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 .
Priority
The instant application, filed 12/10/2021, is a Continuation of PCT/US2020/037233, filed 06/11/2020. Acknowledgment is made of applicant’s claim of foreign priority to PCT/CN2019/090714, filed 06/11/2019. Receipt is acknowledged of certified copies of papers required by 37 CFR § 1.55.
Continued Examination Under 37 CFR § 1.114
A request for continued examination under 37 CFR § 1.114, including the fee set forth in 37 CFR 1.17(e), was filed in this application after final rejection. Since this application is eligible for continued examination under 37 CFR § 1.114, and the fee set forth in 37 CFR § 1.17(e) has been timely paid, the finality of the previous Office action has been withdrawn pursuant to 37 CFR § 1.114. Applicant's submission filed on 2/26/2026 has been entered.
Amendments and Claim Status
The amendment filed on 02/02/2026 is acknowledged and entered.
Claim 1 is amended;
Claims 4-10, 13- 15, 18, 19, 21, 23-26, 28, 29, 31- 33, 36, 38, 39, 41-44, 48-50, 52-54, 57-60, 62, 65, 67-70, and 73-103 are cancelled;
Claims 35, 37, 51, 64, 66, 71, and 72 remain withdrawn from further consideration pursuant to 37 CFR § 1.142(b), as being drawn to a non-elected invention and species;
Claims 1-3, 11, 12, 16, 17, 20, 22, 27, 30, 34, 35, 37, 40, 45, 47, 51, 55, 56, 61, 63, 64, 66, 71, and 72 are pending.
Information Disclosure Statement
The Information Disclosure Statement filed on 03/02/2026 is acknowledged and found to be in compliance with the provisions of 37 CFR § 1.97. Accordingly, the information disclosure statement is considered.
Response to arguments
Applicant’s arguments filed 02/02/2026 with respect to the claim rejection under 35 U.S.C. § 103 have been fully considered.
With respect to the rejection of claims 1-3, 11, 12, 16, 17, 20, 27, 30, 34, 40, 55, 56, and 63 under 35 U.S.C. § 103 as being unpatentable over Vacca et al. (WO 2018222918 A1, December 6, 2018, listed on applicant IDS filed 05/03/2022), hereinafter Vacca ‘918 in view of Patani et al., (Chem. Rev. 1996, 96, 3147-3176), hereinafter Patani, Applicants arguments have been fully considered, but have not been found to be persuasive. Applicant’s arguments are addressed, below.
Applicant argues that there is no reason to select the prior art compound as a “lead compound.”
Applicant’s argument is found unpersuasive because a person of ordinary skill in the art would be directly motivated to improve compounds which have poor efficacy. This reasoning mischaracterizes the considerations of a person of ordinary skill in the art in the context of lead compound selection. In medicinal chemistry, the selection of a lead compound does not require that the compound initially exhibit the highest potency or selectivity at the outset. Rather, it is well established that lead compounds are often selected despite suboptimal activity because they provide a tractable chemical scaffold amenable to modification. In fact, compounds of moderate or even poorer activity are frequently chosen for optimization precisely because they leave room for structural improvement through routine structure-activity relationship exploration. The prior art by Vacca ’918, Compound 73 represents such a scaffold. The compound is a disclosed, operative IRE1 inhibitor, rendering it suitable for selection as a starting point based on structural similarity and known activity. The decision to use said compound as a lead would not have required impermissible hindsight, but rather, reflects the standard practice of a person of ordinary skill in the art, who would recognize that incremental modifications to such a scaffold would reasonably be expected to yield improvements in potency, selectivity, and pharmacological profile, as evidenced by MPEP § 2143 (I) (B), Example 9,
