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 the Claims
Claims 1-8 are pending in the instant application and subject to examination herein.
Priority
Acknowledgment is made of applicant’s claim for foreign priority under 35 U.S.C. 119 (a)-(d). The certified copy has been filed in parent Application No. PCT/CN2021/141768, filed on 12/27/2021.
Information Disclosure Statement
The information disclosure statement (IDS) submitted on 07/18/2023 is in compliance with the provisions of 37 CFR 1.97. Accordingly, the information disclosure statement is being considered by the examiner.
Claim Objections
Claims 1-4 are objected to because of the following informalities: The following terms are found misspelled in claims 1-4:
“cycloalkyl” is misspelled “cyclylalkyl” and/or “cycloaklyl” and/or “cyclylakyl”;
“heterocycloalkyl” is misspelled as “heterocyclylalkyl” and/or “hetrocyclylalkyl”;
“heteropolycyclyl” is misspelled as “hetreopolycyclyl”;
“heterocyclic” is misspelled as “heterocycly”.
Appropriate correction is required.
Claim Rejections - 35 USC § 112(b)
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 1-8 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.
Where applicant acts as his or her own lexicographer to specifically define a term of a claim contrary to its ordinary meaning, the written description must clearly redefine the claim term and set forth the uncommon definition so as to put one reasonably skilled in the art on notice that the applicant intended to so redefine that claim term. Process Control Corp. v. HydReclaim Corp., 190 F.3d 1350, 1357, 52 USPQ2d 1029, 1033 (Fed. Cir. 1999). The term “alkyl” in claims 1-4 is used by the claim to mean “an alkyl group having 0-4 carbons,” in the term “-C0-4 alkyl-” that is used to define the structural element “U”. While the accepted meaning of “alkyl” is “an alkane that is missing a hydrogen” – see, for example, Wikipedia1. An “alkyl” group composed of zero carbons cannot be an “alkane missing a hydrogen”. The term is indefinite because the specification does not clearly redefine the term “alkyl” to explain how an alkyl group can be composed of zero carbons. The claims are ambiguous because a person of ordinary skill in the art would not understand what is meant by the inclusion of an element that is an alkyl group composed of zero carbons.
Claims 5-8 depend from claims 1-4 directly or indirectly and do not resolve the indefiniteness of claims 1-4.
Claims 1-8 are rejected under 35 U.S.C. 112(b) or 35 U.S.C. 112 (pre-AIA ), second paragraph, as being incomplete for omitting essential structural cooperative relationships of elements, such omission amounting to a gap between the necessary structural connections. See MPEP § 2172.01. The omitted structural cooperative relationships are the following:
Claim 1 describes the linkage “L” between Rings “Ar” and B as having structure selected from a Markush group that includes “bonds”, which a person of ordinary skill in the art would understand, but would not be able to distinguish as meaning that the plurality of “bonds” refers to “L” being a single bond across different possible permutations (structures) of the compounds of Formula (I), or that the structure requires that “L” consist of multiple single bonds (i.e., a ring fusion) or as a double bond or as a triple bond between atoms of Ring “Ar” and B;
Claim 1 limits Ring B to a benzyl group or a 5-10 membered heteroaryl, and simultaneously limits Ring “Ar” to a 6-10 heteroaromatic ring, and claim 1 further states that “the benzyl ring and heteroaromatic ring described above are optionally substituted with one or more R1” but does not clarify how the limitation involving “the heteroaromatic ring” applies if both Rings B and “Ar” are heteroaromatic rings;
Claim 1 limits the element “Z” to a Markush group of structures, including the following structures that include a bond “a” and groups Ra-Rc:
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278
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70
88
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;
Claim 1 further limits bond “a” to being either a double or a triple bond, and limits groups Ra-Rc to a Markush group of available atoms/groups while not permitting the absence of any of groups Ra-Rc ;
A person of ordinary skill in the art would not understand how bond “a” could be a triple bond while the structure simultaneously includes groups Ra-Rc, because the carbon atoms of which bond “a” is composed would require 5 covalent bonds under such a circumstance;
Claim 2 further limits claim 1 to a narrower genus of compounds described by the formula (IIa) as shown below, and describes the limitations of formula IIa in regard to a structural element “U” without describing how the element “U” fits into the structure of formula (IIa):
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;
For purpose of examination, the element “A” in the structural image of formula (IIa) will be treated as equivalent to the element “U” defined in claim 2.
