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 1-21 are pending in the instant invention.
Status of Priority
This invention claims priority under 35 U.S.C. § 119(e) to US Provisional Application No. 63/472,020, filed June 9, 2023.
Restrictions / Election of Species
PNG
media_image1.png
247
320
media_image1.png
Greyscale
The inventor’s or joint inventor’s provisional election of the following, without traverse, in the reply filed on July 6, 2025, is acknowledged: a) Group II - claims 6-16 and 18-21; and b) crystalline form of upadacitinib comprising upadacitinib and magnesium chloride- p. 27, upadacitinib Form APO-1, Example 1, shown to the right above, and hereafter referred to as (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide (Upadacitinib) magnesium chloride co-crystal. Claims 6-13 and 18-20 read on the elected species. Affirmation of this election must be made by the inventor or joint inventor in replying to this Office action.
Similarly, the inventor or joint inventor should further note that the requirement is still deemed proper and is therefore made FINAL.
Likewise, the inventor or joint inventor should further note that the elected species, shown to the left above, was found to be free of the prior art. Thus, the examiner has expanded the forthcoming prosecution to include all claims relevant to the genus of Group II, for a first Office action and prosecution on the merits.
Moreover, the inventor or joint inventor should further note that claims 1-5 and 17 were withdrawn from further consideration, pursuant to 37 CFR 1.142(b), as being drawn to a nonelected or cancelled invention, there being no allowable generic or linking claim.
Thus, a first Office action and prosecution on the merits of claims 6-16 and 18-21 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 should be brief, but technically accurate and descriptive and should contain fewer than 500 characters. See 37 CFR 1.72(a) and MPEP § 606.
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 additionally identifying a particular utility for the solid forms of upadacitinib comprising upadacitinib and magnesium chloride.
The following title is suggested: SOLID FORMS OF UPADACITINIB FOR THE TREAMENT OF JANUS KINASE (JAK)-ASSOCIATED CONDITIONS.
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 the solid form of upadacitinib comprising upadacitinib and magnesium chloride into the abstract, to overcome this objection.
Claim Objections
Claim 6 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b), the existing recitation should be replaced with the following recitation:
A crystalline form of upadacitinib comprising upadacitinib and magnesium chloride of the following formula:
PNG
media_image2.png
632
820
media_image2.png
Greyscale
;
wherein the crystalline form is characterized by a powder X-ray diffraction (PXRD) diffractogram comprising characteristic peaks at diffraction angles (º2q) of 4.3º ± 0.20º, 5.5º ± 0.20º, and 21.1º ± 0.20º.
Appropriate correction is required. See MPEP § 2173.02.
Claim 7 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b), the existing recitation should be replaced with the following recitation:
The crystalline form of claim 6, wherein the molar ratio of upadacitinib to magnesium chloride is in the range of from 1:0.4 to 1:1.
Appropriate correction is required. See MPEP § 2173.02.
Claim 10 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation:
The crystalline form of claim 6, wherein the crystal form is further characterized by a powder X-ray diffraction (PXRD) diffractogram comprising at least three additional characteristic peaks at diffraction angles (º2q) selected from the group consisting of 8.1º ± 0.20º, 8.7º ± 0.20º, 13.3º ± 0.20º, 15.7º ± 0.20º, 17.1º ± 0.20º, and 23.6º ± 0.20º.
Appropriate correction is required. See MPEP § 2173.02.
Claim 11 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation:
The crystalline form of claim 6, wherein the crystal form is further characterized by a powder X-ray diffraction (PXRD) diffractogram comprising additional characteristic peaks at diffraction angles (º2q) of 8.1º ± 0.20º, 8.7º ± 0.20º, 13.3º ± 0.20º, 15.7º ± 0.20º, 17.1º ± 0.20º, and 23.6º ± 0.20º.
Appropriate correction is required. See MPEP § 2173.02.
Claim 12 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation:
The crystalline form of claim 6, wherein the crystal form is further characterized by a powder X-ray diffraction (PXRD) diffractogram as shown in Figure 1.
Appropriate correction is required. See MPEP § 2173.02.
Claim 13 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation:
The crystalline form of claim 6, wherein the crystal form is further characterized by a powder X-ray diffraction (PXRD) diffractogram as shown in Figure 9.
Appropriate correction is required. See MPEP § 2173.02.
