[Ip-health] A US court judgment that is relevant to Novartis case

[chan park]

--
[ Picked text/plain from multipart/alternative ]
fyi - the full decision is available at http://fedcir.gov/opinions/06-1261.=
pdf.

this decision casts doubt on the validity of all patents and pending patent=
 applications relating to converting a drug into a "pharmaceutically accept=
able" salt form.  in arguing that it was obvious to convert amlodipine (the=
 active ingredient) to amlodipine besylate, apotex argued that it was well =
known in the art to convert a drug into its salt form in order to improve i=
ts stability, solubility, hygroscopicity, manufacturability, etc.

in the present case, apotex relied on a 1977 article:  Berge, "Pharmaceutic=
al Salts," J. Pharm. Sci. 66(1):1-19 (Jan 1977) to show that it was well kn=
own in the art to convert a drug into its salt form for these reasons.  sin=
ce the priority date of the patent at issue in this case, there have been f=
urther advancements in the science of salt selection.  for instance, in the=
 gleevec opposition, we successfully relied on the following article to sho=
w that the salt selection process was routine and non-inventive :

Morris, et al., =93An integrated approach to the selection of optimal salt =
form for a new drug candidate,=94 International Journal of Pharmacuetics 10=
5 (1994) presented an integrated, three-tiered approach to selecting the op=
timal salt for any given new drug candidate.  Starting from a pool of seven=
 possible salts, the authors proposed an approach by which the least time-c=
onsuming experiments were conducted in the first tier, and the more time-co=
nsuming experiments were conducted as more and more candidates were elimina=
ted in the earlier tiers.  Using this approach, the authors concluded that =
the entire salt-selection process could be completed within 4-6 weeks or le=
ss and easily be adopted into the drug development program.

the holding in the pfizer v. apotex case supports the proposition that conv=
ersion of a drug into a salt form to improve its stability, solubility, hyg=
roscopicity, manufacturability, etc will essentially always be non-inventiv=
e, because such improvements, even if real, are very well known in the art,=
 and are neither "unexpected" nor "surprising."

this decision is also notable for its rejection of pfizer's proffer of evid=
ence to show that it had invested substantial sums of money into research a=
nd development as a secondary consideration of nonobviousness.  the court a=
lso implicitly holds that one must compare the compound at issue against th=
e "entire range of prior art compounds,"  even if not expressly disclosed i=
n the prior art.

this is significant - particularly in india with section 3d - because it pl=
aces the burden on the applicant to show that its application represents no=
t only an improvement over the free base compound, but over all other deriv=
atives contemplated by the disclosure of the free base.  we successfully us=
ed this argument in the gleevec patent opposition to show that any improvem=
ent in "efficacy" had to be shown as between b-crystalline imatinib mesylat=
e versus other forms of imatinib mesylate, and not the free base, imatinib.

happy opposing,

chan

Joana Ramos <joaninha@comcast.net> wrote: http://www.hindu.com/thehindu/hol=
nus/006200703251901.htm


A US court judgment that is relevant to Novartis case

The Hindu Online
Business

D Murali

Chennai, March 25: A recent decision of a US court may be relevant for a
case currently on in Chennai court, says Ms Srividhya Ragavan, Associate
Professor of Law, University of Oklahoma Law Center, in a mail sent to
Business Line. "On March 22, the United States Court of Appeals for the
Federal Circuit, which is the highest court in the US for patent
appeals, issued a judgment on the same lines as the Indian statute and
the Chennai Patent office," she explains. Novartis, which has been
criticised by health activists for challenging Indian patent law in
Chennai court, is said to be seeking the support of the European
Parliament's members.

Here's more from Ms Ragavan about the case.

First, the Novartis case, in India.