Claims 2-8 depend from claim 1 and do not resolve the ambiguity in structural relationships of claim 1. Claims 5-8 depend from claim 2 and do not resolve the ambiguity in structural relationships of claim 2.
Claims 1-8 are rejected under 35 U.S.C. 112(b) or 35 U.S.C. 112 (pre-AIA ), second paragraph, as being incomplete for omitting an essential element, such omission amounting to a gap between the elements. See MPEP § 2172.01. The omitted element is “R2”. Claim 1 describes group “R2” as a group found attached to some of the available (optional) embodiments of group “R1”, including “-OR2”, “-NR2R3” and “-C(O)NR2R3”; however, claim 1 does not provide any definition of the limits of group “R2”. Claims 2-8 depend from claim 1 and do not resolve the ambiguity of the undefined group “R2”.
Claim 5 is indefinite because the category of invention being claimed is ambiguous: the claim purports to limit claims 1-4, drawn to genera of compounds, to a Markush group of specific compounds, while at the same time claiming the “Preparation of ” a specific compound indicated as compound 22. Thus, it is not clear whether the claim is drawn to a composition of matter or a method of preparing compound 2; further, if the invention of claim 5 is intended as a method, the method is unclear as no step(s) have been provided in the claim. Claims 6-8 depend from claim 5 and do not resolve the ambiguity of the category of invention of claim 5.
Claim Rejections - 35 USC § 101
35 U.S.C. 101 reads as follows:
Whoever invents or discovers any new and useful process, machine, manufacture, or composition of matter, or any new and useful improvement thereof, may obtain a patent therefor, subject to the conditions and requirements of this title.
Claims 7 and 8 are rejected under 35 U.S.C. 101 because the claimed invention is directed to non-statutory subject matter. The claims do not fall within at least one of the four categories of patent eligible subject matter because the claims are “use” claims that do not recite any method, machine, manufacture, or composition of matter as the claimed invention, but rather are directed to the "use" of a compound of claim 1 in the preparation of drugs for the treatment of FGFR-mediated diseases.
Claim Rejections - 35 USC § 112(d)
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.
Claim 5 is 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 5 further limits the genera of compounds of claims 1-4 to a Markush group of specific compounds; however, many of the compounds named in claim 5 do not conform to any of the structural formulae of claims 1-4:
Claim 1 requires Ring B of formula (I) to be “a benzyl or a 5-10 membered heteroaryl”;
A benzyl group is defined as “a monovalent radical C6H5CH2- derived from toluene”; see, for example, the online Merriam-Webster dictionary3;
Compounds corresponding to numbers 1-35 include a phenyl ring as Ring B, rather than any benzyl or 5-10 membered heteroaryl; see, for example, compound 14, which has a dimethoxyphenyl ring as Ring B:
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Applicant may cancel the claim, amend the claim(s) to place the claim in proper dependent form, rewrite the claim in independent form, or present a sufficient showing that the dependent claim complies with the statutory requirements.
Claim Rejections - 35 USC § 102
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.
Claim 1 is anticipated by CAS 954869-14-8.
Claim 1 is rejected under 35 U.S.C. 102(a)(1) as being anticipated by CAS 954869-14-8 (Chemical Abstracts Service, registry number 954869-14-8, originally entered on 19Nov2007 by Ambinter).
Claim 1 is drawn to a genus of compounds, designated as Formula (I), composed of two ring systems (“B” and “Ar”) bridged by an optional linker “L” and a pendant chain of groups “U”, “Y” and “Z” as shown below:
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(general formula (I) from claim 1).
CAS 954869-14-8 discloses a compound5 that anticipates general formula (I) as shown in the table below:
Claim Number(s) of Instant Application
Instant Application
CAS 954869-14-8
1
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170
130
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wherein:
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146
284
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Thus, claim 1 is anticipated by the disclosure of CAS 954869-14-8.
Claims 1-2 are anticipated by CAS 1153183-98-2.
Claims 1-2 are rejected under 35 U.S.C. 102(a)(1) as being anticipated by CAS 1153183-98-2 (Chemical Abstracts Service, registry number 1153183-98-2, originally entered on 07Jun2009 by UkrOrgSynthesis).
The limitations of claim 1 are discussed in the rejection above and hereby incorporated into the instant application.
