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 the Claims
Claims 1-18 are pending. Claims 2-5 and 11-14 are objected to. Claims 1, 6-10 and 15-18 are rejected.
Priority
This is a 35 U.S.C. 371 National Stage Filing of International Application No.
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, which claims priority under 35 U.S.C. 119(a-d) to
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. Receipt is acknowledged of papers submitted under 35 U.S.C. 119(a)-(d).
Information Disclosure Statement
The Information Disclosure Statement (IDS’s) submitted on 1/12/2024, 1/23/2025, and 9/3/2025 were considered by the Examiner.
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 8 and 18 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.
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). In the present instance, claims 8 and 18 recite the broad recitation “(1.1-1.3): 1”, and the claim also recites “preferably 1.2:1” which is the narrower statement of the range/limitation. The claim(s) are considered indefinite because there is a question or doubt as to whether the feature introduced by such narrower language is (a) merely exemplary of the remainder of the claim, and therefore not required, or (b) a required feature of the claims.
Regarding claims 8 and 18, the phrase "preferably" renders the claim indefinite because it is unclear whether the limitation(s) following the phrase are part of the claimed invention. See MPEP § 2173.05(d). Examiner recommends deleting this phrase.
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.
This application currently names joint inventors. In considering patentability of the claims the examiner presumes that the subject matter of the various claims was commonly owned as of the effective filing date of the claimed invention(s) absent any evidence to the contrary. Applicant is advised of the obligation under 37 CFR 1.56 to point out the inventor and effective filing dates of each claim that was not commonly owned as of the effective filing date of the later invention in order for the examiner to consider the applicability of 35 U.S.C. 102(b)(2)(C) for any potential 35 U.S.C. 102(a)(2) prior art against the later invention.
(1 of 5) Claim(s) 1, 6-10, and 15-18 is/are rejected under 35 U.S.C. 103 as being unpatentable over Hu et al. (WO2021143803), in view of Stahl et al. (Handbook of Pharmaceutical Salts, 2002, 1-374).
The applied reference has a common applicant with the instant application. Based upon the earlier effectively filed date of the reference, it constitutes prior art under 35 U.S.C. 102(a)(2). This rejection under 35 U.S.C. 102(a)(2) might be overcome by: (1) a showing under 37 CFR 1.130(a) that the subject matter disclosed in the reference was obtained directly or indirectly from the inventor or a joint inventor of this application and is thus not prior art in accordance with 35 U.S.C. 102(b)(2)(A); (2) a showing under 37 CFR 1.130(b) of a prior public disclosure under 35 U.S.C. 102(b)(2)(B) if the same invention is not being claimed; or (3) a statement pursuant to 35 U.S.C. 102(b)(2)(C) establishing that, not later than the effective filing date of the claimed invention, the subject matter disclosed in the reference and the claimed invention were either owned by the same person or subject to an obligation of assignment to the same person or subject to a joint research agreement.
Determining the scope and contents of the prior art. (See MPEP § 2141.01)
Hu discloses the following compound in claim 27, or a pharmaceutically acceptable salt thereof:
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, which may be in a form of a pharmaceutical composition with a pharmaceutically acceptable carrier (see claim 29). The prior art compound may be used to treat MOR related diseases, including pain (see claims 30 and 31). Hu fails to specifically disclose the compound H-7a as a maleate, L-tartrate or succinate salt.
Stahl et al. discloses tartrate as a common pharmaceutical salt former (See Table 1). Stahl again highlights tartrate salts on p. 255-256:
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, with the following procedure:
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. (“(+)-tartaric acid” is equivalent to L-tartaric acid). Regarding polymorphs and crystallization, Stahl teaches the following on p. 4, left column: “As with crystallization in general, also crystallization of salts is associated with the realm of polymorphism. Crystallizations in the pharmaceutical industry are mostly carried out batch-wise. The techniques used are cooling, evaporation, drowning-out, and reaction crystallization”.
