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 20-39 are pending in the instant invention. According to the Amendments to the Claims, filed October 31, 2022, claims 1-19 were cancelled and claims 20-39 were added.
Status of Priority
This invention is a 35 U.S.C. § 371 National Stage Filing of International Application No. PCT/CN2021/143703, filed December 31, 2021, which claims priority under 35 U.S.C. § 119(a-d) to CN 202011644306.2, filed December 31, 2020.
Restrictions / Election of Species
PNG
media_image1.png
200
400
media_image1.png
Greyscale
The inventor’s or joint inventor’s provisional election of the following, without traverse, in the reply filed on June 25, 2009, is acknowledged: a) Group I - claims 20, 22-33, 35 and 36; and b) substituted pyridin-2-amine of formula (I) - p. 37, Example 33, compound no. N55, shown to the right below, and hereafter referred to as N3-butyl-5-(4-((dimethylamino)methyl)benzyl)-6-methylpyridine-2,3-diamine, where R1 = -NR7R8, wherein R7 = -H and R8 = -(CH2)3CH3; R2 = -H; R3 = -CH2-(1,4-phenylene)-CH2N(CH3)2; R4 = -CH3; R5 = -H; and R6 = -H. Claims 20, 22-33, 35 and 36 read on the elected species. Affirmation of this election must be made by the inventor or joint inventor in replying to this Office action.
PNG
media_image2.png
200
400
media_image2.png
Greyscale
Similarly, 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 pyridin-2-amines of the formula (I), where R1 = -NR7R8, wherein R7 = -H and R8 = -substituted or unsubstituted alkyl; R2 = -H; R3 = -substituted or unsubstituted aralkyl; R4 = -substituted or unsubstituted alkyl; R5 = -H; and R6 = -H, 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 pyridin-2-amines of the formula (I), where R1 = -substituted or unsubstituted C1-C12 alkyl or NR7R8, wherein R7 = -H and R8 = -substituted or unsubstituted C1-C12 alkyl; R2 = -H; R3 = -substituted or unsubstituted C1-C12 alkylene-aryl; R4 = -substituted or unsubstituted C1-C12 alkyl; R5 = -H; and R6 = -H, respectively; 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 pyridin-2-amines of the formula (I), where R1 = -substituted or unsubstituted C1-C12 alkyl or NR7R8, wherein R7 = -H and R8 = -substituted or unsubstituted C1-C12 alkyl; R2 = -H; R3 = -substituted or unsubstituted C1-C12 alkylene-aryl; R4 = -substituted or unsubstituted C1-C12 alkyl; R5 = -H; and R6 = -H, respectively, particularly as stated in the section below entitled Claim Objections.
Likewise, 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.
Next, 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 21, 34 and 37-39 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 20, 22-33, 35 and 36 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 particular utility for the substituted pyridin-2-amines of the formula (I).
The following title is suggested: SUBSTITUTED PYRIDIN-2-AMINES AS TLR8 AGONISTS.
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 20 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(a), 35 U.S.C. § 112(b), Improper Markush Grouping and/or compliance with the Requirement for Restriction/Election of Species, mailed on October 8, 2025, the existing recitation should be replaced with the following recitation:
