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 1-30 are pending in the instant invention. According to the In The Claims, filed August 26, 2026, claim 1 was amended.
Status of Priority
This invention is a Divisional (DIV) of US Application No. 18/488,924, filed October 17, 2023 and now US 12,054,475, which is a Continuation (CON) of International Application No. PCT/US2022/026059, filed April 22, 2022, which claims priority under 35 U.S.C. § 119(e) to US Provisional Application No. 63/178,309, filed April 22, 2021.
Restrictions / Election of Species
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The inventor’s or joint inventor’s provisional election of the following, without traverse, in the reply filed on August 26, 2026, is acknowledged: a) Group I - claims 1-30; and b) substituted heterocycle of Formula (IV) - p. 124, Example 6, compound 140, shown to the right below, and hereafter referred to as 3-ethyl-N-(8-methyl-2-oxo-1,2,3,4-tetrahydroquinolin-6-yl)isonicotinamide, where p = 1; at C-3, R100 = -CH2CH3; ring A = -pyridin-4-yl; L = -C(O)NH-; R22’ = -H; R22 = -CH3; and R32 and R33, taken together with the carbon atoms to which they are attached, form a 2-oxo-5,6-piperidinylene. Claims 1-14, 17-27 and 30 read on the elected species. Affirmation of this election must be made by the inventor or joint inventor in replying to this Office action.
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Similarly, 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 the elected species, shown to the right above, was found to be free of the prior art. Thus, the examiner has expanded the forthcoming prosecution to include all claims relevant to the genus of Group I, for a first Office action and prosecution on the merits.
Thus, a first Office action and prosecution on the merits of claims 1-30 is contained within.
Specification Objection - Disclosure
The inventor or joint inventor is advised to format the specification according to 37 CFR 1.77(c). Revisions should particularly address bold-type, underline, and/or upper case formatting. Appropriate correction may be required.
Specification Objection - 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 (IV) into the abstract, to overcome this objection.
Claim Objections
Claim 1 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(a), the existing recitation should be replaced with the following recitation:
A method for inducing male contraception in a subject in need thereof, wherein the method comprises administering to the subject a therapeutically effective amount of a compound of Formula (IV):
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(IV)
or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof,
wherein:
ring A is a heterocyclyl or heteroaryl;
each R100 is independently halo, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkylene-carbocyclyl, or C1-6 alkylene-heterocyclyl;
p is 0, 1, or 2;
L is -C(O)NH-, -NH-, -S(O)-, -S(O)NH-, -S(O)2-, or -S(O)2NH-;
R22’ is H, halo, C1-6 alkyl, or C1-6 haloalkyl;
R22 is halo, CN, C1-6 alkyl, C1-6 haloalkyl, C1-6 cyanoalkyl, or carbocyclyl; or
R22’ and R22, taken together with the carbon atoms to which they are attached, form a carbocyclyl, heterocyclyl, or heteroaryl, wherein the carbocyclyl, heterocyclyl, or heteroaryl is optionally substituted with one or more independently selected halo substituents;
R32 and R33, taken together with the carbon atoms to which they are attached, form a heterocyclyl of the following structure:
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;
wherein the heterocyclyl is optionally substituted on any available carbon atom other than the carbon atom in the phenyl ring with one or more independently selected R101 substituents; and
each R101 is independently halo or C1-6 alkyl.
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:
A method for providing male contraception in a subject in need thereof, wherein the method comprises administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of Formula (IV):
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(IV)
or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof,
wherein:
ring A is a heterocyclyl or heteroaryl;
each R100 is independently halo, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkylene-carbocyclyl, or C1-6 alkylene-heterocyclyl;
p is 0, 1, or 2;
L is -C(O)NH-, -NH-, -S(O)-, -S(O)NH-, -S(O)2-, or -S(O)2NH-;
R22’ is H, halo, C1-6 alkyl, or C1-6 haloalkyl;
R22 is halo, CN, C1-6 alkyl, C1-6 haloalkyl, C1-6 cyanoalkyl, or carbocyclyl; or
R22’ and R22, taken together with the carbon atoms to which they are attached, form a carbocyclyl, heterocyclyl, or heteroaryl, wherein the carbocyclyl, heterocyclyl, or heteroaryl is optionally substituted with one or more independently selected halo substituents;
R32 and R33, taken together with the carbon atoms to which they are attached, form a heterocyclyl of the following structure:
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, or
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;
wherein the heterocyclyl is optionally substituted on any available carbon atom other than the carbon atom in the phenyl ring with one or more independently selected R101 substituents; and
each R101 is independently halo or C1-6 alkyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 3 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 1, wherein the compound is of Formula (IV-A):
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(IV-A)
or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof,
wherein:
L1 is absent, -C(O)-, -S(O)-, or -S(O)2-.
