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 .
Priority
The instant application, filed 11/08/2023, is a 371 filing of PCT/CN2022/091066, filed 05/06/2022, which claims foreign priority to PCT/CN2021/092257, filed 05/08/2021. Receipt is acknowledged of certified copies of papers required by 37 CFR § 1.55.
Restriction/Election
Applicant’s election without traverse of Group I in the reply filed on 07/10/2026 is acknowledged. However, Applicant failed to elect a single and specific compound of Formula (I), as required in the requirement for restriction/election, filed 02/25/2026. Nevertheless, in order to advance prosecution and prevent further delays, the examiner has searched the full scope of the claims with respect to a compound of Formula (I). All claims pertaining to Group I, i.e. 1-8, 10-13, and 15-17, are examined on the merits, and found to make a contribution over the prior art of record. However, the claims are not deemed allowable for reasons set forth hereinafter.
Status of Claims
Claims 1-18 are pending in the instant application. Claims 9 and 14 are withdrawn from further consideration pursuant to 37 CFR § 1.142(b), as being drawn to a non-elected invention and species. Therefore, claims 1-8, 10-13, and 15-17 read on an elected invention and are therefore under consideration in the instant application, and examined on the merits as such.
Information Disclosure Statement
The Information Disclosure Statement filed on 09/06/2024, 11/21/2024, and 07/17/2025 are acknowledged and found to be in compliance with the provisions of 37 CFR § 1.97. Accordingly, the information disclosure statements are considered.
Claim Rejections - 35 U.S.C. § 112 (a)
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.
The following is a quotation of the first paragraph of pre-AIA 35 U.S.C. § 112:
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 of carrying out his invention.
Claims 1-8, 10-13, and 15-17 are rejected under 35 U.S.C. § 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, as failing to comply with the written description requirement. The claim(s) contains subject matter which was not described in the specification in such a way as to reasonably convey to one skilled in the relevant art that the inventor or a joint inventor, or for applications subject to pre-AIA 35 U.S.C. 112, the inventor(s), at the time the application was filed, had possession of the claimed invention.
Claims 1-8, 10-13, and 15-17 of the instant application are drawn to compounds having following substituents:
Het is a monocyclic 5- or 6-membered aromatic ring containing one, two or three nitrogen atoms and optionally a carbonyl moiety; wherein said monocyclic 5- or 6-membered aromatic ring is substituted with one C3-6cycloalkyl and wherein said monocyclic 5- or 6-membered aromatic ring is optionally substituted with one or two additional substituents selected from the group consisting of C3-6cycloalkyl, cyano, and C1-4alkyl;
R1b is F or Cl;
Y1 is —CR5aR5b—, —O—, —S—, or —NR5c—;
R2 is hydrogen, halo, C1-4alkyl, —O—C1-4alkyl, and —NR7aR7b;
U is N or CH;
n1 is 1 and 2;
n2 is 1 and 2;
n3 is 1 and 2;
n4 is 1 and 2;
R4 is C1-5alkyl
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;
R5a, R5b, R5c, R7a, and R7b, are hydrogen, C1-4alkyl and C3-6cycloalkyl;
R3 is Het1, Het2, Cy2 and —C1-6alkyl-NRxcRxd;
Rxc is Cy1; Het5; —C1-6alkyl-Cy1; —C1-6alkyl-Het3; —C1-6alkyl-Het4, or —C1-6alkyl-phenyl;
Rxd represents hydrogen; C1-4alkyl; or C1-4alkyl substituted with one, two or three substituents selected from the group consisting of halo, —OH, —O—C1-4alkyl, and cyano; or Rxc and Rxd are taken together to form together with the N-atom to which they are attached a 4- to 7-membered monocyclic fully saturated heterocyclyl containing one N-atom and optionally one additional heteroatom selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted with one, two or three substituents selected from the group consisting of halo, —OH, —O—C1-4alkyl, and cyano;
Het1 is a monocyclic C-linked 4- to 7-membered fully saturated heterocyclyl containing one N-atom and optionally one or two additional heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; or a bicyclic C-linked 6- to 11-membered fully saturated heterocyclyl containing one N-atom and optionally one or two additional heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one nitrogen with a substituent selected from the group consisting of R6, —C(═O)—Cy1, and —C(═O)—R8; and wherein said heterocyclyl is optionally substituted on one or two carbon atoms with in total one, two, three or four substituents each independently selected from the group consisting of halo, R6, Het6a, Het6b, C1-4alkyl, oxo, —NR9aR9b and —OH;
Het2 is a C-linked pyrazolyl or triazolyl; which may be optionally substituted on one nitrogen atom with R6a;.
