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 .
DETAILED ACTION
This office action is in reply to the Response to Election/Restriction filed 16 July 2026 for application 19/559,551 filed 06 March 2026. Claims 5 and 18 are amended. Currently, claims 1-29 are pending.
Election/Restrictions
Applicant’s election of Group I without traverse in the Remarks filed on 16 July 2026 is acknowledged.
The elected species, per the Election Requirement and Applicant’s remarks, reads upon claims 1-22 and 26. As such, claims 23-25 and 27-29 are withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a non-elected invention or species, there being no allowable generic or linking claim. Election was made in the reply filed on 16 July 2026.
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 35 U.S.C. 103 which forms the basis for all obviousness rejections set forth in this Office action:
A patent for a claimed invention may not be obtained, notwithstanding that the claimed invention is not identically disclosed as set forth in section 102, if the differences between the claimed invention and the prior art are such that the claimed invention as a whole would have been obvious before the effective filing date of the claimed invention to a person having ordinary skill in the art to which the claimed invention 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 35 U.S.C. 103 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 non-obviousness.
Claims 1-2 and 21 are rejected under 35 U.S.C. 103 as being unpatentable over Khire et al. (MEK inhibitors useful in the treatment of diseases, US 9,034,861 B2, 2015; entered into the IDS on 06 March 2026) in view of Gardner et al. (Application of high throughput technologies to drug substance and drug product development, Computers and Chemical Engineering 2004, 28, 943-953).
Khire discloses example 8, 8a and 8b, example 8b illustrated below (pgs. 34-35, col. 62-63, lines 52-50):
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Example 8 is identified as the racemic mixture where as 8a and 8b are the isolated diastereomers. The correct diastereomer is identified as example 8b, CAS 1808259-27-9.
They do not, however, teach the use of various solid forms of compound 1.
Gardner rectifies this deficiency by outlining the importance of high throughput physical-chemical technologies in the pharmaceutical discovery and development process as rapid target identification and libraries of hundreds of thousands of possible drug candidates require the support of an efficient high throughput synthetic process. Part of this process includes the rapid generation, characterization and testing of varying salt forms of small molecules and crystallization in a variety of polymorphs as these various forms of active pharmaceutical ingredients have a very broad range of pharmacokinetic, and therefore, therapeutic properties. Gardner also notes that, despite chemo-informatic programs, there is no means to determine the extent of polymorphism of any one compound and therefore the only developmental choice is to subject the active pharmaceutical ingredient to a wide variety of crystallization conditions. To that point, Gardner elevates their proprietary technology, capable of high throughput selection of forms and formulations of pharmaceutical candidates and products as a means to overcome the previously described limitation.
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The process, CrystalMax, is described as a unit capable of screening 18,000 crystallizations in parallel and can conduct thousands of studies on a single active pharmaceutical ingredient in parallel. Gardner demonstrates this process on the FDA approved drug Ritonavir by conducting 2000 parallel crystallization experiments, obtaining and identifying the two polymorphs published by Abbott in the drug’s developmental history.
Even if the compounds described by Khire are not identical to the claimed polymorphs/solid forms, it would have nonetheless been obvious to the person of ordinary skill in the art at the time of Applicant’s earliest effective filing date to follow the teachings of Gardner and obtain Applicant’s claimed polymorphs/solid forms. The person of ordinary skill in the art would have had a reasonable expectation of successfully obtaining Applicant’s claimed polymorphs/solid forms by using Gardner’s high throughput technology which permits the person of ordinary skill in the art to evaluate thousands of crystallization experiments in parallel and identify all polymorphs of a particular active agent. A rationale to support a conclusion that a claim would have been obvious is that all the claimed elements were known in the prior art and one skilled in the art could have combined the elements as claimed by known methods with no change in their respective functions, and the combination would have yielded nothing more than predictable results to one of ordinary skill in the art.
As such, it would be prima facie obvious, to a person of ordinary skill in the art, before the effective filing date, to explore different solid forms of compound 1 knowing that other drugs historically have exhibited different chemical, physical and biological properties with different solid forms. This is reinforced by Gardner who presents a technological method to perform what is traditionally a labor and time intensive process in a rapid and efficient manner.
Regarding the limitations of claim 2, comprising a free base of compound 1, is met by Khire as they disclose isolating compound 8b using chiral HPLC utilizing hexane/ethanol as the eluent. There is no indication that what is obtained is a salt form, hydrate, or other form that is not a free base.
Concerning the limitations of claim 21, an amorphous solid comprising compound 1, is met by the argument of obviousness as presented in paragraphs 5-9.
Claims 22 and 26 are rejected under 35 U.S.C. 103 as being unpatentable over Khire and Gardner as applied to claims 1-2 and 21 above, and further in view of Allen et al. (Ansel’s pharmaceutical dosage forms and drug delivery systems 10th edition, Wolters Kluwer Health 2005).
Khire discloses example 8b which reads upon compound 1 along with pharmaceutical compositions (pgs. 12, col. 19, line 60 to pg. 16, col. 28, line 32) while Gardner teaches the motivation to explore solid forms of small molecules due to their varied drug-like properties.
This is reinforced by Allen who extensively covers many topics within the field of drug formulation, including, but not limited to, typical properties of select excipients, incompatibilities, safety, related substances, along with numerous other examples in categories such as disintegrants, adhesives, and surfactants (select reading; pg. 1 – section I: introduction to drugs, drug dosage forms, and drug delivery systems; pg. 101 – section II: drug dosage form and drug delivery system design).
As such, it would be prima facie obvious, to a person of ordinary skill in the art, before the effective filing date, to incorporate the teachings of Allen to help develop an appropriate formulation for a solid form of compound 1 for use in the desired method of treatment utilizing well established literature that is exemplified by Allen.
Regarding the limitations of claim 26, a pharmaceutical composition comprising the amorphous solid of claim 21 and a pharmaceutically acceptable excipient or carrier, are met in the argument of obviousness outlined in paragraphs 12-15.
Allowable Subject Matter
Claims 3-20 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.
Reasons for Allowable Subject Matter
The following is a statement of reason for the indication of allowable subject matter: characterization of solid forms of compound 1 was not found in the prior art in a 100% embodiment. The closest match is disclosed by Khire et al. (MEK inhibitors useful in the treatment of diseases, US 9,034,861 B2, 2015), example 8b which reads upon compound 1 as a polymorph but without any further exploration into other solid forms.
Summary
Claims 1-2, 21-22 and 26 are rejected under 35 U.S.C. 103. Claims 3-20 are objected to as being dependent on a rejected base claim.
Conclusion
Claims 1-2, 21-22 and 26 are rejected. Claims 3-20 are objected to.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to Allen Chao whose telephone number is (571)272-7001. The examiner can normally be reached Monday - Friday 0700-1300.
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If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, James H Alstrum-Acevedo can be reached at 571-272-5548. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/ALLEN CHAO/Examiner, Art Unit 1622
/JAMES H ALSTRUM-ACEVEDO/Supervisory Patent Examiner, Art Unit 1622
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