Appropriate correction is required. See MPEP § 2173.02.
Claim 4 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 1, wherein ring A is a 3- to 8-membered heterocyclyl, fused 5,6-bicyclic heterocyclyl, fused 6,6-bicyclic heterocyclyl, 5- or 6-membered heteroaryl, a fused 5,6-bicyclic heteroaryl, or fused 6,6-bicyclic heteroaryl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 5 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 1, wherein ring A is morpholinyl, pyridinyl, pyridazinyl, pyrimidinyl, quinazolinyl, or quinoxalinyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 6 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 1, wherein ring A-(R100)p is:
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, or
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.
The inventor or joint inventor should note that one occurrence of pyridazin-4-yl-(R100)p is omitted. If the inventor’s or joint inventor’s intent was to recite pyridazin-3-yl-(R100)p, please amend the specification and insert pyridazin-3-yl-(R100)p into the claim in response to this Office action. Appropriate correction is required. See MPEP § 2173.02.
Claim 7 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 6, wherein ring A-(R100)p is:
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, or
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.
Appropriate correction is required. See MPEP § 2173.02.
Claim 8 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 7, wherein ring A-(R100)p is:
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.
Appropriate correction is required. See MPEP § 2173.02.
Claim 9 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 3, wherein L1 is -C(O)-.
Appropriate correction is required. See MPEP § 2173.02.
Claim 10 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 1, wherein the compound is of Formula (IV-B):
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(IV-B)
or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof,
wherein:
Z1 is CH or N;
Z2 is CH or N;
Z3 is CH or N; and
Z4 is CH or N;
with the proviso that at least one of Z1, Z2, Z3, and Z4 is N.
Appropriate correction is required. See MPEP § 2173.02.
Claim 11 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 10, wherein one or two of Z1, Z2, Z3, and Z4 are N and the rest of Z1, Z2, Z3, and Z4 are CH.
Appropriate correction is required. See MPEP § 2173.02.
Claim 12 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 11, wherein
(i) Z1 is CH;
Z2 is N;
Z3 is CH; and
Z4 is CH; or
(ii) Z1 is CH;
Z2 is N;
Z3 is CH; and
Z4 is N; or
(iii) Z1 is CH;
Z2 is N;
Z3 is N; and
Z4 is CH; or
(iv) Z1 is N;
Z2 is CH;
Z3 is N; and
Z4 is CH; or
(v) Z1 is N;
Z2 is N;
Z3 is CH; and
Z4 is CH.
Appropriate correction is required. See MPEP § 2173.02.
Claim 13 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 12, wherein
(i) Z1 is CH;
Z2 is N;
Z3 is CH; and
Z4 is CH; or
(v) Z1 is N;
Z2 is N;
Z3 is CH; and
Z4 is CH.
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(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 method of claim 1, wherein R32 and R33, taken together with the carbon atoms to which they are attached, form a heterocyclyl of the following structure:
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.
Appropriate correction is required. See MPEP § 2173.02.
Claim 15 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 1, wherein:
(i) R22’ and R22, taken together with the carbon atoms to which they are attached, form a 5-membered carbocyclyl, wherein the 5-membered carbocyclyl is optionally substituted with one or more fluoro substituents; or
(ii) R22’ and R22, taken together with the carbon atoms to which they are attached, form a 6-membered heterocyclyl;
wherein the 6-membered heterocyclyl contains one or two ring heteroatoms independently selected from the group consisting of nitrogen and oxygen; and
wherein the 6-membered heterocyclyl is optionally substituted with one or more fluoro substituents; or
(iii) R22’ and R22, taken together with the carbon atoms to which they are attached, form a 5- or 6-membered heteroaryl, wherein the 5- or 6-membered heteroaryl contains one or two ring heteroatoms independently selected from the group consisting of nitrogen, oxygen, and sulfur.
