This analysis shows how IP, regulatory, and marketing strategy have to interfere for maximizing the lifetime of IP protection in pharmaceuticals. In contrast to mechanical inventions you can use special aspects of chemical /pharmaceutical patents like medical use or SPCs and PTE or variations in formulation to optimize your product protection. Using the example of an active ingredient it is shown how filing strategy, product development and finally IP life cycle management can be combined to achieve the maximum market success.

1. 20 years is not enough
Ch. Hoock – PATON
18.10.2016

2. 2
20yrs// ICIC
Heidelberg 2016
Agenda
 PATON
 Patent strategy
 Life cycle management of
pharmaceutical patents

3. 3
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
• Thuringia Patent Centre PATON, founded 1895,
since 1957 located at the Technical University Ilmenau
• Dedicated to support you regarding all aspects of
industrial intellectual property (IP)
• From idea to innovation

4. 4
20yrs// ICIC
Heidelberg 2016
PATONINFORM
About us
PIZNET (PATLIBS)
PATON – State patent centre at Technical
University Ilmenau
(Landespatentzentrum Thüringen)
Public reading/searching room
Receiving of patent filings, utility models,
designs, and trademarks on behalf of
DPMA (German Patent office)
Search & Analysis Services
PATON-Academy:
University curricula, seminars, training on
scientific and patent information
Technology transfer:
assessment of the economic potential of
an invention; selling/out-licensing of IP
PATINFO (31.05.-02. 06.2017)
Patent Information Technology:
software development
full text services
statistical analyses of patent data

5. 5
20yrs// ICIC
Heidelberg 2016
PATONINFORM
About us
Receiving of patent
/trademark
filings
Patent marketing/
technology transfer
PatentIdea Innovation
Customized in-
house databases
Custom Online
searches
Trend analysis in
Science & business,
competitive
intelligence
Full text delivery
Patent library:
assisted online
searches
Consulting
Support
Training
One Stop Shop for all Patent Services

6. 6
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy general
 To file or not to file
 When
 Where

7. 7
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy general
SMEs
SME strategies of IP protection:
source: Inno-Tec Study 2010 LMU
Patents Secrecy Copyright complex design head start
suitable very suitableOKNot suitableTotally unsuitable

8. 8
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy general
As soon as possible:
• How likely is competition?
Danger of patent filing by
competitors or publication
• Observe patent strategy of
competitors
As soon as necessary:
• estimate development time
(<20yrs?)
• Development projection:
satisfy 18m to disclosure?
• Is the market ready?
when
R & D
First
effects
Testing
secure
knowledge
Date of filing

9. 9
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy general
Advantages:
- Flexibility
- Competitors long in the dark
- Developments of the invention
can be used for drafting more
precise claims
- Diversion divisional applications
- DE: “Branch off” of utility model
from pending application
- …
Disadvantages:
-Filed vs. granted patents in
patent statistics (portfolio value,
stakeholder)
-Poorer legal position in case of
infringement
-Utility patents not for
procedures, methods
when
Late Granting

10. 10
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
Economic relevance of the designated state
• Market size in the range of the invention
• Own position in the market
• Licensing potential
Legal framework
• Patentability
• grant procedure (length, costs, examination?)
• Enforceability in case of infringement
• Licensability to third parties
patent strategy general
where

11. 11
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma

12. 12
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
general
Differences to technical patents:
- Long development time (10 – 20 yrs.)
- Long product cycle (30 yrs. or more)
- High costs of development (NCE 500- 1000 Mio. €)
- High value of single invention
- High risk
- Special IPR for use („medical use“)
- Registration procedure necessary
- SPCs / term extensions

13. 13
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
general
Differences determine procedures for:
• Filing – Strategy
• Litigation - Strategy
• Market Strategy (launch)
• R & D - strategy
• Registration strategy (market authorisation)

