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 1-138 were originally filed June 1, 2022.
The amendment received July 7, 2022 canceled claims 1-138 and added new claims 139-159.
Claims 139-159 are currently pending.
Claims 139-146 and 148-158 are currently under consideration.
Election/Restrictions
Applicant’s election of Group I (claims 139-158) in the reply filed on July 29, 2025 is acknowledged. Because applicant did not distinctly and specifically point out the supposed errors in the restriction requirement, the election has been treated as an election without traverse (MPEP § 818.01(a)). Please note: applicants stated that the election was made with traverse, but no traversal was provided.
Claim 159 is withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a nonelected method, there being no allowable generic or linking claim. Election was made without traverse in the reply filed on July 29, 2025.
Applicant’s election of SEQ ID NO: 10, docetaxel, and 2 (at about 1% (w/w)), acetyl, succinic acid linker, dextrose at about 5% (w/v), formic acid at about 0.04% (v/v), polysorbate 80 at about 10% (w/v), pH of 4.1-4.5, and formate salt as the species in the reply filed on July 29, 2025 is acknowledged. Because applicant did not distinctly and specifically point out the supposed errors in the restriction requirement, the election has been treated as an election without traverse (MPEP § 818.01(a)).
Claim 147 is withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a nonelected species, there being no allowable generic or linking claim. Election was made without traverse in the reply filed on July 29, 2025.
Potential Rejoinder
Applicant elected claims directed to a product. If a product claim is subsequently found allowable, withdrawn process claims that depend from or otherwise include all the limitations of the allowable product claim will be rejoined in accordance with the provisions of MPEP § 821.04. Process claims that depend from or otherwise include all the limitations of the patentable product will be entered as a matter of right if the amendment is presented prior to final rejection or allowance, whichever is earlier. Amendments submitted after final rejection are governed by 37 CFR 1.116; amendments submitted after allowance are governed by 37 CFR 1.312.
In the event of rejoinder, the requirement for restriction between the product claims and the rejoined process claims will be withdrawn, and the rejoined process claims will be fully examined for patentability in accordance with 37 CFR 1.104. Thus, to be allowable, the rejoined claims must meet all the criteria for patentability including the requirements of 35 U.S.C. 101, 102, 103, and 112. Until an elected product claim is found allowable, an otherwise proper restriction requirement between product claims and process claims may be maintained. Withdrawn process claims that are not commensurate in scope with an allowed product claim will not be rejoined. See “Guidance on Treatment of Product and Process Claims in light of In re Ochiai, In re Brouwer and 35 U.S.C. § 103(b),” 1184 O.G. 86 (March 26, 1996). Additionally, in order to retain the right to rejoinder in accordance with the above policy, applicant is advised that the process claims should be amended during prosecution either to maintain dependency on the product claims or to otherwise include the limitations of the product claims. Failure to do so may result in a loss of the right to a rejoinder. Further, note that the prohibition against double patenting rejections of 35 U.S.C. 121 does not apply where the restriction requirement is withdrawn by the examiner before the patent issues. See MPEP § 804.01.
Priority
The present application is a 371 (National Stage) of PCT/CA2020/051686 filed December 7, 2020 which claims the benefit of 62/945,111 filed December 6, 2019.
Information Disclosure Statement
The information disclosure statements (IDS) submitted on December 14, 2022 and April 28, 2025 are being considered by the examiner (see notes on the IDSs).
Nucleotide and/or Amino Acid Sequence Disclosures
REQUIREMENTS FOR PATENT APPLICATIONS CONTAINING NUCLEOTIDE AND/OR AMINO ACID SEQUENCE DISCLOSURES
Items 1) and 2) provide general guidance related to requirements for sequence disclosures.
37 CFR 1.821(c) requires that patent applications which contain disclosures of nucleotide and/or amino acid sequences that fall within the definitions of 37 CFR 1.821(a) must contain a "Sequence Listing," as a separate part of the disclosure, which presents the nucleotide and/or amino acid sequences and associated information using the symbols and format in accordance with the requirements of 37 CFR 1.821 - 1.825. This "Sequence Listing" part of the disclosure may be submitted:
In accordance with 37 CFR 1.821(c)(1) via the USPTO patent electronic filing system (see Section I.1 of the Legal Framework for Patent Electronic System (https://www.uspto.gov/PatentLegalFramework), hereinafter "Legal Framework") as an ASCII text file, together with an incorporation-by-reference of the material in the ASCII text file in a separate paragraph of the specification as required by 37 CFR 1.823(b)(1) identifying:
the name of the ASCII text file;
ii) the date of creation; and
iii) the size of the ASCII text file in bytes;
In accordance with 37 CFR 1.821(c)(1) on read-only optical disc(s) as permitted by 37 CFR 1.52(e)(1)(ii), labeled according to 37 CFR 1.52(e)(5), with an incorporation-by-reference of the material in the ASCII text file according to 37 CFR 1.52(e)(8) and 37 CFR 1.823(b)(1) in a separate paragraph of the specification identifying:
the name of the ASCII text file;
the date of creation; and
the size of the ASCII text file in bytes;
In accordance with 37 CFR 1.821(c)(2) via the USPTO patent electronic filing system as a PDF file (not recommended); or
In accordance with 37 CFR 1.821(c)(3) on physical sheets of paper (not recommended).
When a “Sequence Listing” has been submitted as a PDF file as in 1(c) above (37 CFR 1.821(c)(2)) or on physical sheets of paper as in 1(d) above (37 CFR 1.821(c)(3)), 37 CFR 1.821(e)(1) requires a computer readable form (CRF) of the “Sequence Listing” in accordance with the requirements of 37 CFR 1.824.
