DETAILED ACTION
Notice of Pre-AIA or AIA Status
The present application, filed on or after March 16, 2013, is being examined under the first inventor to file provisions of the AIA .
Election/Restrictions
Applicant's election with traverse of Group I, claims 1-20 and 22 (drawn to a compound of formula I), and species election of the compound
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in the reply filed on April 8, 2026 is acknowledged. The traversal is on the ground(s) that the single general inventive concept shared by the presently claimed compounds is the common core of an aminoquinazoline group substituted by at least two substituents, which is a substantial structural feature that is essential to the activity of the LRRK2 inhibitor compounds. Applicant submits that the compounds’ shared structural feature is essential to the utility of treating Parkinsons disease. Applicant argues that a search of the prior art would result in a search for the invention when examining claims directed to LRRK2 inhibitors and no serious burden for examination is present.
This is not found persuasive because the substantial structural feature identified by Applicant, i.e., an aminoquinazoline group substituted by at least two substituents, is not a special technical feature as it does not make a contribution over the prior art in view of Lyssikatos et al., U.S. 20120322785 A1 (cited on Applicant’s IDS of May 2, 2024). In particular, Lyssikatos et al. disclose a compound comprising an aminoquinazoline group substituted by at least two substituents:
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(see Table 1 at page 47).
The requirement is still deemed proper and is therefore made FINAL.
Therefore Group II, claims 21 and 23-24 (drawn to methods of use), are withdrawn from further consideration pursuant to 37 CFR 1.142(b), as being drawn to a nonelected invention, there being no allowable generic or linking claim.
Information Disclosure Statement
The information disclosure statements (IDS) submitted on May 2, 2026, September 18, 2025, and September 19, 2025, are in compliance with the provisions of 37 CFR 1.97. Accordingly, the information disclosure statements have been considered by the examiner, please refer to the signed copies of Applicant’s PTO-1449 forms, attached herewith.
Claim Rejections - 35 USC § 112
6. The following is a quotation of the first paragraph of 35 U.S.C. 112(a):
(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.
The following is a quotation of the first paragraph of pre-AIA 35 U.S.C. 112:
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 of carrying out his invention.
7. Claims 1-20 and 22 are rejected under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, as failing to comply with the written description requirement. The claims contains 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 a joint inventor, or for applications subject to pre-AIA 35 U.S.C. 112, the inventors, at the time the application was filed, had possession of the claimed invention.
8. In particular, support cannot be found for the full scope of compounds of Formula (I), as instantly claimed.
9. The MPEP §2163 states that the purpose of the written description requirement is to ensure that the inventor had possession, as of the filing date of the application, of the specific subject matter later claimed by him. In the case of chemical entities, Applicant's attention is further directed to Regents of the University of California v. Eli Lilly & Co., 119 F.3d 1559 (Fed. Cir. 1997), cert. denied, 523 U.S. 1089, 118 S. Ct. 1548 (1998), which notes that an adequate written description requires a precise definition, such as by structure, formula, chemical name, or physical properties, “not a mere wish or plan for obtaining the claimed chemical invention.” While the court recognizes that, “[i]n claims involving chemical materials, generic formulae usually indicate with specificity what the generic claims encompass” (Id.), it is also recognized that for a broad generic claim, the specification must provide adequate written description to identify the genus of the claim and/or the genus must be sufficiently detailed to show that applicant was in possession of the claimed invention as a whole (see Vas-Cath, Inc. v. Mahurkar, 935 F.2d 1555 (Fed. Cir. 1991)). If a genus has substantial variance, the disclosure must present a sufficient number of representative species that encompass the genus in order to adequately describe the genus (i.e., the disclosure must describe a sufficient variety of species to reflect the variation within that genus). See MPEP § 2163. Otherwise, as stated by the court in Ariad Pharmaceuticals, Inc., v. Eli Lilly and Company (Fed. Cir. 2010), “a generic claim may define the boundaries of a vast genus of chemical compounds, and yet the question may still remain whether the specification, including original claim language, demonstrates that the applicant has invented species sufficient to support a claim to a genus.