14. 14
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
* Patent expiry:
Lipitor: November 2011
Seroquel: April 2012
Plavix: May 2012
Diovan: September 2012
Zyprexa: October 2011
Sales of blockbuster drugs before and after the patent expiration * in 2011 and 2012 (in bill. $)
7.087
9.580
5.665
4.622
4.338
2.547
3.900
4.417
1.701
1.294
0
2.000
4.000
6.000
8.000
10.000
12.000
Plavix (Sanofi/ BMS) Lipitor (Pfizer) Diovan (Novartis) Zyprexa (Eli Lilly) Seroquel IR (Astra
Zeneca)
SalesinMioUSD
Drug (Originator)
Sales 2011 Sales 2012
Source: Thomson Reuters

15. 15
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
Source: IMS health /GPhA 2015
Development of the price reduction of medicines after patent expiry in the US in 2015
-90,0%
-80,0%
-70,0%
-60,0%
-50,0%
-40,0%
-30,0%
-20,0%
-10,0%
0,0%
0 12 24 36 48 60 72 84 96 108 120
Pricedecline
Months after patent expiry
Oral drugs all drug forms

16. 16
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
Active
Ingredient
Indication
Process
Formulation
Dosage
patent strategy Pharma
general

17. 17
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
Active
Ingredient
Indication
Process
Formulation
Dosage
Indication II, III
Intermediates
Analysis methods
Test systems for identification
of mode of action
process II, III…
Packaging
Routes of
administration
SPC
patent strategy Pharma
general
Dosage form

18. 18
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
what
source: VFA, “Forschung für das Leben 2015”
Drug developments of VFA members with est. MA by 2017 (NMEs)
Bio-tech
Vaccines
Natural products
Cells
Chem. Synthesis
Size of drug molecules
a) Chem. Synth.:
ASA (aspirin) 21 atoms
b) Chem. Synth.: Ramipril 62 atoms
c) Natural product:
Ciclosporin 196 atoms
d) Biotech: Insuline 790 atoms
e) Biotech: mABs 20.000 atoms

19. 19
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
Pre-clin.
Lab
0 Pers.
Months to yrs
clin. ph. I
Pharmacokinetics,
pharmacodynamics,
safety and
tolerability of the
drug
10-50 Pers.
Weeks/months
clin. ph. II
a) Proof of
concept
b) Dose finding
50 – 200 Pers.
months
clin. ph III
Proof of
effectiveness in
studies, often
against standard
placebo
Often> 1000
pers.
Months to years
clin. ph. IV
Observations on
the market,
Often the basis
for further
development
Filing date
Marketing authorisation,
launch
Phases of clinical development
patent strategy Pharma
general -when
5y
10 y 15 y 20 y

20. 20
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
Pre-clin.
Lab
5.000-
10.000
clin. ph. I
6.7
clin. ph. II
4.3
clin. ph III
3.3
clin. ph.
IV
1
Marketing authorisation,
launch
patent strategy Pharma
general -when
Success rates for market entry are low – selection from 5.000-10.000:
source: Paul, S.M., et al.: Nature Reviews Drug Discovery 9, 203–214 (2010)

21. 21
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
general -when
First filing without exact definition of
structure: Markush- formula
Publication of drug effect of pre-clinic
or early clin. phases as long possible
linked to „Lab-Codes“
Lab-Codes not clearly defined:
not for 1 substance, but for project or
for group of substances
1 Lab code  more substances or
1 substance  more Lab Codes:
„Losartan“ (DuPont):
MK 954, DuP 753, L-158086,
MK-0954, E-3340

22. 22
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
where
Due to high investment: broad protection necessary
First filing national (to win priority year), PCT focussed to:
• Developed countries (potential production sites)
• Market (with premium price!)
• Countries where patent protection influences sales price (e.g. EU, CN)
 Costs for filing + prosecution often of secondary interest
 Often > 20 countries
Reason:
• competitors will use regional patent gaps as high profit margins give
good opportunities, even if the market is limited to small countries.
• Reduce development/production in "patent-free countries“ –
changed situation in China, India (Israel)
• Expensive development + authorization procedure must be recouped
through worldwide revenues.