If the "Sequence Listing" required by 37 CFR 1.821(c) is filed via the USPTO patent electronic filing system as a PDF, then 37 CFR 1.821(e)(1)(ii) or 1.821(e)(2)(ii) requires submission of a statement that the "Sequence Listing" content of the PDF copy and the CRF copy (the ASCII text file copy) are identical.
If the "Sequence Listing" required by 37 CFR 1.821(c) is filed on paper or read-only optical disc, then 37 CFR 1.821(e)(1)(ii) or 1.821(e)(2)(ii) requires submission of a statement that the "Sequence Listing" content of the paper or read-only optical disc copy and the CRF are identical.
Specific deficiencies and the required response to this Office Action are as follows:
Specific deficiency – Nucleotide and/or amino acid sequences appearing in the specification are not identified by sequence identifiers in accordance with 37 CFR 1.821(d).
See paragraphs 95 and 111. See claim 147.
Required response – Applicant must provide:
A substitute specification in compliance with 37 CFR 1.52, 1.121(b)(3) and 1.125 inserting the required sequence identifiers, consisting of:
A copy of the previously-submitted specification, with deletions shown with strikethrough or brackets and insertions shown with underlining (marked-up version);
A copy of the amended specification without markings (clean version); and
A statement that the substitute specification contains no new matter.
Claim Objections
Claim 143 is objected to because of the following informalities: the recitation of “Formula (XXXIX)” and “(XXXIX)” is unnecessary as the formula name does not provide any additional information. Appropriate correction is required.
Sequence Interpretation
The Office interprets claims comprising SEQ ID NOs: in the following manner: “comprising a sequence of SEQ ID NO: 1” requires only a 2mer of SEQ ID NO: 1, “comprising the sequence of SEQ ID NO: 1” requires the full-length sequence with 100% identity to SEQ ID NO: 1 with any N-/C-terminal additions or any 5’/3’ additions, “consisting of SEQ ID NO: 1” requires the full-length sequence with 100% identity to SEQ ID NO: 1 and the same length as SEQ ID NO: 1, and “selected from the group consisting of SEQ ID NOs: 1, 2, and 3” requires the full-length sequence with 100% identity to SEQ ID NOs: 1, 2, or 3 and the same length as SEQ ID NOs: 1, 2, or 3. Any claim requiring a specific percent identity, necessarily requires at least the recited percent identity.
Claim Rejections - 35 USC § 112
The following is a quotation of the first paragraph of 35 U.S.C. 112(a):
(a) IN GENERAL.—The specification shall contain a written description of the invention, and of the manner and process of making and using it, in such full, clear, concise, and exact terms as to enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the same, and shall set forth the best mode contemplated by the inventor or joint inventor of carrying out the invention.
The following is a quotation of the first paragraph of pre-AIA 35 U.S.C. 112:
The specification shall contain a written description of the invention, and of the manner and process of making and using it, in such full, clear, concise, and exact terms as to enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the same, and shall set forth the best mode contemplated by the inventor of carrying out his invention.
Claim 142 is rejected under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, as failing to comply with the written description requirement. The claim(s) contains subject matter which was not described in the specification in such a way as to reasonably convey to one skilled in the relevant art that the inventor or a joint inventor, or for applications subject to pre-AIA 35 U.S.C. 112, the inventor(s), at the time the application was filed, had possession of the claimed invention. This is a new matter rejection. A succinyl protecting group is only associated with SEQ ID NO: 6 in the originally filed specification. A succinyl protecting group for SEQ ID NO: 10 is not taught in the originally filed specification.
Claim 158 is rejected under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, as failing to comply with the written description requirement. The claim(s) contains subject matter which was not described in the specification in such a way as to reasonably convey to one skilled in the relevant art that the inventor or a joint inventor, or for applications subject to pre-AIA 35 U.S.C. 112, the inventor(s), at the time the application was filed, had possession of the claimed invention. This is a new matter rejection. A pharmaceutically acceptable acid addition salt which is acetate or formate is not taught in the originally filed specification.
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.
Claims 139-146, 148-150, 154, 155, 157, and 158 are rejected under 35 U.S.C. 103 as being unpatentable over Beliveau et al. WO 2017/088058 published June 1, 2017 and Kaur et al., 2017, Developments of Polysorbate (Tween) based microemulsions: Preclinical drug delivery, toxicity and antimicrobial applications, international Journal of Pharmaceutics, 529: 134-160.
For present claims 139-146, 148-150, 154, 157, and 158, Beliveau et al. teach a conjugate of A-(B)n wherein A is SEQ ID NO: 10 (i.e. same length and 100% identity to present SEQ ID NO: 10) conjugated to B which are cancer therapeutics including docetaxel, doxorubicin, cabazitaxel, auristatin, or amanitin wherein conjugation can be via lysines or via a linker including succinic acid, and n can be 1-4 wherein A can be protected via an N-terminal acetyl (i.e. see SEQ ID NO: 15 which has the same length and 100% identity with present SEQ ID NO: 15) and pharmaceutically acceptable acid addition salts including fumaric (i.e. formate) and buffers including formic acid (please refer to the entire specification particularly the abstract; paragraphs 2, 10-16, 19, 20, 34-39, 41, 42, 44, 48-58, 61, 62, 68, 73, 74, 78-83, 86-117, 127-130, 136-141, 143, 145, 146, 148, 151, 154-175, 193, 194, 196, 197, 220-236, 242, 247, 248, 252, 256, 260, 266-272, 280-287, 289, 290, 295, 297-300, 360, 369, 378, 381, 384-410, 416-426, 429-433; SEQ ID NOs: 8 and 14; Tables 3, 4, 5; Examples; claims). Please note: the “]” in several of the paragraph numbers is showing as a “1”. The present citations are referring to the sequential numbering of the paragraphs. Beliveau et al. also teach 2 mM or 18 mg/kg of conjugate (see Figures 11A, 11B, 15C, 25A, 25C, 26A, 26B) and 2 mM, 5 mM, 10 mM, 6 mg/kg doxorubicin (see Figures 15 A, 15B, 15C, 25A, 25C). Beliveau et al. also teach SEQ ID NOs: 6 and 7 with 85.2% identity to present SEQ ID NO: 10 and SEQ ID NOs: 1 and 5 with 65.4% identity to present SEQ ID NO: 10.
