Rotigotine - USA

On Jun 24, 2019, Federal Circuit affirmed district court’s decision that Actavis infringed the valid patent of Neupro® patch.

This appeal concerns UCB’s Patent Nos. US 6,884,434 and US 8,232,414. The ’434 patent claims a transdermal therapeutic system comprising rotigotine, a drug used for the treatment of Parkinson’s disease. The ’414 patent claims a polymorph of rotigotine. Delaware court found that Watson / Actavis’s generic products infringed the ’434 patent under the doctrine of equivalents & also upheld the validity of the ’434 patent over Actavis’s obviousness and anticipation challenges. Actavis appeals the district court’s infringement and validity judgments. UCB cross-appeals the district court’s invalidation of the ’414 patent under 35 U.S.C. § 102(a) as known and used by others in the United States before the date of invention.

A. Infringement of the ’434 Patent:

The only asserted independent claim reads:

1. A transdermal therapeutic system comprising a self-adhesive matrix layer containing the free base [rotigotine] in an amount effective for the treatment of the symptoms of Parkinson’s syndrome, wherein the matrix is based on an acrylate-based or silicone-based polymer adhesive system having a solubility of ≧5% (w/w) for the free base [rotigotine], all of said free base being present in the matrix in the absence of water; a backing layer inert to the components of the matrix layer; and a protective foil or sheet covering the matrix layer to be removed prior to use.

Actavis’s product contains polyisobutylene adhesive, which is different from the claimed acrylate-based or silicone-based polymer adhesives. But UCB argued that, under the doctrine of equivalents, polyisobutylene-based adhesives are interchangeable with the claimed adhesives. Actavis argued that UCB was “barred” from asserting the doctrine of equivalents here because of prosecution history estoppel, intentional narrow claiming, vitiation, or ensnarement.

a. Prosecution History Estoppel –

Actavis argued that UCB’s election of the Group I claims (limited to silicone- and acrylate-based polymer adhesive) after the examiner issued a restriction requirement should prevent UCB from now asserting infringement under the doctrine of equivalents. The Group II claims were not limited to silicone- and acrylate-based polymer adhesive systems. In Actavis’s view, because UCB withdrew those claims, it gave up claim scope of adhesives that are not silicates or acrylates and should not be allowed to recapture that subject matter through the doctrine of equivalents. Federal Circuit, however, sided with District court & said that here the examiner’s restriction requirement did not relate to polyisobutylene, and the examiner was not communicating anything about the patentability of polyisobutylene-based adhesive systems. UCB never added a polyisobutylene-excluding limitation by amendment, and its election cannot be read as such. Court concluded that UCB did not make a narrowing amendment in respect to the restriction requirement. Therefore,  court found no good basis in the prosecution history to bar the application of the doctrine of equivalents to polyisobutylene-based polymer adhesive systems.

b. Narrow Claiming –

Actavis argued that UCB had chosen to draft narrow claims and should not be permitted to expand the scope of those claims through the doctrine of equivalents. Specifically, Actavis argued that Dr. Mueller, an inventor of the ’434 patent, knew that polyisobutylene was a polymer that could be used in transdermal patches but chose not to prosecute a claim broad enough to cover polyisobutylene. Court said that ’434 patent’s specification does not rely on any unique characteristics of acrylate or silicone-based polymer adhesive systems that would not be present in a polyisobutylene-based system. And the fact that the specification repeatedly recites acrylate- and silicone-based polymers is irrelevant to the issue of whether it describes those polymers in a manner that would suggest to a skilled artisan that polyisobutylene is not an equivalent. There is not enough indication from the patent specification, claims, or the record evidence of the inventor’s knowledge here to conclude that UCB surrendered polyisobutylene as a possible equivalent. In the absence of such facts, Federal Circuit agreed with the district court that UCB’s claiming of acrylates and silicates does not bar treating polyisobutylenes as an equivalent for infringement purposes.

c. Vitiation -

Actavis argued that UCB’s doctrine of equivalents infringement theory should fail because it vitiates the “acrylate-based or silicone-base polymer adhesive system” limitation of claim 1. Federal Circuit did not agree with finding that polyisobutylene to be an equivalent gives the element “an acrylate-based or silicone-based polymer adhesive system” such broad play that the element would disappear entirely. The district court did not broaden the right to exclude so widely as to cover all adhesive systems and vitiate the “acrylate-based or silicone-based” claim language.

d. Ensnarement –

Actavis argued that a hypothetical claim including polyisobutylene-based polymers would ensnare the prior art. Court said that Actavis offers no examples of prior art that would be ensnared by the addition of polyisobutylene to the claim, in contrast to the claim as is. Federal Circuit said that District court correctly found that there is no an ensnarement issue here and found that “UCB’s equivalence theory does not ensnare the prior art.”

