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 .
Status of Claims
Claims 1-8 and 11-21 are pending.
Priority
Instant application 18/720,635, filed 06/15/2024 claims priority as follows:
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Receipt is acknowledged of certified copies of papers required by 37 CFR 1.55.
Information Disclosure Statement
All references from IDS(s) received 06/15/2024, 11/28/2024, 03/31/2025, and 04/03/2026 have been considered unless marked with a strikethrough.
Claim Interpretation
Claim 5 recites the phrase “an X-ray powder diffraction pattern basically as shown in Fig.
7”. The phrase “basically as shown in the figure” is defined in the specification on page 23, [0133]:
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The above definition is being applied to the interpretation of “basically as shown in Fig. 7” in claim 5 to mean that any crystal form satisfying both of (1) the criteria in claim 4 and (2) one of the alternative criteria set forth in the definition (i.e., having at least 50%, or at least 60%, or…at least 99% of the peaks shown in FIG. 7) reads on the claim.
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.
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.
Claims 6 and 19 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.
Claims 6 and 19 recite that “the content of the solvent ranges from 0.1% to 6.0%” and
“the content of water ranges from 0.1% to 4.0%”. However, the claims fail to state the basis of the percentage (w/w, w/v, mol%, etc.). A person having ordinary skill could not readily discern which basis applies (e.g. is the percentage required on a weight basis or a weight/volume basis?). Because multiple reasonable interpretations apply and each interpretation results in different claim scope, claims 6 and 19 are indefinite.
Please note: in the interest of compact prosecution, the examiner recommends amending the claims to recite the percentage basis (e.g., “% w/w”) in order to clarify the claim language and overcome the rejection.
Claims 11, 13, 15, and 17 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.
Claims 11, 13, 15, and 17 recite “a method for treating an S1P1 receptor-related disease
in a subject in need thereof”. The phrase “subject in need thereof” is being interpreted as a subject in need of treatment of the S1P1 receptor-related disease. However, the metes and bounds of the claims are unclear due to the phrase “S1P1 receptor-related disease”.
“S1P1 receptor-related” defines the disease by a relationship rather than identity; therefore the limitation is being interpreted as a functional limitation. See MPEP 2173.05(g) in this regard: Functional language is indefinite where it fails “to provide a clear-cut indication of the scope of the subject matter embraced by the claim”.
The phrase “S1P1 receptor-related” is not meaningfully defined in the claims or the specification, and has no single art-recognized meaning. The undefined term “-related” fails to establish the nature or degree of the required connection between S1P1 and the disease. Nothing tells the reader whether S1P1 must cause the disease, merely be expressed in the affected tissue, contribute to pathogenesis, or just render the disease responsive to modulation. Multiple reasonable interpretations therefore apply and each results in meaningfully different claim scope.
Therefore, claims 11, 13, 15, and 17 are indefinite.
Please note: in the interest of compact prosecution, the examiner recommends amending the claims to recite the disease list of dependent claims 12, 14, 16, and 18 in order to clarify the claim language and overcome the rejection.
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 1-2, 15-18, and 20-21 are rejected under 35 U.S.C. 103 as being unpatentable over LU (WO2020114475A1; published 2020; cited in IDS). Citations refer to the US counterpart publication (US 20220017513 A1; cited in IDS), which is being relied upon as an English translation of LU.
Lu discloses the compound of formula (I) recited in instant claim 1 (LU, page 4, [0050]; page 65, compound 16):
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Lu does not explicitly disclose a discrete embodiment where the calcium salt of compound 16 was prepared.
However, Lu discloses pharmaceutically acceptable salts of compounds therein, including compound 16 (page 4, [0050]); and notes that pharmaceutically acceptable salts includes “a base addition salt…obtained by contacting the neutral form of the compound with a sufficient amount of base in a pure solution or a suitable inert solvent. The pharmaceutically acceptable base addition salt includes a salt of sodium, potassium, calcium, ammonium, organic amine or magnesium or similar salts.”
Therefore, Lu teaches calcium salts of the compounds disclosed therein.
Finding of prima facie obviousness
The Supreme Court in KSR Int'l Co. v. Teleflex Inc., 550 U.S. 398, 415-421, 82 USPQ2d 1385, 1395-97 (2007) identified a number of rationales to support a conclusion of obviousness which are consistent with the proper "functional approach" to the determination of obviousness as laid down in Graham. See MPEP 2143.
