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/Restriction
Applicant’s election without traverse of Group I (claims 1 – 11, and 13 – 14) drawn to a compound represented by general formula (I-1)
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wherein X1-4, R, Rb, Ring B, R5-6, and y are defined and the species election of (S)-1-(3-(7-acetyl-4-amino-3-(pyrazolo[1,5-a ]pyridine-6-ethynylene )-1H-pyrazolo[4,3-c]pyridine-1-yl)pyrrolidine-1-methyl)prop-2-en-1-one,
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in the reply filed on August 24th, 2026 is acknowledged.
Claims 16 – 18 are withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a nonelected Group II (a method for treating and/or preventing cancer, achondroplasia, and other related diseases), there being no allowable generic or linking claim. Moreover claim 13 is withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to nonelected compound species where R is a 5-membered heterocyclo substituted with an amino protective group. Election was made without traverse in the reply filed on August 24th, 2026.
However, upon the initial search of the elected species, the elected species of (S)-1-(3-(7-acetyl-4-amino-3-(pyrazolo[1,5-a ]pyridine-6-ethynylene )-1H-pyrazolo[4,3-c]pyridine-1-yl)pyrrolidine-1-methyl)prop-2-en-1-one, that is,
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was found to be free of the prior art. Consequently, the search was expanded to include chemical species of general formula (I-1) where X2 = CR4 where R4 = H; ring B =
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; and R6 = NH2. Nevertheless, outside of the above delineated chemical species; the election of species required in the Restriction Requirement mailed June 24th, 2026 is maintained. Moreover, the restriction between Groups I and Group II is maintained in the Restriction Requirement mailed June 24th, 2026 is maintained.
Hence claims 1 – 11, and 14 are being examined on the merits.
Claim Rejections - 35 USC § 112
The following is a quotation of 35 U.S.C. 112(b):
(b) CONCLUSION.—The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the inventor or a joint inventor regards as the invention.
The following is a quotation of 35 U.S.C. 112 (pre-AIA ), second paragraph:
The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the applicant regards as his invention.
Claims 1 – 11, and 14 are rejected under 35 U.S.C. 112(b) or 35 U.S.C. 112 (pre-AIA ), second paragraph, as being indefinite for failing to particularly point out and distinctly claim the subject matter which the inventor or a joint inventor (or for applications subject to pre-AIA 35 U.S.C. 112, the applicant), regards as the invention.
Regarding claim 1, the phrase "preferably" renders the claim indefinite because it is unclear whether the limitation(s) following the phrase are part of the claimed invention. See MPEP § 2173.05(d). As a consequence, one of ordinary skill in the art would not be reasonably apprised of the scope of the invention. Specifically one of ordinary skill in the art would not be reasonably apprised of where the limitation after the “preferably,” is required or not. Therefore, given the uncertainty around the “preferably” throughout claim 1; claim 1 is rejected under 35 U.S.C. 112(b). Moreover, claims 2 – 11, and 14 are included in the rejection since the claims are dependent from claim 1 but do not address the deficiency.
Regarding claim 2, the phrase "preferably" renders the claim indefinite because it is unclear whether the limitation(s) following the phrase are part of the claimed invention. See MPEP § 2173.05(d). As a consequence, one of ordinary skill in the art would not be reasonably apprised of the scope of the invention. Specifically one of ordinary skill in the art would not be reasonably apprised of where the limitation after the “preferably,” is required or not. Therefore, given the uncertainty around the “preferably” throughout claim 2; claim 2 is rejected under 35 U.S.C. 112(b).
Regarding claim 3, the phrase "preferably" renders the claim indefinite because it is unclear whether the limitation(s) following the phrase are part of the claimed invention. See MPEP § 2173.05(d). As a consequence, one of ordinary skill in the art would not be reasonably apprised of the scope of the invention. Specifically one of ordinary skill in the art would not be reasonably apprised of where the limitation after the “preferably,” is required or not. Therefore, given the uncertainty around the “preferably” throughout claim 3; claim 3 is rejected under 35 U.S.C. 112(b).