Appropriate correction is required. See MPEP § 2173.02.
Claim 16 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 15, wherein R22’ and R22, taken together with the carbon atoms to which they are attached, form a 6-membered heteroaryl, wherein the 6-membered heteroaryl contains one nitrogen ring heteroatom.
Appropriate correction is required. See MPEP § 2173.02.
Claim 17 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 1, wherein R22’ is H, F, CH3, or CF3.
Appropriate correction is required. See MPEP § 2173.02.
Claim 18 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 1, wherein R22’ is H, halo, or C1-6 alkyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 19 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 18, wherein R22’ is H, F, or CH3.
Appropriate correction is required. See MPEP § 2173.02.
Claim 20 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 1, wherein R22’ is H or halo.
Appropriate correction is required. See MPEP § 2173.02.
Claim 21 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 20, wherein R22’ is H or F.
Appropriate correction is required. See MPEP § 2173.02.
Claim 22 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 21, wherein R22’ is H.
Appropriate correction is required. See MPEP § 2173.02.
Claim 23 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 1, wherein each R100 is independently halo, C1-6 alkyl, C1-6 haloalkyl, or C1-6 alkylene-carbocyclyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 24 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation:
The method of claim 1, wherein each R100 is independently Cl, CH3, CH2CH3, CF2CH3, CH2CF3, CH2-cyclopropyl, CH2-cyclobutyl, or CH2-oxetanyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 25 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 24, wherein each R100 is independently Cl, CH3, CH2CH3, CH2CF3, CH2-cyclopropyl, CH2-cyclobutyl, or CH2-oxetanyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 26 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 24, wherein each R100 is independently Cl, CH3, CH2CH3, CH2CF3, or CH2-cyclopropyl.
Appropriate correction is required. See MPEP § 2173.02.
Claim 27 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 1, wherein the compound, or stereoisomer thereof, is selected from the group consisting of:
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or a pharmaceutically acceptable salt or tautomer thereof.
Appropriate correction is required. See MPEP § 2173.02.
Claim 28 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 1, wherein the compound is:
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or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof.
Appropriate correction is required. See MPEP § 2173.02.
Claim 29 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 1, wherein the compound is:
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or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof.
Appropriate correction is required. See MPEP § 2173.02.
Claim 30 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 1, wherein the compound is:
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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.
Written Description - Substituted heterocycles of the Formula (IV)
Claims 1-6 and 9-22 are rejected under 35 U.S.C. § 112(a) as failing to comply with the written description requirement. The claims contain subject matter which was not described in the specification in such a way as to reasonably convey to one skilled in the relevant art that the inventor or joint inventor, at the time the invention was filed, had possession of the claimed invention. Specifically, the substituted heterocycles of the Formula (IV), wherein… R100 is CN, lack adequate support within the original specification, as filed. The specification, on page 62, discloses generic substituted heterocycles of the Formula (IV), which fail to expressly include substituted heterocycles of the Formula (IV), wherein… R100 is CN. Consequently, one of ordinary skill in the art, at the time this invention was filed, may neither be reasonably apprised of the scope of the instantly recited substituted heterocycles of the Formula (IV), nor recognize that the inventor or joint inventor was in possession of the instantly recited substituted heterocycles of the Formula (IV), in view of the original specification of the invention.
The inventor or joint inventor should note that under 35 U.S.C. § 132 and 35 U.S.C. § 251, the proscription against the introduction of new matter in a patent invention serves to prevent an inventor or joint inventor from adding information that goes beyond the subject matter originally filed. {See In re Rasmussen, 650 F.2d 1212, 1214, 211 USPQ 323, 326 (CCPA 1981); and MPEP § 2163.06-2183.07}.