The Federal Circuit in Eisai makes it clear that from the perspective of the law of obviousness, any known compound might possibly serve as a lead compound: "Obviousness based on structural similarity thus can be proved by identification of some motivation that would have led one of ordinary skill in the art to select and then modify a known compound (i.e. a lead compound) in a particular way to achieve the claimed compound." Eisai, 533 F.3d at 1357, 87 USPQ2d at 1455. Thus, Office personnel should recognize that a proper obviousness rejection of a claimed compound that is useful as a drug might be made beginning with an inactive compound, if, for example, the reasons for modifying a prior art compound to arrive at the claimed compound have nothing to do with pharmaceutical activity. The inactive compound would not be considered to be a lead compound by pharmaceutical chemists, but could potentially be used as such when considering obviousness. Office personnel might also base an obviousness rejection on a known compound that pharmaceutical chemists would not select as a lead compound due to expense, handling issues, or other business considerations. However, there must be some reason for starting with that particular lead compound other than the mere fact that the "lead compound" exists. See Altana Pharma AG v. Teva Pharm. USA, Inc., 566 F.3d 999, 1007, 91 USPQ2d 1018, 1024 (Fed. Cir. 2009) (holding that there must be some reason "to select and modify a known compound"); Ortho-McNeil Pharm., Inc. v. Mylan Labs, Inc., 520 F.3d 1358, 1364, 86 USPQ2d 1196, 1201 (Fed. Cir. 2008).
PNG
media_image1.png
117
346
media_image1.png
Greyscale
Thus, Applicant’s argument that only the “most potent” compound could serve as a lead is inconsistent with established and routine principles of drug discovery practice, and imposes an unduly restrictive standard that is inconsistent with established Federal Circuit precedent. Therefore, the argument is found not persuasive. Nevertheless, the elected species, as well as the compounds instantly claimed are sufficiently novel, with respect to the simultaneous of RF as a benzyl group, as opposed to a phenyl group as taught in the prior art, and the substitution of a heterocycle at CyA’ of Formula (I) of the prior art.
Applicant argues that there is no motivation to modify the compounds, to arrive at the instantly claimed.
Applicant's argument is unconvincing because the stated modifications constitute routine medicinal chemistry optimizations to preserve the core scaffold and activity, providing a reasonable expectation of success, individually. However, upon further consideration, the simultaneous modification of RF as a benzyl group and a heterocycle at RA in contrast to the teachings of the prior art would not be considered obvious to a person of ordinary skill in the art. A person of ordinary skill in the art would not expect that making such modifications would retain an identical active, and would not be directed to make some modifications based on the prior art teachings.
Applicant argues that benzyl and phenyl are not homologous substitutions.
Applicant’s argument is unconvincing because the phenyl to benzyl modification is minor structural variation, differing only by a single -CH2- between LA and RF. However, upon further consideration, the benzyl moiety confers flexibility in the form of a “hinge” -CH2- to a phenyl substituent that was once more fixed in position.
As such, the consideration of Applicant’s arguments in addition to the sum total modifications from the prior art compound referenced in the office action filed 09/03/2025 is overcome the rejection. As such, the rejection is hereby withdrawn.
As a result of the withdrawal of the rejection, the instant claims, starting with the elected species, have been further searched. It has been determined that the instantly claimed compounds of claim 61 and compounds/pharmaceutical compositions of claim 1 and its dependent claims are allowable over the prior art. However, in consideration of whether or not the specification supports the written description requirement of the instant claims, it has been determined that the entire scope is not patentable. As such, in a rejection under 35 U.S.C. § 112 is included hereinafter.
Status of Claims
Claims 1-3, 11, 12, 16, 17, 20, 22, 27, 30, 34, 35, 37, 40, 45, 47, 51, 55, 56, 61, 63, 64, 66, 71, and 72 are pending in the instant application. Claims 35, 37, 51, 64, 66, 71, and 72 are withdrawn from further consideration pursuant to 37 CFR § 1.142(b), as being drawn to a non-elected invention and species. Therefore, claims 1-3, 11, 12, 16, 17, 20, 22, 27, 30, 34, 40, 45, 47, 55, 56, 61, and 63 read on an elected invention and species and are therefore under consideration in the instant application.