A compound of the formula (I):
PNG
media_image3.png
200
400
media_image3.png
Greyscale
(I)
or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof,
wherein:
R1 is C1-C12 alkyl, C1-C12 alkylene-cycloalkyl, C1-C12 alkylene-aryl, C1-C12 alkylene-heterocyclyl, C2-C12 alkenyl, or NHC1-C12 alkyl;
wherein the C1-C12 alkyl or C1-C12 alkylene is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, NO2, C(O)R’, C(O)NR’R’, C(O)NR’OR’, C(O)NR’S(O)2R’, C(O)OR’, NR’R’, NR'C(NR’)NR’R’, NR’C(O)R’, NR'S(O)2R’, N[C(O)R’]2, =NR’, N3, OR’, OC(O)R’, OC(O)NR’R’, OC(O)OR’, =O, OS(O)2R’, OS(O)3R’, P(O)R’OR’, P(O)NR’R’OR’, P(O)OR’OR’, SR’, S(O)R’, and S(O)2R’;
wherein the C2-C12 alkenyl is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, NO2, C(O)R’, C(O)NR’R’, C(O)NR’OR’, C(O)NR’S(O)2R’, C(O)OR’, NR’R’, NR'C(NR’)NR’R’, NR’C(O)R’, NR'S(O)2R’, N[C(O)R’]2, =NR’, N3, OR’, OC(O)R’, OC(O)NR’R’, OC(O)OR’, =O, OS(O)2R’, OS(O)3R’, P(O)R’OR’, P(O)NR’R’OR’, P(O)OR’OR’, SR’, S(O)R’, S(O)2R’, C3-C10 cycloalkyl, aryl, and heterocyclyl; and
wherein the cycloalkyl, aryl, or heterocyclyl of C1-C12 alkylene-cycloalkyl, C1-C12 alkylene-aryl, C1-C12 alkylene-heterocyclyl is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, NO2, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, C(O)R’, C(O)NR’R’, C(O)NR’OR’, C(O)NR’S(O)2R’, C(O)OR’, NR’R’, NR'C(NR’)NR’R’, NR’C(O)R’, NR'S(O)2R’, N[C(O)R’]2, =NR’, N3, OR’, OC(O)R’, OC(O)NR’R’, OC(O)OR’, =O, OS(O)2R’, OS(O)3R’, P(O)R’OR’, P(O)NR’R’OR’, P(O)OR’OR’, SR’, S(O)R’, S(O)2R’, C3-C10 cycloalkyl, aryl, and heterocyclyl;
R2 is H;
R3 is C1-C12 alkylene-aryl;
wherein the C1-C12 alkylene is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, NO2, C(O)R’, C(O)NR’R’, C(O)NR’OR’, C(O)NR’S(O)2R’, C(O)OR’, NR’R’, NR'C(NR’)NR’R’, NR’C(O)R’, NR'S(O)2R’, N[C(O)R’]2, =NR’, N3, OR’, OC(O)R’, OC(O)NR’R’, OC(O)OR’, =O, OS(O)2R’, OS(O)3R’, P(O)R’OR’, P(O)NR’R’OR’, P(O)OR’OR’, SR’, S(O)R’, and S(O)2R’; and
wherein the aryl of C1-C12 alkylene-aryl is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, NO2, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, C(O)R’, C(O)NR’R’, C(O)NR’OR’, C(O)NR’S(O)2R’, C(O)OR’, NR’R’, NR'C(NR’)NR’R’, NR’C(O)R’, NR'S(O)2R’, N[C(O)R’]2, =NR’, N3, OR’, OC(O)R’, OC(O)NR’R’, OC(O)OR’, =O, OS(O)2R’, OS(O)3R’, P(O)R’OR’, P(O)NR’R’OR’, P(O)OR’OR’, SR’, S(O)R’, S(O)2R’, C3-C10 cycloalkyl, aryl, and heterocyclyl;
R4 is C1-C12 alkyl, C1-C12 alkylene-cycloalkyl, C1-C12 alkylene-aryl, C1-C12 alkylene-heterocyclyl, or C2-C12 alkenyl;
wherein the C1-C12 alkyl or C1-C12 alkylene is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, NO2, C(O)R’, C(O)NR’R’, C(O)NR’OR’, C(O)NR’S(O)2R’, C(O)OR’, NR’R’, NR'C(NR’)NR’R’, NR’C(O)R’, NR'S(O)2R’, N[C(O)R’]2, =NR’, N3, OR’, OC(O)R’, OC(O)NR’R’, OC(O)OR’, =O, OS(O)2R’, OS(O)3R’, P(O)R’OR’, P(O)NR’R’OR’, P(O)OR’OR’, SR’, S(O)R’, and S(O)2R’;
wherein the C2-C12 alkenyl is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, NO2, C(O)R’, C(O)NR’R’, C(O)NR’OR’, C(O)NR’S(O)2R’, C(O)OR’, NR’R’, NR'C(NR’)NR’R’, NR’C(O)R’, NR'S(O)2R’, N[C(O)R’]2, =NR’, N3, OR’, OC(O)R’, OC(O)NR’R’, OC(O)OR’, =O, OS(O)2R’, OS(O)3R’, P(O)R’OR’, P(O)NR’R’OR’, P(O)OR’OR’, SR’, S(O)R’, S(O)2R’, C3-C10 cycloalkyl, aryl, and heterocyclyl; and