However, Beliveau et al. does not teach polysorbate.
For present claims 139-146, 148-150, 154, 157, and 158, Kaur et al. teach utilizing polysorbate 80 in polypeptide therapeutics at a weight % of 4, 8, or 12, at 75 or 80 mg, or 15, 20, or 25 (%v/v) (please refer to the entire reference particularly the abstract; Introduction, Section 2; Tables 1, 4, 7, 12, 15, 18).
Generally, differences in concentration or temperature will not support the patentability of subject matter encompassed by the prior art unless there is evidence indicating such concentration or temperature is critical. "[W]here the general conditions of a claim are disclosed in the prior art, it is not inventive to discover the optimum or workable ranges by routine experimentation." See In re Aller, 220 F.2d 454, 456, 105 USPQ 233, 235 (CCPA 1955) and Peterson, 315 F.3d at 1330, 65 USPQ2d at 1382 ("The normal desire of scientists or artisans to improve upon what is already generally known provides the motivation to determine where in a disclosed set of percentage ranges is the optimum combination of percentages."). See In re Hoeschele, 406 F.2d 1403, 160 USPQ 809 (CCPA 1969) (Claimed elastomeric polyurethanes which fell within the broad scope of the references were held to be unpatentable thereover because, among other reasons, there was no evidence of the criticality of the claimed ranges of molecular weight or molar proportions.). For more recent cases applying this principle, see Merck & Co. Inc. v. Biocraft Lab. Inc., 874 F.2d 804, 809, 10 USPQ2d 1843, 1848 (Fed. Cir. 1989), cert. denied, 493 U.S. 975 (1989)(Claimed ratios were obvious as being reached by routine procedures and producing predictable results); In re Kulling, 897 F.2d 1147, 1149, 14 USPQ2d 1056, 1058 (Fed. Cir. 1990)(Claimed amount of wash solution was found to be unpatentable as a matter of routine optimization in the pertinent art, further supported by the prior art disclosure of the need to avoid undue amounts of wash solution); and In re Geisler, 116 F.3d 1465, 1470, 43 USPQ2d 1362, 1366 (Fed. Cir. 1997)(Claims were unpatentable because appellants failed to submit evidence of criticality to demonstrate that that the wear resistance of the protective layer in the claimed thickness range of 50-100 Angstroms was "unexpectedly good"); Smith v. Nichols, 88 U.S. 112, 118-19 (1874) (a change in form, proportions, or degree "will not sustain a patent"); In re Williams, 36 F.2d 436, 438, 4 USPQ 237 (CCPA 1929) ("It is a settled principle of law that a mere carrying forward of an original patented conception involving only change of form, proportions, or degree, or the substitution of equivalents doing the same thing as the original invention, by substantially the same means, is not such an invention as will sustain a patent, even though the changes of the kind may produce better results than prior inventions.").
The claims would have been obvious because a particular known technique (i.e. utilizing surfactants including polysorbate 80 in polypeptide therapeutic formulations) was recognized as part of the ordinary capabilities of one skilled in the art. See KSR International Co. v. Teleflex Inc., 82 USPQ2d 1385 (U.S. 2007).
Claims 139-146 and 148-158 are rejected under 35 U.S.C. 103 as being unpatentable over Beliveau et al. WO 2017/088058 published June 1, 2017 and Mcauley et al. WO 2018/141910 published August 9, 2018.
For present claims 139-146 and 148-158, Beliveau et al. teach a conjugate of A-(B)n wherein A is SEQ ID NO: 10 (i.e. same length and 100% identity to present SEQ ID NO: 10) conjugated to B which are cancer therapeutics including docetaxel, doxorubicin, cabazitaxel, auristatin, or amanitin wherein conjugation can be via lysines or via a linker including succinic acid, and n can be 1-4 wherein A can be protected via an N-terminal acetyl (i.e. see SEQ ID NO: 15 which has the same length and 100% identity with present SEQ ID NO: 15) and pharmaceutically acceptable acid addition salts including fumaric (i.e. formate) and buffers including formic acid (please refer to the entire specification particularly the abstract; paragraphs 2, 10-16, 19, 20, 34-39, 41, 42, 44, 48-58, 61, 62, 68, 73, 74, 78-83, 86-117, 127-130, 136-141, 143, 145, 146, 148, 151, 154-175, 193, 194, 196, 197, 220-236, 242, 247, 248, 252, 256, 260, 266-272, 280-287, 289, 290, 295, 297-300, 360, 369, 378, 381, 384-410, 416-426, 429-433; SEQ ID NOs: 8 and 14; Tables 3, 4, 5; Examples; claims). Please note: the “]” in several of the paragraph numbers is showing as a “1”. The present citations are referring to the sequential numbering of the paragraphs. Beliveau et al. also teach 2 mM or 18 mg/kg of conjugate (see Figures 11A, 11B, 15C, 25A, 25C, 26A, 26B) and 2 mM, 5 mM, 10 mM, 6 mg/kg doxorubicin (see Figures 15 A, 15B, 15C, 25A, 25C). Beliveau et al. also teach SEQ ID NOs: 6 and 7 with 85.2% identity to present SEQ ID NO: 10 and SEQ ID NOs: 1 and 5 with 65.4% identity to present SEQ ID NO: 10.
However, Beliveau et al. does not teach polysorbate, dextrose, or a pH of about 3.5 to about 4.5.