Ascertainment of the differences between the prior art and the claims. (See MPEP § 2141.02)
There is not a single embodiment in the prior art of instant compound X:
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as an L-tartrate salt. Additional limitations will be addressed below.
Finding of prima facie obviousness --- rationale and motivation (See MPEP § 2142-2143)
Regarding instant claims 1, 15, 16, and 17, it would have been obvious to skilled artisan to arrive at a L-tartrate salt of instant compound X, particularly with the usefulness in treating MOR related diseases, such as pain, including that of a pharmaceutical composition. Compound X was previously taught to treat MOR diseases and L-tartrate salts are commonly and effectively utilized in the pharmaceutical industry. A PHOSITA would have had a reasonable expectation of success in arriving at an L-tartrate salt of instant compound X, as an effective MOR disease treatment. Additionally, regarding the different stereochemistry of the prior art compound and instant compound X, “An optically active isomer is unpatentable over a prior art racemate or optical isomer of opposite rotation in the absence of unexpected or unobvious beneficial properties”. In re Adamson et al. (CCPA) 1960 275 F2d 952, 125 USPQ 233. The instant disclosure does not disclose superiority of the specific stereochemistry of instant compound X specifically over the prior art form.
Regarding instant claims 6 and 8-9, it would have been obvious to a skilled artisan to arrive at the instantly claimed method of “mixing the compound of formula X, an acid, and a solvent and performing a salt-forming reaction…”. The sequence of claim 6 would have been a result of routine experimentation by a skilled artisan and the specifics of claims 8 and 9 would have been also obvious as a function of routine optimization of procedural details.
Regarding instant claims 7, 10, and 18, it would have been obvious to a skilled artisan to arrive at a polymorph as a result of a crystallization technique, such as cooling. Particularly, claim 18 would have been obvious as a result of routine optimization of procedural details, with a reasonable expectation of success.
(2 of 5) Claim(s) 1, 6-10, and 15-18 is/are rejected under 35 U.S.C. 103 as being unpatentable over Hu et al. (WO2021143801), in view of Stahl et al. (Handbook of Pharmaceutical Salts, 2002, 1-374).
The applied reference has a common applicant with the instant application. Based upon the earlier effectively filed date of the reference, it constitutes prior art under 35 U.S.C. 102(a)(2). This rejection under 35 U.S.C. 102(a)(2) might be overcome by: (1) a showing under 37 CFR 1.130(a) that the subject matter disclosed in the reference was obtained directly or indirectly from the inventor or a joint inventor of this application and is thus not prior art in accordance with 35 U.S.C. 102(b)(2)(A); (2) a showing under 37 CFR 1.130(b) of a prior public disclosure under 35 U.S.C. 102(b)(2)(B) if the same invention is not being claimed; or (3) a statement pursuant to 35 U.S.C. 102(b)(2)(C) establishing that, not later than the effective filing date of the claimed invention, the subject matter disclosed in the reference and the claimed invention were either owned by the same person or subject to an obligation of assignment to the same person or subject to a joint research agreement.
Determining the scope and contents of the prior art. (See MPEP § 2141.01)
Hu discloses the following compound in claim 27 or a pharmaceutically acceptable salt:
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, which may be in a form of a pharmaceutical composition with a pharmaceutically acceptable carrier (see claim 28). The prior art compound may be used to treat MOR related diseases, including pain (see claims 29 and 30). Hu fails to specifically disclose the compound as a maleate, L-tartrate or succinate salt.
Stahl et al. discloses tartrate as a common pharmaceutical salt former (See Table 1). Stahl again highlights tartrate salts on p. 255-256:
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, with the following procedure:
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. (“(+)-tartaric acid” is equivalent to L-tartaric acid). Regarding polymorphs and crystallization, Stahl teaches the following on p. 4, left column: “As with crystallization in general, also crystallization of salts is associated with the realm of polymorphism. Crystallizations in the pharmaceutical industry are mostly carried out batch-wise. The techniques used are cooling, evaporation, drowning-out, and reaction crystallization”.
