Update #1

[Anonymous]

-i-
I. RELIEF REQUESTED ...................................................................................................... 1*
II. BRIEF SUMMARY OF THE ARGUMENT .................................................................... 1* III. REASONS WHY THE REQUESTED RELIEF SHOULD BE GRANTED .................... 1* A. Estoppel Does Not Apply ...................................................................................... 1* B. The Opinion Of Prof. Wnuk Is Unreliable ............................................................. 1* C. The Storer Claims Are Enabled ............................................................................. 3* 1. One of Ordinary Skill In The Art Could Have Synthesized Compounds Of The Storer Claims Without Undue Experimentation ......................................................................................... 4* (a) One Of Ordinary Skill In The Art Could Have Synthesized 2'-Methyl (up)-2'-F (down) Nucleosides Without Undue Experimentation ............................................................................. 5* (b) Clark’s Argument Regarding C-Linked Bases Is Unsupported and Irrelevant .......................................................... 14* 2. One Of Ordinary Skill In The Art Would Have Known How To Use The Invention Without Undue Experimentation .............................. 14* (a) One Skilled In The Art As Of June 28, 2002 Would Have Known That The 2'-Modified Nucleosides Of The Storer Claims Had A Specific And Credible Utility .............................. 15* (b) One Skilled In The Art As Of June 28, 2002 Would Have Known How To Assess The Utility Of The 2'-Modified Nucleosides Of The Storer Claims With Only Routine Experimentation ........................................................................... 16* (c) Antiviral Activity Was Confirmed For The 2'-Modified Nucleosides Of The Storer Claims And Structurally Similar Compounds .................................................................................. 17* (d) One Skilled In The Art As Of June 28, 2002 Would Have Known How-To-Use The 2'-Modified Nucleosides Of The Storer Claims In The Claimed Methods ...................................... 18* D. The ’907 App. Discloses Formulae That Satisfy The Written Description Requirement For The Claims Of The Storer Patent ............................................. 18* 1. The ’907 App. Discloses Formulae That Fully Support The Claims Of The Storer Patent ................................................................................ 19* (a) Formula (IX) Alone Fully Supports The Claims of The Storer Patent ................................................................................. 19*
TABLE OF CONTENTS (continued)
Page
-ii-
(b) Formula (IV(a)) Alone Fully Supports The Claims Of The Storer Patent ................................................................................. 21* 2. The ’907 App. Discloses Species Within The Scope of The Claims of The Storer Patent ................................................................................. 24* IV. CONCLUSION ................................................................................................................ 25*

 

[Anonymous]

agreed, one of ordinary skill in the art would have expected deoxyfluorination of a tertiary
alcohol to proceed with inversion of configuration. (Ex 2139 2 , at 134:2-6.) Furthermore, skilled
3 chemists are accustomed to adapting reaction conditions to overcome the problem of
4 unanticipated side products or failures to obtain the desired product. As such, one of ordinary
5 skill in the art, armed with his or her own training and experience, coupled with the wealth of
6 knowledge and examples of set forth in the prior art directed to fluorinated chemical compounds,
would have been able to synthesize 2′ 7 -F (down) compounds of the Storer Claims by
deoxyfluorination of nucleosides with a 2′-OH (up) tertiary alcohol using DAST. (Ex 1200 8 , ¶88.)
Clark also argues on p. 14, ll. 8-15 and p. 16, l. 4 to p. 17, l. 9 1 that the ’907 app. does not
10 include working examples of, or provide any guidance regarding, how to make compounds
11 falling within the Storer Claims. The response is that the specification does provide guidance to
12 one of ordinary skill in the art for synthesizing compounds of the Storer claims without undue
13 experimentation. As a legal matter, the specification need not teach how to make a compound if
the artisan would have known how to do so at the time of filing. Martin 14 , 454 F.2d at 752;
Goeddel, Paper 109, at 40-42, 45; Rochester 15 , 358 at 921. Furthermore, starting materials and
working examples of how to make a compound, are not required. In re Strahilevitz 16 , 668 F.2d
1129, 1232 (C.C.P.A. 1982); Martin 17 , 454 F.2d at 752. Nevertheless, the specification expressly
18 describes starting materials, reagents and reactions that would have been applicable to the
preparation of compounds of the Storer Claims. (Ex 1132,¶¶65-69; Ex 1200, ¶97; Ex 1002 19 , at
122:21 to 125:15, at 135:10-20; Ex 1003 20 , at 1948:1-15; 2706:1-15.)
21 Both experts agree that the structure of the compounds of the Storer Claims would inform
one of ordinary skill in the art that a fluorination reagent would be required for synthesis. 22
(Ex 1200, ¶89; Ex 2139 23 , at 101:8-15.) And as discussed above, the fluorination reagent, DAST,