Similarly, the inventor or joint inventor should further note that in order to comply with the written description requirement of 35 U.S.C. § 112(a), each claim limitation must be expressly, implicitly, or inherently supported in the originally filed specification. [W]hen an explicit limitation in a claim is not present in the written description whose benefit is sought, it must be shown that a person of ordinary skill would have understood, at the time the patent application was filed, that the description requires that limitation. {See Hyatt v. Boone, 146 F.3d 1348, 1353, 47 USPQ2d 1128, 1131 (Fed. Cir. 1998); and In re Wright, 866 F.2d 422, 425, 9 USPQ2d 1649, 1651 (Fed. Cir. 1989)}.
Likewise, the inventor or joint inventor should further note that [N]ew or amended claims, which introduce elements or limitations which are not supported by the as-filed disclosure, violate the written description requirement. {See In re Lukach, 442 F.2d 967, 169 USPQ 795 (CCPA 1971); and In re Smith, 458 F.2d 1389, 1395, 173 USPQ 679, 683 (CCPA 1972)}.
Moreover, the inventor or joint inventor should further note that when filing an amendment, support should be shown in the original specification for new or amended claims. See MPEP § 714.02 and § 2163.06.
The examiner suggests amending the claims, particularly as stated in the section above entitled Claim Objections, to overcome this section of the rejection.
Scope of Enablement - Method of male contraception in a subject in need thereof, the method comprising administering… a substituted heterocycle of the Formula (IV)
Claims 1-26 are rejected under 35 U.S.C. § 112(a) because the specification, while being enabling for performing a method of male contraception in a subject in need thereof, the method comprising administering… a substituted heterocycle of the Formula (IV), wherein the substituted heterocycle of the Formula (IV) is as presented herein in the section above entitled Claim Objections, does not reasonably provide enablement for performing a method of male contraception in a subject in need thereof, the method comprising administering… a substituted heterocycle of the Formula (IV), wherein the substituted heterocycle of the Formula (IV) is not as presented herein in the section above entitled Claim Objections. The specification does not enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and/or use (perform) the invention commensurate in scope with these claims. A method of male contraception in a subject in need thereof, the method comprising administering… a substituted heterocycle of the Formula (IV), wherein the substituted heterocycle of the Formula (IV) is not as presented herein in the section above entitled Claim Objections, as recited in claim 1, has 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 (perform) a method of male contraception in a subject in need thereof, the method comprising administering… a substituted heterocycle of the Formula (IV), wherein the substituted heterocycle of the Formula (IV) is not as presented herein in the section above entitled Claim Objections.
There are many factors to be considered when determining whether there is sufficient evidence to support a determination that a disclosure does not satisfy the enablement requirement and whether any necessary experimentation is undue. These factors include, but are not limited to: (a) breadth of the claims; (b) nature of the invention; (c) state of the prior art; (d) level of one of ordinary skill in the art; (e) level of predictability in the art; (f) amount of direction provided by the inventor or joint inventor; (g) existence of working examples; and (h) quantity of experimentation needed to make or use the invention based on the content of the disclosure. {See Ex parte Forman 230 USPQ 546 (Bd. Pat. App. & Inter. 1986); and In re Wands, 8 USPQ2d 1400 (Fed. Cir. 1988)}.