Ascertainment of the differences between the prior art and the claims. (See MPEP § 2141.02)
There is not a single embodiment in the prior art of instant compound X:
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as an L-tartrate salt. Additional limitations will be addressed below.
Finding of prima facie obviousness --- rationale and motivation (See MPEP § 2142-2143)
Regarding instant claims 1, 15, 16, and 17, it would have been obvious to skilled artisan to arrive at a L-tartrate salt of instant compound X, particularly with the usefulness in treating MOR related diseases, such as pain, including that of a pharmaceutical composition. Compound X was previously taught to treat MOR diseases and L-tartrate salts are commonly and effectively utilized in the pharmaceutical industry. A PHOSITA would have had a reasonable expectation of success in arriving at an L-tartrate salt of instant compound X, as an effective MOR disease treatment. Additionally, regarding the different stereochemistry of the prior art compound and instant compound X, “An optically active isomer is unpatentable over a prior art racemate or optical isomer of opposite rotation in the absence of unexpected or unobvious beneficial properties”. In re Adamson et al. (CCPA) 1960 275 F2d 952, 125 USPQ 233. The instant disclosure does not disclose superiority of the specific stereochemistry of instant compound X specifically over the prior art form.
Regarding instant claims 6 and 8-9, it would have been obvious to a skilled artisan to arrive at the instantly claimed method of “mixing the compound of formula X, an acid, and a solvent and performing a salt-forming reaction…”. The sequence of claim 6 would have been a result of routine experimentation by a skilled artisan and the specifics of claims 8 and 9 would have been also obvious as a function of routine optimization of procedural details.
Regarding instant claims 7, 10, and 18, it would have been obvious to a skilled artisan to arrive at a polymorph as a result of a crystallization technique, such as cooling. Particularly, claim 18 would have been obvious as a result of routine optimization of procedural details, with a reasonable expectation of success.
(3 of 5) Claim(s) 1, 6-10, and 15-18 is/are rejected under 35 U.S.C. 103 as being unpatentable over Hu et al. (US20230128062), in view of Stahl et al. (Handbook of Pharmaceutical Salts, 2002, 1-374).
The applied reference has a common applicant with the instant application. Based upon the earlier effectively filed date of the reference, it constitutes prior art under 35 U.S.C. 102(a)(2). This rejection under 35 U.S.C. 102(a)(2) might be overcome by: (1) a showing under 37 CFR 1.130(a) that the subject matter disclosed in the reference was obtained directly or indirectly from the inventor or a joint inventor of this application and is thus not prior art in accordance with 35 U.S.C. 102(b)(2)(A); (2) a showing under 37 CFR 1.130(b) of a prior public disclosure under 35 U.S.C. 102(b)(2)(B) if the same invention is not being claimed; or (3) a statement pursuant to 35 U.S.C. 102(b)(2)(C) establishing that, not later than the effective filing date of the claimed invention, the subject matter disclosed in the reference and the claimed invention were either owned by the same person or subject to an obligation of assignment to the same person or subject to a joint research agreement.
Determining the scope and contents of the prior art. (See MPEP § 2141.01)
Hu discloses the following compound in claim 27 or a pharmaceutically acceptable salt:
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, which may be in a form of a pharmaceutical composition with a pharmaceutically acceptable carrier (see claim 28). The prior art compound may be used to treat MOR related diseases, including pain (see claims 29 and 30). Hu fails to specifically disclose the compound as a maleate, L-tartrate or succinate salt.
Stahl et al. discloses tartrate as a common pharmaceutical salt former (See Table 1). Stahl again highlights tartrate salts on p. 255-256:
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, with the following procedure:
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. (“(+)-tartaric acid” is equivalent to L-tartaric acid). Regarding polymorphs and crystallization, Stahl teaches the following on p. 4, left column: “As with crystallization in general, also crystallization of salts is associated with the realm of polymorphism. Crystallizations in the pharmaceutical industry are mostly carried out batch-wise. The techniques used are cooling, evaporation, drowning-out, and reaction crystallization”.
