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 1-14 and 16-19 are pending in the instant invention. According to the Amendments to the Claims, filed October 31, 2022, claims 2-13 and 16-19 were amended and claim 15 was cancelled.
Status of Priority
This invention is a 35 U.S.C. § 371 National Stage Filing of International Application No. PCT/EP2021/061318, filed April 29, 2021, which claims priority under 35 U.S.C. § 119(a-d) to EP 20172580.1, filed May 1, 2020.
Restrictions / Election of Species
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The forthcoming first Office action and prosecution on the merits includes (1) claims 1-14 and 19, drawn to substituted 1,2,3-triazoles of the Formula (1), shown to the right, and/or a pharmaceutical composition thereof; and (2) claims 16-18, drawn to a method of treating or preventing a bacterial infection and/or a fungal infection in a subject, comprising administering… a substituted 1,2,3-triazole of the Formula (1), shown to the right above, or a pharmaceutical composition thereof, respectively.
Thus, a first Office action and prosecution on the merits of claims 1-14 and 16-19 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 1,2,3-triazoles of the Formula (1); and b) a particular utility for the substituted 1,2,3-triazoles of the Formula (1).
The following title is suggested: SUBSTITUTED 1,2,3-TRIAZOLES AS ANTIBACTERIAL AND ANTIFUNGALPLEUROMUTILIN CONJUGATES.
Appropriate correction is required.
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 (1):
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(1)
or a pharmaceutically acceptable salt or stereoisomer thereof,
wherein:
Ra is H, C1-C5 alkyl, C1-C5 aminoalkyl, C1-C5 hydroxyalkyl, NH2, OH, OCH3, or OCH2CH3;
------ is a single bond;
ring A is aryl or heteroaryl, wherein the aryl or heteroaryl is optionally substituted with one or more substituents independently selected from the group consisting of D, F, Cl, Br, I, CN, NO2, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C(O)NH2, C(O)OH, NH2, NHC1-C6 alkyl, N(C1-C6 alkyl)2, OH, OC1-C6 alkyl, C3-C8 cycloalkyl, heterocyclyl, aryl, and heteroaryl; and
(i) X is C1-C5 alkylene, C2-C5 alkenylene, C2-C5 alkynylene, -NH-, -O-, or -S-;
wherein the -NH- is optionally substituted with one substituent selected from the group consisting of D and C1-C3 alkyl; and
wherein the C1-C5 alkylene, C2-C5 alkenylene, or C2-C5 alkynylene is optionally substituted with one or more substituents independently selected from the group consisting of D, F, Cl, Br, and I; and
R1 is F, Cl, Br, I, CN, NO2, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, CH(NH), C(O)H, C(O)NH2, C(O)NHNH2, C(O)OH, C(O)OC1-6 alkyl, C(O)OC2-6 alkenyl, C(O)OC2-6 alkynyl, C(O)SH, C(O)phenyl, C(O)aminophenyl, C(O)hydroxyphenyl, C(O)methoxyphenyl, C(O)pyridinyl, C(O)aminopyridinyl, C(O)hydroxypyridinyl, C(O)methoxypyridinyl, C(O)pyridazinyl, C(O)aminopyridazinyl, C(O)hydroxypyridazinyl, C(O)methoxypyridazinyl, C(O)pyrimidinyl, C(O)aminopyrimidinyl, C(O)hydroxypyrimidinyl, C(O)methoxypyrimidinyl, C(O)pyrazinyl, C(O)aminopyrazinyl, C(O)hydroxypyrazinyl, C(O)methoxypyrazinyl, NH2, NHC1-C6 alkyl, NHC1-C6 aminoalkyl, NHC(NH)NH2, N(C1-C6 alkyl)2, OH, OC1-C6 alkyl, SH, S(O)2OH, C3-C8 cycloalkyl, heterocyclyl, aryl, or heteroaryl;
