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 .
DETAILED ACTION
Status of 18/705,952
Claims 1-15 are currently pending.
Priority
Instant application 18/705,952, filed 4/29/2024, claims priority as follows:
PNG
media_image1.png
94
390
media_image1.png
Greyscale
The priority documents submitted in the file wrapper are not translated to English and as a result, priority cannot be established. Thus, the instant claims are granted the effective filing date of 10/28/2022.
Information Disclosure Statement
All references from the IDS submitted on 4/29/2024 have been considered unless marked with a strikethrough.
Objection to the Abstract
The abstract of the disclosure is objected to for insufficient length, as it is less than 50 words. The abstract should generally be within the range of 50 to 150 words in length, and chemical abstracts in particular should provide the structure of the compound of a formula thereof in addition to methods of use. See MPEP § 608.01. Appropriate correction is required.
Election/Restriction
Applicant’s election of Group I, claims 1-13, drawn to compounds and compositions of Chemical Formula 1, without traverse, in the reply filed 6/24/2026 is acknowledged. Applicant’s election of compound 3:
PNG
media_image2.png
205
261
media_image2.png
Greyscale
In the same reply, without traverse, is also acknowledged.
Examination will begin with the elected species. In accordance with MPEP § 803.02, if upon examination of the elected species, no prior art is found that would anticipate or render obvious the instant invention based on the elected species, the search of the Markush-type claim will be extended. If prior art is then found that anticipates or renders obvious the non- elected species, the Markush-type claim will be rejected. It should be noted that the prior art search will not be extended unnecessarily to cover all non-elected species. Should Applicant overcome the rejection by amending the claim, the amended claim will be examined again. The prior art search will be extended to the extent necessary to determine patentability of the Markush-type claim. In the event prior art is found during further examination that renders obvious or anticipates the amended Markush-type claim, the claim will be rejected and the action made final.
The elected species was searched and no prior art was identified. The search was then expanded to compounds of Chemical Formula I where R3 is halo, L is -NH-S(=O)2-L1-(CH2)n-L2, where L1 and L2 are null and n is 0, and Z is a substituted aryl. See the 102 rejection below. The full scope of the claims has not yet been searched in accordance with Markush search practice. Claims 1-6, and 8-13 read on the expanded species. Claims 4, 7, and 14-15 are withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to nonelected species and/or group, there being no allowable generic or linking claim.
Claim Interpretation
Claims 9-11 recite a pharmaceutical composition comprising a compound of instant Chemical Formula 1 for preventing or treating diseases, and claims 12-13 recite a pharmaceutical composition comprising a compound of instant Chemical Formula 1 for preventing or treating c-KIT or PDGFR-related diseases. The phrases “for preventing or treating” are intended use of the pharmaceutical composition, and is not what the composition is, but rather what the composition does. The intended use does not further limit the structural limitations of the composition and is not granted patentable weight, and thus, the claims are currently being interpreted as the respective pharmaceutical composition comprising the compound of Chemical Formula 1. Claims 9-11 and 12-13 are currently being interpreted as having the same scope as claim 8.
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 9-13 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.
Claims 9 and 12 recite pharmaceutical compositions for preventing or treating diseases, which are merely intended uses of the composition already recited by claim 8. See the claim interpretation section above. Accordingly, claims 9 and 12 are essentially duplicates of the pharmaceutical composition recited by claim 8. Dependent claims 10, 11, and 13, which further limit the diseases to treat and targets to inhibit, do not resolve this issue and are thus also rejected.
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 § 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 1-6 and 8-13 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.
Claims 1-3 and 6 recite the term, “may be” in reference to substitutions of functional groups of Chemical Formula 1. This term is ambiguous and it is unclear if what follows this term is required, or just examples of what is required. Dependent claims 4-5 and 8-13 do not resolve the issue by reciting the specific substitutions, and are therefore also rejected. Appropriate correction is required. The Examiner suggests using the terminology “optionally substituted” in place of “may be” to overcome this rejection.