10. The factors considered in the Written Description requirement are:
(1) level of skill and knowledge in the art,
(2) partial structure,
(3) physical and/or chemical properties,
(4) functional characteristics alone or coupled with a known or disclosed
correlation between structure and function, and
(5) the method of making the claimed invention.
11. Level of skill and knowledge in the art: The level of skill to practice the art of the instantly claimed invention is high and requires a variety of skills usually found in institutions and companies that employ highly trained and skilled scientists and/or physicians to carry out these tasks.
12. Partial structure; Physical and/or chemical properties; and Functional characteristics: The claims are drawn to a method of treating mild cognitive impairment in a subject in need thereof, comprising administering an effective amount of a compound of Formula (I)
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, or a pharmaceutically acceptable salt thereof. In the instant case, it is evident that the genus of compounds embraced by Formula (I) is broad and has substantial variance, i.e., the moiety R1 alone can be any of C1-6 alkyl,–(R)-phenyl, -(R)-C3-8 cycloalkyl, -(R)-C3-10 membered heterocyclyl, or –(R)-C5-10 membered heteroaryl; R3 can be C1-6 alkyl, C3-8 cycloalkyl, or the heterocyclyl rings tetrahydropyranyl, piperidinyl, or oxabicycloheptanyl; Ra includes any C3-10 membered heterocyclyl and C5-6 membered heteroaryl rings; and Rc includes the heterocyclyl rings: azetidinyl, pyrrolidinyl, oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, and dioxidothietanyl. Indeed, the genus is virtually without limit, embracing hundreds of millions of potential compounds bearing little structural resemblance to one another what-so-ever.
Yet, the instant Specification discloses the preparation of only approximately a few dozen structurally related compound species within Formula (I) in the syntheses (i.e., Schemes 31-52, see pages 66-180). Said schemes are primarily limited to the preparation of compounds of Formula (I) wherein R2 is 7-halogen (specifically, chloro) and R1 and R3 are cycloalkyl; or wherein R1 is cycloalkyl and R3 is piperidinyl; or wherein R1 is oxaspirooctane and R3 is piperidinyl; or wherein R1 is tetrahydropyran and R3 is piperidinyl; or wherein R1 and R3 are piperidinyl; or wherein R1 is tetrahydropyran and R3 is cycloalkyl; or wherein R1 is piperidinyl and R3 is cycloalkyl; or wherein R1 is morpholinyl and R3 is cycloalkyl; or wherein R1 is cyclopropafuropyridinyl and R3 is cycloalkyl; or wherein R1 is substituted alkyl and R3 is piperidinyl; or wherein R1 is pyrazolyl and R3 is piperidinyl; or wherein R1 is oxazolyl and R3 is piperidinyl; or wherein R1 is methyl-tetrahydrofuran and R3 is piperidinyl; or wherein R1 is methyl-pyrazolyl and R3 is piperidinyl; or wherein R1 is methyl-pyridinyl and R3 is cycloalkyl; or wherein R1 is methyl-phenyl and R3 is cycloalkyl; or wherein R1 is methyl-morpholinyl and R3 is cycloalkyl; or wherein R1 is tetrahydrofuran and R3 is cycloalkyl; or wherein R1 is tetrahydrofuran and R3 is piperidinyl; or wherein R1 is pyrrolidinyl and R3 is cycloalkyl; or wherein R1 is pyridinyl and R3 is cycloalkyl; or wherein R1 is methyl-pyridinyl and R3 is piperidinyl; or wherein R1 is oxabicycloheptane and R3 is piperidinyl; or wherein R1 is oxabicyclohexane and R3 is piperidinyl; or wherein R1 is oxaspirooctane and R3 is tetrahydropyran; or wherein R1 is oxaspirooctane and R3 is substituted alkyl; or wherein R1 is cycloalkyl and R3 is substituted alkyl; or wherein R1 is oxaspirooctane and R3 is oxabicycloheptane; ; or wherein R1 is oxaspirooctane and R3 is cycloalkyl; or wherein R1 is pyrazolyl and R3 is cyclohexyl.