23. 23
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
SPC
Definitions
SPC = Supplementary Protection Certificate
PTE = patent term extension
SPCs can extend the protection (exclusivity period) for DRUGS and
Plant protection products up to 5 years.
PIP = Paediatric Investigation Plan
Paediatric studies can extend the SPC term by 6 months
Art. 63 EPC (DE Art 49a PatG)
EEC1992 no 1768/92 products for human or veterinary use
EC 1996 no 1610/96 products for plant protection
EC 2006 no 1901,1902/2006 medicinal products for pediatric use
EC 2009 no 469/2009 medicinal products

24. 24
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
- Market success depends on patent protection +
marketing authorisation
Extension of the exclusivity 1: SPC
Extension of the SPC 2: PIP (ZLV) Zertifikatslaufzeitverlängerung
Patent Marketing Auth.
SPC/PIP
0 J.
20J. 25J.
SPC PIP (ZLV)Patent
M.A.
patent strategy Pharma
SPC

25. 25
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
Patent filing
Max 25,5 yrs
protection
20 yrs (PatG §16,
Art. 63 EPC)
1. EEC-M.A.
max. 15,5 yrs
max. 5,5 yrs
Patent/SPC-expiry
Launch generics
SPC
dossier protection 8+2+1 yrs
(Art. 10 Dir. 2004/27/EC)
1-2 y. generics
development
M.A.
generics
current model of generic drug approval in EU
patent strategy Pharma
Calculation of SPC expiry

26. 26
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
SPC
1986 launch of Prozac® (Fluoxetine - antidepressant ) in UK,
Patent expiry 1995. About 80% of Prozac sales during SPC term
source: IMS health
„SPCs worth millions to Pharma Companies in Europe”

27. 27
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
SPC
SPC-Impact
INN EU_MA SPC PAT_EXP SPC-yrs
Carvedilol 18.04.1990 07.04.2004 07.04.1999 5
Enalapril HCT 15.11.1993 10.12.2004 10.12.1999 5
Ciclosporin 01.04.1992 26.02.2004 26.02.1999 5
Lamotrigin 05.11.1990 30.05.2005 30.05.2000 5
Terbinafin 03.10.1990 07.08.2005 07.08.2000 5

28. 28
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
SPC
0
10.000.000
20.000.000
30.000.000
40.000.000
50.000.000
60.000.000
70.000.000
80.000.000
90.000.000
1991 1992 1993 1994 1995 1996 1997 1998 1999 2000 2001 2002 2003 2004 2005
CARVEDILOL
7.4.1999
Ca 150 Mio € Ca 350 Mio €
7.4.2004
Sales for Carvedilol in DE (per yr, originator).
30% during patent term( to 07.04.99), 70% during SPC (to 7.4.2004)

29. 29
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
SPC
LAMOTRIGIN
0
10.000.000
20.000.000
30.000.000
40.000.000
50.000.000
60.000.000
70.000.000
80.000.000
90.000.000
1991 1992 1993 1994 1995 1996 1997 1998 1999 2000 2001 2002 2003 2004 2005 2006
Ca 100 Mio € Ca 250 Mio €
30.5.2000 30.5.2005
Sales for Lamotrigine in DE (per yr, originator).
35% during patent term( to 30.05.00), 65% during SPC (to 30.5.2005)

30. 30
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
SPC/PTE where
Introduction varies nationally:
US 1984 Hatch-Waxman Act
JP 1988
In Europe in 27 EU countries + NO, IS, CH
1993: Belgium, Denmark, France, Germany, Ireland, Italy,
Luxembourg, Netherlands, UK
1994 EFTA - Austria, Finland, Iceland, Norway, Sweden
(+ Liechtenstein / Switzerland from 03.02.1995)
1998: Greece, Spain, Portugal
New EU Countries: From May 2004, Croatia (07/2013), different
transition periods
PTE / SPC also available in: Australia, Israel, Japan, Morocco, Russia,
Singapore, South Korea, Taiwan, Ukraine, Belarus, Serbia (2013..)
Not in: China, India, Canada, South America, South Africa, …

31. 31
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
„Me too“
"Me too" strategy
First member of a new class of agents (NCE = "new chemical entity") often
is not perfectly protected.
Other originators use gaps in the scope of the patent protection
"Me too" versions may not be covered by general Markush structure and
/ or show a selection, special, unexpected benefits, … in
Pharmacokinetics, efficacy, tolerance etc.
 NDA (complete new MA) needed

