research agreement. A terminal disclaimer must be signed in compliance with 37 CFR 1.321(b).
The USPTO internet Web site contains terminal disclaimer forms which may be used. Please visit http://www.uspto.gov/forms/. The filing date of the application will determine what form should be used. A web-based eTerminal Disclaimer may be filled out completely online using web-screens. An eTerminal Disclaimer that meets all requirements is auto-processed and approved immediately upon submission. For more information about eTerminal Disclaimers, refer to http://www.uspto.gov/patents/process/file/efs/guidance/eTD-info-I.jsp.
Claims 1-6, 13 and 14 are rejected on the ground of nonstatutory obviousness-type double patenting as being unpatentable over claims 1, 8-17 and 19-20 of U.S. Patent No. 9138434 in view of Berge et al. (Journal of Pharmaceutical Sciences, 1977, 66(1), 1-19), Kath et al. (US 6844349) and Ku et al. (US 2007019552).
. Although the conflicting claims are not identical, they are not patentably distinct from each other because of the same reasoning provided above in the 102 and 103 rejections. Moreover, the species in claims 19-20 of the ‘434 patent are homologues of the presently claimed compound.
The MPEP 2144.09 states “Compounds which are position isomers (compounds having the same radicals in physically different positions on the same nucleus) or homologs (compounds differing regularly by the successive addition of the same chemical group, e.g., by -CH2- groups) are generally of sufficiently close structural similarity that there is a presumed expectation that such compounds possess similar properties. In re Wilder, 563 F.2d 457, 195 USPQ 426 (CCPA 1977).
Applicant traverses by stating, “It is submitted that claim 1 is not obvious in view of the claims of US 9,138,434 and the cited art for the reasons discussed above.”
This is not persuasive, and therefore, the rejection is maintained for the reasons set forth in the rejection and the response to arguments, which are equally applicable.
Conclusion
THIS ACTION IS MADE FINAL. Applicant is reminded of the extension of time policy as set forth in 37 CFR 1.136(a).
A shortened statutory period for reply to this final action is set to expire THREE MONTHS from the mailing date of this action. In the event a first reply is filed within TWO MONTHS of the mailing date of this final action and the advisory action is not mailed until after the end of the THREE-MONTH shortened statutory period, then the shortened statutory period will expire on the date the advisory action is mailed, and any nonprovisional extension fee (37 CFR 1.17(a)) pursuant to 37 CFR 1.136(a) will be calculated from the mailing date of the advisory action. In no event, however, will the statutory period for reply expire later than SIX MONTHS from the mailing date of this final action.
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/SUSANNA MOORE/Primary Examiner, Art Unit 1624