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, 4-13, 38 and 40 are pending and under examination.
Specification
The objection to the title of the invention is withdrawn based on the amendments.
The disclosure is objected to because of the following informalities: the peaks from the x-ray diffractogram and the differential scanning calorimetry should be reported with a standard error (±). Appropriate correction is required.
The above objection was not addressed, and therefore, is maintained.
Claim Rejections - 35 USC § 112
The rejection of claim 2 under 35 U.S.C. 112, 4th paragraph, as being of improper dependent form for claim 2 not further limiting claim 1, is withdrawn based on the amendments.
The rejection of claim 3 under 35 U.S.C. 112, 4th paragraph, as being of improper dependent form for claim 3 not further limiting claim 1, is withdrawn based on the amendments.
The rejection of claim 3 under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, as failing to comply with the written description requirement is withdrawn based on the amendments.
The following is a quotation of 35 U.S.C. 112(b):
(B) CONCLUSION.—The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the inventor or a joint inventor regards as the invention.
The following is a quotation of 35 U.S.C. 112 (pre-AIA ), second paragraph:
The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the applicant regards as his invention.
Claims 4-5 and 11-12 are rejected under 35 U.S.C. 112(b) or 35 U.S.C. 112 (pre-AIA ), second paragraph, as being indefinite for failing to particularly point out and distinctly claim the subject matter which the inventor or a joint inventor, or for pre-AIA the applicant regards as the invention.
Regarding claims 4-6 and 11-13, the x-ray and differential scanning calorimetry peaks and should be provided with a standard error (±). The standard error is not disclosed. Therefore, said claims are vague.
Applicant amended the claims to “±0.2” for the standard error for the x-ray peaks and noted in the Remarks that support for the amendment may be found throughout the specification, e.g. in paragraphs [0005] and [0035]. However, the standard error is not found in either one of said paragraphs, nor elsewhere in the specification. Thus, the rejection is maintained.
The rejection may be overcome by submitting a declaration.
The following is a quotation of 35 U.S.C. 112(a):
(a) IN GENERAL.—The specification shall contain a written description of the invention, and of the manner and process of making and using it, in such full, clear, concise, and exact terms as to enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the same, and shall set forth the best mode contemplated by the inventor or joint inventor of carrying out the invention.
The following is a quotation of 35 U.S.C. 112 (pre-AIA ), first paragraph:
The specification shall contain a written description of the invention, and of the manner and process of making and using it, in such full, clear, concise, and exact terms as to enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the same and shall set forth the best mode contemplated by the inventor of carrying out his invention.
Claims 4-5 and 11-12 are rejected under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, as failing to comply with the written description requirement. The claim(s) contains subject matter which was not described in the specification in such a way as to reasonably convey to one skilled in the relevant art that the inventor or a joint inventor, or for applications subject to pre-AIA 35 U.S.C. 112, the inventor(s), at the time the application was filed, had possession of the claimed invention. This is a new matter rejection based on the 112b rejection above. Applicant amended the claims to “±0.2” for the standard error but said amendment is not supported by the specification.
The rejection may be overcome by submitting a declaration.
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
The rejection of claim(s) 1, 2, 7, 38 and 41 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 Li et al. (US 9073936), is withdrawn based on the amendments.
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, 4-13, 38 and 40 are rejected under AIA 35 U.S.C. 103(a) as being unpatentable over Li et al. (US 9073936) in view of Berge (J. of Pharmaceutical Sciences, 1977, 66(1), pp. 1-19).
The present application claims a crystal of the compound 2-(4-acetylbenzyl)-3-((4-fluorophenyl)amino)- 5,7,7-trimethyl-7,8-dihydro-2H-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one in free base form and a crystal of the compound 2-(4-acetylbenzyl)-3-((4- fluorophenyl)amino)-5,7,7-trimethyl-7, 8-dihydro-2H-imidazo[1,2-a]pyrazolo[4,3- e]pyrimidin-4(5H)-one in acid addition salt form, wherein the acid addition salt form of the compound is selected from the group consisting of succinate, citrate, adipate, tartrate, malate, gluconate, maleate, fumarate, aspartate, hippurate, sebacate, glycolate,galactarate, benzoate, pamoate, oxalate and malonate salt form, see claims 1 and 7. Claim 38 is drawn to a method of producing an acid addition salt of the same scope as claim 7.
