Grünenthal GmbH v. Antecip Bioventures II LLC

PGR2018-00001 (US 9,539,268 B2)
Final Written Decision
April 29, 2019

Brief summary: GG found to have demonstrated by a preponderance of the evidence that Antecip’s claims related to zoledronic acid and methods for using the same to treat arthritis are unpatentable for lack of enablement.

Summary: Grünenthal GmbH (GG) requested post-grant review (PGR) of Antecip’s claims 3-30 (claims 1 and 2 were statutorily disclaimed) of US 9,539,268 B2 relating to “[a] method of treating arthritis comprising orally administering a dosage form” of zoledronic acid, as well as pharmaceutical oral dosage forms thereof. The FWD explains that FWDs also issued regarding the parent patent of the ‘268 patent (US 9,408,862) (PGR2017-00022 and PGR2017-00008). In this case, GG alleged lack of enablement (§ 112(a)), indefiniteness (§ 112(b)), anticipation in view of “Leonard” (§ 102), and obviousness in view of Leonard, “Aronhime”, and the “Merrion Poster”, or “Fox”, “Laslett”, Leonard, and the Merrion Poster (§ 103), supported by three expert declarations. The Board first agreed with Antecip regarding the level of ordinary skill in the art, noting it “would reach the same conclusion on enablement even under Petitioner’s proposed levels of ordinary skill” and that “the prior art itself demonstrates the level of skill in the art at the time of the invention” (Okajima, FC 2001). The Board also determined that “no claim term requires express construction for the purposes of this decision” (broadest reasonable construction in light of the specification (§ 42.200(b) (2018); In re Translogic, FC 2007 (uner BRC, claims are assigned their “ordinary and customary meaning”; Vivid, FC 1999 (“[o]nly claims in controversy need be construed”)). On enablement, the Board explained that “[t]he touchstone of enablement is whether undue experimentation would have been required to practice the claimed invention” (In re Wands, FC 1998 (the Wands factors)). GG’s expert testified that “[t]he claimed invention…is within the unpredictable field of pharmaceutical formulations”, which Antecip did not dispute. Regarding the Wands factors, the Board also found that “the ordinary skilled artisan would have expected all dosage forms of zoledronic acid to have relatively low bioavailabilities that fall outside the ranges specified in the challenged claims” (e.g., “about 1.1 to about 4%”), that the “eleven disodium salt forms” (to which the claims are not limited) described in the ‘268 specification “could have different properties, including different solubilities and bioavailabilities”, and that the ‘268 specification does not identify any “bioavailability-enhancing ingredients or provide any “actual data…on any particular dosage form…regarding bioavailability”. On whether “the quantity of experimentation required” would have been undue, the Board “observe[d] that the public reference advanced by Patent Owner describes the bioavailability of zoledronic acid in beagle dogs” and that that study “would not have provided sufficient guidance” regarding bioavailability in humans (“[a]n ordinarily skilled artisan would have recognized that bioavailability in humans differs from…dogs”) (the Board noting that “extrinsic evidence can substitute for disclosure in the specification to provide enabling support”, but also that “the specification…must supply the novel aspects…to constitute adequate enablement” (Genentech, FC 1997)). After balancing the Wands factors, the Board determined that GG had demonstrated by a preponderance of the evidence that claims 3-30 are unpatentable for lack of enablement.

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Endo Pharm. Inc., Mallinckrodt LLC v. Actavis LLC et al.


Docket No. 2018-1054

WALLACH, CLEVENGER, STOLL
May 3, 2019

Brief summary: DC holding that Endo’s claims to low “ABUK” oxymorphone were not shown to be invalid for obviousness affirmed.

