Notice of Pre-AIA or AIA Status
The present application, filed on or after March 16, 2013, is being examined under the first inventor to file provisions of the AIA .
DETAILED ACTION
Status of Claims
Claims 1, 7-8, 13, 15, 19, 20, 33, 36, 40, 44, 46-47, 55, 57, 63, 65, 67, 69, and 71 are pending.
Election/Restrictions
Applicants’ election of Group I and the following compound:
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(enobosarm), as a species of a selective androgen receptor modulator (SARM) in the reply filed on 3/2/2026 is acknowledged. The election was made without traverse.
Accordingly, claims 20, 33, 36, 40, 44, 57, 63, 65, 67, 69, and 71 are withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a nonelected group or species, there being no allowable generic or linking claim. Claims 1, 7-8, 13, 15, 19, 46-47, and 55 are under examination in the instant office action.
During the search for the elected species, other selective androgen receptor modulator such as bicalutamide (BLT) was found and therefore the examination was expanded to include BLT.
Claim Objections
Claims 1 and 47 are objected to because of the following informalities: typographical errors.
In claim 1, the word “select” before “androgen receptor modulator” in line 2 should be corrected to -- selective --. In addition, the same typographical errors should be corrected in the specification.
In claim 47, “of” is missing between “The composition” and “claim 1” in line 1.
Claim Rejections - 35 USC § 112 (b)
The following is a quotation of 35 U.S.C. 112(b):
(b) CONCLUSION.—The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the inventor or a joint inventor regards as the invention.
The following is a quotation of 35 U.S.C. 112 (pre-AIA ), second paragraph:
The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the applicant regards as his invention.
Claims 1, 7-8, 13, 15, 19, 46-47, and 55 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 pre-AIA the applicant regards as the invention. All the dependent claims are included.
Claim 1 recites “A sustained release composition comprising one or more particles comprising a polymer and an amount of a select androgen receptor modulator (SARN) and a pharmaceutically acceptable carrier; wherein: the particles comprise a synthetic polymer, the synthetic polymer comprising 85 to 95% poly lactic-co-glycolic acid (PLGA).
A broad range or limitation together with a narrow range or limitation that falls within the broad range or limitation (in the same claim) may be considered indefinite if the resulting claim does not clearly set forth the metes and bounds of the patent protection desired. See MPEP § 2173.05(c).
In the present instance, claim 1 recites the broad recitation “particles comprising a polymer” in line 2, and the claim also recites “particles comprising a synthetic polymer”, which is the narrower statement of said “polymer” as a “polymer” encompasses natural polymer as well as synthetic polymer. The claim(s) are considered indefinite because there is a question or doubt as to whether the particles can comprise any polymers including natural polymers or require comprising only a synthetic polymer, which is PLGA. Clarification is required.
Also, it is unclear whether the percentage of PLGA in the recitation of “the synthetic polymer comprising 85 to 95% poly lactic-co-glycolic acid” is based on the total weight of particles or total weight of synthetic polymers, which may comprise additional synthetic polymer other than PLGA. Also, it is unclear whether the “percentage (%)” in the claims refers to mass fraction (% w/w), mass concentration (% w/v) or volume concentration (% v/v). Thus, it renders the claims indefinite. Clarification is required.
For the examination purpose, it is treated as if it recites “A sustained release composition comprising one or more particles comprising a polymer and an amount of a select androgen receptor modulator (SARN) and a pharmaceutically acceptable carrier; wherein the polymer is polylactic-co-glycolic acid (PLGA) and the particles comprise about 85 to 95% w/w PLGA” in light of the specification (see [0008]).
In addition, claim 13 recites “C-6, S-23, BA321, FL442, MK-45412, LGD226, S-40542, S-1, S-4, GLPG0492, GTx-024 (enobosarm), LY2452473, GSK2881078, GSK2849466, PF-06260414, or LGD-4044”. They are proprietary names (brand or trade names) or code names, which may not be well-known. Accordingly, one of ordinary skill in the art would not ascertain what they refer to without their chemical names. Also, the scope of the claim is uncertain since the trademark or trade name cannot be used properly to describe any particular material or product. In fact, the value of a trademark would be lost to the extent that it became the generic name of a product, rather than used as an identification of a source or origin of a product. Thus, the use of a trademark or trade name in a claim to describe a material or product would not only render a claim indefinite, but would also constitute an improper use of the trademark or trade name. See MPEP 2173.05 (u).
