DETAILED ACTION
Notice of Pre-AIA or AIA Status
The inventor or joint inventor should note that the instant invention, 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 39-57 are pending in the instant invention. According to the Amendments to the Claims, filed June 27, 2024, claims 1-38 were cancelled and claims 39-57 were added.
Status of Priority
This invention is a Continuation (CON) of US Application No. 17/823,889, filed August 31, 2022 and now US 12,070,457, which is a Continuation (CON) of US Application No. 17/506,220, filed October 20, 2021 and now US 11,478,474, which is a Continuation (CON) of International Application No. PCT/CN2021/076869, filed February 19, 2021, which claims priority under 35 U.S.C. § 119(a-d) to: a) CN 202110169142.0, filed February 7, 2021; and b) CN 202010104062.2, filed February 20, 2020.
Restrictions / Election of Species
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The forthcoming first Office action and prosecution on the merits includes (1) claims 39 and 40, drawn to a method for inhibiting Bruton’s tyrosine kinase (BTK) activity in a subject or in a cell, wherein the method comprises administering… or contacting the cell with… 2-(3’-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)-amino)-6-oxo-1,6-dihydro-[3,4’-bipyridin]-2’-yl)-7,7-dimethyl-7,8-dihydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one, shown to the right above; (2) claims 41-54, drawn to a method for the treatment of a disease mediated at least in part by Bruton’s tyrosine kinase (BTK)… in a subject, wherein the method comprises administering… 2-(3’-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)-amino)-6-oxo-1,6-dihydro-[3,4’-bipyridin]-2’-yl)-7,7-dimethyl-7,8-dihydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one, shown to the right above; and (3) claims 55-57, drawn to a pharmaceutical combination comprising at least one additional therapeutic agent and… 2-(3’-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)-piperazin-1-yl)pyridin-2-yl)-amino)-6-oxo-1,6-dihydro-[3,4’-bipyridin]-2’-yl)-7,7-dimethyl-7,8-dihydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one, shown to the right above, respectively.
Thus, a first Office action and prosecution on the merits of claims 39-57 is contained within.
Specification Objection - Disclosure
The inventor or joint inventor is advised to format the specification according to 37 CFR 1.77(c). Revisions should particularly address bold-type, underline, and/or upper case formatting. Appropriate correction may be required.
Specification Objection - Title
The inventor or joint inventor is reminded of the proper content of the title of the invention.
The title of the invention is not technically accurate and descriptive. A new title is required that is clearly indicative of the invention to which the claims are directed. In the revised title, the examiner suggests identifying: a) 2-(3’-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4’-bipyridin]-2’-yl)-7,7-dimethyl-7,8-dihydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one; and b) a particular utility for 2-(3’-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4’-bipyridin]-2’-yl)-7,7-dimethyl-7,8-dihydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]-pyrazin-1(6H)-one.
The following title is suggested: 2-(3’-(HYDROXYMETHYL)-1-METHYL-5-((5-(2-METHYL-4-(OXETAN-3-YL)PIPERAZIN-1-YL)PYRIDIN-2-YL)AMINO)-6-OXO-1,6-DIHYDRO-[3,4’-BIPYRIDIN]-2’-YL)-7,7-DIMETHYL-7,8-DIHYDRO-2H-CYCLOPENTA[4,5]PYRROLO[1,2-a]PYRAZIN-1(6H)-ONE AS A BTK INHIBITOR.
Appropriate correction is required.
Specification Objection - Abstract
The inventor or joint inventor is reminded of the proper content of an abstract of the disclosure.
With regard particularly to chemical patents, for compounds or compositions, the general nature of the compound or composition should be given as well as the use thereof, e.g., The compounds are of the class of alkyl benzene sulfonyl ureas, useful as oral anti-diabetics. Exemplification of a species could be illustrative of members of the class. For processes, the reactions, reagents and process conditions should be stated, generally illustrated by a single example, unless variations are necessary. See MPEP § 608.01(b), Section B.
The abstract of the disclosure is objected to because it fails to exemplify any members or formulae illustrative of its class. Correction is required. See MPEP § 608.01(b).
The examiner suggests incorporating the structure of 2-(3’-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4’-bipyridin]-2’-yl)-7,7-dimethyl-7,8-dihydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one into the abstract, to overcome this objection.
Claim Objections
Claim 39 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation(s):
39. A method for inhibiting Bruton’s tyrosine kinase (BTK) activity in a cell, wherein the method comprises contacting the cell with an effective amount of a compound of the following formula:
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or a pharmaceutically acceptable salt, deuterated isotope, or stereoisomer thereof.