13. While the MPEP does not define what constitutes a sufficient number of representative species, the courts have indicated what does not constitute a representative number of species to adequately describe a broad generic. For example, in In re Gostelli, the courts determined that the disclosure of two chemical compounds within a subgenus did not describe that subgenus. In re Gostelli, 872 F.2d 1008 (Fed. Cir. 1989). In the instant case, it is similarly determined that the disclosure of a few dozen structurally related compounds does not adequately describe a subgenus embracing hundreds of millions of additional compound species bearing no structural relationship with those disclosed compounds. That is, the Specification does not disclose a sufficient variety of species to reflect the extreme variance in the genus.
14. The instant specification teaches that the instant genus of compounds of Formula (I) are Leucine-Rich Repeat Kinase 2 (LRRK2) inhibitors, which are useful for treating certain neurodengerative diseases including Parkinson’s disease (page 1, paragraphs 1-3). As discussed above, the Specification discloses the preparation of a few dozen species of compounds of Formula (I) (see Schemes 31-52, see pages 66-180), which are primarily limited to compounds of paragraph “12,” above. The Specification provides data demonstrating the potency of certain exemplary compounds towards inhibiting LRRK2 in vitro in the Table at pages 181-188. Thus, the instant Specification has not demonstrated support for all possible alternatives of the genus of compounds of Formula (I).
15. Despite the advanced training of those in the art, the pharmaceutical art is highly unpredictable. It is still not possible to predict the pharmacological activity or treatment efficacy of a compound based on the structure alone. Typically, in order to verify that a compound will be effective in a method or treating a disease, the compounds must be either tested directly in a patient or in a model that has been established as being predictive of efficacy. It is not predictable from the specification or from the prior art that the full scope of the genus of compounds of Formula (I) inhibit LRRK2 in a culture or in the cells of a subject, for the treatment of a neurodegenerative disease, for example.
16. The level of detail required to satisfy the written description requirement varies depending on the nature and scope of the claims and on the complexity and predictability of the relevant technology. Ariad, 598 F.3d at 1351, 94 USPQ2d at 1172; Capon v. Eshhar, 418 F.3d 1349, 1357-58, 76 USPQ2d 1078, 1083-84 (Fed. Cir. 2005).
Applicants have failed to provide guidance or data or evidence as to how the skilled artisan would be able to extrapolate from the disclosure to use the claimed invention. “A description of what a material does, rather than of what it is, usually does not suffice." Rochester, 358 F 3d at 923; Eli Lilly, 119 at 1568. Instead, the “disclosure must allow one skilled in the art to visualize or recognize the identity of the subject matter purportedly described.” Vas-Cath Inc. v. Mahurkar, 19 USPQ2d 1111, makes clear the "applicant must convey with reasonable clarity to those skilled in the art that, as of the filing date sought, he or she was in possession of the invention. The invention is, for purposes of the 'written description' inquiry, whatever is now claimed." (See page 1117.) 17. The specification does not "clearly allow persons of ordinary skill in the art to recognize that [he or she] invented what is claimed." (See Vas-Cath at page 1116).
The description requirement of the patent statue requires a description of an invention, not an indication of a result that one might achieve if one made that invention. See In re Wilder, 736, F.2d 1516, 1521,222 USPQ 369, 372-73 (Fed. Cir. 1984) (affirming rejection because the specification does "little more than outlin[e] goals appellants hope the claimed invention achieves and the problems the invention will hopefully ameliorate.").
18. Accordingly, it is deemed that the specification fails to provide adequate written description for the claimed invention and does not reasonably convey to one skilled in the relevant art that the inventors had possession of the entire scope of the claimed invention.
As such, claims 1-20 and 22 are rejected.
Claim Rejections - 35 USC § 103
19. The following is a quotation of 35 U.S.C. 103 which forms the basis for all obviousness rejections set forth in this Office action:
A patent for a claimed invention may not be obtained, notwithstanding that the claimed invention is not identically disclosed as set forth in section 102, if the differences between the claimed invention and the prior art are such that the claimed invention as a whole would have been obvious before the effective filing date of the claimed invention to a person having ordinary skill in the art to which the claimed invention pertains. Patentability shall not be negated by the manner in which the invention was made.