32. 32
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
Agopton®, Takeda
patented : 1985
authorized:1990
Losec®, Haessle/AZ,
patented:1979
authorized: 1987
Pantozol®, Byk Gulden/Altana,
patented: 1985
authorized:1994
Pariet®, Eisai,
patented: 1987
authorized:1998
patent strategy Pharma
„Me too“

33. 33
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
1960 1963 1965
1963 1980 CH 1978
patent strategy Pharma
„Me too“

34. 34
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
Life Cycle Management usually begins shortly after 1. M.A.
Reason: term of basic patent after M.A. often only 5-10 y. protection,
with SPC up to 15 years (+ possibly. 6m)
Possibilities:
Formulation patents (for example, 3 * times/d  1 * daily,
capsule  effervescent tablet)
New routes of administration: tablet, injection, suppositories
Identification of additional effects
Structural variants:
 Salts
 Hydrates /Solvates
 Pure enantiomers instead of racemates
 Polymorphs
 Prodrugs
combination products
E.g.: Antihypertensives + diuretics,
aspirin complex (aspirin + pseudoephedrine HCl)
patent strategy Pharma
„Life Cycle“

35. 35
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
Basic patent is often "only" protection of the active substance,
if necessary with reference to a possible pharmaceutical
application, for example alendronate
For substance X effect E1 is detected  first medical indication
Art. 54(4) EPC = 1st Medical Use
patent strategy Pharma
1st medical use
Broadest claim is functional:
"Use of effectors of dipeptidyl peptidase for lowering blood
sugar levels"

36. 36
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
1st medical use
Examples:
Alendronate, Henkel 1981 (EP39033):
Markush structure
use for water softening …
also suitable for production of cosmetic or
pharmaceutical preparations
MSD (Inst Gentili.) 1983:
Patent claim:
(US04621077A)

37. 37
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
For substance X effects are E2, E3 discovered 
second and further medical use
The second indication is defined as a new and not obvious therapeutic use
of an already known substance in another field of medicine
The substances for medical use are also new, if this application is not part
of the prior art. (Art. 54 (5) EPC) = 2. Medical Indication
Example: Pfizer Sildenafil
E1) EP 0463756, 1991, Pyrazolopyrimidone as agents against angina
E2) EP 0702555, 1994, for the treatment of erect. Dysfunction (Viagra®)
E3) EP 1097711, 2000, treatment of pulmonary hypertension (Revatio®)
 SPC for E1 to 2013
patent strategy Pharma
2nd medical use

38. 38
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
2nd + further medical use
Source: Thomson-Reuters White Paper Sept. 2012 KNOWLEDGE-BASED DRUG REPOSITIONING TO DRIVE R&D PRODUCTIVITY
DRUGS THAT HAVE BEEN SUCCESSFULLY REPOSITIONED
DRUG ORIGINAL INDICATION NEW INDICATION
Amphotericin B Fungal infections Leishmaniasis
Aspirin Inflammation, pain Antiplatelet
Bromocriptine Parkinson’s disease Diabetes mellitus
Finasteride Prostate hyperplasia Hair loss
Gemcitabine Viral infections Cancer
Methotrexate Cancer Psoriasis, rheumatoid arthritis
Minoxidil Hypertension Hair loss
Raloxifene Cancer Osteoporosis
Thalidomide Morning sickness Leprosy, multiple myeloma
Sildenafil Angina Erectile dysfunction,
pulmonary hypertension

39. 39
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
In good time before expiry of the patent for a racemate of active ingredient
file a new patent protecting on pure enantiomer, usually in combination
with manufacturing processes.
Example 1: Haessle / AstraZeneca omeprazole  esomeprazole
Omeprazole EP 05129 filed 1979, 1st MA 1987 
Esomeprazole EP124495 fil.1984, 1st MA 2000 SPC to 2009
patent strategy Pharma
„Chiral switch“

