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, 5, 19, 25, 28, 32, 49, 54, 57, 66, 68, 76, 86, 89, 90, 92-94 and 96 are pending in the instant invention. According to the Amendments to the Claims, filed August 20, 2026, claims 2-4, 6-18, 20-24, 26, 27, 29-31, 33-48, 50-53, 55, 56, 58-65, 67, 69-75, 77-85, 87, 88, 91, 95 and 97-99 were cancelled.
Status of Priority
This invention is a 35 U.S.C. § 371 National Stage Filing of International Application No. PCT/US2022/052224, filed December 8, 2022, which claims priority under 35 U.S.C. § 119(e) to US Provisional Application No. 63/287,479, filed December 8, 2021.
Restrictions / Election of Species
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The inventor’s or joint inventor’s provisional election of the following, with traverse, in the reply filed on August 20, 2026, is acknowledged: a) Group I - claims 1, 5, 19, 25, 28, 32, 49 and 89; and b) substituted pyrimidine of Formula I - p. 43, Example 1, compound 1, shown to the right below, and hereafter referred to as 5-methoxy-2- morpholino-N-phenyl-6-(1-pheny1-1H-pyrazol-3-yl)pyrimidine-4-carboxamide, where R4 = -NHR8, wherein R8 = -phenyl; V = -C(O)-; R1 = -morpholin-4-yl; R2 = -OCH3; and R3 = -1-phenylpyrazol-3-yl. Claims 1, 19, 32, 49 and 89 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 since supposed errors in the restriction requirement were not distinctly and specifically pointed out, the election has been treated as an election, without traverse. See MPEP § 818.03(a).
Likewise, the inventor or joint inventor should further note that, in accordance with MPEP § 803.02, the instant Markush claim has been examined, with respect to the elected species, and further to the extent necessary to determine patentability. In the instant case, the substituted pyrimidines of the Formula I, where R4 = -NHR8, wherein R8 = -phenyl; V = -C(O)-; R1 = -morpholin-4-yl; R2 = -OCH3; and R3 = -optionally substituted pyrazol-3-yl, respectively, which encompass the elected species, have been found to be free of the prior art.
Accordingly, the inventor or joint inventor should further note that the examiner has expanded scope of the instant Markush claim to further encompass substituted pyrimidines of the Formula I, where R2 and R3, together with the ring to which they are attached, do not combine to form an optionally substituted C4-C12 heteroaryl; however, the instant Markush claim now fails to be free of the prior art, since it is rejected herein below in the section entitled: Claim Rejections - 35 U.S.C. § 102.
Consequently, the inventor or joint inventor should further note that the instant Markush claim is hereby restricted to substituted pyrimidines of the Formula I, where R2 and R3, together with the ring to which they are attached, do not combine to form an optionally substituted C4-C12 heteroaryl, particularly as stated in the section below entitled Claim Objections.
Next, the inventor or joint inventor should further note that scope of the instant Markush claim will not be extended to cover additional nonelected species and/or groups of patentably distinct species.
Then, the inventor or joint inventor should further note that the requirement is still deemed proper and is therefore made FINAL.
Moreover, the inventor or joint inventor should further note that claims 28, 54, 57, 66, 68, 76, 86, 90, 92-94 and 96 were 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, 5, 19, 25, 32, 49 and 89 is contained within.
Specification Objection - Disclosure
The following guidelines illustrate the preferred layout for the specification of a utility application. These guidelines are suggested for the inventor’s or joint inventor’s use.
Arrangement of the Specification
As provided in 37 CFR 1.77(b), the specification of a utility invention should include the following sections in order. Each of the lettered items should appear in upper case, without underlining or bold type, as a section heading. If no text follows the section heading, the phrase Not Applicable should follow the section heading:
(a) TITLE OF THE INVENTION.
(b) CROSS-REFERENCE TO RELATED APPLICATIONS.