It is advised to provide their full chemical names.
Claim 46 recites “The composition or method of claim 1” in line 1. There is insufficient antecedent basis for “method” in the claim 1. Applicant is advised to delete “or method”.
Claim 55 recites “The composition or method of claim 47” in line 1. There is insufficient antecedent basis for “method” in the claim 1. Applicant is advised to delete “or method”.
Claim Rejections - 35 USC § 102
The following is a quotation of the appropriate paragraphs of 35 U.S.C. 102 that form the basis for the rejections under this section made in this Office action:
A person shall be entitled to a patent unless –
(a)(1) the claimed invention was patented, described in a printed publication, or in public use, on sale or otherwise available to the public before the effective filing date of the claimed invention.
(a)(2) the claimed invention was described in a patent issued under section 151, or in an application for patent published or deemed published under section 122(b), in which the patent or application, as the case may be, names another inventor and was effectively filed before the effective filing date of the claimed invention.
Claims 1 and 46 are rejected under 35 U.S.C. 102(a)(1) as being anticipated by Guo et al. (EXPERIMENTAL AND THERAPEUTIC MEDICINE 10: 2305-2310, 2015) as evidenced by US 2014/0107088 (hereafter, Wilsey).
Guo et al. teaches bicalutamide-loaded PLGA nanoparticles, which provide sustained drug-release (sustained release composition) (abstract, p3, lines 3-15, claims 8 and 11).
Guo et al. disclose that BLT-loaded PLGA nanoparticles were prepared by a nanoprecipitation method as follow: 5 mg BLT and 50 mg PLGA were dissolved in 10 ml acetone and dissolved by vortexing and sonication; to this solution, 0.5% poloxamer 407 solution (10 ml) was added drop-by-drop in a controlled manner; the solution was stirred at a high speed in a magnetic stirrer and kept overnight at room temperature, following evaporation of the organic solvents, drug-loaded nanoparticles were collected by centrifuging at 5,000 × g for 20 min at 37°C; and the supernatant was removed and the pellet was re-dispersed with water (pharmaceutical acceptable carrier) and stored until use. The resulting nanoparticles comprise 5 mg BLT and 50 mg PLGA, thus the particles comprise about 91% PLGA (50/55x100=90.9).
Guo et al. further teaches that bicalutamide (BLT) is a nonsteroidal antiandrogen (p2306, col 1, para 2) and a selective androgen receptor modulator as evidenced by US 2014/0107088 ([0042]).
As such, the instant claims 1 and 46 are anticipated by Guo et al.
Claim Rejections - 35 USC § 103
The following is a quotation of 35 U.S.C. 103 which forms the basis for all obviousness rejections set forth in this Office action:
A patent for a claimed invention may not be obtained, notwithstanding that the claimed invention is not identically disclosed as set forth in section 102 of this title, if the differences between the claimed invention and the prior art are such that the claimed invention as a whole would have been obvious before the effective filing date of the claimed invention to a person having ordinary skill in the art to which the claimed invention pertains. Patentability shall not be negated by the manner in which the invention was made.
This application currently names joint inventors. In considering patentability of the claims the examiner presumes that the subject matter of the various claims was commonly owned as of the effective filing date of the claimed invention(s) absent any evidence to the contrary. Applicant is advised of the obligation under 37 CFR 1.56 to point out the inventor and effective filing dates of each claim that was not commonly owned as of the effective filing date of the later invention in order for the examiner to consider the applicability of 35 U.S.C. 102(b)(2)(C) for any potential 35 U.S.C. 102(a)(2) prior art against the later invention.
The factual inquiries set forth in Graham v. John Deere Co., 383 U.S. 1, 148 USPQ 459 (1966), that are applied for establishing a background for determining obviousness under 35 U.S.C. 103 are summarized as follows:
1. Determining the scope and contents of the prior art.
2. Ascertaining the differences between the prior art and the claims at issue.
3. Resolving the level of ordinary skill in the pertinent art.
4. Considering objective evidence present in the application indicating obviousness or nonobviousness.
Claims 1, 7-8, 13, 15, 19, 46-47, and 55 are rejected under 35 U.S.C. 103 as being unpatentable over US 2014/0107088 (hereafter, Wilsey) in view of US2004/0224030 (hereafter, Shastri; cited in the IDS filed on 2/7/2024).
