Its only a matter of time before Gilead is TOAST!!!

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Anonymous said:
I am a High school Chemistry teacher. Will that do? I disagree. Many do. These new Patents are Novel forms of the Pro-Drug. The Methyl ( a 200- 209 pM diameter) group is what causes the chain termination thru classic steric hindrance. The Fluoro doesn't cause any harm as was always feared and seams to as stable as the hydroxyl group (which is what is natural) and it sure helped gilead attempt to go around the "Method-of-Treatment" patents for 2' Methyl Nucleosides which also was first. My humble suggestion: don't be so arrogant about how this will all play out. My guess is a settlement at some time prior to the first Jury ( which is the only place that penalties such as the 3X penalty, I forget what USC code it is for launching at risk and being judged to not own the patents). Other than that - Good Luck (in a sincere way)
Click to expand...

From: Clark request for rehearing #2
ThisisthesecondinterferencebetweenClarkandStorer/Sommadossi.Thefirst
interference,No.105,871,wasbetweenClark’sU.S.PatentNo.7,429,572B2(“’572patent”)
andStorer’sAppl.No.12/131,868filedJune2,2008(“S5”),andthecountcoveredasetof
compoundscalledN-nucleosidessubstitutedatthe2’positionwithafluorineatom(F)“down”
andamethylgroup(CH3)“up”(“2’-fluoro-2’-methylnucleosides”).(Ex2005,p.2:5-19;Ex
2007,p.2:9-3:7;Ex2008,p.8:7-20.)Thetimelinebelowsummarizestheparties’various
applicationsleadingtothetwointerferences:

(picture )

Inthefirstinterference,StorerwasinitiallyaccordedthebenefitofAppl.No.10/608,907filed
June27,2003(“S4”),whichissuedasStorer’sinvolvedU.S.PatentNo.7,608,600B2(“’600
patent”),anditmovedforbenefitofProvisionalAppl.No.60/392,350filedJune28,2002
(“S1”).Inresponsetotheparties’motions,theBoardheldthatS4failedtoenabletheskilled
artisantomakeevenasingle2’-fluoro-2’-methylnucleoside,andthusdeniedStorerbenefitof
bothS4andS1.(Ex2005,pp.20:3-26:13.)Asaresult,theBoarddesignatedClarkseniorparty
inthefirstinterference,andClarkultimatelyprevailedinthepriorityphase.(SeeEx1173,p.
2:1-3.)
Thepresentinterferenceinvolvesacountcoveringamethodofusingcompounds,which
encompassthecompoundsthatwereatissueinthefirstinterference,fortreatinghepatitisC
virus(“HCV”)infections.Critically,allofthecompoundsatissueinbothinterferencesrequirea
fluorineatomatthe2’“down”position,whichispreciselywhattheBoardfoundtolack
enablementinS1andS4.StorerneversoughtbenefitofProvisionalAppl.Nos.60/466,194filed
April28,2003(“S2”)or60/470,949filedMay14,2003(“S3”)inthefirstinterference.The
presentinterferenceisbetweenStorer’s’600patent—thepatentthatresultedfromS4,whichthe
Boardheldinthefirstinterferencedoesnotenabletheskilledartisantomakethose
compounds—andClark’sAppl.No.11/854,218filedSeptember12,2007(“C3”),whichclaims
prioritytothesameapplication,Appl.No.10/828,753filedApril21,2004(“C2”),thatledto
Clark’s’572patentinvolvedinthepriorinterference.
Giventheoverlappingscopeofthecompoundsincludedwithinbothcountsrequiringa
fluorineatomatthe2’“down”position,andthefactthatthesamelackofenablement
establishedinthefirstinterferencepreventsStorerfromobtainingbenefitofitsearlier-filed
provisionalapplicationshere,Clarkhassoughttohavethepresentinterferenceredeclaredwith......
 






"A middle school chemistry teacher could tell you it's not worth bringing this one to the patent brawl."