Ascertainment of the differences between the prior art and the claims. (See MPEP § 2141.02)
There is not a single embodiment in the prior art of instant compound X:
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as an L-tartrate salt. Additional limitations will be addressed below.
Finding of prima facie obviousness --- rationale and motivation (See MPEP § 2142-2143)
Regarding instant claims 1, 15, 16, and 17, it would have been obvious to skilled artisan to arrive at a L-tartrate salt of instant compound X, particularly with the usefulness in treating MOR related diseases, such as pain, including that of a pharmaceutical composition. Compound X was previously taught to treat MOR diseases and L-tartrate salts are commonly and effectively utilized in the pharmaceutical industry. A PHOSITA would have had a reasonable expectation of success in arriving at an L-tartrate salt of instant compound X, as an effective MOR disease treatment. Additionally, regarding the different stereochemistry of the prior art compound and instant compound X, “An optically active isomer is unpatentable over a prior art racemate or optical isomer of opposite rotation in the absence of unexpected or unobvious beneficial properties”. In re Adamson et al. (CCPA) 1960 275 F2d 952, 125 USPQ 233. The instant disclosure does not disclose superiority of the specific stereochemistry of instant compound X specifically over the prior art form.
Regarding instant claims 6 and 8-9, it would have been obvious to a skilled artisan to arrive at the instantly claimed method of “mixing the compound of formula X, an acid, and a solvent and performing a salt-forming reaction…”. The sequence of claim 6 would have been a result of routine experimentation by a skilled artisan and the specifics of claims 8 and 9 would have been also obvious as a function of routine optimization of procedural details.
Regarding instant claims 7, 10, and 18, it would have been obvious to a skilled artisan to arrive at a polymorph as a result of a crystallization technique, such as cooling. Particularly, claim 18 would have been obvious as a result of routine optimization of procedural details, with a reasonable expectation of success.
(4 of 5) Claim(s) 1, 6-10, and 15-18 is/are rejected under 35 U.S.C. 103 as being unpatentable over Hu et al. (US12540138), in view of Stahl et al. (Handbook of Pharmaceutical Salts, 2002, 1-374).
The applied reference has a common applicant with the instant application. Based upon the earlier effectively filed date of the reference, it constitutes prior art under 35 U.S.C. 102(a)(2). This rejection under 35 U.S.C. 102(a)(2) might be overcome by: (1) a showing under 37 CFR 1.130(a) that the subject matter disclosed in the reference was obtained directly or indirectly from the inventor or a joint inventor of this application and is thus not prior art in accordance with 35 U.S.C. 102(b)(2)(A); (2) a showing under 37 CFR 1.130(b) of a prior public disclosure under 35 U.S.C. 102(b)(2)(B) if the same invention is not being claimed; or (3) a statement pursuant to 35 U.S.C. 102(b)(2)(C) establishing that, not later than the effective filing date of the claimed invention, the subject matter disclosed in the reference and the claimed invention were either owned by the same person or subject to an obligation of assignment to the same person or subject to a joint research agreement.
Determining the scope and contents of the prior art. (See MPEP § 2141.01)
Hu teaches a compound or a pharmaceutically acceptable salt of the following genus:
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(see claim 1). In claim 6, which depends from claim 1, the following species is disclosed:
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(see column 77). Claim 8 recites a “pharmaceutical composition comprising a pharmaceutically acceptable carrier and the compound according to claim 6, or a pharmaceutically acceptable salt thereof”. Additionally, Hu claims the following regarding MOR receptors and pain:
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. Hu fails to specifically disclose the compound as a maleate, L-tartrate or succinate salt.
Stahl et al. discloses tartrate as a common pharmaceutical salt former (See Table 1). Stahl again highlights tartrate salts on p. 255-256:
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, with the following procedure:
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. (“(+)-tartaric acid” is equivalent to L-tartaric acid). Regarding polymorphs and crystallization, Stahl teaches the following on p. 4, left column: “As with crystallization in general, also crystallization of salts is associated with the realm of polymorphism. Crystallizations in the pharmaceutical industry are mostly carried out batch-wise. The techniques used are cooling, evaporation, drowning-out, and reaction crystallization”.
