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 .
Priority
The instant application, filed 01/10/2023, is a 371 filing of PCT/IB2021/056157, filed 07/08/2021, which claims domestic priority to provisional U.S. application number to 63/051,977, filed 07/15/2020.
Status of the claims
The following amendments are acknowledged and entered.
Claims 2-5 and 7-9 are amended;
Claims 6, 10, and 12 are cancelled;
Claims 1-5, 7-9, 11, and 13 are pending and are under prosecution.
Information Disclosure Statement
The Information Disclosure Statement filed on 01/10/2023 and 02/23/2023 are acknowledged and found to be in compliance with the provisions of 37 CFR § 1.97. Accordingly, the information disclosure statements are considered.
Drawings
The drawings filed on 01/10/2023 are found to be in compliance with 37 CFR §§ 1.121 and 1.84, and are hereby accepted.
Claim Objections
Claims 2-5 are objected to for depending on a rejected claim (claim 1).
Claim Rejections - 35 U.S.C. § 103
The following is a quotation of pre-AIA 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.
Claim 1, 7-9, 11, and 13 are rejected under 35 U.S.C. § 103 as being unpatentable over Tatlock et al., (US 20170348313 A1, published), in view of Hamaed et al. (J Am Chem Soc, Volume 130, Issue 33, pg. 11056-11065, published July 26, 2008).
The instant claims are drawn to a crystalline polymorph of a monohydrochloride salt
Specifically, Tatlock teaches (15,25,3S,5R)-3-((6-(difluoromethyl)-5-fluoro-1,2,3,4-tetrahydroisoquinolin-8-yl)oxy)-5-(4-methyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclopentane-1,2-diol as compound ZZZ-16 (page 188) also known as CAS Registry Number: RN 2159123-14-3 [Database Registry Chemical Abstracts Service, Columbus, Ohio, Accession No. RN 2159123-14-3, Entered STN: 15 Dec 2017]. For the purposes of this office action, the compound is hereinafter referred to as Compound (I). Claim 1 of the disclosure by Tatlock teaches a compound of Formula (I)
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, which may be administered as crystalline or amorphous products (paragraph [0144]). Tatlock teaches a pharmaceutical composition comprising compound 1 and a pharmaceutically acceptable carrier (claim 14). Furthermore, the compound is taught specifically for the purposes of treating abnormal cell growth in mammals as a pharmaceutical composition of an anticancer agent paragraph ([0001]). Finally, Tatlock teaches a method of treating abnormal cell growth in a mammal comprising the administration of a therapeutically effective amount of the compound (claim 15).
Tatlock fails to teach a mono hydrochloride crystal polymorph of Compound (I).
The deficiencies of Tatlock are remedied by Hamaed, who teaches hydrochloride pharmaceutical salts of pharmaceuticals to create crystal polymorph. Specifically, Hamaed teaches wherein 50% of all pharmaceutical salts are hydrogen chloride pharmaceuticals, and that chlorine is present in final formulations of roughly 25% of drugs (pg. 11057). Hamaed teaches that the application of different polymorphs is of great importance in the pharmaceutical industry, because different polymorphs can have distinct physicochemical properties such as solubility, melting point, dissolution rate, density, hardness, and/or crystal morphology all of which can affect the bioavailability, handling, packaging, shelf life and/or patenting of a drug (page 11056).
Regarding claims 1, and 7, it is well-known in the prior art, and specifically taught by Hamaed, that monohydrochloride is a common binding partner for crystalline polymorphs. Thus, a person having ordinary skill in the art, prior to the effective filing date of the instant application, would have found it prima facie obvious to modify Compound (I), which is taught by Tatlock to be formulated in crystalline form, to create a hydrogen chloride (HCl) polymorph of compound I, as taught by Hamaed, in order to develop a more pharmaceutically bioavailable compound. MPEP 2143.
Regarding claims 8 and 9, wherein the claims are drawn to an intended use of compound I as a medicament, or the intended use for treating abnormal cell growth in a mammal, respectively, these are merely recitations of intended use of the composition. Where the prior art structure is capable of performing the presently claimed use, the prior art renders the instant claim obvious.
Regarding claim 11, Tatlock teaches that Compound (I) may be used in a method of treatment of abnormal cell growth in a mammal (claim 15).