Regarding claim 4, the phrase "preferably" renders the claim indefinite because it is unclear whether the limitation(s) following the phrase are part of the claimed invention. See MPEP § 2173.05(d). As a consequence, one of ordinary skill in the art would not be reasonably apprised of the scope of the invention. Specifically one of ordinary skill in the art would not be reasonably apprised of where the limitation after the “preferably,” is required or not. Therefore, given the uncertainty around the “preferably” throughout claim 4; claim 4 is rejected under 35 U.S.C. 112(b). Moreover, claim 9 is included in the rejection since the claim depends from claim 4 but does not address the deficiency.
Moreover, claim 4 recites the limitation "L1" in the structure of general formula (I-2); however, “L1” is not mentioned in independent claim 1 which dependent claim 4 depends. There is insufficient antecedent basis for this limitation in the claim. Moreover, claim 9 is included in the rejection since the claim depends from claim 4 but does not address the deficiency.
Regarding claim 5, the phrase "preferably" renders the claim indefinite because it is unclear whether the limitation(s) following the phrase are part of the claimed invention. See MPEP § 2173.05(d). As a consequence, one of ordinary skill in the art would not be reasonably apprised of the scope of the invention. Specifically one of ordinary skill in the art would not be reasonably apprised of where the limitation after the “preferably,” is required or not. Therefore, given the uncertainty around the “preferably” throughout claim 5; claim 5 is rejected under 35 U.S.C. 112(b).
Regarding claim 6, the phrase "preferably" renders the claim indefinite because it is unclear whether the limitation(s) following the phrase are part of the claimed invention. See MPEP § 2173.05(d). As a consequence, one of ordinary skill in the art would not be reasonably apprised of the scope of the invention. Specifically one of ordinary skill in the art would not be reasonably apprised of where the limitation after the “preferably,” is required or not. Therefore, given the uncertainty around the “preferably” throughout claim 6; claim 6 is rejected under 35 U.S.C. 112(b).
Regarding claim 7, the phrase "preferably" renders the claim indefinite because it is unclear whether the limitation(s) following the phrase are part of the claimed invention. See MPEP § 2173.05(d). As a consequence, one of ordinary skill in the art would not be reasonably apprised of the scope of the invention. Specifically one of ordinary skill in the art would not be reasonably apprised of where the limitation after the “preferably,” is required or not. Therefore, given the uncertainty around the “preferably” throughout claim 7; claim 7 is rejected under 35 U.S.C. 112(b).
Regarding claim 8, the phrase "preferably" renders the claim indefinite because it is unclear whether the limitation(s) following the phrase are part of the claimed invention. See MPEP § 2173.05(d). As a consequence, one of ordinary skill in the art would not be reasonably apprised of the scope of the invention. Specifically one of ordinary skill in the art would not be reasonably apprised of where the limitation after the “preferably,” is required or not. Therefore, given the uncertainty around the “preferably” throughout claim 8; claim 8 is rejected under 35 U.S.C. 112(b).
Regarding claim 9, the phrase "preferably" renders the claim indefinite because it is unclear whether the limitation(s) following the phrase are part of the claimed invention. See MPEP § 2173.05(d). As a consequence, one of ordinary skill in the art would not be reasonably apprised of the scope of the invention. Specifically one of ordinary skill in the art would not be reasonably apprised of where the limitation after the “preferably,” is required or not. Therefore, given the uncertainty around the “preferably” throughout claim 9; claim 9 is rejected under 35 U.S.C. 112(b).
Regarding claim 10, the phrase "preferably" renders the claim indefinite because it is unclear whether the limitation(s) following the phrase are part of the claimed invention. See MPEP § 2173.05(d). As a consequence, one of ordinary skill in the art would not be reasonably apprised of the scope of the invention. Specifically one of ordinary skill in the art would not be reasonably apprised of where the limitation after the “preferably,” is required or not. Therefore, given the uncertainty around the “preferably” throughout claim 10; claim 10 is rejected under 35 U.S.C. 112(b).
Claim Rejections - 35 USC § 112
The following is a quotation of 35 U.S.C. 112(d):
(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.
The following is a quotation of pre-AIA 35 U.S.C. 112, fourth paragraph:
Subject to the following paragraph [i.e., the fifth paragraph of pre-AIA 35 U.S.C. 112], 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.
