DETAILED ACTION
Notice of Pre-AIA or AIA Status
The inventor or joint inventor should note that the instant invention, filed on or after March 16, 2013, is being examined under the first inventor to file provisions of the AIA .
Status of the Claims
Claims 1, 3, 8, 24, 26, 28, 29, 31, 36, 41, 44, 48, 51, 53, 57, 62 and 63 are pending in the instant invention. According to the Amendments to the Claims, filed June 22, 2026, claims 1 and 41 were amended and claims 2, 4-7, 9-23, 25, 27, 30, 32-35, 37-40, 42, 43, 45-47, 49, 50, 52, 54-56, 58-61, 64 and 65 were cancelled.
Status of Priority
This invention is a 35 U.S.C. § 371 National Stage Filing of International Application No. PCT/CN2022/126096, filed October 19, 2022, which claims priority under 35 U.S.C. § 119(a-d) to: a) International Application No. PCT/CN2022/116510, filed September 1, 2022; and b) International Application No. PCT/CN2021/125035, filed October 20, 2021.
Restrictions / Election of Species
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The inventor’s or joint inventor’s provisional election of the following, without traverse, in the reply filed on June 22, 2026, is acknowledged: a) Group I - claims 1, 3, 8, 24, 26, 28, 29, 31, 36, 41, 44, 48, 51, 53, 57 and 62; and b) substituted heteroaryl of Formula (I) - p. 99, Example 33, Compound 33, shown to the right below, and hereafter referred to as 1-(2-methylpyridin-3-yl)-4-(prop-2-yn-1-ylamino)-7-(trifluoro-methyl)quinazolin-2(1H)-one, where m = 1; n = 1; R1 = -H; R2 = -H; R3 = -H; X = -NR4-, wherein R4 = -H; Z3 = CR6, wherein R6 =-H; Z1 = CR7, wherein R7 =-H; Z2 = CR9, wherein R9 =-H; R8 = -CF3; ring A= -pyridin-3-yl; and at C-2, R14 = -CH3. Claims 1, 3, 8, 24, 26, 29, 31, 36, 41, 44, 48, 51, 53, 57 and 62 read on the elected species. Affirmation of this
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election must be made by the inventor or joint inventor in replying to this Office action.
Similarly, the inventor or joint inventor should further note that the requirement is still deemed proper and is therefore made FINAL.
Likewise, the inventor or joint inventor should further note that the elected species, shown to the right, was found to be free of the prior art. Thus, the examiner has expanded the forthcoming prosecution to include all claims relevant to the genus of Group I, for a first Office action and prosecution on the merits.
Moreover, the inventor or joint inventor should further note that claim 63 was withdrawn from further consideration, pursuant to 37 CFR 1.142(b), as being drawn to a nonelected or cancelled invention, there being no allowable generic or linking claim.
Thus, a first Office action and prosecution on the merits of claims 1, 3, 8, 24, 26, 28, 29, 31, 36, 41, 44, 48, 51, 53, 57 and 62 is contained within.
Specification Objection - Disclosure
The inventor or joint inventor is advised to format the specification according to 37 CFR 1.77(c). Revisions should particularly address bold-type, underline, and/or upper case formatting. Appropriate correction may be required.
Specification Objection - Title
The inventor or joint inventor is reminded of the proper content of the title of the invention.
The title of the invention should be brief, but technically accurate and descriptive and should contain fewer than 500 characters. See 37 CFR 1.72(a) and MPEP § 606.
The title of the invention is not technically accurate and descriptive. A new title is required that is clearly indicative of the invention to which the claims are directed. In the revised title, the examiner suggests additionally identifying the substituted heteroaryls of the Formula (I).
The following title is suggested: SUBSTITUTED QUINAZOLINES, PYRIDO[2,3-d]PYRIMIDINES, PYRIDO[3,2-d]PYRIMIDINES, PYRIDO[2,3-d]PYRIMIDINES, AND PYRIMIDO[4,5-d]PYRIMIDINES AS METHIONINE ADENOSYL TRANSFERASE 2A (MAT2A) INHIBITORS.
Appropriate correction is required.
Specification Objection - Abstract
The inventor or joint inventor is reminded of the proper content of an abstract of the disclosure.
With regard particularly to chemical patents, for compounds or compositions, the general nature of the compound or composition should be given as well as the use thereof, e.g., The compounds are of the class of alkyl benzene sulfonyl ureas, useful as oral anti-diabetics. Exemplification of a species could be illustrative of members of the class. For processes, the reactions, reagents and process conditions should be stated, generally illustrated by a single example, unless variations are necessary. See MPEP § 608.01(b), Section B.
The abstract of the disclosure is objected to because it fails to exemplify any members or formulae illustrative of its class. Correction is required. See MPEP § 608.01(b).
The examiner suggests incorporating the structure of Formula (I) into the abstract, to overcome this objection.
