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 .
Status of Claims
Claims 1, 3-8, 11, 13-14, 20, 28, 30, 43, 54-55, 57-61 are pending in the instant application. Claims 2, 9-10, 12, 15-19, 21-27, 29, 31-42, 44-53 and 56 are cancelled and claims 1, 11, 28 and 54 are amended via the amendment filed October 9th, 2025.
Priority
This is a 35 U.S.C. 371 National Stage filing of International Application No. PCT/CN2021/111236 filed August 6th, 2021, which claims priority under 35 U.S.C. 119(a-d) to PCT/CN2020/107800, filed August 7th, 2020. Receipt is acknowledged of papers submitted under 35 U.S.C. 119(a)-(d)
Response to Restriction/Election Requirement
Applicant’s election with traverse of “compound 88” to prosecute the invention of Group I, drawn to a compound, in the reply filed on October 9th, 2025 is acknowledged.
Applicant disagrees with the position that the technical feature does not make a contribution over the prior art in view of WO 2010/075257. Applicant argues that none of the compounds in the prior art possess the feature represented by ring B of Formula (VIII). This is not found persuasive in view of the cited prior art below.
As per MPEP 803.02, the examiner will determine whether the entire scope of the claims is patentable. Applicants' elected species is not allowable. Therefore, according to MPEP 803.02:
Following election, the Markush claim will be examined fully with respect to the elected species and further to the extent necessary to determine patentability.
If the Markush claim is not allowable, the provisional election will be given effect and examination will be limited to the Markush claim and claims to the elected species, with claims drawn to species patentably distinct from the elected species held withdrawn from further consideration.
If on examination the elected species is found to be anticipated or rendered obvious by prior art, the Markush claim and claims to the elected species will be rejected, and claims to the nonelected species will be held withdrawn from further consideration.
As the elected species has been found not allowable, the Markush-type claims have been rejected and claims to the nonelected invention held withdrawn from further consideration. Claims 1, 3-4, 11, 13-14, 20, 28, 43, and 54-55 have been examined to the extent that they are readable on the elected compound 88. Since the elected species is not allowable, subject matter not embraced by the elected embodiment is therefore withdrawn from further consideration.
Claims 5-8, 30 and 57-61 are withdrawn from further consideration by the examiner, 37 CFR 1.142(b), as being drawn to a non-elected invention or species. Election was made with traverse in reply filed October 9th, 2025.
Claim Rejections - 35 USC § 103
In the event the determination of the status of the application as subject to AIA 35 U.S.C. 102 and 103 (or as subject to pre-AIA 35 U.S.C. 102 and 103) is incorrect, any correction of the statutory basis (i.e., changing from AIA to pre-AIA ) for the rejection will not be considered a new ground of rejection if the prior art relied upon, and the rationale supporting the rejection, would be the same under either status.
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.
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.
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.
Claim(s) 1, 3-4, 11, 13-14, 20, 28, 43 and 54-55 is/are rejected under 35 U.S.C. 103 as being unpatentable over Li et al (WO 2020/182384, which claims priority to 62/816,726, filed March 11th, 2019, which is appended to the reference) in view of Ritchie et al (European Journal of Medicinal Chemistry 124 (2016) 1057e1068).
Determining the scope and contents of the prior art. (See MPEP § 2141.01)
The instant application claims the following compound, compound 88, as a compound of instant formula (VIII):
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Li teaches the following compound of formula (Ia), INF011 (page 46, which finds priority in claim 9 of the priority document):
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This compound is nearly embraced by instant formula (VIII), wherein R1 is aryl, substituted with R11, wherein R11 is alkyl substituted with halogen, L1 is -C(O)NH-, R6 is H, L2 is -C(O)-, R3 is aryl substituted with R31, wherein R31 is alkyl and halogen, L3 is a bond, RQ is H and W is a heterocycloalkyl. The only difference between the compound taught by Li, INF011, and instant compound 88 is a benzene ring where compound 88 has a cyclopentane ring.