(c) STATEMENT REGARDING FEDERALLY SPONSORED RESEARCH OR
DEVELOPMENT.
(d) THE NAMES OF THE PARTIES TO A JOINT RESEARCH AGREEMENT.
(e) INCORPORATION-BY-REFERENCE OF MATERIAL SUBMITTED ON A
COMPACT DISC.
(f) BACKGROUND OF THE INVENTION.
(1) Field of the Invention.
(2) Description of Related Art (including information disclosed under 37 CFR 1.97
and 1.98).
(g) BRIEF SUMMARY OF THE INVENTION.
(h) BRIEF DESCRIPTION OF THE SEVERAL VIEWS OF THE DRAWING(S).
(i) DETAILED DESCRIPTION OF THE INVENTION.
(j) CLAIM OR CLAIMS (commencing on a separate sheet).
(k) ABSTRACT OF THE DISCLOSURE (commencing on a separate sheet).
(l) SEQUENCE LISTING (See MPEP § 2424 and 37 CFR 1.821-1.825).
The inventor or joint inventor is advised to format the specification according to 37 CFR 1.77(b) above and 37 CFR 1.77(c). Revisions should particularly include and/or address: a) section headings (b-i), where applicable; and b) 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 identifying: a) the substituted pyrimidines of the Formula I; and b) a particular utility for the substituted pyrimidines of the Formula I.
The following title is suggested: SUBSTITUTED PYRIMIDINES AS PIKFYVE 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) and/or Improper Markush Grouping, 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, stereoisomer, or tautomer thereof,
wherein:
R4 is NHR8, 1-methylpiperidin-3-yl, pyridin-3-yl, pyridin-4-yl, 1-methyl-1-pyridinium-4-yl, or pyridazin-3-yl;
wherein the 1-methylpiperidin-3-yl is optionally substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of halogen, CN, NO2, alkyl, heteroalkyl, C(O)NH2, C(O)NH(alkyl), C(O)N(alkyl)2, NH2, NH(alkyl), N(alkyl)2, N3, OH, O(alkyl), =O, SH, S(alkyl), carbocyclyl, heterocyclyl, aryl, and heteroaryl;
wherein the pyridin-3-yl, pyridin-4-yl, 1-methyl-1-pyridinium-4-yl, or pyridazin-3-yl is optionally substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of halogen, CN, NO2, alkyl, heteroalkyl, C(O)NH2, C(O)NH(alkyl), C(O)N(alkyl)2, NH2, NH(alkyl), N(alkyl)2, N3, OH, O(alkyl), SH, S(alkyl), carbocyclyl, heterocyclyl, aryl, and heteroaryl;
wherein each carbocyclyl and heterocyclyl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, O(alkyl), and =O; and
wherein each aryl and heteroaryl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, and O(alkyl);
R8 is C3-C6 cycloalkyl or phenyl;
wherein the C3-C6 cycloalkyl is optionally substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of halogen, CN, NO2, alkyl, heteroalkyl, C(O)NH2, C(O)NH(alkyl), C(O)N(alkyl)2, NH2, NH(alkyl), N(alkyl)2, N3, OH, O(alkyl), =O, SH, S(alkyl), carbocyclyl, heterocyclyl, aryl, and heteroaryl;
wherein the phenyl is optionally substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of halogen, CN, NO2, alkyl, heteroalkyl, C(O)NH2, C(O)NH(alkyl), C(O)N(alkyl)2, NH2, NH(alkyl), N(alkyl)2, N3, OH, O(alkyl), SH, S(alkyl), carbocyclyl, heterocyclyl, aryl, and heteroaryl;
wherein each carbocyclyl and heterocyclyl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, O(alkyl), and =O; and
wherein each aryl and heteroaryl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, and O(alkyl);
V is -CH2NH-, -CH2NR5-, -CH(OH)-, -C(O)-, -NH-, -NR5-, or -O-;
R5 is C1-C6 alkyl;
wherein the C1-C6 alkyl is optionally substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of halogen, CN, NO2, C(O)NH2, C(O)NH(alkyl), C(O)N(alkyl)2, NH2, NH(alkyl), N(alkyl)2, N3, OH, O(alkyl), =O, SH, S(alkyl), carbocyclyl, heterocyclyl, aryl, and heteroaryl;