Claim Objections
Claim 1 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b), the existing recitation should be replaced with the following recitation:
A compound of Formula (I):
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Formula (I)
or a pharmaceutically acceptable salt or stereoisomer thereof,
wherein:
R1 is H, halogen, C1-6 alkyl, C1-6 haloalkyl, CH2C(O)NR10R11, CH2NR12C(O)R13, CH2S(O)2R13, CH2S(O)2NR10R11, C2-6 alkenyl, C2-6 alkynyl, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, Si(C1-6 alkyl)3, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, S(O)2NR10R11, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl is optionally substituted with one, two, or three independently selected R15a substituents;
each R15a is independently halogen, CN, C1-6 alkyl, CH2C(O)NR10R11, CH2NR12C(O)R13, CH2S(O)2R13, CH2S(O)2NR10R11, CH2-C3-6 cycloalkyl, CH2-C2-9 heterocycloalkyl, CH2-C6-10 aryl, CH2-C1-9 heteroaryl, C2-6 alkenyl, C2-6 alkynyl, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, =O, Si(C1-6 alkyl)3, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, S(O)2NR10R11, C3-10 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl;
wherein each C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl is optionally and independently substituted with one, two, or three substituents independently selected from the group consisting of halogen, CN, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, =O, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, and S(O)2NR10R11; and
wherein each C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, and C1-9 heteroaryl is optionally and independently substituted with one, two, or three substituents independently selected from the group consisting of halogen, CN, C1-6 alkyl, C1-6 haloalkyl, CH2C(O)NR10R11, CH2NR12C(O)R13, CH2S(O)2R13, CH2S(O)2NR10R11, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, =O, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, and S(O)2NR10R11;
each R2 is independently H, halogen, C1-6 alkyl, C1-6 haloalkyl, CH2C(O)NR10R11, CH2NR12C(O)R13, CH2S(O)2R13, CH2S(O)2NR10R11, C2-6 alkenyl, C2-6 alkynyl, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, =O, Si(C1-6 alkyl)3, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, S(O)2NR10R11, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl, wherein each C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, and C1-9 heteroaryl is optionally and independently substituted with one, two, or three independently selected R15b substituents;
each R3 is independently H, halogen, C1-6 alkyl, C1-6 haloalkyl, CH2C(O)NR10R11, CH2NR12C(O)R13, CH2S(O)2R13, CH2S(O)2NR10R11, C2-6 alkenyl, C2-6 alkynyl, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, =O, Si(C1-6 alkyl)3, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, S(O)2NR10R11, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl, wherein each C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, and C1-9 heteroaryl is optionally and independently substituted with one, two, or three independently selected R15b substituents; or
any R2 and R3, taken together with the carbon atom to which they are attached, independently forms a C3-6 cycloalkyl or C2-9 heterocycloalkyl;
each R15b is independently halogen, CN, C1-6 alkyl, CH2C(O)NR10R11, CH2NR12C(O)R13, CH2S(O)2R13, CH2S(O)2NR10R11, CH2-C3-6 cycloalkyl, CH2-C2-9 heterocycloalkyl, CH2-C6-10 aryl, CH2-C1-9 heteroaryl, C2-6 alkenyl, C2-6 alkynyl, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, =O, Si(C1-6 alkyl)3, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, S(O)2NR10R11, C3-10 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl;
wherein each C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl is optionally and independently substituted with one, two, or three substituents independently selected from the group consisting of halogen, CN, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, =O, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, and S(O)2NR10R11; and
wherein each C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, and C1-9 heteroaryl is optionally and independently substituted with one, two, or three substituents independently selected from the group consisting of halogen, CN, C1-6 alkyl, C1-6 haloalkyl, CH2C(O)NR10R11, CH2NR12C(O)R13, CH2S(O)2R13, CH2S(O)2NR10R11, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, =O, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, and S(O)2NR10R11;
n is 0, 1, 2, 3, 4, 5, or 6;
X is -CR5R5a-, -NR4-, or -O-;
R4 is H, halogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl;
wherein the C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl is optionally substituted with one, two, or three substituents independently selected from the group consisting of halogen, CN, OH, OC1-6 alkyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, and C1-9 heteroaryl; and
wherein the C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl is optionally substituted with one, two, or three substituents independently selected from the group consisting of halogen, CN, C1-6 alkyl, C1-6 haloalkyl, OH, OC1-6 alkyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, and C1-9 heteroaryl; or
R4 and R3, taken together with the carbon atom and nitrogen atom to which they are attached, form a C2-9 heterocycloalkyl, wherein the C2-9 heterocycloalkyl is optionally substituted with one, two, or three substituents independently selected from the group consisting of halogen, CN, C1-6 alkyl, C1-6 haloalkyl, OH, OC1-6 alkyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, and C1-9 heteroaryl;
R5 is H, halogen, C1-6 alkyl, C1-6 haloalkyl, CH2C(O)NR10R11, CH2NR12C(O)R13, CH2S(O)2R13, CH2S(O)2NR10R11, C2-6 alkenyl, C2-6 alkynyl, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, Si(C1-6 alkyl)3, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, S(O)2NR10R11, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl;
wherein the C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl is optionally substituted with one, two, or three substituents independently selected from the group consisting of halogen, CN, OH, OC1-6 alkyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, and C1-9 heteroaryl; and
wherein the C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl is optionally substituted with one, two, or three substituents independently selected from the group consisting of halogen, CN, C1-6 alkyl, C1-6 haloalkyl, OH, OC1-6 alkyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, and C1-9 heteroaryl;
R5a is H, halogen, C1-6 alkyl, C1-6 haloalkyl, CH2C(O)NR10R11, CH2NR12C(O)R13, CH2S(O)2R13, CH2S(O)2NR10R11, C2-6 alkenyl, C2-6 alkynyl, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, Si(C1-6 alkyl)3, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, S(O)2NR10R11, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl;