Wilsey teaches an implantable medical device comprising a drug depot that releases the anabolic agent over at least 2 days (sustained release), wherein the drug depot comprises an anabolic agent such as selective androgen receptor modulators (SARMs), a biodegradable polymer, and a suitable pharmaceutical carrier (abstract, [0013], [0042], [0133], [0135], and claim 1, 7-9). The SARMs comprises (2S)-3-(4-cyanophenoxy)-N-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide)(ostarine) ([0042] and claim 7), which is the elected compound (
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).
Wilsey further teaches that the at least one biodegradable polymer comprises PLGA and comprises at least 40 wt. %, at least 45 wt. %, at least 50 wt. %, at least 55 wt. %, at least 60 wt. %, at least 70 wt. %, at least 80 wt. %, at least 85 wt. %, at least 90 wt. %, at least 95 wt. % or at least 97 wt. % of the formulation ([0159], [0165], and claims 8-9). The range of the polymer overlaps the range recited in claim 1
Wilsey also teaches that the medical device (e.g., drug depot) may be designed for sustained release ([0022]) and the phrases "sustained release" and "sustain release" (also referred to as extended release or controlled release) are used herein to refer to one or more therapeutic agent(s) that is introduced into the body of a human or other mammal and continuously or continually releases a stream of one or more therapeutic agents over a predetermined time period and at a therapeutic level sufficient to achieve a desired therapeutic effect throughout the predetermined time period ([0025]).
In addition, Wilsey teaches that the anabolic agent is encapsulated in a plurality of depots comprising microparticles, microspheres, microcapsules, and/or microfibers and the drug particle size (e.g., anabolic agent) in the depot is from about 1 to about 25 micrometers, or about 5 to 50 micrometers ([0135], [0058] and [0162]). The range of the particle size falls within the range recited in claim 8.
Wilsey further teaches that the anabolic agent may be in a polymer-based depot administered by continuous infusion through a pump (injectable formulation) ([0124] and claim 20).
The specific combination of features claimed is disclosed within the broad genera of taught by Wilsey, but such “picking and choosing” within several variables does not necessarily give rise to anticipation. Corning Glass Works v. Sumitomo Elec., 868 F.2d 1251, 1262 (Fed. Circ. 1989). Where, as here, the reference does not provide any motivation to select this specific combination of variables, anticipation cannot be found.
That being said, however, it must be remembered that “[w]hen a patent simply arranges old elements with each performing the same function it had been known to perform and yields no more than one would expect from such an arrangement, the combination is obvious”. KSR v. Teleflex, 127 S.Ct. 1727, 1740 (2007) (quoting Sakraida v. A.G. Pro, 425 U.S. 273, 282 (1976)). “[W]hen the question is whether a patent claiming the combination of elements of prior art is obvious”, the relevant question is “whether the improvement is more than the predictable use of prior art elements according to their established functions.” (Id.). Addressing the issue of obviousness, the Supreme Court noted that the analysis under 35 USC 103 “need not seek out precise teachings directed to the specific subject matter of the challenged claim, for a court can take account of the inferences and creative steps that a person of ordinary skill in the art would employ.” KSR v. Teleflex, 127 S.Ct. 1727, 1741 (2007). The Court emphasized that “[a] person of ordinary skill is… a person of ordinary creativity, not an automaton.” Id. at 1742.
Consistent with this reasoning, it would have been prima facie obvious to one of ordinary skill in the art before the effective filing date of the claimed invention to have selected various combinations of the selective androgen receptor modulators and biodegradable polymers within the disclosure of Wilsey for preparing a sustained release depot (microparticles) composition to arrive at compositions “yielding no more than one would expect from such an arrangement”. As stated above, Wilsey specifically discloses and claims the elected compound as one of selective androgen receptor modulators and PLGA as one of suitable biodegradable polymers for their sustained release formulation. While it does not specifically disclose an example of sustained release depot (microparticles) composition comprising the elected compound and PLGA, one of ordinary skill in the art would have envisaged such formulation and have been motivated to prepare it with a reasonable expectation of success since such combination has been taught and suggested by the prior art.