Claim Rejections - 35 U.S.C. § 112
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.
Claims 1-3, 11, 12, 16, 17, 20, 22, 27, 30, 34, 40, 45, 47, 55, 56, and 63 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 claim(s) 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 inventor(s), at the time the application was filed, had possession of the claimed invention.
Claims 1-3, 11, 12, 16, 17, 20, 22, 27, 30, 34, 35, 37, 40, 45, 47, 51, 55, 56, and 63 of the instant application are drawn to compounds having following substituents:
LA is —NHSO2—, —SO2NH—, or —NH;
RA is RG-substituted or unsubstituted bicyclic 7 to 10 membered spiro-heterocycloalkyl,
PNG
media_image2.png
152
284
media_image2.png
Greyscale
;
RB and RC are independently hydrogen or RN-substituted or unsubstituted C1-6 alkyl, RN-substituted or unsubstituted C3-7 cycloalkyl, or RN-substituted or unsubstituted 3 to 7 membered heterocycloalkyl, or RB and RC are taken together with the nitrogen atom to which they are attached to form a RN-substituted or unsubstituted 4 to 57 membered heterocycloalkyl;
RD is hydrogen, halogen, —CN, —ORI, —S(O)2RI, —NRJRK, RN-substituted or unsubstituted C1-6 alkyl, RN-substituted or unsubstituted C1-6 haloalkyl, RN-substituted or unsubstituted C3-7 cycloalkyl, RN-substituted or unsubstituted 3 to 7 membered heterocycloalkyl, RN-substituted or unsubstituted C6 aryl, or RN-substituted or unsubstituted 5 to 7 membered heteroaryl;
each RE is hydrogen, halogen, —ORI, —CN, —S(O)2RI, RM-substituted or unsubstituted C1-6 alkyl, RM-substituted or unsubstituted C1-6 haloalkyl, or RM-substituted or unsubstituted C3-7 cycloalkyl;
n is 0, 1, 2, 3, or 4;
RF is RN-substituted or unsubstituted C1-6 alkyl, RN-substituted or unsubstituted C3-7 cycloalkyl, RN-substituted or unsubstituted benzyl, RN-substituted or unsubstituted 3 to 7 membered heterocycloalkyl, or RN substituted or unsubstituted 5 to 7 membered heteroaryl comprising at least one N atom;
each RG is independently halogen, —ORI, RM-substituted or unsubstituted C1-6 alkyl, or RM-substituted or unsubstituted C1-6 haloalkyl;
t is 0, 1, 2, 3, 4, 5, or 6;
each RH is independently halogen, C1-3 alkyl, C1-3 haloalkyl, or cyclopropyl;
j is 0, 1, or 2; 1
each RI, RJ, and RK is independently hydrogen, RM-substituted or unsubstituted C1-6 alkyl, RM-substituted or unsubstituted C1-6 haloalkyl, RM-substituted or unsubstituted C3-7 cycloalkyl, RM-substituted or unsubstituted 3 to 7 membered heterocycloalkyl, RM-substituted or unsubstituted C6 membered aryl, or RM-substituted or unsubstituted 5 to 7 membered heteroaryl;
each RM is independently hydrogen, halogen, —CN, —OH, —OCH3, —OCF3, —S(O)2H, —S(O)2NH2, —NH2, —NH(CH3), —N(CH3)2, —CF3, —CHF2, —CH2F, —C(CH3)2F, —C(CH3)F2, unsubstituted C1-6 alkoxy, unsubstituted C1-6 alkyl, unsubstituted C1-6 haloalkyl, unsubstituted C3-7 cycloalkyl, unsubstituted 3 to 6 membered heterocycloalkyl, unsubstituted C6 aryl, or unsubstituted 5 to 7 membered heteroaryl;
