DETAILED ACTION
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 1-20 are pending. Examiner previously required a restriction (dated October 24, 2025). In response, Applicant elected, without traverse, Group I which encompasses claims 1-13, 19, and 20. Accordingly, claims 14-18 are withdrawn.
Status of Priority
The present application claims priority to U.S. Provisional Application No. 63/356,670, filed on June 29, 2022.
Election/Restrictions
As a reminder, Applicant elected, without traverse, Group I which corresponds to claims 1-13, 19, and 20. Applicant also elected the following species, without traverse:
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and indicated claims 1, 2, 5-13, 19, and 20 read on said species. The elected species was not found in the prior art and, thus, the search was expanded.
Specification - Abstract
Applicant is reminded of the proper content of an abstract of the disclosure.
In chemical patent abstracts for compounds or compositions, the general nature of the compound or composition should be given as well as its use, e.g., “The compounds are of the class of alkyl benzene sulfonyl ureas, useful as oral anti-diabetics.” Exemplification of a species could be illustrative of members of the class. For processes, the type of reaction, reagents and process conditions should be stated, generally illustrated by a single example unless variations are necessary.
Applicant is reminded of the proper language and format for an abstract of the disclosure.
The abstract should be in narrative form and generally limited to a single paragraph on a separate sheet within the range of 50 to 150 words in length. The abstract should describe the disclosure sufficiently to assist readers in deciding whether there is a need for consulting the full patent text for details.
The language should be clear and concise and should not repeat information given in the title. It should avoid using phrases which can be implied, such as, “The disclosure concerns,” “The disclosure defined by this invention,” “The disclosure describes,” etc. In addition, the form and legal phraseology often used in patent claims, such as “means” and “said,” should be avoided.
Specification - Disclosure
The specification has not been checked to the extent necessary to determine the presence of all possible minor errors. Applicant’s cooperation is requested in correcting any errors of which applicant may become aware in the specification.
Claim Objections
Claims 1 and 19 are objected to because of the following informalities:
In claim 1, to ensure proper valency amongst substituents:
“R3 is… C2-15 heterocyclyl, each of which may be substituted with 1, 2, 3, or 4 groups selected, independently, from halogen, O, …” should read“R3 is… C2-15 heterocyclyl, each of which may be substituted with 1, 2, 3, or 4 groups selected, independently, from halogen, =O, …”
In claim 19, for consistency:
“R2 is… C3-4 heteroaryl substituted with C1-3 alkyl…” should read“R2 is… C3-4 heteroaryl substituted with 1 or 2 groups selected, independently, from C1-3 alkyl…”
Appropriate correction is required.
Claim 12 is objected to under 37 CFR 1.75 as being a substantial duplicate of claim 1. See “Claim Rejections - 35 USC § 112(d)” section below for an explanation. When two claims in an application are duplicates or else are so close in content that they both cover the same thing, despite a slight difference in wording, it is proper after allowing one claim to object to the other as being a substantial duplicate of the allowed claim. See MPEP § 608.01(m).
Claim Rejections – Improper Markush Grouping
Claims 1, 2, 6-9, 11-13, and 20 are rejected on the judicially-created basis that it contains an improper Markush grouping of alternatives. See In re Harnisch, 631 F.2d 716, 721-22 (CCPA 1980) and Ex parte Hozumi, 3 USPQ2d 1059, 1060 (Bd. Pat. App. & Int. 1984). The improper Markush grouping includes species of the claimed invention that do not share both a substantial structural feature and a common use that flows from the substantial structural feature.
A Markush claim contains an “improper Markush grouping” if: (1) the species of the Markush group do not share a single structural similarity,” or (2) the species do not share a common use. Members of a Markush group share a "single structural similarity” when they belong to the same recognized physical or chemical class or to the same art-recognized class. Members of a Markush group share a common use when they are disclosed in the Specification or known in the art to be functionally equivalent (see Federal Register, Vol. 76, No. 27, Wednesday, February 9, 2011, p. 7166, left and middle columns, bridging paragraph).
