Amsterdam Lecture.285123142

8/8/2019 Amsterdam Lecture.285123142

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* To the extent that any legal theories or opinions are expressed, such theories and opinions are those of the author and

not those of the Perrigo Company. Nothing in this presentation constitutes the providing of legal advice or analysis.

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2


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Trends in API / Pharma

Patent Filingand Par. IV Activity

Number of generic filings on the rise

Number of generic filers on the rise Increased number of Par. IV filers

Larger proportion of Par. IV challenges

Intensification of the brand-generic patent litigations

Earlier generic filing Inter-generic litigations

Brands seem to deal less with true inventions and more withgenerics blocking

3


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Number of Brand Patent Families

in 2006 Returned to the 1996 Values

Pfizer

GSK

AstraZeneca

Merck&

Co

BMS

0

100

200

300

400

500

600

700

1996Publication Year

NoofatentFamilies P

fizer

GSK

AstraZeneca

Merc

k&Co

BMS

0

100

200

300

400

500

600

700

2001

Publication Year

No

ofPa

tentfamilies

Pfizer

GSK

Astra

Zeneca

Merck&Co

BMS

0

100

200

300

400

500

600

700

2006Publication Year

No

of

a

tentfamilies

Pfizer GSK AstraZeneca Merck & Co BMS

Source: Perrigo

Data from: Chemical Abstracts database 4

1. Pfizer search included the companies Warner Lambert, Pharmacia, Kabi Pharmacia, GD Searle, Calgene and Farmitalia

2. search included the companies Burroughs Wellcome, Corixa, SmithKline Beecham, Smith KlineFrench, and all Glaxo Smith Kline subsidiaries3. AstraZeneca search included all AstraZeneca subsidiaries and Zeneca Group

4. Merc Co. search included all Merck & Co. subsidiaries and Merck Sharp & Dohme5. BM search included all E R Squibb subsidiaries and all Bristol-Myers Squibb subsidiaries


5/44

Brand Life-cycle Extension

trategies Also nown as total product strategies, evergreening or lifecycle maximization

Brands stand to lose 70-80 % of their revenue on first generics launch and up to 85-95 % onmultiple launch, so the incentive for LcE is very strong

The generic penetration increases every year, with US penetration reaching 54% (or 61%including approved generics) and EU penetration varying according to country from 5-65%.

LcE activities begin very early but become more aggressive towards the end of patents life.

Brand LcE tactics are improving all the time and adapt to changing legislation and generictactics

Brands spend $50-400 mill dollars per product for LcE

An important part of the LcE budget is used for lobbying for new legislation favoring brands,

placating generic legislation, patent law, etc Litigations and patenting activity are the largest LcE budget item

Multiple strategies are employed for each product

5Source: Combating Generics:

Pharmaceutical Brand Defense for 2007


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Brand IP and Regulatory Tactics

API Patenting the genus and disclosing the species in a later patent, several years later.

Sketchy description of the NCE in the seminal patent (NMR, etc), with full characterization ina later patent (e.g. oily to crystalline)

New salts, new derivatives

Next generation products (active enantiomer, etc)

Increasingly complex, difficult to synthesize organics and new biological molecules

Final Dosage Forms

New formulations, such as modified release (controlled, extended, fast-release, once-daily,pulsatile, ODT)

New indications

New dosage forms (nasal, buccal, injectable, spray, patch, transdermal, foam, etc)

New dosages, new dosage regimens, patient monitoring, database dispensing

Combination products (two or more drugs in one delivery form)

Administration in conjunction with other drugs (pre-treatments, etc) Rx to OTC switch

Pediatric studies, population change

Legal action (litigations, motions) and regulatory action (citizen petitions, etc)

Generic subsidiaries and Authorized Generics

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To file or not to file?Pro

May help evade future

FtO problems

Deter competition

Strengthen marketing

Positioning

Safeguard IP

Con

Disclosing your strategy

to competitors

Providing ammunition

to the brand in Par. IV

Providing third parties

with litigation grounds

8

Defensive publication is a viable option but, as a fact,

it is not widely used


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Freedom-to-Operate vs.

