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 .
Status of Claims
Claims 1-2, 44-45, 48-49, 55, 58, and 61 are pending in the instant application.
Claims 3-43, 46-47, 50-54, 56-57, 59-60, and 62-86 have been canceled.
Election/Restriction
This action is in response to an election from a restriction requirement filed on October 17th, 2025. There are 9 claims pending and 6 claims under consideration. Claims 48-49 and 55 have been withdrawn as claims drawn to a non-elected invention. This is the first action on the merits. The present invention relates to a crystalline form of a compound having the structure:
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Applicant’s election of Group I, Claims 1-2, 44-45, 58, and 61 without traverse in the reply filed January 20th, 2026 is acknowledged. The requirement for restriction is deemed proper and therefore made FINAL.
Domestic Benefit
Acknowledgement is made of Applicant’s claim for domestic benefit based on the U.S. Provisional Application No. 63/050,642, filed July 10th, 2020. Claims 1-2, 44-45, 58, and 61, presently under consideration, are fully supported by this application and will be evaluated with an effective filing date of July 10th, 2020.
Information Disclosure Statement
The Information Disclosure Statements filed on October 24th, 2023, December 12th, 2023, April 11th, 2024, July 25th, 2024, and December 13th, 2024 have been fully considered by the examiner except where marked with a strikethrough.
Specification
The specification has not been checked to the extent necessary to determine the presence of all possible minor errors. Applicant’s cooperation is requested in correcting any of the errors of which Applicant may become aware of in the specification.
Drawings
Acknowledgement is made of the drawings received on January 10th, 2023. These drawings are acceptable.
Claim Rejections - 35 USC § 112
The following is a quotation of 35 U.S.C. 112(d):
(d) REFERENCE IN DEPENDENT FORMS.—Subject to subsection (e), a claim in dependent form shall contain a reference to a claim previously set forth and then specify a further limitation of the subject matter claimed. A claim in dependent form shall be construed to incorporate by reference all the limitations of the claim to which it refers.
The following is a quotation of pre-AIA 35 U.S.C. 112, fourth paragraph:
Subject to the following paragraph [i.e., the fifth paragraph of pre-AIA 35 U.S.C. 112], a claim in dependent form shall contain a reference to a claim previously set forth and then specify a further limitation of the subject matter claimed. A claim in dependent form shall be construed to incorporate by reference all the limitations of the claim to which it refers.
Claim 2 is rejected under 35 U.S.C. 112(d) or pre-AIA 35 U.S.C. 112, 4th paragraph, as being of improper dependent form for failing to further limit the subject matter of the claim upon which it depends, or for failing to include all the limitations of the claim upon which it depends.
Claim 1 is drawn to a crystalline form of a compound having the structure
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wherein the crystalline form is Form A. Dependent Claim 2 recites limitations specifying the crystalline form is anhydrous and is characterized by the properties recited in the claim. These additional recited limitations, however, fail to further limit Claim 1. In the instant specification, Figure 1 shows an X-ray diffraction pattern (XRPD) including a diffractogram corresponding to anhydrous Form A, and Figures 3A and 3B correspond to thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC) curves of anhydrous Form A. Further, the methods of producing crystalline Form A are drawn to producing anhydrous Form A, for example as disclosed in the instant specification at Page 50, Paragraph 0182, Page 52, Paragraph 0189. At Page 74, Paragraph 0239, it is stated “Forms A, B, Material D, and Form E are anhydrous forms of Compound 1.” Beginning at Page 75, experimental data disclosing the characterization of Form A including XRPD peaks, it is noted it belongs to space group C2/c, the parameters of the unit cell, and that the DSC curve exhibits an exotherm with an onset of 207oC.
Therefore, by definition, Form A is an anhydrous crystalline form of the compound recited at Claim 1 with the characteristics specifically recited at Claim 2. Because Claim 1 is drawn to Form A of the compound, the characteristics recited at Claim 2 are, by definition, included in the recitation of the limitation that the compound is crystalline Form A, and therefore, Claim 2 fails to further limit Claim 1.
Applicant may cancel the claim(s), amend the claim(s) to place the claim(s) in proper dependent form, rewrite the claim(s) in independent form, or present a sufficient showing that the dependent claim(s) complies with the statutory requirements.
Claim Rejections - 35 USC § 103
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 nonobviousness.
Claims 44-45 are rejected under 35 U.S.C. 103 as being unpatentable over Mekonnen et. al. (WO 2019/246300 A1; cited on Applicant’s Information Disclosure Statement filed October 24th, 2023; hereinafter referred to as Mekonnen) in view of Giron (“Thermal analysis and calorimetric methods in the characterization of polymorphs and solvates”, Thirmochimica Acta, 248, 1-59, 2019; hereinafter referred to as Giron).
At Page 238, Mekonnen teaches a compound at entry 606 having the structure:
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This is the same structure as is instantly recited at Claim 1.
At Page 664, Claim 13, Mekonnen teaches a pharmaceutical composition comprising a compound according to any one of claims 1-12 (including the above compound, recited at Claim 12) or a polymorph thereof.
Regarding Claim 45, Mekonnen teaches at Claims 14-15 a pharmaceutical composition as noted above further comprising a second therapeutic agent wherein the second therapeutic agent is selected from an antipsychotic, memantine and an acetylcholine esterase inhibitor (AChE-I), as recited at instant Claim 45. At Page 269, Paragraph 0209, Mekonnen teaches liquid dosage forms may contain inert diluents commonly used in the art such as water.
Mekonnen does not teach a crystalline form of this compound wherein the crystalline form is Form A.
At Page 47, Paragraph 0174 of the instant specification, Applicant states, “In some embodiments, pharmaceutical compositions or combinations (or one or more of their components) according to the disclosure may also be in an aqueous or non-aqueous liquid dosage form including solution … In some embodiments, the pharmaceutical composition or combination of the disclosure is in an aqueous solution.” Therefore, the broadest reasonable interpretation of the pharmaceutical composition as recited at instant Claim 44 includes an aqueous solution comprising the crystalline Form A of the compound according to Claim 1.
At Page 1, under “Introduction,” Giron teaches, “The solid forms of the same compound are called polymorphs or crystalline modifications. Polymorphs show the same properties in the liquid or gaseous state but they behave differently in the solid state.” In view of this, a person having ordinary skill in the art would expect the properties unique to Form A as recited at instant Claim 1 would not be observed upon dissolution of Form A to generate an aqueous solution. Therefore, a pharmaceutical composition taught by Mekonnen, as noted above, obviates the instantly claimed compositions at Claims 44-45 despite being generated from a form other than Form A as recited at instant Claim 1 because the polymorphic properties of Form A will not be retained upon dissolution in aqueous media.
Allowable Subject Matter
Claims 1, 58, and 61 are allowed.
Conclusion
Claims 2 and 44-45 are rejected.
Claims 1, 58, and 61 are allowed.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to DANIEL JOHN BURKETT whose telephone number is (703)756-5390. The examiner can normally be reached Monday - Friday.
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/D.J.B./Examiner, Art Unit 1624
/JEFFREY H MURRAY/Supervisory Patent Examiner, Art Unit 1624