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 .
Priority
The present application is the U.S. National Stage Application, pursuant to 35 U.S.C.371, of PCT International Application No. PCT US2022/027837 filed on May 5, 2022, which claims priority to US Provisional Application No. 63/184,593 filed May 5, 2021.
Requirement for Election/Restriction -Status of the Claims
In response to the Restriction Requirement mailed on May 4, 2026, Applicants have made a proper election of species in their Reply filed on July 6, 2026. Election was made without traverse of the following:
Applicant elects form 6 as the single specific solid form of the mono-tosylate compound and elects’ glaucoma as the single ocular disease or disorder.
Claims 1, 7-14, and 29-34 read on the compound of form 6.
Claims 1, 7-14, and 29-32 read on the specific ocular disease, glaucoma.
Therefore, for the reasons above and those made of record at p.2-5 of the Office Action dated May 4, 2026, the requirement remains proper and is hereby made FINAL.
Claims 1-14 and 29-34 are pending and examined on their merits.
Information Disclosure Statement
The Information Disclosure Statement (IDS) submitted on February 20, 2024 (4 references) has been received entered into the present application, in compliance with the provisions of 37CFR 1.97. Accordingly, the Information Disclosure Statement is being considered by the Examiner.
Claim Rejections - 35 USC § 112(a)
The following is a quotation of the first paragraph 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 the first paragraph of pre-AIA 35 U.S.C. 112:
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 1, 7-14, and 29-34 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.
Claim 1 recites:
A solid form of Compound 1 mono-tosylate, selected from form 1 of Compound 1 mono-tosylate, form 2 of Compound 1 mono-tosylate, form 3 of Compound 1 mono-tosylate, form 4 of Compound 1 mono-tosylate, form 5 of Compound 1 monotosylate,or form 6 of Compound 1 mono-tosylate, wherein Compound 1 is
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Claim 7 recites:
The solid form of claim 1, wherein the solid form is a crystalline form 6 of
Compound 1 mono-tosylate characterized by data selected from one or more of the following: (i) an x-ray powder diffraction (XRPD) pattern having two or more signals
selected, independently, from 9.7, 11.2, 12.8, 14.5, or 23.0 degrees 28 ± 0.2 degrees 28;
(ii) an XRPD pattern substantially as depicted in FIG. 12;
(iii) an XRPD pattern having two or more signals selected, independently, from 9. 7,
11.2, 12.8, 14.5, or 23.0 degrees 28 ± 0.2 degrees 28, and having one, two, three, or four
additional signals selected from 10.9, 20.0, 22.2, or 25.6 degrees 28 ± 0.2 degrees 28; and
(iv) combinations of any of (i)-(iii).
Claim 8 recites:
The solid form of claim 1, having an XRPD pattern substantially as shown in FIG. 1, FIG. 4, FIG. 18, FIG. 7, FIG. 10, or FIG. 12
The specification [0052] refers to FIG. 12 shows the XRPD for crystalline form 6 of Compound 1 mono-tosylate.
Claims 9 and 10 refer to differential scanning calorimetry (DSC), (as in claim 9) and thermogravimetric analysis (TGA) (as in claim 10). Each of these claims refers to figures listed in the specification. The figures listed in FIG. 3, FIG. 6, FIG. 9, FIG. 11, or FIG. 13 (as in claim 9) and in FIG. 3, FIG. 6, FIG. 9, FIG. 11, or FIG. 13 (as in claim 10).
All of the references noted in the FIGs listed above refer to the “crystalline form” of the compound. The instant claims 1, 7-14, and 29-34 all refer to a “solid form” of the compound. The scope described by applicants’ description supports a “crystalline form” of the compounds, but the claims make no mention of the crystalline form and refer to the compounds as “solid forms”.
Support for none of the solid forms of the compounds listed in claims 1, 7-14, and 29-34 is found in the specification and is thereby considered new matter.
Claim Rejections – 35 USC § 112(d)
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.
Claims 7-12 are 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.
Each of claims 7-12 is directed to a crystalline form of a mono-tosylate compound with the only further limitation based on the inherent properties of the crystalline form with no further limitation. For example, although the applicant hasn’t claimed the molecular weight the molecules it is an inherent property and cannot further limit the claim as claiming the compound alone. The same is true of how the solid crystalline salt behaves when subjected to X-rays, DCS, melting point, IR, etc.
7. (Original) The solid form of claim 1, wherein the solid form is a crystalline form 6 of
Compound 1 mono-tosylate characterized by data selected from one or more of the following:
(i) an x-ray powder diffraction (XRPD) pattern having two or more signals
selected, independently, from 9.7, 11.2, 12.8, 14.5, or 23.0 degrees 28 ± 0.2 degrees 28;
(ii) an XRPD pattern substantially as depicted in FIG. 12;
(iii) an XRPD pattern having two or more signals selected, independently, from 9. 7,
11.2, 12.8, 14.5, or 23.0 degrees 28 ± 0.2 degrees 28, and having one, two, three, or four
additional signals selected from 10.9, 20.0, 22.2, or 25.6 degrees 28 ± 0.2 degrees 28; and
(iv) combinations of any of (i)-(iii).