Examples of rationales that may support a conclusion of obviousness include:
(A) Combining prior art elements according to known methods to yield predictable results;
(B) Simple substitution of one known element for another to obtain predictable results;
(C) Use of known technique to improve similar devices (methods, or products) in the same way;
(D) Applying a known technique to a known device (method, or product) ready for improvement to yield predictable results;
(E) "Obvious to try" – choosing from a finite number of identified, predictable solutions, with a reasonable expectation of success;
(F) Known work in one field of endeavor may prompt variations of it for use in either the same field or a different one based on design incentives or other market forces if the variations are predictable to one of ordinary skill in the art;
(G) Some teaching, suggestion, or motivation in the prior art that would have led one of ordinary skill to modify the prior art reference or to combine prior art reference teachings to arrive at the claimed invention.
The skill level in the art of pharmaceutical salt formation is relatively high. Applying KSR example rationale (A) and/or (G), it would have been prima facie obvious to prepare the calcium salt of Lu’s compound 16 in view of Lu’s teaching of pharmaceutically acceptable salts. The motivation is derived explicitly from Lu, but also from general knowledge in the art about the common use of salts such as calcium, and the “normal desire of scientists or artisans to improve upon what is already generally known”. See In re Peterson, 315 F.3d 1325, 1330 (Fed. Cir. 2003). See also Pfizer, Inc. v. Apotex, Inc. 82 USPQ2d 1321. The Lu reference provides a reasonable expectation of success that a calcium salt of compound 16 would have similar properties to the neutral compound.
Claims 1-2 are therefore obvious over Lu.
With respect to claims 15-18, Lu teaches a method for preventing and/or treating diseases related to S1P1-receptor related diseases including ulcerative colitis, Crohn’s disease, multiple sclerosis, etc. (see e.g. Lu’s [0052]-[0053] or claims 21-24). Therefore, it would have been obvious to apply the calcium salt of compound 16 taught by Lu in the method of treatment taught by Lu. Accordingly, claims 15-18 are obvious over Lu.
With respect to claims 20-21, Lu teaches pharmaceutical compositions comprising the pharmaceutically acceptable salt and one or more pharmaceutically acceptable carriers, diluents, or excipients (see e.g. Lu’s [0050] or claim 20). Therefore, it would have been obvious to prepare a pharmaceutical composition comprising the calcium salt of compound 16 taught by Lu. Accordingly, claims 20-21 are obvious over Lu.
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.
Claims 1-2, 15-18, and 20-21 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-16 of U.S. Patent No. 12,195,457 (“the reference patent”).
The reference patent is the issued patent of US 20220017513 A1 relied upon as an English translation of LU cited in the rejection above.
The reference patent recites the compound of formula (I) recited by instant claim 1 (see claim 10 of the reference patent):
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The reference patent does not explicitly recite a calcium salt of compound 16.
However, the reference patent recites the above compound “or a pharmaceutically acceptable salt thereof” (claim 10 of the reference patent). Reading the claims of the reference patent in light of the specification, the phrase “pharmaceutically acceptable salt thereof” is supported by col. 15, lines 45-56, noting that pharmaceutically acceptable salts include “a base addition salt…obtained by contacting the neutral form of the compound with a sufficient amount of base in a pure solution or a suitable inert solvent. The pharmaceutically acceptable base addition salt includes a salt of sodium, potassium, calcium, ammonium, organic amine or magnesium or similar salts.”
Therefore, the reference patent provides support for calcium salts of the compounds recited in its claims, including claim 10.
Finding of prima facie obviousness
The Supreme Court in KSR Int'l Co. v. Teleflex Inc., 550 U.S. 398, 415-421, 82 USPQ2d 1385, 1395-97 (2007) identified a number of rationales to support a conclusion of obviousness which are consistent with the proper "functional approach" to the determination of obviousness as laid down in Graham. See MPEP 2143.