R6 is Het3; Het4; —C(═O)—NH—Cy1; —C(═O)—NH—R8; C1-6alkyl optionally substituted with one or two substituents each independently selected from the group consisting of Het3, Het4, Het6a, Het6b, Cy1, —CN, —OH, —O—C1-4alkyl, —C(═O)—NH—C1-4alkyl, —C(═O)—NH—C1-4alkyl-C3-6cycloalkyl, —C(═O)—OH, —NR11aR11b, and —NH—S(═O)2—C1-4alkyl; and C3-6cycloalkyl optionally substituted by one or two substituents each independently selected from the group consisting of —CN, —OH, —O—C1-4alkyl, —C(═O)—NH—C1-4alkyl, —NH—S(═O)2—C1-4alkyl, and C1-4alkyl optionally substituted with one substituent selected from the group consisting of OH, —O—C1-4alkyl, —C(═O)—NH—C1-4alkyl and —NH—S(═O)2—C1-4alkyl;
R6a is Het3; Het4; —C(═O)—NH—Cy1; —C(═O)—NH—R8; C1-6alkyl optionally substituted with one or two substituents each independently selected from the group consisting of Het3, Het4, Het6a, Het6b, Cy1, —CN, —OH, —O—C1-4alkyl, —C(═O)—NH—C1-4alkyl, —C(═O)—NH—C1-4alkyl-C3-6cycloalkyl, —C(═O)—OH, —NR11aR11b, and —NH—S(═O)2—C1-4alkyl; and C3-6cycloalkyl optionally substituted by one or two substituents each independently selected from the group consisting of —CN, —OH, —O—C1-4alkyl, —C(═O)—NH—C1-4alkyl, —NH—S(═O)2—C1-4alkyl, and C1-4alkyl optionally substituted with one substituent selected from the group consisting of OH, —O—C1-4alkyl, —C(═O)—NH—C1-4alkyl and —NH—S(═O)2—C1-4alkyl;
R8 represents —O—C1-6alkyl, C1-6alkyl; or C1-6alkyl substituted with one, two or three substituents each independently selected from —OH, halo, cyano, —NR11aR11b, Het3a, and Het6a;
Het3 each independently represent a monocyclic C-linked 4- to 7-membered fully saturated heterocyclyl containing one, two or three heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; or a bicyclic C-linked 6- to 11-membered fully saturated heterocyclyl containing one, two or three heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one carbon atom with C1-4alkyl, halo, —OH, —NR11aR11b, or oxo; and wherein said heterocyclyl is optionally substituted on one nitrogen atom with C1-4alkyl;
Het3a each independently represent a monocyclic C-linked 4- to 7-membered fully saturated heterocyclyl containing one, two or three heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; or a bicyclic C-linked 6- to 11-membered fully saturated heterocyclyl containing one, two or three heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one carbon atom with C1-4alkyl, halo, —OH, —NR11aR11b, or oxo; and wherein said heterocyclyl is optionally substituted on one nitrogen atom with C1-4alkyl;
Het5 each independently represent a monocyclic C-linked 4- to 67-membered fully saturated heterocyclyl containing one, two or three heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; or a bicyclic C-linked 6- to 11-membered fully saturated heterocyclyl containing one, two or three heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one carbon atom with C1-4alkyl, halo, —OH, —NR11aR11b, or oxo; and wherein said heterocyclyl is optionally substituted on one nitrogen atom with C1-4alkyl;
Het5a each independently represent a monocyclic C-linked 4- to 7-membered fully saturated heterocyclyl containing one, two or three heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; or a bicyclic C-linked 6- to 11-membered fully saturated heterocyclyl containing one, two or three heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one carbon atom with C1-4alkyl, halo, —OH, —NR11aR11b, or oxo; and wherein said heterocyclyl is optionally substituted on one nitrogen atom with C1-4alkyl;
Het4 is a monocyclic C-linked 5- or 6-membered aromatic ring containing one, two or three heteroatoms each independently selected from O, S, and N, or a fused bicyclic C-linked 9- or 10-membered aromatic ring containing one, two, three or four heteroatoms each independently selected from O, S, and N; wherein said aromatic ring is optionally substituted on one nitrogen atom with C1-4alkyl or —(C═O)—O—C1-4alkyl; and wherein said aromatic ring is optionally substituted on one or two carbon atoms with in total one or two substituents each independently selected from the group consisting of —OH, halo, C1-4alkyl, —O—C1-4alkyl, —NR11aR11b, C1-4alkyl-NR11aR11b, —NH—C(═O)—C1-4alkyl, cyano, —COOH, —NH—C(═O)—O—C1-4alkyl, —NH—C(═O)—Cy3, —NH—C(═O)—NR10aR10b, —(C═O)—O—C1-4alkyl, —NH—S(═O)2—C1-4alkyl, Het8a, —C1-4alkyl-Het8a, Het8b, Het9, and —C(═O)—NR10aR10b;
Het7 is a monocyclic C-linked 5- or 6-membered aromatic ring containing one, two or three heteroatoms each independently selected from O, S, and N, or a fused bicyclic C-linked 9- or 10-membered aromatic ring containing one, two, three or four heteroatoms each independently selected from O, S, and N; wherein said aromatic ring is optionally substituted on one nitrogen atom with C1-4alkyl or —(C═O)—O—C1-4alkyl; and wherein said aromatic ring is optionally substituted on one or two carbon atoms with in total one or two substituents each independently selected from the group consisting of —OH, halo, C1-4alkyl, —O—C1-4alkyl, —NR11aR11b, C1-4alkyl-NR11aR11b, —NH—C(═O)—C1-4alkyl, cyano, —COOH, —NH—C(═O)—O—C1-4alkyl, —NH—C(═O)—Cy3, —NH—C(═O)—NR10aR10b, —(C═O)—O—C1-4alkyl, —NH—S(═O)2—C1-4alkyl, Het8a, —C1-4alkyl-Het8a, Het8b, Het9, and —C(═O)—NR10aR10b;
Het6a is a monocyclic N-linked 4- to 7-membered fully saturated heterocyclyl containing one N-atom and optionally one or two additional heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one or two carbon atoms with in total one, two, three or four substituents each independently selected from the group consisting of halo, —OH, oxo, —NH—C(═O)—C1-4alkyl, —NH—C(═O)—Cy3, —(C═O)—NR10aR10b, —O—C3-6cycloalkyl, —S(═O)2—C1-4alkyl, cyano, C1-4alkyl, —C1-4alkyl-OH, —O—C1-4alkyl, —O—(C═O)—NR10aR10b, and —O—(C═O)—C1-4alkyl; and wherein said heterocyclyl is optionally substituted on one nitrogen with a substituent selected from the group consisting of —C(═O)—C1-4alkyl and —(C═O)—NR10aR10b;