wherein the cycloalkyl, aryl, or heterocyclyl of C1-C12 alkylene-cycloalkyl, C1-C12 alkylene-aryl, C1-C12 alkylene-heterocyclyl is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, NO2, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, C(O)R’, C(O)NR’R’, C(O)NR’OR’, C(O)NR’S(O)2R’, C(O)OR’, NR’R’, NR'C(NR’)NR’R’, NR’C(O)R’, NR'S(O)2R’, N[C(O)R’]2, =NR’, N3, OR’, OC(O)R’, OC(O)NR’R’, OC(O)OR’, =O, OS(O)2R’, OS(O)3R’, P(O)R’OR’, P(O)NR’R’OR’, P(O)OR’OR’, SR’, S(O)R’, S(O)2R’, C3-C10 cycloalkyl, aryl, and heterocyclyl;
R5 is H;
R6 is H; and
each R’ is independently H, halogen, CN, NO₂, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, C(O)H, C(O)alkyl, C(O)OH, NH₂, OH, SH, C3-C10 cycloalkyl, aryl, or heterocyclyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 22 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(a), 35 U.S.C. § 112(b), 35 U.S.C. § 112(d), and/or Improper Markush Grouping, the existing recitation should be replaced with the following recitation:
The compound according to claim 20, wherein the compound is of formula (III):
PNG
media_image4.png
200
400
media_image4.png
Greyscale
(III)
or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein:
A is phenylene-RA, or naphthalenylene-RA;
each RA is independently H, halogen, CN, NO2, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, C(O)R’, C(O)NR’R’, C(O)NR’OR’, C(O)NR’S(O)2R’, C(O)OR’, NR’R’, NR'C(NR’)NR’R’, NR’C(O)R’, NR'S(O)2R’, N[C(O)R’]2, =NR’, N3, OR’, OC(O)R’, OC(O)NR’R’, OC(O)OR’, =O, OS(O)2R’, OS(O)3R’, P(O)R’OR’, P(O)NR’R’OR’, P(O)OR’OR’, SR’, S(O)R’, S(O)2R’, C3-C10 cycloalkyl, aryl, or heterocyclyl;
L is -(CH2)m-X-(CH2)n-:
X is -CR7R8-;
m is 0, 1, 2, 3, 4, or 5; and
n is 0, 1, 2, 3, 4, 5, or 6.
Appropriate correction is required. See MPEP § 2173.02.
Claim 23 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(a), 35 U.S.C. § 112(b), 35 U.S.C. § 112(d), and/or Improper Markush Grouping, the existing recitation should be replaced with the following recitation:
The compound according to claim 22, wherein the compound is of the following formula:
PNG
media_image5.png
200
400
media_image5.png
Greyscale
or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein:
RA0 is H, halogen, CN, NO2, C1-C12 alkyl, C(O)R’, C(O)NHR’, C(O)OR’, NR’R’, NHC(O)R’, OR’, OC(O)R’, SR’, S(O)R’, S(O)2R’, C3-C10 cycloalkyl, aryl, or heterocyclyl;
RA0’ is H, halogen, CN, NO2, C1-C12 alkyl, C(O)R’, C(O)NHR’, C(O)OR’, NR’R’, NHC(O)R’, OR’, OC(O)R’, SR’, S(O)R’, S(O)2R’, C3-C10 cycloalkyl, aryl, or heterocyclyl; and
RAp is H, halogen, CN, NO2, C1-C12 alkyl, C(O)R’, C(O)NHR’, C(O)OR’, NR’R’, NHC(O)R’, OR’, OC(O)R’, SR’, S(O)R’, S(O)2R’, C3-C10 cycloalkyl, aryl, or heterocyclyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 24 is objected to because of the following informalities: for brevity, clarity, precision and to avoid issues under 35 U.S.C. § 112(a), 35 U.S.C. § 112(b), 35 U.S.C. § 112(d), and/or Improper Markush Grouping, the existing recitation should be replaced with the following recitation:
The compound according to claim 23, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein:
m is 0, 1, 2, or 3; and
n is 0, 1, 2, or 3.
Appropriate correction is required. See MPEP § 2173.02.