wherein the C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, or OC1-C6 alkyl is optionally substituted with one or more substituents independently selected from the group consisting of D, F, Cl, Br, I, CN, NO2, CH(NH), C(O)H, C(O)NH2, C(O)NHNH2, C(O)OH, C(O)OC1-6 alkyl, C(O)OC2-6 alkenyl, C(O)OC2-6 alkynyl, C(O)SH, NH2, NHC1-C6 alkyl, NHC1-C6 aminoalkyl, NHC(NH)NH2, N(C1-C6 alkyl)2, OH, OC1-C6 alkyl, SH, S(O)2OH, C3-C8 cycloalkyl, piperazinyl, aryl, and heteroaryl;
wherein the C3-C8 cycloalkyl or heterocyclyl is optionally substituted with one or more substituents independently selected from the group consisting of D, F, Cl, Br, I, CN, NO2, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, CH(NH), C(O)H, C(O)NH2, C(O)NHNH2, C(O)OH, C(O)OC1-6 alkyl, C(O)OC2-6 alkenyl, C(O)OC2-6 alkynyl, C(O)SH, NH2, NHC1-C6 alkyl, NHC1-C6 aminoalkyl, NHC(NH)NH2, N(C1-C6 alkyl)2, OH, OC1-C6 alkyl, =O, SH, S(O)2OH, C3-C8 cycloalkyl, piperazinyl, aryl, and heteroaryl;
wherein the aryl or heteroaryl is optionally substituted with one or more substituents independently selected from the group consisting of D, F, Cl, Br, I, CN, NO2, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, CH(NH), C(O)H, C(O)NH2, C(O)NHNH2, C(O)OH, C(O)OC1-6 alkyl, C(O)OC2-6 alkenyl, C(O)OC2-6 alkynyl, C(O)SH, NH2, NHC1-C6 alkyl, NHC1-C6 aminoalkyl, NHC(NH)NH2, N(C1-C6 alkyl)2, OH, OC1-C6 alkyl, SH, S(O)2OH, C3-C8 cycloalkyl, piperazinyl, aryl, and heteroaryl; and
wherein each piperazinyl substituent is optionally and independently substituted with one or more independently selected C1-C5 alkyl substituents; or
(ii) XR1 is CN.
Appropriate correction is required. See MPEP § 2173.02.
Claim 2 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 according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein ring A is a 6-membered aryl or 6-membered heteroaryl, wherein the 6-membered aryl or 6-membered heteroaryl is optionally substituted with one or more substituents independently selected from the group consisting of D, F, Cl, Br, I, CN, NO2, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C(O)NH2, C(O)OH, NH2, NHC1-C6 alkyl, N(C1-C6 alkyl)2, OH, OC1-C6 alkyl, C3-C8 cycloalkyl, heterocyclyl, aryl, and heteroaryl.
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 according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein ring A is aryl or heteroaryl, wherein the aryl or heteroaryl is optionally substituted with one or more substituents independently selected from the group consisting of D, F, Cl, Br, I, CN, NO2, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, C(O)NH2, C(O)OH, NH2, NHC1-C4 alkyl, N(C1-C4 alkyl)2, OH, OC1-C4 alkyl, C3-C6 cycloalkyl, aryl, and heteroaryl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 4 is objected to because of the following informalities: for brevity, 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 according to claim 1, or a stereoisomer thereof, wherein the stereoisomer of the compound is represented by Formula (2):
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(2)
or a pharmaceutically acceptable salt thereof,
wherein:
G is CH or N;
Q is CH or N;
Y is CH or N;
Z is CH or N;
R2 is H, D, F, Cl, Br, I, CN, NO2, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C(O)NH2, C(O)OH, NH2, NHC1-C6 alkyl, N(C1-C6 alkyl)2, OH, OC1-C6 alkyl, C3-C8 cycloalkyl, aryl, and heteroaryl; and
R3 is H, D, F, Cl, Br, I, CN, NO2, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C(O)NH2, C(O)OH, NH2, NHC1-C6 alkyl, N(C1-C6 alkyl)2, OH, OC1-C6 alkyl, C3-C8 cycloalkyl, aryl, and heteroaryl;
with the proviso that X is bonded to the meta or para position.
Appropriate correction is required. See MPEP § 2173.02.