wherein the C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl is optionally substituted with one, two, or three substituents independently selected from the group consisting of halogen, CN, OH, OC1-6 alkyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, and C1-9 heteroaryl; and
wherein the C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl is optionally substituted with one, two, or three substituents independently selected from the group consisting of halogen, CN, C1-6 alkyl, C1-6 haloalkyl, OH, OC1-6 alkyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, and C1-9 heteroaryl;
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is:
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,
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,
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,
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, or
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;
R6 is H, halogen, CN, C1-6 alkyl, C1-6 haloalkyl, CH2C(O)NR10R11, CH2NR12C(O)R13, CH2S(O)2R13, CH2S(O)2NR10R11, C2-6 alkenyl, C2-6 alkynyl, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, Si(C1-6 alkyl)3, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, S(O)2NR10R11, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl is optionally substituted with one, two, or three independently selected R15c substituents;
R7 is H, halogen, CN, C1-6 alkyl, C1-6 haloalkyl, CH2C(O)NR10R11, CH2NR12C(O)R13, CH2S(O)2R13, CH2S(O)2NR10R11, C2-6 alkenyl, C2-6 alkynyl, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, Si(C1-6 alkyl)3, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, S(O)2NR10R11, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl is optionally substituted with one, two, or three independently selected R15c substituents;
R8 is H, halogen, CN, C1-6 alkyl, C1-6 haloalkyl, CH2C(O)NR10R11, CH2NR12C(O)R13, CH2S(O)2R13, CH2S(O)2NR10R11, C2-6 alkenyl, C2-6 alkynyl, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, Si(C1-6 alkyl)3, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, S(O)2NR10R11, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl is optionally substituted with one, two, or three independently selected R15c substituents;
R9 is H, halogen, CN, C1-6 alkyl, C1-6 haloalkyl, CH2C(O)NR10R11, CH2NR12C(O)R13, CH2S(O)2R13, CH2S(O)2NR10R11, C2-6 alkenyl, C2-6 alkynyl, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, Si(C1-6 alkyl)3, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, S(O)2NR10R11, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl is optionally substituted with one, two, or three independently selected R15c substituents;
each R15c is independently halogen, CN, C1-6 alkyl, CH2C(O)NR10R11, CH2NR12C(O)R13, CH2S(O)2R13, CH2S(O)2NR10R11, CH2-C3-6 cycloalkyl, CH2-C2-9 heterocycloalkyl, CH2-C6-10 aryl, CH2-C1-9 heteroaryl, C2-6 alkenyl, C2-6 alkynyl, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, =O, Si(C1-6 alkyl)3, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, S(O)2NR10R11, C3-10 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl;
wherein each C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl is optionally and independently substituted with one, two, or three substituents independently selected from the group consisting of halogen, CN, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, =O, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, and S(O)2NR10R11; and
wherein each C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, and C1-9 heteroaryl is optionally and independently substituted with one, two, or three substituents independently selected from the group consisting of halogen, CN, C1-6 alkyl, C1-6 haloalkyl, CH2C(O)NR10R11, CH2NR12C(O)R13, CH2S(O)2R13, CH2S(O)2NR10R11, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, =O, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, and S(O)2NR10R11;
each R10 is independently H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl;
wherein each C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl is optionally and independently substituted with one, two, or three substituents independently selected from the group consisting of halogen, CN, OH, OC1-6 alkyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, and C1-9 heteroaryl; and
wherein each C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, and C1-9 heteroaryl is optionally and independently substituted with one, two, or three substituents independently selected from the group consisting of halogen, CN, C1-6 alkyl, C1-6 haloalkyl, OH, OC1-6 alkyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, and C1-9 heteroaryl;
each R11 is independently H, C1-6 alkyl, or C1-6 haloalkyl; or
any R10 and R11, taken together with the nitrogen atom to which they are attached, independently forms a C2-9 heterocycloalkyl;
each R12 is independently H, C1-6 alkyl, or C1-6 haloalkyl;
each R13 is independently C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl;
wherein each C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl is optionally and independently substituted with one, two, or three substituents independently selected from the group consisting of halogen, CN, OH, OC1-6 alkyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, and C1-9 heteroaryl; and
wherein each C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, and C1-9 heteroaryl is optionally and independently substituted with one, two, or three substituents independently selected from the group consisting of halogen, CN, C1-6 alkyl, C1-6 haloalkyl, OH, OC1-6 alkyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, and C1-9 heteroaryl;
ring A is C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-10 heteroaryl;
each R14 is independently halogen, C1-6 alkyl, C1-6 haloalkyl, CH2C(O)NR10R11, CH2NR12C(O)R13, CH2S(O)2R13, CH2S(O)2NR10R11, C2-6 alkenyl, C2-6 alkynyl, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, Si(C1-6 alkyl)3, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, S(O)2NR10R11, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl, wherein each C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl is optionally substituted with one, two, or three independently selected R15d substituents;
m is 0, 1, 2, 3, 4, or 5; and
each R15d is independently halogen, CN, C1-6 alkyl, CH2C(O)NR10R11, CH2NR12C(O)R13, CH2S(O)2R13, CH2S(O)2NR10R11, CH2-C3-6 cycloalkyl, CH2-C2-9 heterocycloalkyl, CH2-C6-10 aryl, CH2-C1-9 heteroaryl, C2-6 alkenyl, C2-6 alkynyl, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, =O, Si(C1-6 alkyl)3, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, S(O)2NR10R11, C3-10 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl;
