Notice of Pre-AIA or AIA Status
The present application is being examined under the pre-AIA first to invent provisions.
DETAILED ACTION
Claims 1-10 are pending in the instant application.
Claims 1-10 are examined herein.
Priority
The instant application claims benefit of priority to U.S. Provisional Application No. 61/408517 filed on 29 October 2010, and is a continuation of the applications listed below. The claims to the benefit of priority are acknowledged. As such, the effective filing date of the claims is 29 October 2010.
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Information Disclosure Statement
The information disclosure statement (IDS), submitted on 20 August 2024 is acknowledged and considered. The submissions are in compliance with the provisions of 37 CFR 1.97.
Claim Interpretation
Claim 1 step (b) recites the relative term “essentially” within the phrase “essentially non-crystalline.” This phrase is clearly defined in paragraph [01225] of the specification.
Claim Objections
Claim 1 is objected to because of the following informalities:
Claim 1 recites “…(a) dissolving in a suitable solvent comprises one or more…” The claim should recite “…solvent which comprises one or more…” or “…solvent comprising one or more…”
Appropriate correction is required.
Double Patenting
A rejection based on double patenting of the “same invention” type finds its support in the language of 35 U.S.C. 101 which states that “whoever invents or discovers any new and useful process... may obtain a patent therefor...” (Emphasis added). Thus, the term “same invention,” in this context, means an invention drawn to identical subject matter. See Miller v. Eagle Mfg. Co., 151 U.S. 186 (1894); In re Vogel, 422 F.2d 438, 164 USPQ 619 (CCPA 1970); In re Ockert, 245 F.2d 467, 114 USPQ 330 (CCPA 1957).
A statutory type (35 U.S.C. 101) double patenting rejection can be overcome by canceling or amending the claims that are directed to the same invention so they are no longer coextensive in scope. The filing of a terminal disclaimer cannot overcome a double patenting rejection based upon 35 U.S.C. 101.
Claim 5 is/are rejected under 35 U.S.C. 101 as claiming the same invention as that of claim 6 of U.S. Patent No. 10213433B2. This is a statutory double patenting rejection.
Regarding claim 5, the U.S. Patent recites the process of claim 1, wherein the solvent comprises a dichloromethane/methanol or THF/water mixture (claim 6).
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 conflicting claims 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); 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 nonstatutory double patenting provided the reference application or patent either is shown to be commonly owned with the examined application, or claims an invention made as a result of activities undertaken within the scope of a joint research agreement. See MPEP § 717.02 for applications subject to examination under the first inventor to file provisions of the AIA as explained in MPEP § 2159. See MPEP § 2146 et seq. for applications not subject to examination under the first inventor to file provisions of the AIA . A terminal disclaimer must be signed in compliance with 37 CFR 1.321(b).
The filing of a terminal disclaimer by itself is not a complete reply to a nonstatutory double patenting (NSDP) rejection. A complete reply requires that the terminal disclaimer be accompanied by a reply requesting reconsideration of the prior Office action. Even where the NSDP rejection is provisional the reply must be complete. See MPEP § 804, subsection I.B.1. For a reply to a non-final Office action, see 37 CFR 1.111(a). For a reply to final Office action, see 37 CFR 1.113(c). A request for reconsideration while not provided for in 37 CFR 1.113(c) may be filed after final for consideration. See MPEP §§ 706.07(e) and 714.13.
The USPTO Internet website contains terminal disclaimer forms which may be used. Please visit www.uspto.gov/patent/patents-forms. The actual filing date of the application in which the form is filed determines what form (e.g., PTO/SB/25, PTO/SB/26, PTO/AIA /25, or PTO/AIA /26) 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 www.uspto.gov/patents/apply/applying-online/eterminal-disclaimer.
Claims 1-4 and 6-10 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-5, 7-10, and 12 of U.S. Patent No. 10213433B2. Although the claims at issue are not identical, they are not patentably distinct from each other.
Regarding claim 1, the U.S. patent recites a process for preparing a solid dispersion, comprising (a) dissolving in a suitable solvent (i) an active pharmaceutical ingredient (API) comprising a compound of Formula I, (ii) a water-soluble polymeric carrier and (iii) at least one surfactant and (b) removing the solvent to provide a solid matrix comprising the three aforementioned components (claim 1); wherein the solvent comprises one or more of methanol, ethanol, acetone, tetrahydrofuran and dichloromethane (claim 5).