Claim 25 is objected to because of the following informalities: for brevity, clarity, precision and to avoid issues under 35 U.S.C. § 112(a), 35 U.S.C. § 112(b), 35 U.S.C. § 112(d), and/or Improper Markush Grouping, the existing recitation should be replaced with the following recitation:
The compound according to claim 24, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein:
m is 0 or 1; and
n is 0 or 1.
Appropriate correction is required. See MPEP § 2173.02.
Claim 26 is objected to because of the following informalities: for brevity, clarity, precision and to avoid issues under 35 U.S.C. § 112(a), 35 U.S.C. § 112(b), 35 U.S.C. § 112(d), and/or Improper Markush Grouping, the existing recitation should be replaced with the following recitation:
The compound according to claim 23, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein:
RA0 is H, F, Cl, Br, C(O)R’, C(O)OR’, NR’R’, OR’, OC(O)R’, azetidin-1-yl, pyrrolidin-1-yl, piperidin-1-yl, azepan-1-yl, piperazin-1-yl, morpholin-4-yl, or 2-oxa-6-azaspiro[3.3]heptan-6-yl;
RA0’ is H, F, Cl, Br, C(O)R’, C(O)OR’, NR’R’, OR’, OC(O)R’, azetidin-1-yl, pyrrolidin-1-yl, piperidin-1-yl, azepan-1-yl, piperazin-1-yl, morpholin-4-yl, or 2-oxa-6-azaspiro[3.3]heptan-6-yl;
RAp is H, F, Cl, Br, C(O)R’, C(O)OR’, NR’R’, OR’, OC(O)R’, azetidin-1-yl, pyrrolidin-1-yl, piperidin-1-yl, azepan-1-yl, piperazin-1-yl, morpholin-4-yl, or 2-oxa-6-azaspiro[3.3]heptan-6-yl; and
each R’ is independently H, C1-C12 alkyl, or C3-C10 cycloalkyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 27 is objected to because of the following informalities: for brevity, clarity, precision and to avoid issues under 35 U.S.C. § 112(a), 35 U.S.C. § 112(b), 35 U.S.C. § 112(d), and/or Improper Markush Grouping, the existing recitation should be replaced with the following recitation:
The compound according to claim 26, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein:
RA0 is H, F, Cl, Br, C(O)OH, C(O)OC1-C10 alkyl, NH2, NHC1-C10 alkyl, NHC3-C10 cycloalkyl, N(C1-C10 alkyl)(C1-C10 alkyl), OH, OC1-C10 alkyl, azetidin-1-yl, pyrrolidin-1-yl, piperidin-1-yl, azepan-1-yl, piperazin-1-yl, morpholin-4-yl, or 2-oxa-6-azaspiro[3.3]heptan-6-yl;
RA0’ is H, F, Cl, Br, C(O)OH, C(O)OC1-C10 alkyl, NH2, NHC1-C10 alkyl, NHC3-C10 cycloalkyl, N(C1-C10 alkyl)(C1-C10 alkyl), OH, OC1-C10 alkyl, azetidin-1-yl, pyrrolidin-1-yl, piperidin-1-yl, azepan-1-yl, piperazin-1-yl, morpholin-4-yl, or 2-oxa-6-azaspiro[3.3]heptan-6-yl; and
RAp is H, F, Cl, Br, C(O)OH, C(O)OC1-C10 alkyl, NH2, NHC1-C10 alkyl, NHC3-C10 cycloalkyl, N(C1-C10 alkyl)(C1-C10 alkyl), OH, OC1-C10 alkyl, azetidin-1-yl, pyrrolidin-1-yl, piperidin-1-yl, azepan-1-yl, piperazin-1-yl, morpholin-4-yl, or 2-oxa-6-azaspiro[3.3]heptan-6-yl.