Claim 5 is objected to because of the following informalities: for brevity, 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 according to claim 1, or a stereoisomer thereof, wherein the stereoisomer of the compound is represented by Formula (2a):
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(2a)
or a pharmaceutically acceptable salt thereof,
wherein:
G is CH or N;
Q is CH or N;
Y is CH or N;
Z is CH or N;
R2 is H, D, F, Cl, Br, I, CN, NO2, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C(O)NH2, C(O)OH, NH2, NHC1-C6 alkyl, N(C1-C6 alkyl)2, OH, OC1-C6 alkyl, C3-C8 cycloalkyl, aryl, and heteroaryl; and
R3 is H, D, F, Cl, Br, I, CN, NO2, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C(O)NH2, C(O)OH, NH2, NHC1-C6 alkyl, N(C1-C6 alkyl)2, OH, OC1-C6 alkyl, C3-C8 cycloalkyl, aryl, and heteroaryl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 6 is objected to because of the following informalities: for brevity, 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 according to claim 1, or a stereoisomer thereof, wherein the stereoisomer of the compound is represented by Formula (2b):
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(2b)
or a pharmaceutically acceptable salt thereof,
wherein:
G is CH or N;
Q is CH or N;
Y is CH or N;
Z is CH or N;
R2 is H, D, F, Cl, Br, I, CN, NO2, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C(O)NH2, C(O)OH, NH2, NHC1-C6 alkyl, N(C1-C6 alkyl)2, OH, OC1-C6 alkyl, C3-C8 cycloalkyl, aryl, and heteroaryl; and
R3 is H, D, F, Cl, Br, I, CN, NO2, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C(O)NH2, C(O)OH, NH2, NHC1-C6 alkyl, N(C1-C6 alkyl)2, OH, OC1-C6 alkyl, C3-C8 cycloalkyl, aryl, and heteroaryl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 7 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 according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein X is C1-C5 alkylene, C2-C5 alkenylene, C2-C5 alkynylene, -NH-, -O-, or -S-;
wherein the -NH- is optionally substituted with one C1-C3 alkyl substituent; and
wherein the C1-C5 alkylene, C2-C5 alkenylene, or C2-C5 alkynylene is optionally substituted with one or more substituents independently selected from the group consisting of D, F, Cl, Br, and I.
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 according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R1 is F, Cl, Br, I, CN, NO2, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, CH(NH), C(O)H, C(O)NH2, C(O)NHNH2, C(O)OH, C(O)OC1-4 alkyl, C(O)OC2-4 alkenyl, C(O)OC2-4 alkynyl, C(O)SH, C(O)phenyl, C(O)aminophenyl, C(O)hydroxyphenyl, C(O)methoxyphenyl, C(O)pyridinyl, C(O)aminopyridinyl, C(O)hydroxypyridinyl, C(O)methoxypyridinyl, C(O)pyridazinyl, C(O)aminopyridazinyl, C(O)hydroxypyridazinyl, C(O)methoxypyridazinyl, C(O)pyrimidinyl, C(O)aminopyrimidinyl, C(O)hydroxypyrimidinyl, C(O)methoxypyrimidinyl, C(O)pyrazinyl, C(O)aminopyrazinyl, C(O)hydroxypyrazinyl, C(O)methoxypyrazinyl, NH2, NHC1-C4 alkyl, NHC1-C4 aminoalkyl, NHC(NH)NH2, N(C1-C4 alkyl)2, OH, OC1-C4 alkyl, SH, S(O)2OH, C3-C6 cycloalkyl, heterocyclyl, aryl, or heteroaryl;