each RN is independently hydrogen, halogen, —CN, —ORR, —S(O)2RR, —NRSRT, RP-substituted or unsubstituted C1-6 alkyl, RP-substituted or unsubstituted C1-6 haloalkyl, RP-substituted or unsubstituted C1-6 alkoxy, RP-substituted or unsubstituted C3-7 cycloalkyl, RP-substituted or unsubstituted 3 to 5 6 membered heterocycloalkyl, RP-substituted or unsubstituted C6 aryl, or RP-substituted or unsubstituted 5 to 7 membered heteroaryl;
each RR, RS and RT is independently hydrogen, RV-substituted or unsubstituted C1-6 alkyl, RV-substituted or unsubstituted C1-6 haloalkyl, RV-substituted or unsubstituted C3-7 cycloalkyl, or RV-substituted or unsubstituted 3 to 7 membered heterocycloalkyl;
each RV is independently hydrogen, halogen, —CN, —OH, —OCH3, —OCF3, —S(O)2H, —S(O)2NH2, —NH2, —NH(CH3), —N(CH3)2, —CF3, —CHF2, —CH2F, —C(CH3)2F, —C(CH3)F2, unsubstituted C1-6 alkoxy, unsubstituted C1-6 alkyl, unsubstituted C1-6 haloalkyl, unsubstituted C3-7 cycloalkyl, unsubstituted 3 to 6 membered heterocycloalkyl, unsubstituted C6 aryl, or unsubstituted 5 to 7 membered heteroaryl;
each RP is independently hydrogen, halogen, —CN, —ORW, —S(O)2RW, —NRXRY, RU-substituted or unsubstituted C1-6 alkyl, RU-substituted or unsubstituted C1-6 haloalkyl, RU-substituted or unsubstituted C3-7 cycloalkyl, RU-substituted or unsubstituted 3 to 6 membered heterocycloalkyl, RU-substituted or unsubstituted C6 aryl, or RU-substituted or unsubstituted 5 to 7 membered heteroaryl;
each RW, RX and RY is independently hydrogen, unsubstituted C1-6 alkyl, unsubstituted C1-6 haloalkyl, unsubstituted C3-7 cycloalkyl, or unsubstituted 3 to 7 membered heterocycloalkyl, and each RU is independently hydrogen, halogen, —CN, —OH, —OCH3, —OCF3, —S(O)2H, —S(O)2NH2, —NH2, —NH(CH3), —N(CH3)2, —CF3, —CHF2, —CH2F, —C(CH3)2F, —C(CH3)F2, unsubstituted C1-6 alkoxy, unsubstituted C1-6 alkyl, unsubstituted C1-6 haloalkyl, unsubstituted C3-7 cycloalkyl, unsubstituted 3 to 6 membered heterocycloalkyl, unsubstituted C6 aryl, or unsubstituted 5 to 7 membered heteroaryl;
RE1, RE2, RE3, and RE4 are each independently hydrogen, halogen, or, RM-substituted or unsubstituted C1-6 alkyl;
35 U.S.C. 112(a) and the first paragraph of pre-AIA 35 U.S.C. 112 require that the "specification shall contain a written description of the invention ...." This requirement is separate and distinct from the enablement requirement. Ariad Pharm., Inc. v. Eli Lilly & Co., 598 F.3d 1336, 1340, 94 USPQ2d 1161, 1167 (Fed. Cir. 2010) (en banc); Vas-Cath, Inc. v. Mahurkar, 935 F.2d 1555, 1560, 19 USPQ2d 1111,1114 (Fed. Cir. 1991); see also Univ. of Rochester v. G.D. Searle & Co., 358 F.3d 916, 920-23, 69 USPQ2d 1886, 1890-93 (Fed. Cir. 2004) (discussing the history and purpose of the written description requirement); In re Curtis, 354 F.3d 1347, 1357, 69 USPQ2d 1274, 1282 (Fed. Cir. 2004) ("conclusive evidence of a claim’s enablement is not equally conclusive of that claim’s satisfactory written description"). The written description requirement