The members of the improper Markush grouping do not share a substantial feature and/or a common use that flows from the substantial structural feature for the following reasons:
Depicted below are the two different core structures found in the formulas disclosed in instant claim 1:
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and
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Although both core structures comprise a pyrimidine moiety, the overall core structures are materially different. One alternative comprises a monocyclic, pyrimidine scaffold (i.e., planar), while the other comprises a fused bicyclic system in which the pyrimidine ring is fused to a cyclopentane ring, resulting in an overall non-planar scaffold. Since molecular geometry directly influences chemical and biological properties, the two core structures cannot reasonably be regarded as sharing a single substantial structural feature. Thus, the structural differences between the planar monocyclic pyrimidine and the non-planar fused bicyclic system represent distinct core structures rather than mere core variations.
In response to this rejection, Applicant should either amend the claim(s) to recite only individual species or grouping of species that share a substantial structural feature as well as a common use that flows from the substantial structural feature, or present a sufficient showing that the species recited in the alternative of the claims(s) in fact share a substantial structural feature as well as a common use that flows from the substantial structural feature. This is a rejection on the merits and may be appealed to the Board of Patent Appeals and Interferences in accordance with 35 U.S.C. § 134 and 37 CFR41.31 (a) (1) (emphasis provided).
Claims 2, 6-9, 11-13, and 20, which are dependent on claim 1, are also rejected for further requiring and/or reciting the improper Markush grouping of claim 1.
Claim Rejections - 35 USC § 112(a) – Scope of Enablement
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 1-4, 6-9, 11-13, and 20 are rejected under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, because the specification, while being enabling for:
A compound, having a formula:
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when the compound is represented by
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:
R1, R2, R3, R4, and R5 are as listed in instant claim 1
when the compound is represented by
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or
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:
R2 = C3 heteroaryl wherein:
the heteroaryl comprises two heteroatoms selected from N and S and
the heteroaryl may be substituted with one group wherein the group is a C1-6 alkyl
R3 = C4-8 heterocyclyl (that is not a heteroaryl) wherein:
the heterocyclyl comprises at least one N atom as the heteroatom
the heterocyclyl can be substituted with one group selected from halogen, O-(C1-6 alkyl), or C1-6 alkyl
R4 = CH2CN
R5 = H
does not reasonably provide enablement for elements that are outside the scope of the enabling elements listed above. The specification does not enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the invention commensurate in scope with these claims.
As stated in the MPEP 2164.01(a), “There are many factors to be considered when determining whether there is sufficient evidence to support a determination that a disclosure does not satisfy the enablement requirement and whether any necessary experimentation is “undue.”
In evaluating the enablement question, several factors are to be considered. According to In re Wands, 8 USPQ2d 1400 (Fed. Cir. 1988), these factors include:
1) The nature of the invention,
2) the state of the prior art,
3) the predictability or lack thereof in the art,
4) the amount of direction or guidance present,
5) the presence or absence of working examples,
6) the breadth of the claims, and
7) the quantity of experimentation needed to make and use the invention based on the content of the disclosure, and
8) the level of the skill in the art.
In the instant case, the Wands factors are relevant for the following reasons:
The nature of the invention
The nature of the invention claims a compound represented by the following general formulas:
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useful as inhibitors of Janus kinase (JAK) proteins. The variables of the above formulas are defined in instant claim 1.
State of the prior art
See “Claim Rejections - 35 USC § 102” and “Claim Rejections - 35 USC § 103” sections below.
The predictability or lack thereof in the art
As stated in the “Claim Rejections - 35 USC § 103” section below, there is prior art that discloses compounds that are structurally similar to certain embodiments of the presently claimed compounds (see Ellis; WO 2023/279105 A1). In particular, some of the claimed compounds differ from the prior art compounds only in that they are position isomers (i.e., the same substituents are bonded to different carbon atoms on the same core structure). Given the close structural similarity between such position isomers and the prior art compounds, there is a degree of predictability in the art with respect to their preparation and their JAK inhibitory activity.