For present claims 139-146 and 148-158, Mcauley et al. teach low pH pharmaceutical compositions comprising polypeptide conjugates including linkers at 5% weight or 0.1-8 mg/ml wherein the compositions comprise buffers, dextrose or sucrose at 2-12% (w/v), polysorbate 80 at 0.001-0.5% w/v, and formic acid at 0.1% (v/v) at a pH of 3.5-6 (please refer to the entire specification particularly the abstract; paragraphs 10, 19, 24, 25, 30-32, 35, 37, 46, 47, 67, 95, 113, 225, 237, 265, 266, 278, 280, 324, 325, 332, 333, 340, 343; Examples).
Generally, differences in concentration or temperature will not support the patentability of subject matter encompassed by the prior art unless there is evidence indicating such concentration or temperature is critical. "[W]here the general conditions of a claim are disclosed in the prior art, it is not inventive to discover the optimum or workable ranges by routine experimentation." See In re Aller, 220 F.2d 454, 456, 105 USPQ 233, 235 (CCPA 1955) and Peterson, 315 F.3d at 1330, 65 USPQ2d at 1382 ("The normal desire of scientists or artisans to improve upon what is already generally known provides the motivation to determine where in a disclosed set of percentage ranges is the optimum combination of percentages."). See In re Hoeschele, 406 F.2d 1403, 160 USPQ 809 (CCPA 1969) (Claimed elastomeric polyurethanes which fell within the broad scope of the references were held to be unpatentable thereover because, among other reasons, there was no evidence of the criticality of the claimed ranges of molecular weight or molar proportions.). For more recent cases applying this principle, see Merck & Co. Inc. v. Biocraft Lab. Inc., 874 F.2d 804, 809, 10 USPQ2d 1843, 1848 (Fed. Cir. 1989), cert. denied, 493 U.S. 975 (1989)(Claimed ratios were obvious as being reached by routine procedures and producing predictable results); In re Kulling, 897 F.2d 1147, 1149, 14 USPQ2d 1056, 1058 (Fed. Cir. 1990)(Claimed amount of wash solution was found to be unpatentable as a matter of routine optimization in the pertinent art, further supported by the prior art disclosure of the need to avoid undue amounts of wash solution); and In re Geisler, 116 F.3d 1465, 1470, 43 USPQ2d 1362, 1366 (Fed. Cir. 1997)(Claims were unpatentable because appellants failed to submit evidence of criticality to demonstrate that that the wear resistance of the protective layer in the claimed thickness range of 50-100 Angstroms was "unexpectedly good"); Smith v. Nichols, 88 U.S. 112, 118-19 (1874) (a change in form, proportions, or degree "will not sustain a patent"); In re Williams, 36 F.2d 436, 438, 4 USPQ 237 (CCPA 1929) ("It is a settled principle of law that a mere carrying forward of an original patented conception involving only change of form, proportions, or degree, or the substitution of equivalents doing the same thing as the original invention, by substantially the same means, is not such an invention as will sustain a patent, even though the changes of the kind may produce better results than prior inventions.").
The claims would have been obvious because a particular known technique (i.e. utilizing saccharides in pharmaceutical formulations, utilizing surfactants including polysorbate 80 in polypeptide therapeutic formulations; making polypeptide conjugates with a low pH) was recognized as part of the ordinary capabilities of one skilled in the art. See KSR International Co. v. Teleflex Inc., 82 USPQ2d 1385 (U.S. 2007).
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 139-146 and 148-158 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 51, 52, 69-71, 73-79, and 82 of copending Application No. 17/270,787 in view of Beliveau et al. WO 2017/088058 published June 1, 2017 and Mcauley et al. WO 2018/141910 published August 9, 2018.
Copending Application No. 17/270,787 claims A-(B)n wherein A is SEQ ID NO: 10, B is an anticancer therapeutic including doxorubicin, and n is 1-4, linkers, and protecting groups of acetyl or succinyl.
Beliveau et al. teach a conjugate of A-(B)n wherein A is SEQ ID NO: 10 (i.e. same length and 100% identity to present SEQ ID NO: 10) conjugated to B which are cancer therapeutics including docetaxel, doxorubicin, cabazitaxel, auristatin, or amanitin wherein conjugation can be via lysines or via a linker including succinic acid, and n can be 1-4 wherein A can be protected via an N-terminal acetyl (i.e. see SEQ ID NO: 15 which has the same length and 100% identity with present SEQ ID NO: 15) and pharmaceutically acceptable acid addition salts including fumaric (i.e. formate) and buffers including formic acid (please refer to the entire specification particularly the abstract; paragraphs 2, 10-16, 19, 20, 34-39, 41, 42, 44, 48-58, 61, 62, 68, 73, 74, 78-83, 86-117, 127-130, 136-141, 143, 145, 146, 148, 151, 154-175, 193, 194, 196, 197, 220-236, 242, 247, 248, 252, 256, 260, 266-272, 280-287, 289, 290, 295, 297-300, 360, 369, 378, 381, 384-410, 416-426, 429-433; SEQ ID NOs: 8 and 14; Tables 3, 4, 5; Examples; claims). Please note: the “]” in several of the paragraph numbers is showing as a “1”. The present citations are referring to the sequential numbering of the paragraphs. Beliveau et al. also teach 2 mM or 18 mg/kg of conjugate (see Figures 11A, 11B, 15C, 25A, 25C, 26A, 26B) and 2 mM, 5 mM, 10 mM, 6 mg/kg doxorubicin (see Figures 15 A, 15B, 15C, 25A, 25C). Beliveau et al. also teach SEQ ID NOs: 6 and 7 with 85.2% identity to present SEQ ID NO: 10 and SEQ ID NOs: 1 and 5 with 65.4% identity to present SEQ ID NO: 10.