The above factors, regarding the instant invention, are summarized as follows:
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(a) Breadth of the claims - the breadth of the claims includes a method of male contraception in a subject in need thereof, the method comprising administering… a substituted heterocycle of the Formula (IV), shown to the right;
(b) Nature of the invention - the nature of the invention is performance of a method of male contraception in a subject in need thereof, the method comprising administering… a substituted heterocycle of the Formula (IV), shown to the right above;
(c) State of the prior art - Nature Reviews: Drug Discovery, as provided in the file and cited on the IDS, offers a snapshot of the state of the drug development art. Herein, drug development is stated to follow the widely accepted Ehrlich model which includes: (1) development of a broad synthetic organic chemistry program; (2) subsequent testing of compounds in an appropriate laboratory model for the disease to be treated; and (3) screening of compounds with low toxicity in prospective clinical trials (Jordan, V. C. Nature Reviews: Drug Discovery, 2, 2003, 205). Moreover, WO 22/226383 illustrates the synthesis of substituted heterocycles of the Formula (IV), and/or methods of use thereof {Esposito, et al. WO 22/226383, 2022};
(d) Level of one of ordinary skill in the art - the artisans performing the inventor’s or joint inventor’s method of male contraception in a subject in need thereof, the method comprising administering… a substituted heterocycle of the Formula (IV), wherein the substituted heterocycle of the Formula (IV) is not as presented herein in the section above entitled Claim Objections, would be a collaborative team of synthetic chemists and/or health practitioners, possessing commensurate degree level and/or skill in the art, as well as several years of professional experience;
(e) Level of predictability in the art - Synthetic organic chemistry is quite unpredictable (See In re Marzocchi and Horton 169 USPQ at 367 ¶3). Similarly, it is unclear based on the combination of the instant specification, and Esposito, et al. in WO 22/226383, whether performing the instantly recited method of male contraception in a subject in need thereof, the method comprising administering… a substituted heterocycle of the Formula (IV), wherein the substituted heterocycle of the Formula (IV) is not as presented herein in the section above entitled Claim Objections, is enabled. Moreover, the following excerpt is taken from Dörwald, as provided in the file and cited on the IDS, which has relevance to the synthesis of substituted heterocycles of the Formula (IV), wherein the substituted heterocycles of the Formula (IV) are not as presented herein in the section above entitled Claim Objections (Dörwald, F. Zaragoza. Side Reactions in Organic Synthesis: A Guide to Successful Synthesis Design, Weinheim: WILEY-VCH Verlag GmbH & Co. KGaA, 2005, Preface):
Most non-chemists would probably be horrified if they were to learn how many attempted syntheses fail, and how inefficient research chemists are. The ratio of successful to unsuccessful chemical experiments in a normal research laboratory is far below unity, and synthetic research chemists, in the same way as most scientists, spend most of their time working out what went wrong, and why.
Despite the many pitfalls lurking in organic synthesis, most organic chemistry textbooks and research articles do give the impression that organic reactions just proceed smoothly and that the total synthesis of complex natural products, for instance, is maybe a labor-intensive but otherwise undemanding task. In fact, most syntheses of structurally complex natural products are the result of several years of hard work by a team of chemists, with almost every step requiring careful optimization. The final synthesis usually looks quite different from that originally planned, because of unexpected difficulties encountered in the initially chosen synthetic sequence. Only the seasoned practitioner who has experienced for himself the many failures and frustrations which the development (sometimes even the repetition) of a synthesis usually implies will be able to appraise such work.
Chemists tend not to publish negative results, because these are, as opposed to positive results, never definite (and far too copious).
(f) Amount of direction provided by the inventor - the invention lacks direction with respect to making and/or using (performing) a method of male contraception in a subject in need thereof, the method comprising administering… a substituted heterocycle of the Formula (IV), wherein the substituted heterocycle of the Formula (IV) is not as presented herein in the section above entitled Claim Objections;
(g) Existence of working examples - the inventor or joint inventor has provided sufficient guidance to make and/or use (perform) a method of male contraception in a subject in need thereof, the method comprising administering… a substituted heterocycle of the Formula (IV), wherein the substituted heterocycle of the Formula (IV) is as presented herein in the section above entitled Claim Objections; however, the disclosure is insufficient to allow extrapolation of the limited examples to enable performing the instantly recited method of male contraception in a subject in need thereof, the method comprising administering… a substituted heterocycle of the Formula (IV), wherein the substituted heterocycle of the Formula (IV) is not as presented herein in the section above entitled Claim Objections. The specification lacks working examples of performing a method of male contraception in a subject in need thereof, the method comprising administering… a substituted heterocycle of the Formula (IV), wherein the substituted heterocycle of the Formula (IV) is not as presented herein in the section above entitled Claim Objections.
Within the specification, [A]t least one specific operative embodiment or example of the invention must be set forth. The example(s) and description should be of sufficient scope as to justify the scope of the claims. Markush claims must be provided with support in the disclosure for each member of the Markush group. Where the constitution and formula of a chemical compound is stated only as a probability or speculation, the disclosure is not sufficient to support claims identifying the compound by such composition or formula. See MPEP § 608.01(p) and MPEP § 2173.05.