wherein the C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, or OC1-C4 alkyl is optionally substituted with one or more substituents independently selected from the group consisting of D, F, Cl, Br, I, CN, NO2, CH(NH), C(O)H, C(O)NH2, C(O)NHNH2, C(O)OH, C(O)OC1-4 alkyl, C(O)OC2-4 alkenyl, C(O)OC2-4 alkynyl, C(O)SH, NH2, NHC1-C4 alkyl, NHC1-C4 aminoalkyl, NHC(NH)NH2, N(C1-C4 alkyl)2, OH, OC1-C4 alkyl, SH, S(O)2OH, C3-C6 cycloalkyl, piperazinyl, aryl, and heteroaryl;
wherein the C3-C6 cycloalkyl or heterocyclyl is optionally substituted with one or more substituents independently selected from the group consisting of D, F, Cl, Br, I, CN, NO2, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, CH(NH), C(O)H, C(O)NH2, C(O)NHNH2, C(O)OH, C(O)OC1-4 alkyl, C(O)OC2-4 alkenyl, C(O)OC2-4 alkynyl, C(O)SH, NH2, NHC1-C4 alkyl, NHC1-C6 aminoalkyl, NHC(NH)NH2, N(C1-C4 alkyl)2, OH, OC1-C4 alkyl, =O, SH, S(O)2OH, C3-C6 cycloalkyl, piperazinyl, aryl, and heteroaryl;
wherein the aryl or heteroaryl is optionally substituted with one or more substituents independently selected from the group consisting of D, F, Cl, Br, I, CN, NO2, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, CH(NH), C(O)H, C(O)NH2, C(O)NHNH2, C(O)OH, C(O)OC1-4 alkyl, C(O)OC2-4 alkenyl, C(O)OC2-4 alkynyl, C(O)SH, NH2, NHC1-C4 alkyl, NHC1-C4 aminoalkyl, NHC(NH)NH2, N(C1-C4 alkyl)2, OH, OC1-C4 alkyl, SH, S(O)2OH, C3-C6 cycloalkyl, piperazinyl, aryl, and heteroaryl; and
wherein each piperazinyl substituent is optionally and independently substituted with one or more independently selected C1-C5 alkyl substituents.
Appropriate correction is required. See MPEP § 2173.02.
Claim 9 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 according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R1 is a monocyclic heterocyclyl, bicyclic heterocyclyl, monocyclic heteroaryl, or bicyclic heteroaryl;
wherein the monocyclic heterocyclyl or bicyclic heterocyclyl is optionally substituted with one or more substituents independently selected from the group consisting of D, F, Cl, Br, I, CN, NO2, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, CH(NH), C(O)H, C(O)NH2, C(O)NHNH2, C(O)OH, C(O)OC1-6 alkyl, C(O)OC2-6 alkenyl, C(O)OC2-6 alkynyl, C(O)SH, NH2, NHC1-C6 alkyl, NHC1-C6 aminoalkyl, NHC(NH)NH2, N(C1-C6 alkyl)2, OH, OC1-C6 alkyl, =O, SH, S(O)2OH, C3-C8 cycloalkyl, piperazinyl, aryl, and heteroaryl;
wherein the monocyclic heteroaryl or bicyclic heteroaryl is optionally substituted with one or more substituents independently selected from the group consisting of D, F, Cl, Br, I, CN, NO2, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, CH(NH), C(O)H, C(O)NH2, C(O)NHNH2, C(O)OH, C(O)OC1-6 alkyl, C(O)OC2-6 alkenyl, C(O)OC2-6 alkynyl, C(O)SH, NH2, NHC1-C6 alkyl, NHC1-C6 aminoalkyl, NHC(NH)NH2, N(C1-C6 alkyl)2, OH, OC1-C6 alkyl, SH, S(O)2OH, C3-C8 cycloalkyl, piperazinyl, aryl, and heteroaryl; and
wherein each piperazinyl substituent is optionally and independently substituted with one or more independently selected C1-C5 alkyl substituents.
Appropriate correction is required. See MPEP § 2173.02.