The ‘936 patent teaches 2-(4-acetylbenzyl)-3-((4- fluorophenyl)amino)-5,7,7-trimethyl-7, 8-dihydro-2H-imidazo[1,2-a]pyrazolo[4,3- e]pyrimidin-4(5H)-one in free or salt form, see column 9, lines 5-20 and column 10, line 3. Acid addition salts is taught in column 10, lines 45-51. The reference does not teach specific salts, e.g. citric acid, adipic acid, tartaric acid, malic acid, succinic acid, gluconic acid, maleic acid, fumaric acid, aspartic acid, hippuric acid, sebacic acid, glycolic acid, galactaric acid, benzoic acid, pamoic acid, oxalic acid and malonic acid.
Berge teaches succinate, amongst many others, as an FDA approved commercially marketed salt, cation salt, see Table 1, page 2.
The primary reference teaches the base compound, which can be prepared with any organic acid. The specific acid of the claims is not named in the primary references. Thus, the difference between the claims and the prior art is that applicants have prepared a novel salt of an old drug. The secondary reference teaches the succinate salt, among many others.
When the exact 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.”
The ‘936 patent does not teach the crystalline base compound or crystalline salt thereof. However, it is conventional practice to attempt to crystallize a compound to facilitate the purification or for separation purposes. Moreover, it is conventional to make salts of compounds for different reasons, e.g. to purify compounds by crystallization, to resolve enantiomers, to change pharmacokinetics of compounds, etc. Making acid salts and selecting solvents to make the salts is routine practice in organic chemistry.
Therefore, it would be obvious of one of ordinary skill in the art to make the succinate salt of compound A because a succinate salt is one of the specific salts taught in the secondary reference. Thus, said claims are rendered obvious over Li et al.
Applicant traverses by stating, “Choosing the appropriate salt is difficult and the beneficial effect produced thereby is unpredictable. As a matter of fact, Berge teaches that choosing the appropriate salt is very difficult. Specifically, Berge discloses in the last paragraph in left column of page 1 that "choosing the appropriate salt, however, can be a very difficult task, since each salt imparts unique properties to the parent compound", and in lines 5-7 in the CONCLUSIONS on page 16 that "at present, selecting a salt form that exhibits the desired combination of properties is a difficult semiempirical choice". Berge teaches that the obtaining of the claimed salts is not obvious and the beneficial effect produced thereby is unpredictable. Furthermore, it is even more difficult to predict which salts will form crystalline structures with favorable properties, due to the inherent unpredictability of crystal formation and the resulting crystal characteristics.”
This is not persuasive. Making salts is routine and conventional in an organic chemistry lab for purification, separation, improve pharmacokinetics, etc. Berge provides the most common FDA approved salts in Table 2.
Applicant further contends, “With regard to claim 1, Li also does not disclose a crystal of Compound A in in free base form. Free base forms are often less favored or even unstable, so a skilled person may not be motivated to isolate or crystallize the free base for a pharmaceutical composition, especially if the salt is already known. As disclosed in paragraph [0004] of the present application, the free base crystals of Compound A are not only stable, but are also advantageous in the preparation of the salt crystals of Compound A. This is not taught by Li. A skilled person, starting from the teaching of Li, would reasonably follow the disclosed route-i.e., prepare the salt directly-and would have no motivation to first isolate and crystallize the free base, especially in light of the common understanding that salt forms are often more stable and pharmaceutically suitable. In many cases, free base forms are oily, hygroscopic, or unstable, and often present difficulties in purification or handling. Therefore, the ability to obtain a stable and crystalline free base form of Compound A is a non-trivial and unexpected achievement, especially when the prior art suggests proceeding directly to salt formation. The present application teaches specific benefits of crystalline free base form of compound A for the preparation of its salt crystals. Accordingly, it would not be obvious to isolate and crystallize the free base of Compound A.”