Also stated in the “Claim Rejections - 35 USC § 103” section below, the instant specification does not provide any in vitro or in vivo data demonstrating that the claimed compounds exhibit properties that are unexpected relative to the structurally similar position isomers disclosed in Ellis. The instant specification only provides a general reaction scheme (see instant Figure 1) and a general procedure for how to conduct ROCK and JAK assays (see instant Example 1). In the absence of evidence indicating unpredictability or a demonstrated difference in activity, it is reasonable to presume that the claimed compounds would be expected to exhibit properties similar to their corresponding position isomers disclosed in Ellis.
However, the instant claims are not limited to position isomers of the prior art compounds. The instant claims also encompass compounds that possess a similar but structurally distinct core framework (i.e., see the first two formulas listed in instant claim 1; herein, will refer to the formulas as claim-1-formula-1 and claim-1-formula-2, respectively). With respect to compounds having a core structure represented by claim-1-formula-1 and claim-1-formula-2, there is a lack of predictability in the prior art.
The presence or absence of working examples
The prior art (i.e., Ellis), does not provide working examples demonstrating that compounds having these two distinct core structures (i.e., claim-1-formula-1 and claim-1-formula-2) can inhibit JAK. As stated above, the instant specification does not provide any in vitro or in vivo data demonstrating that compounds having a structure represented by claim-1-formula-1 and claim-1-formula-2 can inhibit JAK.
The amount of direction or guidance present and the quantity of experimentation needed to make and use the invention based on the content of the disclosure
The prior art also does not provide sufficient guidance identifying which specific substituent combinations are necessary to achieve JAK inhibition activity. In the absence of such guidance, a person of ordinary skill in the art would be required to synthesize and screen a substantial number of structurally diverse compounds in order to identify operative JAK inhibitors that have a core structure represented by claim-1-formula-1 or claim-1-formula-2.
The level of the skill in the art
The level of ordinary skill in the art is relatively high. A person of ordinary skill would typically have formal training in medicinal chemistry and organic synthesis and would be familiar with standard methods for evaluating therapeutic efficacy of compounds.
The breadth of the claims
The claims are broad insofar as the instant claims recite a compound represented by one of any of the three formulas recited in instant claim 1 wherein the compound can possess a structurally diverse range of chemical groups.
Claims 2-4, 6-9, 11-13, and 20, which are dependent on claim 1, are also rejected for further requiring and/or reciting the non-enabling elements listed above.
Claim Rejections - 35 USC § 112(b)
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 1, 4-7, 11-13, and 20 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.
Claim 1 recites “or R3 and R4, together with the atoms to which they are attached, combine to form… CC(H)-(C0-6 alkylene)CN…”
Examiner understands how R3 and R4 in the following formula:
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can be combined with the atoms to which they are attached to form CC(H)-(C0-6 alkylene)CN.
Examiner does not understand how R3 and R4 in the following formulas:
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can be combined with the atoms to which they are attached to form CC(H)-(C0-6 alkylene)CN since now there are two ring atoms that would also have to be combined.
For clarity, claim 1 can be amended to recite the following:
“…or R3 and R4, together with the atoms to which they are attached, combine to form C3-7 cycloalkyl, C2-8 heterocycloalkyl, C3-7 cycloalkyl substituted with 1 or 2 groups selected, independently, from halogen or (C1-6 alkylene)CN, or C2-8 heterocycloalkyl substituted with 1 or 2 groups selected, independently, from halogen or (C1-6 alkylene)CN;or when R3 and R4 are bonded to the same carbon, R3 and R4, together with the atoms to which they are attached, combine to form CC(H)-(C0-6 alkylene)CN.”
Claim 11 recites the limitation:
“R2 is…
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…
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…
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…
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…
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…
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” Claim 11 is dependent on claim 1 which does not state that R2 can be a C6-16 aryl that is substituted with at least a heterocyclyl (wherein the heterocyclyl can be further substituted with an OH group) and/or a haloalkyl. Thus, there is insufficient antecedent basis for this limitation in the claim.