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U.S. Patent Formula I Instant Application Formula I
Regarding claim 2, the U.S. Patent recites the process of claim 1 where the API comprises a compound of Formula I or a pharmaceutically acceptable salt thereof in parent-compound form; and the process further comprises adding a pharmaceutically acceptable acid before removing the solvent (claim 2).
Regarding claim 3, the U.S. Patent recites the process of claim 1, wherein the solvent is removed under heat and/or vacuum (claim 3).
Regarding claim 4, the U.S. Patent recites the process of claim 1, wherein the solvent is removed by rotary evaporation or by spray-drying (claim 4).
Regarding claim 6, the U.S. Patent recites the process of claim 1, wherein no more than about 5% of the compound of Formula I or the pharmaceutically acceptable salt thereof in the solid matrix is crystalline as observed by X-ray diffraction analysis (claim 7).
Regarding claim 7, the U.S. Patent recites the process of claim 1, wherein no more than about 2% of the compound of Formula I or the pharmaceutically acceptable salt thereof in the solid matrix is crystalline as observed by X-ray diffraction analysis (claim 8).
Regarding claim 8, the U.S. Patent recites the process of claim 1, wherein no more than about 1% of the compound of Formula I or the pharmaceutically acceptable salt thereof in the solid matrix is crystalline as observed by X-ray diffraction analysis (claim 9).
Regarding claim 9, the U.S. Patent recites the process of claim 1, wherein API is 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl ]methyl }piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl} sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharmaceutically acceptable salt thereof (claim 10).
Regarding claim 10, the U.S. Patent recites the process of claim 11, wherein the pharmaceutically acceptable surfactant is a polysorbate (claim 12).
Claim Rejections - 35 USC § 103
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 (i.e., changing from AIA to pre-AIA ) 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.
The following is a quotation of pre-AIA 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, 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 negated by the manner in which the invention was made.
The factual inquiries for establishing a background for determining obviousness under pre-AIA 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 pre-AIA 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 pre-AIA 35 U.S.C. 103(c) and potential pre-AIA 35 U.S.C. 102(e), (f) or (g) prior art under pre-AIA 35 U.S.C. 103(a).
Claim 1-10 is/are rejected under pre-AIA 35 U.S.C. 103(a) as being unpatentable over Bruncko et al. (US 2010/0305122, cited by applicant on 1449 IDS) in view of Packhaeuser et al. (US 2010/031064, cited by applicant on 1449 IDS) in further view of Bechtold et al. (US 2010/0098763 A1; cited by applicant on 1449 IDS) and Ghebremeskel et al. (Use of Surfactants as Plasticizers in Preparing Solid Dispersions of Poorly Soluble API: Stability Testing of Selected Solid Dispersions, 2006, Pharmaceutical Research, Vol. 23, No. 8, pages 1928-1936; cited by applicant on 1449 IDS).
In claim 1 applicant recites a method for preparing a solid dispersion, comprising:
(a) Dissolving the following in a suitable solvent:
(i) A compound of formula I or salt thereof
(ii) At least one water-soluble polymeric carrier
(iii) At least one surfactant
(b) Removing the solvent to provide a solid matrix comprising the polymer and surfactant and having the compound of formula I dispersed in an essentially non-crystalline form therein.
In claim 9, they recite a compound of formula I: (Claim 59)
It has the following chemical structure:
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(Also referred to as ABT-199 or Compound 5)
Bruncko et al. is generally directed towards methods of making Bcl-2 inhibiting compounds for treatment of cancer. They teach the claimed compound 5 and they teach compositions with excipients but they do not explicitly teach solid dispersions.