Summary: Actavis appealed DC holding that claims 1-6 of Endo’s US 8,871,779 claiming “[a] hydrochloride salt of oxymorphone comprising less than 0.001% of 14-hydroxymorphinone” (see FN3 explaining that this is an oxymorphone impurity/precursory, aka “oxymorphone ABUK”; and 14-hydroxycodeinone is an ABUK impurity in oxycodone, aka “oxycodone ABUK”). Actavis argued that the DC erred by “misconstruing the claim term 14-hydroxymorphinone” and in the obviousness determination. The FC panel explained that in a claim construction analysis in which the DC “consult[s] extrinsic evidence”, “as here”, the FC reviews the DC’s “factfinding…for clear error: (Teva, US 2015; Profectus, FC 2016 (“definite and firm conviction that a mistake has been made”)). Actavis argued that the 14-hydroxymorphinone limitation required no construction due to the plain meaning of the term but the DC relied “on intrinsic and extrinsic evidence” to “determine[] that a PHOSITA would understand” it “to mean ’14-hydroxymorphinone hydrochloride,’ i.e., the ‘salt form’”. The FC panel reviewed the claims (Phillips, FC 2005; “the Asserted Claims only claim 14-hydroxymorphinone as part of the salt”), “the broader specification” (Trs. of Columbia, FC 2016 (“always highly relevant to the claim construction analysis and is, in fact, the single best guide to the meaning of a disputed term”); e.g., “14-hydroxymorphinone’s use in the broader specification is relatively unsupportive of either proferred construction”), and the extrinsic evidence (Phillips, FC 2005; e.g., expert testimony regarding the ‘779 examples)), but not the prosecution history since neither party “identified anything” therein “that further elucidates the proper construction”. The FC panel concluded that “the intrinisic and extrinsic evidence support the [DC’s] construction of 14-hydroxymorphinone as 14-hydroxymorphinone hydrochloride” (which also eliminated Actavis’ anticipation argument, not addressed by the FC panel (Knowles, FC 2018)). On obviousness, the DC “held that a PHOSITA ‘would have understood it would not have been feasible’ to employ Chapman’s solution to the reappearing ABUK problem to Weiss’s catalytic hydrogenation process for oxymorphone”, that the PHOSITA would not have had a reasonable expectation in success in practicing Rapoport’s “low-ABUK” process, or from the “FDA communications” (which the FC panel, but not the DC, held to be prior art (see FN9; OddzOn, FC 1997 (§ 102(f) ‘does not pertain only to public knowledge, but also applies to private communications between the inventor and another which may never become public’” (pre-AIA, “he did not himself invent the subject matter”); Geo. M. Martin, FC 2010 (“a reference need not work to qualify as prior art”)). The FC panel concluded that the DC “did not clearly err” in finding no reasonable expectation of success in combining Weiss, Chapman, and Rapoport (e.g., “Weiss…does not provide key reaction conditions” and “disclosed a material difficulty”, Endo’s expert testified that “a PHOSITA would not believe that Rapoport “would ever be able to get to…10 [ppm]”, and “FDA communications recite a goal without teaching how the goal is attained” (Abbott, FC 2008; Innogenetics, FC 2008 (“[K]knowledge of a problem and motivation to solve it are entirely different from motivation to combine particular references.”); Allergan, FC 2013 (“potential for FDA approval…may properly be considered”); “the inventors of the ‘779 patent engaged in extensive experimentation, involving much failure, to ultimately produce the oxymorphone of the Asserted Claims”). Thus, the DC decision was affirmed. Judge Stoll’s dissent argued, e.g., that “the FDA’s mandate disclose[s] every limitation of claim 1” and the DC “erred in imposing a requirement that a reference must teach how to solve a problem to provide a motivation to combine, conflating enablement and reasonable expectation of success requirements with motivation.”

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Endo Pharm. Inc., Mallinckrodt LLC v. Actavis LLC et al.


Docket No. 2018-1054

WALLACH, CLEVENGER, STOLL
May 3, 2019

Brief summary: DC holding that Endo’s claims to low “ABUK” oxymorphone were not shown to be invalid for obviousness affirmed.

