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, 3-6, 10 and 14-17 are pending in this application.
Election/Restrictions
Applicant’s election of species in the reply filed on June 24, 2026 is acknowledged. All claims were examined in its entirety.
Claim Objections
Claims 1 and 3-6 are objected to because of the following informalities: the claims recite “A chymase inhibitor….”. Examiner suggest amending the claims to “A compound….” (i.e., delete “chymase inhibitor”). Appropriate correction is required.
Claim Rejections - 35 USC § 112, 2nd paragraph
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.
Claims 14-15 (including claims dependent thereon) are 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 pre-AIA the applicant regards as the invention.
Regarding claim 14, the phrase "such as" renders the claim indefinite because it is unclear whether the limitations following the phrase are part of the claimed invention. See MPEP § 2173.05(d).Correction is required.
Claim Rejections - 35 USC § 112, first paragraph
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, 3-6, 10 and 14-17 (including claims dependent thereon or claims that relate back) are rejected under 35 U.S.C. 112, first paragraph, as failing to comply with the enablement requirement. The claims 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 and 3-6 are rejected under 35 U.S.C. 112, first paragraph, as failing to comply with the enablement requirement. The claims are directed to compounds and/or pharmacal compositions or medicaments comprising the claimed compounds. The claims are rejected for lack of enablement because there is an insufficient teaching of how to use the claimed compounds as claimed. A compound used for a medicament or pharmaceutical composition specify that least some therapeutic benefit arise from some property of the compound and the medicament comprising the compound. Intended use claims do not have patentability weight. A pill, for example is a pill no matter what it is used for, and thus, intended use are not consider patentable. Therefore, Applicant has not taught how to use the compounds of the invention to therapeutic effect for any condition. Examiner suggests amending claims to method claims or delete the use of the compound from the claims.
Claims 1, 3-6, 10 and 14-17 (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 and 3-4 (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 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 1-99 are rejected because the claims recite specific compounds and prodrugs and solvates of said compounds. However, the specification fails to teach the preparation or identity of solvates. Therefore, the specification is not adequately enabled for making and/or using solvates.
Identifying an solvates 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 prodrugs and solvates of the instant compounds and compositions.
Applicants have not provided any clear guidance that would provide solvates 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 prodrugs and solvates are suitable for the instant compounds. Generally, prodrugs and solvates 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 are also intended. The nature of solvates 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 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 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. The lack of guidance to prepare any solvates is telling. There is no direction or guidance provided by Applicant to prepare solvates of the instant invention.
Breadth of claims
The breath of the recited compounds and compositions in the claims includes solvates 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 can be used in the instant claim, with no assurance of success. Therefore, applicant must show that the specification teach the preparation of solvates or limit the claims accordingly.
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 1, 3-6, 10 and 14-17 are rejected under 35 U.S.C. 102(a)(1) as being anticipated by Furstner et al. (US Pub. 2015/00148340).
Applicant claims chymase inhibitor compounds, pharmaceutical compositions comprising said compound, and methods for treating thromboembolic disorders of the following formula (I):
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(I)
wherein all the variables are defined in the claims.
This reference discloses chymase inhibitor compounds, pharmaceutical compositions, and methods for treating thromboembolic disorders of formula I. (See Abstract, paragraphs [0008]-[0051], [0359]-[0360], [0377], [0383], [0391], [0393], and pages 149-153, and Examples). The compounds, compositions and methods read on the instant claim. Since this reference teaches the exact compounds and methods, Applicant’s claims are anticipated, and thus, rejected under 35 U.S.C. 102.
Claims 1, 3-6, 10 and 14-17 are rejected under 35 U.S.C. 102(a)(1) as being anticipated by Olenik et al. (US Pub. 2016/0289220).
Applicant claims chymase inhibitor compounds, pharmaceutical compositions comprising said compound, and methods for treating thromboembolic disorders of the following formula (I):
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(I)
wherein all the variables are defined in the claims.
This reference discloses chymase inhibitor compounds, pharmaceutical compositions, and methods for treating thromboembolic disorders of formula I. (See Abstract, paragraphs [0002], [0023]-[0024], [0027], and page 7, and Examples). The compounds, compositions and methods read on the instant claim. Since this reference teaches the exact compounds and methods, Applicant’s claims are anticipated, and thus, rejected under 35 U.S.C. 102.
Claim Rejections - 35 USC § 103
The following is a quotation of 35 U.S.C. 103(a) which forms the basis for all obviousness rejections set forth in this Office action:
(a) A patent may not be obtained though the invention is not identically disclosed or described as set forth in section 102 of this title, if the differences between the subject matter sought to be patented and the prior art are such that the subject matter as a whole would have been obvious at the time the invention was made to a person having ordinary skill in the art to which said subject matter pertains. Patentability shall not be negatived by the manner in which the invention was made.
Claims 1, 3-6, 10 and 14-17 are rejected under 35 U.S.C. 103(a) as being unpatentable over Furstner et al. (US Pub. 2015/00148340).
Applicant claims chymase inhibitor compounds, pharmaceutical compositions comprising said compound, and methods for treating thromboembolic disorders of the following formula (I):
,
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(I)
wherein all the variables are defined in the claim.
This reference discloses a generic group of chymase inhibitor compounds, compositions and methods for treating thromboembolic disorders which embraces Applicants’ claimed compounds. The claims differ from the reference by reciting specific species and a more limited genus than the reference. However, it would have been obvious to one having ordinary skill in the art at the time of the invention to select any of the species of the genus taught by the reference, including those instantly claimed, because the skilled chemist would have the reasonable expectation that any of the species of the genus would have similar properties, and thus, the same use as taught for the genus as a whole. One of ordinary skill in the art would have been motivated to select the claimed compounds from the genus in the reference since such compounds would have been suggested by the reference as a whole. A prior art disclosed genus of useful compounds is sufficient to render prima facie obvious a species falling within a genus. Thus, Applicant’s claims are obvious, and therefore, rejected under 35 U.S.C. 103.
Claims 1, 3-6, 10 and 14-17 are rejected under 35 U.S.C. 103(a) as being unpatentable over Olenik et al. (US Pub. 2016/0289220).
Applicant claims chymase inhibitor compounds, pharmaceutical compositions comprising said compound, and methods for treating thromboembolic disorders of the following formula (I):
,
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154
208
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(I)
wherein all the variables are defined in the claim.
This reference discloses a generic group of chymase inhibitor compounds, compositions and methods for treating thromboembolic disorders which embraces Applicants’ claimed compounds. The claims differ from the reference by reciting specific species and a more limited genus than the reference. However, it would have been obvious to one having ordinary skill in the art at the time of the invention to select any of the species of the genus taught by the reference, including those instantly claimed, because the skilled chemist would have the reasonable expectation that any of the species of the genus would have similar properties, and thus, the same use as taught for the genus as a whole. One of ordinary skill in the art would have been motivated to select the claimed compounds from the genus in the reference since such compounds would have been suggested by the reference as a whole. A prior art disclosed genus of useful compounds is sufficient to render prima facie obvious a species falling within a genus. Thus, Applicant’s claims are obvious, and therefore, rejected under 35 U.S.C. 103.
Double Patenting
Claims 1, 3-6, 10 and 14-17 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-16 of co-pending Application No. 18/854,816.
This is a provisional non-statutory double patenting rejection.
Conclusion
Claims 1, 3-6, 10 and 14-17 are pending. Claims 1, 3-6, 10 and 14-17 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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If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, James Alstrum-Acevedo can be reached at 571-272-5548. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/PAUL V WARD/ Primary Examiner, Art Unit 1622
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