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 .
Status of Claims
Claims 1, 3, 5, 15-16, 18-19, 22-23, 30-31, 35-36, 41, 45-46, and 51-54 are pending in the instant application.
Claims 2, 4, 6-14, 17, 20-21, 24-29, 32-34, 37-40, 42-44, 47-50, and 55-57 have been canceled.
Election/Restriction
This action is in response to an election from a restriction requirement filed on June 11th, 2026. There are 20 claims pending and 16 claims under consideration. Claims 51-54 have been withdrawn as claims drawn to a non-elected invention. This is the first action on the merits. The present invention relates to a compound of formula (I) as recited at instant Claim 1.
Applicant’s election without traverse of Group I, Claims 1, 3, 5, 15-16, 18-19, 22-23, 30-31, 35-36, 41, and 45-46 and species election of
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as a single species of a compound of formula (I) in the reply received August 11th, 2026 is acknowledged. Therefore, the restriction is considered proper and thus made FINAL
The elected species was found to be free of the prior art. Thus, examination was extended to all species of a compound of formula (I).
Priority
Acknowledgement is made of Applicant’s claim for foreign priority based on the IN202241006964 application filed in the Republic of India on February 9th, 2022.
Information Disclosure Statement
The Information Disclosure Statements Received on December 16th, 2024, March 20th, 2025, and March 26th, 2026 have been fully considered by the examiner, except where marked with a strikethrough.
Specification
The specification has not been checked to the extent necessary to determine the presence of all possible minor errors. Applicant’s cooperation is requested in correcting any of the errors of which Applicant may become aware of in the specification.
Claim Objections
Claims 23, 31, 36, and 45 are objected to because of the following informalities:
Claims 23, 31, and 36 include the variable “Ra” in the structural formulae (IA), (IB), and (IC). Claim 1, from which these claims depend, recites this variable as “Ra”. For consistency, the variable recited in claims 23, 31, and 36 should be presented as “Ra”.
Claim 45 refers to compounds 5-6, 33-34, 36-37, 41-42, 44-45 by the identifiers “Isomer-1” and “Isomer-2”. The full structures of the isomers are disclosed in the specification. Per MPEP 2173.05(s), “Where possible, claims are to be complete in themselves. Incorporation by reference to a specific figure or table "is permitted only in exceptional circumstances where there is no practical way to define the invention in words and where it is more concise to incorporate by reference than duplicating a drawing or table into the claim. Incorporation by reference is a necessity doctrine, not for applicant’s convenience." Ex parte Fressola, 27 USPQ2d 1608, 1609 (Bd. Pat. App. & Inter. 1993) (citations omitted).”
Appropriate correction is required.
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, 3, 5, 15-16, 18-19, 22-23, 30-31, 35-36, 41, and 46 are rejected under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, because the specification, while being enabling for a compound of formula (I) in which A is phenyl or pyridinyl, Ra is halogen, R1 is phenyl, methoxy, halo, trifluoromethyl, pyridinyl,
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, wherein phenyl or pyridinyl is optionally substituted by hydroxy, halogen, halomethyl, or methoxy, R2 is H, L is a bond, -N(CH3)=CH2CH2-O-, -O-CH2-, -O-CH2CH2CH2CH2-, -O-CH2CH2-O-,
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,
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,
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,
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, Rd is hydroxy, alkyl, or any two Rd groups attached with the same C atom together form an oxo group, R3 and R8 are isopropyl or isobutyl, R4 and R9 are hydrogen, and R5, R6, R10, and R11 are either hydrogen or methyl does not reasonably provide enablement for compounds of formula (I) in which A, Ra, R1, R2, L, Rd, R3 and R8, R4 and R9, R5, R6, R10, and R11 are otherwise defined. 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.