Claims 4 and 9 are rejected under 35 U.S.C. 112(d) or pre-AIA 35 U.S.C. 112, 4th paragraph, 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. Claim 4 is drawn to the compound of according to claim 1 wherein the compound is further as represented by general formula (I-2):
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where L is selected from a list of structural features including a bond, C1-3 alkylene, C3-8 cycloalkylene, etc. See claim 4 limitation. However, independent claim 1 , from which claim 4 depends, directs to a compound represented by general formula (I-1) of structure
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where L can only be an acyclic triple bond. Thus claim 4 fails to further limit what L can be based on independent claim 1, and instead expands what L can be outside of what independent claim 1 recites. Moreover, claim 9 is included in the rejection since the claim depends from claim 4 but does not address the deficiency. Applicant may cancel the claim(s), amend the claim(s) to place the claim(s) in proper dependent form, rewrite the claim(s) in independent form, or present a sufficient showing that the dependent claim(s) complies with the statutory requirements.
Claim Rejections - 35 USC § 102
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 the appropriate paragraphs of 35 U.S.C. 102 that form the basis for the rejections under this section made in this Office action:
A person shall be entitled to a patent unless –
(a)(1) the claimed invention was patented, described in a printed publication, or in public use, on sale, or otherwise available to the public before the effective filing date of the claimed invention.
(a)(2) the claimed invention was described in a patent issued under section 151, or in an application for patent published or deemed published under section 122(b), in which the patent or application, as the case may be, names another inventor and was effectively filed before the effective filing date of the claimed invention.
Claims 1 – 10, and 14 are rejected under 35 U.S.C. 102(a)(1) and 35 U.S.C. 102(a)(2) as being anticipated by International Publication Number WO 2021/247971 A1 to Kaldor et. al. (Kaldor’971; cited on the ISR form).
Regarding claims 1 – 10, and 14, Kaldor’971 teach inhibitors of fibroblast growth factor receptor (FGFR) kinases, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases. See page 1 paragraph 0003. In particular, Kaldor’971 teach an embodiment where the compound has the structure of Formula (I):
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See page 1 paragraph 0004. Specifically, Kaldor’971 teach species compound 156 of structure
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where examined X1 = N; examined X2 = CR4 where R4 = H; examined X3 = N; examined X4 = C; R5 = H; R6 = NH2; ring B =
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where y = 3 and where one Rb = CH3, and two Rb = F; and R =
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substituted with 1 R’ where one R’ = -C(O)CH=CH2 and n = 0. See page 78 Table 1 Example 156. See claim 1 limitation for a compound represented by general formula (I-1)
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where X1 = N; X2 = CR4 where R4 = H; X3 = N; X4 = C; R5 = H; R6 = NH2; ring B = 9 membered heteroaryl; y = 3; two Rb = halogen and one Rb = C1 alkyl; R = 5 membered heterocyclyl substituted with R’ where R’ = -C(O)CRa=CRb(CH2)nRc where n = 0, Ra = Rb = Rc = H. See claim 2 limitation for the compound according to claim 1 represented by general formula (II-1)
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where X1 = N; X2 = CR4 where R4 = H; X3 = N; X4 = C; R5 = H; R6 = NH2; ring B = 9 membered heteroaryl; y = 3; two Rb = halogen and one Rb = C1 alkyl; R = heterocyclyl further substituted. See claim3 limitation for the compound according to claim 1 where R = 5 membered heterocyclyl substituted with R’ where R’ = -C(O)CRa=CRb(CH2)nRc where n = 0, Ra = Rb = Rc = H. See claim 4 limitation for the compound according to claim 1 wherein the compound is further as represented by general formula (I-2)
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where X1 = N; X2 = CR4 where R4 = H; X3 = N; X4 = C; L1 = C2 alkynylene; R5 = H; R6 = NH2; t = 1; R7 = H where p = 3; ring B = 9 membered heteroaryl; y = 3; two Rb = halogen and one Rb = C1 alkyl; R’ = 5 membered heterocyclyl substituted with R’ where R’ = -C(O)CRa=CRb(CH2)nRc where n = 0, Ra = Rb = Rc = H. See claim 5 limitation for the compound according to claim 1 wherein the compound is further as represented by general formula (IV)