20. The factual inquiries for establishing a background for determining obviousness under 35 U.S.C. 103 are summarized as follows:
1. Determining the scope and contents of the prior art.
2. Ascertaining the differences between the prior art and the claims at issue.
3. Resolving the level of ordinary skill in the pertinent art.
4. Considering objective evidence present in the application indicating obviousness or nonobviousness.
21. This application currently names joint inventors. In considering patentability of the claims the examiner presumes that the subject matter of the various claims was commonly owned as of the effective filing date of the claimed invention(s) absent any evidence to the contrary. Applicant is advised of the obligation under 37 CFR 1.56 to point out the inventor and effective filing dates of each claim that was not commonly owned as of the effective filing date of the later invention in order for the examiner to consider the applicability of 35 U.S.C. 102(b)(2)(C) for any potential 35 U.S.C. 102(a)(2) prior art against the later invention.
22. Claims 1-20 and 22 are rejected under 35 U.S.C. 103 as being unpatentable over Lyssikatos et al., U.S. 20120322785 A1.
Claim 1 is drawn to a compound according to Formula I:
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or a pharmaceutically acceptable salt thereof, wherein:
R1 is selected from C1-6 alkyl, -(R)-phenyl, monocyclic, spirocyclic or bicyclic -(R)-C3-8 cycloalkyl, -(R)-C3-1o heterocyclyl, and -(R)o-3C3-1o heteroaryl, said alkyl, phenyl, cycloalkyl, heterocyclyl and heteroaryl optionally substituted with 1 to 4 groups selected from Ra;
R is a bond or straight or branched C1-6 alkylenyl;
R2 is selected from hydrogen, C1-6 alkyl, and halogen;
R3 is in the 6-position and is selected from C1-6 alkyl, spiropentanyl, cyclopropyl, cyclobutyl, cyclohexyl, and C-linked tetrahyropyranyl, C-linked piperidinyl, and C-linked oxabicycloheptanyl, said alkyl, spiropentanyl, cyclopropyl, cyclobutyl, cyclohexyl, tetrahyropyranyl, piperidinyl, and oxabicycloheptanyl are unsubstituted or substituted with 1 to 3 groups independently selected from 1 to 3 groups from Rc;
Ra is independently selected from the group consisting of H, halogen, -OH, CN, -OC1-6 alkyl, C1-6 alkyl, C3-6 cycloalkyl, C(O)CF3, C(O)C1-6 alkyl, C1-3 haloalkyl, C1-3 haloalkoxy, NH(C1-6 alkyl), N(C1-6 alkyl)2, -OC1-3 haloalkyl, (CH2)nC5-6 hetero-aryl, (CH2)nC3-1o heterocyclyl, -NH2, said alkyl, heterocyclyl, and heteroaryl optionally substituted with 1 to 3 groups of Rb;
Rb is independently selected from the group consisting of C1-6 alkyl, -OC1-6 alkyl, halogen, OH, CN, and C1-3 haloalkyl;
Rc is independently selected from the group consisting of hydrogen, C1-6 alkyl, OC1-6 alkyl, C3-6 cycloalkyl, CN, OH, halogen, azetidinyl, pyrrolidinyl, oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, and dioxidothietanyl, wherein said alkyl, cycloalkyl, azetidinyl, pyrrolidinyl, oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, and dioxidothietanyl are optionally substituted with 1 to 3 groups independently selected from C1-6 alkyl, halogen, CN, OC1-6 alkyl, C3-6 cycloalkyl and OH; and n is selected from 0 to 3;
more specifically:
wherein R1 is cyclopropyl (claims 2-4), R2 is hydrogen (claim 5); R3 is cyclohexyl (claims 6, 9, 10 and 18) or optionally substituted alkyl (claims 6, 7, and 18).