Claim 11 further recites the limitation:
“R3 is…
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…” Claim 11 is dependent on claim 1 which does not recite that R3 can be a -NH2 or -NH(C1-6 alkyl) group that is substituted with one C3 heterocyclyl, wherein the heterocyclyl is substituted with a C1-3 alkyl. Thus, there is insufficient antecedent basis for this limitation in the claim.
Claim 11 further recites the limitation:
“R3 is…
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…
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…” Claim 11 is dependent on claim 1 which does not recite that R3 can be a C2-15 heterocyclyl group that is substituted with a cyclopropyl group, wherein the cyclopropyl can be further substituted with one or two halogens. Thus, there is insufficient antecedent basis for this limitation in the claim.
Claim 11 further recites the limitation:
“R3 is…
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…” Claim 11 is dependent on claim 1 which recites that R3 can be a C2-15 heterocyclyl that is substituted with a (C1-6 alkylene)-(C6-10 haloaryl). However, claim 1 does not recite that the (C1-6 alkylene)-(C6-10 haloaryl) substituent can be further substituted with an alkyl group. Thus, there is insufficient antecedent basis for this limitation in the claim.
Claim 11 further recites the limitation:
“R3 is…
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…” Claim 11 is dependent on claim 1 which does not recite:1) that R3 can be a C1 alkyl substituted with a heterocyclyl group, wherein the heterocyclyl group is further substituted with a halogen or
2) that R3 can be a (C1 alkylene)-(heterocyclyl) that is substituted with a halogen.
Claims 4-7, 11-13, and 20 which are dependent on claim 1, are also rejected for further requiring and/or reciting the indefinite limitation of claim 1.
Claim Rejections - 35 USC § 112(d)
The following is a quotation of 35 U.S.C. 112(d):
(d) REFERENCE IN DEPENDENT FORMS.—Subject to subsection (e), a claim in dependent form shall contain a reference to a claim previously set forth and then specify a further limitation of the subject matter claimed. A claim in dependent form shall be construed to incorporate by reference all the limitations of the claim to which it refers.
The following is a quotation of pre-AIA 35 U.S.C. 112, fourth paragraph:
Subject to the following paragraph [i.e., the fifth paragraph of pre-AIA 35 U.S.C. 112], a claim in dependent form shall contain a reference to a claim previously set forth and then specify a further limitation of the subject matter claimed. A claim in dependent form shall be construed to incorporate by reference all the limitations of the claim to which it refers.
Claim 12 is rejected under 35 U.S.C. 112(d) or pre-AIA 35 U.S.C. 112, 4th paragraph, as being of improper dependent form for failing to further limit the subject matter of the claim upon which it depends, or for failing to include all the limitations of the claim upon which it depends.
Instant claim 12 is directed towards a composition comprising the compound according to claim 1 with no additional components specified. The claim language of claim 12 suggests that the composition can be made up of 100% of the compound of claim 1. Hence, claim 12 is not further limiting the subject matter of the claim upon which it depends and is, in fact, a duplicate of the independent claim.
Applicant may cancel the claim(s), amend the claim(s) to place the claim(s) in proper dependent form, rewrite the claim(s) in independent form, or present a sufficient showing that the dependent claim(s) complies with the statutory requirements.
Note on 35 USC § 102 and § 103 Rejections
In the event the determination of the status of the application as subject to AIA 35 U.S.C. 102 and 103 (or as subject to pre-AIA 35 U.S.C. 102 and 103) is incorrect, any correction of the statutory basis (i.e., changing from AIA to pre-AIA ) for the rejection will not be considered a new ground of rejection if the prior art relied upon, and the rationale supporting the rejection, would be the same under either status.
Claim Rejections - 35 USC § 102
The following is a quotation of the appropriate paragraphs of 35 U.S.C. 102 that form the basis for the rejections under this section made in this Office action:
A person shall be entitled to a patent unless –
(a)(1) the claimed invention was patented, described in a printed publication, or in public use, on sale, or otherwise available to the public before the effective filing date of the claimed invention.
