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 .
Election/Restrictions
Applicant’s election without traverse of Group I (claims 1-25) and the species (a) SEQ ID NO: 306, (b) Eicosanedioyl-gamma-Glu-gamma-Glu-OEG-OEG, or (c) amino acid sequence of SEQ ID NO: 252 in the reply filed on 6/3/2026 is acknowledged.
Status of Application, Amendments, And/Or Claims
Claims 1-30 are pending.
Claims 26-30 are withdrawn for being drawn to non-elected inventions (i.e., Groups II-IV). Claims 15-24 are withdrawn for being drawn to a non-elected species (i.e., SEQ ID Nos: 5, 7, 241, 242, 247, 248, 255, 257, 277 and 278).
Claims 1-25 are under examination to the extent they read on elected species.
Information Disclosure Statement
The Information Disclosure Statement filed on 12/16/2025, 2/9/2026 and 6/9/2026 have been considered.
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.
Claims 1-13 and 25 are 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.
The written description in this case only sets forth only a peptide or a pharmaceutically acceptable salt thereof, wherein the peptide comprises amino acid sequences of SEQ ID NO: 1-167 and 240-244, 247-,248, 251, 252, 257-259, 267, 270, 275, 277 and 278 as gastrin releasing peptide, and therefore, the written description is not commensurate in scope with the claims which read on any peptide having Formula V: . XO-X1-X2-Ar-X4-X5-V-X7-X8-L-X10-X11-X12, wherein: X0 is absent or Glu; X1 is D-Ser, Ser, or Gly; X2 is Asn, Glu, Arg, Ala, Asp, Gln, or Lys(Ac); Ar is His, 3-(3-pyridyl)alanine (3Pal), 3-(4-pyridyl)alanine (4Pal), or 3-(2-pyridyl)alanine (2Pal); X4 is Arg, His, Trp, 7-methyltryptophan (7MeTrp), 6-methyltryptophan (6MeTrp), 7- fluorotryptophan (7FTrp), 6-fluorotryptophan (6FTrp), or 3-(2-naphthyl)alanine (2Nal); X5 is Ala, a-aminoisobutyric acid (Aib), or D-Ala; X7 is D-Ala, P-Ala, a-aminoisobutyric acid (Aib), Gly, Ala, or S-p-aminobutanoic acid (BABA); X8 is His or NMeHis; X10 is absent, Met, Arg, norleucine (Nle), 3-(3-pyridyl)alanine (3Pal), or Lys(Me)3; X11 is absent, sarcosine (Sar), a-aminoisobutyric acid (Aib), or Arg; and X12 is absent; each L' is independently -((CH2)vNR1)W-CO(CH2)x0(PEG)y(CH2)zNR-;PEG is -CH2CH20-;v is 2-6; w is 0-1; x is 1-4; y is 1-4; z is 2-24;R1 is H or -CH3; or each L1 is OEG;OEG is -NH-PEG-PEG-CH2C(=O)-;PEG is -CH2CH20-; each L2 is independently a natural or unnatural amino acid or amino acid analog; each L3 is independently a substituted or unsubstituted C2-C26 fatty acyl group; a is 1, 2, 3, or 4;p is 0-8;q is 0-6; and r is 1 or 2, and a pharmaceutical composition comprising the same.
The claims broadly encompass millions of peptide variants encompassed by Formula V that comprises the functionality of reducing body weight in a subject in need thereof.
The specification at pg. 1-2, describes that gastrin releasing peptide (GRP) is a 27 amino acid peptide that stimulates release of gastrin and regulates gastric acid secretion. The specification at pg.175-178, Table 4 discloses that peptides 1-278 when tested in vitro for GRPR activity, its EC50 ranged from nanomolar to greater than >1000 nm, or >10,000 nm (very little activity). The specification at pg. 178-179, Tables 5-6, discloses a total of 8 peptides (peptides 5-8, 241, 242, 247, 248, and 277-278) that show reduction in food intake in vivo and change in body weight. The specification does not disclose any peptide having GRPR activity EC50 >10,000 nm that reduces food intake or body weight.
To provide adequate written description and evidence of possession of a claimed genus, the specification must provide sufficient distinguishing identifying characteristics of the genus. Some of the factual considerations that are weighed when determining a written description include the level of skill and knowledge in the art, the disclosure of complete or partial structures, the disclosure of physical and or chemical properties, adequate disclosure of the functional characteristics, the correlation between structure and function, and disclosure of methods of making.