Het8 is a monocyclic N-linked 4- to 67-membered fully saturated heterocyclyl containing one N-atom and optionally one or two additional heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one or two carbon atoms with in total one, two, three or four substituents each independently selected from the group consisting of halo, —OH, oxo, —NH—C(═O)—C1-4alkyl, —NH—C(═O)—Cy3, —(C═O)—NR10aR10b, —O—C3-6cycloalkyl, —S(═O)2—C1-4alkyl, cyano, C1-4alkyl, —C1-4alkyl-OH, —O—C1-4alkyl, —O—(C═O)—NR10aR10b, and —O—(C═O)—C1-4alkyl; and wherein said heterocyclyl is optionally substituted on one nitrogen with a substituent selected from the group consisting of —C(═O)—C1-4alkyl and —(C═O)—NR10aR10b;
Het8a is a monocyclic N-linked 4- to 7-membered fully saturated heterocyclyl containing one N-atom and optionally one or two additional heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one or two carbon atoms with in total one, two, three or four substituents each independently selected from the group consisting of halo, —OH, oxo, —NH—C(═O)—C1-4alkyl, —NH—C(═O)—Cy3, —(C═O)—NR10aR10b, —O—C3-6cycloalkyl, —S(═O)2—C1-4alkyl, cyano, C1-4alkyl, —C1-4alkyl-OH, —O—C1-4alkyl, —O—(C═O)—NR10aR10b, and —O—(C═O)—C1-4alkyl; and wherein said heterocyclyl is optionally substituted on one nitrogen with a substituent selected from the group consisting of —C(═O)—C1-4alkyl and —(C═O)—NR10aR10b;
Het6b is a bicyclic N-linked 6-9 to 11-membered fully saturated heterocyclyl containing one N-atom and optionally one or two additional heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one or two carbon atoms with in total one or two substituents each independently selected from the group consisting of C1-4alkyl, —OH, oxo, —(C═O)—NR10aR10b, —NH—C(═O)—C1-4alkyl, —NH—C(═O)—Cy3, and —O—C1-4alkyl; and wherein said heterocyclyl is optionally substituted on one nitrogen with a substituent selected from the group consisting of —C(═O)—C1-4alkyl, —C(═O)—Cy3, —(C═O)—C1-4alkyl-OH, —C(═O)—C1-4alkyl-O—C1-4alkyl, —C(═O)—C1-4alkyl-NR11aR11b, and C1-4alkyl;
Het8b is a bicyclic N-linked 6- to 11-membered fully saturated heterocyclyl containing one N-atom and optionally one or two additional heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one or two carbon atoms with in total one or two substituents each independently selected from the group consisting of C1-4alkyl, —OH, oxo, —(C═O)—NR10aR10b, —NH—C(═O)—C1-4alkyl, —NH—C(═O)—Cy3, and —O—C1-4alkyl; and wherein said heterocyclyl is optionally substituted on one nitrogen with a substituent selected from the group consisting of —C(═O)—C1-4alkyl, —C(═O)—Cy3, —(C═O)—C1-4alkyl-OH, —C(═O)—C1-4alkyl-O—C1-4alkyl, —C(═O)—C1-4alkyl-NR11aR11b, and C1-4alkyl;
Het9 represents a monocyclic C-linked 5- or 6-membered aromatic ring containing one, two or three heteroatoms each independently selected from O, S, and N, or a fused bicyclic C-linked 9- or 10-membered aromatic ring containing one, two or three heteroatoms each independently selected from O, S, and N; wherein said aromatic ring is optionally substituted on one nitrogen atom with C1-4alkyl; and wherein said aromatic ring is optionally substituted on one or two carbon atoms with in total one or two substituents each independently selected from the group consisting of —OH, halo, and C1-4alkyl;
Cy1 represents C3-6cycloalkyl optionally substituted with one, two or three substituents selected from the group consisting of —OH, —NH—C(═O)—C1-4alkyl, C1-4alkyl, —NH—S(═O)2—C1-4alkyl, —S(═O)2—C1-4alkyl, and —O—C1-4alkyl;
Cy2 represents C3-5-7cycloalkyl; wherein said C3-7cycloalkyl is optionally substituted with one, two, three or four substituents each independently selected from the group consisting of halo, R6, Het6a, Het6b, —NR9aR9b, —OH, C1-4alkyl, and C1-4alkyl substituted with one or two substituents each independently selected from the group consisting of Het3a, Het6a, Het6b, and —NR9aR9b;
Cy3 represents C3-7cycloalkyl; wherein said C3-7cycloalkyl is optionally substituted with one, two or three halo substituents;
R9a is hydrogen; C1-4alkyl; C3-6cycloalkyl; —C(═O)—C1-4alkyl; —C(═O)—C3-6cycloalkyl; —S(═O)2—C1-4alkyl; Het5; Het7; —C1-4alkyl-R16; —C(═O)—C1-4alkyl-Het3a; —C(═O)—R14; C3-6cycloalkyl substituted with one, two or three substituents selected from the group consisting of halo, —OH, —O—C1-4alkyl, —NR11aR11b, and cyano; and C1-4alkyl substituted with one, two or three substituents selected from the group consisting of halo, —OH, —O—C1-4alkyl, —NR11aR11b, and cyano;
R9b is hydrogen; C1-4alkyl; C3-6cycloalkyl; —C(═O)—C1-4alkyl; —C(═O)—C3-6cycloalkyl; —S(═O)2—C1-4alkyl; Het5; Het7; —C1-4alkyl-R16; —C(═O)—C1-4alkyl-Het3a; —C(═O)—R14; C3-6cycloalkyl substituted with one, two or three substituents selected from the group consisting of halo, —OH, —O—C1-4alkyl, —NR11aR11b, and cyano; and C1-4alkyl substituted with one, two or three substituents selected from the group consisting of halo, —OH, —O—C1-4alkyl, —NR11aR11b, and cyano;
R11a is hydrogen and C1-4alkyl;
R11b is hydrogen and C1-4alkyl;
R13b is hydrogen and C1-4alkyl;
R15a is hydrogen and C1-4alkyl;
R15b is hydrogen and C1-4alkyl;
R17a is hydrogen and C1-4alkyl;
R17a is hydrogen and C1-4alkyl;
R10a is hydrogen, C1-4alkyl, and C3-6cycloalkyl;
R10b is hydrogen, C1-4alkyl, and C3-6cycloalkyl;
R14 is Het5a; Het7; Het8a; —O—C1-4alkyl; —C(═O)NR15aR15b; C3-6cycloalkyl substituted with one, two or three substituents selected from the group consisting of —O—C1-4alkyl and halo; or C1-4alkyl substituted with one, two or three substituents selected from the group consisting of —O—C1-4alkyl, —NR13aR13b, halo, cyano, —OH, Het8a, and Cy1;
R16 is —C(═O)—NR17aR17b, —S(═O)2—C1-4alkyl, Het5, Het7, or Het8