Ascertainment of the differences between the prior art and the claims. (See MPEP § 2141.02)
There is not a single embodiment in the prior art of instant compound X:
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as an L-tartrate salt. Additional limitations will be addressed below.
Finding of prima facie obviousness --- rationale and motivation (See MPEP § 2142-2143)
Regarding instant claims 1, 15, 16, and 17, it would have been obvious to skilled artisan to arrive at a L-tartrate salt of instant compound X, particularly with the usefulness in treating MOR related diseases, such as pain, including that of a pharmaceutical composition. Compound X was previously taught to treat MOR diseases and L-tartrate salts are commonly and effectively utilized in the pharmaceutical industry. A PHOSITA would have had a reasonable expectation of success in arriving at an L-tartrate salt of instant compound X, as an effective MOR disease treatment. Additionally, regarding the different stereochemistry of the prior art compound and instant compound X, “An optically active isomer is unpatentable over a prior art racemate or optical isomer of opposite rotation in the absence of unexpected or unobvious beneficial properties”. In re Adamson et al. (CCPA) 1960 275 F2d 952, 125 USPQ 233. The instant disclosure does not disclose superiority of the specific stereochemistry of instant compound X specifically over the prior art form.
Regarding instant claims 6 and 8-9, it would have been obvious to a skilled artisan to arrive at the instantly claimed method of “mixing the compound of formula X, an acid, and a solvent and performing a salt-forming reaction…”. The sequence of claim 6 would have been a result of routine experimentation by a skilled artisan and the specifics of claims 8 and 9 would have been also obvious as a function of routine optimization of procedural details.
Regarding instant claims 7, 10, and 18, it would have been obvious to a skilled artisan to arrive at a polymorph as a result of a crystallization technique, such as cooling. Particularly, claim 18 would have been obvious as a result of routine optimization of procedural details, with a reasonable expectation of success.
(5 of 5) Claim(s) 1, 6-10, and 15-18 is/are rejected under 35 U.S.C. 103 as being unpatentable over Hu et al. (US12545680), in view of Stahl et al. (Handbook of Pharmaceutical Salts, 2002, 1-374).
The applied reference has a common applicant with the instant application. Based upon the earlier effectively filed date of the reference, it constitutes prior art under 35 U.S.C. 102(a)(2). This rejection under 35 U.S.C. 102(a)(2) might be overcome by: (1) a showing under 37 CFR 1.130(a) that the subject matter disclosed in the reference was obtained directly or indirectly from the inventor or a joint inventor of this application and is thus not prior art in accordance with 35 U.S.C. 102(b)(2)(A); (2) a showing under 37 CFR 1.130(b) of a prior public disclosure under 35 U.S.C. 102(b)(2)(B) if the same invention is not being claimed; or (3) a statement pursuant to 35 U.S.C. 102(b)(2)(C) establishing that, not later than the effective filing date of the claimed invention, the subject matter disclosed in the reference and the claimed invention were either owned by the same person or subject to an obligation of assignment to the same person or subject to a joint research agreement.
Determining the scope and contents of the prior art. (See MPEP § 2141.01)
Hu teaches a compound or a pharmaceutically acceptable salt of the following genus:
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(see claim 1). In claim 12, which depends from claim 1, the following species is disclosed:
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(see column 107). Claim 13 of the patent teaches pharmaceutical compositions with pharmaceutically acceptable carriers. Additionally, the patent claims the following regarding MOR receptors and pain:
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. Hu fails to specifically disclose the compound as a maleate, L-tartrate or succinate salt.
Stahl et al. discloses tartrate as a common pharmaceutical salt former (See Table 1). Stahl again highlights tartrate salts on p. 255-256:
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, with the following procedure:
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. (“(+)-tartaric acid” is equivalent to L-tartaric acid). Regarding polymorphs and crystallization, Stahl teaches the following on p. 4, left column: “As with crystallization in general, also crystallization of salts is associated with the realm of polymorphism. Crystallizations in the pharmaceutical industry are mostly carried out batch-wise. The techniques used are cooling, evaporation, drowning-out, and reaction crystallization”.