As many of us are already aware, the Chennai Patent office's refusal to
award patent protection on Gleevac has been challenged by the drug maker
in the High Court. The Chennai Patent office rejected an application on
Gleevac on the grounds that the material sought to be patented by
Novartis was obvious and hence, unpatentable. An invention has to be
useful, novel and nonobvious in order to become eligible for patent
protection. In order to determine whether something is nonobvious, the
material (sought to be patented) is compared with the existing materials
in the same field of science. If the application material embodies
adequate levels of skill when compared with the existing state of
knowledge, then it can be deemed nonobvious.

What does the Indian law on the subject say?

As far as chemical inventions are concerned, Section 3 (d) of the Indian
Patent Act deems a mere discovery of a new form of a known substance as
being obvious and hence, not patentable unless it also results in an
enhanced efficacy. (What amounts to enhanced efficacy is left to the
purview of the examiner through patent office guidelines). The statute
outlines that forms of known compounds like "salts, esters, ethers,
polymorphs, metabolites, pure form, particle size, isomers, mixtures of
isomers, complexes, combinations and other derivatives" would be treated
as the same substance or just as obvious variations. The Indian Patent
Act deems that if Chemical A is already known, other forms of Chemical A
like salts, isomers, esters etc., are just considered as different forms
of Chemical A and not as a new invention.

How is that relevant to the Novartis case?

The Novartis application seems to relate to an isomer of an existing
compound. That is, the active ingredient in Gleevac was known. Novartis
felt that it was the first to invent the isomer of that compound. The
Chennai patent office felt that it is just another form of an already
known and existing compound and hence, did not qualify as an invention.
When the atoms of a known compound are arranged differently, we call
them isomers. Thus, an isomer of Chemical A will have the same chemical
formula although the atoms are arranged differently. (Different
structure but same formula). Novartis argues that isomers should be
considered nonobvious over the existing compound.

Now, the US case. What was it about?

Pfizer, a huge pharmaceutical giant filed a suit against Apotex, a
generic drug maker for infringing its patent on Norvasc. Norvasc is used
to treat hypertension and some forms of angina. The active ingredient in
the drug Norvasc is amlodipine but the ingredient is tinkered with and
made into acid addition salt form. Thus, Norvasc is a besylate form of
amlodipine (amlodipine besylate). Besylates are anacid addition salt
forms of the original chemical. That is, if we assume that Chemical A is
the original compound, Besylate of Chemical A is the salt form of
Chemical A. In this case, amlodipine besylates is an acid addition salt
form of amlodipine. Pfizer acquired a patent bearing number 4,879,303
over amlodipine besylate in 1989.

What was the contention of Apotex?

When Pfizer sued for infringement, Apotex alleged that Pfizer's patent
is invalid because the invention was obvious from Pfizer's own previous
patent on amlodipine. Apotex pointed out that Pfizer was the patent
owner over amlodipine (US Patent No. 4,572,909) which was issued in
1986. Amlodipine besylates, Apotex argued, are just the salt form of
amlodipine and hence, are just obvious improvements.

What was the decision?

The Federal Circuit agreed with Apotex and held that amlodipine
besylates was prima facie obvious over amlodipine. It is notable that
there was no significant or enhanced utility in the besylate form. The
Federal Circuit ruling merely reiterates an established principle that
salts of known compounds are deemed to be obvious unless there is an
unexpected utility or improvement or efficacy.

On the verdict's relevance to India

The principle reiterated by the Federal Circuit is what is already
present in the Indian statute. Section 3(d) also states the same
principle - salts, isomers, esters are not inventions but mere different
forms of the same substance. In rare instances, they may be considered
as inventions if they have an enhanced utility. The burden to prove and
convince an examiner that there is an enhanced utility was clearly on
Novartis. And, Novartis failed. Having failed its burden, Novartis lacks
sufficient grounds to argue that the Indian statute should be amended.
If at all, the US Federal Circuit judgment indirectly supports and
affirms the Chennai patent office decision.


--
Joana Ramos, MSW
Cancer Resources & Advocacy
7303 23rd Ave. NE
Seattle, WA  98115
206-229-2420
http://ramoslink.info/

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