e. Doctrine of Equivalents – Merits

Court applied the insubstantial difference test here because it may be more suitable . . . for determining equivalence in the chemical arts,” and identified “structural equivalen[cy]” as particularly relevant when comparing chemical equivalents. Mylan Institutional LLC v. Aurobindo Pharma Ltd., 857 F.3d 858, 869 (Fed. Cir. 2017). The district court found that, at the time the ’434 patent was filed, silicates, acrylates, and polyisobutylenes were the most commonly used pressure-sensitive adhesives in transdermal patches. The district court then identified a set of properties that silicates, acrylates, and polyisobutylenes share: they are pressure-sensitive, adhesive, biologically inert, non-irritating, and non-toxic. Thus, the district court found that a skilled artisan “would recognize that polyisobutylene is not substantially different from the classes of adhesives literally within the scope of the claims.” The district court also made fact findings as to the differences between polyisobutylene and silicates/acrylates (e.g., lack of heteroatoms and functional groups, different polarity, etc.). But these differences do not matter for how the claimed invention works. The district correctly concluded that “[t]hese results show that the polyisobutylene-based polymer adhesive system did not alter the way rotigotine is transdermally delivered compared to a silicone-based polymer adhesive system,” nor did it “alter rotigotine transdermal delivery rates,” showing that “polyisobutylene is interchangeable with silicone in the claimed polymer adhesive system.” Therefore, polyisobutylene-based adhesive system is an insubstantial modification of the claimed invention.

B. Validity of the ’434 Patent:

The district court found that Cygnus prior art did not disclose a crucial element of claim 1: a patch containing rotigotine in free base form. On appeal, Actavis points to Cygnus’s Example 15 as teaching a patch with some rotigotine in free base form. But Actavis’s argument is flawd because there is nothing in Cygnus that teaches a water-free patch with rotigotine in free base form. All the patches in Cygnus’s examples— including those with rotigotine—contain significant amounts of water (10–15% w/w). Other prior arts, Lipp & Pfister  did not fill this gap. Both disclose transdermal patches containing PVP, but neither discloses any anti-Parkinson’s drugs, much less rotigotine free base in the absence of water.

The district court also rejected Actavis’s argument that the asserted claims of the ’434 patent would have been obvious in light of Miranda combined with Timmerman. Miranda discloses most of the things but does not specifically name rotigotine as a suitable drug for its patches. Timmerman is a 1988 study in which rats were treated transdermally on the skin of their necks with a solution containing rotigotine free base. On appeal, Actavis argues that the district court failed to find obviousness over this combination only because it applied an “unduly rigid” analysis in concluding that Actavis had not shown a motivation to combine or reasonable expectation of success. Federal Circuit said that even accepting Actavis’s argument that a skilled artisan would start with Timmerman, there is still an evidentiary gap as to why a skilled artisan would think of using a transdermal patch, as taught in Miranda, based on Timmerman’s “transdermal administration” disclosure of applying a liquid dose of the drug on the hairless skin on the neck of a rat. As to lack of reasonable expectation of success, Federal Circuit affirmed the district court’s finding.  Court said that based on the disclosures, it was reasonable to conclude that Miranda is less of a “recipe” for the claimed rotigotine transdermal patch and more of a list of thousands of possibilities out of which a skilled artisan would have to select the claimed combination as one to try. Miranda does not provide a reasonable expectation of success for making a transdermal patch of rotigotine without undue experimentation, and Timmerman cannot fill in this gap, as it does not contemplate using a patch to administer rotigotine transdermally. Also transdermal patch field was not a common, widespread one during the relevant time, and that of the drugs available as patches, rotigotine was the only active ingredient that was introduced as a patch without first being available in a different type of formulation.

Thus, Federal Circuit affirmed the district court’s findings upholding the validity of the asserted ’434 patent claims.

