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 .
Continued Examination Under 37 CFR 1.114
A request for continued examination under 37 CFR 1.114, including the fee set forth in 37 CFR 1.17(e), was filed in this application after final rejection. Since this application is eligible for continued examination under 37 CFR 1.114, and the fee set forth in 37 CFR 1.17(e) has been timely paid, the finality of the previous Office action has been withdrawn pursuant to 37 CFR 1.114. Applicant's submission filed on December 22, 2025 has been entered.
Detailed Action
This office action is a response to applicant’s communication submitted December 22, 2025, wherein claims 1 and 30 are amended. This application is a national stage application of PCT/EP2021/063463, filed May 20, 2021, which claims priority to foreign application EP20175820.8, filed May 20, 2020.
Claims 1-9, 12, 16, 24, 25, 28, 30, 31, and 34-45 are pending in this application.
Claims 1-9, 12, 16, 24, 25, 28, 30, 31, and 34-45 as amended are examined on the merits herein.
Withdrawn Rejections
Applicant’s amendment, submitted December 22, 2025, with respect to the rejection of claims 30, 34, and 39-45 under 35 USC 102(a)(1) for being anticipated by Luk et al., has been fully considered and found to be persuasive to remove the rejection as the claims have been amended so as to refine R1 in a way excluding the compounds of Luk et al. Therefore the rejection is withdrawn.
Applicant’s amendment, submitted December 22, 2025, with respect to the rejection of claims 30, 34, and 39-45 under 35 USC 102(a)(1) for being anticipated by Luk et al., has been fully considered and found to be persuasive to remove the rejection as the claims have been amended so as to refine R1 in a way excluding the compounds of Luk et al. Therefore the rejection is withdrawn.
Applicant’s amendment, submitted December 22, 2025, with respect to the rejection of claim 38 under 35 USC 103 for being obvious over Luk et al., has been fully considered and found to be persuasive to remove the rejection as the claims have been amended so as to refine R1 in a way excluding the compounds of Luk et al., and furthermore it is seen that none of the specific compounds described by Luk could be routinely and predictably modified to arrive at compounds of the present claims wherein R1 is a lower alkyl. Therefore the rejection is withdrawn.
Applicant’s amendment, submitted December 22, 2025, with respect to the rejection of claims 1-9, 16, 24, 28, 36, and 37 under 35 USC 103 for being obvious over Luk et al. in view of Li et al., has been fully considered and found to be persuasive to remove the rejection as the claims have been amended so as to refine R1 in a way excluding the compounds of Luk et al. Therefore the rejection is withdrawn.
Applicant’s amendment, submitted December 22, 2025, with respect to the rejection of claim 35 under 35 USC 103 for being obvious over Luk et al. in view of McNally et al., has been fully considered and found to be persuasive to remove the rejection as the claims have been amended so as to refine R1 in a way excluding the compounds of Luk et al. Therefore the rejection is withdrawn.
The following new grounds of rejection are introduced:
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.
Claims 30, 34, 38, 40, 41, 43, and 45 are rejected under 35 U.S.C. 102(a)(1) as being anticipated by Engelhardt et al. (US pre-grant publication 2014/0296229, cited in PTO-892)
Independent claim 30 claims a compound having a particular structure (Ia):
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wherein the variable groups are as defined in the claim. Engelhardt et al. discloses a compound having a formula
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which is defined in such a way as to overlap the scope of compounds recited in present claim 30. (p. 1 paragraph 7) In particular, claim 30 defines the variable R3 as including a “heterocycloalkyl” group which can be substituted with one or more Rcyc that can include methyl, as one potential option, which would be infringed by the dimethyl oxazole group appearing in compounds (I) of Engelhardt. Specific compounds disclosed by Engelhardt include
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, (p. 28 paragraph 328) which anticipates present claim 30.
Regarding claim 34, p. 2 paragraph 35 of Engelhardt discloses pharmaceutical compositions of these compounds in combination with pharmaceutical excipients or carriers.
Regarding claims 38, 40, 41, 43, and 45, these claims merely define the variable groups of structure (Ia) in a way that is still infringed by the compound
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.
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.