23. Lyssikatos et al. teach a genus of functionally related isoquinoline derivatives having the same isoquinoline-carboxamide core structure that is instantly recited by Applicant and specifically disclose the following compound species in Table 1:
Compound No. 34:
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, which is the same as a compound of Applicant’s instant Formula (I) wherein R1 is cyclopropyl and R3 is 7-cyclohexyl, but differs solely in the position of the cyclohexyl substituent on the isoquinoline ring;
Compound 156:
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71
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, which is the same as a compound of Applicant’s instant Formula (I) wherein R1 is cyclopropyl and R3 is 7-alkyl, but differs solely in the position of the alkyl substituent on the isoquinoline ring;
Compound 175:
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, Compound 214 and Compound 215:
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, which are the same as a compound of Applicant’s instant Formula (I) wherein R1 is cyclopropyl and R3 is 7-hydroxy-alkyl, but differ solely in the position of the hydroxy-alkyl substituent on the isoquinoline ring (see Table 1, pages 19, 42 and 49).
24. As such, the genus of compounds disclosed by Lyssikatos et al. fully encompasses the compounds of the instant invention and also demonstrates kinase inhibitory activity for treating neurodegenerative diseases, for example, but Lyssikatos et al. do not teach the administration of a single disclosed compound or species that anticipates the instant claims.
25. Yet, compounds that are position isomers (compounds having the same radicals in physically different positions on the same nucleus) are generally of sufficiently close structural similarity that there is a presumed expectation that such compounds possess similar properties. In re Wilder, 563 F.2d 457, 195 USPQ 426 (CCPA 1977). See also In re May, 574 F.2d 1082, 197 USPQ 601 (CCPA 1978) (stereoisomers prima facie obvious). See MPEP 2144.09.
26. Therefore, one of skill in the art before the effective filing date of the claimed invention would have been motivated to prepare the instantly recited position isomers of the isoquinoline-carboxamide compounds species which are substituted by R3 in the 6-position rather than the compounds taught by Lyssikatos et al that are substituted by “R3” moieties in the 7-position, and would have had a reasonable expectation of success. It would have been obvious to one skilled in the art before the effective filing date of the claimed invention to substitute the instantly recited position isomer (i.e., wherein the optionally substituted alkyl group or cyclohexyl ring is in the 6-position), for the compounds taught by Lyssikatos et al. wherein the alkyl moiety or cyclohexyl ring is in the 7-position, because compounds that are similar in structure (e.g., position isomers) are expected to behave similarly.
As such, claims 1-7, 9, 10, and 18 are prima facie obvious.
Claim 20 is drawn to a pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.
27. Lyssikatos et al. go on to teach a pharmaceutical composition:
“the invention also provides for compositions and medicaments comprising a compound of Formula I and at least one pharmaceutically acceptable carrier, diluent or excipient,”
(see paragraph [0088]). Therefore, one skilled in the art before the effective filing date of the claimed invention would have been motivated to combine the position isomer of Compounds 34, 156, 175, 214 or 215, as discussed above, with a pharmaceutically acceptable carrier in composition form, with a reasonable expectation of success.
As such, claim 20 is prima facie obvious.
Claim 22 is drawn to a compound according to claim 1 for use in therapy.
28. Regarding claims 22, Applicant is reminded that the preamble recites a compound, and while the use of a descriptive clause, i.e., “for use in…,” when referring to the contemplated use (i.e. “intended use”) of a claimed compound is proper, it is not a limitation and thus of no significance in determining the patentability thereof over the prior art, please refer to In re Thomas (CCPA 1949) 178 F2d 412, 84 USPQ 132. Therefore, claim 22, drawn to the compound of claim 1, is prima facie obvious.
Claim Objections
29. Claims 8, and 11-17 are also objected to as being dependent upon a base claim rejected under 35 U.S.C. 103.
Double Patenting
30. 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 double patenting rejection is appropriate where the conflicting claims are not identical, but at least one examined application claim is not patentably distinct from the reference claim(s) because the examined application claim is either anticipated by, or would have been obvious over, the reference claim(s). See, e.g., 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); In re Thorington, 418 F.2d 528, 163 USPQ 644 (CCPA 1969).