Summary: Actavis appealed DC holding that claims 1-6 of Endo’s US 8,871,779 claiming “[a] hydrochloride salt of oxymorphone comprising less than 0.001% of 14-hydroxymorphinone” (see FN3 explaining that this is an oxymorphone impurity/precursory, aka “oxymorphone ABUK”; and 14-hydroxycodeinone is an ABUK impurity in oxycodone, aka “oxycodone ABUK”). Actavis argued that the DC erred by “misconstruing the claim term 14-hydroxymorphinone” and in the obviousness determination. The FC panel explained that in a claim construction analysis in which the DC “consult[s] extrinsic evidence”, “as here”, the FC reviews the DC’s “factfinding…for clear error: (Teva, US 2015; Profectus, FC 2016 (“definite and firm conviction that a mistake has been made”)). Actavis argued that the 14-hydroxymorphinone limitation required no construction due to the plain meaning of the term but the DC relied “on intrinsic and extrinsic evidence” to “determine[] that a PHOSITA would understand” it “to mean ’14-hydroxymorphinone hydrochloride,’ i.e., the ‘salt form’”. The FC panel reviewed the claims (Phillips, FC 2005; “the Asserted Claims only claim 14-hydroxymorphinone as part of the salt”), “the broader specification” (Trs. of Columbia, FC 2016 (“always highly relevant to the claim construction analysis and is, in fact, the single best guide to the meaning of a disputed term”); e.g., “14-hydroxymorphinone’s use in the broader specification is relatively unsupportive of either proffered construction”), and the extrinsic evidence (Phillips, FC 2005; e.g., expert testimony regarding the ‘779 examples)), but not the prosecution history since neither party “identified anything” therein “that further elucidates the proper construction”. The FC panel concluded that “the intrinisic and extrinsic evidence support the [DC’s] construction of 14-hydroxymorphinone as 14-hydroxymorphinone hydrochloride” (which also eliminated Actavis’ anticipation argument, not addressed by the FC panel (Knowles, FC 2018)). On obviousness, the DC “held that a PHOSITA ‘would have understood it would not have been feasible’ to employ Chapman’s solution to the reappearing ABUK problem to Weiss’s catalytic hydrogenation process for oxymorphone”, that the PHOSITA would not have had a reasonable expectation in success in practicing Rapoport’s “low-ABUK” process, or from the “FDA communications” (which the FC panel, but not the DC, held to be prior art (see FN9; OddzOn, FC 1997 (§ 102(f) ‘does not pertain only to public knowledge, but also applies to private communications between the inventor and another which may never become public’” (pre-AIA, “he did not himself invent the subject matter”); Geo. M. Martin, FC 2010 (“a reference need not work to qualify as prior art”)). The FC panel concluded that the DC “did not clearly err” in finding no reasonable expectation of success in combining Weiss, Chapman, and Rapoport (e.g., “Weiss…does not provide key reaction conditions” and “disclosed a material difficulty”, Endo’s expert testified that “a PHOSITA would not believe that Rapoport “would ever be able to get to…10 [ppm]”, and “FDA communications recite a goal without teaching how the goal is attained” (Abbott, FC 2008; Innogenetics, FC 2008 (“[K]knowledge of a problem and motivation to solve it are entirely different from motivation to combine particular references.”); Allergan, FC 2013 (“potential for FDA approval…may properly be considered”); “the inventors of the ‘779 patent engaged in extensive experimentation, involving much failure, to ultimately produce the oxymorphone of the Asserted Claims”). Thus, the DC decision was affirmed. Judge Stoll’s dissent argued, e.g., that “the FDA’s mandate disclose[s] every limitation of claim 1” and the DC “erred in imposing a requirement that a reference must teach how to solve a problem to provide a motivation to combine, conflating enablement and reasonable expectation of success requirements with motivation.”

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Grünenthal GmbH v. Antecip Bioventures II LLC

PGR2018-00001 (US 9,539,268 B2)
Final Written Decision
April 29, 2019

Brief summary: GG found to have demonstrated by a preponderance of the evidence that Antecip’s claims related to zoledronic acid and methods for using the same to treat arthritis are unpatentable for lack of enablement.