has several policy objectives. "[T]he ‘essential goal’ of the description of the invention requirement is to clearly convey the information that an applicant has invented the subject matter which is claimed." In re Barker, 559 F.2d 588, 592 n.4, 194 USPQ 470, 473 n.4 (CCPA 1977). Another objective is to convey to the public what the applicant claims as the invention. See Regents of the Univ. of Cal. v. Eli Lilly, 119 F.3d 1559, 1566, 43 USPQ2d 1398, 1404 (Fed. Cir. 1997), cert, denied, 523 U.S. 1089 (1998). "The ‘written description’ requirement implements the principle that a patent must describe the technology that is sought to be patented; the requirement serves both to satisfy the inventor’s obligation to disclose the technologic knowledge upon which the patent is based, and to demonstrate that the patentee was in possession of the invention that is claimed." Capon v. Eshhar, 418 F.3d 1349, 1357, 76 USPQ2d 1078, 1084 (Fed. Cir. 2005). Further, the written description requirement promotes the progress of the useful arts by ensuring that patentees adequately describe their inventions in their patent specifications in exchange for the right to exclude others from practicing the invention for the duration of the patent’s term.
To satisfy the written description requirement, a patent specification must describe the claimed invention in sufficient detail that one skilled in the art can reasonably conclude that the inventor had possession of the claimed invention. See, e.g., Moba, B.V. v. Diamond Automation, Inc., 325 F.3d 1306, 1319, 66 USPQ2d 1429, 1438 (Fed. Cir. 2003); Vas-Cath, Inc. v. Mahurkar, 935 F.2d at 1563, 19 USPQ2d at 1116.
An applicant shows possession of the claimed invention by describing the claimed invention with all of its limitations using such descriptive means as words, structures, figures, diagrams, and formulas that fully set forth the claimed invention. Lockwood v. Amer. Airlines, Inc., 107 F.3d 1565, 1572, 41 USPQ2d 1961, 1966 (Fed. Cir. 1997). Possession may be shown in a variety of ways including description of an actual reduction to practice, or by showing that the invention was "ready for patenting" such as by the disclosure of drawings or structural chemical formulas that show that the invention was complete, or by describing distinguishing identifying characteristics sufficient to show that the applicant was in possession of the claimed invention. See, e.g., Pfaffv. Wells Bees., Inc., 525 U.S. 55, 68, 119 S.Ct. 304, 312, 48 USPQ2d 1641, 1647 (1998); EliLilly, 119 F.3d at 1568, 43 USPQ2d at 1406; Amgen, Inc. v. Chugai Pharm.,927 F.2d 1200, 1206, 18 USPQ2d 1016, 1021 (Fed. Cir. 1991). An application specification may show actual reduction to practice by describing testing of the claimed invention.
In the present case, the important factors leading to a conclusion of inadequate written description is the absence of any working example of the invention as claimed, and the lack of predictability in the art.