12
1 was known to one of ordinary skill in the art for substituting a fluorine for a hydroxyl group with
2 inversion. Therefore, recognizing that inversion will occur, one of ordinary skill in the art would
3 have known to start with a nucleoside having a similar structure to that defined by the claims, but
4 with a 2'-OH (up), in order to obtain the desired 2'-F (down) structure of the compounds of the
Storer Claims. (Ex 1200 5 , ¶90.)
At page p. 11, l. 17 to p. 12, l. 6 4, Clark argues that the efforts of Idenix’s scientists and
7 the advice provided by Idenix’s consultants is informative regarding enablement. The response
8 is that Clark offers no evidence that the efforts of the scientists were efforts that would have been
9 made by one of ordinary skill, or that the Idenix scientists followed the consultant’s advice.
Furthermore, Idenix scientist, Jingyang Wang, made a 2′-methyl (up)-2′ 10 -F (down) nucleoside on
her first attempt using DAST without the benefit of Clark’s publication (Ex 2013). (Ex 1231 11 ).
In his expert report, Dr. Wnuk identified a compound that he named (2′R)-2′-deoxy-2′ 12 -
fluoro-2′-C 13 -methyluridine as a nucleoside that one of ordinary skill would have recognized as
within the scope of the Storer Claims (Ex 2001 14 , ¶¶323-324) (“Claimed Compound”). Dr. Wnuk
agreed that one of ordinary skill in the art would have recognized compound 17 15 in the Matsuda
article, (“Matsuda Compound 17 16 ”), as a precursor to a compound within the scope of the Storer
Claims depicted at ¶ 323 of his report (“Claimed Compound”). (Ex 2139 17 , at 107:18-108:6,
110:25-112:7; Ex 1144 & Ex 2019, at 949; Ex 2001 18 , ¶ 323.) The two compounds are depicted
19 below:
Matsuda

 

[Anonymous]

I like this part: Idenix scientist, Jingyang Wang, made a 2′-methyl (up)-2′ 10 -F (down) nucleoside on
her first attempt using DAST without the benefit of Clark’s publication (Ex 2013). (Ex 1231 11 ).


You guys are GOING DOWN!!!

 

[Anonymous]

I like this part: Idenix scientist, Jingyang Wang, made a 2′-methyl (up)-2′ 10 -F (down) nucleoside on
her first attempt using DAST without the benefit of Clark’s publication (Ex 2013). (Ex 1231 11 ).

but when?

2004?
2005?
...after years spent with consultants that Idenix hired because they couldn't make 2F down??

That's funny because you are also arguing that anyone "skilled in the art" could whip up some 2F down like it was microwaving some mac n cheese

 

[Anonymous]

Storer alleged that Idenix had a team of chemists, several with doctoral degrees, “diligently” attempting to make a 2’-fluoro-2’-methyl nucleoside for several years, including trying numerous different fluorinating agents, synthetic approaches, seeking additional training in fluorination, scouring the literature, and consulting experts (and even then Storer alleged it was successful only after Clark’s application published as C2-Pub and Idenix scientists followed a procedure therein).

 

[Anonymous]

Storer alleged that Idenix had a team of chemists, several with doctoral degrees, “diligently” attempting to make a 2’-fluoro-2’-methyl nucleoside for several years, including trying numerous different fluorinating agents, synthetic approaches, seeking additional training in fluorination, scouring the literature, and consulting experts (and even then Storer alleged it was successful only after Clark’s application published as C2-Pub and Idenix scientists followed a procedure therein).

This just in, no one reads a post longer than 3 sentences, but if you want to keep replying to your own posts, go ahead. Smh....so sad

 

[Anonymous]

but when?