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where X1 = N; X2 = CR4 where R4 = H; L1 = C2 alkynylene; R5 = H; R6 = NH2; t = 1; ring B = 9 membered heteroaryl; y = 3; two Rb = halogen and one Rb = C1 alkyl; R’ = 5 membered heterocyclyl substituted with R’ where R’ = -C(O)CRa=CRb(CH2)nRc where n = 0, Ra = Rb = Rc = H. See claim 6 limitation for the compound according to claim 1 where ring B = 9 membered bicyclic heteroaryl. See claim 7 limitation for a compound according to claim 1 where R4 = H; R5 = H; and R6 = NH2. See claim 8 limitation for the compound according to claim 1 where the R is
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R’ = 5 membered heterocyclyl substituted with R’ where R’ = -C(O)CRa=CRb(CH2)nRc where n = 0, Ra = Rb = Rc = H; t = 1; R7 = H where p = 3. See claim 9 limitation for the compound according to claim 4 where the compound is further as represented by general formula (II-3)
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where R4 = H; t = 1; R7 = H where p = 3; ring C = phenyl; ring D = 5 membered heteroaryl; y = 3; two Rb = halogen and one Rb = C1 alkyl. See claim 10 limitation for the compound according to claim 1 where the compound is further as represented by general formula (VII-1)
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where R4 = H; t = 1; R7 = H where p = 3; ring C = phenyl; ring D = 5 membered heteroaryl; Rk = H; Rj = C1 alkyl; Rn = H; and Rl = Rm = halogen.
Additionally, Kaldor’971 teach that compounds of the disclosure, which include compound 156, are FGFR inhibitors. See page 19 paragraph 0071. Moreover, Kaldor’971 teach that compounds of the disclosure, which include compound 156, as useful in methods of treating cancer or neoplastic disease. See page 97 paragraph 00105. Furthermore, Kaldor’971 teach that compounds of the disclosure, which include compound 156, can combine with a pharmaceutically suitable or acceptable carrier or excipient. See page 95 paragraph 0090. See claim 14 limitation for a pharmaceutical composition comprising a therapeutically effective dose of the compound or the stereoisomer or pharmaceutically acceptable salt thereof according to claim 1, and one or more pharmaceutically acceptable carriers or excipients.
Claim Rejections - 35 USC § 103
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.
Claim 11 is rejected under 35 U.S.C. 103 as being unpatentable International Publication Number WO 2021/247971 A1 to Kaldor et. al. (Kaldor’971; cited on the ISR form) in view of Meanwell ((2011), Synopsis of Some Recent Tactical Application of Bioisosteres in Drug Design, J. Med. Chem., 54, 2529 – 2591).
The teachings of Kaldor’971 as they relate to claim 1, from which claim 11 depends, are given previously in this office action and are fully incorporated here.
However, Kaldor’971 fails to teach a compound of structure
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. See claim 11 limitation.
Nevertheless, Meanwell teach that in the contemporary practice of medicinal chemistry, the development and application of bioisosteres have been adopted as a fundamental tactical approach useful to address a number of aspects associated with the design and development of drug candidates. See page 2529 column 1 paragraph 1. Additionally, Meanwell teach that bioisosteres are typically less than exact structural mimetics and are often more alike in biological rather than physical properties. See page 2529 column 1 paragraph 1. Moreover, Meanwell teach that H, F, and CH3 are classical monovalent bioisosteres. See page 2530 column 1 Table 1. Thus Meanwell suggest the ability to substitute or interchange F, CH3, and H with a reasonable expectation that compounds with either F, H, or CH3 would have similar biological properties.
Therefore, it would have been obvious to one of ordinary skill in the art before the effective filling date of the instant application to modify compound 156 of Kaldor’971 in view of Meanwell, that is to substitute one of the F for a H and substitute one of the H for a CH3 group. One of ordinary skill in the art would be motivated to make this modification and have a reasonable expectation of success because H, F and CH3 are classical monovalent bioisosteres and would be reasonable expected to at least have the same biological properties.
Conclusion
Claims 1 – 11, and 14 are rejected.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to DAWANNA S WHITE whose telephone number is (703)756-4687. The examiner can normally be reached 7:00 am - 5:00 pm [EST] M - Th.
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/DAWANNA SHAR-DAY WHITE/Examiner, Art Unit 1627
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