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
Claims 1, 3, 5-6 and 8 are presented for examination.
Acknowledgement is made of the present application as a continuation of U.S. Patent Application No. 16/542,461, filed August 16, 2019, now abandoned, which is a continuation of U.S. Patent Application No. 15/387,113, filed December 21, 2016, now U.S. Patent No. 10,426,783, which is a continuation of U.S. Patent Application No. 14/362,850, filed June 4, 2014, now abandoned, which is a National Stage (371) entry of PCT Application No. PCT/JP2014/001123, filed March 3, 2014, which claims benefit under 35 U.S.C. §119(a-d) to Japanese Patent Application No. 2013-090851, filed April 24, 2013. Receipt is acknowledged of a certified copy of the ‘851 Japanese application filed January 17, 2017 in the parent ‘113 application, as required by 37 C.F.R. §1.55.
Information Disclosure Statement
Applicant’s Information Disclosure Statement (IDS) filed March 15, 2024 (seven pages total) has been received and entered into the present application. As reflected by the attached, completed copy of form PTO/SB/08a, the Examiner has considered the cited references.
Priority
Acknowledgement is made of the present application as a continuation of U.S. Patent Application No. 16/542,461, filed August 16, 2019, which is a continuation of U.S. Patent Application No. 15/387,113, filed December 21, 2016, which is a continuation of U.S. Patent Application No. 14/362,850, filed June 4, 2014, now abandoned, which is a National Stage (371) entry of PCT Application No. PCT/JP2014/001123, filed March 3, 2014, which claims benefit under 35 U.S.C. §119(a-d) to Japanese Patent Application No. 2013-090851, filed April 24, 2013. The later-filed application must be an application for a patent for an invention which is also disclosed in the prior application (the parent or original non-provisional application or provisional application). The disclosure of the invention in the parent application and in the later-filed application must be sufficient to comply with the requirements of 35 U.S.C. §112(a) or the first paragraph of pre-AIA 35 U.S.C. §112, except for the best mode requirement. See Transco Products, Inc. v. Performance Contracting, Inc., 38 F.3d 551, 32 USPQ2d 1077 (Fed. Cir. 1994).
The disclosure of prior-filed U.S. Patent Application No. 15/387,113, filed December 21, 2016, and U.S. Patent Application No. 14/362,850, filed June 4, 2014, each provide adequate written support and enabling guidance as set forth under the requirements of 35 U.S.C. §112(a) or the first paragraph of pre-AIA 35 U.S.C. §112. Moreover, since the ‘850 application was filed as a National Stage (371) entry of PCT Application No. PCT/JP2014/001123, filed March 3, 2014, adequate written support and enabling guidance as set forth under the requirements of 35 U.S.C. §112(a) or the first paragraph of pre-AIA 35 U.S.C. §112 may be found in the ‘123 PCT application by virtue of the identical disclosures.
However, the disclosure of prior-filed Japanese Patent Application No. 2013-090851, filed April 24, 2013, is published in Japanese and, therefore, cannot be fully evaluated to determine its sufficiency of support for the claimed invention as it was not published in English and a certified English language translation has not been provided in the record.
Accordingly, the effective filing date of claims 1, 3, 5-6 and 8 is March 3, 2014 (the filing date of PCT Application No. PCT/JP2014/001123).
The Examiner will revisit the issue of priority as necessary each time the claims are amended.
Claim Rejections - 35 USC § 112(b) (Pre-AIA Second Paragraph)
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.
(1) Claims 1, 3, 5-6 and 8 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 applications subject to pre-AIA 35 U.S.C. 112, the applicant), regards as the invention.
In claim 1, Applicant recites “[a] method of preventing or treating ocular fundus disease” via the step of “administering an agent comprising (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine, a salt thereof, or a solvate thereof to a subject in need thereof”, which renders the claim indefinite because the “need” of the recited subject is not clearly and precisely set forth. For example, it is unclear if the subject is in need of “preventing or treating ocular fundus disease”, or in need of (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine (or salt or solvate thereof) itself for any therapeutic purpose.
Clarification is required.
As claims 3, 5-6 and 8 do not remedy this point of confusion in claim 1, they propagate the ambiguity of claim 1 and, therefore, must be rejected on the same grounds.
