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 .
Claims 1-14 are before the Examiner.
Claim Rejections - 35 USC § 112
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.
Claim 14 is rejected under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, as failing to comply with the enablement requirement. The claim(s) contains subject matter which was not described in the specification in such a way as to enable one skilled in the art to which it pertains, or with which it is most nearly connected, to make and/or use the invention.
The determination that "undue experimentation" would have been needed to make and use the claimed invention is not a single, simple factual determination. Rather, it is a conclusion reached by weighing all the relevant factual considerations.
Enablement is considered in view of the Wands factors (MPEP 2164.01 (a)). These include: (1) breadth of the claims; (2) nature of the invention; (3) state of the prior art; (4) amount of direction provided by the inventor; (5) the level of predictability in the art; (6) the existence of working examples; (7) quantity of experimentation needed to make or use the invention based on the content of the disclosure; and (8) relative skill in the art.
All of the factors have been considered with regard to the claims, with the most relevant factors discussed below:
Thus the recited formula for the ingredients contain large number of variable groups layered with substituents layered on substituents encompassing wide variety and number of conceivable structures that find little support in the specification. These substituents and hence the compounds of given formula are drawn to species that vary widely in physical and chemical properties such as size, molecular weight, stereochemistry, logP, acidity, basicity, etc. These factors are known in the art (see multiple references cited below) to greatly influence biological properties, for example, binding interaction between target protein and small molecule and art recognized concepts relating to productive small molecule-macromolecule interaction.
There is no guidance on what to choose from these large number of structural moieties or where and how to link these moieties. Enablement is a two prong (make and use) requirement. There is no structural guidance such as pharmacophore definition disclosed in the specification to guide one of skill in the art to choose from the plethora possibilities recited for the variables. Disclosure in Table 1 starting at page 286 indicated compounds having the same invariable template of the recited formula show wide range of activities This is consistent with the unpredictability in the pharmaceutical art. Biological properties are unpredictable and are ultimately tide to the chemical structure. See “Role of the Development Scientist in Compound Lead Selection and Optimization” by Venkatesh, J. Pharm. Sci. 89, 145-154 (2000) (p. 146, left column). Likewise, J. G. Cannon, Chapter Nineteen in Burger's Medicinal Chemistry and Drug Discovery, Fifth Edition, Volume I: Principles and Practice, Wiley-Interscience 1995, pp. 783-802, 784, teaches many caveats in analog design such as
Alteration of distances between portions of the pharmacophore of a molecule (or
even' between other portions). may produce profound qualitative and/or
quantitative changes in pharmacological actions.
State of the art with respect to modulating SIK activity is not supportive for treating any and all of the diseases recited:
See Darling, Biochem J. 2021 Apr 16;478(7):1377-1397. Darling titled ‘Nuts and bolts of the salt-inducible kinases (SIKs), (see Abstract) summarizes current knowledge of the SIKs and the evidence underpinning these findings. Darling concludes that many outstanding questions remain, (page 1392) and regulation of SIKs provide fertile areas for future research. At page 1384, Darling teahes that the SIK inhibitors in current use have limitations and additional structurally unrelated SIK inhibitors with enhanced specificity are needed, including compounds selective for particular SIK isoforms. Compounds that may have improved specificity, such as ARN-3236 (Figure 3) are beginning to emerge now that interest in targeting SIKs for the treatment of disease is increasing (see SIK-inhibiting drugs for the treatment of disease). Neither in Darling nor in the specification support for predictable use of SIK modulators as instantly recited. Similarly, Jagannath, titled THE MULTIPLE ROLES OF SALT-INDUCIBLEKINASES IN REGULATING PHYSIOLOGY, Physiol Rev 103: 2231–2269, 2023, teaches that In summary, the members of the SIK family are emerging as master regulators of multiple aspects of physiology, including metabolism, immune function, development, and sleep and circadian rhythms. As SIKs are unique in their ability to be exquisitely modulated by extracellular signals, the SIKs serve to alter transcriptional and posttranscriptional responses to inputs that modify physiology. thus providing the substrate with which this important family of kinases can be developed for therapeutic application. See page column B, page 2258. Jagannath concludes ‘Future research will address these important questions, thus providing the substrate with which this important family of kinases can be developed for therapeutic application’. Genentech Inc. v. Novo Nordisk A/S (CA FC) 42 USPQ2d 1001, states “a patent is not a hunting license. It is not a reward for search, but compensation for its successful conclusion” and “[p]atent protection is granted in return for an enabling disclosure of an invention, not for vague intimations of general ideas that may or may not be workable”.
There is a substantial gap between what is taught in the specification and what is being claimed. For these reasons, one skilled in the art would be faced with undue amount of research. The specification lacks disclosure sufficient to make and use the invention, in predictable manner.
MPEP 2164.01(a) states, “A conclusion of Iack of enablement means that, based on the evidence regarding each of the above factors, the specification, at the time the application was filed, would not have taught one skilled in the art how to make and/or use the full scope of the claimed invention without undue experimentation. ln re Wright, 999 F.2d 1557,1562, 27 USPQ 2d 1510, 1513 (Fed. Cir. 1993).'' That conclusion is clearly justified here. Thus, undue experimentation would be required to make and use Applicants' invention.
The prior art made of record and not relied upon is considered pertinent to applicant's disclosure.
Sakamoto, The Salt-Inducible Kinases: Emerging Metabolic Regulators
Trends in Endocrinology & Metabolism, December 2018, Vol. 29, No. 12, 827-840;
Shi, Salt-inducible Kinase Regulation of Adipose Tissue Metabolism, Endocrinology, Volume 166, Issue 7, July 2025.
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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.
Claim(s) 1, 2, 3,4, 6, 7, 8, 10, 12, 13 is/are rejected under 35 U.S.C. 102(a)(1) as being
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16
76
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or
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12
246
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as
as ascertained from the Chemical Abstract Service, a data base approved by the patent office;
The numbers below are Chemical Abstract Service Registry Numbers, unque to the compounds, .
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134
562
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142
850
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.
These compounds correspond to formula I as correlated below
R1 = R2 = R4 = R5 = H;
R2’=methyl
A1 =A 2 = A3 = bond
Claims 5, 9, 11, 12 are objected to as being dependent upon a rejected base claim, but would be allowable if rewritten in independent form including all of the limitations of the base claim and any intervening claims.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to NIZAL S CHANDRAKUMAR whose telephone number is (571)272-6202. The examiner can normally be reached M-F 8-5 EST.
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If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Andrew Kosar can be reached at (571) 272-0913. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/NIZAL S CHANDRAKUMAR/Primary Examiner, Art Unit 1625
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