Summary: Grünenthal GmbH (GG) requested post-grant review (PGR) of Antecip’s claims 3-30 (claims 1 and 2 were statutorily disclaimed) of US 9,539,268 B2 relating to “[a] method of treating arthritis comprising orally administering a dosage form” of zoledronic acid, as well as pharmaceutical oral dosage forms thereof. The FWD explains that FWDs also issued regarding the parent patent of the ‘268 patent (US 9,408,862) (PGR2017-00022 and PGR2017-00008). In this case, GG alleged lack of enablement (§ 112(a)), indefiniteness (§ 112(b)), anticipation in view of “Leonard” (§ 102), and obviousness in view of Leonard, “Aronhime”, and the “Merrion Poster”, or “Fox”, “Laslett”, Leonard, and the Merrion Poster (§ 103), supported by three expert declarations. The Board first agreed with Antecip regarding the level of ordinary skill in the art, noting it “would reach the same conclusion on enablement even under Petitioner’s proposed levels of ordinary skill” and that “the prior art itself demonstrates the level of skill in the art at the time of the invention” (Okajima, FC 2001). The Board also determined that “no claim term requires express construction for the purposes of this decision” (broadest reasonable construction (BRC) in light of the specification (§ 42.200(b) (2018); In re Translogic, FC 2007 (under BRC, claims are assigned their “ordinary and customary meaning”; Vivid, FC 1999 (“[o]nly claims in controversy need be construed”)). On enablement, the Board explained that “[t]he touchstone of enablement is whether undue experimentation would have been required to practice the claimed invention” (In re Wands, FC 1998 (the Wands factors)). GG’s expert testified that “[t]he claimed invention…is within the unpredictable field of pharmaceutical formulations”, which Antecip did not dispute. Regarding the Wands factors, the Board also found that “the ordinary skilled artisan would have expected all dosage forms of zoledronic acid to have relatively low bioavailabilities that fall outside the ranges specified in the challenged claims” (e.g., “about 1.1 to about 4%”), that the “eleven disodium salt forms” (to which the claims are not limited) described in the ‘268 specification “could have different properties, including different solubilities and bioavailabilities”, and that the ‘268 specification does not identify any “bioavailability-enhancing ingredients or provide any “actual data…on any particular dosage form…regarding bioavailability”. On whether “the quantity of experimentation required” would have been undue, the Board “observe[d] that the public reference advanced by Patent Owner describes the bioavailability of zoledronic acid in beagle dogs” and that that study “would not have provided sufficient guidance” regarding bioavailability in humans (“[a]n ordinarily skilled artisan would have recognized that bioavailability in humans differs from…dogs”) (the Board noting that “extrinsic evidence can substitute for disclosure in the specification to provide enabling support”, but also that “the specification…must supply the novel aspects…to constitute adequate enablement” (Genentech, FC 1997)). After balancing the Wands factors, the Board determined that GG had demonstrated by a preponderance of the evidence that claims 3-30 are unpatentable for lack of enablement.

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Amarin Pharma, Inc. et al. v. International Trade Commission (ITC) (Appellee) and Royal DSM NV, et al. (Intervenors) (Docket No. 2018-1247)


Docket Nos. 2018-1247 and 2018-114

PROST, WALLACH (D), HUGHES
May 1, 2019

Brief summary: ITC decision “that Amarin’s allegations are precluded by the FDCA” affirmed since, e.g., “[p]rivate parties may not bring [FDCA] enforcement suits.”