Mcauley et al. teach low pH pharmaceutical compositions comprising polypeptide conjugates including linkers at 5% weight or 0.1-8 mg/ml wherein the compositions comprise buffers, dextrose or sucrose at 2-12% (w/v), polysorbate 80 at 0.001-0.5% w/v, and formic acid at 0.1% (v/v) at a pH of 3.5-6 (please refer to the entire specification particularly the abstract; paragraphs 10, 19, 24, 25, 30-32, 35, 37, 46, 47, 67, 95, 113, 225, 237, 265, 266, 278, 280, 324, 325, 332, 333, 340, 343; Examples).
Generally, differences in concentration or temperature will not support the patentability of subject matter encompassed by the prior art unless there is evidence indicating such concentration or temperature is critical. "[W]here the general conditions of a claim are disclosed in the prior art, it is not inventive to discover the optimum or workable ranges by routine experimentation." See In re Aller, 220 F.2d 454, 456, 105 USPQ 233, 235 (CCPA 1955) and Peterson, 315 F.3d at 1330, 65 USPQ2d at 1382 ("The normal desire of scientists or artisans to improve upon what is already generally known provides the motivation to determine where in a disclosed set of percentage ranges is the optimum combination of percentages."). See In re Hoeschele, 406 F.2d 1403, 160 USPQ 809 (CCPA 1969) (Claimed elastomeric polyurethanes which fell within the broad scope of the references were held to be unpatentable thereover because, among other reasons, there was no evidence of the criticality of the claimed ranges of molecular weight or molar proportions.). For more recent cases applying this principle, see Merck & Co. Inc. v. Biocraft Lab. Inc., 874 F.2d 804, 809, 10 USPQ2d 1843, 1848 (Fed. Cir. 1989), cert. denied, 493 U.S. 975 (1989)(Claimed ratios were obvious as being reached by routine procedures and producing predictable results); In re Kulling, 897 F.2d 1147, 1149, 14 USPQ2d 1056, 1058 (Fed. Cir. 1990)(Claimed amount of wash solution was found to be unpatentable as a matter of routine optimization in the pertinent art, further supported by the prior art disclosure of the need to avoid undue amounts of wash solution); and In re Geisler, 116 F.3d 1465, 1470, 43 USPQ2d 1362, 1366 (Fed. Cir. 1997)(Claims were unpatentable because appellants failed to submit evidence of criticality to demonstrate that that the wear resistance of the protective layer in the claimed thickness range of 50-100 Angstroms was "unexpectedly good"); Smith v. Nichols, 88 U.S. 112, 118-19 (1874) (a change in form, proportions, or degree "will not sustain a patent"); In re Williams, 36 F.2d 436, 438, 4 USPQ 237 (CCPA 1929) ("It is a settled principle of law that a mere carrying forward of an original patented conception involving only change of form, proportions, or degree, or the substitution of equivalents doing the same thing as the original invention, by substantially the same means, is not such an invention as will sustain a patent, even though the changes of the kind may produce better results than prior inventions.").
The claims would have been obvious because a particular known technique (i.e. utilizing saccharides in pharmaceutical formulations, utilizing surfactants including polysorbate 80 in polypeptide therapeutic formulations; making polypeptide conjugates with a low pH) was recognized as part of the ordinary capabilities of one skilled in the art. See KSR International Co. v. Teleflex Inc., 82 USPQ2d 1385 (U.S. 2007).
This is a provisional nonstatutory double patenting rejection.
Claims 139-146 and 148-158 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 78-97 of copending Application No. 18/278,821 in view of Beliveau et al. WO 2017/088058 published June 1, 2017 and Mcauley et al. WO 2018/141910 published August 9, 2018.
Copending Application No. 18/278,821 claims A-(B)n wherein A is SEQ ID NO: 10, B is an antitumor agent including doxorubicin, and n is 0-5, and protecting groups of acetyl.
Beliveau et al. teach a conjugate of A-(B)n wherein A is SEQ ID NO: 10 (i.e. same length and 100% identity to present SEQ ID NO: 10) conjugated to B which are cancer therapeutics including docetaxel, doxorubicin, cabazitaxel, auristatin, or amanitin wherein conjugation can be via lysines or via a linker including succinic acid, and n can be 1-4 wherein A can be protected via an N-terminal acetyl (i.e. see SEQ ID NO: 15 which has the same length and 100% identity with present SEQ ID NO: 15) and pharmaceutically acceptable acid addition salts including fumaric (i.e. formate) and buffers including formic acid (please refer to the entire specification particularly the abstract; paragraphs 2, 10-16, 19, 20, 34-39, 41, 42, 44, 48-58, 61, 62, 68, 73, 74, 78-83, 86-117, 127-130, 136-141, 143, 145, 146, 148, 151, 154-175, 193, 194, 196, 197, 220-236, 242, 247, 248, 252, 256, 260, 266-272, 280-287, 289, 290, 295, 297-300, 360, 369, 378, 381, 384-410, 416-426, 429-433; SEQ ID NOs: 8 and 14; Tables 3, 4, 5; Examples; claims). Please note: the “]” in several of the paragraph numbers is showing as a “1”. The present citations are referring to the sequential numbering of the paragraphs. Beliveau et al. also teach 2 mM or 18 mg/kg of conjugate (see Figures 11A, 11B, 15C, 25A, 25C, 26A, 26B) and 2 mM, 5 mM, 10 mM, 6 mg/kg doxorubicin (see Figures 15 A, 15B, 15C, 25A, 25C). Beliveau et al. also teach SEQ ID NOs: 6 and 7 with 85.2% identity to present SEQ ID NO: 10 and SEQ ID NOs: 1 and 5 with 65.4% identity to present SEQ ID NO: 10.