2004?
2005?
...after years spent with consultants that Idenix hired because they couldn't make 2F down??

That's funny because you are also arguing that anyone "skilled in the art" could whip up some 2F down like it was microwaving some mac n cheese

It was completed right before the 2C patent application was published (early 2005). Yes, it was just about that easy. It really does not matter either way. Constructive reduction to practice was fulfilled the moment the Method-of-Use conception was inked in proper format thru a proper patent application, which was well in advance of team Gilead's (on three occasions; S1, S2, S3 and S4 which turned into their 600 patent). The reason is due to the fact that this patent was enabled thru the wealth of prior art of deoxyflourination schemes which enjoyed well established techniques for around 15 years prior to the key applications. Therefore there was no need "to teach" in those applications. The structure alone "taught" those skilled in the art.

Its really that simple. Just use this information to slowly exit your dangerous GILD positions. If you can stomach the purchase - you can buy into Idenix. It will be the smartest move of your life.

 

[Anonymous]

The dirty little secret here is that Idenix did not care too much about an actual reduction to practice with a "down" flouro. I have quoted early work with NM107 vs PSI 6130 which showed absolutely no difference between the efficacy of the two molecules (if you are not familiar with these two nomenclatures: one is a 2' Methyl 2' Hydroxyl and one is a 2' Methyl 2' Flouro) I really don't think they care much now.

The difference is back then, a Flouro often meant mitochondrial toxicity and cell death (think FIAU and the disaster that happened 10 years earlier with Dr Hoefnagel and the NIH) I sure remember that well. Google "FIAU structure" and google what happened with HBV back in 93 timeframe. It scared the heck out of everyone). Now with Hindsight bias we know that a 2' Flouro in the SP diastereoisomer position is probably helpful or at least it doesn't hurt. I doubt that the current crop of Nucs that Idenix has in their pipeline are Flourinated sugars, but they might. It really doesn't matter. The Hydroxyl is what is more natural.

The current 3 judge panel seems to be clearly understanding the real situation here. If you listen closely to their reasoning you will hear an understanding of the clear theft which happened 10 years ago by pharmasett. They couldn't wait to sell their company to Gilead or actually anyone. They tried for years and finally someone bought into this scam: hook, line and sinker. Too bad that it will end badly for those who buy stolen property.

 

[Anonymous]

The dirty little secret here is that Idenix did not care too much about an actual reduction to practice with a "down" flouro.

that's too bad because that's exactly what will cost Idenix the case

 

[Anonymous]

We will see. I would say that Idenix has about an 85% chance of winning this Interference. We will know in a more definitive way come January when the motions are ruled on. If IDIX keeps senior status then chances are they will win this Interference and it will go to appeal. Its a long war with many battles left to be fought in many countries, but - don't be fooled into thinking that Idenix is the Underdog and has no chance of winning. I know this case well, and still feel that in the end Gilead will be forced to settle in a significant way. If not they risk (in a significant way) losing their company. Big stakes at play here and team Idenix has a rock solid case with the earlier Patents on their side.

 

[Anonymous]

Oh, one more thing. Just by entering into these interferences and Patent invalidity cases without settling the case, Gilead has opened itself up to areas that it could not foresee when their lawyers performed a year long due diligence prior to buying Pharmasett. These cases involve discovery. As mentioned recently, Idenix plans to take recently revealed evidence about Improper Inventorship and Inequitable conduct which came to light through Prothonotary Tabib's court back in early January. The discovery in this Canadian court will now be utilized and has been accepted to be heard by the current USPTO board and if substantiated can and will mean that Gilead's patents will be vacated through fraud. See "Storer Response To Order To Show Cause" with a more thorough explanation as to the nature of this Inequitable Conduct on pages 8-10.

Again....Gilead should have settled (that is if Idenix would even allow a settlement; They may want the whole company instead. Not sure)

 

[Anonymous]

So you think that gilead is a good buy until at least January? I would like your opinion as to why your stock hasn't even cracked 10 dollars a share yet and every time it heads that way it gets knocked down to 3 or 4 dollars a share. If what you are saying is even remotely true, then your stock should be at 20+ , 30+, 40+ or even higher? So what gives mr stock Guru?