Pursuant to In re Wands, 858 F.2d 731, 737, 8 USPQ2d 1400, 1404 (Fed. Cir. 1988), one considers the following factors to determine whether undue experimentation is required: (1) The breadth of the claims, (2) The nature of the invention, (3) The state of the prior art, (4) The level of one of ordinary skill, (5) The level of predictability in the art, (6) The amount of direction provided by the inventor, (7) The existence of working examples and (8) The quantity of experimentation needed to make or use the invention based on the content of the disclosure.
Nature of the invention:
The invention is drawn to a compound of formula (I) as recited at instant Claim 1 or a pharmaceutically acceptable salt or stereoisomer or tautomer thereof.
Breadth of the invention:
The scope of the claimed invention is very broad, as it is drawn to compounds of the formula:
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allowing for myriad combinations of the recited variables thereof.
State of the prior art and predictability in the art:
The invention is directed toward medicine and is therefore physiological in nature. 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).
In terms of the law, MPEP 2107.03 states “evidence of pharmacological or other biological activity of a compound will be relevant to an asserted therapeutic use if there is reasonable correlation between the activity in question and the asserted utility. Cross v. Iizuka, 753 F. 2d 1040, 224 USPQ 739 (Fed. Cir. 1985); In re Jolles, 628 F. 2d 1322, 206 USPQ 885 (CCPA 1980); Nelson v. Bowler, 626 F. 2d 853, 206 USPQ 881 (CCPA 1980).” If correlation is lacking, it cannot be relied upon, Ex parte Powers, 220 USPQ 924; Rey-Bellet and Spiegelberg v. Engelhardt v. Schindler, 181 USPQ 453; Knapp v. Anderson, 177 USPQ 688. Indeed, the correlation must have been established “at the time the tests were performed”, Hoffman v. Klaus, 9 USPQ2d 1657.
Level of ordinary skill in the art:
An ordinary artisan in the area of drug development would have experience in synthesizing chemical compounds for particular activities. The synthesis of new drug candidates, while complex, is routine in the art. The process of finding new drugs that have in vitro activity against a particular biological target (i.e., receptor, enzyme, etc.) is well known. Additionally, while high throughput screening assays can be employed, developing a therapeutic method, as claimed, prior to synthesizing and testing compounds is generally not well-known or routine, given the complexity of certain biological systems.
The amount of direction provided and working examples:
The compound core depicted with specific substituents represents a narrow subgenus for which applicant has provided sufficient guidance to make and use; however, this disclosure is not sufficient to allow extrapolation of the limited examples to enable the scope of the compounds instantly claimed. Applicant has provided no working examples of any compounds, compositions, or pharmaceutically acceptable salts in which the variables A, Ra, R1, R2, L, Rd, R3 and R8, R4 and R9, R5, R6, R10, and R11 were not defined as mentioned above in the instant application.
Within the specification, “specific operative embodiments or examples of the invention must be set forth. Examples and description should be of sufficient scope as to justify the scope of the claims.” Markush claims must be provided with support in the disclosure for each member of the Markush group. Where the constitution and formula of a chemical compound is stated only as a probability or speculation, the disclosure is not sufficient to support claims identifying the compound by such composition or formula. See MPEP 608.01(p).
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 that Applicant is not enabled for making these compounds.
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.
(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.
Claims 1, 3, 5, 15-16, 18, and 46 are rejected under 35 U.S.C. 102(a)(1) as being anticipated by Ji et. al. (WO 2020/251971 A1; cited on Applicant’s Information Disclosure Statement filed December 16th, 2024; hereinafter referred to as Ji).
At Page 333, Ji teaches the following compound as I-452:
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This compound reads on a compound of formula (I) as recited at instant Claim 1 when the variables are defined as follows:
A is 5-membered heteroaylenyl.
R1 is 6-membered aryl, wherein aryl is phenyl, substituted with one hydroxy group.
R2 is hydrogen.
Q is amino.
L is -heterocycloalkenyl-(CRxRy)p-, wherein heterocycloalkenyl is piperidinyl, Rx and Ry are each hydrogen, and p is 1.
