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 THE CLAIMS: Claims 1-14 and 19-24 are pending in this application.
Election/Restrictions
Applicant’s election of species in the reply filed on January 22, 2026 is acknowledged. All claims were examined in its entirety.
Claim Rejections - 35 USC § 112, first paragraph
The following is a quotation of the first paragraph of 35 U.S.C. 112(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 1-14 and 19-24 (including claims dependent thereon and claims that relate back to independent claim 1) 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 1-14 and 19-24 (including claims dependent thereon and claims that refer to interdependent claims) are rejected under 35 U.S.C. 112, first paragraph, because the specification, while being enabling for specific compounds disclosed in the specification, does not reasonably provide enablement for solvates, isotopologue and tautomer of those compounds and composition containing same. The specification does not enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the invention commensurate in scope with these claims.
Claims 1 and 19 are rejected because the claims recite specific compounds and solvates, isotopologue and tautomer of said compounds. However, the specification fails to teach the preparation or identity of solvates, isotopologue and tautomer. Therefore, the specification is not adequately enabled for making and/or using solvates, isotopologue and tautomer.
Identifying an solvates, isotopologue and tautomer requires knowledge of in vivo regeneration pathways of instant compounds and short of extensive experimentation, would be the skilled artisan would need much more data to determine solvates, isotopologue and tautomer of the instant compounds and compositions.
Applicants have not provided any clear guidance that would provide solvates, isotopologue and tautomer of the instant compounds that will regenerate in vivo to the instant compounds by one or more biological processes or methods for preparing solvates. It is not the norm that one can predict with any accuracy whether a particular ester form of an active compound will be more soluble, more easily handled in formulations or more bioavailable without art recognized data to support same. The specification provides no guidance as to what type(s) of solvates, isotopologue and tautomer are suitable for the instant compounds. Generally, solvates, isotopologue and tautomer themselves are not considered to be therapeutically active but only to provide the active compound in vivo.
For rejections under 35 U.S.C. 112, first paragraph, the following factors must be considered (In re Wands, 8 USPQ2d 1400, 1404 (CAFC, 1988)):
1) Nature of invention.
2) State of prior art.
3) Quantity of experimentation needed
4) Level of predictability in the art.
5) Amount of direction and guidance provided by the inventor.
6) Existence of working examples.
7) Breadth of claims.
8) Level of ordinary skill in the art.
Nature of the invention
The nature of the invention is the preparation of compounds and compositions under the genus of structural formula I. As stated, however, solvates, isotopologue and tautomer are also intended. The nature of solvates, isotopologue and tautomer is not set forth nor is the manner in which the solvates are to be prepared or the core compounds modified.
State of the prior art
The state of the prior art is that acceptable salts are known in the pharmaceutical industry. Solvates, isotopologue and tautomer in related compounds are not modified.
Quantity of experimentation needed
The quantity of experimentation needed is undue. The skilled artisan would need to regenerate in vivo the instant compounds by one or more biological processes. All of which require undue experimentation. Applicant has not postulated a metabolic pathway or mechanism, which facilitate conversion of the solvates into an active agent.
Level of predictability in the art
The art pertaining to the preparation and use of solvates, isotopologue and tautomer are compound specific and not all solvates have the ability to regenerate in vivo. (See “Wolff, M.E., “Burger’s Medicinal Chemistry”, pp. 975-977, and Banker et al., “Modern Pharmaceuticals”, p. 596).
Amount of direction and guidance provided by the inventor
There is no guidance provided as all the examples in the specification are drawn to the preparation of compounds disclosed in the specification and not to solvates. The lack of guidance to prepare any esters is not provided by the inventor.
Existence of working examples
As discussed above, working examples are drawn to the preparation of compounds disclosed in the specification and not to solvates, isotopologue and tautomer. The lack of guidance to prepare any solvates is telling. There is no direction or guidance provided by Applicant to prepare solvates, isotopologue and tautomer of the instant invention.