Mcauley et al. teach low pH pharmaceutical compositions comprising polypeptide conjugates including linkers at 5% weight or 0.1-8 mg/ml wherein the compositions comprise buffers, dextrose or sucrose at 2-12% (w/v), polysorbate 80 at 0.001-0.5% w/v, and formic acid at 0.1% (v/v) at a pH of 3.5-6 (please refer to the entire specification particularly the abstract; paragraphs 10, 19, 24, 25, 30-32, 35, 37, 46, 47, 67, 95, 113, 225, 237, 265, 266, 278, 280, 324, 325, 332, 333, 340, 343; Examples).
Generally, differences in concentration or temperature will not support the patentability of subject matter encompassed by the prior art unless there is evidence indicating such concentration or temperature is critical. "[W]here the general conditions of a claim are disclosed in the prior art, it is not inventive to discover the optimum or workable ranges by routine experimentation." See In re Aller, 220 F.2d 454, 456, 105 USPQ 233, 235 (CCPA 1955) and Peterson, 315 F.3d at 1330, 65 USPQ2d at 1382 ("The normal desire of scientists or artisans to improve upon what is already generally known provides the motivation to determine where in a disclosed set of percentage ranges is the optimum combination of percentages."). See In re Hoeschele, 406 F.2d 1403, 160 USPQ 809 (CCPA 1969) (Claimed elastomeric polyurethanes which fell within the broad scope of the references were held to be unpatentable thereover because, among other reasons, there was no evidence of the criticality of the claimed ranges of molecular weight or molar proportions.). For more recent cases applying this principle, see Merck & Co. Inc. v. Biocraft Lab. Inc., 874 F.2d 804, 809, 10 USPQ2d 1843, 1848 (Fed. Cir. 1989), cert. denied, 493 U.S. 975 (1989)(Claimed ratios were obvious as being reached by routine procedures and producing predictable results); In re Kulling, 897 F.2d 1147, 1149, 14 USPQ2d 1056, 1058 (Fed. Cir. 1990)(Claimed amount of wash solution was found to be unpatentable as a matter of routine optimization in the pertinent art, further supported by the prior art disclosure of the need to avoid undue amounts of wash solution); and In re Geisler, 116 F.3d 1465, 1470, 43 USPQ2d 1362, 1366 (Fed. Cir. 1997)(Claims were unpatentable because appellants failed to submit evidence of criticality to demonstrate that that the wear resistance of the protective layer in the claimed thickness range of 50-100 Angstroms was "unexpectedly good"); Smith v. Nichols, 88 U.S. 112, 118-19 (1874) (a change in form, proportions, or degree "will not sustain a patent"); In re Williams, 36 F.2d 436, 438, 4 USPQ 237 (CCPA 1929) ("It is a settled principle of law that a mere carrying forward of an original patented conception involving only change of form, proportions, or degree, or the substitution of equivalents doing the same thing as the original invention, by substantially the same means, is not such an invention as will sustain a patent, even though the changes of the kind may produce better results than prior inventions.").
The claims would have been obvious because a particular known technique (i.e. utilizing saccharides in pharmaceutical formulations, utilizing surfactants including polysorbate 80 in polypeptide therapeutic formulations; making polypeptide conjugates with a low pH) was recognized as part of the ordinary capabilities of one skilled in the art. See KSR International Co. v. Teleflex Inc., 82 USPQ2d 1385 (U.S. 2007).
This is a provisional nonstatutory double patenting rejection.
Claims 139-146 and 148-158 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-20 of U.S. Patent No. 12,269,902 in view of Beliveau et al. WO 2017/088058 published June 1, 2017 and Mcauley et al. WO 2018/141910 published August 9, 2018.
U.S. Patent No. 12,269,902 claims conjugates of A-(B)n wherein A is SEQ ID NO: 10 or SEQ ID NO: 15, B is a therapeutic agent including docetaxel, and n is 0-5, linkers, and acetyl at the N-terminus.
Beliveau et al. teach a conjugate of A-(B)n wherein A is SEQ ID NO: 10 (i.e. same length and 100% identity to present SEQ ID NO: 10) conjugated to B which are cancer therapeutics including docetaxel, doxorubicin, cabazitaxel, auristatin, or amanitin wherein conjugation can be via lysines or via a linker including succinic acid, and n can be 1-4 wherein A can be protected via an N-terminal acetyl (i.e. see SEQ ID NO: 15 which has the same length and 100% identity with present SEQ ID NO: 15) and pharmaceutically acceptable acid addition salts including fumaric (i.e. formate) and buffers including formic acid (please refer to the entire specification particularly the abstract; paragraphs 2, 10-16, 19, 20, 34-39, 41, 42, 44, 48-58, 61, 62, 68, 73, 74, 78-83, 86-117, 127-130, 136-141, 143, 145, 146, 148, 151, 154-175, 193, 194, 196, 197, 220-236, 242, 247, 248, 252, 256, 260, 266-272, 280-287, 289, 290, 295, 297-300, 360, 369, 378, 381, 384-410, 416-426, 429-433; SEQ ID NOs: 8 and 14; Tables 3, 4, 5; Examples; claims). Please note: the “]” in several of the paragraph numbers is showing as a “1”. The present citations are referring to the sequential numbering of the paragraphs. Beliveau et al. also teach 2 mM or 18 mg/kg of conjugate (see Figures 11A, 11B, 15C, 25A, 25C, 26A, 26B) and 2 mM, 5 mM, 10 mM, 6 mg/kg doxorubicin (see Figures 15 A, 15B, 15C, 25A, 25C). Beliveau et al. also teach SEQ ID NOs: 6 and 7 with 85.2% identity to present SEQ ID NO: 10 and SEQ ID NOs: 1 and 5 with 65.4% identity to present SEQ ID NO: 10.