C. Invalidity of the ’414 Patent:

On cross-appeal, UCB asked court to reverse the district court’s invalidation of the asserted ’414 patent claims due to prior public use under § 102(a) because the record evidence allegedly did not support the district court’s inferences as to how UCB’s Form II invention was in actual use before the correct invention date. The district court reasonably found that a patient in the United States used Neupro patches that contained Form II rotigotine before November 28, 2007—the ’414 patent’s filing date—and that therefore, the ’414 patent claims were invalid under § 102(a). In November 2007, one female patient patient purchased Neupro patches that were from lot 47808—one of the lots later discovered to have contained Form II rotigotine. While using these lot 47808 patches, the patient began “clearly back-sliding, experiencing previous [Parkinson’s] symptoms of losing mobility, shaking and freezing.” The patient experienced the adverse event two days after the priority date of the ’414 patent, but she had been using the patches for “one week,” necessarily implying that she was using the patches before the ’414 patent’s priority date of November 28, 2007. Federal Ciruit rejected UCB’s arguments & said that there is plenty of evidence that most, if not all, of the patches in lot 47808 contained crystals, and that those crystals contained Form II. There is also evidence that the patient, who reported backsliding only after one week of using lot 47808 patches and who reported improvement (even if short-lived) when a new set of patches was used thereafter, used patches with Form II and that her symptoms matched up with use of Form II. Therefore court fond no clear error in the district court’s finding that Actavis presented clear and convincing evidence of public use before the date of invention under § 102(a). Thus it affirmed the district court’s invalidation of the asserted ’414 patent claims.

In conclusion, Federal Circuit affirmed the district court’s judgment of infringement and validity of the asserted ’434 patent claims, as well as invalidity of the asserted ’414 patent claims.

Itraconazole / Saperconazole – USA

On Jun 21 2019, Federal Circuit affirmed PTAB’s decision & found composition patent covering Mayne pharma’s antifungal drug invalid.

Mayne owns US 6,881,745 patent, which discloses and claims pharmaceutical compositions of azole antifungal drugs that are practically insoluble in aqueous media. Each claim at issue requires a pharmaceutical composition consisting essentially of about 100 mg of an azole antifungal drug and at least one polymer having acidic functional groups, wherein the composition exhibits certain pharmacokinetic properties in vivo. Specifically, claims 2, 9, 10, and 11 require that the in vivo composition provides a mean CMAX of at least 100 ng/ml, while claims 6, 12, 13, and 14 require a mean AUC of at least 800 ng.h/ml. Merck Sharp & Dohme Corp. (“MSD”) filed IPR for claims 1–3, 5–7, and 9–14 of the ’745 patent. The Board issued decision & finally held each of the challenged claims unpatentable.

On appeal Mayne argued that the Board erred in two respects: (1) by instituting review when the petition should have been found time-barred under 35 U.S.C. § 315(b) and (2) by declining to limit the claims to nontoxic compositions that produce the claimed pharmacokinetic profile in humans.

Mayne first raised its argument at institution, urging the Board to reject the petition because Merck & Co., Inc. (“MCI”) should have been identified as a real party in interest. Mayne also requested rehearing of the institution decision, arguing that the Board abused its discretion by failing to find the petition incomplete and time-barred. Mayne contends that the PTO’s clear and unambiguous rules provide that a petition can only be considered and accorded a filing date after all real parties in interest are identified. According to Mayne, because MCI was a real party in interest, the Board could not allow a correction without re-setting the petition’s filing date to the date of the amendment, which it did not do. Because MSD did not name MCI until December 14, 2017, more than a year after the service of Mayne’s complaint against it, Mayne maintains that the petition should have been time-barred. Federal Circuit, however,  sided with PTAB & said that the Board relied on “interests of justice” language in 37 C.F.R. § 42.5(c)(3), its late-action rule: “A late action will be excused on a showing of good cause or upon a Board decision that consideration on the merits would be in the interests of justice.” In applying § 42.5(c)(3), the Board did not plainly err in finding that MSD’s amendment would serve the interests of justice. Both MSD and MCI agreed to be bound by the estoppel effects flowing from the proceeding, and the Board found that it was properly apprised of conflicts relating to MCI from the identification of MSD. There was no evidence suggesting that MSD intended to conceal MCI’s identity. Conversely, unwinding the proceedings based on a strict view of the real-party-in-interest disclosure requirement would be at odds with the PTO policy expressed in § 42.1(b) that Part 42 “be construed to secure the just, speedy, and inexpensive resolution of every proceeding.”

Second, on the merits, Mayne argued to the Board that it should construe the claims as limited to nontoxic compositions that produce the claimed pharmacokinetic profile in humans. Mayne argues that the Board construed the term “pharmaceutical composition” too broadly to encompass toxic compositions that do not have any demonstrated beneficial therapeutic properties. MSD responds that the specification expressly discloses saperconazole as a “pharmaceutical composition,” but that extrinsic evidence indicates that saperconazole is toxic. Thus, in its view, the claims are not limited to non-toxic compounds. Federal Circuit agreed with MSD and the Board that the term “pharmaceutical composition” is not limited to nontoxic compositions. Because the specification is silent as to whether the claimed pharmaceutical composition is limited to being nontoxic, there is no basis to import such a limitation into the claim. Federal Circuit also said that extrinsic evidence also supports the Board’s construction.