8. (Original) The solid form of claim 1, having an XRPD pattern substantially as shown in FIG. 1, FIG. 4, FIG. 18, FIG. 7, FIG. 10, or FIG. 12.
9. (Original) The solid form of claim 1, having a differential scanning calorimetry (DSC)
thermogram substantially as shown in FIG. 3, FIG. 6, FIG. 9, FIG. 11, or FIG. 13.
10. (Original) The solid form of claim 1, having a thermogravimetric analysis (TGA)
substantially as shown in FIG. 3, FIG. 6, FIG. 9, FIG. 11, or FIG. 13.
11. (Original) The solid form of claim 1, having a melting point range of about 114-131,
123-131, 182-200, 183-199, or 196-202 ± about 3 °C.
12. (Original) The solid form of claim 1, having a DSC signal of about 52.9, 128.9, 201.3, 131.0, 199.7, 115.3, 199.9, 186.8, 198.7, 223.8, or 201.5 ± about 3 °C.
Claim Rejections - 35 USC § 102
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 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.
Claim Rejections - 35 USC § 102
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 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.
Claims 1-14 and 29-34 are rejected under 35 U.S.C. 102(a)(1) as being anticipated by WO 2019/191654 A1, AERIE Pharmaceuticals, Delong, et.al., 3 October 2019 (hereinafter referred to as ‘654).
Claims 1, 7-14, and 29-34 are directed towards a solid form of Compound 1 mono-tosylate, selected from form 1 of Compound 1 mono-tosylate, form 2 of Compound 1 mono-tosylate, form 3 of Compound 1 mono-tosylate, form 4 of Compound 1 mono-tosylate, form 5 of Compound 1 monotosylate,or form 6 of Compound 1 mono-tosylate, wherein Compound 1 is
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“654 discloses various salts of Compound 1. Specifically, the mono-tosylate salt monohydrate is disclosed in Example 11 and Table 10 on pages 42 and 43. It should also be noted from the melting point identified below, as 135-140 degrees C, that the compound is a solid.
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Claim 1 and the dependent claims 7-13 refer to solid forms listed as mono-tosylates identified as forms 1-6. The forms taught by ‘654 are mono tosylate forms of the compounds listed in claim 1. The form listed above in Table 10 cannot be distinguished from the instant claims or any of the solid forms identified as forms 1-6.
Therefore ‘654 anticipates the mono-tosylate form of Compound 1 of claim 1.
Claims 14 and 29-34 purport a pharmaceutical composition of Compound 1 (and forms 1-6) (as in claim 14), and methods of treating various ocular diseases (as in claim 29), delivering a therapeutic amount (as in claim 30), administering to the vitreous humor of an eye (as in claim 31), ocular disease or disorder is glaucoma, a neurodegenerative disease or disorder, ocular hypertension, an inflammatory disease or disorder ocular disorders including glaucoma (as in claim 32), the ocular disease or disorder is diabetic eye disease, wet age-related macular degeneration, dry aged-related macular degeneration, inflammation, dry eye (as in claim 33), the ocular disease or disorder is uveitis, a corneal ulcer, endophthalmitis, an autoimmune disease of the cornea or ocular surface, an ophthalmic manifestation of HIV disease, or ocular herpes.
‘654 identifies using the compound 1 of the instant application to treating disease comprises glaucoma, an inflammatory eye disease, dry eye, ocular hypertension, or a neurodegenerative eye disease (as in claim 50), the disease comprises diabetic eye disease, wet age- related macular degeneration, or dry age-related macular degeneration (as in claim 51). Claims 53 and 54 are also related to ocular disorders.
Therefore, 654 anticipates using a mono-tosylate of Compound 1 of the instant application to treat the exact ocular disorders identified in Claims 14 and 29-34.
Conclusion
Claims 1, 7-14, and 29-34 are rejected.
No claims are allowed.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to PAUL RANDALL GAUGER whose telephone number is (571)272-1325. The examiner can normally be reached M-F 7:30-5:00.
Examiner interviews are available via telephone, in-person, and video conferencing using a USPTO supplied web-based collaboration tool. To schedule an interview, applicant is encouraged to use the USPTO Automated Interview Request (AIR) at http://www.uspto.gov/interviewpractice.
If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Jeffery Lundgren can be reached at (571)272-5541. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/P.R.G./Examiner, Art Unit 1629
/JEFFREY S LUNDGREN/Supervisory Patent Examiner, Art Unit 1629
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