For these reasons, the claims fail to meet the tenor and express requirements of 35 U.S.C. §112(b) (pre-AIA second paragraph) and are, thus, properly rejected.
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.
(2) Claims 1, 3, 5-6 and 8 are rejected under 35 U.S.C. 102(a)(1) as being anticipated by Hidaka et al. (U.S. Patent Application Publication No. 2008/0064681 A1; 2008, cited by Applicant on the 03/15/24 IDS),
citing to Sawai (U.S. Patent No. 9,616,069 B2; 20171, cited by Applicant on the 03/15/24 IDS) and Bock et al. (“Classifying Glaucoma with Image-Based Features from Fundus Photographs”, 2007, Presented in Pattern Recognition. DAGM 2007. Lecture Notes in Computer Science, Vol.4713, cited by Applicant on the 03/15/24 IDS) as evidence.
Hidaka et al. teaches compounds of formula (1), which has the chemical structure
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111
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, in which ring A represents a 5- to 11-membered cyclic amino group, which may be further substituted, and X is a halogen atom, or more specifically compounds of the narrower structure of formula (4)
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122
161
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, in which X is a halogen atom, in particular, bromine, chlorine or fluorine, which are effective to reduce intraocular pressure when administered to a glaucoma patient (abstract; p.1, para.[0007]-[0008]; p.2-3, para.[0025]; p.3, para.[0026]). Hidaka et al. teaches that the compound may also be in the form of a salt or a solvate, such as a hydrate (p.3, para.[0027]). Hidaka et al. teaches that the efficacy of the compounds to reduce intraocular pressure and thereby treat glaucoma renders them particularly useful when formulated as eye drops using a pharmaceutically acceptable carrier therefor (p.4, para.[0039]-[0040]). Hidaka et al. exemplifies synthesis of the compound “F7”, also known as (S)-hexahydro-1-(4-fluoroisoquinoline-5-sulfonyl)-2-methyl-1H-1,4-diazepine dihydrochloride, which has the chemical structure
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123
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and corresponds to Hidaka’s compounds of formula (4), in which X is fluorine (Ex.1, p.4, para.[0043]). Hidaka et al. teaches the compound F7 as having inhibitory activity on Rho-kinase, as evidenced by the IC50 value reported in Table 1 (p.13, para.[0115]). Hidaka et al. teaches the preparation of compound F7 into an eye drop formulation, obtained by dissolving 1.0 g of the compound in a phosphate buffer solution (which was prepared by dissolving 0.8 g of sodium dihydrogen phosphate and 0.5 g of sodium chloride in purified water to a final weight of 100 g, after which the pH was adjusted to 7.0 using sodium hydroxide), for administration to rabbits to determine the effect of the compound on intraocular pressure (Ex.2, p.13, para.[0117]-[0119]). Hidaka et al. teaches that instillation of the F7-containing eye drop was effective to reduce intraocular pressure 1.9x more than control Rho-kinase inhibitor compound M, and that the period of time in which the intraocular pressure-reducing effect was demonstrated was also about 3 h longer than that of control compound M (p.13, para.[0120]-[0121]).
F7 identified in Hidaka et al. corresponds to Applicant’s instantly claimed compound (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine, as evidenced by Sawai’s teachings that instantly claimed (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine is also known as ripasudil, and has the chemical structure
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133
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(col.1, l.18-34, col.1, l.60-63), which is identical to Hidaka’s chemical structure.
In claim 1, Applicant recites “[a] method of preventing or treating ocular fundus disease” via administering an agent comprising (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine to a subject in need thereof.
Regarding Applicant’s embodiment directed to the treatment of an ocular fundus disease (claim 1), Hidaka et al. clearly teaches the administration of (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine for the treatment of glaucoma, which is an ocular fundus disease as evidenced by Bock’s teaching that glaucoma is an ocular disease characterized by changes in the fundus (“1. Introduction”, p.355, para.1).