In the instant specification, there is no disclosure of compounds having the following claimed substituents:
LA as —SO2NH—, or —NH;
RA as RG-substituted or unsubstituted bicyclic 7 to 10 membered spiro-heterocycloalkyl;
RB as RC RN-substituted or unsubstituted C2-6 alkyl, RN-substituted or unsubstituted C4-7 cycloalkyl, or RN-substituted or unsubstituted 4 to 7 membered heterocycloalkyl, or RB and RC are taken together with the nitrogen atom to which they are attached to form a RN-substituted or unsubstituted 4 or 6 to 7 membered heterocycloalkyl
RD as halogen, —CN, —ORI, —S(O)2RI, —NRJRK, RN-substituted or unsubstituted C4-6 alkyl, RN-substituted or unsubstituted C1-6 haloalkyl, RN-substituted or unsubstituted C3-7 cycloalkyl, RN-substituted or unsubstituted 3 to 7 membered heterocycloalkyl, RN-substituted or unsubstituted C6 aryl, or RN-substituted or unsubstituted 5 to 7 membered heteroaryl;
RE as —ORI, —CN, —S(O)2RI, RM-substituted or unsubstituted C2-6 alkyl, RM-substituted or unsubstituted C1-6 haloalkyl, or RM-substituted or unsubstituted C3-7 cycloalkyl;
n as 4;
RF as RN-substituted or unsubstituted C5-6 alkyl, RN-substituted or unsubstituted C3-7 cycloalkyl, RN-substituted or unsubstituted benzyl, RN-substituted or unsubstituted 3 to 7 membered heterocycloalkyl, or RN substituted or unsubstituted 5 to 7 membered heteroaryl comprising at least one N atom;
RG as —ORI, RM-substituted or unsubstituted C2-6 alkyl, or RM-substituted or unsubstituted C1-6 haloalkyl;
t as 2, 3, 4, 5, or 6;
RH as C1-3 alkyl, C1-3 haloalkyl, or cyclopropyl;
j as 2;
RI, RJ, and RK as independently hydrogen, RM-substituted or unsubstituted C1-6 alkyl, RM-substituted or unsubstituted C1-6 haloalkyl, RM-substituted or unsubstituted C3-7 cycloalkyl, RM-substituted or unsubstituted 3 to 7 membered heterocycloalkyl, RM-substituted or unsubstituted C6 membered aryl, or RM-substituted or unsubstituted 5 to 7 membered heteroaryl;
RM as —CN, —OH, —OCH3, —OCF3, —S(O)2H, —S(O)2NH2, —NH2, —NH(CH3), —N(CH3)2, —CF3, —CHF2, —CH2F, —C(CH3)2F, —C(CH3)F2, unsubstituted C1-6 alkoxy, unsubstituted C1-6 alkyl, unsubstituted C1-6 haloalkyl, unsubstituted C3-7 cycloalkyl, unsubstituted 3 to 6 membered heterocycloalkyl, unsubstituted C6 aryl, or unsubstituted 5 to 7 membered heteroaryl;
RN as —CN, —ORR, —S(O)2RR, —NRSRT, RP-substituted or unsubstituted C1-6 alkyl, RP-substituted or unsubstituted C1-6 haloalkyl, RP-substituted or unsubstituted C1-6 alkoxy, RP-substituted or unsubstituted C3-7 cycloalkyl, RP-substituted or unsubstituted 6 membered heterocycloalkyl, or RP-substituted or unsubstituted 5 to 7 membered heteroaryl;
RR, RS and RT as hydrogen, RV-substituted or unsubstituted C1-6 alkyl, RV-substituted or unsubstituted C1-6 haloalkyl, RV-substituted or unsubstituted C3-7 cycloalkyl, or RV-substituted or unsubstituted 3 to 7 membered heterocycloalkyl;
RV as halogen, —CN, —OH, —OCH3, —OCF3, —S(O)2H, —S(O)2NH2, —NH2, —NH(CH3), —N(CH3)2, —CF3, —CHF2, —CH2F, —C(CH3)2F, —C(CH3)F2, unsubstituted C1-6 alkoxy, unsubstituted C1-6 alkyl, unsubstituted C1-6 haloalkyl, unsubstituted C3-7 cycloalkyl, unsubstituted 3 to 6 membered heterocycloalkyl, unsubstituted C6 aryl, or unsubstituted 5 to 7 membered heteroaryl;
RP as —ORW, —S(O)2RW, —NRXRY, RU-substituted or unsubstituted C2-6 alkyl, RU-substituted or unsubstituted C1-6 haloalkyl, RU-substituted or unsubstituted C3-7 cycloalkyl, RU-substituted or unsubstituted 3 to 6 membered heterocycloalkyl, RU-substituted or unsubstituted C6 aryl, or RU-substituted or unsubstituted 5 to 7 membered heteroaryl;