58. A method for inhibiting Bruton’s tyrosine kinase (BTK) activity in a subject, wherein the method comprises administering to the subject in need thereof a therapeutically effective amount of a compound of the following formula:
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or a pharmaceutically acceptable salt, deuterated isotope, or stereoisomer thereof.
Appropriate correction is required. See MPEP § 2173.02.
Claim 40 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation(s):
40. The method of claim 39, wherein the method comprises contacting the cell with an effective amount of a compound, or stereoisomer thereof, of the following formula:
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or a pharmaceutically acceptable salt or deuterated isotope thereof.
59. The method of claim 58, wherein the method comprises administering to the subject in need thereof a therapeutically effective amount of a compound, or stereoisomer thereof, of the following formula:
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or a pharmaceutically acceptable salt or deuterated isotope thereof.
Appropriate correction is required. See MPEP § 2173.02.
Claim 41 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
A method for the treatment of a disease mediated at least in part by Bruton’s tyrosine kinase (BTK) in a subject, wherein the method comprises administering to the subject in need thereof a therapeutically effective amount of a compound of the following formula:
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or a pharmaceutically acceptable salt, deuterated isotope, or stereoisomer thereof;
wherein the disease mediated at least in part by Bruton’s tyrosine kinase (BTK) is selected from the group consisting of an autoimmune disease, cancer, graft versus host disease, and an inflammatory disease.
Appropriate correction is required. See MPEP § 2173.02.
Claim 42 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 41, wherein the method comprises administering to the subject in need thereof a therapeutically effective amount of a compound, or stereoisomer thereof, of the following formula:
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or a pharmaceutically acceptable salt or deuterated isotope thereof.
Appropriate correction is required. See MPEP § 2173.02.
Claim 43 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 42, wherein the autoimmune disease, graft versus host disease, or inflammatory disease is selected from the group consisting of an allergic disease, antineutrophil cytoplasmic antibody vasculitis, arthritis, asthma, autoimmune hemolytic anemia, chronic obstructive pulmonary disease, Crohn’s disease, a disease associated with kidney transplantation, dermatitis, idiopathic thrombocytopenic purpura, inflammation associated with immunosuppression, local inflammation, lupus erythematosus, multiple sclerosis, organ-graft rejection, osteoporosis, pemphigus vulgaris, psoriasis, scleroderma, sicca syndrome, Sjögren’s syndrome, systemic inflammation, and ulcerative colitis.
Appropriate correction is required. See MPEP § 2173.02.
Claim 46 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 42, wherein the cancer is a hematologic malignancy or a solid tumor.
Appropriate correction is required. See MPEP § 2173.02.
Claim 47 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 46, wherein the hematologic malignancy or solid tumor is selected from the group consisting of leukemia, lymphoma, and myeloma.
Appropriate correction is required. See MPEP § 2173.02.
Claim 48 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The method of claim 42, wherein the cancer is selected from the group consisting of acute lymphoblastic leukemia, B-cell lymphoma, a B-cell malignancy, Burkitt’s lymphoma, follicular lymphoma, hairy cell leukemia, Hodgkin’s lymphoma, human acute monocytic leukemia, lymphoblastic lymphoma, lymphocytic leukemia, mantle cell lymphoma, marginal zone lymphoma, myelodysplastic syndrome, myelogenous leukemia, myeloma, non-Hodgkin’s lymphoma, small lymphocytic lymphoma, and Waldenstrom’s macroglobulinemia.
Appropriate correction is required. See MPEP § 2173.02.
Claim 55 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
A pharmaceutical combination comprising at least one additional therapeutic agent and a compound of the following formula:
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or a pharmaceutically acceptable salt or deuterated isotope thereof.
Appropriate correction is required. See MPEP § 2173.02.
Claim Rejections - Obviousness-type Double Patenting
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. A nonstatutory obviousness-type double patenting rejection is appropriate where the conflicting claims are not identical, but at least one examined invention claim is not patentably distinct from the reference claims because the examined invention claim is either anticipated by, or would have been obvious over, the reference claims. {See In re Berg, 140 F.3d 1428, 46 USPQ2d 1226 (Fed. Cir. 1998); 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)}.
US Patent No. 11,478,474
Consequently, claims 39-57 are rejected on the ground of nonstatutory obviousness-type double patenting as being unpatentable over claims 1-15 of US Patent No. 11,478,474. Although the conflicting claims are not identical, they are not patentably distinct from each other because claim 1 in US 11,478,474 recites 2-(3’-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4’-bipyridin]-2’-yl)-7,7-dimethyl-7,8-dihydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one, shown to the left below, which
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is administered within the instantly recited method for inhibiting Bruton’s tyrosine kinase (BTK) activity in a subject or in a cell, wherein the method comprises administering… or contacting the cell with… 2-(3’-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)-pyridin-2-yl)-amino)-6-oxo-1,6-dihydro-[3,4’-bipyridin]-2’-yl)-7,7-dimethyl-7,8-dihydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one, shown to the left above.