Packhaeuser teaches making solid dispersions of compounds that are Bcl-2 inhibitors, and both Bruncko and Packhaeuser are from the same assignee, Abbott Laboratories. They teach copovidone as a preferred polymer of their dispersions. Similarly to Packhaeuser, Bechtold also teaches solid dispersions with copovidone and they go into more detail on the two main methods for forming solid dispersions, solvent evaporation and melt-extrusion processes. Bechtold teaches how one can formulate solid dispersions with copovidone and a surfactant via both methods as well as teaching that these systems achieve good stability. Lastly, Ghebremeskel is also drawn to solid dispersions of active agents and they specifically tested the effects of adding a surfactant to the dispersion, a factor taught as an option by Packhaeuser and Bechtold but not discussed in detail. Ghebremeskel teaches that adding a surfactant such as polysorbate 80 to solid dispersions with copovidone improves the dissolution and water uptake and does not significantly affect the stability with respect to crystallinity. Thus it would have been obvious to add a surfactant such as polysorbate 80 (tween 80) to the dispersions as taught in each of the Packhaeuser, Bechtold and Ghebremeskel references and there is a reasonable expectation that this system with copovidone and surfactant could be used for compounds in Bruncko as well due to the similarity to the compound in Packhaeuser as well as the diversity in active agents demonstrated by the three different references.
Specifically, Bruncko teaches compounds which are Bcl-2 proteins for treating cancer (Abstract) and they teach compounds of a general formula I:
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(Page 1, [0007], Bruncko)
They teach the compound of claim 59 specifically:
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(Page 8, [0182])
And also in example 5L:
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(Page 122, [2480-2481])
They also specifically teach forming pharmaceutical compositions with excipients:
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(Page 89, [2324])
Bruncko also teaches incorporating various excipients including disintegrating agents and releasing agents (Page 90, [2340]) as well as cross-povidone and povidone as a suitable excipient for oral solid dosage forms (See page 90, [2341], end of column 1 and first 15 lines of column 2). They do not explicitly teach copovidone and they do not explicitly mention solid dispersions, however it would have been obvious to formulate these compounds from Bruncko into solid dispersions with copovidone and polysorbates as that was a common solid dispersion system for poorly soluble active agents.
Packhaeuser et al. is generally directed towards solid dispersions of a compound ABT-263, which is a Bcl-2 inhibitor:
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(Abstract, Packhaeuser)
They teach that this compound is a preferred Bcl-2 family inhibitor and has a structure that is similar to that of applicant’s compound 5:
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(Page 1, [0004], Packhaeuser)
They teach that these types of compounds have poor solubility and poor bioavailability in the crystalline form:
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(Page 1, [0005])
They teach that they found by formulating the compound ABT-263 in a solid dispersion with a polymer that it not only shows adequate oral bioavailability but is a storage-stable, ready to use form:
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(Page 1, [0013])
They teach that this dosage form includes ABT-263 in combination with other Bcl-2 family inhibitors:
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(Page 2, [0033], Packhaeuser)
As shown above, the claimed compound is taught as a Bcl-2 inhibitor, and both Bruncko and Packhaeuser are from Abbott labs (assignee in both applications). Packhaeuser goes on to teach that in addition to a polymer they include a solubilizer, which is preferably a non-ionic surfactant:
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(Page 3, [0036])
And they teach various polysorbates (Tween 80, Tween 65, etc.; claim 60) as options for the solubilizer:
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(Page 3, [0040])
They teach using polymers that are water-soluble, water-dispersible or water-swellable and they teach the co-polymer of N-vinyl pyrrolidone and vinyl acetate as a preferred polymer:
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(Page 4, [0049] and [0053])
They teach that the solid dispersions can be made by various methods known in the art, the primary options being the melt-extrusion method (Page 4, [0056]) and that the preparation can involve the use of solvents to form the dispersion:
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(Page 4, [0058])
See also Example 1:
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(Example 1, Pages 9-10, [0132-0133])
They teach various formulations 1-15 in Table 1; all of these include copovidone as the polymer and formulations 4 and 12 contain polysorbate 20 (at 5 and 10%):
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(Table 1, formulations 1-4 (from first part of table) and 12-15 (from 2nd part of table), page 10)
They teach that formulations 4, 12, 13 and 14 were the only ones that there was no crystals detected at some point and 12-14, had no crystals the entire time:
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(Page 12, Table 5)
As seen above, examples 4 and 12 had polysorbate 20 as the surfactant/solublizer, while formulations 4, 13-14 had Vitamin E-TPGS as the solublizer, thus clearly those resulted in better formulations than when Span 20 was used (formulations 5-6 or 15) or SDS (formulations 2-4, 11, 15). In each instance however they clearly teach that a solid dispersion with the Bcl-2 inhibitor and copovidone resulted in a stable formulation that remained non-crystalline.