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(a), 35 U.S.C. § 112(b), 35 U.S.C. § 112(d) and/or Improper Markush Grouping, the existing recitation should be replaced with the following recitation:
The compound according to claim 23, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein R1 is C1-C12 alkyl, C1-C12 alkylene-cycloalkyl, C1-C12 alkylene-aryl, or C1-C12 alkylene-heterocyclyl;
wherein the C1-C12 alkyl or C1-C12 alkylene is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, NO2, C(O)R’, C(O)NR’R’, C(O)NR’OR’, C(O)NR’S(O)2R’, C(O)OR’, NR’R’, NR'C(NR’)NR’R’, NR’C(O)R’, NR'S(O)2R’, N[C(O)R’]2, =NR’, N3, OR’, OC(O)R’, OC(O)NR’R’, OC(O)OR’, =O, OS(O)2R’, OS(O)3R’, P(O)R’OR’, P(O)NR’R’OR’, P(O)OR’OR’, SR’, S(O)R’, and S(O)2R’; and
wherein the cycloalkyl, aryl, or heterocyclyl of C1-C12 alkylene-cycloalkyl, C1-C12 alkylene-aryl, C1-C12 alkylene-heterocyclyl is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, NO2, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, C(O)R’, C(O)NR’R’, C(O)NR’OR’, C(O)NR’S(O)2R’, C(O)OR’, NR’R’, NR'C(NR’)NR’R’, NR’C(O)R’, NR'S(O)2R’, N[C(O)R’]2, =NR’, N3, OR’, OC(O)R’, OC(O)NR’R’, OC(O)OR’, =O, OS(O)2R’, OS(O)3R’, P(O)R’OR’, P(O)NR’R’OR’, P(O)OR’OR’, SR’, S(O)R’, S(O)2R’, C3-C10 cycloalkyl, aryl, and heterocyclyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 29 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(a), 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 according to claim 20, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein R1 is CH2CH2CH2OCH3, CH2CH2CH2CH2CH3, or NHCH2CH2CH2CH3.
Appropriate correction is required. See MPEP § 2173.02.
Claim 30 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(a), 35 U.S.C. § 112(b), 35 U.S.C. § 112(d) and/or Improper Markush Grouping, the existing recitation should be replaced with the following recitation:
The compound according to claim 29, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, whereinR1 is CH2CH2CH2OCH3 or CH2CH2CH2CH2CH3.
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(a), 35 U.S.C. § 112(b), 35 U.S.C. § 112(d) and/or Improper Markush Grouping, the existing recitation should be replaced with the following recitation:
The compound according to claim 20, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein R4 is C1-C10 alkyl, wherein the C1-C10 alkyl is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, NO2, C(O)R’, C(O)NR’R’, C(O)NR’OR’, C(O)NR’S(O)2R’, C(O)OR’, NR’R’, NR'C(NR’)NR’R’, NR’C(O)R’, NR'S(O)2R’, N[C(O)R’]2, =NR’, N3, OR’, OC(O)R’, OC(O)NR’R’, OC(O)OR’, =O, OS(O)2R’, OS(O)3R’, P(O)R’OR’, P(O)NR’R’OR’, P(O)OR’OR’, SR’, S(O)R’, and S(O)2R’.
Appropriate correction is required. See MPEP § 2173.02.
Claim 32 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(a), 35 U.S.C. § 112(b), 35 U.S.C. § 112(d) and/or Improper Markush Grouping, the existing recitation should be replaced with the following recitation:
The compound according to claim 20, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein R4 is C1-C6 alkyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 33 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(a), 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 according to claim 32, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein R4 is CH3.
Appropriate correction is required. See MPEP § 2173.02.