M is M-1, wherein R3 is alkyl wherein alkyl is isobutyl, R4 is hydrogen, R5 and R6 are each hydrogen, and R7 is thiazolyl substituted with alkyl, wherein alkyl is methyl. Regarding Claim 18, M-1 is
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.
At Page 333, Ji teaches the following compound as I-453:
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This compound reads on a compound of formula (I) as recited at instant Claim 1 when the variables are defined as follows:
A is 5-membered heteroaylenyl.
R1 is 6-membered aryl, wherein aryl is phenyl, substituted with one hydroxy group.
R2 is hydrogen.
Q is amino.
L is -heterocycloalkenyl-(CRxRy)p-, wherein heterocycloalkenyl is piperidinyl, Rx and Ry are each hydrogen, and p is 2.
M is M-1, wherein R3 is alkyl wherein alkyl is isobutyl, R4 is hydrogen, R5 and R6 are each hydrogen, and R7 is thiazolyl substituted with alkyl, wherein alkyl is methyl. Regarding Claim 18, M-1 is
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.
At Page 334, Ji teaches the following compound as I-454:
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This compound reads on a compound of formula (I) as recited at instant Claim 1 when the variables are defined as follows:
A is 5-membered heteroaylenyl.
R1 is 6-membered aryl, wherein aryl is phenyl, substituted with one hydroxy group.
R2 is hydrogen.
Q is amino.
L is -heterocycloalkenyl-(CRxRy)p-, wherein heterocycloalkenyl is piperidinyl, Rx and Ry are each hydrogen, and p is 3.
M is M-1, wherein R3 is alkyl wherein alkyl is isobutyl, R4 is hydrogen, R5 and R6 are each hydrogen, and R7 is thiazolyl substituted with alkyl, wherein alkyl is methyl. Regarding Claim 18, M-1 is
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.
At Page 334, Ji teaches the following compound as I-455:
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This compound reads on a compound of formula (I) as recited at instant Claim 1 when the variables are defined as follows:
A is 5-membered heteroaylenyl.
R1 is 6-membered aryl, wherein aryl is phenyl, substituted with one hydroxy group.
R2 is hydrogen.
Q is amino.
L is -heterocycloalkenyl-(CRxRy)p-, wherein heterocycloalkenyl is piperidinyl, Rx and Ry are each hydrogen, and p is 4.
M is M-1, wherein R3 is alkyl wherein alkyl is isobutyl, R4 is hydrogen, R5 and R6 are each hydrogen, and R7 is thiazolyl substituted with alkyl, wherein alkyl is methyl. Regarding Claim 18, M-1 is
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.
At Page 334, Ji teaches the following compound as I-456:
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This compound reads on a compound of formula (I) as recited at instant Claim 1 when the variables are defined as follows:
A is 5-membered heteroaylenyl.
R1 is 6-membered aryl, wherein aryl is phenyl, substituted with one hydroxy group.
R2 is hydrogen.
Q is amino.
L is -heterocycloalkenyl-(CRxRy)p-, wherein heterocycloalkenyl is piperidinyl, Rx and Ry are each hydrogen, and p is 5.
M is M-1, wherein R3 is alkyl wherein alkyl is isobutyl, R4 is hydrogen, R5 and R6 are each hydrogen, and R7 is thiazolyl substituted with alkyl, wherein alkyl is methyl. Regarding Claim 18, M-1 is
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.
At Page 334, Ji teaches the following compound as I-457:
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This compound reads on a compound of formula (I) as recited at instant Claim 1 when the variables are defined as follows:
A is 5-membered heteroaylenyl.
R1 is 6-membered aryl, wherein aryl is phenyl, substituted with one hydroxy group.
R2 is hydrogen.
Q is amino.