Claims 1-3 and 6 recite opening and closing square brackets and braces used as parentheses in reference to substitutions of functional groups of Chemical Formula 1. The terms inside the brackets and braces are indefinite because it is unclear if the phrases are required, or just examples of what is required. Dependent claims 4-5 and 8-13 do not resolve the issued by reciting specific substitutions, and are therefore also rejected. Appropriate correction is required.
Claim Rejections - 35 USC § 102
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.
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.
Claims 1-3, 5-6, and 8-13 are rejected under 35 U.S.C. 102(a)(1) and 102(a)(2) as being anticipated by Plexxikon Inc. (WO 2014/039714 A2, cited in the IDS of 4/29/2024, herein after “Plexxikon”). This rejection applies to the expanded species.
The reference Plexxikon discloses compounds active on c-kit protein kinases or mutants thereof (abstract), and specifically discloses compounds P-0249, P-0250, P-0255, P-0256, P-0260, P-0261, and P-0262 (pages 165-167):
PNG
media_image3.png
144
560
media_image3.png
Greyscale
PNG
media_image4.png
152
569
media_image4.png
Greyscale
PNG
media_image5.png
149
569
media_image5.png
Greyscale
PNG
media_image6.png
150
563
media_image6.png
Greyscale
PNG
media_image7.png
149
563
media_image7.png
Greyscale
PNG
media_image8.png
149
562
media_image8.png
Greyscale
PNG
media_image9.png
151
566
media_image9.png
Greyscale
.
The compounds P-0249, P-0250, P-0255, P-0256, P-0260, P-0261, and P-0262 anticipate a compound of instant Chemical Formula 1:
PNG
media_image10.png
341
284
media_image10.png
Greyscale
When R3 is halo, L is -NH-S(=O)2-L1-(CH2)n-L2, where L1 and L2 are null and n is 0, and Z is a substituted aryl. Furthermore, compounds P-0249 and P-0250 anticipate a compound of instant Chemical Formula 1 when R1 and R2 are C1 alkyl and -(CH2)m-Rx where m is 3 and -Rx is heterocycloalkyl, respectively, and the substitution of the aryl Z is a C1 alkoxy in P-0249 and halo in P-0250. Compounds P-0255 and P-0256 anticipate a compound of instant Chemical Formula 1 when R1 and R2 are -(CH2)m-Rx where m is 3 and -Rx is heterocycloalkyl and C1 alkyl, respectively, and the substitution of the aryl Z variable is a C1 alkoxy in P-0255 and a halo in P-0256. Compounds P-0260, P-0261, and P-0262 anticipate a compound of instant Chemical Formula 1 when R1 and R2 are both -(CH2)m-Rx where m is 3 and Rx is C1 alkoxy and the substitution of the aryl Z is a halo in the case of P-0260 and P-0261 and C1 alkoxy in the case of P-0262. Additionally, compounds were dissolved in DMSO for biological assays, indicating a pharmaceutical composition (page 273, line 2).
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.
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 1-6 and 8-13 are rejected under 35 U.S.C. 103 as being unpatentable over Plexxikon Inc. (WO 2014/039714 A2, cited in the IDS of 4/29/2024, herein after “Plexxikon”), as applied to claims 1-3, 5-6, and 8-13 above. This rejection applies to the elected species.
Determining the scope and contents of the prior art
The reference Plexxikon teaches as disclosed above, and at least those teachings are incorporated herein. Additionally, Plexxikon teaches compound P-0273 (page 169):
PNG
media_image11.png
335
1223
media_image11.png
Greyscale
Which maps to instant Chemical Formula 2:
PNG
media_image12.png
298
268
media_image12.png
Greyscale
When R1 is C1 alkyl, R2 is C1 alkyl, R3 is halo, L is -NH-S(=O)2-L1-(CH2)n-L2, where L1 and L2 are null and n is 0, and Z is a phenyl substituted with C1 alkoxy. Additionally, P-0273 was found to have an IC50 of 0.0001 to 1 μM against KIT D816V (page 282). The Examiner notes compound P-0273 does not anticipate a compound of instant Chemical Formula 1 or instant Chemical Formula 2 because the instant claims do not allow for R1 and R2 to be methyl at the same time. However, compound P-0273 is relevant because it contains the halo substituent of R3 at the site ortho- to the L-Z tail.