Regarding Applicant’s embodiment directed to the prevention of an ocular fundus disease (claim 1), such as diabetic macular edema (claim 3), Applicant’s method requires the administration of (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine to a subject in need of prevention of an ocular fundus disease (such as diabetic macular edema) to yield the recited therapeutic objective of preventing the ocular fundus disease. As any subject is reasonably in need of prevention of an ocular fundus disease (such as diabetic macular edema) – including those subjects of Hidaka et al. – the resultant effect of preventing ocular fundus disease (such as diabetic macular edema) must necessarily yield from the practice of Hidaka’s method. This is because products of identical chemical composition cannot have mutually exclusive properties when used in an identical manner. A compound and its attributed properties are inseparable. MPEP §2112.
MPEP §2112 states that, “[T]he discovery of a previously unappreciated property of a prior art composition, or of a scientific explanation for the prior art’s functioning, does not render the old composition patentably new to the discoverer.” Atlas Powder Co. v. Ireco Inc., 190 F.3d 1342, 1347, 51 USPQ2d 1943, 1947 (Fed. Cir. 1999). Thus the claiming of a new use, new function or unknown property which is inherently present in the prior art does not necessarily make the claim patentable. In re Best, 562 F.2d 1252, 1254, 195 USPQ 430, 433 (CCPA 1977).” There is no requirement that a person of ordinary skill in the art would have recognized the newly cited function and/or property at the time of invention, as long as the function and/or property is reasonably expected to be present. Schering Corp. v. Geneva Pharm. Inc., 339 F.3d 1373, 1377, 67 USPQ2d 1664, 1668 (Fed. Cir. 2003); see also Toro Co. v. Deere & Co., 355 F.3d 1313, 1320, 69 USPQ2d 1584, 1590 (Fed. Cir. 2004) (“[T]he fact that a characteristic is a necessary feature or result of a prior-art embodiment … is enough for inherent anticipation, even if that fact was unknown at the time of the prior invention”).
MPEP §2131.01 states that “[n]ormally, only one reference should be used in making a rejection under 35 U.S.C. 102”, but that it is proper to apply a second reference when the extra reference is cited for the purpose of “show[ing] that a characteristic not disclosed in the reference is inherent”.
Therefore, instant claims 1, 3, 5-6 and 8 are properly anticipated under AIA 35 U.S.C. §102(a)(1).
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.
Provisional Rejections
(3) Claims 1, 3, 5-6 and 8 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 2, 8, 11, 14, 16, 18 and 20 of U.S. Patent Application No. 17/430,068.
Claims 2 and 11 of the ‘068 application recite a method for modulating expression of an extracellular matrix protein by corneal endothelial cells in a subject comprising administering (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine (or a salt or solvate thereof) to the eye of the subject. Claim 8 of the ‘068 application specifies that the administration to the eye is in the form of an eye drop.
Claim 14 of the ‘068 application recites a method for preventing and/or suppressing guttae formation by modulating an expression of an extracellular matrix protein by corneal endothelial cells in a subject comprising administering (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine (or a salt or solvate thereof) to the eye of the subject in the form of an eye drop. Claim 16 of the ‘068 application specifies that the subject is an FECD patient and the administration to the eye is in the form of an eye drop.
Claim 18 of the ‘068 application recites a method for preventing and/or suppressing recurrence of guttae formation in a subject comprising administering (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine (or a salt or solvate thereof) to the eye of the subject in the form of an eye drop. Claim 20 of the ‘068 application specifies that the subject is an FECD patient and the administration to the eye is in the form of an eye drop.
The embodiments of the ‘068 claims directed to the modulation of expression of an extracellular matrix protein by corneal endothelial cells anticipates Applicant’s claimed embodiment directed to “preventing” ocular fundus disease, as the subject of the instant claims must simply be “in need” of ocular fundus disease prevention, which reasonably circumscribes any subject and is, thus, necessarily met by those subjects of the ‘068 claims.
As the ‘068 claims provide for the combination to be administered directly to the eye, such as via eye drop, such teachings clearly satisfy Applicant’s requirement that the (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine is (i) an ophthalmic preparation (claim 5), or (ii) administered via ocular instillation (claims 6, 8).
This is a provisional nonstatutory double patenting rejection.
(4) Claims 1, 3, 5-6 and 8 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1, 5, 7-9, 11-16, 22, 28-33 and 40-47 of U.S. Patent Application No. 18/270,728.