The inventor or joint inventor should note that [T]he discovery of a previously unappreciated property of a prior art compound, or of a scientific explanation for the prior art’s functioning, does not render the old compound patentably new to the discoverer. {See Atlas Powder Co. v. Ireco Inc., 190 F.3d 1342, 1347, 51 USPQ2d 1943, 1947 (Fed. Cir. 1999)}.
Similarly, the inventor or joint inventor should further note that [T]he claiming of a new use, new function or unknown property which is inherently present in the prior art does not necessarily make the claim patentable. {See In re Best, 562 F.2d 1252, 1254, 195 USPQ 430, 433 (CCPA 1977); and In re Crish, 393 F.3d 1253, 1258, 73 USPQ2d 1364, 1368 (Fed. Cir. 2004)}.
Likewise, the inventor or joint inventor should note that [W]hen the claim recites using an old compound and the use is directed to a result or property of that compound, then the claim is anticipated. {See In re May, 574 F.2d 1082, 1090, 197 USPQ 601, 607 (CCPA 1978); and In re Tomlinson, 363 F.2d 928, 150 USPQ 623 (CCPA 1966)}.
Next, the inventor or joint inventor should further note that [P]roducts of identical chemical composition may not have mutually exclusive properties. A chemical composition and its properties are inseparable. Therefore, if the prior art teaches the identical chemical structure, the properties the inventor or joint inventor discloses and/or claims are necessarily present. {See In re Spada, 911 F.2d 705, 709, 15 USPQ2d 1655, 1658 (Fed. Cir. 1990)}.
Then, the inventor or joint inventor should further note that [A] claim to a method of using a composition is not patentably distinct from an earlier claim to the identical composition in a patent disclosing the identical use. {See Sun Pharmaceuticals Industries Ltd. v. Eli Lilly and Co., 611 F.3d 1381, 95 USPQ2d 1797 (Fed. Cir. 2010); Pfizer, Inc. v. Teva Pharmaceuticals USA, Inc., 518 F.3d 1353, 1363, 86 USPQ2d 1001 (Fed. Cir. 2008); and Geneva
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Pharmaceuticals, Inc. v. GlaxoSmithKline PLC,
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349 F.3d 1373, 68 USPQ2d 1865, (Fed. Cir. 2003)}.
Moreover, the inventor or joint inventor should further note that [A] pure optical isomer is not patentable over the racemic mixture unless it possesses properties not possessed by the racemic mixture. {See In re Anthony, 414 F.2d 1383, 162 USPQ 594, (CCPA 1969)}.
Furthermore, the inventor or joint inventor should also note that [I]t is obvious to add a carrier or solvent to an unpatentable compound. {See Ex parte Douros and Vanderweff, 163 USPQ 667, (BPAI 1968)}.
US Patent No. 12,070,457
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Claims 39-57 are further rejected on the ground of nonstatutory obviousness-type double patenting as being unpatentable over at least claims 1-8, 10-16 and 20-38 of US Patent No. 12,070,457. Although the conflicting claims are not identical, they are not patentably distinct from each other because claim 1 in US 12,070,457 recites a substituted heteraoryl of the formula (I),
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shown to the left above, where Cy is shown to the left below, wherein R11 = -CH3, U = CR12, where R12 = -H, and V = CR12, where R12 = -H; R1 and R2, together with the carbon atoms
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to which they are attached, form formula (I-1), shown to the right below, wherein m = 2 and at C-7, each R6 = -CH3; R3 = -H; R4 = -CH2OH; R5 = -pyridin-2-yl, substituted at C-5 with 2-methyl-4-(oxetan-3-yl)piperazin-1-yl; X1 = CH; X2 = CH; X3 = N; X4 = C; Y1 = CR10, where R10 = -H; and Y2 = CR10, where R10 = -H, respectively, which is administered within the instantly recited method for inhibiting Bruton’s tyrosine kinase (BTK) activity in a subject or in a cell, wherein the method comprises administering… or contacting the
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cell with… 2-(3’-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)-pyridin-2-yl)-amino)-6-oxo-1,6-dihydro-[3,4’-bipyridin]-2’-yl)-7,7-dimethyl-7,8-dihydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one, shown to the right.