One more point - these latter patents have nothing to do with the current patent litigation. These are all new IP. I was just showing that Idenix has the IP to bring newer and more novel forms of Nucs to market - in this space and in the future Infectious Disease space that's ahead of us for the next 50 years. Viruses are easy compared to attacking mutant DNA due to the nature of Flaviviruses, how they affect the liver and therefore are accessible thru a Liver-targeted Pro-drug, replicate and the like. Cancers are a whole different ball of wax (yes, I know Gemcitabine is a nucleoside) But its also very toxic. A lot like NM-283 was. New novel pro-drugs like the SATE variety has the capacity to dramatically increase absorption across gastric barriers and thus increase active metabolites in circulation. Just a thought -
 






Anonymous said:
"A middle school chemistry teacher could tell you it's not worth bringing this one to the patent brawl."

One more point - these latter patents have nothing to do with the current patent litigation. These are all new IP. I was just showing that Idenix has the IP to bring newer and more novel forms of Nucs to market - in this space and in the future Infectious Disease space that's ahead of us for the next 50 years. Viruses are easy compared to attacking mutant DNA due to the nature of Flaviviruses, how they affect the liver and therefore are accessible thru a Liver-targeted Pro-drug, replicate and the like. Cancers are a whole different ball of wax (yes, I know Gemcitabine is a nucleoside) But its also very toxic. A lot like NM-283 was. New novel pro-drugs like the SATE variety has the capacity to dramatically increase absorption across gastric barriers and thus increase active metabolites in circulation. Just a thought -
Click to expand...

Geeks. All of you posting on this thread.
 






Anonymous said:
Dude, That's not your argument. Your side already admitted that Idenix "invented" the 2' Methyl 2' Flouro like 1.5 years before they ever "conceived" of the idea. Their arguemts have been all about "Enablement" and "reduction to Practice". Idenix did not do a good job showing how to make a 2' Flouro 2' Methyl and rely on "constructive reduction to practice". They also argue that "anyone skilled in the arts as of 2001 (when they patented) could produce this variant with essentially the chemical formula. With a chemistry degree, I would agree but I am not a Patent attorney. Needless to say, my guess is that they have over 50% chance of winning this, especially since S1-4 (the 4 patents and Patent applications that were submitted prior to Clarks patent being submitted) were dated prior to Clarks original patent. That's essentially why they "lost" 105871 Patent Interference - its because Gilead convinced the Judge to not "allow" these earlier patents to be considered. It is going to appeal with Judge Stark's court before a jury. My humble opinion (because once you see this laid out its a little bit overwhelming - You will lose. Gilead also argued that Idenix's "enablement was not complete. To do this they actually used the vacation and sick leave schedules of Key Idenix employees from the date of filing saying essentially "If they were serious - They used the lawyer term of Diligence, Then these employees would not have taken vacation or have been absent on these days.

Idenix may lose in the end but trust me ...this thing is MUCH closer than anyone can call. THe BPAI still did not rule on "Clarks" request or Gileads request for a re-hearing on 105981 - My gut is that this judge is siding on Idenix side. I will know a lot more based on his ruling to the 4/25 & 5/01 requests.

oh, that's just for the US. You still have China, Europe, Canada, Norway (on appeal) and Australia (each with different laws governing IP). Again, I hope you make a lot of money on Gilead (sincerely) just saying that to hold this stock - you have bigger cohonas than me.

oh, just one more thing...You do realize that the C-SWIFT trial is just a proxy until IDX-21437 is "allowed" back in the US for US Site addition to its NUC (which is as effective or slightly more effective than SOF) + IDX-719 (just think GS-5816).
My guess is a exclusive sub-license to Merck for a 4-6 week 3 class regimen that might just be very competitive (if not more competitive) than your third generation.

Don't worry - You guys are actively looking for a PI to add to your combo too: Look up US 2014/0017198 published Jan 16, 2014

Chow!!
Click to expand...

I am not a patent lawyer, but all I see in 6,914,054 and 7,608,597 is a desperate attempt to vomit up every permutation of nucleoside analogs... And it seems like they omitted a few key functional groups.

All the other stuff argued previously (the enablement, the no consistent diligent reduction to practice) will just be icing on the cake.
 












