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 .
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.
Claims 1-22 and 24-26 are 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. Claims 1-20 are directed to a compound and to a pharmaceutical composition. Claims 21-22 and 24-26 are directed to methods of treating various diseases including fibrotic conditions, inflammatory disorders, autoimmune disorders NASH, NAFDL, PSC, chronic and diabetic kidney disease among others. The claims directed to compounds are included in this rejection because in order to be patentable a product must have a credible utility disclosed in the specification. Since the only disclosed utility of the claimed compound is in a method of treating one of the above listed diseases, treatment of diseases must be enabled in order to satisfy the credible utility requirement. The compounds are rejected because a credible utility for the compounds has not been established.
There are many factors to be considered when determining whether there is sufficient evidence to support a determination that a disclosure does not satisfy the enablement requirement and whether any necessary experimentation is "undue." These factors include, but are not limited to: (a) the nature of the invention; (b) the breadth of the claims; (c) the state of the prior art; (d) the amount of direction provided by the inventor; (e) the existence of working examples; (f) the relative skill of those in the art; (g) whether the quantity of experimentation needed to make or use the invention based on the content of the disclosure is "undue"; and (h) the level of predictability in the art (MPEP 2164.01 (a)).
Nature of the invention and Breadth of the claims:
The claims are directed to a method of treating a disease selected from including fibrotic conditions, inflammatory disorders, autoimmune disorders NASH, NAFDL, PSC, PBC, chronic kidney disease, diabetic kidney disease, cancer. The scope of diseases to be treated is very large as it encompasses different types of conditions that are conventionally treated by different therapeutic agents. Additionally diseases such as cancer and autoimmune diseases and inflammatory disease are themselves geniuses of different diseases that comprise multitudes of specific species.
State of the prior art and level of predictability in the art:
Currently claimed compounds are selective inhibitors of TLR9 receptors. With regards to treatment of diseases there are ample articles supporting the hypothesis that targeting TLR9 receptors could be a strategy for modulating the progression of disease that comprise an inflammatory component. However, Examiner was unable to uncover any selective TLR9 inhibitor being on the market for treatment of any disease. It appears the research in this field is ongoing and has not been successfully reduced to clinical practice.
Neilsen et al (ImmunoTargets and Therapy, 2025, 14, 1531-1554) discusses the role TLR9 receptors play in pathogenesis of the currently claimed conditions. On page 1546, Section “TLR9 antagonists”, Neilsen teaches with regards to cancer: “Despite demonstrating some efficacy in preclinical models, TLR9 antagonists lack sufficient evidence to progress to clinical trials”
On page 1547, “Conclusion” Neilsen teaches “therapeutic strategies to inhibit TLR9 are extremely limited as TLR9 antagonists have shown minimal success in translational studies”
Amount of direction provided by the inventor and existence of working examples:
The examples in the specification are directed to synthesis of the claimed compound. The sole biological example is an in vitro assay of TLR7/8/9 inhibition. The assay indicates that the claimed compound is a selective inhibitor of TLR9.
Specification does not disclose any experiments directed to treatment of any of the claimed diseases. There are no art recognized model that have been utilized to support a claim of clinical efficacy of the claimed compounds.
Although, the specification need not contain an example if the invention is otherwise disclosed in such manner that one skilled in the art will be able to practice it without an undue amount of experimentation. In re Borkowski, 422 F.2d 904, 908, 164 USPQ 642, 645 (CCPA 1970), lack of a working example is a factor to be considered, especially in a case involving an unpredictable and undeveloped art.
With regard to actually practicing the claimed method, the specification provides only generalizations and intent to treat the claimed diseases, but no data to support this assertion. Thus, the disclosure clearly does not otherwise disclosed the process of practicing the invention in such manner that one skilled in the art will be able to practice it without an undue amount of experimentation.
Relative skill of those in the art and quantity of experimentation needed to make or use the invention:
Although the relative level of skill in the art is high, one of ordinary skill would not be able to treat cancer or any other claimed disease according to the claimed method without engaging in undue experimentation. The art clearly recognizes that TLR9 inhibitors are an area of interest for treatment of the claimed diseases, but as of 2025, there appear to be no successful implementation of this hypothesis. Specification does not resolve this lack of efficacy because it only established the activity of the claimed compounds in a single in vitro assay and provides no data that would support the assertion of the claimed clinical efficacy. Thus, without specific guidance as to an effective dosage and route of administration of the agent, assuming that one exists, and the additional manipulations required for effective therapy, one of ordinary skill in the art must experiment to establish the effective parameters and do extensive testing in multiple disease models. Even with all of that experimentation completed, it is still uncertain that cancer and other claimed disorders can be treated by administration of the claimed compound because no disease is currently being treated by administration of a selective TLR9 inhibitor.
Thus, given these considerations, one of ordinary skill in the art clearly would not be able to practice the claimed method such that it can be used as contemplated in the specification without first engaging in substantial and undue experimentation. Therefore, the claims are rejected under 35 U.S.C. §112, first paragraph, as lacking and enabling disclosure.
MPEP 2164.01(a) states, “A conclusion of lack 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. In re Wright, 999 F.2d 1557,1562, 27 USPQ2d 1510, 1513 (Fed. Cir. 1993).” That conclusion is clearly justified here. Thus, undue experimentation will be required to practice Applicants' invention.
Conclusion
Claims 1-22 and 24-26 are pending
Claims 1-22 and 24-26 are rejected
Any inquiry concerning this communication or earlier communications from the examiner should be directed to YEVGENY VALENROD whose telephone number is (571)272-9049. The examiner can normally be reached Mon-Fri 9am-5pm.
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If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Amy L Clark can be reached at 571-272-1310. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/YEVGENY VALENROD/Primary Examiner, Art Unit 1628
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