Breadth of claims
The breath of the recited compounds and compositions in the claims includes solvates, isotopologue and tautomer for which there have been provided no specific examples or procedural steps to prepare solvates. Failure to teach how to make the instant compounds makes teaching how to use the compounds unduly difficult, if not impossible.
Level of ordinary skill in the art
The level of ordinary skill in the art is high due to the unpredictability in the chemical art.
Hence, as discussed above, to practice the claimed invention herein, a person of ordinary skill in the art would have to engage in undue experimentation to test which solvates, isotopologue and tautomer can be used in the instant claim, with no assurance of success.
Therefore, applicant must show that the specification teach the preparation of solvates, isotopologue and tautomer or limit the claims accordingly.
Claims 1-13 (including claims dependent thereon) 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.
Claim 1 is is directed to a method of treating airway diseases. In light of this, it can be asserted that in spite of the vast expenditure of human and capital resources in recent years, no one drug has been found which is effective in treating all types airway diseases. In re Hokum, 226 USPQ 353 (ComrPats 1985).
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 above noted factual considerations. In re Wands, 858 F.2d at 737, 8 USPQ2d at 1404.
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 breadth of the claims;
(B) The nature of the invention;
(C) The state of the prior art;
(D) The level of one of ordinary skill;
(E) The level of predictability in the art;
(F) The amount of direction provided by the inventor;
(G) The existence of working examples; and
(H) The quantity of experimentation needed to make or use the invention based on the content of the disclosure.
The breadth of the claims
The breadth of the instant claims is seen to encompass methods for treating airway diseases, by administering to a patient in need of such treatment a therapeutically effective amount of the compound claim. Applicant fails to disclose which specific diseases are treated. Thus, the claims are extremely broad.
The nature of the invention
The nature of the invention is the treatment of these disorders through the use of the claimed compound according to formula I and derivatives thereof . Currently, there are no known agents that treat these diseases all inclusively.
The level of predictability in the art
The treatment of these disorders is highly unpredictable. It is well established that “the scope of enablement varies inversely with the degree of unpredictability of the factors involved,” and physiological activity is generally considered to be an unpredictable factor. See In re Fisher, 427 F.2d 833, 839, 166 USPQ 18, 24 (CCPA 1970).
The amount of direction provided by the inventor.
The applicant has not demonstrated sufficient guidance provided in the form of administration profiles, combination ratios of the active agents or reference to the same in the prior art to provide a skilled artisan with sufficient guidance to practice the instant treatment of disorders claimed. Further, the applicant discloses that an effective amount of the compound will be administered without providing any direction other than that the compounds of the invention have a high therapeutic index and follows this with a definition readily found in a basic pharmacology textbook. It should be noted that the therapeutic index of a drug in humans is almost never known and is only determined through clinical experience.
The existence of working examples.
There is not seen in the disclosure, sufficient evidence to support Applicant’s claims of treating of these disorders. 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, 27 USPQ2d 1510 (CAFC). The disclosure does not demonstrate sufficient evidence to support the applicant's claim to the treatment. There are not sufficient working examples or data from references of the prior art to provide a nexus between those examples and a method of treating the disorders with the claimed compound.
The level of one of ordinary skill.
The level of skill is that of one with a doctoral understanding of airway diseases therapeutics. Applicant’s data is not convincing as to make the production and use of pharmaceutical compositions comprising the recited compounds feasible without undue, un-predictable experimentation.
The quantity of experimentation.
A great deal of experimentation is required for the method of treating airway disorders. Furthermore, direction, in the form of examples, must be shown to determine what an effective dose may be. The references submitted do not demonstrate this. Therefore, one of ordinary skill in the art would require a significant amount of experimentation in order to determine the effective dosage to treat the multitudes of different types of diseases with the claimed compound individually or in combination with other therapeutic agents.
Thus, it can be safely concluded that the instant case fails to provide an enabling disclosure for the treatment of airway diseases.
Claims 1-14 (including claims dependent thereon) 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.
Claim 1 is rejected under 35 U.S.C. 112, first paragraph, because the specification, while being enabling for “treating”, does not reasonably provide enablement for “preventing” or “ameliorate/ameliorating” or “prophylaxis”. The specification does not enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to practice the invention commensurate in scope with these claims. Applicant is entitled to treatment or treating, not “ameliorating”.