Claims 39 and 44 are rejected under 35 U.S.C. 103 as being unpatentable over Engelhardt et al. (US pre-grant publication 2014/0296229, cited in PTO-892)
The disclosure of Englehardt et al. is discussed above. Engelhardt et al. does not specifically disclose an embodiment wherein R4 is a halogen or R5 is lower alkoxy. However, the definition of generic structure (I) in p. 1 paragraph 7 of Engelhardt discloses that the group R2 (The phenyl in the compound mentioned in the rejection under 102, to which R4 and R5 are attached) can be substituted with one or more R7 which can be halogen or -O-C1-3 alkyl. Furthermore specific examples are given (Compound 5 on p. 16, compound 28 on p. 31) which specifically have a halogen atom in a position corresponding to position R4 in the present claims. It would therefore have been obvious to one of ordinary skill in the art at the time of the invention to modify the specific compound mentioned under 35 USC 102 so as to have a halogen atom at position R4 One of ordinary skill in the art would have seen this modification to be obvious by a rationale of lead compound modification within the scope of structures suggested by the reference.
Therefore the invention taken as a whole is prima facie obvious.
Claims 1-4, 6-8, 28, and 35-37 are rejected under 35 U.S.C. 103 as being unpatentable over Engelhardt et al. as applied to claims 30, 34, 38-41, and 43-45 above, and further in view of Gabel et al. ( US pre-grant publication 2018/0318285, cited in PTO-892)
The disclosure of Engelhardt et al. is discussed above. Regarding claims 1, 28, 35, and 37, Engelhardt et al. does not describe the disclosed compounds as being useful for treating fragile X syndrome, autism, or an autism spectrum disorder. However, Engelhardt et al. does disclose the compounds as being inhibitors of BRD4. (p. 1 paragraph 1, pp. 32-33 paragraphs 369-373)
Gabel et al. discloses a method of treating autism spectrum disorder and fragile X syndrome comprising administering an agent that affects expression of long genes in the brain. (p. 1 paragraphs 8-9) Among the particular agents that can be used is a BRD4 inhibitor. (p. 2 paragraphs 13-15, p. 8 paragraphs 62-63) Therefore it would have been obvious to one of ordinary skill in the art at the time of the invention to administer the BRD4 inhibitors described by Engelhardt et al. to a subject suffering from Fragile X syndrome or autism spectrum disorder. One of ordinary skill in the art would have found this to be obvious in view of the disclosure by Gabel et al. that BRD4 inhibitors can be used to treat these conditions. Regarding claims 2, 4, 6-8, and 36, these dependent claims merely further limit the structure of the compound (I) used in base claim 1 in a manner consistent with the disclosure of Engelhardt et al.
For these reasons the invention taken as a whole is prima facie obvious.
Claims 30, 34, and 38-44 are rejected under 35 U.S.C. 103 as being unpatentable over Christensen et al. (US pre-grant publication 2010/0227863, cited in PTO-892)
Independent claim 30 claims a compound having a particular structure (Ia):
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wherein the variable groups are as defined in the claim. Christensen et al. discloses compounds having the formula (I):
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which is defined in such a way as to overlap the scope of compounds recited in present claim 30. (p. 7 paragraph 21) Christensen et al. furthermore discloses specific compounds including
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(p. 31 paragraph 362)
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(p. 31 paragraph 366)
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(p. 32 paragraph 274)
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(p. 32 paragraph 378)
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(p. 32 paragraph 382) and
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. (p. 38 paragraph 440) These compounds are similar to those of present claim 30 but differ in the definition of R6, which according to present claim 30 cannot be methyl, and cannot be only halo groups. However, as discussed in p. 7 paragraph 21 of Christensen et al. these positions (R1-R4 in the reference) can be other groups such as C2 or higher alkyl. Therefore it would have been obvious to one of ordinary skill in the art at the time of the invention to modify the specific compounds described by Christensen et al. in such a way that they would fall within the scope of the exclusionary provisos limiting R6 in claim 30, for example by including one C2-5 alkyl or haloalkyl group in one of these positions. Doing so would involve only conservative, predictable modification of specific lead compounds described by Christensen et al.
Regarding claim 34, Christensen et al. describes pharmaceutical composition comprising said compounds. (p. 14 paragraphs 159-160) Regarding claims 38-44, these claims merely specify additional structural features already disclosed by Christensen et al.
Therefore the invention taken as a whole is prima facie obvious.
Conclusion
Claims 1-4, 6-8, 28, 30, and 34-45 are rejected. Claims 25 and 31 are seen to be allowable. Claims 5, 9, 12, 16, and 24 are objected to for depending form a rejected base claim but would be allowable if rewritten in independent form incorporating all the limitations of the rejected base claim and any intervening claims.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to ANDREA OLSON whose telephone number is (571)272-9051. The examiner can normally be reached M-F 6am-3:00pm.
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/ANDREA OLSON/ Primary Examiner, Art Unit 1693 2/18/2026