Mayne next argued that the Board erred in failing to limit the claimed pharmacokinetic parameters to humans. In support of its position, Mayne cites the district court’s conclusion that “a person of ordinary skill ‘would immediately understand’ – given the results reported from administration of an about 100 mg dose – ‘that the claims of the ’745 patent are directed to humans only.’”  Federal Circuit agreed with MSD that the broadest reasonable interpretation of the claims is not limited to humans. The term ‘in vivo’ in general means, in the living body of a plant or animal. In light of this statement in the specification, a person of skill would understand the claims to include animals. Mayne further argued that, because the embodiment in the specification is from a human trial, the claims should be limited to humans. But Court said that it is improper to import a limitation from an embodiment into the claim. Accordingly, Court concluded that the Board did not err in its constructions of either “pharmaceutical composition” or the “wherein” clauses.

Therefore, Federal Circuit affirmed PTAB & held that Kai anticipates claims 2, 6, 9, 11, 12, and 14, and its combination with Sangekar and Babcock renders claims 2, 6, and 9–14 obvious.

Weekly Patent Round-up

Eli Lilly and Company v. Fresenius Kabi Nederland B.V., District Court The Hague, 19 June 2019, Case no. ECLI:NL:RBDHA:2019:6107

Contrary to the Court of Appeal in summary proceedings, and contrary to various foreign decisions in parallel proceedings, the District Court of the Hague rules in the case on the merits that the scope of protection of Eli Lilly’s patent EP 1 313 508 (hereafter: EP 508), entitled ‘Combination containing an antifolate and methylmalonic acid lowering agent’ is limited to the use of pemetrexed disodium and that the pemetrexed tromethamine used by Fresenius falls outside the scope of protection, as the claims are consciously limited to pemetrexed disodium.….

http://eplaw.org/nl-eli-lilly-v-fresenius-case-on-the-merits/

English High Court refuses to grant Pfizer Arrow declaration

Pfizer’s attempt to secure an Arrow declaration in relation to its proposed launch of a cancer drug in Europe was shot down yesterday, June 20, by the English High Court. Pfizer was seeking an Arrow declaration (a declaration that certain acts would have been obvious in light of the state of the art at a particular date) for its proposed launch of a biosimilar monoclonal antibody drug called Zirabev (bevacizumab), which is used to treat various cancers in combination with other drugs….

https://www.lifesciencesipreview.com/news/english-high-court-refuses-to-grant-pfizer-arrow-declaration-3569

Purdue Pharma Patent Suit Against Collegium Survives Dismissal

·   Purdue’s right to sue would exhaust after first sale

·   Questions remained about first sale

An agreement between Purdue Pharma L.P. and Assertio Therapeutics Inc. that forbade Collegium NF LLC from selling Nucynta doesn’t actually prevent Collegium from selling the pain-relief drug. The doctrine of patent exhaustion allows Collegium to resell the drug after a licensed purchase from Assertio, the U.S. District Court for the District of Delaware said June 19. But questions remained as to whether Assertio transferred the drug’s title to Collegium, preventing the court from dismissing the case…

https://news.bloomberglaw.com/ip-law/purdue-pharma-patent-suit-against-collegium-survives-dismissal

Fed. Circ.'s Vimovo Ruling Harms Innovation, Horizon Says

The Federal Circuit has heightened the standard for patenting new drugs by requiring companies to prove that new inventions are effective to satisfy written description requirements, Horizon Pharma and Nuvo Pharmaceuticals said in a bid to get two patents for the pain reliever Vimovo revived.…

https://www.law360.com/articles/1169914/fed-circ-s-vimovo-ruling-harms-innovation-horizon-says

AstraZeneca Settles Patent Suit on Copycat Faslodex Cancer Drug

AstraZeneca settled a lawsuit in which it had accused three companies of violating patents with a proposed generic version of Faslodex, an injectable treatment for breast cancer.