Similarly to Packhaeuser, Bechtold also teaches solid dispersions with copovidone. Bechtold is drawn to solid dispersions with polymers that exhibit low hygroscopicity and high softening temperature, such as copovidone:
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(Abstract, Bechtold)
They teach their invention results in formulations with improved bioavailability for active agents that are poorly soluble and the compound they use is also for treating cancer (Page 1, [0002-0003]). The compound they tested has the following formula (hereafter known as compound 1):
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(Page 1, [0004], Bechtold)
They teach that they were able to increase the bioavailability of the compound by making a solid dispersion:
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(Page 2, [0016])
They further teach that the active agent is in amorphous form and that they want to prevent crystallization (Page 2, [0017-0021]), they teach that copovidone is a preferred polymer:
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(Page 3, [0028])
They further teach surfactants such as polysorbates can be included:
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(Page 4, [0061])
They also teach that there are various ways known in the art to make solid dispersions including hot-melt extrusion and solvent/evaporation:
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(Page 5, [0065])
They specifically describe the solvent system:
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(Page 5, [0066])
They further teach a system for screening various polymers and solvent systems:
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(Table 5, page 8, [0118])
They also report results of the screening for copovidone in acetone and methanol, see table 6, middle of table for copovidone:
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(Page 10, Table 6, above [0122])
They teach that some systems were unstable such as those with low-melting poloxamers and Eudragit E (See Page 10, [0122]) but that copovidone was identified as a preferred polymer. They then describe formulating a solid dispersions by both the solvent evaporation process and the melt extrusion process:
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(Page 12, section 4.6.1 and 4.6.2, [0131-0135], Section 4.6.1 highlighted here)
As seen above they used methanol and dichloromethane as the solvent in that system. They further test the stability of the solid dispersion tablet in Table 16, reporting that there was no crystallinity found for the whole time (4 months), and the impurity level stayed constant at 0.44%:
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(Page 15, Table 16, [0151])
Lastly they compared bioavailability of various forms including immediate release, suspensions, and various dispersions with the copovidone dispersion having the best bioavailability, approximately 5x better than immediate release (See table 28, page 21, [0204]). Thus as taught by Bechtold, the system of copovidone provided improved bioavailability and good stability for their formulation.
Lastly, Ghebremeskel also teaches solid dispersions systems, their focus being on generic active agents and the effect of surfactants on stability. Ghebremeskel teaches that they studied solid dispersions of poorly water-soluble drugs using PVP-K30, Plasdone-S630 (copovidone), and HPMC-E5, together with surfactants including Tween 80:
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(Abstract, Purpose and Method Sections)
They teach that while the effect of surfactants as plasticizers to improve processability was well known, that they also studied the effect the surfactants had on the stability and dissolution performance of dispersions:
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(Page 1929, column 1, first paragraph, Ghebremeskel)
They used Plasdone S-630, which is copovidone and Tween 80, which is Polysorbate 80 (See page 1929, column 1, Materials) and they tested the effect on water-uptake as well as crystallinity in Table II:
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(Table II, page 1930, first half of table shown here)
As seen in Table II, the addition of Tween-80 to the plasdone dispersion increased water-uptake and caused a minimal effect on recrystallization (smallest of all the surfactants). They used a hot-melt extrusion process to make their dispersions (Page 1931, column 2) however the effects on dissolution and crystallinity should be relevant regardless of whether solvent or extrusion processes are used.