wherein each carbocyclyl and heterocyclyl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, O(alkyl), and =O; and
wherein each aryl and heteroaryl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, and O(alkyl);
R1 is 2-oxopyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl, pyridin-3-yl, pyridin-4-yl, or pyridazinyl;
wherein the 2-oxopyrrolidin-1-yl, piperidin-1-yl, or morpholin-4-yl is optionally substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of halogen, CN, NO2, alkyl, heteroalkyl, C(O)NH2, C(O)NH(alkyl), C(O)N(alkyl)2, NH2, NH(alkyl), N(alkyl)2, N3, OH, O(alkyl), =O, SH, S(alkyl), carbocyclyl, heterocyclyl, aryl, and heteroaryl;
wherein the pyridazinyl is optionally substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of halogen, CN, NO2, alkyl, heteroalkyl, C(O)NH2, C(O)NH(alkyl), C(O)N(alkyl)2, NH2, NH(alkyl), N(alkyl)2, N3, OH, O(alkyl), SH, S(alkyl), carbocyclyl, heterocyclyl, aryl, and heteroaryl;
wherein each carbocyclyl and heterocyclyl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, O(alkyl), and =O; and
wherein each aryl and heteroaryl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, and O(alkyl);
R2 is halogen, (CH2)1-6OH, C(O)NR7aR7b, OC1-6 alkyl, P(O)R7cR7d, SR7e, S(O)R7e, S(O)2R7e, 2-oxopyrrolidin-1-yl, or C2-C9 heteroaryl;
wherein the OC1-6 alkyl is optionally substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of halogen, CN, NO2, C(O)NH2, C(O)NH(alkyl), C(O)N(alkyl)2, NH2, NH(alkyl), N(alkyl)2, N3, OH, O(alkyl), =O, SH, S(alkyl), carbocyclyl, heterocyclyl, aryl, and heteroaryl;
wherein the 2-oxopyrrolidin-1-yl is optionally substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of halogen, CN, NO2, alkyl, heteroalkyl, C(O)NH2, C(O)NH(alkyl), C(O)N(alkyl)2, NH2, NH(alkyl), N(alkyl)2, N3, OH, O(alkyl), =O, SH, S(alkyl), carbocyclyl, heterocyclyl, aryl, and heteroaryl;
wherein the C2-C9 heteroaryl is optionally substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of halogen, CN, NO2, alkyl, heteroalkyl, C(O)NH2, C(O)NH(alkyl), C(O)N(alkyl)2, NH2, NH(alkyl), N(alkyl)2, N3, OH, O(alkyl), SH, S(alkyl), carbocyclyl, heterocyclyl, aryl, and heteroaryl;
wherein each carbocyclyl and heterocyclyl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, O(alkyl), and =O; and
wherein each aryl and heteroaryl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, and O(alkyl);
R7a is H or C1-C6 alkyl;
wherein the C1-C6 alkyl is optionally substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of halogen, CN, NO2, C(O)NH2, C(O)NH(alkyl), C(O)N(alkyl)2, NH2, NH(alkyl), N(alkyl)2, N3, OH, O(alkyl), =O, SH, S(alkyl), carbocyclyl, heterocyclyl, aryl, and heteroaryl;
wherein each carbocyclyl and heterocyclyl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, O(alkyl), and =O; and
wherein each aryl and heteroaryl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, and O(alkyl);
R7b is H or C1-C6 alkyl;
wherein the C1-C6 alkyl is optionally substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of halogen, CN, NO2, C(O)NH2, C(O)NH(alkyl), C(O)N(alkyl)2, NH2, NH(alkyl), N(alkyl)2, N3, OH, O(alkyl), =O, SH, S(alkyl), carbocyclyl, heterocyclyl, aryl, and heteroaryl;
wherein each carbocyclyl and heterocyclyl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, O(alkyl), and =O; and
wherein each aryl and heteroaryl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, and O(alkyl); or
