Patent Application 17771083 - Small Molecule Compound - Rejection

Patent Application 17771083 - Small Molecule Compound

Title: Small Molecule Compound

Application Information

• Invention Title: Small Molecule Compound
• Application Number: 17771083
• Submission Date: 2025-04-07T00:00:00.000Z
• Effective Filing Date: 2022-04-22T00:00:00.000Z
• Filing Date: 2022-04-22T00:00:00.000Z
• National Class: 514
• National Sub-Class: 210180
• Examiner Employee Number: 100014
• Art Unit: 1626
• Tech Center: 1600

Rejection Summary

• 102 Rejections: 1
• 103 Rejections: 0

Cited Patents

No patents were cited in this rejection.

Office Action Text

    guireDETAILED 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 1-10 are pending in the application. Claims 1-10 are rejected.
Priority
	This application is a 35 U.S.C. 371 National Stage Filing of International Application No. PCT/CN2020/120132, filed 10/10/2020, which claims priority under 35 U.S.C. 119(a)-(d) to CN 201911019837.X, filed 10/24/2019.  Receipt is acknowledged of papers submitted under 35 U.S.C. 119(a)-(d), which papers have been placed of record in the file.
Information Disclosure Statement
	The Examiner has considered the Information Disclosure Statement(s) filed on April 22, 2022.
Claim Objections
Claims 1 and 7-9 are objected to because of the following informalities:
Claim 1, line 3 should state “hydrate, solvate, metabolite, [[and]] or pharmaceutically acceptable salt or prodrug thereof.”
Claim 7, line 3 should state “the R1 is bonded to a nitrogen.”  
Claim 8, line 5 should state “heterocycloalkyl, [[and]] or substituted heterocycloalkyl.”
Claim 9, line 5 should state “substituted alkynyl, heterocycloalkyl, [[and]] or substituted heterocycloalkyl.”
Appropriate correction is required.
Claim Interpretation
	The Examiner has interpreted claim 6 as a product-by-process claim. According to MPEP 2113 I, the patentability of such claims must be determined by the structure: “‘[E]ven though product-by-process claims are limited by and defined by the process, determination of patentability is based on the product itself. The patentability of a product does not depend on its method of production. If the product in the product-by-process claim is the same as or obvious from a product of the prior art, the claim is unpatentable even though the prior product was made by a different process.’ In re Thorpe, 777 F.2d 695, 698, 227 USPQ 964, 966 (Fed. Cir. 1985).”
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 1-10 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 is drawn to a small molecule compound which is characterized by being a compound of structural formula 
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 wherein X1 and X2 are selected from carbon or nitrogen. Given the open language of the claim, i.e. “characterized by”, it is unclear what positions are open to substitution. A person having ordinary skill in the art would know that where X1 and/or X2 is carbon, there would need to be a bond to some other atom or group to fill the valency requirement for carbon(s) in the ring, but this atom/group is unspecified in the claim. The same general issue exists relative to positions that other appear to be defined, such as the -CH= groups in the heteroaromatic rings. MPEP 2111.03 states: “The transitional term "comprising", which is synonymous with "including," "containing," or "characterized by," is inclusive or open-ended and does not exclude additional, unrecited elements or method steps. See, e.g., Mars Inc. v. H.J. Heinz Co., 377 F.3d 1369, 1376, 71 USPQ2d 1837, 1843 (Fed. Cir. 2004)”. In this situation, it is unclear whether the defined positions are open to substitution or similarly whether the variables R1 and R2 are even relevant since the structures could be considered to be otherwise open-ended at any possible position. Thus, claim 1 is indefinite. 
Applicant may amend the claim to distinctly claim the subject matter which the inventor regards as the invention. It is suggested that Applicant amend the beginning of claim 1 as follows: “A small molecule compound
Dependent claims 2-10 are rejected as indefinite for the same reason since they do not correct the indefiniteness issue of their parent claims.
Claim 5 recites the limitation wherein “the end of the carbon chain of R11 is terminated by cyano.” However, it is unclear which carbon chain is being referenced since there is no singular option for said group. For instance, does this limitation apply to only the substituted alkyl or any possible option that might have a carbon chain such as a substituted aryl?
Applicant may amend the claim to distinctly claim the subject matter which the inventor regards as the invention. This rejection may be overcome, for example, by amending the claim to specify the carbon chain that should be terminated by a cyano group.
Claim 7 recites “the R1 is bonded to a nitrogen”. Claim 1, from which claim 7 depends, recites multiple possible instances of R1 and it is unclear if claim 7 is requiring that only R1 is present or that any multiple R1 substituents may be present so long as each is bound to nitrogen.
Applicant may amend the claim to distinctly claim the subject matter which the inventor regards as the invention. This rejection may be overcome, for example, by amending the claim to specify which R1 is bonded to nitrogen.
Claim 10 is drawn to a small molecule compound wherein the compound “is used for treating, preventing and relieving inflammatory skin diseases related to autoimmunity”. The claim appears to be a product claim, but the “is used” terminology suggests method claims are intended. As such, a skilled artisan would not be able to determine the metes and bounds of the invention in order to avoid infringement. Additionally, to the extent the claim recites a process of using, it is unclear how the process must be carried out because there are no active steps. For the purposes of applying prior art, claim 10 is interpreted as a product claim with an intended use. Therefore, the prior art need not teach the “use” so long as it teaches or suggests the same product.
Applicant may cancel the claim or amend the claim to distinctly claim the subject matter which the inventor regards as the invention. This rejection may be overcome, for example, by re-writing claim 10 as a proper product claim.
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.