RW, RX and RY as independently hydrogen, unsubstituted C1-6 alkyl, unsubstituted C1-6 haloalkyl, unsubstituted C3-7 cycloalkyl, or unsubstituted 3 to 7 membered heterocycloalkyl, and each RU is independently hydrogen, halogen, —CN, —OH, —OCH3, —OCF3, —S(O)2H, —S(O)2NH2, —NH2, —NH(CH3), —N(CH3)2, —CF3, —CHF2, —CH2F, —C(CH3)2F, —C(CH3)F2, unsubstituted C1-6 alkoxy, unsubstituted C1-6 alkyl, unsubstituted C1-6 haloalkyl, unsubstituted C3-7 cycloalkyl, unsubstituted 3 to 6 membered heterocycloalkyl, unsubstituted C6 aryl, or unsubstituted 5 to 7 membered heteroaryl;
RE1, RE2, RE3, and RE4 as RM-substituted or unsubstituted C2-6 alkyl;
The instant specification (pages 35-45 and 68-98) teaches compounds which are characterized as having only the following substituents:
LA is —NHSO2—
RA is
PNG
media_image2.png
152
284
media_image2.png
Greyscale
RB and RC are hydrogen, RN-substituted or unsubstituted C1 alkyl, cyclopropyl, 3 membered heterocycloalkyl, or RB and RC are taken together with the nitrogen atom to which they are attached to form an unsubstituted 5 membered heterocycloalkyl;
RD is H, CH2CH3, CH(CH3)2
RE is hydrogen, halogen, CH3
n is 0, 1, 2, or 3
RF is RN-substituted or unsubstituted C1-4 alkyl,
RG is halogen and CH3
t is 0 or 1
RH is halogen
j is 0 or 1
RI, RJ, and RK are not exemplified
RM is hydrogen, halogen
RN is independently hydrogen, halogen, RP-substituted or unsubstituted 3 to 5 heterocycloalkyl, RP-substituted or unsubstituted C6 aryl
RR, RS and RT are not exemplified
RV is not exemplified
RP is hydrogen, halogen, —CN, or unsubstituted C1-6 alkyl
RW, RX and RY are not exemplified.
RE1, RE2, RE3, and RE4 are hydrogen, halogen, or, unsubstituted C1 alkyl
Therefore, the methods/compounds described in the instant specification detail only a limited number of the total substituents claimed (see substituents 1-19, above). All working examples presented in the instant specification are related to the compounds containing a fraction of the total claimed substituents (see substituents 39-57, above).
There are no working examples in the instant specification for the wide range of substituents claimed, but for which evidence of possession has not been provided (see substituents 20-38, above). Thus the instant specification does not provide any evidence that Applicant was in possession of the claimed invention prior to the effective filing of the instant application.
Vas-Cath Inc. 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.) 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).
Finally, University of California v. Eli Lilly and Co., 43 USPQ2d 1398, 1404, 1405 held that: ...To fulfill the written description requirement, a patent specification must describe an invention and do so in sufficient detail that one skilled in the art can clearly conclude that "the inventor invented the claimed invention." Lockwood v. American Airlines, Inc., 107 F. 3d 1565, 1572, 41 USPQ2d 1961, 1966(1997); In re Gosteli, 872 F.2d 1008, 1012,10 USPQ2d 1614, 1618 (Fed Cir. 1989) ("[T]he description must clearly allow persons of ordinary skill in the art to recognize that [the inventor] invented what is claimed.") Thus, an applicant complies with the written description requirement "by describing the invention, with all its claimed limitations, not that which makes it obvious," and by using "such descriptive means as words, structures, figures, diagrams, formulas, etc., that set forth the claimed invention." Lockwood, 107 F.3d at 1572, 41 USPQ2d at 1966.