R7a and R7b, taken together with the nitrogen atom to which they are attached, form a C2-C9 heterocyclyl;
wherein the C2-C9 heterocyclyl is optionally substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of halogen, CN, NO2, alkyl, heteroalkyl, C(O)NH2, C(O)NH(alkyl), C(O)N(alkyl)2, NH2, NH(alkyl), N(alkyl)2, N3, OH, O(alkyl), =O, SH, S(alkyl), carbocyclyl, heterocyclyl, aryl, and heteroaryl; and
wherein each carbocyclyl and heterocyclyl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, O(alkyl), and =O; and
wherein each aryl and heteroaryl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, and O(alkyl);
R7c is C1-C6 alkyl, OH, or OC1-C6 alkyl;
wherein the C1-C6 alkyl or OC1-C6 alkyl is optionally substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of halogen, CN, NO2, C(O)NH2, C(O)NH(alkyl), C(O)N(alkyl)2, NH2, NH(alkyl), N(alkyl)2, N3, OH, O(alkyl), =O, SH, S(alkyl), carbocyclyl, heterocyclyl, aryl, and heteroaryl;
wherein each carbocyclyl and heterocyclyl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, O(alkyl), and =O; and
wherein each aryl and heteroaryl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, and O(alkyl);
R7d is C1-C6 alkyl, OH, or OC1-C6 alkyl;
wherein the C1-C6 alkyl or OC1-C6 alkyl is optionally substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of halogen, CN, NO2, C(O)NH2, C(O)NH(alkyl), C(O)N(alkyl)2, NH2, NH(alkyl), N(alkyl)2, N3, OH, O(alkyl), =O, SH, S(alkyl), carbocyclyl, heterocyclyl, aryl, and heteroaryl;
wherein each carbocyclyl and heterocyclyl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, O(alkyl), and =O; and
wherein each aryl and heteroaryl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, and O(alkyl);
R7e is C1-C6 alkyl, OH, or OC1-C6 alkyl;
wherein the C1-C6 alkyl or OC1-C6 alkyl is optionally substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of halogen, CN, NO2, C(O)NH2, C(O)NH(alkyl), C(O)N(alkyl)2, NH2, NH(alkyl), N(alkyl)2, N3, OH, O(alkyl), =O, SH, S(alkyl), carbocyclyl, heterocyclyl, aryl, and heteroaryl;
wherein each carbocyclyl and heterocyclyl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, O(alkyl), and =O; and
wherein each aryl and heteroaryl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, and O(alkyl); and
R3 is C6-C10 aryl, pyrazol-1-yl, pyrazol-3-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyridazin-3-yl, or pyrimidin-4-yl;
wherein the C6-C10 aryl, pyrazol-1-yl, pyrazol-3-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyridazin-3-yl, or pyrimidin-4-yl is optionally substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of halogen, CN, NO2, alkyl, heteroalkyl, C(O)NH2, C(O)NH(alkyl), C(O)N(alkyl)2, NH2, NH(alkyl), N(alkyl)2, N3, OH, O(alkyl), SH, S(alkyl), carbocyclyl, heterocyclyl, aryl, and heteroaryl;
wherein each carbocyclyl and heterocyclyl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, O(alkyl), and =O; and
wherein each aryl and heteroaryl substituent is optionally and independently substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of alkyl, heteroalkyl, alkylene-aryl, OH, and O(alkyl).
Appropriate correction is required. See MPEP § 2173.02.
Claim 5 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The compound of claim 1, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein R1 is:
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112
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, or
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.
Appropriate correction is required. See MPEP § 2173.02.