Ascertainment of the differences between the prior art and the claims. (See MPEP § 2141.02)
There is not a single embodiment in the prior art of instant compound X:
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as an L-tartrate salt. Additional limitations will be addressed below.
Finding of prima facie obviousness --- rationale and motivation (See MPEP § 2142-2143)
Regarding instant claims 1, 15, 16, and 17, it would have been obvious to skilled artisan to arrive at a L-tartrate salt of instant compound X, particularly with the usefulness in treating MOR related diseases, such as pain, including that of a pharmaceutical composition. Compound X was previously taught to treat MOR diseases and L-tartrate salts are commonly and effectively utilized in the pharmaceutical industry. A PHOSITA would have had a reasonable expectation of success in arriving at an L-tartrate salt of instant compound X, as an effective MOR disease treatment. Additionally, regarding the different stereochemistry of the prior art compound and instant compound X, “An optically active isomer is unpatentable over a prior art racemate or optical isomer of opposite rotation in the absence of unexpected or unobvious beneficial properties”. In re Adamson et al. (CCPA) 1960 275 F2d 952, 125 USPQ 233. The instant disclosure does not disclose superiority of the specific stereochemistry of instant compound X specifically over the prior art form.
Regarding instant claims 6 and 8-9, it would have been obvious to a skilled artisan to arrive at the instantly claimed method of “mixing the compound of formula X, an acid, and a solvent and performing a salt-forming reaction…”. The sequence of claim 6 would have been a result of routine experimentation by a skilled artisan and the specifics of claims 8 and 9 would have been also obvious as a function of routine optimization of procedural details.
Regarding instant claims 7, 10, and 18, it would have been obvious to a skilled artisan to arrive at a polymorph as a result of a crystallization technique, such as cooling. Particularly, claim 18 would have been obvious as a result of routine optimization of procedural details, with a reasonable expectation of success.
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.
(1 of 2) Claims 1, 6-10, and 15-18 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-17 of U.S. Patent No. 12545680 in view of Stahl et al. (Handbook of Pharmaceutical Salts, 2002, 1-374).
U.S. Patent No. 12545680 teaches a compound or a pharmaceutically acceptable salt of the following genus:
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(see claim 1). In claim 12, which depends from claim 1, the following species is disclosed:
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(see column 107). Claim 13 of the patent teaches pharmaceutical compositions with pharmaceutically acceptable carriers. Additionally, the patent claims the following regarding MOR receptors and pain:
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. The patent fails to specifically disclose the compound as a maleate, L-tartrate or succinate salt.
Stahl et al. discloses tartrate as a common pharmaceutical salt former (See Table 1). Stahl again highlights tartrate salts on p. 255-256:
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, with the following procedure:
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. (“(+)-tartaric acid” is equivalent to L-tartaric acid). Regarding polymorphs and crystallization, Stahl teaches the following on p. 4, left column: “As with crystallization in general, also crystallization of salts is associated with the realm of polymorphism. Crystallizations in the pharmaceutical industry are mostly carried out batch-wise. The techniques used are cooling, evaporation, drowning-out, and reaction crystallization”.
Regarding instant claims 1, 15, 16, and 17, it would have been obvious to skilled artisan to arrive at a L-tartrate salt of instant compound X, particularly with the usefulness in treating MOR related diseases, such as pain, including that of a pharmaceutical composition. Compound X was previously taught to activate or antagonize a MOR receptor in a patient and L-tartrate salts are commonly and effectively utilized in the pharmaceutical industry. A PHOSITA would have had a reasonable expectation of success in arriving at an L-tartrate salt of instant compound X, as an effective MOR related disease treatment. Additionally, regarding the different stereochemistry of the prior art compound and instant compound X, “An optically active isomer is unpatentable over a prior art racemate or optical isomer of opposite rotation in the absence of unexpected or unobvious beneficial properties”. In re Adamson et al. (CCPA) 1960 275 F2d 952, 125 USPQ 233. The instant disclosure does not disclose superiority of the specific stereochemistry of instant compound X specifically over the prior art form.