Claim 14 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and to attain compliance with the Requirement for Restriction/Election of Species, mailed on May 20, 2026, the existing recitation should be replaced with the following recitation:
An amorphous solid dispersion of upadacitinib comprising upadacitinib and magnesium chloride of the following formula:
PNG
media_image2.png
632
820
media_image2.png
Greyscale
.
Appropriate correction is required. See MPEP § 2173.02.
Claim 15 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b), the existing recitation should be replaced with the following recitation:
The amorphous solid dispersion of claim 14, wherein the molar ratio of upadacitinib to magnesium chloride is in the range of from 1:0.4 to 1:1.
Appropriate correction is required. See MPEP § 2173.02.
Claim 16 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b), the existing recitation should be replaced with the following recitation:
The amorphous solid dispersion of claim 15, wherein the molar ratio of upadacitinib to magnesium chloride is in the range of from 1:0.4 to 1:0.6.
Appropriate correction is required. See MPEP § 2173.02.
Claim 18 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
A pharmaceutical composition comprising at least one pharmaceutically acceptable excipient and the crystalline form of claim 6.
Appropriate correction is required. See MPEP § 2173.02.
Claim 19 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The pharmaceutical composition of claim 18, wherein the pharmaceutical composition is formulated as a capsule or a tablet.
Appropriate correction is required. See MPEP § 2173.02.
Claim 20 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
The pharmaceutical composition of claim 19, wherein the tablet is an extended-release tablet.
Appropriate correction is required. See MPEP § 2173.02.
Claim 21 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation:
A pharmaceutical composition comprising at least one pharmaceutically acceptable excipient and the amorphous solid dispersion of claim 14.
Appropriate correction is required. See MPEP § 2173.02.
Claim Rejections - 35 U.S.C. § 112(b)
The following is a quotation of the second paragraph of 35 U.S.C. § 112:
(b) CONCLUSION. The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the inventor or joint inventor regards as the invention.
Claims 6-8 and 18-20 are rejected under 35 U.S.C. § 112(b) as being indefinite for failing to set forth the subject matter which the inventor or joint inventor regards as the invention.
The inventor or joint inventor should note that claim 9 recites the physicochemical property, A crystalline form of upadacitinib comprising upadacitinib and magnesium chloride in line 1 of the claim.
Similarly, the inventor or joint inventor should further note that the aforementioned physicochemical property renders the instant invention ambiguous, vague, incoherent, opaque and/or otherwise unclear to the examiner and fails to meet the statutory requirements of 35 U.S.C. § 112(b), since the limitation merely states a physicochemical property (i.e. crystalline) without providing any clarity regarding how the physicochemical property is imparted.
Likewise, the inventor or joint inventor should further note that the instantly recited crystalline physicochemical property does not appear to emanate from and/or does not appear to be an inherent or salient property of the instantly recited form of upadacitinib comprising upadacitinib and magnesium chloride.
Next, the inventor or joint inventor should further note that the examiner is uncertain whether the instantly recited form of upadacitinib comprising upadacitinib and magnesium chloride requires an additional unrecited component to be admixed therewith, such as a stabilizer, bulking agent, solvent, or buffer, to impart the crystalline physicochemical property.
Consequently, the inventor or joint inventor should further note that since the instantly recited form of upadacitinib comprising upadacitinib and magnesium chloride incorporates the aforementioned ambiguous, vague, incoherent, opaque and/or otherwise unclear crystalline physicochemical property, the instantly recited form of upadacitinib comprising upadacitinib and magnesium chloride is rendered indefinite under 35 U.S.C. § 112(b), since one of ordinary skill in the art may not reasonably determine the metes and bounds of the instantly recited form of upadacitinib comprising upadacitinib and magnesium chloride due to an inability to establish the metes and bounds encompassed by the crystalline physicochemical property.
Then, the inventor or joint inventor should further note that [A] claim which omits matter disclosed to be essential to the invention, as described in the specification or in other statements of record, may also be rejected under 35 U.S.C. § 112(a), as not enabling. {See In re Mayhew, 527 F.2d 1229, 188 USPQ 356 (CCPA 1976); and MPEP § 2164.08(c)}.
Moreover, the inventor or joint inventor should further note that [C]laims which depend from indefinite claims are also indefinite. {See Ex parte Cordova, 10 USPQ 2d 1949, 1952 (PTO Bd. App. 1989)}.