Competitor Bloc ing Freedom-to-operate is a must, competitor blocking is desirable

Multiple approvals are commonplace (recently 13 approvals for Ambien),so competitor blocking is sometimes a life or death activity for the product

The brand is in a better position to block generics than generics are to blocktheir generic competitors

The timing of the application filing is paramount. FtO must be determinedvery early, while the impact of patent applications on CB can varyaccording to the timing of filing

Can generic patents totally block competition? In principle, yes, but thosecases are rare. Generic tactics can help

There are cases in which the generic competition is made particularlydifficult, although not always impossible

Brand and generic blocking patent filing activity intensified lately

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API Filing trategies

for eneric Products Aggressive and massive patenting, to scare away would-be

competitors

Potentially avoiding future FtO problems by early filing Filing competitor blocking patents

Countering generic competitors' IP by defensive patenting

Improved quality of the product

API polymorphs and amorphous forms

Various other properties related to solid state (particle size,flow properties, morphology)

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Pharma eneric Filing trategies

Limitations

Product must be bio-equivalent in order to get AB-rating.505(b)2 route presumes branding

New formulations must include inactives that are approved forthe same route of administration for at least the requiredconcentration (IIG). New inactives must be approved by amore complicated and expensive regulatory process and mayamount in 505(b)2 designation

Devices, packings, bottles, canisters, coatings, valves, arepatented separately and must be designed around as well.Designing around may amount in losing the look-alike effectneeded for marketing

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Generic

Competitor-Bloc ing trategies Processes

Patenting all the practical synthetic processes for the API

API properties

Patenting the amorphous API when the crystalline API is already protected(valganciclovir, candesartan cilexetil)

Patenting all the practical stable polymorphs and processes for the seminalpolymorph, if any

Patenting the API with low level of impurity and requestingpharmacopoeial monograph update to the new purity

Analytical methods Patenting a specific method of analysis and its marker, and requesting

pharmacopoeial monograph update to include this method

Formulations

Patenting the practical bioequivalent formulations

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Early Generic Filing

How early?

Onset of R&D activity for filing purposes should be

shortly after the identification of the API candidate

Ideally, this should start shortly after the brandproduct takes off in the first country

The CB may start somewhat later

Generic R&D activity for filing 15 years before theactual generic launch is not uncommon

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Purity Patents Purity patents (high assay, low level of specific impurities and solvents).

Brands do not always patent or otherwise make known the purity levels, so it maybe difficult to find prior art to challenge a purity patent. Analysis of the brandproduct to challenge novelty of the generic patent is not easy, and old samples

(before the filing) are not easy to find. Buying and storing brand samples detailingbatch production dates as soon as you start a project may, in the future, serve asuseful evidence of prior art purity profiles

The relevant ICH guideline is Impurities in New Drug Substances Q3A (R2),second revision, issued in October 2006. For any drug substance, this guidelinestates that any impurity present at a level of 0.05% or above must be reported. Thestructure of any impurity present at a level of 0.10% or more must be determined.

For impurities present at a level of 0.15% or more, a toxicological qualification toassess its risk to humans is required

The usefulness of such patents outside the US is questionable (see German AppealBoard decision T 990/96 on non-novelty of high purity claims)

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Solid

State API Patents

New polymorphs

Hydrates

Solvates, clathrates

Amorphous APIs

APIs with specific particle size ranges, or other

supposedly advantageous properties Specific particle surface area ranges

Specific particle morphology17


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Intermediates Patents Newly discovered intermediates, resulting

from new or known processes

Processes using specific intermediates

Polymorphic forms of intermediates

APIs containing low level of specific intermediates

The usefulness of such patents in the US and EP isquestionable if there are viable alternatives

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Patenting as a Mar eting Tool

As the market situation stands today, the product's IP

standing is a heavy argument, sometimes making orbreaking the deal

A secure IP standing for the finished drug form buysthe market entrance ticket, and sells the API. Moreand more, Marketing Managers are talking patents

with the prospective clients, and every newapplication published needs to be scrutinized andgiven a clean bill of health before the deal goesfurther

19


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PublishedGeneric Patent Families for

the period 2002-2006

Source: Perrigo

Data from: Data from: Chemical Abstracts database

and Thomson-Micropat

Torrent Pharma.

Woc hardt

lan/ atriurobindo Pharma

lembic td.

Glenmar Pharma.