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 above noted factual considerations. In re Wands, 858 F.2d at 737, 8 USPQ2d at 1404.
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 breadth of the claims;
(B) The nature of the invention;
(C) The state of the prior art;
(D) The level of one of ordinary skill;
(E) The level of predictability in the art;
(F) The amount of direction provided by the inventor;
(G) The existence of working examples; and
(H) The quantity of experimentation needed to make or use the invention based on the content of the disclosure.
The breadth of the claims
The breadth of the instant claims is seen to encompass methods for ameliorating airway disorders by administering to a patient in need of such treatment a therapeutically effective amount of the compound of formula I. Applicant failed to exactly defined how to prevent these diseases. Additionally, it is clear that Applicant has not limited his definition of prevention to one particular disease. Thus, claim is extremely broad.
The nature of the invention
Currently, there are no known agents with the therapeutic efficacy to prevent or ameliorate these disorders. The art does not disclose an active agent or combination of active agents, which is recognized as prevention for the conditions cited supra. The prior art does not teach or disclose a treatment modality wherein healthy subjects are treated with an active agent or agents and there is no evidence that none of the associated symptoms or disease state characteristics are ever manifested. The disclosure does not direct the skilled artisan to an art, which satisfies the requirement for preventing a disease state associated with these disorders.
The level of predictability in the art
Since the art does not disclose any therapeutic preventative agents, the skilled artisan would not predict, in the absence of proof to the contrary, that the active agent(s) instantly claimed are efficacious in preventing the conditions as broadly claimed. The assertion of a broad application, as set forth in the instant method claims, necessarily requires evidence to support Applicant’s asserted methods. The Examiner notes there are no known agents recognized as preventative agents, and one of skill in this art could not predict, from the evidence of record, that the active agents asserted to be useful in the instantly claimed method, can indeed ameliorate these disorders.
The amount of direction provided by the inventor
The Examiner notes, there is not seen sufficient guidance provided in the form of administration profiles, combination ratios of the active agents or reference to same in the prior art to provide the skilled artisan with sufficient guidance to practice the instant preventative method. Prevention is seen to encompass administering the active agent to a subject in need, and noting the fact that symptoms of conditions such as these disorders never manifest themselves. The data and evidence provided in the instant disclosure leads the examiner to doubt the objective truth of assertions of prevention of any of the conditions.
The existence of working examples
There is not seen in the disclosure, sufficient evidence to support Applicant’s claims of prevention. There is not seen sufficient working examples or data from references of the prior art providing a nexus between that which applicant asserts as proof of a method for ameliorating these disorders from the data and evidence currently provided on the record to support methods drawn to ameliorating any condition.
The level of one of ordinary skill
The ordinary skill artisan would not be able to practice the claimed invention of ameliorating these disorders with the current disclosure.
The quantity of experimentation
A great deal of experimentation is required. In lieu of the fact that no animal models exists which can reasonably suggest successful ameliorating of these disorders, it may be necessary for an ordinary skilled artisan to have clinical data in order to practice the claimed invention.
Thus, it can be safely concluded that the instant case fails to provide an enabling disclosure for the ameliorating of airway diseases.
Allowable Subject Matter
Claims 19-24 will be allowed if amended to overcome the rejection under 35 U.S.C. 112, first paragraph for reciting for solvates, isotopologue and tautomer. The prior art (US Pub. 2017/0136023) does not teach or suggest the compounds substituted in the manner claimed by the Applicant. Therefore, these claims will be allowed, if amended to overcome objection and rejection under 35 U.S.C. 112, first paragraph.
Conclusion
Claims 1-14 and 19-24 are pending. Claims 1-14 and 19-24 are rejected. No claims are allowed.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to PAUL V WARD whose telephone number is (571)272-2909. The examiner can normally be reached M-F 9am to 5pm.
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/PAUL V WARD/ Primary Examiner, Art Unit 1622
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