Claim 19 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The compound of claim 1, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein R8 is cyclopropyl or phenyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 25 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The compound of claim 1, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein R4 is pyridin-3-yl or pyridin-4-yl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 32 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The compound of claim 1, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein R2 is Cl, CH2OH, C(O)N(CH3)2, C(O)-azetidin-1-yl, OCH3, P(O)(CH3)(CH3), S(O)CH3, or oxazol-2-yl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 49 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The compound of claim 1, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein R3 is:
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,
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99
160
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,
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111
203
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,
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141
212
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,
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111
170
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161
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156
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108
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, or
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182
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.
Appropriate correction is required. See MPEP § 2173.02.
Claim 89 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
A pharmaceutical composition comprising a pharmaceutically acceptable excipient and the compound of claim 1, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof.
Appropriate correction is required. See MPEP § 2173.02.
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, 5, 19, 25, 28, 32, 49 and 89 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 the phrase, optionally substituted, in claim 1, with regard to R1, R2, R3, R2 and R3, R4, R5, R7a, R7b, R7c, R7d, R7e, and/or R8, respectively, is a relative phrase which renders the claims indefinite. The phrase, optionally substituted, is not defined by the claim, the specification does not provide an adequate standard for ascertaining the requisite degree, and one of ordinary skill in the art would not be reasonably apprised of the metes and bounds of the invention. The specification, on pages 24-25, uses open language, such as include, to define the term, substituent, using a boiler plate list of functional groups, such as aryl, carbocyclyl, etc., and further discloses that the substituents themselves may be further substituted; however, neither the specification, nor the claim, explicitly limits the invention to any specifically disclosed or recited embodiments. Consequently, the substituted pyrimidines of the Formula I have been rendered indefinite by the use of the phrase, optionally substituted, with regard to R1, R2, R3, R2 and R3, R4, R5, R7a, R7b, R7c, R7d, R7e, and/or R8, respectively.
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 Rejections - 35 U.S.C. § 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, 25, 32 and 89 are rejected under 35 U.S.C. § 102(a)(1) as being anticipated by Nuss, et al. in WO 2004/048365.
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The inventor or joint inventor should note that the instant invention recites a substituted pyrimidine of the Formula I, shown to the left, where R4 = -optionally substituted pyridin-3-yl; V = -NH-; R1 = -optionally substituted morpholin-4-yl; R2 = -(CH2)nOH, wherein n = 1; and R3 = -optionally substituted C6-C10 aryl, respectively, and/or a pharmaceutical composition thereof, as a FYVE-type zinc finger containing phosphoinositide kinase (PIKfyve) inhibitor.
Similarly, the inventor or joint inventor should further note that Nuss, et al. (WO
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2004/048365), as provided in the file and cited on the IDS, teaches a substituted pyrimidine of the Formula I, shown to the right, where R4 = -pyridin-3-yl; V = -NH-; R1 = -morpholin-4-yl; R2 = -(CH2)nOH, wherein n = 1; and R3 = -3-methoxy-phenyl, respectively, and/or a pharmaceutical formulation thereof, as a phosphatidylinositol 3-kinase (PI3K) inhibitor [p. 87, Scheme 1, compound 2; and pharmaceutical formulations – p. 25, lines 27-29].
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, although not explicitly discussed herein, this reference contains additional species that may anticipate the instantly recited substituted pyrimidines of the Formula I. Consequently, any amendments to the claims and/or arguments formulated to overcome rejections rendered under 35 U.S.C. § 102 should address this reference as a whole and should not be limited to the species discussed or disclosed explicitly herein.
Moreover, the inventor or joint inventor should further note that in the event the determination of the status of the invention as subject to AIA 35 U.S.C. § 102 (or as subject to pre-AIA 35 U.S.C. § 102) is incorrect, any correction of the statutory basis for the instant 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.