Ghebremeskel further teaches that the surfactants significantly increased the dissolution rate, with the addition of Tween 80 to the plasdone system increasing the dissolution from 45 mins to 10 minutes:
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(Page 1936, column 1, 2nd paragraph)
They further teach that almost all of the dispersions were stable and that while the HPMC-E5 system was somewhat destabilized by the surfactant that the result is much more reduced in the Plasdone S-630 and PVP-K30 systems:
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(Page 1936, end of Column 1, first paragraph in Column 2)
Thus Ghebremeskel teaches that the surfactants such as polysorbate 80 (Tween 80) can be added to the solid dispersion system without fearing of hurting the stability significantly and that it can be reasonably expected to increase dissolution as expected. Together Ghebremeskel, Bechtold and Packhaeuser each demonstrate that the copovidone solid dispersion system was a preferred solid dispersion for poorly soluble active agents. Each of these used different active agents, and while the one in Packhaeuser was quite similar to the claimed compound 5, the highlighting of three different references teaching the same benefit for 3 different active agent is cited specifically to show that this benefit was known and obvious for a variety of active agents. As demonstrated by Bechtold, these dispersions can be made by solvent evaporation processes or hot-melt extrusion processes, and it would be obvious that both options are viable options and it is well within the limits of routine optimization for the ordinary artisan to select which process, and which solvent to use for the particular active agent being processed, and in particular how heat-sensitive that active agent is. Bechtold teaches that the copovidone solid dispersion can be made with the solvent process and methanol:dichloromethane as the solvents (see Example 4.6.1 in Bechtold, above or page 12). There is a reasonable expectation of success because the system is known to be useful for a variety of active agents, including other Bcl-2 inhibitors as well as other active agents. It would be an obvious benefit to increase the bioavailability and stability of the compounds in Bruncko and thus claims 50 and 59-60 are unpatentable over Bruncko in view of Packhaeuser in further view of Bechtold and Ghebremeskel.
In claim 2 applicant recites the process of claim 50, where the process further comprises adding an acid before removing the solvent. Bechtold teaches that in addition to the polymer and surfactant that additional ingredients can be included like lubricants, including stearic acid, myristic acid, and palmitic acid, (See Page 4, [0052], Bechtold). They further teach surfactants that are acids such as lauric acid (Page 4, [0061]). Thus it would be obvious to include an acid into the dispersion, which would be incorporated before the solvent is removed, thus claims 50 and 51 are also unpatentable over Bruncko in view of Packhaeuser in further view of Bechtold and Ghebremeskel.
In claims 3-4 applicant recites that the solvent is removed by heat and/or vacuum (claim 52) or rotary evaporation or spray drying (claim 53). As mentioned above, Bechtold describes the solvent process and teaches using the rotary evaporator as well as drying under vacuum at 40C (See Page 12, [0132] or above). Thus claims 52-53 are also unpatentable over Bruncko in view of Packhaeuser in further view of Bechtold and Ghebremeskel.
In claim 5 applicant recites that the solvent includes methanol, acetone, ethanol or dichloromethane (claim 54) or is a mixture of dichloromethane/methanol or THF/water (claim 55). As indicated above, Bechtold specifically describes the solvent process and teaches using dichloromethane and methanol, thus claims 54-55 are also unpatentable over Bruncko in view of Packhaeuser in further view of Bechtold and Ghebremeskel.
Claims 6-8 recite "the process of claim 50, wherein no more than about 5% of the compound of formula I... in the solid matrix is crystalline as observed by X-ray diffraction analysis (claim 32) or no more than about 2% (claim 56) or no more than 1% (claim 58). These are properties of the composition which results from the process and as such must necessarily be present in any product produced by the process. Applicant has elected the process of making and is therefore reciting a property resulting from the process, and since the process of claim 50 is obvious and it would be obvious to formulate the compounds of Bruncko, such as compound 5L, in a solid dispersion in order to increase the bioavailability of the compound and improve stability against crystallization, such a process would necessarily result in these recited levels. Further, there is a reasonable expectation of success because other formulations such as those made in Ghebremeskel had crystallinity levels that would be within those limits, as well as the compositions in Bechtold. Those are with different active agents but it would be obvious to use those systems for the compounds of Bruncko and there is a reasonable expectation that one could achieve similarly stability with regards to crystallinity. Thus claims 6-8 are also unpatentable over Bruncko in view of Packhaeuser in further view of Bechtold and Ghebremeskel.
Conclusion
Claims 1-10 are rejected.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to Jerica K Wilson whose telephone number is (703)756-4690. The examiner can normally be reached Monday-Friday 9:00-5:00.
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If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Clinton Brooks can be reached on (571)270-7682. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/J.K.W./Examiner, Art Unit 1621
/CLINTON A BROOKS/Supervisory Patent Examiner, Art Unit 1621
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