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
Priority and Status of the Claims
1. This application is a CON of 17524558 11/11/2021 PAT 12048748, which is CON of 16/882,236 05/22/2020 PAT 11185592, which is a DIV of 16/186,334 11/09/2018 PAT 10660968, which is a CON of PCT/US2017/032031 05/10/2017, which claims benefit of 62/334,130 05/10/2016.
2. Claims 1-20 are pending in the application.
Claim Rejections - 35 USC § 112
3. 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.
Claims 18-20 are rejected under 35 U.S.C. 112(a) or 112 first paragraph (pre-AIA ), because the specification does not reasonably provide enablement of “disorder” without limitation (i.e., no named disorder), see claims 12 and 20. The specification does not enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make the invention commensurate in scope with these claims.
ln In re Wands, 8 USPQ2d 1400 (1988), factors to be considered in determining
whether a disclosure meets the enablement requirement of 35 U.S.C. 112, first
paragraph, have been described. They are:
1. the nature of the invention,
2. the state of the prior art,
3. the predictability or Iack thereof in the art,
4. the amount of direction or guidance present,
5. the presence or absence of working examples,
6. the breadth of the claims,
7. the quantity of experimentation needed, and
8. the level of the skill in the art.
In the instant case:
The nature of the invention
The nature of the invention is drawn to intent methods of use for treating “disorder” without limitation (i.e., no named disorder), see claims 18- 20.
The state of the prior art and the predictability or lack thereof in the art
The state of the prior art is that the pharmacological art involves screening in
vitro and in vivo to determine which compound exhibit the desired pharmacological activities (i.e., what compound iloperidone can treat which specific disorder by what mechanism). There is no absolute predictability even in view of the seemingly high Ievel of skill in the art. The existence of these obstacles establishes that the contemporary knowledge in the art would prevent one of ordinary skill in the art from accepting any therapeutic regimen on its face. The prior art is prior art is Phillips et al. US12,048,748, it discloses a compound of formula (I) for treating cancer, see columns 373-383.
The instant claimed invention is highly unpredictable as discussed below:
It is noted that the pharmaceutical art is unpredictable, requiring each
embodiment to be individually assessed for physiological activity. In re Fisher, 427 F.2d 833,166 USPQ 18 (CCPA 1970) indicates that the more unpredictable an area is, the more specific enablement is necessary in order to satisfy the statute.
Applicants are claiming intent methods of use using the instant compound for
treating “disorder” without limitation (i.e., no named disorder). As such, the specification fails to enable the skilled artisan to use the instant compound for treating “disorder” without limitation (i.e., no named disorder). In addition, there is no established correlation between in vitro or in vivo activity and accomplishing “disorder” without limitation (i.e., no named disorder), and those skilled in the art would not accept allegations in the instant specification to be reliable predictors of success, and those skilled in the art would not be able to use the instant compounds since there is no description of an actual method “disorder” without limitation (i.e., no disorder) in a host is treated.
Hence, one of skill in the art is unable to fully predict possible results from the administration of the instant compound due to the unpredictability of “disorder” without limitation (i.e., no named disorder). The “disorder” without limitation (i.e., no named disorder) is known to have many obstacles that would prevent one of ordinary skill in the art from accepting treating regimen on its face.
The amount of direction or guidance present and the presence or absence of working examples
The only direction or guidance present in the instant specification is the description of treating a number of disorder, see pages 20-22 of the
specification. There are no in vitro or in vivo working examples present for
“disorder” without limitation (i.e., no named disorder) by the administration of the
instant invention.
The breadth of the claims
The breadth of the claims is methods of use of the instant compounds for treating “disorder” without limitation (i.e., no named disorder).
The quantity of experimentation needed
The quantity of experimentation needed is undue experimentation. One of skill in
the art would need to determine how “disorder” without limitation (i.e., no named disorder) would be benefited (i.e., treated) by the administration of the instant invention and would furthermore then have to determine which of the claimed methods of use would provide “disorder” without limitation (i.e., no named disorder), if any.
The Ievel of the skill in the art
The Ievel of skill in the art is high. However, due to the unpredictability in the pharmaceutical art, it is noted that each embodiment of the invention is required to be individually assessed for physiological activity by successful conclusion'' and ''patent protection is granted in return for an enabling disclosure of an invention, not for vague intimations of general ideas that may or may not be workable''.
in vitro and in vivo screening to determine which methods of use exhibit the desired pharmacological activity and which would benefit from this activity. Thus, the specification fails to provide sufficient support of the broad use of the pharmaceutical composition of the instant claims for the various disorder or disorders.