35 U.S.C. 112(a) and the first paragraph of pre-AIA 35 U.S.C. 112 require that the "specification shall contain a written description of the invention ...." This requirement is separate and distinct from the enablement requirement. Ariad Pharm., Inc. v. Eli Lilly & Co., 598 F.3d 1336, 1340, 94 USPQ2d 1161, 1167 (Fed. Cir. 2010) (en banc); Vas-Cath, Inc. v. Mahurkar, 935 F.2d 1555, 1560, 19 USPQ2d 1111,1114 (Fed. Cir. 1991); see also Univ. of Rochester v. G.D. Searle & Co., 358 F.3d 916, 920-23, 69 USPQ2d 1886, 1890-93 (Fed. Cir. 2004) (discussing the history and purpose of the written description requirement); In re Curtis, 354 F.3d 1347, 1357, 69 USPQ2d 1274, 1282 (Fed. Cir. 2004) ("conclusive evidence of a claim’s enablement is not equally conclusive of that claim’s satisfactory written description"). The written description requirement has several policy objectives. "[T]he ‘essential goal’ of the description of the invention requirement is to clearly convey the information that an applicant has invented the subject matter which is claimed." In re Barker, 559 F.2d 588, 592 n.4, 194 USPQ 470, 473 n.4 (CCPA 1977). Another objective is to convey to the public what the applicant claims as the invention. See Regents of the Univ. of Cal. v. Eli Lilly, 119 F.3d 1559, 1566, 43 USPQ2d 1398, 1404 (Fed. Cir. 1997), cert, denied, 523 U.S. 1089 (1998). "The ‘written description’ requirement implements the principle that a patent must describe the technology that is sought to be patented; the requirement serves both to satisfy the inventor’s obligation to disclose the technologic knowledge upon which the patent is based, and to demonstrate that the patentee was in possession of the invention that is claimed." Capon v. Eshhar, 418 F.3d 1349, 1357, 76 USPQ2d 1078, 1084 (Fed. Cir. 2005). Further, the written description requirement promotes the progress of the useful arts by ensuring that patentees adequately describe their inventions in their patent specifications in exchange for the right to exclude others from practicing the invention for the duration of the patent’s term.
To satisfy the written description requirement, a patent specification must describe the claimed invention in sufficient detail that one skilled in the art can reasonably conclude that the inventor had possession of the claimed invention. See, e.g., Moba, B.V. v. Diamond Automation, Inc., 325 F.3d 1306, 1319, 66 USPQ2d 1429, 1438 (Fed. Cir. 2003); Vas-Cath, Inc. v. Mahurkar, 935 F.2d at 1563, 19 USPQ2d at 1116.
An applicant shows possession of the claimed invention by describing the claimed invention with all of its limitations using such descriptive means as words, structures, figures, diagrams, and formulas that fully set forth the claimed invention. Lockwood v. Amer. Airlines, Inc., 107 F.3d 1565, 1572, 41 USPQ2d 1961, 1966 (Fed. Cir. 1997). Possession may be shown in a variety of ways including description of an actual reduction to practice, or by showing that the invention was "ready for patenting" such as by the disclosure of drawings or structural chemical formulas that show that the invention was complete, or by describing distinguishing identifying characteristics sufficient to show that the applicant was in possession of the claimed invention. See, e.g., Pfaffv. Wells Bees., Inc., 525 U.S. 55, 68, 119 S.Ct. 304, 312, 48 USPQ2d 1641, 1647 (1998); EliLilly, 119 F.3d at 1568, 43 USPQ2d at 1406; Amgen, Inc. v. Chugai Pharm.,927 F.2d 1200, 1206, 18 USPQ2d 1016, 1021 (Fed. Cir. 1991). An application specification may show actual reduction to practice by describing testing of the claimed invention.
In the present case, the important factors leading to a conclusion of inadequate written description is the lack of a representative number of species that characterizes the entire claimed genus and accounts for variations between species of the genus.
In the instant specification, there is no disclosure of compounds having the following claimed substituents:
Het as a monocyclic 5- or 6-membered aromatic ring containing three nitrogen atoms and optionally a carbonyl moiety; wherein said monocyclic 5- or 6-membered aromatic ring is substituted with one C4-6cycloalkyl and wherein said monocyclic 5- or 6-membered aromatic ring is optionally substituted with one or two additional substituents selected from the group consisting of C3-6cycloalkyl, cyano, and C1-4alkyl;
R1b as Cl;
Y1 as —CR5aR5b— , —S—, or —NR5c—;
R2 as halo, C1-4alkyl, —O—C1-4alkyl, and —NR7aR7b;
U as CH;
n1 as 1;
n2 as 2;
n3 as 2;
n4 as 2;
R4 as
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R5a, R5b, R5c, R7a, and R7b as hydrogen, C1-4alkyl and C3-6cycloalkyl;
R3 as Het2 and —C1-6alkyl-NRxcRxd;
Rxc as Cy1; Het5; —C1-6alkyl-Cy1; —C1-6alkyl-Het3; —C1-6alkyl-Het4, or —C1-6alkyl-phenyl;
Rxd as hydrogen; C1-4alkyl; or C1-4alkyl substituted with one, two or three substituents selected from the group consisting of halo, —OH, —O—C1-4alkyl, and cyano; or Rxc and Rxd are taken together to form together with the N-atom to which they are attached a 4- to 7-membered monocyclic fully saturated heterocyclyl containing one N-atom and optionally one additional heteroatom selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted with one, two or three substituents selected from the group consisting of halo, —OH, —O—C1-4alkyl, and cyano;
Het1 as a monocyclic C-linked 4- to 7-membered fully saturated heterocyclyl containing one N-atom and optionally one or two additional heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; or a bicyclic C-linked 6- to 11-membered fully saturated heterocyclyl containing one N-atom and optionally one or two additional heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one nitrogen with a substituent selected from the group consisting of R6, —C(═O)—Cy1, and —C(═O)—R8; and wherein said heterocyclyl is optionally substituted on two carbon atoms with in total two, three or four substituents each independently selected from the group consisting of halo, R6, C1-4alkyl, oxo, —NR9aR9b and —OH;
Het2 as a C-linked pyrazolyl or triazolyl; which may be optionally substituted on one nitrogen atom with R6a;
