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 .
Priority
U.S. Pat. Appln. Ser. No.: 18/700,110, Filed: 04/10/2024 is a 371 Nat.’l Stage Entry of PCT/US2022/046760, Intern.’l Filing Date: 10/14/2022, which claims priority from U.S. Prov. Appln. 63/300,826, Filed: 01/19/2022 and U.S. Prov. Appln. 63/255,899, Filed: 10/14/2021
Status
The present office action is in responsive to April 10, 2024 Preliminary Amendment and corresponding miscellaneous documents.
Claims 1-6, 8-10, 12-13, 15-19, 21, 23 and 26-28 are pending/under examination, claims 2-6, 9, 12-13,15-18 and 21 are original, claims 1, 8, 10, 19, 23 and 26-28 are currently amended, claims 7, 11, 14, 20, 22 and 24-25 are cancelled in the above-identified application.
Information Disclosure Statement
An Information Disclosure Statements (IDS) submitted on February 6, 2025 is in compliance with the provisions of 37 CFR 1.97.
Accordingly, Information Disclosure Statements have been considered by the Examiner.
Claim Rejections - 35 USC § 102
In the event the determination of the status of the application as subject to AIA 35 U.S.C. 102 and 103 (or as subject to pre-AIA 35 U.S.C. 102 and 103) is incorrect, any correction of the statutory basis (i.e., changing from AIA to pre-AIA ) for the rejection will not be considered a new ground of rejection if the prior art relied upon, and the rationale supporting the rejection, would be the same under either status.
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 –
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.
(a)(2) the claimed invention was described in a patent issued under section 151, or in an application for patent published or deemed published under section 122(b), in which the patent or application, as the case may be, names another inventor and was effectively filed before the effective filing date of the claimed invention.
Claim(s) 1, 3-4, 8 and 26-27 are rejected under 35 U.S.C. 102(a)(1) and 102(a)(2) as being anticipated by:
WO 2021/127265 A1 (CHDI FOUNDATION INC [US]) 24 June 2021 (2021-06-24 “WO ‘265 Appln”) .
[a] The WO ‘265 Appln. disclose and teaches:
7,8-dihydro-5H-1,6-naphthyridine derivatives (i.e., e.g. page 103, example 27; which reads on claims 1, 3, 8 and 26);
corresponding pharmaceutical compositions (i.e., which reads on claim 27); and
treatment methods for treating neurological disorders (i.e., which reads on claim 28 given that HD is an example of a neurological disease)
of the present invention.
WO ‘265 Appln. also teaches specific examples at page 103, example 27 (i.e., which reads on claims 1, 4, 8 and 26;
Example 27: 6-(5-Methoxypyridin-2-yl)-3-[(5-methoxypyridin-2-yl)methoxy]-5,6,7,8-tetrahydro- 1,6-naphthyridine
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750
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[AltContent: ]where: G1 =
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, R6 = R5= R4 = H, R8= -OMe, Z1 = CR1, Z3 = CR3 (i.e., R1= R3 = H),
Z2 = CR2 , R2 =
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, (R7)n, n=0.
.
Therefore, WO ‘265 Appln. anticipates the claimed invention .
Claims 1-3, 23 and 26-27 are rejected under 35 U.S.C. 102(a)(1) and 102(a)(2) are anticipated by WO 2021/122064 A1 (NEUROSEARCH AS [DK]) 28 October 2010 (“WO ‘264 Appln”)
[a] WO ‘064 Appln. discloses:
7,8-dihydro-5H-1,6-naphthyridine derivatives; i.e., e.g., see page 38, example 2; claims 1, 9 to 12, 15 and 16).
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G1 =
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, R2 = Cl, R5=CH3, R6 = H,
R4= G3 =
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333
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substituted with halogen= pyrrolidine sub with Cl
R8=
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,
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corresponding pharmaceutical compositions (i.e., see page 20, lines 24-37 to page 25, lines 1-8, i.e., which reads on claim 27); and
treatment methods for treating neurological disorders and psychiatric disorders or disease (i.e., see generally at page 17, lines 19 to page 19, lines 1-19,:
Therefore, WO 2021/122064 A1. anticipates the claimed invention
Claim Rejections - 35 USC § 103
In the event the determination of the status of the application as subject to AIA 35 U.S.C. 102 and 103 (or as subject to pre-AIA 35 U.S.C. 102 and 103) is incorrect, any correction of the statutory basis (i.e., changing from AIA to pre-AIA ) for the rejection will not be considered a new ground of rejection if the prior art relied upon, and the rationale supporting the rejection, would be the same under either status.