•             Sino Biopharm’s Chia Tai Tianqing, Athenex, and The WhiteOak Group are blocked from selling their copy of Faslodex “except as specifically authorized” in the settlement agreement, according to consent judgment approved Friday in federal court in Camden, New Jersey

•             Faslodex had U.S. sales of $537 million in 2018, 2.6% of AstraZeneca’s revenue, according...

https://news.bloomberglaw.com/health-law-and-business/astrazeneca-settles-patent-suit-on-copycat-faslodex-cancer-drug?utm_source=rss&utm_medium=HLNW&utm_campaign=0000016b-6622-d5ae-adeb-6eab7b440000

Momenta, Amphastar settle generic Lovenox drug patent case

Amphastar Pharmaceuticals Inc on Wednesday said Momenta Pharmaceuticals Inc and Novartis AG’s Sandoz unit will pay it $59.9 million to resolve patent and antitrust lawsuits over their dueling generic versions of the blood-thinner Lovenox. The settlement ends an appeal by Momenta and Sandoz of a Boston federal jury’s 2017 verdict finding that a patent they claimed Amphastar infringed was invalid, a decision that exposed them to losing $100 million that they had posted as a bond earlier in the litigation.….

https://www.reuters.com/article/health-amphastar/momenta-amphastar-settle-generic-lovenox-drug-patent-case-idUSL2N23Q1VK

Fingolimod - USA

On Jun 17, 2019 Delaware Court granted Mylan’s (MPI) motion to dismiss for improper venue & denied Novartis’ motion for additional venue discovery.

In a patent infringement action, venue is governed solely and exclusively by the patent venue statute, 28 U.S.C. § 1400(b) [TC Heartland LLC v. Kraft Foods Grp. Brands LLC, 137 S. Ct. 1514, 1516 (2017)]. The general venue statute, 28 U.S.C. § 1391, does not have any application in a patent case. Section 1400(b) provides: "Any civil action for patent infringement may be brought in the judicial district [i] where the defendant resides, or [ii] where the defendant has committed acts of infringement and has a regular and established place of business."

Novartis argued that, the general venue statute, Section 1391, and not the patent venue statute, Section 1400(b), governs venue in Hatch-Waxman cases. Specifically, Novartis asserts that "a Hatch-Waxman case under 35 U.S.C. § 271(e) is not a 'civil action for patent infringement' under Section 1400(b)," because it "provides for unique forms of regulatory relief prior to actual infringement." Novartis concludes that using Section 1391 leads to the most efficient outcome of permitting it to litigate its similar patent disputes against all ANDA-filing defendants in a single action in a single District, thus "encouraging the uniform determination of patent rights."

But, Court said that as in BMS II (Apixaban case), this court found that the instant action is "incontestably a ' civil action for patent infringement,' governed solely and exclusively by§ 1400(b)." Novartis, like BMS, expressly alleged in its complaint that it was filing a "patent infringement" action against MPI and cited solely Section 1400(b) as the statutory basis for venue. Novartis' cause of action arises under Section 271(e)(2)(A), which makes it an "act of patent infringement" to do as MPI is alleged to have done here: file an ANDA with the U.S. Food and Drug Administration seeking approval of a pharmaceutical product that reads on a valid, enforceable, unexpired patent. Moreover, under TC Heartland, the proper venues for such patent infringement actions are determined solely and exclusively by Section 1400(b).

Court next turned to whether Novartis has met its burden to show that venue is proper in this District under Section 1400(b). Court said that MPI is not incorporated in Delaware and, therefore, indisputably does not reside here. Nevertheless, Novartis contends that it should be given an opportunity to pursue venue-related discovery, which would likely yield sufficient evidence that some MPI-related entity is incorporated in Delaware and/or maintains a regular and established place of business here, and these contacts might be imputable to MPI itself. But court said that in BMS II, this court found that, after a year of discovery directed at (in part) MPI, any further discovery would amount to a fishing expedition. In denying the request for discovery, the Court has considered - and rejected- Novartis' contention that venue may turn out to be proper in this District based on the existence of a single MPI employee who lives and works in Delaware. Court further said that nothing in the record supports Novartis' assertion that "it is not happenstance that [the employee] lives in the very territory she covers." Also, it is uncontested that Delaware is not the employee's only territory. No evidence indicates that MPI required or even encouraged the employee to live in Delaware. Merely doing business in Delaware does not make Delaware a regular and established place of business for MPI. "The statute clearly requires that venue be laid where the defendant has a regular and established place of business, not where the defendant's employee owns a home in which he carries on some of the work that he does for the defendant."

Finally, Novartis included a new, additional request in its supplemental post-BMS II briefing. Novartis asked for leave to file an amended complaint which would include a declaratory judgment claim against MPI, pursuant to 28 U.S.C. Section 2201. Novartis states that by seeking this amendment, it is opting to forgo "the unique regulatory remedies that [the Hatch-Waxman Act, 35 U.S.C. § 271(e)] provides," and that it is willing to do so "in order to keep its case against MPI together with the cases against over 20 other generics in this district."  But court said that Novartis did not include a declaratory judgment claim in its original complaint, did not seek or suggest it would seek leave to amend to add such a claim during the first two months that MPI's motion to dismiss was pending, and only first suggested it wished to pursue this approach in supplemental briefing the Court sua sponte invited after issuing its BMS II decision. Novartis could and should have anticipated that the Court might resolve MPI's co-pending motion to dismiss in BMS II in favor of MPI, and should have moved to amend substantially sooner.

