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 .
DETAILED ACTION
Election/Restrictions
Priority
The Information Disclosure Statement filed on INSERT DATE is in compliance with the provisions of 37 CFR 1.97 and has been considered in full. A signed copy of references cited from the IDS is included with this Office Action.
Information Disclosure Statement
The Information Disclosure Statements filed on March 20th 2024 and December 22nd 2025 are in compliance with the provisions of 37 CFR 1.97 and have been considered in full. A signed copy of references cited from the IDS is included with this Office Action.
Claim Rejections - 35 USC § 112
Prodrug
Isomer
FGFR2 mediated disorder
Claim Rejections - 35 USC § 102
1, 4, 10, 14, 20, 21, 26, 29, 30, 33, 35, 37, 41-43, 45 77, 79, 81, and 83-85
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.
Claims 1, 4, 10, 14, 20, 21, 26, 29, 30, 33, 35, 37, 41-43, 45, 48, 51, 57, 59, 62, 67, 69, 75, 77, 79, 81, and 83-85 are rejected under 35 U.S.C. 103 as being unpatentable over Toure (WO 2020/231990 A1 published on November 19th 2020) in view of Brown (Brown, Bioisosteres in Medicinal Chemistry, 2012) and
The application is directed towards compounds with fibroblast growth factor receptor (FGFR) inhibition activity. In particular, compounds of the genus,
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One such compound is applicant’s elected species of
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which is encompassed by claims 1, 4, 10, 14, 20, 21, 26, 29, 30, 33, 35, 37, 41-43, 45, 48, 51, 57, 59, 62, 67, 69, and 75.
Toure teaches the similar FGFR inhibiting compound,
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(Toure, pg. 683).
Toure’s compound differs from applicant’s elected species in only 2 locations:
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That is, applicant’s compound differs from Toure’s compound only in:
The replacement of a fluorine with hydrogen
The replacement of a hydrogen with a nitrile group
One of ordinary skill in the art would have had a reasonable expectation of success in performing each of these replacements, because each of these replacements are well-known in the art of drug discovery to yield predictable results.
Regarding the replacement of a fluorine with a hydrogen, the H⇐⇒F replacement is known as a “classical bioisosteric replacement,” and is one of the most common replacements performed in the field of drug discovery (Brown, pg. 7). Similarly, CN is commonly treated as a pseudohalogen and is considered a common bioisostere of fluorine (Brown, pg. 6, pg. 23). The replacement of the hydrogen with the CN (H⇐⇒F⇐⇒CN) would thereby be considered well within the toolkit of routine experimentation.
See MPEP § 2144.08(II)(A)(4)(c):
“Concepts used to analyze the structural similarity of chemical compounds in other types of chemical cases are equally useful in analyzing genus-species cases. For example, a claimed tetra-orthoester fuel composition was held to be obvious in light of a prior art tri-orthoester fuel composition based on their structural and chemical similarity and similar use as fuel additives. Dillon, 919 F.2d at 692-93, 16 USPQ2d at 1900-02. Likewise, claims to amitriptyline used as an antidepressant were held obvious in light of the structural similarity to imipramine, a known antidepressant prior art compound, where both compounds were tricyclic dibenzo compounds and differed structurally only in the replacement of the unsaturated carbon atom in the center ring of amitriptyline with a nitrogen atom in imipramine. In re Merck & Co., 800 F.2d 1091, 1096-97, 231 USPQ 375, 378-79 (Fed. Cir. 1986). Other structural similarities have been found to support a prima facie case of obviousness. See, e.g., In re May, 574 F.2d 1082, 1093-95, 197 USPQ 601, 610-11 (CCPA 1978) (stereoisomers); In re Wilder, 563 F.2d 457, 460, 195 USPQ 426, 429 (CCPA 1977) (adjacent homologs and structural isomers); In re Hoch, 428 F.2d 1341, 1344, 166 USPQ 406, 409 (CCPA 1970) (acid and ethyl ester); In re Druey, 319 F.2d 237, 240, 138 USPQ 39, 41 (CCPA 1963) (omission of methyl group from pyrazole ring). Generally, some teaching of a structural similarity will be necessary to suggest selection of the claimed species or subgenus. Id.”
See MPEP § 2144.08(II)(A)(4)(d):
“If the claimed invention and the structurally similar prior art species share any useful property, that will generally be sufficient to motivate an artisan of ordinary skill to make the claimed species, e.g., id. For example, based on a finding that a tri-orthoester and a tetra-orthoester behave similarly in certain chemical reactions, it has been held that one of ordinary skill in the relevant art would have been motivated to select either structure. 919 F.2d at 692, 16 USPQ2d at 1900-01. In fact, similar properties may normally be presumed when compounds are very close in structure. Dillon, 919 F.2d at 693, 696, 16 USPQ2d at 1901, 1904. See also In re Grabiak, 769 F.2d 729, 731, 226 USPQ 870, 871 (Fed. Cir. 1985) ("When chemical compounds have ‘very close’ structural similarities and similar utilities, without more a prima facie case may be made."). Thus, evidence of similar properties or evidence of any useful properties disclosed in the prior art that would be expected to be shared by the claimed invention weighs in favor of a conclusion that the claimed invention would have been obvious. Dillon, 919 F.2d at 697-98, 16 USPQ2d at 1905; In re Wilder, 563 F.2d 457, 461, 195 USPQ 426, 430 (CCPA 1977); In re Lintner, 458 F.2d 1013, 1016, 173 USPQ 560, 562 (CCPA 1972).”
One of ordinary skill in the art would thereby have had a reasonable expectation of success in developing applicant’s FGFR inhibitor from Toure’s FGFR inhibitor, and claims 1, 4, 10, 14, 20, 21, 26, 29, 30, 33, 35, 37, 41-43, 45, 48, 51, 57, 59, 62, 67, 69, and 75 are prima facie obvious.
Claim 77 is directed to a pharmaceutical composition comprising a compound of claim 75 and a carrier. Toure teaches pharmaceutical compositions comprising Toure’s FGFR inhibitor and a carrier (Toure, claim 12). Claim 77 is thereby prima facie obvious.
Claim 79 is directed towards a method of inhibiting FGFR2 signaling activity in a subject via administration of a compound of claim 75. Toure teaches a method of inhibiting FGFR2 signaling activity in a subject (Toure, claim 13), rendering claim 79 prima facie obvious.
Claim 81 is directed towards a method of treating an FGFR2-mediated disorder in a subject via administration of a compound of claim 75. Toure teaches the treatment of FGFR2-mediated disorders (Toure, claim 14), and claim 81 is prima facie obvious.
Claims 83-85 are directed towards the treatment of intrahepatic cholangiocarcinoma via administration of a compound of claim 75. Toure teaches treatment of intrahepatic
cholangiocarcinoma (Toure, claim 17), and claims 83-85 are prima facie obvious.
Double Patenting
Double Patenting
Conclusion
Any inquiry concerning this communication or earlier communications from the examiner should be directed to Anthony Seitz whose telephone number is (703)756-4657. The examiner can normally be reached 7:30 AM ET - 5:00 PM ET M-F.
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/ANTHONY JOSEPH SEITZ/Examiner, Art Unit 1629
Prosecution Insights