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(h) Quantity of experimentation needed to make or use the invention based on the content of the disclosure - predicting whether a recited compound is in fact one that produces a desired physiological effect at a therapeutic concentration and with useful kinetics, is filled with experimental uncertainty, and without proper guidance, would involve a substantial amount of experimentation (Jordan, V. C. Nature Reviews: Drug Discovery, 2, 2003, 205-213). Furthermore, it is unclear, based on the guidance provided by the specification, whether a substituted heterocycle of the Formula (IV), such as 6-[(3-ethylpyridin-4-yl)sulfonyl]-8-methyl-2,3-dihydro-1,4-benzoxathiin-2-one, shown to the left above, possesses utility as a therapeutic agent, useful in a method of male contraception in a subject in need thereof, the method comprising administering… a substituted heterocycle of the Formula (IV).
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 (performing) a method of male contraception in a subject in need thereof, the method comprising administering… a substituted heterocycle of the Formula (IV), wherein the substituted heterocycle of the Formula (IV) is not as presented herein in the section above entitled Claim Objections, is clearly justified.
The examiner suggests amending the claims, particularly as stated in the section above entitled Claim Objections, to overcome this section of the 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.
Claim 24 is 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 24 recites the limitation, The method of claim 1, wherein… two adjacent R100 may be joined to form a C5-6 carbocyclyl or a 5-membered heterocyclyl containing a N or O heteroatom;…, in lines 1-4 of the claim. There is insufficient antecedent basis, in claim 1, for this limitation, with respect to the substituted heterocycles of the Formula (IV) administered within the method of male contraception in a subject in need thereof. According to claim 1, two adjacent R100 are not recited as joining to form a C5-6 carbocyclyl or a 5-membered heterocyclyl containing a N or O heteroatom, with respect to the substituted heterocycles of the Formula (IV) administered within the method of male contraception in a subject in need thereof.
The examiner suggests amending the claim, particularly as stated in the section above entitled Claim Objections, to overcome this rejection.
Claim 27 is 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 24 recites the limitation, The method of claim 1, wherein the compound is:… (shown centered below);…, in line 1 of the claim:
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Moreover, the inventor or joint inventor should further note that there is insufficient antecedent basis, in claim 1, for this limitation, with respect to the substituted heterocycles, shown centered above, and administered within the method of male contraception in a subject in need thereof. According to claim 1, the substituted heterocycles, shown centered above, and administered within the method of male contraception in a subject in need thereof, are not recited as substituted heterocycles of the Formula (IV) administered within the method of male contraception in a subject in need thereof, particularly with regard to the phenyl ring bearing R22 and/or R22’, respectively.
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. § 112(d)
The following is a quotation of the fourth paragraph of 35 U.S.C. § 112:
(d) REFERENCE IN DEPENDENT FORMS. Subject to subsection (e), a claim in dependent form shall contain a reference to a claim previously set forth and then specify a further limitation of the subject matter claimed. A claim in dependent form shall be construed to incorporate by reference all the limitations of the claim to which it refers.
Claim 2 is rejected under 35 U.S.C. § 112(d) as being of improper dependent form for failing to further limit the subject matter of the claim upon which it depends, or for failing to include all the limitations of the claim upon which it depends.
The inventor or joint inventor should note that claim 2 is rejected under 35 U.S.C. § 112(d) because the recitation of an additional method performed on a subject administered thereto in a method from which the claim depends, must result in a patentably distinct methodical step in the recited method, in order to be further limiting. In the instant dependent claim, the method of male contraception in a subject in need thereof, the method comprising administering to the subject… a substituted heterocycle of the Formula (IV), as recited in claim 1, further comprises the step of administering to the subject… a pharmaceutical composition comprising… a pharmaceutically acceptable excipient… and a substituted heterocycle of the Formula (IV). Consequently, since the additional method performed on the subject administered thereto in the method of male contraception in a subject in need thereof, the method comprising administering to the subject… a substituted heterocycle of the Formula (IV), as recited in claim 1, whereby the method further comprises the step of administering to the subject… a pharmaceutical composition comprising… a pharmaceutically acceptable excipient… and a substituted heterocycle of the Formula (IV), (1) fails to result in a further patentably distinct methodical step in the method of male contraception in a subject in need thereof, the method comprising administering to the subject… a substituted heterocycle of the Formula (IV), as recited in claim 1, and/or (2) fails to include all the limitations of the method of male contraception in a subject in need thereof, the method comprising administering to the subject… a substituted heterocycle of the Formula (IV), as recited in claim 1, it is not given patentable weight and thus, renders the instant dependent claim improperly dependent under 35 U.S.C. § 112(d). {See MPEP § 2111.02; and 37 CFR 1.75(c)}.