(a)(2) the claimed invention was described in a patent issued under section 151, or in an application for patent published or deemed published under section 122(b), in which the patent or application, as the case may be, names another inventor and was effectively filed before the effective filing date of the claimed invention.
Rejection Part 1:
Claims 1, 5, 12, 13, and 20 are rejected under 35 U.S.C. 102(a)(1) as being anticipated by:
Cai et al. (Cai) (WO 2009/152325 A1; published December 17, 2009)
Cai discloses diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators (abstract). One of the compounds disclosed by Cai is compound 93 which has the following structure (herein, referred to as compound-93-Cai):
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(see pg. 80, starting on line 6). Compound-93-Cai is encompassed by instant claims 1 and 5 wherein:
R1 = R4 = R5 = H
R2 = unsubstituted C4 heterocyclyl (i.e., tetrahydrofuranyl)
R3 = NH2
Further, in order to take the 1H NMR of compound-93-Cai dissolved in CDCl3, the solution must be placed in an NMR tube (i.e., a container; reads on instant claim 20).
According to Cai, “[f]or competition binding studies, cell membranes [i.e., prepared by homogenizing cell pellets in EDTA buffer] were incubated with 2x KD (10 nM), [3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25 °C” (pg. 216, lines 2-9).
In other words, Cai discloses a composition comprising water (a common pharmaceutically acceptable carrier that is present in EDTA buffer) and compound-93-Cai (i.e., a compound encompassed by instant claim 1). Hence, Cai also anticipates instant claims 12 and 13).
Note:
According to the instant specification, “pharmaceutically acceptable carrier” includes excipients (see para. 0026).
The Baldrick reference (i.e., Baldrick, P. Regulatory Toxicology and Pharmacology 2000, 32, 210-218.; pg. 210, right col., middle of 1st paragraph, sentence starts with “Indeed, the 12 most common excipients…”) teaches water as one of the 12 most common pharmaceutically acceptable excipients.
Rejection Part 2:
Claims 1, 5-7, 11-13, and 20 are rejected under 35 U.S.C. 102(a)(2) as being anticipated by
Ellis et al. (Ellis) (WO 2023/279105 A1; filed on July 1, 2022; published January 5, 2023; claims priority to U.S. Provisional Application No. 63/217,607, filed on July 1, 2021 – Effective filing date of prior art is July 1, 2021).
Ellis discloses compounds that are useful as inhibitors of kinases, including JAK proteins (para. 0009). One of the compounds disclosed by Ellis has the following structure (herein, referred to as compound E7; pg. 26):
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. Ellis demonstrates that compound E7 can inhibit JAK2 with an IC50 of less than 50 nM (pg. 26, Table 1, 2nd row). Compound E7 is encompassed by instant claims 1, 5-7, and 11 wherein:
R1 = C1 alkyl (i.e., CH3)
R2 = C3 heterocyclyl (i.e., isothiazolyl) substituted with one C1 alkyl group
R3 = CN
R4 = R5 = H
In order to synthesize E7, a container must be used to hold all reactants and, subsequently, to hold compound E7 as it is being formed. In other words, Ellis anticipates instant claim 20 which is directed to a compound of instant claim 1, in a container.
Ellis also discloses a topical ocular pharmaceutical composition with the following formulation (See Example 3, Table 29):
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wherein “azetidine” is any of the compounds disclosed in Ellis, including E7. Thus, Ellis anticipates instant claims 12 and 13.
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.
Claims 1, 2, 5-13, 19, and 20 are rejected under 35 U.S.C. 103 as being unpatentable over:
Ellis et al. (Ellis) (WO 2023/279105 A1; filed on July 1, 2022; published January 5, 2023; claims priority to U.S. Provisional Application No. 63/217,607, filed on July 1, 2021 – Effective filing date of prior art is July 1, 2021).