wherein each C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl is optionally and independently substituted with one, two, or three substituents independently selected from the group consisting of halogen, CN, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, =O, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, and S(O)2NR10R11; and
wherein each C3-6 cycloalkyl, C2-9 heterocycloalkyl, C6-10 aryl, and C1-9 heteroaryl is optionally and independently substituted with one, two, or three substituents independently selected from the group consisting of halogen, CN, C1-6 alkyl, C1-6 haloalkyl, CH2C(O)NR10R11, CH2NR12C(O)R13, CH2S(O)2R13, CH2S(O)2NR10R11, NR10R11, NR12C(O)R13, NR12C(O)NR10R11, NR12C(O)OR13, NR12S(O)2R13, N=S(O)R13R13, C(O)R13, C(O)C(O)NR10R11, C(O)NR10R11, C(O)OR10, OR10, OC(O)R13, OC(O)NR10R11, =O, P(O)R10R10, SR10, SF5, S(O)R13, S(NR13)(O)R13, S(NH)(O)CR10R10R11, S(NH)(O)NR10R11, S(O)2R13, and S(O)2NR10R11;
with the provisos that:
(1) if R2 is =O, then R3 is absent; and
(2) if R3 is =O, then R2 is absent.
Appropriate correction is required. See MPEP § 2173.02.
Claim 3 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation:
The compound of claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein:
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is:
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,
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,
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, or
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; and
R6 is H, halogen, CN, C1-6 alkyl, C1-6 haloalkyl, NR10R11, or OR10.
Appropriate correction is required. See MPEP § 2173.02.
Claim 8 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation:
The compound of claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein:
X is -NR4-; and
R4 is H or C1-6 alkyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 24 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation:
The compound of claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein each R2 is independently H or C1-6 alkyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 26 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation:
The compound of claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein each R2 is independently H or C1-6 alkyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 28 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation:
The compound of claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein any R2 and R3, taken together with the carbon atom to which they are attached, independently forms a C3-6 cycloalkyl or C2-9 heterocycloalkyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 31 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation:
The compound of claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein:
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,
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, or
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; and
R7 is H, halogen, CN, C1-6 alkyl, C1-6 haloalkyl, NR10R11, or OR10.
Appropriate correction is required. See MPEP § 2173.02.
Claim 36 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation:
The compound of claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein:
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; and
R9 is H, halogen, CN, C1-6 alkyl, C1-6 haloalkyl, NR10R11, or OR10.
Appropriate correction is required. See MPEP § 2173.02.
Claim 41 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation:
The compound of claim 1, wherein the compound is of Formula (Ib):
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Formula (Ib)
or a pharmaceutically acceptable salt or stereoisomer thereof.
Appropriate correction is required. See MPEP § 2173.02.
Claim 44 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation:
The compound of claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein ring A is phenyl or C1-10 heteroaryl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 48 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation:
The compound of claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein each R14 is independently halogen, C1-6 alkyl, C1-6 haloalkyl, NR10R11, or OR10.
Appropriate correction is required. See MPEP § 2173.02.
Claim 51 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation:
The compound of claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein m is 1.
Appropriate correction is required. See MPEP § 2173.02.
Claim 53 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation:
The compound of claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R8 is H, halogen, CN, C1-6 alkyl, C1-6 haloalkyl, OR10, or C3-6 cycloalkyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 57 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation:
The compound of claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R1 is H, or C3-6 cycloalkyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 62 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation:
A pharmaceutical composition comprising at least one pharmaceutically acceptable excipient and a compound of claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof.
Appropriate correction is required. See MPEP § 2173.02.
Claim Rejections - 35 U.S.C. § 112(a)
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.
Substituted heteroaryls of the Formula (I)
Claims 1, 3, 8, 24, 26, 28, 29, 31, 36, 44, 48, 51, 53, 57 and 62 are rejected under 35 U.S.C. § 112(a) because the specification, while being enabling for substituted heteroaryls of the Formula (I), wherein the substituted heteroaryls of the Formula (I) are as presented herein in the section above entitled Claim Objections, does not reasonably provide enablement for substituted hetero-aryls of the Formula (I), wherein the substituted heteroaryls of the Formula (I) are not as presented herein in the section above entitled Claim Objections. 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/or use the invention commensurate in scope with these claims. Substituted heteroaryls of the Formula (I), wherein the substituted heteroaryls of the Formula (I) are not as presented herein in the section above entitled Claim Objections, as recited in claim 1, have not been adequately enabled in the specification to allow any person having ordinary skill in the art, at the time this invention was made, to make and/or use substituted heteroaryls of the Formula (I), wherein the substituted heteroaryls of the Formula (I) are not as presented herein in the section above entitled Claim Objections.