Ascertaining the differences between the prior art and the claims at issue
The reference Plexxikon fails to teach an anticipatory species of Chemical Formula 2 where R3 is halo and R1 and R2 are not both methyl.
Resolving the level of ordinary skill in the pertinent art
The level of ordinary skill in the art is represented by an artisan who has sufficient background in the development of KIT and PDGFR inhibitors with quinazoline cores. An artisan possess the technical knowledge necessary to make adjustments to the inhibitors to enhance their effectiveness. Said artisan has also reviewed the problems in the art as regards to use of said KIT and PDGFR inhibitors with quinazoline cores and understands the solutions that are widely known in the art.
Considering objective evidence present in the application indicating obviousness or nonobviousness
Applying KSR prong (B), it would have been prima facie obvious for one of ordinary skill in the art to substitute the aryl core where R3 is in the meta- position relative to the L-Z tail of compounds P-0249, P-0250, P-0255, P-0256, P-0260, P-0261, and P-0262 with the aryl core where R3 is in the ortho- position relative to the L-Z tail of compound P-0273 because the compounds are known to be active against the same target and structurally similar compounds are expected to have similar properties. Thus, the change in the substitution site of the internal aryl would be expected to have similar properties. A skilled artisan would have been motivated before the effective filing date to make such a substitution to identify additional substitution to identify additional compounds with activity against KIT and would have reasonably predicted success in view of the teachings of Plexxikon.
Close Prior Art Not Cited
Close prior art identified during the search is Tarapeutics Science Inc. (US 2022/0064117 A1, herein after “Tarapeutics”), which is drawn to compounds and compositions that can inhibit wild-type KIT and/or mutant KIT tyrosine kinase activity, and thus treat, prevent, or alleviate diseases, disorders, or conditions associated with the inhibitory kinase activity (abstract). Specifically, Tarapeutics teaches compounds such as Example 9 (page 13):
PNG
media_image13.png
251
334
media_image13.png
Greyscale
Which is similar to the elected species and a compound of instant Chemical Formula 1:
PNG
media_image10.png
341
284
media_image10.png
Greyscale
When R1 and R2 are each independently C1 alkyl, R3 is hydrogen, L is -NH(C=O)-L1-(CH2)n-L2-, where L1 and L2 are null and n is 1, and Z is a n aryl substituted with a C1 haloalkyl.
Compounds of Tarapeutics are known to inhibit wild type KIT and/or mutant KIT, as are the compounds disclosed in the instant specification. However, Example 9 of Tarapeutics differs from compounds of the instant claims because claim 1 recites that R1 and R2 cannot be methyl at the same time, compounds of the instant claims are quinazolines whereas compounds of Tarapeutics are quinolines, and the compounds of Tarapeutics contain an ether linkage from the quinoline core that is not present in the instant compounds.
Conclusion
Claims 1-6 and 8-13 are rejected. Claims 7, and 14-15 are withdrawn.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to Kendall Heitmeier whose telephone number is (703)756-1555. The examiner can normally be reached Monday-Friday 8:30AM-5:00PM ET.
Examiner interviews are available via telephone, in-person, and video conferencing using a USPTO supplied web-based collaboration tool. To schedule an interview, applicant is encouraged to use the USPTO Automated Interview Request (AIR) at http://www.uspto.gov/interviewpractice.
If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Clinton Brooks can be reached at 571-270-7682. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
Information regarding the status of published or unpublished applications may be obtained from Patent Center. Unpublished application information in Patent Center is available to registered users. To file and manage patent submissions in Patent Center, visit: https://patentcenter.uspto.gov. Visit https://www.uspto.gov/patents/apply/patent-center for more information about Patent Center and https://www.uspto.gov/patents/docx for information about filing in DOCX format. For additional questions, contact the Electronic Business Center (EBC) at 866-217-9197 (toll-free). If you would like assistance from a USPTO Customer Service Representative, call 800-786-9199 (IN USA OR CANADA) or 571-272-1000.
/K.N.H./Examiner, Art Unit 1621
/CLINTON A BROOKS/Supervisory Patent Examiner, Art Unit 1621
Prosecution Insights