Claims 1, 5, 7-8, 12-16, 22 and 40-47 of the ‘728 application are directed to a method of treating Fuchs Endothelial Corneal Dystrophy (FECD) affecting the Descemet membrane of a patient’s cornea comprising removing a central portion of the Descemet membrane from the patient’s eye, topically administering to the patient’s eye a therapeutically effective amount of ripasudil (or a pharmaceutically acceptable salt thereof), and tapering the therapeutically effective amount to zero over approximately two weeks. Claims 9 and 28-33 of the ‘728 application define the ripasudil to be administered in the form of a preservative-free liquid formulation.
The embodiments of the ‘728 claims directed to the treatment of FECD affecting the Descemet membrane of a patient’s cornea anticipates Applicant’s instantly claimed embodiment directed to “preventing” ocular fundus disease, as the subject of the instant claims must simply be “in need” of ocular fundus disease prevention, which reasonably circumscribes any subject and is, thus, necessarily met by those subjects of the ‘728 claims.
As the ‘728 claims provide for the combination to be administered topically to the eye (via a liquid formulation), such teachings satisfy Applicant’s requirement that the (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine is (i) an ophthalmic preparation (claim 5), or (ii) administered via ocular instillation (claims 6, 8).
This is a provisional nonstatutory double patenting rejection.
(5) Claims 1 and 3 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-11 of U.S. Patent Application No. 18/608,109.
Claims 1-9 of the '109 application recite a pharmaceutical preparation comprising an aqueous composition of ripasudil (or a salt thereof, or a solvate thereof, or a solvate of the salt), and a package that blocks ultraviolet light with wavelength of 300-335 nm. Claims 9-11 of the '109 application further recite a method for improving photostability of, or for preserving, ripasudil (or a salt thereof, or a solvate thereof, or a solvate of the salt) in an aqueous composition comprising storing an aqueous composition comprising ripasudil (or a salt thereof, or a solvate thereof, or a solvate of the salt) in a package that blocks ultraviolet light with wavelength of 300-335 nm.
In the '109 disclosure, the applicant discloses that the aqueous composition is used for the prevention or treatment of an ocular fundus disease, wherein the ocular fundus disease is further defined as, e.g., diabetic macular edema (p.40, para.[0055]).
This is a provisional nonstatutory double patenting rejection.
Non-Provisional Rejections
(6) Claims 1, 3, 5-6 and 8 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-15 of U.S. Patent No. 8,193,193 B2,
citing to Bock et al. (“Classifying Glaucoma with Image-Based Features from Fundus Photographs”, 2007, Presented in Pattern Recognition. DAGM 2007. Lecture Notes in Computer Science, Vol.4713, cited by Applicant on the 03/15/24 IDS).
‘193 recites a composition comprising the Rho kinase inhibitor (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine, with brinzolamide (or a salt thereof), or a kit thereof, as well as a method of treating glaucoma or ocular hypertension by administering the Rho kinase inhibitor (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine, with brinzolamide (or a salt thereof) to the eye in amounts sufficient to treat the glaucoma (patent claims 1-13). ‘193 further recites that the (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine is the hydrogen chloride dihydrate, and is present in the form of an aqueous solution (patent claims 14-15).
The embodiment of the ‘193 claims directed to the treatment of ocular hypertension anticipates Applicant’s claimed embodiment directed to “preventing” ocular fundus disease, as the subject of the instant claims must simply be “in need” of ocular fundus disease prevention, which reasonably circumscribes any subject and is, thus, necessarily met by the ocular hypertension subject of the ‘193 claims.
As the ‘193 claims clearly recite that the Rho kinase inhibitor is administered directly to the eye, such teachings clearly satisfy Applicant’s requirement that the (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine is (i) an ophthalmic preparation (claim 5), or (ii) administered via ocular instillation (claims 6, 8).
Bock et al. is cited as factual extrinsic evidence necessary to establish that glaucoma is an ocular disease characterized by changes in the fundus (“1. Introduction”, p.355, para.1), thereby constituting an “ocular fundus disease” as recited in Applicant’s instant claim 1.
This is a non-provisional nonstatutory double patenting rejection.
(7) Claims 1, 3, 5-6 and 8 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-28 of U.S. Patent No. 8,629,161 B2.