Claim 10 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 according to claim 9, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R1 is pyrrolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, piperidinyl, tetrahydropyranyl, pyranyl, thianyl, thiopyranyl, pyrazolidinyl, imidazolidinyl, isoxazolidinyl, oxazolidinyl, isothiazolidinyl, thiazolidinyl, dioxolanyl, dithiolanyl, dioxazolyl, dithiazolyl, diazinanyl, morpholinyl, oxazinyl, thiomorpholinyl, thiazinyl, dioxanyl, dioxinyl, triazinanyl, trioxanyl, trithianyl, isoindolyl, indolinyl, phthalimidyl, isochromenyl, chromenyl, tetrahydroquinolinyl, benzooxazinyl, pyrrolyl, furanyl, thiophenyl, pyrazolyl, imidazolyl, isoxazolyl, oxazolyl, isothiazolyl, thiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, pyridinyl, diazinyl, triazinyl, indolyl, isobenzofuranyl, benzofuranyl, benzothiophenyl, indazolyl, benzimidazolyl, benzoisoxazolyl, benzooxazolyl, benzoisothiazolyl, benzothiazolyl, isoquinolinyl, quinolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, azaindolyl, azaindazolyl, purinyl, adeninyl, guaninyl, xanthinyl, hypoxanthinyl, naphthyridinyl, pyridopyrimidinyl, pyridopyrazinyl, or pteridinyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 11 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 according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein:
(a) the C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, or OC1-C6 alkyl of R1 is optionally substituted with one or more substituents independently selected from the group consisting of D, F, Cl, Br, I, CN, NO2, CH(NH), C(O)H, C(O)NH2, C(O)NHNH2, C(O)OH, C(O)OC1-4 alkyl, C(O)OC2-4 alkenyl, C(O)OC2-4 alkynyl, C(O)SH, NH2, NHC1-C4 alkyl, NHC1-C4 aminoalkyl, NHC(NH)NH2, N(C1-C4 alkyl)2, OH, OC1-C4 alkyl, SH, S(O)2OH, C3-C6 cycloalkyl, piperazinyl, aryl, and heteroaryl;
(b) the C3-C8 cycloalkyl or heterocyclyl of R1 is optionally substituted with one or more substituents independently selected from the group consisting of D, F, Cl, Br, I, CN, NO2, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, CH(NH), C(O)H, C(O)NH2, C(O)NHNH2, C(O)OH, C(O)OC1-4 alkyl, C(O)OC2-4 alkenyl, C(O)OC2-4 alkynyl, C(O)SH, NH2, NHC1-C4 alkyl, NHC1-C4 aminoalkyl, NHC(NH)NH2, N(C1-C4 alkyl)2, OH, OC1-C4 alkyl, =O, SH, S(O)2OH, C3-C6 cycloalkyl, piperazinyl, aryl, and heteroaryl;
(c) the aryl or heteroaryl of R1 is optionally substituted with one or more substituents independently selected from the group consisting of D, F, Cl, Br, I, CN, NO2, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, CH(NH), C(O)H, C(O)NH2, C(O)NHNH2, C(O)OH, C(O)OC1-4 alkyl, C(O)OC2-4 alkenyl, C(O)OC2-4 alkynyl, C(O)SH, NH2, NHC1-C4 alkyl, NHC1-C4 aminoalkyl, NHC(NH)NH2, N(C1-C4 alkyl)2, OH, OC1-C4 alkyl, SH, S(O)2OH, C3-C6 cycloalkyl, piperazinyl, aryl, and heteroaryl; and
(d) each piperazinyl substituent is optionally and independently substituted with one or more independently selected C1-C5 alkyl substituents.
Appropriate correction is required. See MPEP § 2173.02.
Claim 12 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 according to claim 1, or a stereoisomer thereof, wherein the compound, or stereoisomer thereof, is selected from the group consisting of:
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, ,
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or a pharmaceutically acceptable salt thereof.
Appropriate correction is required. See MPEP § 2173.02.
Claim 13 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 carrier, diluent, or excipient and a compound according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof.
Appropriate correction is required. See MPEP § 2173.02.
Claim 14 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 pharmaceutical composition according to claim 13, wherein the pharmaceutical composition further comprises at least one adjuvant.
Appropriate correction is required. See MPEP § 2173.02.
Claim 16 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(s):
16. A method for treating a bacterial infection in a subject, wherein the method comprises administering to the subject in need thereof a therapeutically effective amount of a compound according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof.
20. A method for treating a bacterial infection in a subject, wherein the method comprises administering to the subject in need thereof a therapeutically effective amount of the pharmaceutical composition according to claim 13.
21. A method for treating a fungal infection in a subject, wherein the method comprises administering to the subject in need thereof a therapeutically effective amount of a compound according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof.
22. A method for treating a fungal infection in a subject, wherein the method comprises administering to the subject in need thereof a therapeutically effective amount of the pharmaceutical composition according to claim 13.
Appropriate correction is required. See MPEP § 2173.02.
Claim 17 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(s):
17. The method according to claim 16, wherein the bacterial infection is caused by a bacterium or bacteria selected from the group consisting of chlamydia trachomatis, cutibacterium acnes, an enterobacteriacae, an enterococcus, haemophilus influenza, listeria monocytogenes, morganella morganii, mycoplasma pneumonia, methicillin-resistant staphylococcus aureus (MRSA), staphylococcus epidermidis, staphylococcus haemolyticus, an alpha-hemolytic streptococcus, and a beta-hemolytic streptococcus.