Anonymous said:
I am not a patent lawyer, but all I see in 6,914,054 and 7,608,597 is a desperate attempt to vomit up every permutation of nucleoside analogs... And it seems like they omitted a few key functional groups.

All the other stuff argued previously (the enablement, the no consistent diligent reduction to practice) will just be icing on the cake.
Click to expand...

We will see. So hard to tell how this will play out, especially in front of a jury. You have to admit that there really should be more press than there is (This is not an open and shut case for either side

This is were I am following one case. Hope it enlightens. Again, good luck to all: Hope Gilead and Idenix can both prosper immensely

https://acts.uspto.gov/ifiling/Publ...=4&action=filecontent&replyTo=PublicView.jspe)
 






























Anonymous said:
very informative. thanks for sharing this
Click to expand...

Thanks for the Thank You. I hope it helps. My feeling is that Sovaldi is close to being "the perfect drug". It would not hurt to own shares of both companies. Idenix and Pharmasett were the real "owners" of Prodrug Nucleoside technology with Merck being the Grandfather (see the original 2' Methyl Nucleoside Patent : Merck US 3,480,613 and then later patents as US 7,105,499 & US 8,481,712) After getting a 5 -6 log drop with MK-0608 and then seeing Toxicity they just gave up on "nucs" and went after PI's to combat HCV. That's why Idenix never claimed to own the Structural patent over 2' Methyl Nucleosides for the treatment of HCV but only claimed and I think still own the rights for the "method of treatment" patent for 2' Methyl Nucleosides for the treatment of HCV. If you really look close...Merck was the first to Patent the "Up methyl" - "Down Flouro" 2 ' nucleoside before either Idenix or Pharmasett, but they never really "enabled it" because they were betting everything on MK-0608.

In case # Case3:13-cv-04057-JSW Document1 Filed08/30/13 Page1 of 13

Read:

53. The August 5, 2013 letter further provided the following license terms: In consideration of the rights to be granted, Gilead shall pay to Merck a 10% royalty on the Net Sales of Licensed Product (as defined in the Agreement) by Gilead, its distributors or sublicensees, including sales of Licensed Product that is co-packaged with one or more other pharmaceutical products, from the first sale of sofosbuvir until the expiration of the last to expire patent within the Licensed Patent Rights.
54. The August 5, 2013 letter requested a reply by August 31, 2013 and further stated that Merck already has one licensee on the terms specified in the letter. 55. A 10% royalty on products containing sofosbuvir is a prohibitive demand. On information and belief, Merck understands that its license demand is prohibitive and instead is meant to threaten Gilead, on the eve of approval of sofosbuvir, with the prospect of an infringement suit and a substantial claim for damages.


This is the sentence that intrigues me: "stated that Merck already has one licensee on the terms specified in the letter"

My guess is that one licensee is: Idenix (just in case)

thoughts?
 






One more thought: Take a look at exhibit # 1271 from the Interference 105,871

(it shows the original Lab books from Idenix "enabling" or trying to "enable" their conception: The 2' Flouro 2' Methyl Nucleoside (sorry Nucleotide).
 












"That's why Idenix never claimed to own the Structural patent over 2' Methyl Nucleosides for the treatment of HCV but only claimed and I think still own the rights for the "method of treatment" patent for 2' Methyl Nucleosides for the treatment of HCV."

this comes from: Form S-1 (Idenix)
Registration Statement
Filed Dec 15, 2003
"Our hepatitis C clinical drug candidate, NM 283, is a prodrug of the active molecule NM 107, because it is converted into biologically active NM 107 in the body. We believe that NM 283 may be a new compound, and therefore we are attempting to obtain patent protection on NM 283 itself, as well as a method to treat hepatitis C with NM 283. NM 107 was a known compound at the time that the patent applications covering the use of this active form of NM 283 to treat hepatitis C were filed(May 23, 2000). As a result, we cannot obtain patent protection on NM 107. We will pursue patent protection on the method of using NM 107 in medical therapy for the treatment of hepatitis C.
Despite the fact that NM 107 and NM 618 are known compounds, we are aware that a number of companies have recently filed patent applications attempting to cover NM 107 and/or NM 618 specifically as compounds, as well as NM 283 and NV-08B as members of broad classes of compounds. Companies have also filed patent applications covering the use of NM 107 and NM 618 specifically, and NM 283 and NV-08B generically, to treat hepatitis C, or more generally Flaviviridae. These companies include Merck & Co., Inc. together with Isis Pharmaceuticals. We believe that we were the first to file patent applications covering the use of these drug candidates to treat hepatitis C. Patents in countries outside the U.S. are awarded to the first to file on an invention, and we believe that we are entitled to patent protection in these countries."