‘161 recites a method for treating glaucoma in a subject in need thereof comprising administering to said subject a therapeutically effective amount of a Rho kinase inhibitor, which is (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine, at a concentration of 0.5%, and bunazosin at 0.01% in solution (patent claims 1, 3, 11, 13). ‘161 further recites that the Rho kinase inhibitor and bunazosin are combined in an ophthalmological preparation (patent claim 5), such as an aqueous eye drop, eye ointment, etc. (patent claims 6-7). ‘161 further recites a substantially identical method, but for the administration of the Rho kinase inhibitor at a concentration of 1.5% in solution (patent claims 15, 17, 19-21, 25, 27).
‘161 recites a method for treating ocular hypertension in a subject in need thereof comprising administering to said subject a therapeutically effective amount of a Rho kinase inhibitor, which is (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine, at a concentration of 0.5%, and bunazosin at 0.01% in solution (patent claims 2, 4, 12, 14). ‘161 further recites that the Rho kinase inhibitor and bunazosin are combined in an ophthalmological preparation (patent claim 8), such as an aqueous eye drop, eye ointment, etc. (patent claims 9-10). ‘161 further recites a substantially identical method, but for the administration of the Rho kinase inhibitor at a concentration of 1.5% in solution (patent claims 16, 18, 22-24, 26, 28).
The embodiment of the ‘161 claims directed to the treatment of ocular hypertension anticipates Applicant’s instantly claimed embodiment directed to “preventing” ocular fundus disease, as the subject of the instant claims must simply be “in need” of ocular fundus disease prevention, which reasonably circumscribes any subject and is, thus, necessarily met by the ocular hypertension subject of the ‘161 claims.
As the ‘161 claims provide for the combination to be administered directly to the eye, such as via eye drop, such teachings clearly satisfy Applicant’s requirement that the (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine is (i) an ophthalmic preparation (claim 5), or (ii) administered via ocular instillation (claims 6, 8).
This is a non-provisional nonstatutory double patenting rejection.
(8) Claims 1, 3, 5-6 and 8 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 2, 4, 7-8, 14 and 17-19 of U.S. Patent No. 9,616,069 B2.
‘069 recites an aqueous composition comprising from 0.01-5% w/v carbonic anhydrase inhibitor and from 0.01-10% w/v of ripasudil (or a solvate or salt thereof) (patent claims 2, 4). ‘069 further recites a pharmaceutical preparation of the aqueous composition contained inside a polyolefin resin container (patent claim 7), particularly wherein the polyolefin resin container comprises polypropylene (patent claim 8). ‘069 further recites a method for suppressing discoloration of an aqueous composition of ripasudil comprising mixing from 0.01-5% w/v carbonic anhydrase inhibitor with from 0.01-10% w/v of ripasudil (or a solvate or salt thereof) (patent claims 14, 17-19).
In the ‘069 disclosure, the patentee discloses that the aqueous composition is used for the prevention or treatment of an ocular fundus disease (col.3, l.38-41), wherein the ocular fundus disease is further defined as including diabetic macular edema (col.12, l.46-67).
This is a non-provisional nonstatutory double patenting rejection.
(9) Claims 1, 3, 5-6 and 8 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-6 of U.S. Patent No. 9,844,556 B2.
‘556 recites a method for preventing or treating complications following cataract surgery comprising administering to a subject with or at risk of complications after cataract surgery a medicine comprising a preventively or therapeutically effective amount of 4-fluoro-5-{[(2S)-2-methyl-1,4-diazepan-1-yl]sulfonyl}isoquinoline2 (or a salt thereof, or a solvate thereof) as an active ingredient, wherein the complications after cataract surgery is secondary cataract or anterior capsule contraction (patent claim 1-4, 6). ‘556 recites that the medicine is in the form of an ophthalmic solution (patent claim 5).
The embodiment of the ‘556 claims directed to the prevention or treatment of complications following cataract surgery anticipates Applicant’s instantly claimed embodiment directed to “preventing” ocular fundus disease, as the subject of the instant claims must simply be “in need” of ocular fundus disease prevention, which reasonably circumscribes any subject and is, thus, necessarily met by the subject of the ‘556 claims.
The provision of the medicine in the form of an ophthalmic solution necessarily meets Applicant’s instantly claimed requirements directed to the recited compound being in the form of an ophthalmic preparation (claim 5), or that the administration is performed via ocular instillation (claims 6, 8).
