DETAILED ACTION
Notice of 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 the Claims
The amendments filed 1/22/2026 have been entered.
Response to Arguments
Applicant’s arguments, filed 1/22/2026, have been fully considered.
The objection to claims 54-56 is WITHDRAWN in view of Applicant’s amendments to the claims.
The rejection of claims 8 and 54-55 under 35 U.S.C. 112(b) is WITHDRAWN in view of Applicant’s amendments to the claims.
The rejection of claims 1, 4 and 57-58 under 35 U.S.C. 103(a) is WITHDRAWN in view of Applicant’s amendments to the claims.
The rejection of claims 1, 4, 8 and 5-58 on the grounds of Nonstatutory Double Patenting based on 17/054,468 and 10,858,368 are WITHDRAWN in view of Applicant’s amendments to the claims.
Claims 1 and 57-58 are newly rejected under 35 U.S.C. 112(b).
Claims 1 and 54-58 are MAINTAINED rejected on the grounds of Nonstatutory Double Patenting based on 17/776,531.
Applicant traverses the rejection of claims on the grounds of Nonstatutory Double Patenting based on 17/776,531. As argued by Applicant, “[w]hile ODP and obviousness under § 103 are analogous, only the claims of a reference patent and the subject application are compared for ODP” (Applicant Arguments, Page 52). Applicant argues that “the instant claims are patentably distinct from the reference claims” (Applicant Arguments, Page 52).
The argument is not found persuasive. Applicant is advised that the arguments of counsel cannot take the place of evidence in the record. In re Shulze, 346 F.2d 600 (CCPA 1965; see also In re Lovin, 652 F.3d 1349 (Fed. Cir. 2011) where it is noted that “the Board reasonably interpreted Rule 41.37 to require more substantive arguments in an appeal brief than a mere recitation of the claim elements and a naked assertion that the corresponding elements were not found in the prior art”).
The ‘531 application claims a compound of Formula (1*) (claim 1) and compositions thereof (claim 42), specifically reciting the following compound species:
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(claim 41, Compound 6);
which differs from the instantly claimed compounds in comprising -O- in place of -NH- (i.e., comprising a tetrohydrofuran ring as opposed to a pyrrolidine ring), as indicated by arrow.
Yet, as taught by Williams et al “[w]hen a lead compound is first discovered for a particular disease state, it often lacks the required potency and pharmacokinetic properties suitable for making it a viable clinical candidate… The medicinal chemist therefore must modify the compound to reduce or eliminate these undesirable features without losing the desired biological activity. Replacement or modification of functional groups with other groups having similar properties is known as isosteric or bioisosteric replacement” (Page 59). Although it is clear that "the use of bioisosteric replacement (classical or nonclassical) in drug development is highly dependent upon the biological system being investigated” and that “[n]o hard and fast rules exist to determine what bioisosteric replacement is going to work with a given molecule” it is also clear that “some generalizations have been possible” (Page 60). Notably, one such generalization is that -O- and -NH- can replace each other (Page 59, Table 2.8).
Indeed, as similarly taught by Wipf, discussing bioisosteres wherein “substituents or groups which chemical or physical similarities that produce similar biological properties” to “attenuate toxicity, modify activity of lead, and/or alter pharmacokinetics of lead” (Page 43 of 64), the replacement of -O- for -NH-, including in rings to replace tetahydrofuran with pyrrolidine, is a classical isostere (Page 45 of 64).
Accordingly, based further on Williams et al and Wipf, it would have been prima facie obvious to a person of ordinary skill in the art at the time the invention was made to replace -O- in Compound 6 of the ‘531 application with -NH- (i.e., replace the tetrohydrofuran ring with a pyrrolidine ring) to arrive at the instantly claimed compound. The person of ordinary skill in the art at the time the invention was made would have been motivated to make the bioisosteric modifications in an effort to synthesize similar compounds that retain biological activity, but have improved physiochemical properties and better pharmacokinetic behavior, with a reasonable expectation of success.
Claim Rejections - 35 USC § 112
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.
Claims 1 and 57-58 are rejected under 35 U.S.C. 112(b) as being indefinite for failing to particularly point out and distinctly claim the subject matter which the inventor or a joint regards as the invention.
As amended, claim 1 is drawn to a compound of Formula (I’), having the following structure:
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wherein R1N is:
R1N is
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wherein R8j is selected from the group consisting of C1-C7 alkyl, C3-C7 cycloalkyl, C6-C10 aryl, and 5- to 10-membered heteroaryl (Page 2, Lines 3-4), which embraces the structures
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and
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, wherein R8j is C1 alkyl or C2 alkyl; or
R1N is
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or
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(Page 2, Line 12), which fall within the above structure
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.