Claim 35 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(a), 35 U.S.C. § 112(b), 35 U.S.C. § 112(d) and/or Improper Markush Grouping, the existing recitation should be replaced with the following recitation:
A compound selected from the group consisting of:
PNG
media_image6.png
200
400
media_image6.png
Greyscale
,
PNG
media_image7.png
200
400
media_image7.png
Greyscale
,
PNG
media_image8.png
200
400
media_image8.png
Greyscale
,
PNG
media_image9.png
200
400
media_image9.png
Greyscale
,
PNG
media_image10.png
200
400
media_image10.png
Greyscale
,
PNG
media_image11.png
200
400
media_image11.png
Greyscale
,
PNG
media_image12.png
200
400
media_image12.png
Greyscale
,
PNG
media_image13.png
200
400
media_image13.png
Greyscale
,
PNG
media_image14.png
200
400
media_image14.png
Greyscale
,
PNG
media_image15.png
200
400
media_image15.png
Greyscale
,
PNG
media_image16.png
200
400
media_image16.png
Greyscale
,
PNG
media_image17.png
200
400
media_image17.png
Greyscale
,
PNG
media_image18.png
200
400
media_image18.png
Greyscale
,
PNG
media_image19.png
200
400
media_image19.png
Greyscale
,
PNG
media_image20.png
200
400
media_image20.png
Greyscale
,
PNG
media_image21.png
200
400
media_image21.png
Greyscale
,
PNG
media_image22.png
200
400
media_image22.png
Greyscale
,
PNG
media_image23.png
200
400
media_image23.png
Greyscale
,
PNG
media_image24.png
200
400
media_image24.png
Greyscale
,
PNG
media_image25.png
200
400
media_image25.png
Greyscale
,
PNG
media_image26.png
200
400
media_image26.png
Greyscale
,
PNG
media_image27.png
200
400
media_image27.png
Greyscale
,
PNG
media_image28.png
200
400
media_image28.png
Greyscale
,
PNG
media_image29.png
200
400
media_image29.png
Greyscale
,
PNG
media_image30.png
200
400
media_image30.png
Greyscale
,
PNG
media_image31.png
200
400
media_image31.png
Greyscale
,
PNG
media_image32.png
200
400
media_image32.png
Greyscale
,
PNG
media_image33.png
200
400
media_image33.png
Greyscale
,
PNG
media_image34.png
200
400
media_image34.png
Greyscale
,
PNG
media_image35.png
200
400
media_image35.png
Greyscale
,
PNG
media_image36.png
200
400
media_image36.png
Greyscale
,
PNG
media_image37.png
200
400
media_image37.png
Greyscale
,
PNG
media_image38.png
200
400
media_image38.png
Greyscale
,
PNG
media_image39.png
200
400
media_image39.png
Greyscale
,
PNG
media_image40.png
200
400
media_image40.png
Greyscale
,
PNG
media_image41.png
200
400
media_image41.png
Greyscale
,
PNG
media_image42.png
200
400
media_image42.png
Greyscale
,
PNG
media_image43.png
200
400
media_image43.png
Greyscale
,
PNG
media_image44.png
200
400
media_image44.png
Greyscale
,
PNG
media_image45.png
200
400
media_image45.png
Greyscale
,
PNG
media_image46.png
200
400
media_image46.png
Greyscale
,
PNG
media_image47.png
200
400
media_image47.png
Greyscale
,
PNG
media_image48.png
200
400
media_image48.png
Greyscale
,
PNG
media_image49.png
200
400
media_image49.png
Greyscale
,
PNG
media_image50.png
200
400
media_image50.png
Greyscale
,
PNG
media_image51.png
200
400
media_image51.png
Greyscale
,
PNG
media_image52.png
200
400
media_image52.png
Greyscale
,
PNG
media_image53.png
200
400
media_image53.png
Greyscale
,
PNG
media_image54.png
200
400
media_image54.png
Greyscale
,
PNG
media_image55.png
200
400
media_image55.png
Greyscale
,
PNG
media_image56.png
200
400
media_image56.png
Greyscale
,
PNG
media_image57.png
200
400
media_image57.png
Greyscale
,
PNG
media_image58.png
200
400
media_image58.png
Greyscale
,
PNG
media_image59.png
200
400
media_image59.png
Greyscale
,
PNG
media_image60.png
200
400
media_image60.png
Greyscale
,
PNG
media_image61.png
200
400
media_image61.png
Greyscale
,
and
PNG
media_image62.png
200
400
media_image62.png
Greyscale
,
or a pharmaceutically acceptable salt or tautomer thereof.
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(a), 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 a pharmaceutically acceptable excipient and a compound according to claim 20, or a pharmaceutically acceptable salt, stereoisomer, or tautomer 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.
Esters, prodrugs, solvates, and/or isotopic derivatives of substituted pyridin-2-amines of the formula (I)
Claims 20, 22-33, 35 and 36 are rejected under 35 U.S.C. § 112(a) because the specification, while being enabling for substituted pyridin-2-amines of the formula (I), does not reasonably provide enablement for esters, prodrugs, solvates, and/or isotopic derivatives of substituted pyridin-2-amines of the formula (I). 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. Esters, prodrugs, solvates, and/or isotopic derivatives of substituted pyridin-2-amines of the formula (I), as recited in claims 20, 22-33, 35 and 36, respectively, 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 esters, prodrugs, solvates, and/or isotopic derivatives of substituted pyridin-2-amines of the formula (I).