Summary: Amarin, which markets Vascepa(TM) fish oil capsules (“the only purified ethyl ester E-EPA product sold in the [US] as an FDA-approved drug” (E-EPA being the ethyl ester form of eicosapentaenoic acid)), appealed the ITC decision not to institute an unfair competition or unfair act investigation under 19 USC § 1337(a)(1)(A). Amarin filed a complaint under § 337 of the Tariff Act of 1930 alleging “that certain companies” (Royal DSM, Nordic Naturals (the Intervenors)) “were falsely labelling and deceptively advertising their imported synthetically produced omega-3 produces as (or for use in) ‘dietary supplements,’ where the products are actually ‘new drugs’ as defined in the Food, Drug, and Cosmetic Act (‘FDCA’) that have not been approved for sale or use in the” US. Amarin sought “an order under § 337(d) that would exclude synthetically produced omega-3 products from entry into the [US], as well as a cease-and-desist order under § 337(f) to prohibit the respondents from importing, using, or selling synthetically produced omega-3 products.” In declining to institute an investigation and dismissing the complain, the ITC “reasoned that Amarin’s allegations are precluded by the FDCA” and, therefore, “failed to state a cognizable claim under § 337” (as urged by the FDA in a letter to the ITC; POM Wonderful, US 2014 regarding an allegedly mislabeled juice (“Private parties may not bring [FDCA] enforcement suits.”)) The FC panel first explained that it has jurisdiction over the appeal (as argued by Amarin) since the ITC’s “decision ‘clearly reach[ed] the merits of [the] complaint and determinatively decide[d] [Amarin’s] right to proceed in a section 1337 action” (Amgen, FC 1990 (“decision not to institute…is ‘intrinsically a final determination, i.e., a determination on the merits’”); Block, FC 1985 (“order was not a final determination”); Import Motors, CCPA 1976). Amarin also argued that the ITC “had a mandatory duty to institute an investigation” under § 1337(b)(1) as Amarin presented “ a complaint under oath” but the FC panel disagreed since “[t]he facts alleged as the basis for Amarin’s complaint demonstrate” those “are based entirely on violations of the FDCA” and, therefore, “Amarin’s complaint fails to state a cognizable claim for relief” (Syntex, CCPA 1981 (proper to dismiss “where the complain contained insufficient factual allegations”)). The FC panel next explained its agreement with the ITC that the FDA “is charged with administration of the FDCA”, not the ITC, since “the FDCA authorizes the FDA to regulate drugs and dietary supplements” (which “do not require pre-market approval”) and “proving the Lanham Act” (false advertising as “dietary supplement[s]”) “claim in this case requires providing violations of the FDCA” (POM “did not open the door to Lanham Act claims that are based on proving FDCA violations:; Buckman, US 2001; PhotoMedex, 9th Cir. 2010 (FDA has not provided guidance as to whether the products at issue…should be considered ‘new drugs’ that require approval)). Thus, the ITC’s decision not to investigate was affirmed. Judge Wallach dissented, writing that the non-institution decision should not be appealable, and that the case should have been decided under a mandamus jurisdiction (and still denied).

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Neptune Genetics, LLC et al. v. Eli Lilly & Company


Docket No. 2018-1257-8, -1288, -1290 (multiple IPRs)

Moore, WALLACH, HUGHES
April 26, 2019

Brief summary: Board IPR decisions finding Lilly’s claims relating to administration of vitamin B12 with pemetrexed were not shown to be obvious affirmed.

Summary: Neptune Genetics (NG) appealed Board holding that claims 1-22 of Lilly’s US 7,772,209 relating to administering pemetrexed disodium with folic acid and a “methylmalonic acid lowering agent” (MMA; e.g., vitamin B12) were not shown to be unpatentable for obviousness. Claim 12 relates to a similar method but as “[a]n improved method for administering pemetrexed disodium to a patient in need of chemotherapeutic treatment”. Three IPRs alleged obviousness over Calver, Niyikiza I (Niyizaka being the sole named ‘209 inventor), EP 0595005A1 (“EP005”), and US 5,217,974 (IPR2016-00318); Niyikaza I, the ‘974 patent, and EP005 (IPR2016-00237); and Rusthoven and EP005 (IPR2016-00240). The Board “found that it was known in the prior art that pretreatment with folic acid reduces the toxicity associated with administration of an antifolate, like pemetrexed, but there was not a reason to pretreat with vitamin B112 along with folic acid before administering pemetrexed to treat cancer” and that “skepticism of others, particularly the FDA, supported a conclusion of nonobviousness.” The FC panel agreed with the Board’s analysis (e.g., “no observed correlation between vitamin B12 deficiency and pemetrexed-induced toxicity”) that “[e]ach step of the Board’s analysis is supported by substantial evidence” (“supported by additional prior art and are consistent with the testimony of Petitioner’s expert”, “evidence indicates that pemetrexed-induced toxicity correlated with folate deficiencies” (e.g., elevated homocysteine levels) “but not vitamin B12 deficiencies”). “Collectively,” the FC panel wrote, the evidence (e.g., “while elevated levels of homocysteine were known to be predictive of pemetrexed toxicity, elevated levels of MMA were understood not to be predictive of pemetrexed toxicity”) “constitutes substantial evidence…that the art did not provide a motivation for a skilled artisan to administer an MMA lowering agent, such as vitamin B12, in addition to folic acid”. The FC panel acknowledged that “EP005 states that it ‘is applicable to the lowering of total homocysteine blood levels if elevated by any known cause” but “does not discuss antifolates generally, and only generally mentions certain cancers”, and that “the Board found that the levels of homocysteine associated with elevated pemetrexed toxicity risk were not ‘elevated’ as that term is defined in EP005” (also noting that “Niyikiza II explained that pemetrexed did not increase homocysteine levels”). NG also argued that Lilly’s statements to the FDA indicated the prior art suggested pretreating with folic acid and B12, but the FC panel noted that those statements “were made…more than five months after the critical date” and the Board did not err in finding that “the views Lilly expressed about the prior art references…are made through the lens of what they had invented” (In re Copaxone, FC 2018 (“a patent owner’s own disclosures to the FDA may be considered in assessing the state of the prior art”)). The FC panel also found no error with the Board’s in finding the FDA’s skepticism weighed in favor of non-obviousness (WBIP, FC 2016; Circuit Check, FC 2015). The FC also declined to consider NG’s § 101 arguments since IPRs are limited to § 102 and 103 arguments.