Regarding instant claims 6 and 8-9, it would have been obvious to a skilled artisan to arrive at the instantly claimed method of “mixing the compound of formula X, an acid, and a solvent and performing a salt-forming reaction…”. The sequence of claim 6 would have been a result of routine experimentation by a skilled artisan and the specifics of claims 8 and 9 would have been also obvious as a function of routine optimization of procedural details.
Regarding instant claims 7, 10, and 18, it would have been obvious to a skilled artisan to arrive at a polymorph as a result of a crystallization technique, such as cooling. Particularly, claim 18 would have been obvious as a result of routine optimization of procedural details, with a reasonable expectation of success.
(2 of 2) Claims 1, 6-10, and 15-18 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-12 of U.S. Patent No. 12540138 in view of Stahl et al. (Handbook of Pharmaceutical Salts, 2002, 1-374).
U.S. Patent No. 12540138 teaches a compound or a pharmaceutically acceptable salt of the following genus:
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(see claim 1). In claim 6, which depends from claim 1, the following species is disclosed:
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(see column 77). Claim 8 recites a “pharmaceutical composition comprising a pharmaceutically acceptable carrier and the compound according to claim 6, or a pharmaceutically acceptable salt thereof”. Additionally, the patent claims the following regarding MOR receptors and pain:
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. The patent fails to specifically disclose the compound as a maleate, L-tartrate or succinate salt.
Stahl et al. discloses tartrate as a common pharmaceutical salt former (See Table 1). Stahl again highlights tartrate salts on p. 255-256:
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, with the following procedure:
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. (“(+)-tartaric acid” is equivalent to L-tartaric acid). Regarding polymorphs and crystallization, Stahl teaches the following on p. 4, left column: “As with crystallization in general, also crystallization of salts is associated with the realm of polymorphism. Crystallizations in the pharmaceutical industry are mostly carried out batch-wise. The techniques used are cooling, evaporation, drowning-out, and reaction crystallization”.
Regarding instant claims 1, 15, 16, and 17, it would have been obvious to skilled artisan to arrive at a L-tartrate salt of instant compound X, particularly with the usefulness in treating MOR related diseases, such as pain, including that of a pharmaceutical composition. Compound X was previously taught to activate or antagonize a MOR receptor in a patient and L-tartrate salts are commonly and effectively utilized in the pharmaceutical industry. A PHOSITA would have had a reasonable expectation of success in arriving at an L-tartrate salt of instant compound X, as an effective MOR related disease treatment. Additionally, regarding the different stereochemistry of the prior art compound and instant compound X, “An optically active isomer is unpatentable over a prior art racemate or optical isomer of opposite rotation in the absence of unexpected or unobvious beneficial properties”. In re Adamson et al. (CCPA) 1960 275 F2d 952, 125 USPQ 233. The instant disclosure does not disclose superiority of the specific stereochemistry of instant compound X specifically over the prior art form.
Regarding instant claims 6 and 8-9, it would have been obvious to a skilled artisan to arrive at the instantly claimed method of “mixing the compound of formula X, an acid, and a solvent and performing a salt-forming reaction…”. The sequence of claim 6 would have been a result of routine experimentation by a skilled artisan and the specifics of claims 8 and 9 would have been also obvious as a function of routine optimization of procedural details.
Regarding instant claims 7, 10, and 18, it would have been obvious to a skilled artisan to arrive at a polymorph as a result of a crystallization technique, such as cooling. Particularly, claim 18 would have been obvious as a result of routine optimization of procedural details, with a reasonable expectation of success.
Allowable Subject Matter
Claims 2-5 and 11-14 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
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/MEGHAN C HEASLEY/Examiner, Art Unit 1626