R6 as Het4; —C(═O)—NH—R8; C1-6alkyl optionally substituted with one or two substituents each independently selected from the group consisting of Het3, Het4, Het6a, Het6b, Cy1, —CN, —OH, —O—C1-4alkyl, —C(═O)—NH—C1-4alkyl, —C(═O)—NH—C1-4alkyl-C3-6cycloalkyl, —C(═O)—OH, —NR11aR11b, and —NH—S(═O)2—C1-4alkyl; and C3-6cycloalkyl optionally substituted by one or two substituents each independently selected from the group consisting of —CN, —OH, —O—C1-4alkyl, —C(═O)—NH—C1-4alkyl, —NH—S(═O)2—C1-4alkyl, and C1-4alkyl optionally substituted with one substituent selected from the group consisting of OH, —O—C1-4alkyl, —C(═O)—NH—C1-4alkyl and —NH—S(═O)2—C1-4alkyl;
R6a as Het3 —C(═O)—NH—R8; C1-6alkyl optionally substituted with one or two substituents each independently selected from the group consisting of Het3, Het4, Het6a, Het6b, Cy1, —CN, —OH, —O—C1-4alkyl, —C(═O)—NH—C1-4alkyl, —C(═O)—NH—C1-4alkyl-C3-6cycloalkyl, —C(═O)—OH, —NR11aR11b, and —NH—S(═O)2—C1-4alkyl; and C3-6cycloalkyl optionally substituted by one or two substituents each independently selected from the group consisting of —CN, —OH, —O—C1-4alkyl, —C(═O)—NH—C1-4alkyl, —NH—S(═O)2—C1-4alkyl, and C1-4alkyl optionally substituted with one substituent selected from the group consisting of OH, —O—C1-4alkyl, —C(═O)—NH—C1-4alkyl and —NH—S(═O)2—C1-4alkyl;
R8 represents —O—C1-6alkyl, C1-6alkyl; or C1-6alkyl substituted with one, two or three substituents each independently selected from —OH, halo, cyano, —NR11aR11b, Het3a, and Het6a; R8 as —O—C1-6alkyl, C1-6alkyl substituted with two or three substituents each independently selected from —OH, halo, and Het6a; R8 is C1-6alkyl; or C1-6alkyl substituted with one, cyano, —NR11aR11b or Het3a
Het3 as a monocyclic C-linked 4- to 7-membered fully saturated heterocyclyl containing one, two or three heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; or a bicyclic C-linked 6- to 11-membered fully saturated heterocyclyl containing one, two or three heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one carbon atom with C1-4alkyl, halo, —OH, —NR11aR11b, or oxo; and wherein said heterocyclyl is optionally substituted on one nitrogen atom with C1-4alkyl;
Het3a as monocyclic C-linked 5- to 7-membered fully saturated heterocyclyl containing two or three heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; or a bicyclic C-linked 6- to 11-membered fully saturated heterocyclyl containing one, two or three heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one carbon atom with C1-4alkyl, halo, —OH, —NR11aR11b, or oxo; and wherein said heterocyclyl is optionally substituted on one nitrogen atom with C1-4alkyl;
Het5 as a monocyclic C-linked 7-membered fully saturated heterocyclyl containing one, two or three heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; or a bicyclic C-linked 6- to 11-membered fully saturated heterocyclyl containing one, two or three heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one carbon atom with C1-4alkyl, halo, —OH, —NR11aR11b, or oxo; and wherein said heterocyclyl is optionally substituted on one nitrogen atom with C1-4alkyl;
Het5a as monocyclic C-linked 4- to 7-membered fully saturated heterocyclyl containing one, two or three heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; or a bicyclic C-linked 6- to 11-membered fully saturated heterocyclyl containing one, two or three heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one carbon atom with C1-4alkyl, halo, —OH, —NR11aR11b, or oxo; and wherein said heterocyclyl is optionally substituted on one nitrogen atom with C1-4alkyl;
Het4 as a monocyclic C-linked 5- 6-membered aromatic ring containing one, two or three heteroatoms each independently selected from O, S, and N, or a fused bicyclic C-linked 9- or 10-membered aromatic ring containing one, two, three or four heteroatoms each independently selected from O, S, and N; wherein said aromatic ring is optionally substituted on one nitrogen atom with C1-4alkyl or —(C═O)—O—C1-4alkyl; and wherein said aromatic ring is optionally substituted on one or two carbon atoms with in total one or two substituents each independently selected from the group consisting of —OH, halo, C1-4alkyl, —O—C1-4alkyl, —NR11aR11b, C1-4alkyl-NR11aR11b, —NH—C(═O)—C1-4alkyl, cyano, —COOH, —NH—C(═O)—O—C1-4alkyl, —NH—C(═O)—Cy3, —NH—C(═O)—NR10aR10b, —(C═O)—O—C1-4alkyl, —NH—S(═O)2—C1-4alkyl, Het8a, —C1-4alkyl-Het8a, Het8b, Het9, and —C(═O)—NR10aR10b;
Het7 as a monocyclic C-linked 5- or 6-membered aromatic ring containing one heteroatom each independently selected from O, S, and N, or a fused bicyclic C-linked 10-membered aromatic ring containing one or two heteroatoms each independently selected from O and S, and N; wherein said aromatic ring is optionally substituted on one nitrogen atom with C1-4alkyl or —(C═O)—O—C1-4alkyl; and wherein said aromatic ring is optionally substituted on one or two carbon atoms with —OH, , —O—C1-4alkyl, C1-4alkyl-NR11aR11b, —NH—C(═O)—NR10aR10b,—NH—S(═O)2—C1-4alkyl, Het8a, —C1-4alkyl-Het8a, and Het8b ;
Het6a as a monocyclic N-linked 4- to 7-membered fully saturated heterocyclyl containing one N-atom and optionally one or two additional heteroatoms each independently selected from O, wherein said heterocyclyl is optionally substituted on one or two carbon atoms with in total three or four substituents each independently selected from the group consisting of halo, —OH, oxo, —NH—C(═O)—C1-4alkyl, —NH—C(═O)—Cy3, —(C═O)—NR10aR10b, —O—C4-6cycloalkyl, —S(═O)2—C1-4alkyl, cyano, C1-4alkyl, —C1-4alkyl-OH, —O—C1-4alkyl, —O—(C═O)—NR10aR10b, and —O—(C═O)—C1-4alkyl; and wherein said heterocyclyl is optionally substituted on one nitrogen with a substituent selected from the group consisting of —C(═O)—C1-4alkyl and —(C═O)—NR10aR10b ;