This is a non-provisional nonstatutory double patenting rejection.
(10) Claims 1, 3, 5-6 and 8 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-9 of U.S. Patent No. 10,034,885 B2.
‘885 recites a method of modulating a thickness of cornea of a subject comprising measuring the thickness of the cornea of the subject, and administering 1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine to the subject (patent claims 1, 3-7, 10). ‘885 specifies that the compound is in the (S)-configuration (patent claim 2). ‘885 further recites that the compound is administered to the eye (patent claim 8), specifically as an eyedrop (patent claim 9).
In the ‘885 disclosure, the patentee defines the claimed compound of the patent claims as having an (R)- and (S)- isomer (col.4, l.3-10; col.5, l.39-40), thereby establishing that the recitation in patent claim 1 necessarily includes both the (R)- and (S)- forms thereof.
The method of the ‘885 claims anticipates Applicant’s instantly claimed embodiment directed to “preventing” ocular fundus disease, as the subject of the instant claims must simply be “in need” of ocular fundus disease prevention, which reasonably circumscribes any subject and is, thus, necessarily met by the subject of the ‘885 claims.
This is a non-provisional nonstatutory double patenting rejection.
(11) Claims 1, 3, 5-6 and 8 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-9 of U.S. Patent No. 10,220,043 B2,
citing to Bock et al. (“Classifying Glaucoma with Image-Based Features from Fundus Photographs”, 2007, Presented in Pattern Recognition. DAGM 2007. Lecture Notes in Computer Science, Vol.4713, cited by Applicant on the 03/15/24 IDS).
‘043 recites an aqueous composition comprising ripasudil (or a salt thereof, or a solvate thereof), and brimonidine (or a salt thereof) (patent claims 1-2). ‘043 further recites that the ripasudil is ripasudil hydrochloride (patent claim 3), or that the brimonidine is brimonidine tartrate (patent claim 4). ‘043 recites that the aqueous composition is an ophthalmic agent (patent claim 5), or specifically an eye drop (patent claim 6), and further provides for the use of such aqueous composition for the treatment of ocular hypertension or glaucoma when administered to a subject in need of such treatment (patent claims 7-9).
The embodiment of the ‘043 claims directed to the treatment of ocular hypertension anticipates Applicant’s claimed embodiment directed to “preventing” ocular fundus disease, as the subject of the instant claims must simply be “in need” of ocular fundus disease prevention, which reasonably circumscribes any subject and is, thus, necessarily met by the ocular hypertension subject of the ‘043 claims.
Bock et al. is cited as factual extrinsic evidence necessary to establish that glaucoma is an ocular disease characterized by changes in the fundus (“1. Introduction”, p.355, para.1), thereby constituting an “ocular fundus disease” as recited in Applicant’s instant claim 1.
This is a non-provisional nonstatutory double patenting rejection.
(12) Claims 1, 3, 5-6 and 8 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-9 of U.S. Patent No. 10,376,523 B2.
‘523 recites an aqueous composition of ripasudil (or a salt thereof, or a solvate of ripasudil or the salt thereof) and benzalkonium chloride, wherein the composition does not contain brinzolamide, and the content of benzalkonium chloride is from 0.0002-0.0025 parts by mass, relative to 1 part by mass of ripasudil (patent claims 1, 5-9), wherein the aqueous composition is an eye drop (patent claim 2). ‘523 further recites a method of producing the aqueous composition (patent claims 3-4).
In the ‘523 disclosure, the patentee discloses that the aqueous composition is used for the prevention or treatment of an ocular fundus disease, wherein the ocular fundus disease is further defined as including diabetic macular edema (col.10, l.25-44).
The provision of the aqueous composition in the form of an eye drop necessarily meets Applicant’s instantly claimed requirements directed to the recited compound being in the form of an ophthalmic preparation (claim 5), or the administration is performed via ocular instillation (claims 6, 8).
This is a non-provisional nonstatutory double patenting rejection.
(13) Claims 1, 3, 5-6 and 8 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-9 of U.S. Patent No. 10,537,579 B2.
‘579 recites a method for suppressing rejection after cornea transplantation comprising administering an effective amount of the Rho kinase inhibitor ripasudil (or a salt thereof, or a solvate thereof) to a patient in need thereof (patent claims 1-4, 6-12). ‘579 further recites that the Rho kinase inhibitor is administered in an ophthalmic preparation (patent claim 5).
