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 .
Current Status of 17/755,164
This Office Action is responsive to the amended claims and Applicant remarks of 04/26/2026. Claims 1-6, 8, and 13-20 are pending and have been examined on the merits.
Priority
The instant application is a national stage entry of PCT/CN2020/123330, filed 10/23/2020, which claims foreign priority to Chinese Patent Application No. 201911019555.X, filed 10/24/2019. Acknowledgement is made of Applicants submission of an English translation of Chinese Patent Application No. 201911019555.X.
Response to Arguments
Applicants have submitted a certified English translation of the CN priority application CN 201911019555.X.
Regarding the rejections under 35 U.S.C. §112. Claim 13 has been amended to remove the phrase "preventing and/or" from the claim, rendering the previous rejection moot. The rejection is withdrawn.
Regarding the rejections under 35 U.S.C. §103. Applicants have submitted a Declaration of Dawei Cui under 37 C.F.R. §1.132 providing an explanation reconciling the discrepancies between the instant application and La Roche (WO 2009037172 A1). The Applicants point out that the reference discloses a suspension of compound 5 and MGL-3196 whereas the instant application provides a clear solution of the same compounds through altering the solvent system. Applicants present further arguments discussing the additional uncertainties of suspension in in vivo performance in comparison to true solutions. Applicants additionally argue that AUC and Cmax values differ among animals, strains, formulations, formulation types, administration modes, and test methods resulting in different pharmacokinetic parameters.
Applicants allege that the compounds of the instant application are no longer anticipated by La Roche owed to the amendment limiting R17 to C1-C3 alkyl. The reference does not teach compounds bearing an alkyl group at the specified position. These arguments are persuasive and the previous rejection under 35 U.S.C. §102 is withdrawn.
Regarding the rejections under 35 U.S.C. §103, Applicants reiterate the arguments discussed above regarding the lack of teaching or motivation by La Roche to disclose modifying R17 to C1-C3 alkyl. Applicants allege that reference Sun fails to cure the defect of La Roche. Applicants contend that Sun only generally discloses the potential effects on PK and PD properties through methyl incorporation. Applicants support their arguments using Table 2 of Sun, highlighting that other than compounds 22-23 and 31-32 all other disclosed compounds have methyl substitutions on rings. Applicants further contend that although compounds 23 and 32 demonstrated improved PK and PD properties these trends are not universal citing the disclosure of Sun stating that the effect on biological activity of installing a methyl group is highly case dependent. These arguments support the Applicants' position that the combined teachings of La Roche and Sun fail to teach methyl substitution at the R17 position.
Further, Applicants assert that the incorporation of the alkyl group at this position represents unexpectedly improved pharmacokinetic test results. Applicants discuss the results presented in Tables 3-6 highlighting the differences between the reference compound and the instantly claimed compounds. These results demonstrate that the incorporation of an alkyl group at R17 corresponds to improved pharmacokinetic properties with some of the examples improving the properties by nearly twofold. Applicants assert that these properties demonstrate unexpected results. These arguments have been considered and found to be persuasive. The previous rejections are withdrawn.
Claim Rejections - 35 USC § 112
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.
Claim 1 is 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.
A broad range or limitation together with a narrow range or limitation that falls within the broad range or limitation (in the same claim) may be considered indefinite if the resulting claim does not clearly set forth the metes and bounds of the patent protection desired. See MPEP § 2173.05(c). In the present instance, claim 1 recites the broad recitation of the compounds of formulae (I) and (Ia), and the claim also recites the compound of 6B which is the narrower statement of the range/limitation. The claims are considered indefinite because there is a question or doubt as to whether the feature introduced by such narrower language is (a) merely exemplary of the remainder of the claim, and therefore not required, or (b) a required feature of the claims.
Close Art
The closest prior art is La Roche (EP 2203441 B1, found in IDS field 01/03/2024). La Roche discloses compounds of formula (I) which are thyroid hormone receptor agonists useful in treating obesity, hyperlipidemia, hypercholesterolemia, diabetes, nonalcoholic steatohepatitis (NASH), liver steatosis, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and related disorders and diseases (Title, Abstract). The reference discloses example 20
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(pg. 21, [0078]). Example 20 is a compound of the instantly claimed compounds of formula (I)
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with the following substitutions: R1 is H; R2 and R3 are C1 alkyl (methyl); X is C(R17R18)OZ, R17 and R18 are H, Z is -C(O)OR5, R5 is C2 alkyl; R4, R7, and R9 are H; R6 and R8 are Cl; and Y is H. Example 20 anticipates the structures of III-A, IV-A, and V-A (instant claims 14, 2 and 3). La Roche’s compound 20 no longer reads on the Markush group of the compounds of formula (I) due to amendment limiting R17 to C1-3alkyl. While the incorporation of methyl substituents into pharmaceutically active compounds is common in the art, there is no specific teaching or motivation that would have lead the artisan to make a substitution at the position on La Roche’s compound 20 to arrive at the instantly claimed genus. Additionally, the artisan would not have anticipated that this substitution would result in a nearly twofold increase in the PK or PD properties of the molecule, as such substitutions are highly case dependent.
Conclusion
Claim 1 is rejected.
Claims 2-6, 8, and 13-20 are objected to for being dependent upon a rejected base claim.
Applicant's amendment necessitated the new ground(s) of rejection presented in this Office action. Accordingly, THIS ACTION IS MADE FINAL. See MPEP § 706.07(a). Applicant is reminded of the extension of time policy as set forth in 37 CFR 1.136(a).
A shortened statutory period for reply to this final action is set to expire THREE MONTHS from the mailing date of this action. In the event a first reply is filed within TWO MONTHS of the mailing date of this final action and the advisory action is not mailed until after the end of the THREE-MONTH shortened statutory period, then the shortened statutory period will expire on the date the advisory action is mailed, and any nonprovisional extension fee (37 CFR 1.17(a)) pursuant to 37 CFR 1.136(a) will be calculated from the mailing date of the advisory action. In no event, however, will the statutory period for reply expire later than SIX MONTHS from the mailing date of this final action.
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/C.K.E./Examiner, Art Unit 1625 /Andrew D Kosar/Supervisory Patent Examiner, Art Unit 1625
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