31. A timely filed terminal disclaimer in compliance with 37 CFR 1.321(c) or 1.321(d) may be used to overcome an actual or provisional rejection based on nonstatutory double patenting provided the reference application or patent either is shown to be commonly owned with the examined application, or claims an invention made as a result of activities undertaken within the scope of a joint research agreement. See MPEP § 717.02 for applications subject to examination under the first inventor to file provisions of the AIA as explained in MPEP § 2159. See MPEP § 2146 et seq. for applications not subject to examination under the first inventor to file provisions of the AIA . A terminal disclaimer must be signed in compliance with 37 CFR 1.321(b).
32. The filing of a terminal disclaimer by itself is not a complete reply to a nonstatutory double patenting (NSDP) rejection. A complete reply requires that the terminal disclaimer be accompanied by a reply requesting reconsideration of the prior Office action. Even where the NSDP rejection is provisional the reply must be complete. See MPEP § 804, subsection I.B.1. For a reply to a non-final Office action, see 37 CFR 1.111(a). For a reply to final Office action, see 37 CFR 1.113(c). A request for reconsideration while not provided for in 37 CFR 1.113(c) may be filed after final for consideration. See MPEP §§ 706.07(e) and 714.13.
33. The USPTO Internet website contains terminal disclaimer forms which may be used. Please visit www.uspto.gov/patent/patents-forms. The actual filing date of the application in which the form is filed determines what form (e.g., PTO/SB/25, PTO/SB/26, PTO/AIA /25, or PTO/AIA /26) should be used. A web-based eTerminal Disclaimer may be filled out completely online using web-screens. An eTerminal Disclaimer that meets all requirements is auto-processed and approved immediately upon submission. For more information about eTerminal Disclaimers, refer to www.uspto.gov/patents/apply/applying-online/eterminal-disclaimer.
34. Claims 1-20 and 22 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-9, 12, 13, and 16-20 of U.S. Patent No. 12,516,039 B2.
35. Although the claims at issue are not identical, they are not patentably distinct from each other because the instant claims recite the following:
Claim 1 is drawn to a compound according to Formula I:
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or a pharmaceutically acceptable salt thereof, wherein:
R1 is selected from C1-6 alkyl, -(R)-phenyl, monocyclic, spirocyclic or bicyclic -(R)-C3-8 cycloalkyl, -(R)-C3-1o heterocyclyl, and -(R)o-3C3-1o heteroaryl, said alkyl, phenyl, cycloalkyl, heterocyclyl and heteroaryl optionally substituted with 1 to 4 groups selected from Ra; R is a bond or straight or branched C1-6 alkylenyl;
R2 is selected from hydrogen, C1-6 alkyl, and halogen; R3 is selected from C1-6 alkyl, spiropentanyl, cyclopropyl, cyclobutyl, cyclohexyl, and C-linked tetrahyropyranyl, C-linked piperidinyl, and C-linked oxabicycloheptanyl, said alkyl, spiropentanyl, cyclopropyl, cyclobutyl, cyclohexyl, tetrahyropyranyl, piperidinyl, and oxabicycloheptanyl are unsubstituted or substituted with 1 to 3 groups independently selected from 1 to 3 groups from Rc;
Ra is independently selected from the group consisting of H, halogen, -OH, CN, -OC1-6 alkyl, C1-6 alkyl, C3-6 cycloalkyl, C(O)CF3, C(O)C1-6 alkyl, C1-3 haloalkyl, C1-3 haloalkoxy, NH(C1-6 alkyl), N(C1-6 alkyl)2, -OC1-3 haloalkyl, (CH2)nC5-6 hetero-aryl, (CH2)nC3-1o heterocyclyl, -NH2, said alkyl, heterocyclyl, and heteroaryl optionally substituted with 1 to 3 groups of Rb; Rb is independently selected from the group consisting of C1-6 alkyl, -OC1-6 alkyl, halogen, OH, CN, and C1-3 haloalkyl;
Rc is independently selected from the group consisting of hydrogen, C1-6 alkyl, OC1-6 alkyl, C3-6 cycloalkyl, CN, OH, halogen, azetidinyl, pyrrolidinyl, oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, and dioxidothietanyl, wherein said alkyl, cycloalkyl, azetidinyl, pyrrolidinyl, oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, and dioxidothietanyl are optionally substituted with 1 to 3 groups independently selected from C1-6 alkyl, halogen, CN, OC1-6 alkyl, C3-6 cycloalkyl and OH; and n is selected from 0 to 3. Claims 2-4 are drawn to claim 1 and further limit R1. Claim 5 is drawn to claim 1 and further limits R2. Claims 6-12, 15 and 18 are drawn to claim 1 and further limit R3. Claims 13-14 further limit claim 12. Claims 16 and 17 further limit claim 15. Claim 19 is drawn to species of the compound of Formula (I) of claim 1. Claim 20 is drawn to a pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier. Claim 22 is drawn to a compound of claim 1, for use in therapy.