Mcauley et al. teach low pH pharmaceutical compositions comprising polypeptide conjugates including linkers at 5% weight or 0.1-8 mg/ml wherein the compositions comprise buffers, dextrose or sucrose at 2-12% (w/v), polysorbate 80 at 0.001-0.5% w/v, and formic acid at 0.1% (v/v) at a pH of 3.5-6 (please refer to the entire specification particularly the abstract; paragraphs 10, 19, 24, 25, 30-32, 35, 37, 46, 47, 67, 95, 113, 225, 237, 265, 266, 278, 280, 324, 325, 332, 333, 340, 343; Examples).
Generally, differences in concentration or temperature will not support the patentability of subject matter encompassed by the prior art unless there is evidence indicating such concentration or temperature is critical. "[W]here the general conditions of a claim are disclosed in the prior art, it is not inventive to discover the optimum or workable ranges by routine experimentation." See In re Aller, 220 F.2d 454, 456, 105 USPQ 233, 235 (CCPA 1955) and Peterson, 315 F.3d at 1330, 65 USPQ2d at 1382 ("The normal desire of scientists or artisans to improve upon what is already generally known provides the motivation to determine where in a disclosed set of percentage ranges is the optimum combination of percentages."). See In re Hoeschele, 406 F.2d 1403, 160 USPQ 809 (CCPA 1969) (Claimed elastomeric polyurethanes which fell within the broad scope of the references were held to be unpatentable thereover because, among other reasons, there was no evidence of the criticality of the claimed ranges of molecular weight or molar proportions.). For more recent cases applying this principle, see Merck & Co. Inc. v. Biocraft Lab. Inc., 874 F.2d 804, 809, 10 USPQ2d 1843, 1848 (Fed. Cir. 1989), cert. denied, 493 U.S. 975 (1989)(Claimed ratios were obvious as being reached by routine procedures and producing predictable results); In re Kulling, 897 F.2d 1147, 1149, 14 USPQ2d 1056, 1058 (Fed. Cir. 1990)(Claimed amount of wash solution was found to be unpatentable as a matter of routine optimization in the pertinent art, further supported by the prior art disclosure of the need to avoid undue amounts of wash solution); and In re Geisler, 116 F.3d 1465, 1470, 43 USPQ2d 1362, 1366 (Fed. Cir. 1997)(Claims were unpatentable because appellants failed to submit evidence of criticality to demonstrate that that the wear resistance of the protective layer in the claimed thickness range of 50-100 Angstroms was "unexpectedly good"); Smith v. Nichols, 88 U.S. 112, 118-19 (1874) (a change in form, proportions, or degree "will not sustain a patent"); In re Williams, 36 F.2d 436, 438, 4 USPQ 237 (CCPA 1929) ("It is a settled principle of law that a mere carrying forward of an original patented conception involving only change of form, proportions, or degree, or the substitution of equivalents doing the same thing as the original invention, by substantially the same means, is not such an invention as will sustain a patent, even though the changes of the kind may produce better results than prior inventions.").
The claims would have been obvious because a particular known technique (i.e. utilizing saccharides in pharmaceutical formulations, utilizing surfactants including polysorbate 80 in polypeptide therapeutic formulations; making polypeptide conjugates with a low pH) was recognized as part of the ordinary capabilities of one skilled in the art. See KSR International Co. v. Teleflex Inc., 82 USPQ2d 1385 (U.S. 2007).
Claims 139-146 and 148-158 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-21 of U.S. Patent No. 11,780,882 in view of Beliveau et al. WO 2017/088058 published June 1, 2017 and Mcauley et al. WO 2018/141910 published August 9, 2018.
U.S. Patent No. 11,780,882 claims conjugates comprising SEQ ID NO: 10 or SEQ ID NO: 15, an anticancer agent, linkers, and acetyl at the N-terminus.
Beliveau et al. teach a conjugate of A-(B)n wherein A is SEQ ID NO: 10 (i.e. same length and 100% identity to present SEQ ID NO: 10) conjugated to B which are cancer therapeutics including docetaxel, doxorubicin, cabazitaxel, auristatin, or amanitin wherein conjugation can be via lysines or via a linker including succinic acid, and n can be 1-4 wherein A can be protected via an N-terminal acetyl (i.e. see SEQ ID NO: 15 which has the same length and 100% identity with present SEQ ID NO: 15) and pharmaceutically acceptable acid addition salts including fumaric (i.e. formate) and buffers including formic acid (please refer to the entire specification particularly the abstract; paragraphs 2, 10-16, 19, 20, 34-39, 41, 42, 44, 48-58, 61, 62, 68, 73, 74, 78-83, 86-117, 127-130, 136-141, 143, 145, 146, 148, 151, 154-175, 193, 194, 196, 197, 220-236, 242, 247, 248, 252, 256, 260, 266-272, 280-287, 289, 290, 295, 297-300, 360, 369, 378, 381, 384-410, 416-426, 429-433; SEQ ID NOs: 8 and 14; Tables 3, 4, 5; Examples; claims). Please note: the “]” in several of the paragraph numbers is showing as a “1”. The present citations are referring to the sequential numbering of the paragraphs. Beliveau et al. also teach 2 mM or 18 mg/kg of conjugate (see Figures 11A, 11B, 15C, 25A, 25C, 26A, 26B) and 2 mM, 5 mM, 10 mM, 6 mg/kg doxorubicin (see Figures 15 A, 15B, 15C, 25A, 25C). Beliveau et al. also teach SEQ ID NOs: 6 and 7 with 85.2% identity to present SEQ ID NO: 10 and SEQ ID NOs: 1 and 5 with 65.4% identity to present SEQ ID NO: 10.
Mcauley et al. teach low pH pharmaceutical compositions comprising polypeptide conjugates including linkers at 5% weight or 0.1-8 mg/ml wherein the compositions comprise buffers, dextrose or sucrose at 2-12% (w/v), polysorbate 80 at 0.001-0.5% w/v, and formic acid at 0.1% (v/v) at a pH of 3.5-6 (please refer to the entire specification particularly the abstract; paragraphs 10, 19, 24, 25, 30-32, 35, 37, 46, 47, 67, 95, 113, 225, 237, 265, 266, 278, 280, 324, 325, 332, 333, 340, 343; Examples).