The method of the ‘579 claims anticipates Applicant’s instantly claimed embodiment directed to “preventing” ocular fundus disease, as the subject of the instant claims must simply be “in need” of ocular fundus disease prevention, which reasonably circumscribes any subject and is, thus, necessarily met by the subject of the ‘579 claims.
As the ‘579 claims clearly recite that the Rho kinase inhibitor is administered via an ophthalmic preparation, such teachings clearly satisfy Applicant’s requirement that the (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine (ripasudil) is (i) an ophthalmic preparation (claim 5), or (ii) administered via ocular instillation (claims 6, 8).
This is a non-provisional nonstatutory double patenting rejection.
(14) Claims 1, 3, 5-6 and 8 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-7 of U.S. Patent No. 10,426,783 B2.
‘783 recites a method of treating ocular fundus disease, wherein the ocular fundus disease is a diabetic macular edema or exudative age-related macular degeneration, comprising administering an effective amount of an agent comprising (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine, a salt thereof, or a solvate thereof, to a subject in need thereof (patent claims 1-3). ‘783 recites that the agent is an ophthalmic preparation (patent claim 4), or that the administration of the agent is performed by ocular instillation (patent claims 5-7).
The method of treating exudative age-related macular degeneration in the ‘783 claims anticipates Applicant’s claimed embodiment directed to “preventing” ocular fundus disease, as the subject of the instant claims must simply be “in need” of ocular fundus disease prevention, which reasonably circumscribes any subject and is, thus, necessarily met by the subject of the ‘783 claims.
This is a non-provisional nonstatutory double patenting rejection.
Conclusion
Rejection of claims 1, 3, 5-6 and 8 is proper.
No claims of the present application are allowed.
Applicant is requested to specifically point out the support for any amendments made to the disclosure in response to this Office action, including the claims (M.P.E.P. §§ 714.02 and 2163.06). In doing so, applicant is requested to refer to pages and line (or paragraph) numbers (if available) in the as-filed specification, not the published application. Due to the procedure outlined in M.P.E.P. § 2163.06 for interpreting claims, other art may be applicable under 35 U.S.C. § 102 or 35 U.S.C. § 103(a) once the aforementioned issue(s) is/are addressed.
Applicant is reminded that MPEP §2001.06(b) clearly states that “[t]he individuals covered by 37 C.F.R. 1.56 have a duty to bring to the attention of the examiner, or other Office official involved with the examination of a particular application, information within their knowledge as to other copending United States applications which are "material to patentability" of the application in question." See Armour & Co. v. Swift & Co., 466 F.2d 767, 779, 175 USPQ 70, 79 (7th Cir. 1972). MPEP §2001.06(b) clearly indicates that “if a particular inventor has different applications pending in which similar subject matter but patentably indistinct claims are present that fact must be disclosed to the examiner of each of the involved applications.” See Dayco Prod. Inc. v. Total Containment, Inc., 329 F.3d 1358, 1365-69, 66 USPQ2d 1801, 1806-08 (Fed. Cir. 2003).
Any inquiry concerning this communication or earlier communications from the examiner should be directed to Leslie A. Royds Draper whose telephone number is (571)272-6096. The examiner can normally be reached Tuesday to Thursday (08:30 AM to 05:00 PM).
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/Leslie A. Royds Draper/Primary Examiner, Art Unit 1629
March 4, 2026
1 MPEP §2124 states that “references cited to show a universal fact need not be available as prior art before applicant’s filing date. In re Wilson, 311 F.2d 266, 135 USPQ 442 (CCPA 1962). Such facts include the characteristics and properties of a material or a scientific truism.” In the instant case, Sawai is cited for its teaching that the chemical name (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine of the instant claims is synonymous with ripasudil, which is also synonymous with the chemical name (S)-hexahydro-1-(4-fluoroisoquinoline-5-sulfonyl)-2-methyl-1H-1,4-diazepine used in Hidaka et al. As this is a universal fact, such teachings are not required to antedate Applicant’s filing date.
2 This chemical name is synonymous with ripasudil, the instantly claimed compound, as evidenced by the identical chemical structures (‘556, col.4, l.12-27).