Nielsen et al. (IDS, US Pub. No. 20020165148) teaches making analogs and derivatives of gastrin releasing peptide (peptide) of amino acid sequence of SEQ ID NO: 2 for treating diabetes and obesity (Abstract). The specification at pg. 178-179, Tables 5-6, only disclose a total of 8 peptides (peptides 5-8, 241, 242, 247, 248, and 277-278) that show reduction in food intake in vivo and change in body weight. The specification does not disclose any peptide having mutations and GRPR activity EC50 >10,000 nm that reduces food intake or body weight. The specification and claims do not provide any guidance that could distinguish compounds in the genus from others that can comprise mutations including insertion, deletion or substitution while maintain the functionality of the GRP peptide. No common structural attributes identify the members of the genus. The general knowledge and level of skill in the art do not supplement the omitted description because specific, not general, guidance is what is needed.
Applicant is directed to the Guidelines for the Examination of Patent Applications Under the 35 U.S.C. 112, 1 "Written Description" Requirement, Federal Register, Vol. 66, No. 4, pages 1099-1111, Friday January 5, 2001.
Vas-Cath Inc. V. Mahurka, 19 USPQ2d 1111, states that applicant must convey with reasonable clarity to those skilled in the art that, as of the filing date sought, he or she was in possession of the invention. The invention, for purposes of the written description inquiry, is whatever is now claimed (see page 1117). The specification does not “clearly allow persons of ordinary skill in the art to recognize that [he or she] invented what is claimed.” (see Vas-Cath at page 1116).
A description of a genus may be achieved by means of a recitation of a representative number of species falling within the scope of the genus or of a recitation of structural features common to the members of the genus, which features constitute a substantial portion of the genus. Regents of the University of California v. Eli Lilly & Co., 119 F3d 1559, 1569, 43 USPQ2d 1398, 1406 (Fed. Cir. 1997). In Regents of the University of California v. Eli Lilly (43 USPQ2d 1398-1412), the court held that a generic statement which defines a genus of nucleic acids by only their functional activity does not provide an adequate written description of the genus. The court indicated that, while applicants are not required to disclose every species encompassed by a genus, the description of the genus is achieved by the recitation of a representative number of species falling within the scope of the claimed genus. At section B (1), the court states an adequate written description of a DNA ... requires a precise definition, such as by structure, formula, chemical name, or physical properties, not a mere wish or plan for obtaining the claimed chemical invention.
As discussed above, the skilled artisan cannot envision the detailed chemical structure of the genus “peptide of Formula V: XO-X1-X2-Ar-X4-X5-V-X7-X8-L-X10-X11-X12, wherein: X0 is absent or Glu; X1 is D-Ser, Ser, or Gly; X2 is Asn, Glu, Arg, Ala, Asp, Gln, or Lys(Ac); Ar is His, 3-(3-pyridyl)alanine (3Pal), 3-(4-pyridyl)alanine (4Pal), or 3-(2-pyridyl)alanine (2Pal); X4 is Arg, His, Trp, 7-methyltryptophan (7MeTrp), 6-methyltryptophan (6MeTrp), 7- fluorotryptophan (7FTrp), 6-fluorotryptophan (6FTrp), or 3-(2-naphthyl)alanine (2Nal); X5 is Ala, a-aminoisobutyric acid (Aib), or D-Ala; X7 is D-Ala, P-Ala, a-aminoisobutyric acid (Aib), Gly, Ala, or S-p-aminobutanoic acid (BABA); X8 is His or NMeHis; X10 is absent, Met, Arg, norleucine (Nle), 3-(3-pyridyl)alanine (3Pal), or Lys(Me)3; X11 is absent, sarcosine (Sar), a-aminoisobutyric acid (Aib), or Arg; and X12 is absent; each L' is independently -((CH2)vNR1)W-CO(CH2)x0(PEG)y(CH2)zNR-;PEG is -CH2CH20-;v is 2-6; w is 0-1; x is 1-4; y is 1-4; z is 2-24;R1 is H or -CH3; or each L1 is OEG;OEG is -NH-PEG-PEG-CH2C(=O)-;PEG is -CH2CH20-; each L2 is independently a natural or unnatural amino acid or amino acid analog; each L3 is independently a substituted or unsubstituted C2-C26 fatty acyl group; a is 1, 2, 3, or 4;p is 0-8;q is 0-6; and r is 1 or 2” and therefore conception is not achieved until reduction to practice has occurred, regardless of the complexity or simplicity of the method of making a mutation. The compound itself is required. See Fiers v.Revel, 25USPQ2d 1601 at 1606 (CAFC 1993) and Amgen v.Baird, 30 Chugai Pharmaceutical Co. Ltd., 18 USPQ2d 1016. One cannot describe what one has not conceived. See Fiddes v. Baird, 30 USPQ2d 148 at 1483. In Fiddes, claims directed to mammalian FGF's were found to be unpatentable due to lack of written description for that broad class.