Perri o

adila

etero ru s

arr

Watson/ ndr

upin td.

ipla td.

un Pharmaceutical

r. edd s

anba

Te a

rchid

0 0 100 1 0 200 2 0 00 0 00

Generic

ompan

o. of Patent Families

20


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Brea down by Strategy

of Published Generic Patent Families

2002-2006AP

0

20

0

60

80

00

20

0

Process SolidState Purity ntermediate

oofatentfam

ilie

Pharma

0

20

0

60

80

00

20

0

Formulation

odified

elease

e ice

nno

ati

e

0

20

0

60

80

00

20

0

AP

Pharma

Source: Perrigo

Data from: Chemical Abstracts database and Thomson- Micropat

anbaxy Te a r eddys Barr Sun Pharma Ci la

2


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Generic Patent Filing Strategies ofSelectedGenerics

2002-2006 Filings

Source: Perrigo

Data from: Chemical Abstracts database and Thomson- MicropatTable

22

Process Solid S

e Purity Intermediate FormulationModified

ReleaseDevice

!PI Pharma

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9otal

Innovative (%)

Innovative (%)

8

PI (%)

1 @A

B

f total3

@ TC

e following TeD a companie E weF e inclGH

eH

:TeD a I IvaP I NovophaF m, Biogal, BaQ

eF Cummins DeF matologicals, BaQ

eF Cummins Laboratories, BaQ

er Cummins Pharmaceuticals,

BaQ

er Norton Pharmaceuticals, Biocraft Laboratories, Galena, Pharmachemie,R

ssia, PlanteP and Sicor .

3- Plivaand Duramed Pharmaceuticals were included in the Barr search

4- In the Cadila search Cadila Healthcare Cadila Pharmaceuticals and Zydus Cadila were included

5- Perrigo search includedR

gis Industries and Chemagis

GenericPharma (%)

9

otalS

PI (%)T

9otal Pharma

(%)

U

otal No. ofPatent

Families

2002-2006


23/44

Is there a Correlation between the

Generic Patent Filing Activity and the

Number of ANDA Approvals? There is some parallelism

between the patent filing activitiesand ANDA approvals, but thereare exceptions as well (e.g.

Mylan/Matrix). Mylan has a smallnumber of filings but it has a largenumber of Par. IV filings, whichmight explain its success

Steep increase in the Indianpatent filings (see table) andANDA approvals from 12 Indiancompanies, led by Aurobindo,Wockhardt, Ranbaxy, Dr. Reddyand Sun. (Source FDA site andThe Business Standard, May 2007by PB Jayakumar)

Source: Perrigo

Data from: STN, Micropat, FDA.gov and

Paragraphfour.com sites23

AV V roval W irst X e Y eric e Y tative

a

eva/Ivab

/ c icor 354 97 29 12 23 64d

ae

f

ab

y 338 26 6 3 2 11g

r.d

eh h

y i s 235 26 13 4 5 22

Sp

e

q r

armacep

tical 116 10 7 0 9 16s

it

la

u

t

h

. 99 0 0 0 6 6u

p t

ie

u

th

. 70 7 5 3 2 10v

rcr

ih

s r

em &q r

arma 69 2 8 0 0 8w

atsoe

/Ae

h

rb 68 28 10 4 5 19x

arr 66 33 4 2 4 10y

eterog

rp

gs 66 0 0 0 0 0s

ah

ila 63 3 4 1 5 10q

errigo 60 4 7 3 2 12

lee

mar

q r

arma. 55 2 4 1 1 6

Ap

rof

ie

h

oq r

arma 45 3 9 0 7 16

ylae

/

atrib

38 26 9 7 9 25w

oc r

arh

t 33 3 0 0 1 1

rae

h

a

otal 1775 270 115 40 81 236

q

ar. I

filie

gsX e Y eric

otal o. of X e Y eric

ateY t W amilies

2002-2006

2006-AV V

rovals otal V er

om

Va

Yy


24/44

24


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Intensification of the Brand-Generic

Litigationss with aragraph I ha enge

35 33

96 975 92

0

20

40

60

0

00

20

200 2002 2003 2004 2005 2006

ear

u

verof

ar.I

ha

enges

Source: Paragraphfour.com

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Larger Proportion

of Par. IV Challenges

26

Source: FDA, Patent database, IMS Health,

Bernstein estimates and analysis


27/44

Increased Number of Par. IV Filers

20

40

5

6764

7

0

0

20

30

40

50

60

70

0

200 2002 2003 2004 2005 2006

Year

N

.oP

ar.

Vi

ler

After 2003, about 42 genericcompanies had active Par IVfilings.

The number of companies after2006 increased to 67

Thus, new players have enteredthis market.