Court finally said that while it recognizes that this decision is prejudicial to Novartis, Novartis is free to file a new declaratory judgment action against MPI, in any District in which it believes it can prove venue is proper (which may include Delaware).

Mesalamine – USA

On Jun 12 2019, Federal Circuit affirmed PTAB’s decision & found patent covering Salix Pharmaceuticals' ulcerative colitis treatment invalid.

Salix holds NDA for mesalamine extended release capsules (375 mg), marketed under trademark, Apriso®. U.S. Patent No. 8,865,688 (expiring on 05/01/2030) is owned by Dr. Falk Pharma GmbH (“Dr. Falk”) and exclusively licensed to Salix Pharmaceuticals. In 2015, Mylan filed ANDA & subsequently in Jun 2015 Salix and Dr. Falk filed suit alleging infringement.  On Dec. 8, 2015, after Salix and Dr. Falk sued Mylan in district court, GeneriCo and Flat Line filed a petition for IPR challenging claims 1 and 16 of the ’688 patent as obvious over certain prior art references. Following an oral hearing, the Board issued a final written decision on May 19, 2017 finding claims 1 and 16 unpatentable as obvious over the asserted references. Meanwhile in Apr 2016, Northern District of West Virginia after bench trial held that claim 1 of the ’688 patent would not be infringed. Salix & Dr. Falk Pharma appealed both the rulings.

Obviousness:

The ’688 patent relates to a method of maintaining remission of ulcerative colitis with a granulated mesalamine formulation. Patent specification explains that previous delivery methods for oral treatments known at the time of invention were problematic due to the “variation . . . in the release of mesalamine, including premature release, the possibility of dose dumping, and sensitivity to conditions that increase gastric pH and cause premature release of mesalamine. The invention of the ’688 patent purports to improve upon past methods by administering an effective amount of granulated mesalamine formulation.

Claim 1 reads as:

1. A method of maintaining the remission of ulcerative colitis in a subject comprising administering to the subject a granulated mesalamine formulation comprising four capsules each comprising 0.375 g of granulated mesalamine once per day in the morning, without food, wherein:

said method maintains remission of ulcerative colitis in a subject for a period of at least 6 months of treatment; remission is defined as a DAI score of 0 or 1; the granulated mesalamine formulation is not administered with antacids; and wherein 85% to 90% of the mesalamine reaches the terminal ileum and colon.

Board found claims 1 and 16 of the ’688 patent as obvious over certain prior art references: a September 2007 Press Release (Phase III trials), Endonurse (Phase III trials with 375 mg dose), and Davis-1985 (discusses 3 factors relevant to controlled release delivery systems among which “positioned release of drugs in the colon”), in view of either Marakhouski  or Brunner (both references compare pellet formulation with tablet formulation).

Board found that all claimed limitations, including the without food and DAI score limitations, were satisfied by the prior art and that there was a motivation to combine the asserted references with a reasonable expectation of success. Specifically, the Board found that a skilled artisan would have been motivated to combine the method of the September 2007 Press Release and Endonurse with the teachings of either Marakhouski or Brunner that the granulated mesalamine formulation could be administered without food. The Board cited as its rationale the fact that all four prior art references pertain to the same or similar granulated mesalamine formulation for treatment of the same disease and because Marakhouski and Brunner teach that an advantage of a granulated mesalamine formulation is the ability to administer the drug independent of food. The Board also found that a skilled artisan would have had a reasonable expectation of success in maintaining remission of ulcerative colitis by administering granulated mesalamine without food. The Board found that the September 2007 Press Release supports this finding because it announces a successful outcome of a Phase III trial to evaluate the safety and efficacy of the same or similar granulated mesalamine formulation for treatment of the same disease. Notably, the Board found “[t]here is no indication in the [September 2007 Press Release] that the granulated mesalamine had to be administered with food in order to obtain the reported success.”

The Board rejected Dr. Falk’s argument that a skilled artisan would need to conduct a food study to determine if the formulation should be administered with or without food. The Board reiterated that such comparative studies are not necessary in view of the evidence of record especially when the claims at issue do not recite an efficacy requirement related to the effect of food.