Ellis discloses compounds that are useful as inhibitors of kinases, including JAK proteins (para. 0009). One of the compounds disclosed by Ellis has the following structure (herein, referred to as compound E111a; see pg. 95):
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. Ellis demonstrates that compound E111a can inhibit TYK2 and JAK1 with an IC50 of less than 10 nM for both. The structure of compound E111a is very similar to the structure of the species elected by Applicant (i.e., the first compound listed in instant claim 10):
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. The main difference between the two structures is that the -CH2CN group in compound E111a is geminal to the heterocyclic group whereas in the instantly elected species, the -CH2CN group is bonded to the carbon atom that is adjacent to the carbon atom that is bonded to the same heterocyclic group.
Compound E111a and the instantly elected species are position isomers of each other.
According to MPEP 2144.09:
I. REJECTION BASED ON CLOSE STRUCTURAL SIMILARITY IS FOUNDED ON THE EXPECTATION THAT COMPOUNDS SIMILAR IN STRUCTURE WILL HAVE SIMILAR PROPERTIES
A prima facie case of obviousness may be made when chemical compounds have very close structural similarities and similar utilities. "An obviousness rejection based on similarity in chemical structure and function entails the motivation of one skilled in the art to make a claimed compound, in the expectation that compounds similar in structure will have similar properties." In re Payne, 606 F.2d 303, 313, 203 USPQ 245, 254 (CCPA 1979). See In re Papesch, 315 F.2d 381, 137 USPQ 43 (CCPA 1963) (discussed in more detail below) and In re Dillon, 919 F.2d 688, 16 USPQ2d 1897 (Fed. Cir. 1990) (discussed below and in MPEP § 2144) for an extensive review of the case law pertaining to obviousness based on close structural similarity of chemical compounds. See also MPEP § 2144.08, subsection II.A.4.(c).
II. HOMOLOGY AND ISOMERISM ARE FACTS WHICH MUST BE CONSIDERED WITH ALL OTHER RELEVANT FACTS IN DETERMINING OBVIOUSNESS
Compounds which are position isomers (compounds having the same radicals in physically different positions on the same nucleus) or homologs (compounds differing regularly by the successive addition of the same chemical group, e.g., by -CH2- groups) are generally of sufficiently close structural similarity that there is a presumed expectation that such compounds possess similar properties. In re Wilder, 563 F.2d 457, 195 USPQ 426 (CCPA 1977). See also In re May, 574 F.2d 1082, 197 USPQ 601 (CCPA 1978) (stereoisomers prima facie obvious); Aventis Pharma Deutschland v. Lupin Ltd., 499 F.3d 1293, 84 USPQ2d 1197 (Fed. Cir. 2007) (5(S) stereoisomer of ramipril obvious over prior art mixture of stereoisomers of ramipril.).
The instant specification does not provide any in vitro or in vivo data demonstrating that the claimed compounds exhibit properties that are unexpected relative to the structurally similar position isomers disclosed in Ellis. The instant specification only provides a general reaction scheme (see instant Figure 1) and a general procedure for how to conduct ROCK and JAK assays (see instant Example 1). In the absence of evidence indicating unpredictability or a demonstrated difference in activity, it is reasonable to presume that the claimed compounds would be expected to exhibit properties similar to their corresponding position isomers disclosed in Ellis, thus motivating a POSITA to explore such position isomers as disclosed in the instant case. Hence, instant claims 1, 2, 5-11, and 19 are considered obvious.
Ellis also discloses a topical ocular pharmaceutical composition with the following formulation (See Example 3, Table 29):
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wherein “azetidine” is any of the compounds disclosed in Ellis, including E111a. As stated above, since the instantly elected species is presumed to have properties similar to E111a, one or ordinary skill in the art would have found it prima facie obvious before the effective filing date of the instantly claimed invention to modify the pharmaceutical composition disclosed in Ellis by replacing the azetidine compound with any one of the instantly claimed compounds (that are position isomers of the compounds disclosed in Ellis) and to then store the pharmaceutical composition in a container for ease of transport. Hence, instant claims 12, 13, and 20 are also considered obvious.