The following is a quotation of 35 U.S.C. 103 which forms the basis for all obviousness rejections set forth in this Office action:
A patent for a claimed invention may not be obtained, notwithstanding that the claimed invention is not identically disclosed as set forth in section 102, if the differences between the claimed invention and the prior art are such that the claimed invention as a whole would have been obvious before the effective filing date of the claimed invention to a person having ordinary skill in the art to which the claimed invention pertains. Patentability shall not be negated by the manner in which the invention was made.
The factual inquiries for establishing a background for determining obviousness under 35 U.S.C. 103 are summarized as follows:
1. Determining the scope and contents of the prior art.
2. Ascertaining the differences between the prior art and the claims at issue.
3. Resolving the level of ordinary skill in the pertinent art.
4. Considering objective evidence present in the application indicating obviousness or nonobviousness.
This application currently names joint inventors. In considering patentability of the claims the examiner presumes that the subject matter of the various claims was commonly owned as of the effective filing date of the claimed invention(s) absent any evidence to the contrary. Applicant is advised of the obligation under 37 CFR 1.56 to point out the inventor and effective filing dates of each claim that was not commonly owned as of the effective filing date of the later invention in order for the examiner to consider the applicability of 35 U.S.C. 102(b)(2)(C) for any potential 35 U.S.C. 102(a)(2) prior art against the later invention.
Claim 28 is rejected under 35 U.S.C. 103 as being unpatentable over:
[a] WO 2021/127265 A1 (CHDI FOUNDATION INC [US]) 24 June 2021 (2021-06-24 “WO ‘265); and
[b] WO 2021/122064 A1 (NEUROSEARCH AS [DK]) 28 October 2010 (“WO ‘264 ),
each further in view of:
[c] Erskine et al., Drug Discovery Today, Vol 24, Iss. 12, Dec 2019, pp. 2307-2314; and/or
[d] Scarr, CNS Neuroscience and Therapeutics, 26 Feb 2011, 18: 369-379,
https://doi.org/10.1111/j.1755-5949.2011.00249.x
The teachings of WO ‘265 and WO ‘064 Applns. are set forth in rejections supra, which are incorporated herein by reference in its entirety.
While the WO ‘265 and WO ‘264 Applns., respectively, disclose treating a neurological and/or psychiatric disorder with 7,8-dihydro-5H-1,6-naphthyridine compounds derivatives as previously discussed, neither of the aforementioned patent applications:
explicitly disclose method of treating a subset of neurological and/or psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction in a mammal.
However, it is conventionally known in the art that muscarinic acetylcholine receptor (“MAR”) dysfunction is linked to, but is not limited to, the neurological or psychiatric diseases or disorders as taught by these references:
[c] Erskine teaches that:
cholinergic dysfunction is involved in a range of neurological and psychiatric disorders and discussed how “targeted cholinergic therapeutics to the muscarinic receptor subtypes [are] vital in treating several disorders associated with cognitive dysfunction and behavioral and psychological symptoms (i.e., see, Abstract lines 7-9 at p. 2307)”;
that in a “in a larger sample of postmortem schizophrenia brain tissues, large reductions (60–80%) in M1/4 receptor binding as measured by [3H]pirenzepine) in the cortex were found in a subgroup comprising ∼25% of patients who were defined as having a muscarinic receptor-deficit schizophrenia (MRDS) (i.e., see, therein at col. 1, lines 24-29” at p. 2309); i.e., e.g.:
considerable literature implicating cholinergic muscarinic receptor dysfunction, in cognitive and neuropsychiatric features of psychiatric and neurodegenerative disorders” (i.e., Schizophrenia and dementia, LBD (collective term for Parkinson’s disease (PD), Parkinson’s disease dementia (PDD), and dementia with Lewy bodies (DLB) (i.e., see Erskine Abstract at page 2307 and Concluding Remarks Section and at p. 2313, col 1., and Summary Section at col, 1, page 2310 therein); and
[d] Scarr, a comprehensive review article. also teaches:
muscarinic acetylcholine receptors and roles in central nervous system (CNS) disorders (i.e., see Scarr summary at page 1) “discussing data implicating them in the pathophysiology of psychiatric disorders, such as schizophrenia, bipolar disorder, major depressive disorder (MDD), and substance abuse, as well as neurological diseases such as Alzheimer's and Parkinson's diseases (i.e., see introduction at page”; and that
therapeutic potential appears to be targeted by specific muscarinic receptor subtypes M1 to M 5 to treat CNS disorders (i.e., as discussed throughout this reference and summarized at col. 2, last para. at page 376).