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:
PNG
media_image1.png
200
400
media_image1.png
Greyscale
(a) Breadth of the claims - the breadth of the claims includes substituted pyridin-2-amines of the formula (I), shown to the right below, as well as the myriad of potential esters, prodrugs, solvates, and/or isotopic derivatives formulated from these substituted pyridin-2-amines of the formula (I), shown to the right, respectively;
(b) Nature of the invention - the nature of the invention is evaluation of substituted pyridin-2-amines of the formula (I), shown to the right above, and/or esters, prodrugs, solvates, and/or isotopic derivatives thereof, and the pharmacokinetic behavior of these substances as toll-like receptor 8 (TLR8) selective agonists;
(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, EP 4253383 provides a synthesis of the instantly recited substituted pyridin-2-amines of the formula (I) {Liao, et al. EP 4253383, 2023};
(d) Level of one of ordinary skill in the art - the artisans synthesizing the inventor’s or joint inventor’s substituted pyridin-2-amines of the formula (I), and/or esters, prodrugs, solvates, and/or isotopic derivatives thereof, 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 Liao, et al. in EP 4253383, whether the instantly recited esters, prodrugs, solvates, and/or isotopic derivatives of substituted pyridin-2-amines of the formula (I) are enabled. Likewise, the following excerpt is taken from Dörwald, which has relevance to the synthesis of esters and/or isotopic derivatives of substituted pyridin-2-amines of the formula (I) {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).
Next, the following excerpt is taken from Vippagunta, et al., with respect to the synthesis of solvates of substituted pyridin-2-amines of the formula (I) {Vippagunta, et al. Advanced Drug Delivery Reviews, 48, 2001, 18}:
Predicting the formation of solvates or hydrates of a compound and the number of molecules of water or solvent incorporated into the crystal lattice of a compound is complex and difficult. Each solid compound responds uniquely to the possible formation of solvates or hydrates and hence generalizations cannot be made for a series of related compounds. Certain molecular shapes and features favor the formation of crystals without solvent; these compounds tend to be stabilized by efficient packing of molecules in the crystal lattice, whereas other crystal forms are more stable in the presence of water and/or solvents. There may be too many possibilities so that no computer programs are currently available for predicting the crystal structures of hydrates and solvates.
Moreover, the following excerpt is taken from Burger’s, with respect to the synthesis of prodrugs of pyridin-2-amines of the formula (I) {Wolff, Manfred E., Ed. Burger’s Medicinal Chemistry and Drug Discovery - Fifth Edition, Volume 1: Principles and Practice, New York: John Wiley & Sons, 1994, 975-977}:
The design of prodrugs in a rational manner requires that the underlying causes which necessitate or stimulate the use of the prodrug approach be defined and clearly understood. It may then be possible to identify the means by which the difficulties can be overcome. The rational design of the prodrug can thus be divided into three basic steps: (1) identification of the drug delivery problem; (2) identification of the physiochemical properties required for optimal delivery; and (3) selection of a prodrug derivative that has the proper physiochemical properties and that will be cleaved in the desired biological compartment.
The difficulty of extrapolating data from animal to humans encountered during toxicokinetic and toxicologic studies with drugs is amplified with prodrugs, since not only metabolism of the active moiety might differ, but also its availability from the prodrug. As a matter of fact, there is presently no published rational for the conduct of animal and human pharmacokinetic programs during prodrug research and development.
(f) Amount of direction provided by the inventor - the invention lacks direction with respect to making and/or using esters, prodrugs, solvates, and/or isotopic derivatives of substituted pyridin-2-amines of the formula (I);
(g) Existence of working examples - the inventor or joint inventor has provided sufficient guidance to make and/or use substituted pyridin-2-amines of the formula (I); however, the disclosure is insufficient to allow extrapolation of the limited examples to enable the instantly recited esters, prodrugs, solvates, and/or isotopic derivatives of substituted pyridin-2-amines of the formula (I). The specification lacks working examples of esters, prodrugs, solvates, and/or isotopic derivatives of substituted pyridin-2-amines of the formula (I).