Similarly, the inventor or joint inventor should further note that the U.S. Court of Appeals for the Federal Circuit indicated that although the requirements of 35 U.S.C. § 112(d) are related to matters of form, non-compliance with 35 U.S.C. § 112(d) renders the claim unpatentable just as non-compliance with other subsections of 35 U.S.C. § 112 would. {See Pfizer, Inc. v. Ranbaxy Labs., Ltd., 457 F.3d 1284, 1291-92 (Fed. Cir. 2006)}.
Moreover, the inventor or joint inventor should further note that if a dependent claim does not comply with the requirements of 35 U.S.C. § 112(d) the dependent claim should be rejected under 35 U.S.C. § 112(d) as unpatentable rather than objecting to the claim. {See also MPEP § 608.01(n), Section III, Infringement Test for dependent claims}.
The examiner suggests the inventor or joint inventor (1) cancel the dependent claim, (2) amend the dependent claim to place the dependent claim in proper dependent form, (3) rewrite the dependent claim in independent form, particularly as stated in the section above entitled Claim Objections, or (4) present a sufficient showing that the dependent claim complies with the statutory requirements, to overcome this rejection.
Claim Rejections - Obviousness-type Double Patenting
The nonstatutory double patenting rejection is based on a judicially created doctrine grounded in public policy (a policy reflected in the statute), so as to prevent the unjustified or improper timewise extension of the right to exclude granted by a patent and to prevent possible harassment by multiple assignees. A nonstatutory obviousness-type double patenting rejection is appropriate where the conflicting claims are not identical, but at least one examined invention claim is not patentably distinct from the reference claims because the examined invention claim is either anticipated by, or would have been obvious over, the reference claims. {See In re Berg, 140 F.3d 1428, 46 USPQ2d 1226 (Fed. Cir. 1998); In re Goodman, 11 F.3d 1046, 29 USPQ2d 2010 (Fed. Cir. 1993); In re Longi, 759 F.2d 887, 225 USPQ 645 (Fed. Cir. 1985); In re Van Ornum, 686 F.2d 937, 214 USPQ 761 (CCPA 1982); In re Vogel, 422 F.2d 438, 164 USPQ 619 (CCPA 1970); and In re Thorington, 418 F.2d 528, 163 USPQ 644 (CCPA 1969)}.
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Consequently, claims 1-30 are rejected on the ground of nonstatutory obviousness-type double patenting as being unpatentable over claims 1-30 of US Patent No. 12,054,475. Although the conflicting claims are not identical, they are not patentably distinct from each other because claim 1 in US 12,054,475 recites substituted heterocycles of the Formula (IV-C), shown to the left, where p = 1; R100 = -C1-6 alkyl; R22’ = -H; R22 = -C1-6 alkyl; R20’ = -H; R21’ = -H; R20 = -H; and R21 = -H, respectively, which are administered within the instantly recited method of male contraception in a subject in need thereof, the method comprising administering to the subject… a substituted heterocycle of the Formula (IV), shown to the right, where p = 1; R100 = -C1-6 alkyl; ring A = -heteroaryl; L = -C(O)NH-; R22’ = -H; R22 = -C1-6 alkyl; and R32 and R33, taken together with the carbon atoms to which they are attached, form a heterocyclyl substituted with =O, respectively.
The inventor or joint inventor should note that [T]he discovery of a previously unappreciated property of a prior art compound, or of a scientific explanation for the prior art’s functioning, does not render the old compound patentably new to the discoverer. {See Atlas Powder Co. v. Ireco Inc., 190 F.3d 1342, 1347, 51 USPQ2d 1943, 1947 (Fed. Cir. 1999)}.