The examiner suggests amending the claims, particularly as stated in the section above entitled Claim Objections, to overcome this rejection.
Claims 7-13 are rejected under 35 U.S.C. § 112(b) as being indefinite for failing to set forth the subject matter which the inventor or joint inventor regards as the invention.
The inventor or joint inventor should note that the term, about, in claim 7, is a relative term which renders the claim indefinite. The term, about, is not defined by the claim, the specification does not provide an adequate standard for ascertaining the requisite degree, and one of ordinary skill in the art would not be reasonably apprised of the metes and bounds of the invention. The specification fails to adequately define the term, about. Similarly, the meaning of a term cannot depend on the unrestrained, subjective opinion of the inventor or joint inventor practicing the invention. Moreover, neither the specification, nor the claim, explicitly limits the invention to any specifically disclosed or recited embodiments. Consequently, the crystalline form of upadacitinib comprising upadacitinib and magnesium chloride has been rendered indefinite by the use of the term, about. {See Ortho-McNeil Pharm., Inc. v. Caraco Pharm. Labs., Ltd., 476 F.3d 1321, 1326, 81 USPQ2d 1427, 1432 (Fed. Cir.2007); W. L. Gore & Associates, Inc. v. Garlock, Inc., 721 F.2d 1540, 220 USPQ 303 (Fed. Cir. 1983); Amgen, Inc. v. Chugai Pharmaceutical Co., 927 F.2d 1200, 18 USPQ2d 1016 (Fed. Cir. 1991); and MPEP § 2173.05(b)}.
Moreover, the inventor or joint inventor should further note that [C]laims which depend from indefinite claims are also indefinite. {See Ex parte Cordova, 10 USPQ 2d 1949, 1952 (PTO Bd. App. 1989)}.
The examiner suggests amending the claims, particularly as stated in the section above entitled Claim Objections, to overcome this rejection.
Claim 12 is further rejected under 35 U.S.C. § 112(b) as being indefinite for failing to set forth the subject matter which the inventor or joint inventor regards as the invention.
The inventor or joint inventor should note that the term, substantially, is a relative term which renders the claim indefinite. The term, substantially, is not defined by the claim, the specification does not provide an adequate standard for ascertaining the requisite degree, and one of ordinary skill in the art would not be reasonably apprised of the metes and bounds of the invention. The specification fails to adequately define the term, substantially. Similarly, the meaning of a term cannot depend on the unrestrained, subjective opinion of the inventor or joint inventor practicing the invention. Moreover, neither the specification, nor the claim, explicitly limits the invention to any specifically disclosed or recited embodiments. Consequently, the crystalline form of upadacitinib comprising upadacitinib and magnesium chloride has been rendered indefinite by the use of the term, substantially. {See In re Nehrenberg, 280 F.2d 161, 126 USPQ 383 (CCPA 1960); In re Mattison, 509 F.2d 563, 184 USPQ484 (CCPA 1975); Andrew Corp. v. Gabriel Electronics, 847 F.2d 819, 6 USPQ2d 2010 (Fed. Cir.1988); and MPEP § 2173.05(b)}.
The examiner suggests amending the claim, particularly as stated in the section above entitled Claim Objections, to overcome this rejection.
Claim 13 is further rejected under 35 U.S.C. § 112(b) as being indefinite for failing to set forth the subject matter which the inventor or joint inventor regards as the invention.
The inventor or joint inventor should note that the term, substantially, is a relative term which renders the claim indefinite. The term, substantially, is not defined by the claim, the specification does not provide an adequate standard for ascertaining the requisite degree, and one of ordinary skill in the art would not be reasonably apprised of the metes and bounds of the invention. The specification fails to adequately define the term, substantially. Similarly, the meaning of a term cannot depend on the unrestrained, subjective opinion of the inventor or joint inventor practicing the invention. Moreover, neither the specification, nor the claim, explicitly limits the invention to any specifically disclosed or recited embodiments. Consequently, the crystalline form of upadacitinib comprising upadacitinib and magnesium chloride has been rendered indefinite by the use of the term, substantially. {See In re Nehrenberg, 280 F.2d 161, 126 USPQ 383 (CCPA 1960); In re Mattison, 509 F.2d 563, 184 USPQ484 (CCPA 1975); Andrew Corp. v. Gabriel Electronics, 847 F.2d 819, 6 USPQ2d 2010 (Fed. Cir.1988); and MPEP § 2173.05(b)}.