23. The method according to claim 20, wherein the bacterial infection is caused by a bacterium or bacteria selected from the group consisting of chlamydia trachomatis, cutibacterium acnes, an enterobacteriacae, an enterococcus, haemophilus influenza, listeria monocytogenes, morganella morganii, mycoplasma pneumonia, methicillin-resistant staphylococcus aureus (MRSA), staphylococcus epidermidis, staphylococcus haemolyticus, an alpha-hemolytic streptococcus, and a beta-hemolytic streptococcus.
24. The method according to claim 17, wherein the enterobacteriacae is escherichia coli.
25. The method according to claim 17, wherein the enterococcus is enterococcus faecalis or a vancomycin-resistant enterococcus (VRE).
26. The method according to claim 17, wherein the alpha-hemolytic streptococcus or beta-hemolytic streptococcus is streptococcus aureus or streptococcus pneumoniae.
Appropriate correction is required. See MPEP § 2173.02.
Claim 18 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(s):
18. The method according to claim 17, wherein the bacterial infection is caused by a bacterium or bacteria selected from the group consisting of enterococcus faecalis, a vancomycin-resistant enterococcus (VRE), methicillin-resistant staphylococcus aureus (MRSA), and streptococcus pneumoniae.
27. The method according to claim 23, wherein the bacterial infection is caused by a bacterium or bacteria selected from the group consisting of enterococcus faecalis, a vancomycin-resistant enterococcus (VRE), methicillin-resistant staphylococcus aureus (MRSA), and streptococcus pneumoniae.
Appropriate correction is required. See MPEP § 2173.02.
Claim 19 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 kit comprising:
(i) a compound according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof; or
(i) a pharmaceutical composition according to claim 13;
(ii) at least one additional therapeutic agent; and optionally,
(iii) instructions for use.
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 1-11, 13, 14 and 16-19 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 A, X, and R1, respectively, is a relative phrase which renders the claim 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 8-9, uses open language, such as for example, to define the phrase, optionally substituted, as hydroxy, oxo, etc.; however, neither the specification, nor the claim, explicitly limits the invention to any specifically disclosed or recited embodiments. Consequently, the substituted 1,2,3-triazoles of the Formula (1) have been rendered indefinite by the use of the phrase, optionally substituted, with regard to A, X, and R1, 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.
Claims 1-11, 13, 14 and 16-19 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 claims 1 and 4-6 independently recite the broad limitation, H, C1-C5 alkyl, C1-C5 aminoalkyl, C1-C5 hydroxyalkyl, NH2, OH, OCH3, and OCH2CH3, respectively, with regard to Ra, and the claims also independently recite H, with regard to Ra, 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.
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 1-7, 11, 13, 14 and 16-19 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 the phrase, a radical of an optionally substituted mono- or bicyclic ring system or an optionally substituted acyclic system comprising a number of q carbon atoms, in claims 1 and 4-6, respectively, with regard to R1, is a relative phrase which renders the claims indefinite. The phrase, a radical of an optionally substituted mono- or bicyclic ring system or an optionally substituted acyclic system comprising a number of q carbon atoms, is not defined by the claims, 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 fails to adequately define the phrase, a radical of an optionally substituted mono- or bicyclic ring system or an optionally substituted acyclic system comprising a number of q carbon atoms. Similarly, the meaning of a phrase cannot depend on the unrestrained, subjective opinion of the inventor or joint inventor practicing the invention. Likewise, neither the specification, nor the claims, explicitly limits the invention to any specifically disclosed or recited embodiments. Consequently, the substituted 1,2,3-triazoles of the Formula (1) have been rendered indefinite by the use of the phrase, a radical of an optionally substituted mono- or bicyclic ring system or an optionally substituted acyclic system comprising a number of q carbon atoms, with respect to R1. {See Datamize LLC v. Plumtree Software, Inc., 417 F.3d 1342, 1347-48, 75 USPQ2d 1801, 1807 (Fed. Cir. 2005); and MPEP § 2173.05(b)}.