The inventor or joint inventor should note that [T]he discovery of a previously unappreciated property of a prior art compound, or of a scientific explanation for the prior art’s functioning, does not render the old compound patentably new to the discoverer. {See Atlas Powder Co. v. Ireco Inc., 190 F.3d 1342, 1347, 51 USPQ2d 1943, 1947 (Fed. Cir. 1999)}.
Similarly, the inventor or joint inventor should further note that [T]he claiming of a new use, new function or unknown property which is inherently present in the prior art does not necessarily make the claim patentable. {See In re Best, 562 F.2d 1252, 1254, 195 USPQ 430, 433 (CCPA 1977); and In re Crish, 393 F.3d 1253, 1258, 73 USPQ2d 1364, 1368 (Fed. Cir. 2004)}.
Likewise, the inventor or joint inventor should note that [W]hen the claim recites using an old compound and the use is directed to a result or property of that compound, then the claim is anticipated. {See In re May, 574 F.2d 1082, 1090, 197 USPQ 601, 607 (CCPA 1978); and In re Tomlinson, 363 F.2d 928, 150 USPQ 623 (CCPA 1966)}.
Next, the inventor or joint inventor should further note that [P]roducts of identical chemical composition may not have mutually exclusive properties. A chemical composition and its properties are inseparable. Therefore, if the prior art teaches the identical chemical structure, the properties the inventor or joint inventor discloses and/or claims are necessarily present. {See In re Spada, 911 F.2d 705, 709, 15 USPQ2d 1655, 1658 (Fed. Cir. 1990)}.
Then, the inventor or joint inventor should further note that [A] claim to a method of using a composition is not patentably distinct from an earlier claim to the identical composition in a patent disclosing the identical use. {See Sun Pharmaceuticals Industries Ltd. v. Eli Lilly and Co., 611 F.3d 1381, 95 USPQ2d 1797 (Fed. Cir. 2010); Pfizer, Inc. v. Teva Pharmaceuticals USA, Inc., 518 F.3d 1353, 1363, 86 USPQ2d 1001 (Fed. Cir. 2008); and Geneva
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Pharmaceuticals, Inc. v. GlaxoSmithKline PLC,
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349 F.3d 1373, 68 USPQ2d 1865, (Fed. Cir. 2003)}.
Moreover, the inventor or joint inventor should further note that [A] pure optical isomer is not patentable over the racemic mixture unless it possesses properties not possessed by the racemic mixture. {See In re Anthony, 414 F.2d 1383, 162 USPQ 594, (CCPA 1969)}.
Furthermore, the inventor or joint inventor should also note that [I]t is obvious to add a carrier or solvent to an unpatentable compound. {See Ex parte Douros and Vanderweff, 163 USPQ 667, (BPAI 1968)}.
Here, the inventor or joint inventor should further note that that a timely filed terminal disclaimer in compliance with 37 CFR 1.321(c) or 37 CFR 1.321(d) may be used to overcome an actual or provisional rejection based on a nonstatutory double patenting ground, provided the conflicting invention or patent either is shown to be commonly owned with this invention, or claims an invention made as a result of activities undertaken within the scope of a joint research agreement.
Now, the inventor or joint inventor should further note that the USPTO internet Web site contains terminal disclaimer forms which may be used, and the inventor or joint inventor is encouraged to visit http://www.uspto.gov/forms/, where (i) the filing date of the invention will determine what form should be used, and (ii) a web-based eTerminal Disclaimer may be filled out completely online using web-screens, respectively.
Also, the inventor or joint inventor should further note that an eTerminal Disclaimer that meets all requirements is auto-processed and approved immediately upon submission.
Finally, for more information about eTerminal Disclaimers, the inventor or joint inventor should refer to http://www.uspto.gov/patents/process/file/efs/guidance/eTD-info-I.jsp.
Allowable Subject Matter
No claims are allowed.
Conclusion
Any inquiry concerning this communication or earlier communications from the examiner should be directed to DOUGLAS M. WILLIS, whose telephone number is 571-270-5757. The examiner may normally be reached on Monday thru Thursday from 8:00-6:00 EST. The examiner is also available on alternate Fridays.
If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Mr. Jeffrey Murray, may be reached on 571-272-9023. The fax phone number for the organization where this invention or proceeding is assigned is 571-273-8300.
Information regarding the status of an invention may be obtained from Patent Center. For more information about Patent Center, see https://www.uspto.gov/patents/apply/patent-center. Should you have questions on access to Patent Center, contact the Patent Electronic Business Center (PEBC) at 866-217-9197 (toll-free) or ebc@uspto.gov.
/DOUGLAS M WILLIS/
Primary Examiner, Art Unit 1624
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