Based on the foregoing, it would have been prima facie obvious to treat the subset of patients having neurological disorders associated with MAR dysfunction, because the WO '264 and ‘265 Applns., respectively teach administering 8-dihydro-5H-1,6-naphthyridine derivatives to patients are effective to ameliorate symptoms of neurological and/or psychiatric disorders, i.e., e.g., as Erskin and Scarr indicate human patients with cholinergic muscarinic receptor dysfunction, suffer from cognitive and neuropsychiatric features of psychiatric and neurodegenerative disorders” (i.e., which include, but are not limited to Alzheimer's, Schizophrenia and dementia, LBD (collective term for Parkinson’s disease (PD), Parkinson’s disease dementia (PDD), and dementia with Lewy bodies (DLB)of NDD sufferers, bipolar disorder, major depressive disorder (MDD), and substance abuse, etc.)
One of skill in the art would have a reasonable expectation of success in adapting the potent, selective mAChR M4 8-dihydro-5H-1,6-naphthyridine derivatives to treat the subset of patients having neurological disorders associated with MAR dysfunction,as taught in WO '264 and ‘265 Applns., because the patient subset with muscarinic receptor dysfunction exhibits the same or similar symptoms as the broader patient population addressed in the prior art, where compounds efficacious in treatment of one sub-group of MRD patients would necessarily be expected to be efficacious in the other broader group with general neurological and/or psychiatric disorders, vice versa.
One of skill in the art would have been motivated in adapting or treat patients with potent and selective mAChR M4 8-dihydro-5H-1,6-naphthyridine derivative compounds as taught by WO ‘265 and ‘264 Applns., due to positive results indicating efficacious treatment of neurological and/or psychiatric disorders patients (i.e., where subset of muscarinic AChR dysfunction patients exhibit same symptoms as the broader population, use of same compounds would necessarily be efficacious in treating both broader and sub patient populations, who present same/similar disease symptoms) as taught by Erskine and Scarr in the development of alternative treatment methods to encompass a wider ranging patient population.
The claimed invention is rendered obvious over WO ‘265 and ‘264 Applns. in view of the teachings of Erksine and Scarr.
Allowable Subject Matter
Claims 5-6, 9-10, 12-13, 15-19 and 21 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.
Relevant Prior Art
The prior art made of record and not relied upon is considered pertinent to applicant's disclosure:
CN 103 694 163 A (SHANGHAI SIMCERE DRUG RES CO LTD; JIANGSU SIMCERE PHARM RES CO) 2 April 2014 (2014-04-02) “CN163 A”
CN 163 A teaches the following compound shown below (i.e., see therein at page 10, 5th line compound 2):
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,
[AltContent: textbox ()][AltContent: textbox (4)][AltContent: textbox ()][AltContent: textbox ()][AltContent: textbox ()][AltContent: textbox ()]which teaches moiety G1 =
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is defined as attached at a fixed and different position of the pyrimidine ring resulting in a different isomeric compound (i.e., attached to a different position of the pyrimidine ring excluded as a possible attachment position as per definitions of instant application)
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R50 = G30 ≠ G3 ≠ -C1-3-alkenylene-G3 or -O-C1-3-alkenylene-G3
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to form corresponding pharmaceutical compositions and treatment methods for the following diseases epilepsy, inflammatory pain, neuropathic pain, migraine, neurodegenerative diseases, anxiety disorders (i.e., which correspond to those diseases taught in the instant claims invention).
CONCLUSION
Claims 1-6,8-10,12-13,15-19,21,23 and 26-28 are rejected in this action.
Any inquiry concerning this communication or earlier communications from the Examiner should be directed to GRACE C HSU whose telephone number is (571) 270-1689.
The Examiner can normally be reached Monday-Friday 7:30 am - 6 pm. Examiner interviews are available via telephone, in-person, and video conferencing using a USPTO supplied web-based collaboration tool. To schedule an interview, Applicants is encouraged to use the USPTO Automated Interview Request (AIR) at http://www.uspto.gov/interviewpractice.
If attempts to reach the Examiner by telephone are unsuccessful, the Examiner’s supervisor, KORTNEY L. KLINKEL can be reached on 571-270-5239. Information regarding the status of published or unpublished applications may be obtained from Patent Center. Unpublished application information in Patent Center is available to registered users. To file and manage patent submissions in Patent Center, visit: https://patentcenter.uspto.gov. Visit https://www.uspto.gov/patents/apply/patent-center for more information about Patent Center and https://www.uspto.gov/patents/docx for information about filing in DOCX format. For additional questions, contact the Electronic Business Center (EBC) at 866-217-9197 (toll-free). If you would like assistance from a USPTO Customer Service Representative, call 800-786-9199 (IN USA OR CANADA) or 571-272-1000.
/G.C.H./
Examiner, Art Unit 1627
/SCARLETT Y GOON/Supervisory Patent Examiner, Art Unit 1693
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