Double Patenting
The nonstatutory double patenting rejection is based on a judicially created doctrine grounded in public policy (a policy reflected in the statute) so as to prevent the unjustified or improper timewise extension of the “right to exclude” granted by a patent and to prevent possible harassment by multiple assignees. A nonstatutory double patenting rejection is appropriate where the conflicting claims are not identical, but at least one examined application claim is not patentably distinct from the reference claim(s) because the examined application claim is either anticipated by, or would have been obvious over, the reference claim(s). See, e.g., In re Berg, 140 F.3d 1428, 46 USPQ2d 1226 (Fed. Cir. 1998); In re Goodman, 11 F.3d 1046, 29 USPQ2d 2010 (Fed. Cir. 1993); In re Longi, 759 F.2d 887, 225 USPQ 645 (Fed. Cir. 1985); In re Van Ornum, 686 F.2d 937, 214 USPQ 761 (CCPA 1982); In re Vogel, 422 F.2d 438, 164 USPQ 619 (CCPA 1970); In re Thorington, 418 F.2d 528, 163 USPQ 644 (CCPA 1969).
A timely filed terminal disclaimer in compliance with 37 CFR 1.321(c) or 1.321(d) may be used to overcome an actual or provisional rejection based on nonstatutory double patenting provided the reference application or patent either is shown to be commonly owned with the examined application, or claims an invention made as a result of activities undertaken within the scope of a joint research agreement. See MPEP § 717.02 for applications subject to examination under the first inventor to file provisions of the AIA as explained in MPEP § 2159. See MPEP § 2146 et seq. for applications not subject to examination under the first inventor to file provisions of the AIA . A terminal disclaimer must be signed in compliance with 37 CFR 1.321(b).
The filing of a terminal disclaimer by itself is not a complete reply to a nonstatutory double patenting (NSDP) rejection. A complete reply requires that the terminal disclaimer be accompanied by a reply requesting reconsideration of the prior Office action. Even where the NSDP rejection is provisional the reply must be complete. See MPEP § 804, subsection I.B.1. For a reply to a non-final Office action, see 37 CFR 1.111(a). For a reply to final Office action, see 37 CFR 1.113(c). A request for reconsideration while not provided for in 37 CFR 1.113(c) may be filed after final for consideration. See MPEP §§ 706.07(e) and 714.13.
The USPTO Internet website contains terminal disclaimer forms which may be used. Please visit www.uspto.gov/patent/patents-forms. The actual filing date of the application in which the form is filed determines what form (e.g., PTO/SB/25, PTO/SB/26, PTO/AIA /25, or PTO/AIA /26) should be used. A web-based eTerminal Disclaimer may be filled out completely online using web-screens. An eTerminal Disclaimer that meets all requirements is auto-processed and approved immediately upon submission. For more information about eTerminal Disclaimers, refer to www.uspto.gov/patents/apply/applying-online/eterminal-disclaimer.
Claims 1, 2, 5-13, 19, and 20 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over:
claims 1-4, 7-13, 28-36 of U.S. Patent Application No. 18/573,305 (‘305)
Although the claims at issue are not identical, they are not patentably distinct from each other because there is:
overlap between the instant claims and the claim set from the co-pending application (see “Claim Rejections - 35 USC § 102 – Rejection Part 2” section for an example of a compound encompassed by both claim sets) and
the compounds claimed in the co-pending application are obvious homologs of the compounds claimed in the present application (see “Claim Rejections - 35 USC § 103” section for details).
Conclusion
No claims are allowed. Any inquiry concerning this communication or earlier communications from the examiner should be directed to KRISTEN ROMERO whose telephone number is (571)272-6478. The examiner can normally be reached M-F 9:30 AM - 6:00 PM ET.
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/KRISTEN W ROMERO/Examiner, Art Unit 1624
/JEFFREY H MURRAY/Supervisory Patent Examiner, Art Unit 1624