Het8 as a monocyclic N-linked 4- to 5- or 7-membered fully saturated heterocyclyl containing one N-atom and optionally one or two additional heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one or two carbon atoms with in total one, two, three or four substituents each independently selected from the group consisting of halo, —OH, oxo, —NH—C(═O)—C1-4alkyl, —NH—C(═O)—Cy3, —(C═O)—NR10aR10b, —O—C3-6cycloalkyl, —S(═O)2—C1-4alkyl, cyano, C1-4alkyl, —C1-4alkyl-OH, —O—C1-4alkyl, —O—(C═O)—NR10aR10b, and —O—(C═O)—C1-4alkyl; and wherein said heterocyclyl is optionally substituted on one nitrogen with a substituent selected from the group consisting of —C(═O)—C1-4alkyl and —(C═O)—NR10aR10b;
Het8a as a monocyclic N-linked 4- to 7-membered fully saturated heterocyclyl containing one N-atom and optionally one or two additional heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one or two carbon atoms with in total one, two, three or four substituents each independently selected from the group consisting of halo, —OH, oxo, —NH—C(═O)—C1-4alkyl, —NH—C(═O)—Cy3, —(C═O)—NR10aR10b, —O—C3-6cycloalkyl, —S(═O)2—C1-4alkyl, cyano, C1-4alkyl, —C1-4alkyl-OH, —O—C1-4alkyl, —O—(C═O)—NR10aR10b, and —O—(C═O)—C1-4alkyl; and wherein said heterocyclyl is optionally substituted on one nitrogen with a substituent selected from the group consisting of —C(═O)—C1-4alkyl and —(C═O)—NR10aR10b;
Het6b as N-linked 10- to 11-membered fully saturated heterocyclyl containing one N-atom and optionally one or two additional heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one or two carbon atoms with in total one or two substituents each independently selected from the group consisting of C1-4alkyl, —OH, oxo, —(C═O)—NR10aR10b, —NH—C(═O)—C1-4alkyl, —NH—C(═O)—Cy3, and —O—C1-4alkyl; and wherein said heterocyclyl is optionally substituted on one nitrogen with a substituent selected from the group consisting of —C(═O)—C1-4alkyl, —C(═O)—Cy3, —(C═O)—C1-4alkyl-OH, —C(═O)—C1-4alkyl-O—C1-4alkyl, —C(═O)—C1-4alkyl-NR11aR11b, and C2-4alkyl;
Het8b as a bicyclic N-linked 6- to 11-membered fully saturated heterocyclyl containing one N-atom and optionally one or two additional heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one or two carbon atoms with in total one or two substituents each independently selected from the group consisting of C1-4alkyl, —OH, oxo, —(C═O)—NR10aR10b, —NH—C(═O)—C1-4alkyl, —NH—C(═O)—Cy3, and —O—C1-4alkyl; and wherein said heterocyclyl is optionally substituted on one nitrogen with a substituent selected from the group consisting of —C(═O)—C1-4alkyl, —C(═O)—Cy3, —(C═O)—C1-4alkyl-OH, —C(═O)—C1-4alkyl-O—C1-4alkyl, —C(═O)—C1-4alkyl-NR11aR11b, and C1-4alkyl;
Het9 as 6-membered aromatic ring containing one, heteroatoms each independently selected from O, S, and N, or a fused bicyclic C-linked 9- or 10-membered aromatic ring containing one, two or three heteroatoms each independently selected from O, S, and N; wherein said aromatic ring is optionally substituted on one nitrogen atom with C2-4alkyl; and wherein said aromatic ring is optionally substituted on one or two carbon atoms with in total one or two substituents each independently selected from the group consisting of —OH, halo, and C1-4alkyl;
Cy1 as C4-6cycloalkyl optionally substituted with two or three substituents selected from the group consisting of —OH, C1-4alkyl, —NH—S(═O)2—C1-4alkyl, —S(═O)2—C1-4alkyl, and —O—C1-4alkyl;
Cy2 as C6-7cycloalkyl; wherein said cycloalkyl is optionally substituted with one, two, three or four substituents each independently selected from the group consisting of halo, —OH, C1-4alkyl, and C1-4alkyl substituted with one or two substituents each independently selected from the group consisting of Het3a, Het6a, Het6b, and —NR9aR9b;
Cy3 as C4-7cycloalkyl; wherein said C4-7cycloalkyl is optionally substituted with one, two or three halo substituents;
R9a as Het7;—C(═O)—C1-4alkyl-Het3a; C4-6cycloalkyl substituted with, two or three substituents selected from the group consisting of, —OH, —O—C2-4alkyl, —NR11aR11b, and cyano; and C1-4alkyl substituted with one, two or three substituents selected from the group consisting of halo, —OH, —NR11aR11b, and cyano;
R9b as Het7;—C(═O)—C1-4alkyl-Het3a; C4-6cycloalkyl substituted with, two or three substituents selected from the group consisting of, —OH, —O—C2-4alkyl, —NR11aR11b, and cyano; and C1-4alkyl substituted with one, two or three substituents selected from the group consisting of halo, —OH, —NR11aR11b, and cyano;
R11a as C2-4alkyl;
R11b as C2-4alkyl;
R13b as hydrogen and C1-4alkyl;
R15a as hydrogen and C1-4alkyl;
R15b as hydrogen and C1-4alkyl;
R17a as C2-4alkyl;
R17a as C2-4alkyl;
R10a as C3-6cycloalkyl;
R10b as C3-6cycloalkyl;
R14 as Het5a; Het7; Het8a; —O—C1-4alkyl; —C(═O)NR15aR15b; C3-6cycloalkyl substituted with one, two or three substituents selected from the group consisting of —O—C1-4alkyl and halo; or C2-4alkyl substituted with one, two or three substituents selected from the group consisting of —O—C2-4alkyl, —NR13aR13b, halo, —OH, Het8a, and Cy1;
R16 as —S(═O)2—C1-4alkyl, Het5, Het7, or Het8;
The instant specification (pages 234-306) teaches compounds which are characterized as having only the following substituents:
Het is a monocyclic 6-membered aromatic ring containing one or two nitrogen atoms and optionally a carbonyl moiety; wherein said monocyclic 6-membered aromatic ring is substituted with one C3 cycloalkyl
R1b is F;
Y1 is —O—
R2 is hydrogen,
U is N;
n1 is 2
n2 is 1;
n3 is 1;
n4 is 1;
R4 is C1-5alkyl and
PNG
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71
48
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Greyscale
R5a is not exemplified;
R5b is not exemplified;
R5c is not exemplified;
R7a is not exemplified;
R7b is not exemplified;
R3 is Het1 and Cy2 ;
Rxc is not exemplified;
Rxd is not exemplified;
Het1 is a monocyclic C-linked 4- to 7-membered fully saturated heterocyclyl containing one N-atom; wherein said heterocyclyl is optionally substituted on one nitrogen with a substituent selected from the group consisting of R6, —C(═O)—Cy1, and —C(═O)—R8; and wherein said heterocyclyl is optionally substituted on one or two carbon atoms with in total two, three or four substituents each independently selected from Het6a, Het6b;
Het2 is not exemplified.