Claims 6 and 10 are 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. 
Claim 6 recites small molecules obtained after the cyano group recited in claim 5 is no longer present due to the “hydrolysis, substitution, addition and reduction reactions of the cyano”. Thus, claim 6 does not properly depend from claim 5 since its scope does not include the limitations of claim 5.
Claim 10 does not properly depend on claim 1 (or any one of claims 2-9) because claim 1 requires that the G2 ring is a four-membered ring whereas claim 10 replaces the four membered ring with a 5 or 6 membered ring. Applicant may overcome the rejection by, for example, deleting the 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.
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.

Claim 10 is rejected under 35 U.S.C. 102(a)(1) and 102(a)(2) as being anticipated by Ellard et al. in WO 2012062704 A1 as cited in the IDS dated 04/22/2022.
	Ellard teaches pyridine compounds as TYK2 inhibitors, including compound 131 
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 in Table 7 on page 78. 
	Instant claim 10 is drawn to a compound of the formula 
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 as described in claim 1 and wherein the G2 ring is replaced by a five or six-membered carboatomic or nitrogen heterocyclic ring. Compound 131 from Ellard reads on the instant formula wherein X1 = C, X2 = N, G1 = phenyl, and G2 is the five membered nitrogen heterocycle pyrazole. In accordance with a broadest reasonable interpretation of the term “heterocycle,” a person having ordinary skill in the art would expect that heteroaromatic rings are included in the term, especially since the term “heterocycloalkyl” is used elsewhere in the application, which would exclude heteroaromatic rings (see claim 1, line 10; specification page 8, third paragraph; etc.) 
As discussed in section 112(b) of this Office Action, due to the indefiniteness of instant X1 as carbon as recited in claim 1, it is not clear what atoms or groups are present on the carbon. Accordingly, the broadest reasonable interpretation allows for a methyl substituent on the X1 position when X1 is carbon.
Thus, claim 10 is anticipated by the prior art.
Closest Prior Art
	Claims 1-9 are free of the prior art. The closest prior art is from Ellard et al. in WO 2012/062704 A1 as cited in the IDS dated 04/22/2022. 
Ellard teaches compounds of formula (I) that act as TYK2 inhibitors. See page 5, lines 6-13. While Ellard teaches compounds that nearly read on the instant formula of claim 1, 
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, such as compounds 131 
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 and 141 
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, there is no motivation in the art to modify either compound such that it is embraced by the instant formula. Where Ellard’s formula (I) 
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 falls short of anticipating or obviating the claimed invention is with respect to the R2 moiety. R2 would need to be a phenyl or 5 to 6 membered heteroaryl with an R18 substituent defined on page 7, lines 22-26 as 
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and T3 would need to be a 4-membered heterocycloalkyl which is defined on page 7, lines 32-33 as 
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 in order to read on the instant claims where G1 is a phenyl or 5 to 6 membered heteroaryl and G2 is a four-membered ring. While Ellard does teach many examples of compounds where R2 is a substituted phenyl, none of the compounds have a directly attached four-membered ring as the substituent. The closest compounds appear to be 131 and 141 referenced above, however there is no motivation for a person having ordinary skill in the art to modify the structures in such a way as to arrive at the instant compounds.
Additionally, there is no reasonable expectation of success for a PHOSITA to pursue these compounds as leads. On the contrary, these are among the weakest TYK2 and Jak2 inhibitors studied by Ellard et al., as shown on page 95 where the compounds are discussed as having between 0.1 uM and 1 uM IC50 activity against TYK2 and greater than 1 uM IC50 activity against Jak2.
Conclusion
Any inquiry concerning this communication or earlier communications from the examiner should be directed to Jalisa H. Ferguson whose telephone number is (703)756-1489. The examiner can normally be reached Monday - Friday 9:00am - 5:00pm.
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/J.H.F./Examiner, Art Unit 1626                                                                                                                                                                                                        
/MATTHEW P COUGHLIN/Primary Examiner, Art Unit 1626                                                                                                                                                                                                        
/JOSEPH K MCKANE/Supervisory Patent Examiner, Art Unit 1626