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) breadth of the claims; (b) nature of the invention; (c) state of the prior art; (d) level of one of ordinary skill in the art; (e) level of predictability in the art; (f) amount of direction provided by the inventor or joint inventor; (g) existence of working examples; and (h) quantity of experimentation needed to make or use the invention based on the content of the disclosure. {See Ex parte Forman 230 USPQ 546 (Bd. Pat. App. & Inter. 1986); and In re Wands, 8 USPQ2d 1400 (Fed. Cir. 1988)}.
The above factors, regarding the instant invention, are summarized as follows:
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(a) Breadth of the claims - the breadth of the claims includes substituted heteroaryls of the Formula (I), shown to the right;
(b) Nature of the invention - the nature of the invention is evaluation of substituted heteroaryls of the Formula (I), shown to the right above, and the pharmacokinetic behavior of these substances as methionine adenosyl transferase 2a (MAT2a) inhibitors;
(c) State of the prior art - Nature Reviews: Drug Discovery offers a snapshot of the state of the drug development art. Herein, drug development is stated to follow the widely accepted Ehrlich model which includes: (1) development of a broad synthetic organic chemistry program; (2) subsequent testing of compounds in an appropriate laboratory model for the disease to be treated; and (3) screening of compounds with low toxicity in prospective clinical trials (Jordan, V. C. Nature Reviews: Drug Discovery, 2, 2003, 205). Moreover, WO 23/066283, as provided in the file and cited on the IDS, provides a synthesis of the instantly recited substituted heteroaryls of the Formula (I) {Chen, et al. WO 23/066283, 2023};
(d) Level of one of ordinary skill in the art - the artisans synthesizing the inventor’s or joint inventor’s substituted heteroaryls of the Formula (I), wherein the substituted heteroaryls of the Formula (I) are not as presented herein in the section above entitled Claim Objections, would be a collaborative team of synthetic chemists and/or health practitioners, possessing commensurate degree level and/or skill in the art, as well as several years of professional experience;
(e) Level of predictability in the art - Synthetic organic chemistry is quite unpredictable (See In re Marzocchi and Horton 169 USPQ at 367 ¶3). Similarly, it is unclear based on the combination of the instant specification, and Chen, et al. in WO 23/066283, as provided in the file and cited on the IDS, whether the instantly recited substituted heteroaryls of the Formula (I), wherein the substituted heteroaryls of the Formula (I) are not as presented herein in the section above entitled Claim Objections, are enabled. Moreover, the following excerpt is taken from Dörwald, which has relevance to the synthesis of substituted heteroaryls of the Formula (I), wherein the substituted hetero-aryls of the Formula (I) are not as presented herein in the section above entitled Claim Objections (Dörwald, F. Zaragoza. Side Reactions in Organic Synthesis: A Guide to Successful Synthesis Design, Weinheim: WILEY-VCH Verlag GmbH & Co. KGaA, 2005, Preface):
Most non-chemists would probably be horrified if they were to learn how many attempted syntheses fail, and how inefficient research chemists are. The ratio of successful to unsuccessful chemical experiments in a normal research laboratory is far below unity, and synthetic research chemists, in the same way as most scientists, spend most of their time working out what went wrong, and why.
Despite the many pitfalls lurking in organic synthesis, most organic chemistry textbooks and research articles do give the impression that organic reactions just proceed smoothly and that the total synthesis of complex natural products, for instance, is maybe a labor-intensive but otherwise undemanding task. In fact, most syntheses of structurally complex natural products are the result of several years of hard work by a team of chemists, with almost every step requiring careful optimization. The final synthesis usually looks quite different from that originally planned, because of unexpected difficulties encountered in the initially chosen synthetic sequence. Only the seasoned practitioner who has experienced for himself the many failures and frustrations which the development (sometimes even the repetition) of a synthesis usually implies will be able to appraise such work.
Chemists tend not to publish negative results, because these are, as opposed to positive results, never definite (and far too copious).
(f) Amount of direction provided by the inventor - the invention lacks direction with respect to making and/or using substituted heteroaryls of the Formula (I), wherein the substituted heteroaryls of the Formula (I) are not as presented herein in the section above entitled Claim Objections;
(g) Existence of working examples - the inventor or joint inventor has provided sufficient guidance to make and/or use substituted heteroaryls of the Formula (I), wherein the substituted heteroaryls of the Formula (I) are as presented herein in the section above entitled Claim Objections; however, the disclosure is insufficient to allow extrapolation of the limited examples to enable the instantly recited substituted hetero-aryls of the Formula (I), wherein the substituted heteroaryls of the Formula (I) are not as presented herein in the section above entitled Claim Objections. The specification lacks working examples of substituted heteroaryls of the Formula (I), wherein the substituted heteroaryls of the Formula (I) are not as presented herein in the section above entitled Claim Objections.