40. 40
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
Example 2: Lundbeck citalopram  escitalopram (antidepressants)
Citalopram Pat 1976 - 1994 M.A. Jan. 1989
Escitalopram Pat 1989 -2009 to 2014 SPC  2014
Escitalopram (S Enantiomer)
Citalopram: (R)-Isomer
+ (S)-Isomer
As a drug initially was the racemate [1: 1 mixture of the (S) - form and (R) -form] used.
However, the effect is due to the (S) - (+) - enantiomer (escitalopram) of citalopram
patent strategy Pharma
„Chiral switch“

41. 41
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
First development must be launched quickly,
but is often not "ideal" form of the active ingredient.
Salt form:
Active compounds usually „large“ organic molecules which are
sufficiently soluble only as a salt.
Salt partners crucial for stability, solubility, pharmaceutical workability
Examples:
Pfizer -
Amlodipine maleate pat. 1983  2003, M.A. 1989 SPC  2004
Amlodipine besilate fil. 1987  2007 Norvasc®
Sanofi -
Clopidogrel (fil. 1983  2003)
Clopidogrel bisulphate (fil. 1988  1998 SPC  2013, Plavix®)
Generic "non-hydrogen sulphates"
patent strategy Pharma
„Salts, Hydrates, Polymorphes“

42. 42
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
„Salts, Hydrates, Polymorphes“

43. 43
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
Hydrates:
Azithromycin Pfizer / PLIVA
Basic formula, with Markush structure PLIVA, 1981 2001
1. EU approval: 04/1991, SPC  2006
Azithromycin - dihydrate (A * 2 H2O), Pfizer, filing 1988  2008
and
- Sesquihydrate (A * 1.5 H2O) vs. Azithromycin monohydrate and
dihydrate (EP 1390377 revoked 2009)
patent strategy Pharma
„Salts, Hydrates, Polymorphes“
EP298650B

44. 44
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
Polymorphism, that is, arrangement of the molecules in the crystal lattice,
influences:
Macroscopic crystalline form (cubes, columns, needles)
melting point
solubility
wettability
stability ("best before ...")
dissolution rate, …
Determinable by DSC and XRPD or sNMR
Examples:
Flupirtine maleate (Katadolon®), torasemide (UNAT®), ranitidine
(Zantac®), paroxetine (Seroxat®), azithromycin (Zithromax®)
Affected by the crystallization process: temperature, speed, solvents or
by heat treatment after crystallization or even mechanically!
patent strategy Pharma
„Salts, Hydrates, Polymorphes“

45. 45
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
Polymorphs:
DSC famotidine (Pepsid®) sNMR CRYSTAL FORMS OF AZITHROMYCIN
patent strategy Pharma
„Salts, Hydrates, Polymorphes“

46. 46
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
„Salts, Hydrates, Polymorphes“
Polymorphs A and B of Flupirtine Maleate

47. 47
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
Polymorphs of Torasemide (UNAT®, Diuretic)
Az. COMPANY EXP. REMARK PAT_FIL
P 25 16 025.2 Christiaens
Pharma
12.04.1993 Torsemide 12.04.1975
P 35 29 529.5
(Prio f. 36 67 970)
Boehringer
Mannheim
GmbH
01.05.1991 (ZRN4) 17.08.1985
P 36 67 970.4 Roche 12.08.2006 Torasemide Form I (UNAT®) 12.08.1986
P 699 22 977 Pliva 01.10.2019 18.01.08 (NIT0) Nichtigkeitsklage
zurückgenommen
01.10.1999
U 299 24 789 Pliva 02.11.2009 Toracard®; Torasemide N 01.10.1999
P 601 03 276 Teva STABILE PHARMAZEUTISCHE
Formulation DIE TORSEMID
MODIFIKATION II ENTHÄLT
21.02.2001
U 201 22 564 Teva 01.09.09 STABILE PHARMAZEUTISCHE
Formulation DIE TORSEMID
MODIFIKATION II ENTHÄLT
21.02.2001
patent strategy Pharma
„Salts, Hydrates, Polymorphes“