R6 is Het3 and —C(═O)—NH—Cy1;
R6a is Het4 and—C(═O)—NH—Cy1
R8 is C1-6alkyl; or C1-6alkyl substituted with one, cyano, —NR11aR11b or Het3a
Het3 is not exemplified.
Het3a is a monocyclic C-linked 4- membered fully saturated heterocyclyl containing one N
Het5 is a monocyclic C-linked 4- to 6-membered fully saturated heterocyclyl containing one or two heteroatoms each independently selected from O and S wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted with C1alkyl
Het5a is not exemplified.
Het4 is a monocyclic C-linked 6-membered aromatic ring containing two N, wherein said aromatic ring is optionally substituted with Het9
Het7 is a monocyclic C-linked 5- or 6-membered aromatic ring containing two or three heteroatoms each independently selected from O, S, and N, or a fused bicyclic C-linked 9- -membered aromatic ring containing three or four N; wherein said aromatic ring is optionally substituted on one nitrogen atom with C1-4alkyl or —(C═O)—O—C1-4alkyl; and wherein said aromatic ring is optionally substituted on one or two carbon atoms with in total one or two halo, C1-4alkyl, NR11aR11b, —NH—C(═O)—C1-4alkyl, cyano, —COOH, —NH—C(═O)—O—C1-4alkyl, —NH—C(═O)—Cy3,—(C═O)—O—C1-4alkyl, Het9, and —C(═O)—NR10aR10b;
Het6a is a monocyclic N-linked 4- to 7-membered fully saturated heterocyclyl containing one N-atom and optionally one or two additional heteroatoms each independently selected from S, and N, wherein said S-atom might be substituted to form S(═O)2; wherein said heterocyclyl is optionally substituted on one or two carbon atoms with in total one or two halo, —OH, oxo, —(C═O)—NR10aR10b, —O—C3cycloalkyl, —S(═O)2—C1-4alkyl, cyano, C1-4alkyl, —C1-4alkyl-OH, —O—C1-4alkyl, and wherein said heterocyclyl is optionally substituted on one nitrogen with —C(═O)—C1-4alkyl and —(C═O)—NR10aR10b.
Het8 is a monocyclic N-linked 6-membered fully saturated heterocyclyl containing one N-atom and optionally one additional N, wherein said heterocyclyl is optionally substituted on one—(C═O)—NR10aR10b
Het8a is not exemplified.
Het6b is a bicyclic N-linked 6- to 9- membered fully saturated heterocyclyl containing one N-atom and optionally one or two additional heteroatoms each independently selected from O, S, and N, wherein said S-atom might be substituted to form S(═O) or S(═O)2; wherein said heterocyclyl is optionally substituted on one carbon atom with in total one or two substituents each independently selected from the group consisting of C1alkyl, —OH, oxo, and —O—C1-4alkyl; and wherein said heterocyclyl is optionally substituted on one nitrogen with a —C(═O)—C1alkyl, and C1alkyl;
Het8b is not exemplified.
Het9 is a monocyclic C-linked 5- membered aromatic ring containing two or three heteroatoms selected from O and N, wherein said aromatic ring is optionally substituted on one nitrogen atom with C1-4alkyl
Cy1 is C3cycloalkyl optionally substituted with one NH—C(═O)—C1-4alkyl,
Cy2 is C3-5cycloalkyl; wherein said cycloalkyl is optionally substituted with one R6, Het6a, Het6b, —NR9aR9b
Cy3 is C3cycloalkyl optionally substituted with one substituent;
R9a is hydrogen; C1-4alkyl; C3-6cycloalkyl; —C(═O)—C1-4alkyl; —C(═O)—C3cycloalkyl; —S(═O)2—C1-4alkyl; Het5; —C1-4alkyl-R16; —C(═O)—R14; C3cycloalkyl substituted with one, halo, , —O—C1-4alkyl, and C1-4alkyl substituted with one,—O—C1-4alkyl
R9b is hydrogen; C1-4alkyl; C3-6cycloalkyl; —C(═O)—C1-4alkyl; —C(═O)—C3cycloalkyl; —S(═O)2—C1-4alkyl; Het5; —C1-4alkyl-R16; —C(═O)—R14; C3cycloalkyl substituted with one, halo, , —O—C1-4alkyl, and C1-4alkyl substituted with one,—O—C1-4alkyl
R11a is hydrogen and C1alkyl;
R11b is hydrogen and C1alkyl;
R13b is not exemplified;
R15a is not exemplified;
R15b is not exemplified;
R17a is hydrogen and C1alkyl;
R17a is hydrogen and C1alkyl;
R10a is hydrogen and C1-4alkyl;
R10b is hydrogen and C1-4alkyl;
R14 is C1alkyl substituted with one substituent selected from the group consisting of —O—C1-4alkyl, and cyano;
R16 is —C(═O)—NR17aR17b;
Therefore, the compounds and methods described in the instant specification detail only a limited number of the total substituents claimed (see substituents 1-47, above). All working examples presented in the instant specification are related to the compounds containing a fraction of the total claimed substituents (see substituents 96-145, above).