Claim 2 further limits the genus of compounds of claim 1 to a narrower genus, designated as formula (IIa), wherein Ring “Ar” must be a six-membered heteroaryl ring wherein any of ring atoms X1-X5 may be nitrogen and at least one of these X1-X5 ring atoms is nitrogen, as shown in the table below. As discussed above (see 112(b) section), for purpose of examination, the element “A” shown in the structural image of formula (IIa) will be taken as equivalent to the element “U” defined in claim 2.
CAS 1153183-98-2 describes a compound6 that anticipates the genus of formula (IIa), as shown in the table below:
Claim Number(s) of Instant Application
Instant Application
CAS 1153183-98-2
1
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188
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wherein:
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Thus, claims 1 and 2 are anticipated by the disclosure of CAS 1153183-98-2.
Claims 1, 4 and 6-8 are anticipated by Jiang.
Claims 1, 4 and 6-8 are rejected under 35 U.S.C. 102(a)(1) and 102(a)(2) as being anticipated by Jiang (WO 2017/202343 A1)7.
The limitations of claim 1 are discussed in the rejection above and hereby incorporated into the instant rejection.
Claim 4 further limits claim 1 to a narrower genus of compounds, designated as formula IIg, wherein both Ring B and Ring “Ar” are heteroaryl rings of specific size ranges and are directly bonded to each other, as shown in the table below. Jiang discloses a series of compounds as inhibitors of FGFR kinase, including multiple compounds that anticipate the genus of formula IIg, including Jiang’s compound A388 shown in the table below (page 12):
Claim Number(s) of Instant Application
Instant Application
Jiang
1
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140
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wherein:
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Thus, claims 1 and 4 are anticipated by the disclosure of Jiang.
Claim 6 further limits claim 1 to a pharmaceutical composition comprising a compound of instant formula (I), or a prodrug, stable isotope derivative or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
Claim 7 further limits claim 1 to the use of a compound of instant formula (I) in the preparation of drugs for the treatment of FGFR-mediated diseases. Claim 8 further limits claim 7 to a Markush group of specific FGFR-mediated diseases that includes non-small cell lung cancer.
Jiang discloses that compounds of the invention disclosed therein, as FGFR inhibitors, are suitable for treating various diseases related to FGFR enzyme activity, FGFR ligand abnormal expression or activity, including non-small cell lung cancer (page 21, lines 30-349).
Thus, claims 6-8 are anticipated by the disclosure of Jiang.
Conclusion
Any inquiry concerning this communication or earlier communications from the examiner should be directed to W. JUSTIN YOUNGBLOOD whose telephone number is (703)756-5979. The examiner can normally be reached on Monday-Thursday from 8am to 5pm. The examiner can also be reached on alternate Fridays.
If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Jeffrey S. Lundgren, can be reached at telephone number (571) 272-5541. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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Examiner interviews are available via a variety of formats. See MPEP § 713.01. To schedule an interview, applicant is encouraged to use the USPTO Automated Interview Request (AIR) Form at https://www.uspto.gov/InterviewPractice.
/W.J.Y./Examiner, Art Unit 1629
/JEFFREY S LUNDGREN/Supervisory Patent Examiner, Art Unit 1629
1 https://en.wikipedia.org/wiki/Alkyl_group
2 (S)-1-(3-((5-bromo-4-((3,5-dimethoxyphenyl)ethynyl)pyrimidin-2-yl)amino)pyrrolidin-1-yl)prop-2-en-1-one
3 https://www.merriam-webster.com/dictionary/benzyl
4 (S)-1-(3-((4-((3,5-dimethoxyphenyl)ethynyl)pyrimidin-2-yl)amino)pyrrolidin-1-yl)prop-2-en-1-one
5 N-[2-[1-(Phenylmethyl)-1H-benzimidazol-2-yl]ethyl]-2-butenamide
6 N-[6-(1H-Pyrazol-1-yl)-3-pyridinyl]-2-propenamide
7 Cited in Applicants Information Disclosure Statement dated 07/18/2023.
8 4-amino-3-(3,5-dimethyl-1-benzofuran-2-yl)-2-{[1-(prop-2-enoyl)piperidin-4-yl]methyl}-2H,6H,7H-pyrazolo[3,4-d]pyridazin-7-one
9 See paragraph [0158] of the WIPO English (machine) translation.