Examples of rationales that may support a conclusion of obviousness include:
(A) Combining prior art elements according to known methods to yield predictable results;
(B) Simple substitution of one known element for another to obtain predictable results;
(C) Use of known technique to improve similar devices (methods, or products) in the same way;
(D) Applying a known technique to a known device (method, or product) ready for improvement to yield predictable results;
(E) "Obvious to try" – choosing from a finite number of identified, predictable solutions, with a reasonable expectation of success;
(F) Known work in one field of endeavor may prompt variations of it for use in either the same field or a different one based on design incentives or other market forces if the variations are predictable to one of ordinary skill in the art;
(G) Some teaching, suggestion, or motivation in the prior art that would have led one of ordinary skill to modify the prior art reference or to combine prior art reference teachings to arrive at the claimed invention.
The skill level in the art of pharmaceutical salt formation is relatively high. Applying KSR example rationale (A) and/or (G), it would have been prima facie obvious to prepare the calcium salt of the reference patent’s compound 16 in view of the reference patent’s support for calcium salts as “pharmaceutically acceptable salts”. The motivation is derived explicitly from the reference patent, but also from general knowledge in the art about the common use of salts such as calcium, and the “normal desire of scientists or artisans to improve upon what is already generally known”. See In re Peterson, 315 F.3d 1325, 1330 (Fed. Cir. 2003). See also Pfizer, Inc. v. Apotex, Inc. 82 USPQ2d 1321. The reference patent provides a reasonable expectation of success that a calcium salt of compound 16 would have similar properties to the neutral compound.
Claims 1-2 are therefore obvious over the reference patent.
With respect to claims 15-18, the reference patent recites a method for preventing and/or treating diseases related to S1P1-receptor related diseases including ulcerative colitis, Crohn’s disease, multiple sclerosis, etc. (see claims 12-15). Therefore, it would have been obvious to apply the calcium salt of compound 16 taught by the reference patent in the method of treatment recited by the reference patent. Accordingly, claims 15-18 are obvious over the reference patent.
With respect to claims 20-21, the reference patent recites pharmaceutical compositions comprising the pharmaceutically acceptable salt and one or more pharmaceutically acceptable carriers, diluents, or excipients (see claim 11). Therefore, it would have been obvious to prepare a pharmaceutical composition comprising the calcium salt of compound 16 taught by the reference patent. Accordingly, claims 20-21 are obvious over the reference patent.
This rejection is proper according to MPEP 804(II)(B)(1):
Further, those portions of the specification which provide support for the reference claims may also be examined and considered when addressing the issue of whether a claim in the application defines an obvious variation of an invention claimed in the reference patent or application (as distinguished from an obvious variation of the subject matter disclosed in the reference patent or application). In re Vogel, 422 F.2d 438, 441-42, 164 USPQ 619, 622 (CCPA 1970)…The court pointed out that "this use of the disclosure is not in contravention of the cases forbidding its use as prior art, nor is it applying the patent as a reference under 35 U.S.C. 103, since only the disclosure of the invention claimed in the patent may be examined." In AbbVie Inc. v. Kennedy Institute of Rheumatology Trust, 764 F.3d 1366, 112 USPQ2d 1001 (Fed. Cir. 2014), the court explained that it is also proper to look at the disclosed utility in the reference disclosure to determine the overall question of obviousness in a nonstatutory double patenting context. See Sun Pharm. Indus., Ltd. v. Eli Lilly & Co., 611 F.3d 1381, 95 USPQ2d 1797 (Fed. Cir. 2010); Pfizer, Inc. v. Teva Pharm. USA, Inc., 518 F.3d 1353, 86 USPQ2d 1001 (Fed. Cir. 2008); Geneva Pharmaceuticals Inc. v. GlaxoSmithKline PLC, 349 F3d 1373, 1385-86, 68 USPQ2d 1865, 1875 (Fed. Cir. 2003)…In particular, when ascertaining the scope of the reference’s claim(s) to a compound, the examiner should consider the reference’s specification, including all of the compound’s uses that are disclosed. See Sun Pharm. Indus., 611 F.3d at 1386-88, 95 USPQ2d at 1801-02.
Allowable Subject Matter
Claims 3-5, 7-8, 12, and 14 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.
Conclusion
Claims 1-2, 6, 11, 13, and 15-21 are rejected. Claims 3-5, 7-8, 12, and 14 are objected to.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to Kyle Nottingham whose telephone number is (571)270-0640. The examiner can normally be reached M-F from 10:00 am - 6:00 pm.
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If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Clinton Brooks can be reached at (571) 270-7682. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/K.N./Examiner, Art Unit 1621
/CLINTON A BROOKS/Supervisory Patent Examiner, Art Unit 1621
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