Federal circuit sided with Board & said that Board did not change theories on the evidence required to show obviousness of the without food limitation. Board here correctly found that the claims do not recite a food effect. In its institution decision, the Board responded to Dr. Falk’s contention that the claims impliedly contained a food effect limitation by stating that, obviousness “turns on whether administering granulated mesalamine without food would have been predictable and would have led to anticipated success.” Consistent with these statements in its institution decision, the Board stated in its final written decision that “[t]he requirement to show a reasonable expectation of success pertains to the subject matter of the claims,” and, here, because “the claims do not recite a food effect,” there was a reasonable expectation of success of arriving at the without food limitation even though none of the prior art discloses a food effect study.

Dr. Falk contended that, even if the claims do not recite a food effect, the Board still erred in disregarding Dr. Falk’s evidence because evidence relating to unclaimed features is relevant to the inquiry of a motivation to combine with a reasonable expectation of success. In support of this proposition, Dr. Falk cites to Intelligent Bio-Systems, 821 F.3d at 1367–68, in which it contends that this court found evidence relating to an unclaimed feature central to the motivation to combine inquiry and to Institut Pasteur & Universite Pierre et Marie Curie v. Focarino, 738 F.3d 1337, 1346 (Fed. Cir. 2013), in which it contends that this court similarly found that the Board erred in disregarding evidence relating to an unclaimed feature when assessing a motivation to combine with a reasonable expectation of success. Federal Circuit disagreed & said that in Institut Pasteur, we admonished the Board, not because it failed to consider evidence relevant to unclaimed features, but because it failed to consider evidence related to a feature that the Board admitted was implicit in the claims. In contrast, here, the claims do not recite any food effect—either expressly or implicitly. Therefore, Board did not disregard evidence of record, but rather correctly found Dr. Falk’s evidence as falling outside the scope of the claims.

Thus, Federal Circuit affirmed the Board’s final written decision that claims 1 and 16 of the ’688 patent are unpatentable as obvious.  Accordingly, court dismissed as moot Salix’s appeal from the district court’s judgment that claim 1 of the same patent would not be infringed.

Job Update

................................................................................

Function: IPR-formulation

Company: Dr Reddy's Lab.

Location: Hyderabad

Experience: 5 years or more

Qualification: M. Pharmacy / PhD (Pharmaceutics)

Contact info: Mr. Vijay Shelke 
E mail: vijaybs@drreddys.com

................................................................................

Many thanks to my friend Mr Santosh Jagdale for sending this job update. If you know or have any vacancy in your IP department then you can contact me at: 
mahen_gunjal@yahoo.co.in 
WhatsApp: +91-7774007489

Weekly Patent Round-up

Drug Cos. Hit Back In High Court 'Blocking Patent' Fight

A group of generic-drug makers pushed the U.S. Supreme Court on Friday to uphold the so-called “blocking patent” doctrine that was used to strike down multiple Acorda Therapeutics patents for multiple sclerosis drug Ampyra, opening the door for companies to launch generic versions of the medication….

https://www.law360.com/articles/1167222/drug-cos-hit-back-in-high-court-blocking-patent-fight

InvaGen Agrees To Admit Infringing Diabetes Drug To End Suit

Pharmaceutical companies Mitsubishi Tanabe Pharma Corp., Janssen Pharmaceuticals Inc. and Cilag GmbH International have asked a New Jersey federal judge to sign off on their deal to drop a patent infringement lawsuit against InvaGen Pharmaceuticals Inc. over its application for the generic version of Janssen's diabetes treatment Invokamet…

https://www.law360.com/articles/1166738/invagen-agrees-to-admit-infringing-diabetes-drug-to-end-suit

Fumarate and phosphate: Same same, but different?

This case is about an alleged infringement of Gilead’s SPC C00915894; the basic patent is EP 0 915 894 B1 (see EPO Register and Swissreg). Gilead’s products are Truvada® and Atripla® which are pharmaceuticals for the treatment of HIV-1 infection…

https://www.patentlitigation.ch/fumarate-and-phosphate-same-same-but-different/

DE – Federal Court Of Justice Confirms Rejection Preliminary Compulsory License Cholesterol Lowering Drugs

In its decision of 4 June 2019, the tenth senate of the Federal Court of Justice (FCJ) confirmed a rejection of an application for a preliminary compulsory license for a cholesterol-lowering drug. It is just the second time that the FCJ had to deal with the questions of a compulsory licence. The first case concerning an HIV Drug dates from July 2017. In that decision from 2017 the FCJ granted a compulsory licence. Now the FCJ has rejected such a compulsory licence as the facts of the cases differ…

http://eplaw.org/de-federal-court-of-justice-confirms-rejection-preliminary-compulsory-license-cholesterol-lowering-drugs/