Trust me: There is sooooooo much more to this story. I know a VP from Gilead ( I think he is a Senior executive VP or some high title. That's all I will say other than: Trust me...They are worried about Idenix much more than they let on.
 






"covering the use of these drug candidates to treat hepatitis C" They are correct but when filing their first Patent application they forgot the Sp Diastereoisomer ( the Up methyl, down Flouro) of 2' Flouro 2' methyl and before they could correct it with their next application ( I think its S2) Merck beat them to the first ever Filing of both the structural and Method of use (but only for that particular diastereoisomer) the 3/4 other variations were indeed covered in Idenix's prior art.
 






Take a look at exhibit # 1318
Interference 105,801

"Dec31 2002 synthesis report - ex 1318"

It shows "Your" molecule about 1 year before "Your" side admits to "conceiving" it.

See, the argument (so far it has worked with certain Judges) has been that "yes, Idenix patented it first and conceived it first, but those earlier patents and conceptions are meaningless without thorough "reduction to practice" and enablement. Its really a debatable point. It may not hold up with a simple Jury who thinks like we all do and not in "lawyer think".
 






Remember, The "prodrug" portion that Michael Sofia geniously invented is 100% Yours (NO QUESTION); but that's not the active drug. Its the active metabolite that makes the drug and not the salt or Prodrug portion: The following is a typical sentence from a typical patent -

"Summary of the Invention: Methods and compositions for the treatments of infections caused by a coronavirus, togavirus or picornavirus are described that include administering an effective amount of D-Enantiomer or L-Enantiomer-nucleoside of the formula below or a pharmaceutically acceptable salt or prodrug thereof. "


The prodrug portion of Sovaldi is 100% Gilead's. The active agent is what is at debate here.

Aren't you a little bit curious why NO ANALYST is pointing any of this stuff out?
 






I just don't see this playing out. It's typical to have competing medications with the same MOA & similar SARs...

Can you name any previously successful "method of treatment" litigation cases in pharma?
 






Anonymous said:
Take a look at exhibit # 1318
Interference 105,801

"Dec31 2002 synthesis report - ex 1318"

It shows "Your" molecule about 1 year before "Your" side admits to "conceiving" it.

See, the argument (so far it has worked with certain Judges) has been that "yes, Idenix patented it first and conceived it first, but those earlier patents and conceptions are meaningless without thorough "reduction to practice" and enablement. Its really a debatable point. It may not hold up with a simple Jury who thinks like we all do and not in "lawyer think".
Click to expand...

This is why I think Idenix's suit is toast rather than Gilead

Jury folk especially dislike patent trolls who:
1) permutate every conceivable molecule in a patent, then
2) sue anyone who actually tries to discover that it really cures something
(If this scenario was legal, there would be zero innovation)

Jury folk also won't take kindly to a couple thousand pages of painful chemical jargon & hours upon hours of industry experts yammering on and on and on... about a few topics, that quite frankly, America deeply loathes: chemistry & patent law.

And even more so, if in the hundreds of pages of original patent submissions, Idenix failed to include the correct functional groups... instead resorting to decade-old lab logs (which... could.... be.... fabricated?).

Weak sauce indeed

It will be Gilead's simple argument that the Jury will actually wrap their heads around... that Pharmasset actually did some old school research & found a cure (despite the fact that it was written down in an Idenix lab book... and how exactly was Pharmasset supposed to be aware of that?)

I also wish Idenix the best: but it needs to be from finding their own cure rather than attacking another company's success with a legal army.

I am more interested in the Merck method patent; any other thoughts?
whoever OP is... he/she has a great nose
 












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