Within the specification, [A]t least one specific operative embodiment or example of the invention must be set forth. The example(s) 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) and MPEP § 2173.05.
(h) Quantity of experimentation needed to make or use the invention based on the content of the disclosure - predicting whether a recited compound is in fact one that produces a desired physiological effect at a therapeutic concentration and with useful kinetics, is filled with experimental uncertainty, and without proper guidance, would involve a substantial amount of experimentation (Jordan, V. C. Nature Reviews: Drug Discovery, 2, 2003, 205-213). Similarly, the specification, as originally filed, including any references incorporated therein, fails to provide the necessary support
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required by 35 U.S.C. § 112(a) to enable the instantly recited substituted heteroaryls of the Formula (I), wherein the substituted heteroaryls of the Formula (I) are not as presented herein in the section above entitled Claim Objections. Thus, it is unclear, based on the guidance provided by the specification, whether a solvate of a substituted heteroaryl of the Formula (I), such as 1-(2-methylpyridin-3-yl)-4-[(prop-2-yn-1-yl)amino]-7-(trifluoromethyl)-1,2-dihydropteridin-2-one, shown to the left above, is either synthetically feasible or possesses utility as a methionine adenosyl transferase 2a (MAT2a) inhibitor.
A conclusion of lack of enablement means that, based on the evidence regarding each of the above factors, the specification, at the time the invention 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. {See In re Wright, 999 F.2d 1557, 1562, 27 USPQ2d 1510, 1513 (Fed. Cir. 1993)}.
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. (See In re Wands, 858 F.2d at 737, 8 USPQ2d at 1404). These factual considerations are discussed comprehensively in MPEP § 2164.08 (scope or breadth of the claims), § 2164.05(a) (nature of the invention and state of the prior art), § 2164.05(b) (level of one of ordinary skill), § 2164.03 (level of predictability in the art and amount of direction provided by the inventor or joint inventor), § 2164.02 (the existence of working examples) and § 2164.06 (quantity of experimentation needed to make or use the invention based on the content of the disclosure).
Based on a preponderance of the evidence presented herein, the conclusion that the inventor or joint inventor is insufficiently enabled for making and/or using substituted heteroaryls of the Formula (I), wherein the substituted heteroaryls of the Formula (I) are not as presented herein in the section above entitled Claim Objections, is clearly justified.
The examiner suggests amending the claims, particularly as stated in the section above entitled Claim Objections, to overcome this rejection.
Claim Rejections - 35 U.S.C. § 112(b)
The following is a quotation of the second paragraph of 35 U.S.C. § 112:
(b) CONCLUSION. The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the inventor or joint inventor regards as the invention.
Claims 1, 3, 8, 24, 26, 28, 29, 31, 36, 41, 44, 48, 51, 53, 57 and 62 are rejected under 35 U.S.C. § 112(b) as being indefinite for failing to set forth the subject matter which the inventor or joint inventor regards as the invention.
The inventor or joint inventor should note that claim 1 recite the limitation, S(=O)(=NH)C(R10)(R11), with regard to R1, R2, R3, R5, R5a, R6, R7, R8, R9, R14, R15a, R15b, R15c, and/or R15d, respectively, where the limitation is implausible, resulting in an incomplete valence. Claims are unduly speculative where they define only a portion of a substituted heteroaryl of the Formula (I). Consequently, since incomplete valences are not permitted in the structure of the substituted heteroaryls of the Formula (I), an essential portion of the substituted heteroaryls of the Formula (I) is indefinite and one of ordinary skill in the art would not be reasonably apprised of the metes and bounds of the substituted heteroaryls of the Formula (I). {See Ex parte Pedlow and Miner, 90 USPQ 395 (Bd. Pat. App. & Int. 1951)}.
Moreover, the inventor or joint inventor should further note that [C]laims which depend from indefinite claims are also indefinite. {See Ex parte Cordova, 10 USPQ 2d 1949, 1952 (PTO Bd. App. 1989)}.
The examiner suggests amending the claims, particularly as stated in the section above entitled Claim Objections, to overcome this rejection.
Claims 1, 3, 8, 24, 26, 28, 29, 31, 36, 41, 44, 48, 51, 53, 57 and 62 are further rejected under 35 U.S.C. § 112(b) as being indefinite for failing to set forth the subject matter which the inventor or joint inventor regards as the invention.
The inventor or joint inventor should note that a broad limitation together with a narrow limitation that falls within the broad limitation (in the same claim) is considered indefinite, since the resulting claim does not clearly set forth the metes and bounds of the patent protection desired. See MPEP § 2173.05(c), MPEP § 2173.05(h), and/or Eli Lilly & Co. v. Teva Parenteral Meds., 845 F.3d 1357, 1371, 121 USPQ2d 1277, 1287 (Fed. Cir. 2017).
Similarly, the inventor or joint inventor should further note that claim 1 recites the broad limitation, OR10, with regard to optional substituents for R15a, R15b, R15c, and/or R15d, respectively, and the claim also recites C1-6 alkoxy and C1-6 haloalkoxy, with regard to R15a, R15b, R15c, and/or R15d, respectively, which are the narrower statements of the limitation.