Therefore, only a peptide or a pharmaceutically acceptable salt thereof, wherein the peptide comprises amino acid sequences of SEQ ID NO: 1-167 and 240-244, 247-,248, 251, 252, 257-259, 267, 270, 275, 277 and 278 as gastrin releasing peptide, but not the full breadth of the claim meets the written description provision of 35 U.S.C. §112, first paragraph.
Applicant is reminded that Vas-Cath makes clear that the written description provision of 35 U.S.C. 112 is severable from its enablement provision (see page 1115).
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.
Claim(s) 1-13 and 25 are rejected under 35 U.S.C. 103 as being unpatentable over Levy et al. (US Pub. No. 20060293232) in view of Lau et al. (IDS, EP 1863839).
The instantly claimed invention is broadly drawn to a peptide of Formula V: XO-X1-X2-Ar-X4-X5-V-X7-X8-L-X10-X11-X12, wherein: X0 is absent or Glu; X1 is D-Ser, Ser, or Gly; X2 is Asn, Glu, Arg, Ala, Asp, Gln, or Lys(Ac); Ar is His, 3-(3-pyridyl)alanine (3Pal), 3-(4-pyridyl)alanine (4Pal), or 3-(2-pyridyl)alanine (2Pal); X4 is Arg, His, Trp, 7-methyltryptophan (7MeTrp), 6-methyltryptophan (6MeTrp), 7- fluorotryptophan (7FTrp), 6-fluorotryptophan (6FTrp), or 3-(2-naphthyl)alanine (2Nal); X5 is Ala, a-aminoisobutyric acid (Aib), or D-Ala; X7 is D-Ala, P-Ala, a-aminoisobutyric acid (Aib), Gly, Ala, or S-p-aminobutanoic acid (BABA); X8 is His or NMeHis; X10 is absent, Met, Arg, norleucine (Nle), 3-(3-pyridyl)alanine (3Pal), or Lys(Me)3; X11 is absent, sarcosine (Sar), a-aminoisobutyric acid (Aib), or Arg; and X12 is absent; each L' is independently -((CH2)vNR1)W-CO(CH2)x0(PEG)y(CH2)zNR-;PEG is -CH2CH20-;v is 2-6; w is 0-1; x is 1-4; y is 1-4; z is 2-24;R1 is H or -CH3; or each L1 is OEG;OEG is -NH-PEG-PEG-CH2C(=O)-;PEG is -CH2CH20-; each L2 is independently a natural or unnatural amino acid or amino acid analog; each L3 is independently a substituted or unsubstituted C2-C26 fatty acyl group; a is 1, 2, 3, or 4;p is 0-8;q is 0-6; and r is 1 or 2 (claims 1-13), and a pharmaceutical composition of claim 1.
Levy et al teach a peptide GRP for which C-terminal 10 amino acid sequences possess most of the activity and they teach that the sequence is: GNWWAVGHLM (see paragraph [1010]. The sequence taught by Levy encompasses the sequence limitation of formula V having 100% sequence identity, wherein X0, X11 and X12 are absent according to formula V. Levy et al do not teach have a linker acyl moiety at the N-terminal of the GRP peptide. Regarding claim 25, they teach a pharmaceutical composition comprising a peptide and a pharmaceutically acceptable diluent and buffer (see paragraph [0268]).
Lau et al teach acylation of a GLP-1 peptide using a fatty acid linked with OEG-OEG via gamma-glu (see paragraph [0069-0070].
Therefore, it would have been prima facie obvious to one of the skill in the art at the time of the inventio was made to use acyl moiety including HOOC-(CH2)16-gamma glu-OEG-OEG as taught by Lau et to attach with a peptide like GRP ( GNWWAVGHLM ) as taught by Levy et al. Further, one of the skill in the art would have been motivated to use an acyl moiety to attach with GRP as taught by Lau et al because acylation of a peptide increases the half-life of the peptide and it is well known in the art that acyl moiety binds to albumin and reduces degradation to increase the half-life of the peptide. Further, one of the skill would have a reasonable success in acylating the peptide GRP as taught by Levy et al using Acyl moiety taught by Lau et al because Lau teaches attaching acyl moiety to increase the half-life of GLP-1 peptide. Therefore, the instantly claimed invention would have been obvious to one ordinary skill in the art over the combined teachings of the prior art.
Conclusion
Claims 1-13 and 25 are rejected.
It is noted to applicants that the amino acid sequence of SEQ ID NO: 252 is free of prior art.
Claim 14 (to the extent reads on the amino acid sequence of SEQ ID NO: 252) is 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.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to GYAN CHANDRA whose telephone number is (571)272-2922. The examiner can normally be reached Mon-Friday 8:30AM-5:00P.
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/GYAN CHANDRA/Primary Examiner, Art Unit 1674
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