The average number of filers percase has increased from 1.5 to 2.0.High volume products (>500 $

mill) have 6.1 filers and AGs andlower volume have 3.1 filers

Some cases have a much largernumber of challengers (Claritin 15 filers)

Sources: ParagraphFour.com and

Berndt, Mortimer, Parece-April 2007 27


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Patents and the Generic Competition

The Impact of the Indian Penetration into

Regulated Mar ets

Zestril (Lisinopril) 17 companies received FDA approval

Ambien (Zolpidem) 13 companies obtained FDA approval

India has now over100 FDA-approved production facilities

Over 40% of the total DMF files applications are filed byIndian companies

Over 33% of the new ANDAs are filed by Indian companies

The growth of the US generic drug market has slowed fromdouble digits to single digit (from 17% in 2000 to 8.3% in2006)

The market environment has become very crowded

28Source: Business Standard, June 6, 2007 by Joe Matthew/New Delhi


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Generic vs. Generic Litigations

The number of generics offering the same API orformulation on patents expiry is on the rise

The net result is price erosion, as many companies arebuilding large inventories with high hopes ofunloading at launch, only to find out that everybodydid the same

As the generic landscape becomes more and morecrowded, G vs. G litigations might become the rulerather than the exception

29


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Generic vs. Generic Litigations

Other Cases Teva vs. nine generics over carvedilol process and

polymorph patents

Apotex vs. Eon Labs over a cyclosporin formulationpatent

LEK vs. Watson over a polymorph patent ofpravastatin. Watson is the AG for Pravachol.Watsons API is probably supplied by the brand

(Sankyo) Teva vs. Apotex over a polymorph patent and a purity

patent related to pravastatin

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Generics vs. Brand Litigations

LEK sued BMS over Pravastatin, asserting its

rights to a crystalline form. BMS apparently

did not describe the crystalline form in the

seminal patent, but used spray drying,

probably obtaining amorphous form

Synthon sued Pfizer over a amlodipine processpatent. Court decided in Pfizers favor

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Pro-generic S Legislation

and Court Decisions Biosimilars, rebranding (authorized generics) frivolous citizen petitions and

early resolution of patent disputes Waxman Feb. 2007 Access to LifeSaving Medicines

Two bills on authorized generics Rockefeller and Schumer FairPrescription Drug Competition Act of 2007 (Senate) and Emerson andWamp (House)

Reverse payments Kohl January 2007 Preserve Access to AffordableGenerics Act

The positive Court of Appeals declaratory judgment decision in Teva vs.Novartis on Famvir (Famciclovir)

Norvasc (Amlodipine) decision in Apotex vs. Pfizer A U.S. Supreme Court decision that recently rejected rigid application of

the teaching-suggestion-motivation (TSM) standard in the KSR vs.Teleflex case and the Norvasc Apotex vs. Pfizer Court decision mayweaken patent positions on new salts, enantiomers and crystal structures

34


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Pro-generic EP Legislation

and Court Decisions Directive 2004/27/EC and its provisions (the European Bolar)

Teva/Arrow/Generics UK vs. Lundbeck decision over narrowing of theescitalopram (Cipralex) patent

Actavis vs. Merck UK decision on revocation of the finasteride (Proscar)patent 444

Egis Gyogyszergyar and Neolab vs. Ely Lilly German decision onrevocation of the olanzapine (Zyprexa) patent 436

Ivax, Cipla, Neolab, Generics, Arrow vs. GSK decision on Seretide(fluticasone and salmeterol) patent revocation

German Federal Supreme Court decision on carvedilol dosing regimens Clinical studies in Germany for registration purposes are not infringing(Clinical Trials II German Constitutional Court)

35

Source: Perrigo

Simon Cohen Taylor & Wessing

Dr. Thomas Albrecht- Kraus & Weisert


36/44

US Patent Reform Act of2007

First-to-file rights and elimination of interference proceedings

Reform to make it easier to file a patent application withoutthe inventor's cooperation

Limitation of damages to only the economic value of theimprovement as compared to the prior-art;

Specific limitations on when damages may be trebled forwillfulness

Post-grant opposition proceedings with a reduction in the

litigation estoppel effect Limitations on patent venue

Authority to the PTO director to create further regulations

36


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Conclusions

The event horizon of the patenting activity onsetbecomes longer every year

The regulatory environment is a moving target The patent law and its interpretation are changing

The generic landscape has become very crowded, andthis is and will cause quantum leaps in the behavior

of the players Generic patenting has morphed from a scientific

activity to an art form

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Thank you!