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.
PNG
media_image63.png
200
400
media_image63.png
Greyscale
(h) Quantity of experimentation needed to make or use the invention based on the content of the disclosure - predicting whether a recited compound, and/or an ester, prodrug, solvate, and/or isotopic derivative thereof, 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 required by 35 U.S.C. § 112(a) to enable the instantly recited esters, prodrugs, solvates, and/or isotopic derivatives of substituted pyridin-2-amines of the formula (I). Thus, it is unclear, based on the guidance provided by the specification, whether a solvate of a substituted pyridin-2-amine of the formula (I), such as N3-butyl-5-(4-((dimethylamino)methyl)benzyl)-6-methylpyridine-2,3-diamine dihydrate, shown to the left above, is either synthetically feasible or possesses utility as a toll-like receptor 8 (TLR8) selective agonist.
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 esters, prodrugs, solvates, and/or isotopic derivatives of substituted pyridin-2-amines of the formula (I), 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 20, 22-33 and 36 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 term, substituted, in claim 20, with regard to R1, R2, R3, R4, R5, R6, R5 and R6, R7, and/or R8, respectively, is a relative term which renders the claims indefinite. The term, 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 page 16, uses open language, such as such as, to define the term, substituted, using a boiler plate list of functional groups, such as OR’, =O, 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 pyridin-2-amines of the formula (I) have been rendered indefinite by the use of the term, substituted, with regard to R1, R2, R3, R4, R5, R6, R5 and R6, R7, 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 22 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 claim 22 recites the limitation, The pyridin-2-amine… according to claim 20, wherein… L is… -(CH2)m-X-(CH2)n-, wherein X is… -CR7R8-, -CO-, -CONH-, -C(O)O-, -NR7-, -NHCO-, -O-, -OC(O)-, -S-, -S(O)t-, or a combination thereof, in lines 1-8 of the claim. There is insufficient antecedent basis, in claim 20, for this limitation, with respect to the substituted pyridin-2-amines of the formula (I). According to claim 20, R3 is recited as optionally substituted alkyl, optionally substituted alkylene-cycloalkyl, optionally substituted alkylene-aryl, or optionally substituted alkylene-heterocyclyl, with respect to the substituted pyridin-2-amines of the formula (I).
The examiner suggests amending the claim, 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 20, 22-26, 30, 31 and 33 are rejected under 35 U.S.C. § 102(a)(1) as being anticipated by the CAS Registry Database.
PNG
media_image1.png
200
400
media_image1.png
Greyscale
The inventor or joint inventor should note that the instant invention recites a substituted pyridin-2-amine of the formula (I), shown to the left, where R1 = -substituted or unsubstituted alkyl; R2 = -H; R3 = -substituted or unsubstituted aralkyl; R4 = -substituted or unsubstituted alkyl; R5 = -H; and R6 = -H, respectively, as a toll-like receptor 8 (TLR8) selective agonist.
PNG
media_image64.png
200
400
media_image64.png
Greyscale
Similarly, the inventor or joint inventor should further note that the CAS Registry Database teaches a substituted pyridin-2-amine of the formula (I), shown to the right, where R1 = -CH2OH; R2 = -H; R3 = -CH2-phenyl; R4 = -CF3; R5 = -H; and R6 = -H, respectively [CAS Registry Database, RN: 1413281-42-1, entered STN: 10 Dec 2012, accessed by Examiner D. M. Willis on February 9, 2026].
Likewise, the inventor or joint inventor should further 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)}.
Next, 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)}.
Then, 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)}.
Moreover, 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)}.
Also, 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 20, 22-33, 35 and 36 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 pyridin-2-amines of the formula (I) is improper, since the substituted pyridin-2-amines of the formula (I), as recited in claims 20, 35 and 36, 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 pyridin-2-amines of the formula (I), where R1 = -substituted or unsubstituted C1-C12 alkyl or NR7R8, wherein R7 = -H and R8 = -substituted or unsubstituted C1-C12 alkyl; R2 = -H; R3 = -substituted or unsubstituted C1-C12 alkylene-aryl; R4 = -substituted or unsubstituted C1-C12 alkyl; R5 = -H; and R6 = -H, respectively, 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