The examiner suggests amending the claim, particularly as stated in the section above entitled Claim Objections, to overcome this rejection.
Claims 15 and 16 are rejected under 35 U.S.C. § 112(b) as being indefinite for failing to set forth the subject matter which the inventor or joint inventor regards as the invention.
The inventor or joint inventor should note that the term, about, in claims 15 and 16, respectively, is a relative term which renders the claims indefinite. The term, about, is not defined by the claims, the specification does not provide an adequate standard for ascertaining the requisite degree, and one of ordinary skill in the art would not be reasonably apprised of the metes and bounds of the invention. The specification fails to adequately define the term, about. Similarly, the meaning of a term cannot depend on the unrestrained, subjective opinion of the inventor or joint inventor practicing the invention. Moreover, neither the specification, nor the claim, explicitly limits the invention to any specifically disclosed or recited embodiments. Consequently, the amorphous form of upadacitinib comprising upadacitinib and magnesium chloride has been rendered indefinite by the use of the term, about. {See Ortho-McNeil Pharm., Inc. v. Caraco Pharm. Labs., Ltd., 476 F.3d 1321, 1326, 81 USPQ2d 1427, 1432 (Fed. Cir.2007); W. L. Gore & Associates, Inc. v. Garlock, Inc., 721 F.2d 1540, 220 USPQ 303 (Fed. Cir. 1983); Amgen, Inc. v. Chugai Pharmaceutical Co., 927 F.2d 1200, 18 USPQ2d 1016 (Fed. Cir. 1991); and MPEP § 2173.05(b)}.
Moreover, the inventor or joint inventor should further note that [C]laims which depend from indefinite claims are also indefinite. {See Ex parte Cordova, 10 USPQ 2d 1949, 1952 (PTO Bd. App. 1989)}.
The examiner suggests amending the claims, particularly as stated in the section above entitled Claim Objections, to overcome this rejection.
Claim Rejections - 35 U.S.C. § 112(d)
The following is a quotation of the fourth paragraph of 35 U.S.C. § 112:
(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.
Claim 8 is rejected under 35 U.S.C. § 112(d) 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.
The inventor or joint inventor should note that claim 8 is rejected under 35 U.S.C. § 112(d) because the recitation of a physicochemical property for a compound must result in a further structural limitation in the compound, in order to be further limiting. In the instant dependent claim, the crystalline form of upadacitinib comprising upadacitinib and magnesium chloride, as recited in claim 7, is a hydrate. Consequently, since the physicochemical property of the crystalline form of upadacitinib comprising upadacitinib and magnesium chloride, as recited in claim 7, whereby the crystalline form of upadacitinib comprising upadacitinib and magnesium chloride is a hydrate, fails to result in a further structural limitation to the crystalline form of upadacitinib comprising upadacitinib and magnesium chloride, as recited in claim 7, and/or fails to include all the limitations of the crystalline form of upadacitinib comprising upadacitinib and magnesium chloride, as recited in claim 7, it is not given patentable weight and thus, renders the instant dependent claim improperly dependent under 35 U.S.C. § 112(d). {See MPEP § 2111.02; and 37 CFR 1.75(c)}.
Similarly, the inventor or joint inventor should further note that the U.S. Court of Appeals for the Federal Circuit indicated that although the requirements of 35 U.S.C. § 112(d) are related to matters of form, non-compliance with 35 U.S.C. § 112(d) renders the claim unpatentable just as non-compliance with other subsections of 35 U.S.C. § 112 would. {See Pfizer, Inc. v. Ranbaxy Labs., Ltd., 457 F.3d 1284, 1291-92 (Fed. Cir. 2006)}.
Moreover, the inventor or joint inventor should further note that if a dependent claim does not comply with the requirements of 35 U.S.C. § 112(d) the dependent claim should be rejected under 35 U.S.C. § 112(d) as unpatentable rather than objecting to the claim. {See also MPEP § 608.01(n), Section III, Infringement Test for dependent claims}.
The examiner suggests the inventor or joint inventor (1) cancel the dependent claim, (2) amend the dependent claim to place the dependent claim in proper dependent form, (3) rewrite the dependent claim in independent form, or (4) present a sufficient showing that the dependent claim complies with the statutory requirements, to overcome this rejection.
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
Prosecution Insights