L is -heterocycloalkenyl-(CRxRy)p-, wherein heterocycloalkenyl is piperidinyl, Rx and Ry are each hydrogen, and p is 1. Regarding Claim 15, L is
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M is M-1, wherein R3 is alkyl wherein alkyl is isobutyl, R4 is hydrogen, R5 and R6 are each hydrogen, and R7 is thiazolyl substituted with alkyl, wherein alkyl is methyl. Regarding Claim 18, M-1 is
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At Page 335, Ji teaches the following compound as I-458:
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This compound reads on a compound of formula (I) as recited at instant Claim 1 when the variables are defined as follows:
A is 5-membered heteroaylenyl.
R1 is 6-membered aryl, wherein aryl is phenyl, substituted with one hydroxy group.
R2 is hydrogen.
Q is amino.
L is -heterocycloalkenyl-(CRxRy)p-, wherein heterocycloalkenyl is piperidinyl, Rx and Ry are each hydrogen, and p is 2. Regarding Claim 15, L is
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M is M-1, wherein R3 is alkyl wherein alkyl is isobutyl, R4 is hydrogen, R5 and R6 are each hydrogen, and R7 is thiazolyl substituted with alkyl, wherein alkyl is methyl. Regarding Claim 18, M-1 is
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At Page 335, Ji teaches the following compound as I-459:
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This compound reads on a compound of formula (I) as recited at instant Claim 1 when the variables are defined as follows:
A is 5-membered heteroaylenyl.
R1 is 6-membered aryl, wherein aryl is phenyl, substituted with one hydroxy group.
R2 is hydrogen.
Q is amino.
L is -heterocycloalkenyl-(CRxRy)p-, wherein heterocycloalkenyl is piperidinyl, Rx and Ry are each hydrogen, and p is 3. Regarding Claim 15, L is
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M is M-1, wherein R3 is alkyl wherein alkyl is isobutyl, R4 is hydrogen, R5 and R6 are each hydrogen, and R7 is thiazolyl substituted with alkyl, wherein alkyl is methyl. Regarding Claim 18, M-1 is
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At Page 335, Ji teaches the following compound as I-460:
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This compound reads on a compound of formula (I) as recited at instant Claim 1 when the variables are defined as follows:
A is 5-membered heteroaylenyl.
R1 is 6-membered aryl, wherein aryl is phenyl, substituted with one hydroxy group.
R2 is hydrogen.
Q is amino.
L is -heterocycloalkenyl-(CRxRy)p-, wherein heterocycloalkenyl is piperidinyl, Rx and Ry are each hydrogen, and p is 4.
M is M-1, wherein R3 is alkyl wherein alkyl is isobutyl, R4 is hydrogen, R5 and R6 are each hydrogen, and R7 is thiazolyl substituted with alkyl, wherein alkyl is methyl. Regarding Claim 18, M-1 is
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At Page 335, Ji teaches the following compound as I-461:
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This compound reads on a compound of formula (I) as recited at instant Claim 1 when the variables are defined as follows:
A is 5-membered heteroaylenyl.
R1 is 6-membered aryl, wherein aryl is phenyl, substituted with one hydroxy group.
R2 is hydrogen.
Q is amino.
L is -heterocycloalkenyl-(CRxRy)p-, wherein heterocycloalkenyl is piperidinyl, Rx and Ry are each hydrogen, and p is 5.
M is M-1, wherein R3 is alkyl wherein alkyl is isobutyl, R4 is hydrogen, R5 and R6 are each hydrogen, and R7 is thiazolyl substituted with alkyl, wherein alkyl is methyl. Regarding Claim 18, M-1 is
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.
Regarding Claim 46, Ji teaches pharmaceutical compositions comprising these compounds at Page 405, Paragraph [00560].
Conclusion
Claims 1, 3, 5, 15-16, 18-19, 22-23, 30-31, 35-36, 41, and 46 are rejected. Claim 45 is objected to.
No claim is allowed.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to DANIEL JOHN BURKETT whose telephone number is (703)756-5390. The examiner can normally be reached Monday - Friday.
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/D.J.B./ Examiner, Art Unit 1624
/BRENDA L COLEMAN/ Primary Examiner, Art Unit 1624
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