Claim Rejections - Improper Markush Grouping
A Markush claim recites a list of alternatively useable members. The listing of specified alternatives within a Markush claim is referred to as a Markush group or a Markush grouping. {see Abbott Labs v. Baxter Pharmaceutical Products, Inc., 334 F.3d 1274, 1280-81, 67 USPQ2d 1191, 1196-97 (Fed. Cir. 2003). The claim language defined by a Markush grouping requires selection from a closed group consisting of the alternatively useable members (Id. at 1280, 67 USPQ2d at 1196). {See MPEP § 2111.03, subsection II, for a discussion of consisting of in the context of Markush groupings}.
A Markush grouping may be rejected under the judicially-approved improper Markush grouping principles when the Markush claim contains an improper Markush grouping of alternatively useable members, where either: (1) the alternatively useable members of the Markush group do not share a single structural similarity, or (2) the alternatively useable members of the Markush group do not share a common use. {See the Supplementary Examination Guidelines for Determining Compliance with 35 U.S.C. 112 and for Treatment of Related Issues in Patent Applications (Supplementary Guidelines), 76 Fed. Reg. 7162 (February 9, 2011), particularly at 7166 (citing In re Harnisch, 631 F.2d 716, 721-22, 206 USPQ 300, 305 (CCPA 1980)}.
The inventor or joint inventor should note that claims 1, 5, 19, 25, 32, 49 and 89 are rejected on the judicially-approved principles that they contain an improper Markush grouping of alternatively useable members. {See In re Harnisch, 631 F.2d 716, 721-22 (CCPA 1980); and Ex parte Hozumi, 3 USPQ2d 1059, 1060 (Bd. Pat. App. & Int. 1984)}.
Similarly, the inventor or joint inventor should further note that a Markush grouping is proper if: (1) the alternatively useable members of the Markush group (i.e. alternatives from which a selection is to be made in the context of a combination or process, or alternative chemical compounds as a whole) share a single structural similarity and belong to the same recognized physical or chemical class or to the same art-recognized class, and (2) the alternatively useable members of the Markush group (i.e. alternatives from which a selection is to be made in the context of a combination or process, or alternative chemical compounds as a whole) share a common use and are disclosed in the specification or known in the art to be functionally equivalent. {See Supplementary Guidelines at 7166 and MPEP § 2117; and see MPEP § 2111.03 and MPEP § 2173.05(h) for discussions of when a Markush grouping may be indefinite under 35 U.S.C. § 112(b)}.
Likewise, the inventor or joint inventor should further note that the Markush grouping consisting of substituted pyrimidines of the Formula I is improper, since the substituted pyrimidines of the Formula I, as recited in claims 1 and 89, respectively, do not consist of alternatively useable members that share a single structural similarity and a common use that flows from the single structural similarity. {See MPEP § 803.02; and MPEP § 2117}.
Next, the inventor or joint inventor should further note that the rejection of the Markush claims under the judicially-approved principles that they contain an improper Markush grouping of alternatively useable members will be maintained until (1) the Markush claims are amended to recite alternatively useable members that share a single structural similarity and a common use that flows from the single structural similarity, or (2) the inventor or joint inventor presents convincing arguments illustrating why the alternatively useable members recited in the Markush claims share a single structural similarity and a common use. {See MPEP § 803.02 and MPEP § 2117}.
Moreover, the inventor or joint inventor should further note that this is a rejection on the merits and may be appealed to the Patent Trial and Appeal Board in accordance with 35 U.S.C. § 134 and 37 CFR 41.31(a)(1).
In accordance with the principles of compact prosecution, MPEP § 803.02, and MPEP § 2117, respectively, the examiner suggests the inventor or joint inventor amend the scope of the substituted pyrimidines of the Formula I to recite substituted pyrimidines of the Formula I, where R2 and R3, together with the ring to which they are attached, do not combine to form an optionally substituted C4-C12 heteroaryl, particularly as stated in the section above entitled Claim Objections, to overcome this rejection.
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
Prosecution Insights