40/44

Total No. of Pharmaceutical Patents

Over the Years

0

0,000

20,000

30,000

40,000

50,000

60,000

996

997

99

999 2000 200

2002 2003 2004 2005 2006

Publication year (Basic patent)

No.ofpatent

er

entfamilies

The number of patent

families in the broadpharmaceutical

classification has more

than doubled in the last

decade.

Source: Perrigo

Data from: Derwent world patent index database


41/44

B- Derwent Classification Definition

Derwent ClassificationSystem: Pharmaceuticals(http //scientific.thomson.com/support/patents/dwpiref/reftools/classification)

All patents stated to be of pharmaceutical or veterinary interest, as well as those relating to compounds for use asintermediates in the manufacture of pharmaceutical or veterinary products. Compositions used for diagnosis and analysis inthe pharmaceutical and veterinary fields (eg stains for bacterial pathogens) are also included.

Artificial sweeteners, chemical warfare agents and plaque disclosing compositions are also included.

Patents dealing with the production of tablets, pills, capsules, suppositories etc. are included, as are devices for dispensingpharmaceuticals such as - syringes, child-proof closures, calendar pill boxes, aerosols etc.

For each compound where more than one of the classifications given below could be assigned, then the order of priority is B1before B2, B2 before B3.

B01 Steroids - including systems containing carbocyclic and/or heterocyclic rings fused onto the basic steroidal ringstructure.

B02 Fused ring heterocyclics.

B03 Other heterocyclics.

B04 Natural products and polymers. Including testing of body fluids (other than blood typing or cell counting),pharmaceuticals or veterinary compounds of unknown structure, testing of microorganisms for pathogenicity, testing ofchemicals for mutagenicity or human toxicity and fermentative production of DNA or RNA. General compositions.

B05 Other organics - aromatics, aliphatic, organo-metallics, compounds whose substituents vary such that they would beclassified in several of B01 - B05.

B06 Inorganics - including fluorides for toothpastes etc.

B07 General - tablets, dispensers, catheters (excluding drainage and angioplasty), encapsulation etc, but not systems foradministration of blood or saline or IV feeding etc.


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Sertraline Patents and Applications

Source: Dolphin-Thomson Scientific

Assignee Product

Processes

and

intermediates

Formulation Polymorphs New Use Combination

Derivatives

(Salts,Optical

Isomers etc.)

Pfizer (brand) 1(expired)

12 13 1 6 12 2

Teva 0 2 0 6+4 (US appl.) 0 0 1

Ranbaxy 0 1 3 0 0 0 0

Cipla 0 0 0 2 0 0 0

Sandoz 0 0 0 1 0 0 0

Cadila 0 0 0 1 0 0 0

Torrent 0 0 0 1 0 0 0

Comments : Patent count was performed by first counting US patent in the family then US appl., PCT appl. and EP patents


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Tevas Sertraline Patents Tevas Patents in Litigation

US6495721 - Sertraline hydrochloride Form II and methods for the preparation thereof

US6500987- Sertraline hydrochloride polymorphs

US6600073- Methods for preparation of sertraline hydrochloride polymorphs

US6897340- Processes for preparation of polymorphic form II of sertraline hydrochloride

Patents/ application belonging to the litigated family

US7022881 - Sertraline hydrochloride polymorphs (Reissue of 10/218,863 abandoned which is acontinuation of 987 above)

US2006/0241189 - Sertraline hydrochloride polymorphs (continuation of 10/218,863 abandonedwhich is a continuation of 987 above)

US2007/038005 -Sertraline hydrochloride Form II and methods for the preparation thereof

US2007/0093557 -Sertraline hydrochloride Form II and methods for the preparation thereof

Other Teva Patents applications

US6452054 - Novel sertraline hydrochloride polymorphs, processes for preparing them, compositionscontaining them and methods of using them

US6858652 - Novel sertraline hydrochloride polymorphs, processes for preparing them, compositionscontaining them and methods of using them

US2005/0085669 - Process for the preparation of sertraline

US2007/0010694 - Processes for the preparation of sertraline

O2007/008317- Process for preparation of sertraline hydrochloride form I

US20070100165- Process for preparation of sertraline hydrochloride form I


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Number of Brand Patent Families

in the Last Decade

P .B 1996 2001 2004 2005 2006

Pfizer 326 567 612 440 297

SK 212 607 277 287 252

erc 235 222 218 204 225

Astrazeneca 142 232 245 221 240

B S 122 100 159 102 81

Amsterdam Lecture.285123142

Documents

Transcript of Amsterdam Lecture.285123142