There are no working examples in the instant specification for the wide range of substituents claimed, but for which evidence of possession has not been provided (see substituents 48-95, above). Thus, the instant specification does not provide any evidence that Applicant was in possession of the claimed invention prior to the effective filing of the instant application.
Vas-Cath Inc. Mahurkar, 19 USPQ2d 1111, makes clear the "applicant must convey with reasonable clarity to those skilled in the art that, as of the filing date sought, he or she was in possession of the invention. The invention is, for purposes of the 'written description' inquiry, whatever is now claimed." (See page 1117.) The specification does not "clearly allow persons of ordinary skill in the art to recognize that [he or she] invented what is claimed." (See Vas-Cath at page 1116).
Finally, University of California v. Eli Lilly and Co., 43 USPQ2d 1398, 1404, 1405 held that: ...To fulfill the written description requirement, a patent specification must describe an invention and do so in sufficient detail that one skilled in the art can clearly conclude that "the inventor invented the claimed invention." Lockwood v. American Airlines, Inc., 107 F. 3d 1565, 1572, 41 USPQ2d 1961, 1966(1997); In re Gosteli, 872 F.2d 1008, 1012,10 USPQ2d 1614, 1618 (Fed Cir. 1989) ("[T]he description must clearly allow persons of ordinary skill in the art to recognize that [the inventor] invented what is claimed.") Thus, an applicant complies with the written description requirement "by describing the invention, with all its claimed limitations, not that which makes it obvious," and by using "such descriptive means as words, structures, figures, diagrams, formulas, etc., that set forth the claimed invention." Lockwood, 107 F.3d at 1572, 41 USPQ2d at 1966.
It is noted that the pharmaceutical art is unpredictable, requiring each embodiment to be individually assessed for physiological activity. For inventions in emerging and unpredictable technologies, or for inventions characterized by factors not reasonably predictable which are known to one of ordinary skill in the art, more evidence is required to show possession. For example, disclosure of only a method of making the invention and the function may not be sufficient to support a product claim other than a product-by-process claim. See, e.g., Fiers v. Revel, 984 F.2d at 1169, 25 USPQ2d at 1605; Amgen, 927 F.2d at 1206, 18 USPQ2d at 1021.
Thus, since Applicant has not described in adequate detail methods to synthesize compounds containing the claimed substituents, or provided evidence that said compounds have been characterized, or that they exist, an ordinary skilled artisan could not completely envisage Applicants’ invention. Moreover, it is clear that the written description requirement has not been met since Applicant has not provided any evidence that Applicant was in possession of the claimed invention prior to the effective filing of the instant application. Thus, claims 1-8, 10-13, and 15-17 of the instant application are not supported by the instant specification and thus a rejection under 35 U.S.C. § 112 (a) for failing to comply with the written description requirement is proper.
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.
Claim 10-13 and 15-17 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 15, the claim recites the limitation “The method according to claim 13.” There is insufficient antecedent basis for this limitation in the claim, because claim 13 is drawn to a compound, and not a method. Furthermore, the claim recites, “wherein the disorder is cancer.” However, there is no recitation of “disorder” or “cancer” claim 13, upon which claim 15 depends.
Therefore, claim 15 lacks antecedent basis for the aforementioned limitations. A person of ordinary skill in the art would not be able to ascertain the metes and bounds of claim 15, as it is not clear as to whether or not this claim is drawn to a method, or whether or not the method further limits the compound or pharmaceutical composition of claim 13. Furthermore, the claim is drawn to “disorder” or “cancer”
Claims 10-13 and 15-17 are drawn to a compound or pharmaceutical composition “for use” as either a medicament or in the prevention or treatment of a disease or disorder. A single claim which claims both a product and the method steps of using the product is indefinite.
2173.05(p)
II. PRODUCT AND PROCESS IN THE SAME CLAIM
A single claim which claims both an apparatus and the method steps of using the apparatus is indefinite under 35 U.S.C. 112(b) or pre-AIA 35 U.S.C. 112, second paragraph. See In re Katz Interactive Call Processing Patent Litigation, 639 F.3d 1303, 1318, 97 USPQ2d 1737, 1748-49 (Fed. Cir. 2011). In Katz, a claim directed to "[a] system with an interface means for providing automated voice messages…to certain of said individual callers, wherein said certain of said individual callers digitally enter data" was determined to be indefinite because the italicized claim limitation is not directed to the system, but rather to actions of the individual callers, which creates confusion as to when direct infringement occurs. Katz, 639 F.3d at 1318, 97 USPQ2d at 1749 (citing IPXL Holdings v. Amazon.com, Inc., 430 F.3d 1377, 1384, 77 USPQ2d 1140, 1145 (Fed. Cir. 2005), in which a system claim that recited "an input means" and required a user to use the input means was found to be indefinite because it was unclear "whether infringement … occurs when one creates a system that allows the user [to use the input means], or whether infringement occurs when the user actually uses the input means."); Ex parte Lyell, 17 USPQ2d 1548 (Bd. Pat. App. & Inter. 1990) (claim directed to an automatic transmission workstand and the method of using it held ambiguous and properly rejected under 35 U.S.C. 112, second paragraph).[AltContent: rect]
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 15 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.
Regarding claim 15, the claim is drawn to “The method according to claim 13.” However, claim 13 is drawn to a compound, and not a method. Furthermore, the claim recites, “wherein the disorder is cancer.” However, there is no recitation of “disorder” or “cancer” claim 13, upon which claim 15 depends. Therefore, claim 15 fails to further limit the subject matter or to include all the limitations of claim 13, upon which it depends.
Applicant may cancel the claim, amend the claim 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.
Correspondence
No claim is allowed.
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/SOPHIA P HIRAKIS/Examiner, Art Unit 1623
/VALERIE RODRIGUEZ-GARCIA/Primary Examiner, Art Unit 1621
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