Regarding claim 13, combining equivalents known for the same purpose is rendered obvious. According to MPEP § 2144.06:
It is prima facie obvious to combine two compositions each of which is taught by the prior art to be useful for the same purpose, in order to form a third composition to be used for the very same purpose.... [T]he idea of combining them flows logically from their having been individually taught in the prior art." In re Kerkhoven, 626 F.2d 846, 850, 205 USPQ 1069, 1072 (CCPA 1980) (Claims to a process of preparing a spray-dried detergent by mixing together two conventional spray-dried detergents were held to be prima facie obvious.).
Compound (I) is known in the art to treat abnormal cell growth (Tatlock). Therefore, it would have been prima facie obvious to combine Compound (I) and another known anticancer agent in order to treat cancer and abnormal cell growth.
Double Patenting
The nonstatutory double patenting rejection is based on a judicially created doctrine grounded in public policy (a policy reflected in the statute) so as to prevent the unjustified or improper timewise extension of the “right to exclude” granted by a patent and to prevent possible harassment by multiple assignees. A nonstatutory double patenting rejection is appropriate where the conflicting claims are not identical, but at least one examined application claim is not patentably distinct from the reference claim(s) because the examined application claim is either anticipated by, or would have been obvious over, the reference claim(s). See, e.g., In re Berg, 140 F.3d 1428, 46 USPQ2d 1226 (Fed. Cir. 1998); In re Goodman, 11 F.3d 1046, 29 USPQ2d 2010 (Fed. Cir. 1993); In re Longi, 759 F.2d 887, 225 USPQ 645 (Fed. Cir. 1985); In re Van Ornum, 686 F.2d 937, 214 USPQ 761 (CCPA 1982); In re Vogel, 422 F.2d 438, 164 USPQ 619 (CCPA 1970); In re Thorington, 418 F.2d 528, 163 USPQ 644 (CCPA 1969).
A timely filed terminal disclaimer in compliance with 37 CFR 1.321(c) or 1.321(d) may be used to overcome an actual or provisional rejection based on nonstatutory double patenting provided the reference application or patent either is shown to be commonly owned with the examined application, or claims an invention made as a result of activities undertaken within the scope of a joint research agreement. See MPEP § 717.02 for applications subject to examination under the first inventor to file provisions of the AIA as explained in MPEP § 2159. See MPEP § 2146 et seq. for applications not subject to examination under the first inventor to file provisions of the AIA . A terminal disclaimer must be signed in compliance with 37 CFR 1.321(b).
The filing of a terminal disclaimer by itself is not a complete reply to a nonstatutory double patenting (NSDP) rejection. A complete reply requires that the terminal disclaimer be accompanied by a reply requesting reconsideration of the prior Office action. Even where the NSDP rejection is provisional the reply must be complete. See MPEP § 804, subsection I.B.1. For a reply to a non-final Office action, see 37 CFR 1.111(a). For a reply to final Office action, see 37 CFR 1.113(c). A request for reconsideration while not provided for in 37 CFR 1.113(c) may be filed after final for consideration. See MPEP §§ 706.07(e) and 714.13.
The USPTO Internet website contains terminal disclaimer forms which may be used. Please visit www.uspto.gov/patent/patents-forms. The actual filing date of the application in which the form is filed determines what form (e.g., PTO/SB/25, PTO/SB/26, PTO/AIA /25, or PTO/AIA /26) should be used. A web-based eTerminal Disclaimer may be filled out completely online using web-screens. An eTerminal Disclaimer that meets all requirements is auto-processed and approved immediately upon submission. For more information about eTerminal Disclaimers, refer to www.uspto.gov/patents/apply/applying-online/eterminal-disclaimer.
Claims 1, 7-9, 11, and 13 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1, 21, 26, and 28 of copending Application No. 18/004,943, (U.S.P.G.Pub. 2024/0116937 A1) in view of Hamaed. Although the claims at issue are not identical, they are not patentably distinct from each other because both the instant application and the copending application teach crystalline Compound (I) as a pharmaceutical composition, in a method of treating abnormal cell growth, and in combination with an anticancer agent. Although the copending application does not teach a monohydrochloride salt, Hamaed teaches wherein 50% of all pharmaceutical salts are hydrogen chloride pharmaceuticals, and that chlorine is present in final formulations of roughly 25% of drugs (pg. 11057). Hamaed teaches that the application of different polymorphs is of great importance in the pharmaceutical industry, because different polymorphs can have distinct physicochemical properties such as solubility, melting point, dissolution rate, density, hardness, and/or crystal morphology all of which can affect the bioavailability, handling, packaging, shelf life and/or patenting of a drug (page 11056).