Similarly, the inventor or joint inventor should further note that [T]he claiming of a new use, new function or unknown property which is inherently present in the prior art does not necessarily make the claim patentable. {See In re Best, 562 F.2d 1252, 1254, 195 USPQ 430, 433 (CCPA 1977); and In re Crish, 393 F.3d 1253, 1258, 73 USPQ2d 1364, 1368 (Fed. Cir. 2004)}.
Likewise, the inventor or joint inventor should note that [W]hen the claim recites using an old compound and the use is directed to a result or property of that compound, then the claim is anticipated. {See In re May, 574 F.2d 1082, 1090, 197 USPQ 601, 607 (CCPA 1978); and In re Tomlinson, 363 F.2d 928, 150 USPQ 623 (CCPA 1966)}.
Next, the inventor or joint inventor should further note that [P]roducts of identical chemical composition may not have mutually exclusive properties. A chemical composition and its properties are inseparable. Therefore, if the prior art teaches the identical chemical structure, the properties the inventor or joint inventor discloses and/or claims are necessarily present. {See In re Spada, 911 F.2d 705, 709, 15 USPQ2d 1655, 1658 (Fed. Cir. 1990)}.
Then, the inventor or joint inventor should further note that [A] claim to a method of using a composition is not patentably distinct from an earlier claim to the identical composition in a patent disclosing the identical use. {See Sun Pharmaceuticals Industries Ltd. v. Eli Lilly and Co., 611 F.3d 1381, 95 USPQ2d 1797 (Fed. Cir. 2010); Pfizer, Inc. v. Teva Pharmaceuticals USA, Inc., 518 F.3d 1353, 1363, 86 USPQ2d 1001 (Fed. Cir. 2008); and Geneva
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Pharmaceuticals, Inc. v. GlaxoSmithKline PLC,
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349 F.3d 1373, 68 USPQ2d 1865, (Fed. Cir. 2003)}.
Moreover, the inventor or joint inventor should further note that [I]t is obvious to add a carrier or solvent to an unpatentable compound. {See Ex parte Douros and Vanderweff, 163 USPQ 667, (BPAI 1968)}.
Now, the inventor or joint inventor should further note that a timely filed terminal disclaimer in compliance with 37 CFR 1.321(c) or 37 CFR 1.321(d) may be used to overcome an actual or provisional rejection based on a nonstatutory double patenting ground, provided the conflicting invention or patent either is shown to be commonly owned with this invention, or claims an invention made as a result of activities undertaken within the scope of a joint research agreement.
Furthermore, the inventor or joint inventor should also note that the USPTO internet Web site contains terminal disclaimer forms which may be used, and the inventor or joint inventor is encouraged to visit http://www.uspto.gov/forms/, where (i) the filing date of the invention will determine what form should be used, and (ii) a web-based eTerminal Disclaimer may be filled out completely online using web-screens, respectively.
Also, the inventor or joint inventor should further note that an eTerminal Disclaimer that meets all requirements is auto-processed and approved immediately upon submission.
Finally, for more information about eTerminal Disclaimers, the inventor or joint inventor should refer to http://www.uspto.gov/patents/process/file/efs/guidance/eTD-info-I.jsp.
Allowable Subject Matter
No claims are allowed.
Conclusion
Any inquiry concerning this communication or earlier communications from the examiner should be directed to DOUGLAS M. WILLIS, whose telephone number is 571-270-5757. The examiner may normally be reached on Monday thru Thursday from 8:00-6:00 EST. The examiner is also available on alternate Fridays.
If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Mr. Jeffrey Murray, may be reached on 571-272-9023. The fax phone number for the organization where this invention or proceeding is assigned is 571-273-8300.
Information regarding the status of an invention may be obtained from Patent Center. For more information about Patent Center, see https://www.uspto.gov/patents/apply/patent-center. Should you have questions on access to Patent Center, contact the Patent Electronic Business Center (PEBC) at 866-217-9197 (toll-free) or ebc@uspto.gov.
/DOUGLAS M WILLIS/
Primary Examiner, Art Unit 1624
Prosecution Insights