A Functionally Claimed One-Step Method

Eli Lilly and Company v. Erfindergemeinschaft UroPep GbR, SCT Docket No. 18-1515 (Supreme Court 2019)

Lilly’s new petition for writ of certiorari asks an easy question:

“Whether a single-step patent claim that describes its point of novelty solely in functional terms violates the rule against functional claiming set forth in Halliburton Oil Well Cementing Co. v. Walker, 329 U.S. 1 (1946)”…

https://patentlyo.com/patent/2019/06/functionally-claimed-method.html

Tavaborole - USA

IPR decision: Jun 05, 2019

AIA Review	Filing Date	Institution Date	Petitioner	US Patent	Respondent	Final Written Decision
IPR2018-00168	11/21/2017	06/08/2018	FlatWing & Mylan	9,549,938	Anacor Pharma	Claims 1–6 are unpatentable
IPR2018-00169	11/21/2017	06/08/2018	FlatWing & Mylan	9,566,289	Anacor Pharma	Claims 1–15 are unpatentable
IPR2018-00170	11/21/2017	06/14/2018	FlatWing & Mylan	9,566,290	Anacor Pharma	Claims 1–12 are unpatentable
IPR2018-00171	11/21/2017	06/14/2018	FlatWing & Mylan	9,572,823	Anacor Pharma	Claims 1–6 are unpatentable

Note: Mylan’s IPRs joined with Faltwing’s IPR petitions

US 9,549,938 (Anacor Pharmaceuticals, Inc.; Exp: 08/16/2026 with PED) – OB listed

1. A method of treating a Tinea unguium infection of a toenail of a human, the method comprising: topically administering to the toenail of the human a pharmaceutical composition comprising 1,3-dihydro-5-fluoro-1-hydroxy-2,1-benzoxaborole or a pharmaceutically acceptable salt thereof in an amount sufficient to treat the infection.

US 9,566,289 (Anacor Pharmaceuticals, Inc.; Exp: 08/16/2026 with PED) – OB listed

1. A pharmaceutical formulation, comprising: 1,3-dihydro-5-fluoro-1-hydroxy-2,1-benzoxaborole, or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable topical carrier.

12. A pharmaceutical formulation, comprising: about 5% w/w 1,3-dihydro-5-fluoro-1-hydroxy-2,1-benzoxaborole, or a pharmaceutically acceptable salt thereof; propylene glycol; ethanol; and ethylene diamine tetraacetic acid (EDTA) or a pharmaceutically acceptable salt thereof.

US 9,566,290 (Anacor Pharmaceuticals, Inc.; Exp: 08/16/2026 with PED) – OB listed

1. A method of treating a human having onychomycosis of a toenail caused by Trichophyton rubrum or Trichophyton mentagrophytes, the method comprising: topically administering to the toenail a pharmaceutical composition comprising an amount of 1,3-dihydro-5-fluoro-1-hydroxy-2,1-benzoxaborole or a pharmaceutically acceptable salt thereof, effective to inhibit an aminoacyl tRNA synthetase in the Trichophyton rubrum or Trichophyton mentagrophytes.

US 9,572,823 (Anacor Pharmaceuticals, Inc.; Exp: 08/16/2026 with PED) – OB listed

1. A method of delivering a compound, in a human, from a dorsal layer of a nail plate to a nail bed to treat onychomycosis caused by Trichophyton rubrum or Trichophyton mentagrophytes, the method comprising: contacting the dorsal layer of the nail plate with a pharmaceutical composition comprising a compound that penetrates the nail plate, the compound being 1,3-dihydro-5-fluoro-1-hydroxy-2,1-benzoxaborole or a pharmaceutically acceptable salt thereof, thereby treating onychomycosis due to Trichophyton rubrum or Trichophyton mentagrophytes.

Orange book lists 1 more patent for Tavaborole (KERYDIN) solution; US 7,582,621 (expiring on 11/26/2027). On US 7,582,621 patent, Coalition for Affordable Drugs filed IPR (IPR2015-01776) on Aug 20, 2015. PTAB issued final written decision on Feb 23, 2017 & held claims 1–12 unpatentable. Anacor Pharmaceuticals appealed this IPR decision (cafc 17-1947) & Federal Circuit affirmed PTAB decision on May 05, 2018.

With respect to Hatch-Waxman litigation, many ANDA filers (Lupin, Encube, Glasshouse, Flatwing, Aleor, Amneal, Apotex, Ascent, Aurobindo, Cipla, Perrigo, Taro, Zydus  & Mylan) filed ANDA for tavaborole on NCE-1 date of Jul 07, 2018. These cases are under discovery phase in Delaware court. Bench trial is scheduled on Apr 12, 2021.