According to Hamaed, it well-known in the art that monohydrochloride is a common binding partner for crystalline polymorphs (pg. 11057). Thus, a person of ordinary skill in the art prior to the effective filing date of the instantly claimed would have found it obvious to modify the crystalline form of Compound (I) of 18/004,943, known to be effective in treating abnormal cell growth disclosed by the copending application, to create a hydrogen chloride polymorph of said compound, following the teachings of Hamaed, in order to develop a more pharmaceutically bioavailable compound.
This is a provisional nonstatutory double patenting rejection because the patentably indistinct claims have not in fact been patented. If a notice of allowance is issued in the co-pending application 17/424,721 and 18/004,943, upon issue of the patent, the provisionary NSDP rejection over the co-pending application will convert to a NSDP rejection over the published patent.
Claims 1, 7-9, and 13 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-15 of U.S. Patent No. US 10,709,709 B2 in view of Hamaed (see earlier citation). Although the claims at issue are not identical, they are not patentably distinct from each other because both the instant application and the copending application teach crystalline Compound (I) as a pharmaceutical composition. Furthermore, the patent document teaches hydrochloride salt (see claims 10 and 14), Hamaed teaches wherein 50% of all pharmaceutical salts are hydrogen chloride pharmaceuticals, and that chlorine is present in final formulations of roughly 25% of drugs (pg. 11057). Hamaed teaches that the application of different polymorphs is of great importance in the pharmaceutical industry, because different polymorphs can have distinct physicochemical properties such as solubility, melting point, dissolution rate, density, hardness, and/or crystal morphology all of which can affect the bioavailability, handling, packaging, shelf life and/or patenting of a drug (page 11056).
With respect to co-crystal salts to form a polymorph, phosphate, hydrogen phosphate, and dihydrogen phosphate of claims 16 and 17 of the patent document, these salts are known to be equivalents to monohydrochloride of the instant application, used for a common purpose—namely the creation of crystal polymorphs. According to MPEP § 2144.06 (II), art-recognized equivalents substituted for the same purpose are rendered obvious. The courts have stated:
In order to rely on equivalence as a rationale supporting an obviousness rejection, the equivalency must be recognized in the prior art, and cannot be based on applicant’s disclosure or the mere fact that the components at issue are functional or mechanical equivalents. In re Ruff, 256 F.2d 590, 118 USPQ 340 (CCPA 1958) (The mere fact that components are claimed as members of a Markush group cannot be relied upon to establish the equivalency of these components. However, an applicant’s expressed recognition of an art-recognized or obvious equivalent may be used to refute an argument that such equivalency does not exist.); Smith v. Hayashi, 209 USPQ 754 (Bd. of Pat. Inter. 1980) (The mere fact that phthalocyanine and selenium function as equivalent photoconductors in the claimed environment was not sufficient to establish that one would have been obvious over the other. However, there was evidence that both phthalocyanine and selenium were known photoconductors in the art of electrophotography. "This, in our view, presents strong evidence of obviousness in substituting one for the other in an electrophotographic environment as a photoconductor." 209 USPQ at 759.). An express suggestion to substitute one equivalent component or process for another is not necessary to render such substitution obvious. In re Fout, 675 F.2d 297, 213 USPQ 532 (CCPA 1982).
Therefore it would have been prima facie obvious to a person having ordinary skill in the art to substitute phosphate, hydrogen phosphate, and dihydrogen phosphate from claims 16 and 17 of the patented document for monohydrochloride, as the salts are both recognized in the prior art as being used for the purposes of crystal polymorph creation, to arrive at the instantly claimed crystal polymorph. See MPEP 2144.06.
Conclusion
No claim is allowed.
Correspondence
Any inquiry concerning this communication or earlier communications from the examiner should be directed to Sophia P. Hirakis whose telephone number is +1 (571) 272-0118. The examiner can normally be reached within the hours of 5:00 am to 5:00pm EST, Monday-Friday.
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/SOPHIA P HIRAKIS/Examiner, Art Unit 1623
/ADAM C MILLIGAN/Supervisory Patent Examiner, Art Unit 1623