Again, this is unpersuasive. The primary reference teaches the base compound, which can be prepared with any organic acid. It is conventional practice to attempt to crystallize a compound to facilitate the purification or for separation purposes. Making acid salts and selecting solvents to make the salts is routine practice in organic chemistry.
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, 4-13, 38 and 40 are rejected on the ground of nonstatutory obviousness-type double patenting as being unpatentable over claims 1-7, 11-13 and 17-19 of U.S. Patent No. 9073936 in view of Berge (J. of Pharmaceutical Sciences, 1977, 66(1), pp. 1-19). Although the conflicting claims are not identical, they are not patentably distinct from each other because the ‘936 patent claims compound A in free or salt form, see claim 7, and the claims embrace all forms of compound A. Moreover, the same reasons provided in the 103 rejection above are equally applicable here.
Claims 1, 4-13, 38 and 40 are rejected on the ground of nonstatutory obviousness-type double patenting as being unpatentable over claims 1-16 of U.S. Patent No. 9598426 in view of Berge (J. of Pharmaceutical Sciences, 1977, 66(1), pp. 1-19). Although the conflicting claims are not identical, they are not patentably distinct from each other because the ‘426 patent claims compound A in free or salt form, and the claims embrace all forms of compound A. Furthermore, there is no patentable distinction between compounds and methods of intended use of said compounds. Moreover, the same reasons provided in the 103 rejection above are equally applicable here as the disclosure for U.S. Patent No. 9073936 looks similar to the ‘426 patent.
Claims 1, 4-13, 38 and 40 are rejected on the ground of nonstatutory obviousness-type double patenting as being unpatentable over claims 1-15 and 19-24 of U.S. Patent No. 9556186 in view of Berge (J. of Pharmaceutical Sciences, 1977, 66(1), pp. 1-19). Although the conflicting claims are not identical, they are not patentably distinct from each other because the ‘186 patent claims compound A in free or salt form, and the claims embrace all forms of compound A. Furthermore, there is no patentable distinction between compounds and methods of intended use of said compounds. Moreover, the same reasons provided in the 103 rejection above are equally applicable here as the disclosure for U.S. Patent No. 9073936 looks similar to the ‘186 patent.
Claims 1, 4-13, 38 and 40 are rejected on the ground of nonstatutory obviousness-type double patenting as being unpatentable over claims 1, 2, 4 and 7 of U.S. Patent No. 12364695 in view of Berge (J. of Pharmaceutical Sciences, 1977, 66(1), pp. 1-19). Although the conflicting claims are not identical, they are not patentably distinct from each other because the ‘695 patent claims a method of treating an inflammatory disease, condition or disorder comprising administering compound A in free or salt form. Again, the claims embrace all forms of compound A and there is no patentable distinction between compounds and methods of intended use of said compounds.
Applicant states, “The doctrine of nonstatutory double patenting seeks to prevent the unjustified extension of exclusive rights to the same invention or an obvious variant thereof. However, this does not apply where the claims are patentably distinct. In this case, the pending claims of the present application and the claims of the '936 and '426 patents do not cover the same subject matter and do not overlap in scope. The claims of the '936 and '426 patents are directed to free base and salt crystals of Compound A as recited in claims 1 and 7. Furthermore, the claims are not obvious over '936 and '426 patents in view of Berge, as discussed above.”
This is not persuasive for the same reasons noted in the 103 rejection above. Thus, the rejections are maintained.
Conclusion
Applicant's amendment necessitated the new ground(s) of rejection presented in this Office action. Accordingly, THIS ACTION IS MADE FINAL. See MPEP § 706.07(a). 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.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to SUSANNA MOORE whose telephone number is (571)272-9046. The examiner can normally be reached Monday - Friday, 10:00 am to 7:00 pm.
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/SUSANNA MOORE/Primary Examiner, Art Unit 1624
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