A broad range or limitation together with a narrow range or limitation that falls within the broad range or limitation (in the same claim) may be considered indefinite if the resulting claim does not clearly set forth the metes and bounds of the patent protection desired. See MPEP § 2173.05(c).
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 §§ 706.02(l)(1) - 706.02(l)(3) 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 USPTO Internet website contains terminal disclaimer forms which may be used. Please visit www.uspto.gov/patent/patents-forms. The 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/process/file/efs/guidance/eTD-info-I.jsp.
Claims 1 and 54-58 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1, 3-4, 6-10, 41-42, 48-49 of copending Application No. 17/776,531 in view of Williams et al (Foye’s Principles of Medicinal Chemistry, 5th Edition, Pages 59-63, 2002; of record) and Wipf (Pharmacy Lecture Notes on Bioisosterism, Pages 43-49, 2/14/2008 - available online at https://www.yumpu.com/en/document/view/18242742/pharmacy-lecture-08-ccc as of 7/17/2013l; of record).
Although the claims at issue are not identical, they are not patentably distinct from each other. The ‘531 claims are drawn to compound of Formula (1*) (claim 1) and compositions thereof (claim 42), including, for example, the following compound species:
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(claim 41, Compound 6);
which differs from the instantly claimed compounds in comprising -O- in place of -NH- (i.e., comprising a tetrohydrofuran ring as opposed to a pyrrolidine ring), as indicated by arrow.
Yet, as taught by Williams et al “[w]hen a lead compound is first discovered for a particular disease state, it often lacks the required potency and pharmacokinetic properties suitable for making it a viable clinical candidate… The medicinal chemist therefore must modify the compound to reduce or eliminate these undesirable features without losing the desired biological activity. Replacement or modification of functional groups with other groups having similar properties is known as isosteric or bioisosteric replacement” (Page 59). Although it is clear that "the use of bioisosteric replacement (classical or nonclassical) in drug development is highly dependent upon the biological system being investigated” and that “[n]o hard and fast rules exist to determine what bioisosteric replacement is going to work with a given molecule” it is also clear that “some generalizations have been possible” (Page 60). Notably, one such generalization is that -O- and -NH- can replace each other (Page 59, Table 2.8).
Indeed, as similarly taught by Wipf, discussing bioisosteres wherein “substituents or groups which chemical or physical similarities that produce similar biological properties” to “attenuate toxicity, modify activity of lead, and/or alter pharmacokinetics of lead” (Page 43 of 64), the replacement of -O- for -NH-, including in rings to replace tetahydrofuran with pyrrolidine, is a classical isostere (Page 45 of 64).
Accordingly, based further on Williams et al and Wipf, it would have been prima facie obvious to a person of ordinary skill in the art at the time the invention was made to replace -O- in Compound 6 of the ‘531 application with -NH- (i.e., replace the tetrohydrofuran ring with a pyrrolidine ring) to arrive at the instantly claimed compound. The person of ordinary skill in the art at the time the invention was made would have been motivated to make the bioisosteric modifications in an effort to synthesize similar compounds that retain biological activity, but have improved physiochemical properties and better pharmacokinetic behavior, with a reasonable expectation of success.
This is a provisional nonstatutory double patenting rejection because the patentably indistinct claims have not in fact been patented.
Conclusion
The new ground(s) of rejection presented in this Office action are necessitated by Applicant’s amendments to the claims. Accordingly, THIS ACTION IS MADE FINAL. See MPEP § 706.07(a). Applicant is reminded of the extension of time policy as set forth in 37 CFR 1.136(a).
A shortened statutory period for reply to this final action is set to expire THREE MONTHS from the mailing date of this action. In the event a first reply is filed within TWO MONTHS of the mailing date of this final action and the advisory action is not mailed until after the end of the THREE-MONTH shortened statutory period, then the shortened statutory period will expire on the date the advisory action is mailed, and any extension fee pursuant to 37 CFR 1.136(a) will be calculated from the mailing date of the advisory action. In no event, however, will the statutory period for reply expire later than SIX MONTHS from the date of this final action.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to CRAIG D RICCI whose telephone number is (571) 270-5864. The examiner can normally be reached on Monday through Thursday, and every other Friday, 7:30 am - 5:00 pm ET.
If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Bethany Barham can be reached on (571) 272-6175. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/CRAIG D RICCI/Primary Examiner, Art Unit 1611