In addition, Shastri discloses a controlled release formulation containing microspheres (microparticle) comprising blended PLGA copolymers and a biologically active agent, which have controlled release profiles, preferably delayed release profiles, providing prolonged release of a biologically active agent (abstract and [0003]). Shastri teaches that any agent having therapeutic biological activity may be included in the microspheres ([0007] and [0058]) and the timing, rate, quantity, and/or duration of release of a biologically active agent from a microsphere can be controlled or modulated by optimization of the microsphere copolymer ratio ([0027]). Shastri further teaches methods of controlling the duration of release of a biologically active agent from a microsphere by controlling the type and/or ratio of PLGA copolymer ([0050]). For example, the release period of PLGA copolymer having a 75%:25% ratio of racemic lactide DL to glycolide (RG75/25) can continue for more than 7 weeks ([0006] and [0051]). Shastri further teaches that the microspheres fall within the range of 30 to 40 micrometers and the diameter of the microsphere is modulated depending on the desired alteration in release kinetics ([0039]). The range falls within the range recited in claim 8. Shastri also teaches that an important factor in the successful treatment of long-term chronic disease, such as osteoporosis, diabetes, asthma, hepatitis, and arteriosclerosis etc., is patient compliance to the prescribed treatment regimen and PLGA microspheres with controlled release profiles can be implanted into a site in vivo by injection, thereby requiring fewer doses and increasing patient compliance ([0002] and [0028]).
Thus, the skilled artisan would have been further motivated to prepare a sustained release formulation comprising the SARM using PLGA microspheres as taught by Shastri because Shastri teaches the PLGA microspheres with controlled release profiles can be used for any therapeutic agent and can controlling the duration of release of a biologically active agent from a microsphere by controlling the type and/or ratio of PLGA copolymer. The skilled artisan would have been motivated to use PLGA microspheres as taught by Shastri for prolonged release of SARM in the treatments of a long-term chronic disease on the reasonable expectation that the resulting sustained release formulation could be implanted into a site in vivo by injection, thereby requiring fewer doses and increasing patient compliance as taught by Shastri.
As to the percentage of the polymer, Wilsey teaches the range overlapping the claimed rage. In the case where the claimed ranges “overlap or lie inside ranges disclosed by the prior art” a prima facie case of obviousness exists. In re Wertheim, 541 F.2d 257, 191 USPQ 90 (CCPA 1976); In re Woodruff, 919 F.2d 1575, 16 USPQ2d 1934 (Fed. Cir. 1990).
As to claim 15, the prior art does not specifically teach that the androgen receptor modulator is released for up to 10 weeks. However, the prior art teaches that the phrases "sustained release" and "sustain release" (also referred to as extended release or controlled release) are used herein to refer to one or more therapeutic agent(s) that is introduced into the body of a human or other mammal and continuously or continually releases a stream of one or more therapeutic agents over a predetermined time period and at a therapeutic level sufficient to achieve a desired therapeutic effect throughout the predetermined time period ([0025]). In addition, Shastri teaches the duration of release of a biologically active agent from a microsphere can be optimized by controlling the type and/or ratio of PLGA copolymer that comprises the microsphere and the release period of PLGA copolymer having a 75%:25% ratio of racemic lactide DL to glycolide (RG75/25) can continue for more than 7 weeks ([0006] and [0051]). Shastri further teaches that the diameter of the microsphere also can be modulated depending on the desired alteration in release kinetics ([0039]). Thus, it would have been prima facie obvious to one of ordinary skill in the art before the effective filing date of the claimed invention to optimize the time period to release the active agent for achieving a desired therapeutic effect throughout the predetermined time period by adjusting the type and/or ratio of PLGA copolymer and the diameter of microspheres as taught by Shastri.
In addition, it is well-established that merely selecting proportions and ranges is not patentable absent a showing of criticality. In re Becket, 33 USPQ 33; In re Russell, 169 USPQ 426. “[W]here the general conditions of a claim are disclosed in the prior art, it is not inventive to discover the optimum or workable ranges by routine experimentation.” In re Aller, 220 F.2d 454, 456, 105 USPQ 233, 235 (CCPA 1955); see also Peterson, 315 F.3d at 1330, 65 USPQ2d at 1382 (“The normal desire of scientists or artisans to improve upon what is already generally known provides the motivation to determine where in a disclosed set of percentage ranges is the optimum combination of percentages.”)
Conclusion
No claims are allowed.
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/BONG-SOOK BAEK/Primary Examiner, Art Unit 1611