I also did not see a Nuc plus ns5a combo pill regimen in trials on Clinical trials . gov website? I thought you said they had a combo pill in late stage testing?

 

[Anonymous]

Anyone who is looking at this thread is a complete idiot. Some person has a fetish on some stupid wortless want-to-be pharmaceutical company. Don't buy into this idiots nightmare. Just buy more Gilead stock and become rich. RICH, RICH, RICH

 

[Anonymous]

Hey, are you the same person threatening to put bullets in peoples heads just because you don't agree or are threatened with what you are reading?

I enjoy reading what this guy posts. I happen to also like Idenix. I am starting to like it a lot, so why don't you just go away and stop attacking people that you obviously feel threatened by. If you really don't like what this guy posts either: Don't read them or offer a constructive rebuttal.

Stop with all the Hate rhetoric.

 

[Anonymous]

It is my opinion that, as of December 18, 2001, the hypothetical person skilled in
14 the art would have been able to prepare a compound falling within Count 1 based upon the
15 structure of the compound alone, using information available in the chemical literature,
16 commonly available starting materials, reagents, techniques and instrumentation, the skilled
17 person's own expertise and know-how, and routine experimentation. Tn other words, it would
18 take no more than routine experimentation for a person skilled in the art to make such a
19 compound. Although many synthetic routes may be attempted by a person skilled in the art, I
20 believe looking at the structure and knowing the nucleoside field, a person skilled in the art
21 would know that a fluoro group needs to be added to a known 2'-methyl nucleoside. Although a
22 person skilled in the art may think of several fluorination reactions to accomplish this, if a proper
23 literature search is done beforehand, one route is the most logical or obvious path to try

 

[Anonymous]

So you think that gilead is a good buy until at least January? I would like your opinion as to why your stock hasn't even cracked 10 dollars a share yet and every time it heads that way it gets knocked down to 3 or 4 dollars a share. If what you are saying is even remotely true, then your stock should be at 20+ , 30+, 40+ or even higher? So what gives mr stock Guru?

I also did not see a Nuc plus ns5a combo pill regimen in trials on Clinical trials . gov website? I thought you said they had a combo pill in late stage testing?

This whole patent dispute is like a gambler (who has failed over and over and over again) decides to go bet his house & car title on a single roulette space

http://marshallip.com/media/pnc/3/media.723.pdf
Idenix will (likely) lose the patent fight as stated in above document

Idenix cannot get its own treatment on the market until 2017. That's optimistic because most of Idenix's earlier candidates didn't make it.

Hitting the market in 2017 is long after therapies from Gilead, Abbvie, Merck, JNJ, Bristol, and Boehringer Ingelheim are expected.

I think Idenix is also full of shit. Expect late 2018 if their drug actually works (and doesn't kill people)

Even if Idenix succeeds with their own therapy, they don't have a means to produce & market the drug.... Instead they will get a few miserable pennies on the dollar from a shitty royalty agreement.

So there you have it.... a $6 stock that's really worth $2 with all of the stuff it's got going against it.

But boy... some delusional guy in his mom's basement thinks otherwise!!!

 

[Anonymous]

This whole patent dispute is like a gambler (who has failed over and over and over again) decides to go bet his house & car title on a single roulette space

http://marshallip.com/media/pnc/3/media.723.pdf
Idenix will (likely) lose the patent fight as stated in above document

Idenix cannot get its own treatment on the market until 2017. That's optimistic because most of Idenix's earlier candidates didn't make it.

Hitting the market in 2017 is long after therapies from Gilead, Abbvie, Merck, JNJ, Bristol, and Boehringer Ingelheim are expected.

I think Idenix is also full of shit. Expect late 2018 if their drug actually works (and doesn't kill people)

Even if Idenix succeeds with their own therapy, they don't have a means to produce & market the drug.... Instead they will get a few miserable pennies on the dollar from a shitty royalty agreement.

So there you have it.... a $6 stock that's really worth $2 with all of the stuff it's got going against it.

But boy... some delusional guy in his mom's basement thinks otherwise!!!

You gave me a reasoned response and I will give you my humble opinion in return.