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Andersen Corporation v. GED Integrated Solutions, Inc.

Derivation Proceeding DER2017-00007
Petitioner Appln. No. 15/058,862; Respondent Pat. No. 9,428,953 B2
Final Written Decision (March 20, 2019)

Brief summary: In this AIA derivation proceeding, the PTAB found that “Andersen has not demonstrated’ derivation “by a preponderance of the evidence”.

Summary: Andersen requested a derivation proceeding under 35 USC § 135 regarding its ‘862 application relating to window frames, alleging that “an inventor named in the ‘953 patent derived” an invention “recited in claims 1-22 from an inventor named in Andersen’s ‘862 application.” The PTAB’s FWD explains that “[t]o prove derivation, the party asserting derivation must establish (1) prior conception of the claimed subject matter, and (2) communication of that conception to an inventor of the other party” (i.e., “who invented the subject matter at issue”) (Cooper, FC 1993; Hedgewick, CCPA 1974; “Derivation Final Rules”; Davis, CCPA 1967). “Under the AIA,” the FWD explains, “a petitioner must show the respondent, without authorization, filed an application claiming such derived invention” (35 USC § 135(a)(a); 37 CFR § 42.402(b)(2)) by a preponderance of the evidence “because Andersen filed the ‘862 application prior to issuance of the ‘953 patent” (37 CFR §§ 42.400(a); Bruning, FC 1998). And to prove conception of “an invention communicated to an inventor of the other party”, “[a]n inventor ‘must provide independent corroborating evidence in addition to his own statements and documents” (Hahn, CCPA 1981; Coleman, FC 1985 (“[c]onception must be proved by corroborating evidence”); Cumberland, FC 2017 (“must encompass all limitations of the disclosed invention”); 37 CFR § 42.201 (“patentably indistinct…evaluated one-way in the direction from the invention disclosed”); Eaton, FC 2003 (“[t]he communication must be sufficient to enable one of ordinary skill in the art to make the patented invention”); considered under the “rule of reason”). The FWD explains that “[o]ther than the numbering of claim dependencies, claims 60-81 of the ‘862 application are identical to claims 1-22 of the ‘953 patent”. Andersen argued that its inventor (Mr. Oquendo), when an Andersen subsidiary employee, communicated the claimed invention to GED employees, citing “22 different conceptions and corresponding communication[s]”. The PTAB focused on one of the claim limitations, “the ‘stop’-because it is dispositive”, about which GED submitted copy of at least one one of the ‘953 patent’s witnessed notebook pages (reproduced on pp. 36 and 61 of the FWD), which the PTAB determined from the prosecution history was determinative in the allowance of the claims. The PTAB found “no allegation that Mr. Oquendo ever told” the ‘953 inventors about the design (e.g., an “alleged communication was to Mr. McGlinchy, not Mr. Briese, a named inventor of the ‘953 patent…Andersen’s assertion that” McGlinchy “must have passed along unspecified information…is mere speculation”) and that he admitted “that he never mentioned a stop specifically”, the stop is not in Andersen’s prototype, “Andersen’s position is based on an incorrect understanding regarding the existing…design”, and “the timing of events described by the parties support’s GED’s position that the claimed invention was not derived.” Thus, the PTAB found that “Andersen has not demonstrated’ derivation “by a preponderance of the evidence”.

Posted in America Invents Act, Derivation of Invention | Leave a comment