Likewise, the inventor or joint inventor should further note the explanation given by the Board of Patent Appeals and Interferences in Ex parte Wu, 10 USPQ2d 2031, 2033 (Bd. Pat. App. & Inter. 1989), pertaining to where broad language is followed by such as and then narrow language. The Board stated that this can render a claim indefinite by raising a question or doubt as to whether the feature introduced by such language is (a) merely exemplary of the remainder of the claim, and consequently, not required, or (b) a required feature of the claim.
Next, the inventor or joint inventor should further note the explanation given by the Board of Patent Appeals and Interferences in the decisions of Ex parte Steigewald, 131 USPQ 74 (Bd. App. 1961); Ex parte Hall, 83 USPQ 38 (Bd. App. 1948); and Ex parte Hasche, 86 USPQ 481 (Bd. App. 1949).
Moreover, the inventor or joint inventor should further note that [C]laims which depend from indefinite claims are also indefinite. {See Ex parte Cordova, 10 USPQ 2d 1949, 1952 (PTO Bd. App. 1989)}.
The examiner suggests amending the claims, particularly as stated in the section above entitled Claim Objections, to overcome this rejection.
Claims 1, 3, 8, 24, 26, 29, 31, 36, 41, 44, 48, 51, 53, 57 and 62 are further rejected under 35 U.S.C. § 112(b) as being indefinite for failing to set forth the subject matter which the inventor or joint inventor regards as the invention.
The inventor or joint inventor should note that claim 1 recite the limitation, oxo, with regard to R2 and R3, respectively, where the limitation is implausible, resulting in an incomplete valence. Similarly, the examiner asserts that (a) if R2 is oxo (i.e. =O), then R3 must be absent; (b) if R3 is oxo (i.e. =O), then R2 must be absent; and/or (c) R2 and R3 may not simultaneously be oxo (i.e. =O), respectively. Likewise, claims are unduly speculative where they define only a portion of a substituted heteroaryl of the Formula (I). Consequently, since incomplete valences are not permitted in the structure of the substituted heteroaryls of the Formula (I), an essential portion of the substituted heteroaryls of the Formula (I) is indefinite and one of ordinary skill in the art would not be reasonably apprised of the metes and bounds of the substituted heteroaryls of the Formula (I). {See Ex parte Pedlow and Miner, 90 USPQ 395 (Bd. Pat. App. & Int. 1951)}.
Moreover, the inventor or joint inventor should further note that [C]laims which depend from indefinite claims are also indefinite. {See Ex parte Cordova, 10 USPQ 2d 1949, 1952 (PTO Bd. App. 1989)}.
The examiner suggests amending the claims, particularly as stated in the section above entitled Claim Objections, to overcome this rejection.
Claim 41 is further rejected under 35 U.S.C. § 112(b) as being indefinite for failing to set forth the subject matter which the inventor or joint inventor regards as the invention.
The inventor or joint inventor should note that a broad limitation together with a narrow limitation that falls within the broad limitation (in the same claim) is considered indefinite, since the resulting claim does not clearly set forth the metes and bounds of the patent protection desired. See MPEP § 2173.05(c), MPEP § 2173.05(h), and/or Eli Lilly & Co. v. Teva Parenteral Meds., 845 F.3d 1357, 1371, 121 USPQ2d 1277, 1287 (Fed. Cir. 2017).
Similarly, the inventor or joint inventor should further note that claim 41 recites the broad limitation, Formula (Ib), and the claim also recites Formula (Ia), which is the narrower statement of the limitation.
Likewise, the inventor or joint inventor should further note the explanation given by the Board of Patent Appeals and Interferences in Ex parte Wu, 10 USPQ2d 2031, 2033 (Bd. Pat. App. & Inter. 1989), pertaining to where broad language is followed by such as and then narrow language. The Board stated that this can render a claim indefinite by raising a question or doubt as to whether the feature introduced by such language is (a) merely exemplary of the remainder of the claim, and consequently, not required, or (b) a required feature of the claim.
Moreover, the inventor or joint inventor should further note the explanation given by the Board of Patent Appeals and Interferences in the decisions of Ex parte Steigewald, 131 USPQ 74 (Bd. App. 1961); Ex parte Hall, 83 USPQ 38 (Bd. App. 1948); and Ex parte Hasche, 86 USPQ 481 (Bd. App. 1949).
The examiner suggests amending the claim, particularly as stated in the section above entitled Claim Objections, to overcome this rejection.
Claim Rejections - Obviousness-type Double Patenting
The nonstatutory double patenting rejection is based on a judicially created doctrine grounded in public policy (a policy reflected in the statute), so as to prevent the unjustified or improper timewise extension of the right to exclude granted by a patent and to prevent possible harassment by multiple assignees. A nonstatutory obviousness-type double patenting rejection is appropriate where the conflicting claims are not identical, but at least one examined invention claim is not patentably distinct from the reference claims because the examined invention claim is either anticipated by, or would have been obvious over, the reference claims. {See In re Berg, 140 F.3d 1428, 46 USPQ2d 1226 (Fed. Cir. 1998); In re Goodman, 11 F.3d 1046, 29 USPQ2d 2010 (Fed. Cir. 1993); In re Longi, 759 F.2d 887, 225 USPQ 645 (Fed. Cir. 1985); In re Van Ornum, 686 F.2d 937, 214 USPQ 761 (CCPA 1982); In re Vogel, 422 F.2d 438, 164 USPQ 619 (CCPA 1970); and In re Thorington, 418 F.2d 528, 163 USPQ 644 (CCPA 1969)}.