"Idenix will (likely) lose the patent fight as stated in above document"

I do not think so because for several reasons;
- There are about 7 cases which fall under different patent laws (ie - other countries) and Idenix has the earlier patents.
- The first case was over "structure of matter" and I can give you an argument that Merck owns the rights to this. I believe that is why Idenix took a sublicense.
- The current intereference involves "Method-of-use" and is a much stronger case.
- The 2 or 3 judges ruled incorrectly about "enablement" and "reduction to practice" which lead to the denial of the earlier patents which lead to a "loss" in the first case.....WHICH WILL BE APPEALED. Many cases are overturned on appeal.
-There are jury based infringement trials coming. A jury will not be fooled by "Lawyer Tricks" and judge based on the earlier patents.
-It really isn't hard to make the prescribed molecule based on the structure: one can get there many ways if they really put their mind to it. The idea is to get there with the highest yield (ie, above 80-90%)
-Gilead can lose based on things turning up through Discovery: That is exactly what has happened and the current court WILL LOOK AT THIS EVIDENCE

"Idenix cannot get its own treatment on the market until 2017. That's optimistic because most of Idenix's earlier candidates didn't make it. "

That is for the most part true. IDX-184 would have been in-licensed by Merck on a non-exclusive basis if it did not get caught up in something totally unrelated to the drugs safety and efficacy (which was excellent and moderate respectively) It was due to the over-reaction of the FDA to INX-189 (a copy of IDX-184; a very unsafe copy). It would have also done quite well in combination with IDX-719 if the fda didn't freak out. In essence...drug discovery got pushed back 2 years over companies trying to copy the molecules of Idenix. Alios's was also a copy. They both would have faced a patent challenge of their own if ever made it to market. My guess is that 437 will be in more than one combination regimen by early next year: Merck's and Idenix's own combo pill

"Hitting the market in 2017 is long after therapies from Gilead, Abbvie, Merck, JNJ, Bristol, and Boehringer Ingelheim are expected. "
Give me a break. We all know that there is no real competition against Gilead without owning a Nuc (Abbvie.....JNJ.....Boehringer : now I am laughing so hard it hurts) Abbvie's second gen could be a challenge IF NOTHING CHANGED between now and 2017 when they hit the market. It will. A 12 week course will be obsolete by then. Look for Merck and Gilead to both add a DAA to their current combo pill and definitely get down to 6 weeks but try for the 28 day cure. So if Abbvie does not in-license a nuc then their 2nd gen will be obsolete before it ever shows up on the market.

"Even if Idenix succeeds with their own therapy, they don't have a means to produce & market the drug.... Instead they will get a few miserable pennies on the dollar from a shitty royalty agreement."

They have already marketed a HBV medicine together with Novartis. Don't you remember. It was called Tyzeka and they manufactured the drug for this joint arrangement. Second, this therapy is currently marketed by small sales forces of 120-150 individuals. Not complicated.

Your point on a small pennies on the dollar settlement. Wrong, this is a key patent at stake here. The only technolohy not at stake is Gilead's awesome prodrug that was developed by Michael Sofia who I know. He was the reason that the drug is called sofosbuvir. Regardless, a settlement or judgment would bring in 25-40% royalty in my opinion based on the key nature of the patent. The judgment could also bring a 3X penalty along with it.

"So there you have it.... a $6 stock that's really worth $2 with all of the stuff it's got going against it. "
You have no clue about valuations. There is over $2 in value per share based on nothing other than NOL (net operating loss) which is valued at around 300 million (NOL of 900 M x 35% corporate tax rate)

We obviously disagree, but enjoyed the discussion.

 

[Anonymous]

As I prepare my BBQ for an awesome pool party tonight, I think its fair to share my thoughts on current valuation: $500-$600 per share.It will not get there overnight -but it will get there in less than 1000 days. Chow!

 

[Anonymous]

Keep it coming. I am enjoying your posts.

 

[Anonymous]

I still dont know why you continue to throw up your garbage on this board. I really wish you would just go down to your mothers basement and kill yourself. We dont care about idenix or anything you have to say. This company will go broke and bankrupt soon enough and hopefully by then you will not be using up valuable resources like the oxygen that normal people need to breath. Be smart and take a gun to your head.