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 3 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 3 recites the limitation, oxo, with respect to A, where the limitation is implausible, resulting in an incomplete valence. Claims are unduly speculative where they define only a portion of a substituted 1,2,3-triazole of the Formula (1). Consequently, since incomplete valences are not permitted in the structure of the substituted 1,2,3-triazoles of the Formula (1), an essential portion of the substituted 1,2,3-triazoles of the Formula (1) is indefinite and one of ordinary skill in the art would not be reasonably apprised of the metes and bounds of the substituted 1,2,3-triazoles of the Formula (1). {See Ex parte Pedlow and Miner, 90 USPQ 395 (Bd. Pat. App. & Int. 1951)}.
The examiner suggests amending the claim, particularly as stated in the section above entitled Claim Objections, to overcome this rejection.
Claim 8 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 8 recites the limitations, sulfino and phosphono, respectively, with regard to R1, where the limitations are implausible, resulting in an incomplete valence. Claims are unduly speculative where they define only a portion of a substituted 1,2,3-triazole of the Formula (1). Consequently, since incomplete valences are not permitted in the structure of the substituted 1,2,3-triazoles of the Formula (1), an essential portion of the substituted 1,2,3-triazoles of the Formula (1) is indefinite and one of ordinary skill in the art would not be reasonably apprised of the metes and bounds of the substituted 1,2,3-triazoles of the Formula (1). {See Ex parte Pedlow and Miner, 90 USPQ 395 (Bd. Pat. App. & Int. 1951)}.
The examiner suggests amending the claim, particularly as stated in the section above entitled Claim Objections, to overcome this rejection.
Claim 10 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 the phrase, or derivatives thereof, with respect to R1, is a relative phrase which renders the claim indefinite. The phrase, or derivatives thereof, 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 fails to adequately define the phrase, or derivatives thereof. Similarly, the meaning of a phrase cannot depend on the unrestrained, subjective opinion of the inventor or joint inventor practicing the invention. Likewise, neither the specification, nor the claim, explicitly limits the invention to any specifically disclosed or recited embodiments. Consequently, the substituted 1,2,3-triazoles of the Formula (1) have been rendered indefinite by the use of the phrase, or derivatives thereof, with respect to R1. {See Datamize LLC v. Plumtree Software, Inc., 417 F.3d 1342, 1347-48, 75 USPQ2d 1801, 1807 (Fed. Cir. 2005); and MPEP § 2173.05(b)}.
The examiner suggests amending the claim, particularly as stated in the section above entitled Claim Objections, to overcome this section of the rejection.
Next, the inventor or joint inventor should further 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).
Then, the inventor or joint inventor should further note that claim 10 recites the broad limitation, oxadiazole, with respect to R1, and the claim also recites furazan, with respect to R1, which is the narrower statement of the limitation.
Moreover, 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.
Furthermore, the inventor or joint inventor should also 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 section of the rejection.
Claims 13 and 14 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 13 recites the limitation, A pharma-ceutical composition comprising a compound according to claim 1, or a pharmaceutically acceptable salt thereof, in lines 1-2 of the claim. There is insufficient antecedent basis, in claim 1, for this limitation, with respect to the substituted 1,2,3-triazoles of the Formula (1). According to claim 1, or a pharmaceutically acceptable salt thereof is not recited, with respect to the substituted 1,2,3-triazoles of the Formula (1).
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 17 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 17 recites the broad limitations, (1) streptococcus aureus; (2) enterococcus; (3) enterobacteriacae; and (4) alpha-hemolytic streptococcus and beta-hemolytic streptococcus, respectively, and the claim also recites (1) methicillin-resistant staphylococcus aureus (MRSA); (2) enterococcus faecalis and vancomycin-resistant enterococci (VRE); (3) escherichia coli; and (4) streptococcus aureus and streptococcus pneumoniae, respectively, which are the narrower statements of the limitations.
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 18 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 18 recites the broad limitations, methicillin-resistant staphylococcus aureus (MRSA), streptococcus pneumoniae, enterococcus faecalis, and vancomycin-resistant enterococci (VRE), respectively, and the claim also recites vancomycin-resistant enterococci (VRE), which is the narrower statement of the limitations.
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.
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