It is noted that the pharmaceutical art is unpredictable, requiring each embodiment to be individually assessed for physiological activity. For inventions in emerging and unpredictable technologies, or for inventions characterized by factors not reasonably predictable which are known to one of ordinary skill in the art, more evidence is required to show possession. For example, disclosure of only a method of making the invention and the function may not be sufficient to support a product claim other than a product-by-process claim. See, e.g., Fiers v. Revel, 984 F.2d at 1169, 25 USPQ2d at 1605; Amgen, 927 F.2d at 1206, 18 USPQ2d at 1021.
Thus, since Applicant has not described in adequate detail methods to synthesize compounds containing the claimed substituents, or provided evidence that said compounds have been characterized, or that they exist, an ordinary skilled artisan could not completely envisage Applicants’ invention. Moreover, it is clear that the written description requirement has not been met since Applicant has not provided any evidence that Applicant was in possession of the claimed invention prior to the effective filing of the instant application. Thus, claims 1-3, 11, 12, 16, 17, 20, 22, 27, 30, 34, 35, 37, 40, 45, 47, 51, 55, 56, and 63 of the instant application are not supported by the instant specification and thus a rejection under 35 U.S.C. § 112 (a) for failing to comply with the written description requirement is proper.
Allowable Subject Matter
Claim 61 allowed.
The following is a statement of reasons for the indication of allowable subject matter:
PNG
media_image3.png
71
64
media_image3.png
Greyscale
The instant claim is drawn to compounds of a quinazolinyl scaffold. The compounds feature a sulfonamide moiety directly adjacent to a —CH2— group, which is further linked to a moiety, RF, which may be either a substituted alkyl or substituted or unsubstituted aromatic ring.
PNG
media_image4.png
173
515
media_image4.png
Greyscale
Searches of the prior art identified Vacca ‘918 as the closest prior art. Vacca ‘918 teaches a compounds of Formula (I) and pharmaceutical compositions thereof as small molecule inhibitors for the targeting or IRE1 protein family member (claim 1, Abstract). However, the compounds instantly claimed are sufficiently novel, with respect to the simultaneous substitution of either a substituted or unsubstituted aromatic group or substituted alkyl separated by a —CH2— spacer between said terminal group and the sulfonamide connecting the rest of the quinazolinyl moiety. Furthermore, the quinazolinyl moiety is connected to a heterocycle, which is not described by of the prior art at position CyA’ in the prior art by Vacca ‘918. Thus, the prior art reference does not encompass the scope of the instantly claimed compounds, which are novel and nonobvious over the prior art. Furthermore, the prior art of record does not provide a reason rationale for person of ordinary skill in the art to modify these particular structural features from the disclosure of the prior art reference. Vacca ‘918 does not establish why a person of ordinary skill in the art would have been motivated, with a reasonable expectation of success, to modify the prior art compounds in the stated ways, to obtain the specific compounds of claim 61. In view of these numerous distinctions, the claimed subject matter is considered novel and nonobvious over the prior art of record. For at least these reasons, the claim is herein deemed allowable.
Correspondence
Claims 1-3, 11, 12, 16, 17, 20, 22, 27, 30, 34, 35, 37, 40, 45, 47, 51, 55, 56, and 63 are rejected.
Claim 61 is allowed.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to Sophia P Hirakis whose telephone number is +1 (571)272-0118. The examiner can normally be reached within the hours of 5:00 am to 5:00pm EST, Monday through Friday.
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, Adam C. Milligan can be reached on +1 (571) 270-7674. The fax phone number for the organization where this application or proceeding is assigned is +1 (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 +1 (800) 786-9199 (IN USA OR CANADA) or +1 (571) 272-1000.
/SOPHIA P HIRAKIS/Examiner, Art Unit 1623
/KARA R. MCMILLIAN/Primary Examiner, Art Unit 1623
Prosecution Insights