Consequently, claims 1, 3, 8, 24, 26, 28, 29, 31, 36, 41, 44, 48, 51, 53, 57 and 62 are rejected on the ground of nonstatutory obviousness-type double patenting as being unpatentable over at least claims 1-8, 19 and 20 of US Patent No. 11,999,713. Although the conflicting claims are not identical, they are not patentably distinct from each other because claim 1 in US 11,999,713 recites substituted heteroaryls of the Formula (I), where m = 0; n = 1; R1 = -H; R2 = -H; R3 = -H; X = -NR4-, wherein R4 = -H; Z3 = CR6, wherein R6 =-H; Z1 = CR7, wherein R7 =-H; Z2 = CR9, wherein R9 =-H; R8 = -C1-6 haloalkyl; and ring A= -pyridyl, respectively, which provide overlapping subject matter with respect to the instantly recited substituted heteroaryls of the Formula (I), where m = 0; n = 1; R1 = -H; R2 = -H; R3 = -H; X = -NR4-, wherein R4 = -H; Z3 = CR6, wherein R6 =-H; Z1 = CR7, wherein R7 =-H; Z2 = CR9, wherein R9 =-H; R8 = -C1-6 haloalkyl; and ring A= -C1-10 heteroaryl.
The inventor or joint inventor should note that [T]he discovery of a previously unappreciated property of a prior art compound, or of a scientific explanation for the prior art’s functioning, does not render the old compound patentably new to the discoverer. {See Atlas Powder Co. v. Ireco Inc., 190 F.3d 1342, 1347, 51 USPQ2d 1943, 1947 (Fed. Cir. 1999)}.
Similarly, the inventor or joint inventor should further note that [T]he claiming of a new use, new function or unknown property which is inherently present in the prior art does not necessarily make the claim patentable. {See In re Best, 562 F.2d 1252, 1254, 195 USPQ 430, 433 (CCPA 1977); and In re Crish, 393 F.3d 1253, 1258, 73 USPQ2d 1364, 1368 (Fed. Cir. 2004)}.
Likewise, the inventor or joint inventor should note that [W]hen the claim recites using an old compound and the use is directed to a result or property of that compound, then the claim is anticipated. {See In re May, 574 F.2d 1082, 1090, 197 USPQ 601, 607 (CCPA 1978); and In re Tomlinson, 363 F.2d 928, 150 USPQ 623 (CCPA 1966)}.
Next, the inventor or joint inventor should further note that [P]roducts of identical chemical composition may not have mutually exclusive properties. A chemical composition and its properties are inseparable. Therefore, if the prior art teaches the identical chemical structure, the properties the inventor or joint inventor discloses and/or claims are necessarily present. {See In re Spada, 911 F.2d 705, 709, 15 USPQ2d 1655, 1658 (Fed. Cir. 1990)}.
Then, the inventor or joint inventor should further note that a timely filed terminal disclaimer in compliance with 37 CFR 1.321(c) or 37 CFR 1.321(d) may be used to overcome an actual or provisional rejection based on a nonstatutory double patenting ground, provided the conflicting invention or patent either is shown to be commonly owned with this invention, or claims an invention made as a result of activities undertaken within the scope of a joint research agreement.
Moreover, the inventor or joint inventor should further note that the USPTO internet Web site contains terminal disclaimer forms which may be used, and the inventor or joint inventor is encouraged to visit http://www.uspto.gov/forms/, where (i) the filing date of the invention will determine what form should be used, and (ii) a web-based eTerminal Disclaimer may be filled out completely online using web-screens, respectively.
Also, the inventor or joint inventor should further note that an eTerminal Disclaimer that meets all requirements is auto-processed and approved immediately upon submission.
Finally, for more information about eTerminal Disclaimers, the inventor or joint inventor should refer to http://www.uspto.gov/patents/process/file/efs/guidance/eTD-info-I.jsp.
Allowable Subject Matter
No claims are allowed.
Conclusion
Any inquiry concerning this communication or earlier communications from the examiner should be directed to DOUGLAS M. WILLIS, whose telephone number is 571-270-5757. The examiner may normally be reached on Monday thru Thursday from 8:00-6:00 EST. The examiner is also available on alternate Fridays.
If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Mr. Jeffrey Murray, may be reached on 571-272-9023. The fax phone number for the organization where this invention or proceeding is assigned is 571-273-8300.
Information regarding the status of an invention may be obtained from Patent Center. For more information about Patent Center, see https://www.uspto.gov/patents/apply/patent-center. Should you have questions on access to Patent Center, contact the Patent Electronic Business Center (PEBC) at 866-217-9197 (toll-free) or ebc@uspto.gov.
/DOUGLAS M WILLIS/
Primary Examiner, Art Unit 1624
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