36. The claims of U.S. Patent No. 12,516,039 B2 are as follows:
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413
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256
295
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615
306
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34
290
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223
290
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[language omitted from claim 17],
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37. As such, Applicant’s instant claims overlap with the genus of isoquinoline-carboxamide compounds of Formula (I) of U.S. Pat No. 12,516,039, wherein R1 is a monocyclic or bicyclic C3-8 carbocyclic ring; R2 is hydrogen, halogen, or alkyl; and R3 is piperidinyl.
38. The instant claims differ solely in the position of the piperidinyl attachment on the isoquinoline ring, i.e., the instant claims require the limitation that the piperidinyl is C-linked.
39. However, compounds that are position isomers (compounds having the same radicals in physically different positions on the same nucleus) are generally of sufficiently close structural similarity that there is a presumed expectation that such compounds possess similar properties. In re Wilder, 563 F.2d 457, 195 USPQ 426 (CCPA 1977). See also In re May, 574 F.2d 1082, 197 USPQ 601 (CCPA 1978) (stereoisomers prima facie obvious). See MPEP 2144.09.
40. Therefore, one of skill in the art would have been motivated to prepare the instantly recited position isomers of the isoquinoline-carboxamide compounds species which are substituted by R3, wherein R3 is C-piperidinyl, rather than the compounds of U.S. Pat No. 12,516,039 that are substituted by R3 wherein R3 is N-piperidinyl, and would have had a reasonable expectation of success. It would have been obvious to one skilled in the art before the effective filing date of the claimed invention to substitute the instantly recited position isomer for the compounds recited by U.S. Pat No. 12,516,039 because compounds that are similar in structure (e.g., position isomers) are expected to behave similarly.
Conclusion
41. In conclusion, claims 1-24 are pending in the application. Claims 1-20 and 22 are rejected. Claims 21 and 23-24 are presently withdrawn from further consideration as directed to a non-elected invention. No claim is currently allowed.
42. Any inquiry concerning this communication or earlier communications from the examiner should be directed to JANET L COPPINS whose telephone number is (571)272-0680. The examiner can normally be reached Monday-Friday 8:30AM-5PM EST.
Examiner interviews are available via telephone, in-person, and video conferencing using a USPTO supplied web-based collaboration tool. To schedule an interview, applicant is encouraged to use the USPTO Automated Interview Request (AIR) at http://www.uspto.gov/interviewpractice.
If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Amy L Clark can be reached at 571-272-1310. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
Information regarding the status of published or unpublished applications may be obtained from Patent Center. Unpublished application information in Patent Center is available to registered users. To file and manage patent submissions in Patent Center, visit: https://patentcenter.uspto.gov. Visit https://www.uspto.gov/patents/apply/patent-center for more information about Patent Center and https://www.uspto.gov/patents/docx for information about filing in DOCX format. For additional questions, contact the Electronic Business Center (EBC) at 866-217-9197 (toll-free). If you would like assistance from a USPTO Customer Service Representative, call 800-786-9199 (IN USA OR CANADA) or 571-272-1000.
/JANET L COPPINS/Examiner, Art Unit 1628
/AMY L CLARK/Supervisory Patent Examiner, Art Unit 1628
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