Generally, differences in concentration or temperature will not support the patentability of subject matter encompassed by the prior art unless there is evidence indicating such concentration or temperature is critical. "[W]here the general conditions of a claim are disclosed in the prior art, it is not inventive to discover the optimum or workable ranges by routine experimentation." See In re Aller, 220 F.2d 454, 456, 105 USPQ 233, 235 (CCPA 1955) and Peterson, 315 F.3d at 1330, 65 USPQ2d at 1382 ("The normal desire of scientists or artisans to improve upon what is already generally known provides the motivation to determine where in a disclosed set of percentage ranges is the optimum combination of percentages."). See In re Hoeschele, 406 F.2d 1403, 160 USPQ 809 (CCPA 1969) (Claimed elastomeric polyurethanes which fell within the broad scope of the references were held to be unpatentable thereover because, among other reasons, there was no evidence of the criticality of the claimed ranges of molecular weight or molar proportions.). For more recent cases applying this principle, see Merck & Co. Inc. v. Biocraft Lab. Inc., 874 F.2d 804, 809, 10 USPQ2d 1843, 1848 (Fed. Cir. 1989), cert. denied, 493 U.S. 975 (1989)(Claimed ratios were obvious as being reached by routine procedures and producing predictable results); In re Kulling, 897 F.2d 1147, 1149, 14 USPQ2d 1056, 1058 (Fed. Cir. 1990)(Claimed amount of wash solution was found to be unpatentable as a matter of routine optimization in the pertinent art, further supported by the prior art disclosure of the need to avoid undue amounts of wash solution); and In re Geisler, 116 F.3d 1465, 1470, 43 USPQ2d 1362, 1366 (Fed. Cir. 1997)(Claims were unpatentable because appellants failed to submit evidence of criticality to demonstrate that that the wear resistance of the protective layer in the claimed thickness range of 50-100 Angstroms was "unexpectedly good"); Smith v. Nichols, 88 U.S. 112, 118-19 (1874) (a change in form, proportions, or degree "will not sustain a patent"); In re Williams, 36 F.2d 436, 438, 4 USPQ 237 (CCPA 1929) ("It is a settled principle of law that a mere carrying forward of an original patented conception involving only change of form, proportions, or degree, or the substitution of equivalents doing the same thing as the original invention, by substantially the same means, is not such an invention as will sustain a patent, even though the changes of the kind may produce better results than prior inventions.").
The claims would have been obvious because the substitution of one known element (i.e. genus of anticancer agents) for another (i.e. species of docetaxel, doxorubicin, cabazitaxel, auristatin, or amanitin) would have yielded predictable results to one of ordinary skill in the art at the time of the invention. The claims would have been obvious because a particular known technique (i.e. utilizing saccharides in pharmaceutical formulations, utilizing surfactants including polysorbate 80 in polypeptide therapeutic formulations; making polypeptide conjugates with a low pH) was recognized as part of the ordinary capabilities of one skilled in the art. See KSR International Co. v. Teleflex Inc., 82 USPQ2d 1385 (U.S. 2007).
Claims 139-146 and 148-158 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-26 of U.S. Patent No. 11,034,727 in view of Beliveau et al. WO 2017/088058 published June 1, 2017 and Mcauley et al. WO 2018/141910 published August 9, 2018.
U.S. Patent No. 11,034,727 claims conjugates of A-(B)n wherein A is SEQ ID NO: 10 or SEQ ID NO: 15, B is a therapeutic agent including docetaxel, and n is 1-4, linkers, and acetyl at the N-terminus.
Beliveau et al. teach a conjugate of A-(B)n wherein A is SEQ ID NO: 10 (i.e. same length and 100% identity to present SEQ ID NO: 10) conjugated to B which are cancer therapeutics including docetaxel, doxorubicin, cabazitaxel, auristatin, or amanitin wherein conjugation can be via lysines or via a linker including succinic acid, and n can be 1-4 wherein A can be protected via an N-terminal acetyl (i.e. see SEQ ID NO: 15 which has the same length and 100% identity with present SEQ ID NO: 15) and pharmaceutically acceptable acid addition salts including fumaric (i.e. formate) and buffers including formic acid (please refer to the entire specification particularly the abstract; paragraphs 2, 10-16, 19, 20, 34-39, 41, 42, 44, 48-58, 61, 62, 68, 73, 74, 78-83, 86-117, 127-130, 136-141, 143, 145, 146, 148, 151, 154-175, 193, 194, 196, 197, 220-236, 242, 247, 248, 252, 256, 260, 266-272, 280-287, 289, 290, 295, 297-300, 360, 369, 378, 381, 384-410, 416-426, 429-433; SEQ ID NOs: 8 and 14; Tables 3, 4, 5; Examples; claims). Please note: the “]” in several of the paragraph numbers is showing as a “1”. The present citations are referring to the sequential numbering of the paragraphs. Beliveau et al. also teach 2 mM or 18 mg/kg of conjugate (see Figures 11A, 11B, 15C, 25A, 25C, 26A, 26B) and 2 mM, 5 mM, 10 mM, 6 mg/kg doxorubicin (see Figures 15 A, 15B, 15C, 25A, 25C). Beliveau et al. also teach SEQ ID NOs: 6 and 7 with 85.2% identity to present SEQ ID NO: 10 and SEQ ID NOs: 1 and 5 with 65.4% identity to present SEQ ID NO: 10.
Mcauley et al. teach low pH pharmaceutical compositions comprising polypeptide conjugates including linkers at 5% weight or 0.1-8 mg/ml wh