As a result necessitating one of skill to perform an exhaustive search for which metabolic-related disease s can be treated by what pharmaceutical compound of the instant claims in order to practice the claimed invention. Thus, factors such as "sufficient working examples", "the level of skill in the art" and "predictability", etc. have been demonstrated to be sufficiently lacking in the instantly claimed methods. In view of the breadth of the claim, the chemical nature of the invention, and the lack of working examples regarding the activity of the claimed compound regards to the treatment of the many disorders, one having ordinary skill in the art would have to undergo an undue amount of experimentation to use the invention commensurate in scope with the claims.
Genentech lnc. v. Novo Nordisk A/S (CA FC) 42 USPQ2d 1001, states that “ a
patent is not a hunting license. It is not a reward for search, but compensation for its successful conclusion'' and ''patent protection is granted in return for an enabling disclosure of an invention, not for vague intimations of general ideas that may or may not be workable''.
Therefore, in view of the Wands factors and ln re Fisher (CCPA 1970) discussed above, to practice the claimed invention herein, a person of skill in the art would have to engage in undue experimentation, with no assurance of success. This rejection can be overcome by incorporation of named disorder (i.e., claims 19-20) supported by the specification into claim 18 would obviate the rejection.
Double Patenting
4. The nonstatutory double patenting rejection is based on a judicially created doctrine grounded in public policy (a policy reflected in the statute) so as to prevent the unjustified or improper timewise extension of the "right to exclude" granted by a patent and to prevent possible harassment by multiple assignees. See In re Goodman, 11 F.3d 1046, 29 USPQ2d 2010 (Fed. Cir. 1993); In re Longi, 759 F.2d 887, 225 USPQ 645 (Fed. Cir. 1985); In re Van Ornum, 686 F.2d 937, 214 USPQ 761 (CCPA 1982); In re Vogel, 422 F.2d 438, 164 USPQ 619 (CCPA 1970); and In re Thorington, 418 F.2d 528, 163 USPQ 644 (CCPA 1969).
A timely filed terminal disclaimer in compliance with 37 CFR 1.321 (c) may be used to overcome an actual or provisional rejection based on a nonstatutory double patenting ground provided the conflicting application or patent is shown to be commonly owned with this application. See 37 CFR 1.130(b).
Effective January 1, 1994, a registered attorney or agent of record may sign a terminal disclaimer. A terminal disclaimer signed by the assignee must fully comply with 37 CFR 3.73(b).
Claims 1-20 are rejected under the judicially created doctrine of obviousness-type double patenting as being unpatentable independently claim 1 of Phillips et al. US 12,048,748, over claim 1 of Phillips et al. US 10,660,968, over claim 1 of Phillips et al. US 10,849,982, over claim 1 of Phillips et al. US 11,185,592, and over claim 1 of Nasveschuk et al. US 11,584,748. Although the conflicting claims are not identical, they are not patentably distinct from each other and reasons are as follows.
Applicants claim a compound of Formula (I), i.e.,
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230
352
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, or a pharmaceutically acceptable salt or N-oxide thereof; wherein:
W1 is C=0;
W2 is C=0;
X is NH; n is 0, 1, 2, or 3;
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35
43
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is a single or double bond;
Y and Z are each independently selected from CH2, CHR12, C(R12)2, C(O), N, NH, NR13, O, S, and S(O) as permitted by valency; R5 independently selected from hydrogen, alkyl, or hydroxyl, R6 is a bond, wherein Y or Z is substituted with R10; or R6 is a divalent moiety attached to Y and Z that contains 1 to 5 contiguous carbon atoms that form a 3 to 8-membered ring wherein 1, 2, or 3 carbon atoms can be replaced with a nitrogen, oxygen or sulfur atom, and wherein one of the ring atoms is substituted with R10 and the others are optionally substituted with R"; wherein the contiguous atoms of R6 can be attached through a single or double bond, see claim 1. Dependent claims 2-20 further limit the scope of compounds, i.e., n is 0-2, a specific variables R5 and R13 and moiety of
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136
154
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, and for treating cancer.
Phillips et al. ‘748 claims a compound of Formula:
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242
247
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, or a pharmaceutically acceptable salt or N-oxide thereof; wherein:
W1 is C=0;
W2 is C=0;
X is NH; n is 0, 1, 2, or 3;
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35
43
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is a single or double bond;
Y and Z are each independently selected from CH2, CHR12, C(R12)2, C(O), N, NH, NR13, O, S, and S(O) as permitted by valency;
R5 independently selected from hydrogen, alkyl, or hydroxyl, and R15 is
selected from
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93
703
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see claim 1 in columns 373-375.