Ascertainment of the differences between the prior art and the claims. (See MPEP § 2141.02)
The difference between the prior art compound and compound 88 of the instant application is that the prior art compound has a benzene ring where instant compound 88 has a cyclopentane ring.
Finding of prima facie obviousness --- rationale and motivation (See MPEP § 2142-2143)
First, Li teaches that it is preferred that the compounds according to the invention have a IC50 of 100 nM or lower in a Ca2+ mobilization assay. Li teaches that the compound above, INF011, has an IC50 of 100 nM. As Li teaches that compound INF011, is a preferred compound, one of ordinary skill in the art would have been motivated to select this compound as a lead compound to optimize in order to provide the most optimum treatment.
Further, Li teaches compounds of the general formula (Ia) (claim 4, which finds priority in claim 3 of the priority document):
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Li teaches that CYCLE is a saturated or unsaturated mono- or multi-ring carbocycle in which one or more of the ring carbon atoms may be replaced independently from each other by N, S, or O. As such, it should be noted that in the general formula taught by Li, that cycle includes both saturated or unsaturated mono- or multi-ring carbocycle in which one or more of the ring carbon atoms may be replaced independently from each other by N, S, or O. CYCLE being a saturated carbocycle, optionally substituted with N, S, or O, would read on a compound of instant formula (VIII).
Also, Li teaches that this compound is useful in the treatment of a disease or disorder involving pathologic activation of a C5a receptor (claim 14, which finds support in claim 12 of the priority document). This is in the same utility as the instant invention.
Further, Ritchie teaches that benzene and heteroaromatic rings are ubiquitous in drug discovery, with benzene and pyridine being the two most commonly found aromatic systems in marketed drugs. However, too many aromatic rings, particularly carboaromatic rings in a molecule increase the likelihood of encountering poor ADME profiles, due to suboptimal physicochemical properties (page 1057, left column, paragraph 1). Ritchie further teaches that an alternative approach is to replace a benzene ring with a cycloalkyl or a heterocycle (page 1057, left column, paragraph 1). Further, Ritchie teaches that cyclopentane has the same ADMET properties as benzene (page 1060, left column, paragraph 1). Ritchie also teaches that cyclopentane, and other cycloalkyl rings, exhibit ADME profiles very similar to benzene, are popular replacements (page 1066, left column, paragraph 2). Ritchie then teaches that cycloalkanes, in reality, make little difference to ADME profiles when used as benzene replacements and can be considered more as isosteres (Page 1066, right column, paragraph 4).
Thus, regarding claim 1, one of ordinary skill in the art would have chosen the compound INF011 of Li, as Li teaches it as a preferable compound and would be motivated to replace the benzene ring with cyclopentane, as Li teaches that the compound has the same utility as the instant invention, that a cyclopentane would fit within the general formula of Li and Ritchie teaches that cyclopentene and benzene have very similar properties and can be considered more as isosteres.
Regarding claims 3-4, as seen in the argument above, one of ordinary skill in the art would have been motivated to replace the benzene ring in the compound of Li with cyclopentyl.
Regarding claim 11, as seen above, the compound of Li has R6 as H.
Regarding claim 13-14, as seen above, in the compound taught by Li, R1 is phenyl.
Regarding claim 20, R1 is
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Regarding claim 28, RQ is H.
Regarding claim 43, R3 is
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Regarding claim 54, the compound above has rendered compound 88 of the instant application obvious.
Regarding claim 55, teaches that the compound is in a pharmaceutical composition with a pharmaceutically acceptable carrier (claim 12).
Correspondence
Any inquiry concerning this communication or earlier communications from the examiner should be directed to Anna Grace Kuckla whose telephone number is (703)756-5610. The examiner can normally be reached Monday-Friday 7:30-5.
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/A.G.K./Examiner, Art Unit 1626
/FEREYDOUN G SAJJADI/Supervisory Patent Examiner, Art Unit 1699