Phillips et al. ‘968 claims a Degronimer consisting of a Degron covalently linked to a Targeting Ligand, wherein the Degronimer is of Formula:
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173
382
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, or a pharmaceutically acceptable salt or N-oxide thereof; wherein:
W1 is CR4R2, C=0, C=S, C=CH2, SO2, S(O), P(0)0alkyl, P(0)NHalkyl, P(0)N(alkyl)2, P(0)alkyl, P(0)0H, or P(0)NH2;
W2 is CR3R4, C=0, C=S, C=CH2, SO2, S(O), P(0)0alkyl, P(0)NHalkyl, P(0)N(alkyl)2, P(0)alkyl, P(0)0H, or P(0)NH2;
X is independently NH, NR12, CH2, CHR12, C(R12)2, O, or S; n is 0, 1, 2, or 3;
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35
43
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is a single or double bond;
Y and Z are each independently selected from CFL, CHR12, C(R12)2, C(O), N, NH, NR13, O, S, and S(O) as permitted by valency;
R1, R2, R3, R4, R7, and R8, are independently selected from hydrogen, alkyl, aliphatic, heteroaliphatic, aryl, heteroaryl, carbocyclic, hydroxyl, see column 369.
Phillips et al. ‘982 claims a compound of Formula:
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187
447
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, or a pharmaceutically acceptable salt or N-oxide thereof; wherein:
W1 is CR4R2, C=0, C=S, C=CH2, SO2, S(O), P(0)0alkyl, P(0)NHalkyl, P(0)N(alkyl)2, P(0)alkyl, P(0)0H, or P(0)NH2;
W2 is CR3R4, C=0, C=S, C=CH2, SO2, S(O), P(0)0alkyl, P(0)NHalkyl, P(0)N(alkyl)2, P(0)alkyl, P(0)0H, or P(0)NH2;
X is independently NH; n is 0, 1, 2, or 3;
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43
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is a single or double bond;
R1-R8 and R15 is hydrogen, alkyl, heterocyclic, carbocyclic, aryl, or heteroaryl, or R15 and R1 form a 3-6 carbon fused ring, or R15 and R5 form a 3-6 carbon fused ring, see column 410.
Phillips et al. ‘592 claims a method for treating a human with a cancer mediated by a Targeted Protein selected from ABL, BRD4, BRD9, CBP, DOT1L, ERK1, ERK2, EZH2, FGFR3, FGFR4, FKBP, MDM2, NTRK1, PIK3CA, RET, WDR5, EGFR, bromodomain containing protein, glucocorticoid receptor, androgen receptor, and estrogen receptor, comprising administering an effective amount of a compound optionally in a pharmaceutically acceptable carrier, to a patient in need thereof, wherein the compound is of Formula: :
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173
382
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, or a pharmaceutically acceptable salt or N-oxide thereof; wherein:
W1 is CR4R2, C=0, C=S, C=CH2, SO2, S(O), P(0)0alkyl, P(0)NHalkyl, P(0)N(alkyl)2, P(0)alkyl, P(0)0H, or P(0)NH2;
W2 is CR3R4, C=0, C=S, C=CH2, SO2, S(O), P(0)0alkyl, P(0)NHalkyl, P(0)N(alkyl)2, P(0)alkyl, P(0)0H, or P(0)NH2;
X is independently NH, NR12, CH2, CHR12, C(R12)2, O, or S; n is 0, 1, 2, or 3;
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is a single or double bond;
Y and Z are each independently selected from CFL, CHR12, C(R12)2, C(O), N, NH, NR13, O, S, and S(O) as permitted by valency;
R1, R2, R3, R4, R7, and R8, are independently selected from hydrogen, alkyl, aliphatic, heteroaliphatic, aryl, heteroaryl, carbocyclic, hydroxyl, see column 371.
Nasveschuk et al. ‘748 claims a compound of formula (XIV), i.e.,
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147
269
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, wherein R1 is =O and XA1 is heteroarylene, see column 353-354.
The difference between instant claims and Phillips et al. ‘748, ‘968, ‘982 and ‘592, and Nasveschuk et al. ‘748 is that the instant claims are embraced within the scope of Phillips et al. ‘748, ‘968, ‘982 and ‘592, and Nasveschuk et al. ‘748.
One having ordinary skill in the art would find the claims 1-20 prima facie obvious because one would be motivated to employ the compounds/composition and methods of use of Phillips et al. ‘748, ‘968, ‘982 and ‘592, and Nasveschuk et al. ‘748 to obtain instant invention.
The motivation to make the claimed compounds/composition derived from the known compounds/composition and methods of use of Phillips et al. ‘748,’968, ‘982 and ‘592, and Nasveschuk et al. ‘748 would possess similar activity to that which is claimed in the reference.
Conclusion
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/REI TSANG SHIAO/
Rei-tsang Shiao, Ph.D.Primary Examiner, Art Unit 1691
July 27, 2026
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