48. 48
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
Patenting of new galenic formulation
Pharmaceutical formulation affects:
Compatibility (as altered side effect profile with a slower rise in level)
Duration (1 * daily instead of 3 * day)
Potency (better bioavailability - 300mg instead of 1000 mg)
Durability (3 years instead of two years)
Administration (tablet instead syringe)
New formulations often have therapeutic benefits and higher patient
compliance
To block generics, old formulations are taken off the market, dropping
the original marketing authorisation.
patent strategy Pharma
„Formulation“

49. 49
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
Example Omeprazole Prilosec vs. Antra MUPS®
MUPS = Multiple Unit Pellet System. Antra MUPS® tablets are
compressed from small enteric coated pellets that disintegrate rapidly
on contact with fluid  better bioavailability.
Omeprazole MUPS® EP1078628 (filed 1995, rev. 2014), launched 1998,
generic competition for old formulation starting ‘99 (Hexal, Ratiopharm)
patent strategy Pharma
„Formulation“

50. 50
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
Drug is chemically modified (covalent bond).
Derivative is cleaved before / during / after absorption releasing the active
substance.
Benefits in bioavailability and pharmacodynamics and pharmacokinetics
 Is usually regarded as NCEs
Examples: EPO vs. PEG-EPO, PPIs (Sulfinylbenzimidazole), valacyclovir,
fosamprenavir, esters of steroids, insulin derivatives,…
patent strategy Pharma
„Pro-Drugs“

51. 51
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
Timing Life Cycle Management
First mention basic structure
S1: Defined structure
E1: structure S1 with effect E1
Marketing authorization
submit SPC for E1
F1: Formulation to structure S1 with effect E1
F2: Formulation to structure S1 with effect E1
...
E2: structure S1 with effect E2
S2: Combination product with S1 to effect E1
D1: derivative of S1, e.g. new salt
D2: derivative of S1, e.g. hydrate
D2: derivative of S1, e.g. polymorph
S3: pro-drug to S1
By combining: many products + patents possible
Omeprazole from AZ> 80 patent families
patent strategy Pharma
„Life Cycle“

52. 52
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
„Life Cycle“
 Lifecycle-Management can lead to patent thickets (fencing)
lifecycle stage early late
imitation blocking imitation blocking
patent
category
Comple-
mentary
Substi-
tutive
comple-
mentary
Substi-
tutive
Comple-
mentary
substi-
tutive
comple-
mentary
substi-
tutive
substance
•
crystals,
isomers…
• • • • • •
process
• • • •
formulation/
dosing
• • • • • •
fixed dose
combination
• •
indication/ use
• •
Source: Christian Sternitzke Research Policy, 2013, 42(2), 542-551

53. 53
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
Example Degussa / AstaMedica
P1 First mention of the basic structure "AM" as part of a substance class -
Markush structure, disclosure preparation, no effect or impact rather unspecific
as another list of possible applications, especially interesting compounds only in
large list or combination of lists
Registration abroad eg. FR / BE / ZA
Protection: 1967-1987 (1984)
P2 patent of addition, divisional application,
Diversion from P1 with disclosure of
Structure "AM" explicitly, but as one
of many examples, mentioning
possible uses (FR / BE / ZA)
protection as above
patent strategy Pharma
life cycle-ex.

54. 54
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
P3 DE before publication of P1 new application with selected
content from P1 and P3 disclosing selected compounds.
Effect not related to specific structures but LAB codes.
Protection: 1968-1986
P4 1980 In DE Priority filing- new salt form with improved
pharmacological properties as a mixture of different crystal forms,
processes for preparing + application as medicines, publication
withdrawn
P4N 1981 DE subsequent application to P4 (internal priority),  2001
patent strategy Pharma
life cycle-ex

55. 55
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
P5 1985: New method of synthesis of active ingredient
P6 1985: A process for preparing an important precursor
P7 1990: Priority filing: new indication
P8 1992: Priority filing combination product with active X
P9 1993: 1st Sustained-Release formulation
P10 1994: New indication (CNS)
P11 1998: Synthesis of pure polymorph A
P12 2000: New Indication - veterinary pharmaceuticals, transdermal
Formulation
patent strategy Pharma
life cycle-ex

56. 56
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
P13, 2003: Other salt form for new formulation-
new application form: injection
P14 2005: New formulation - once daily
P15, P16, 2008: New salt forms of active ingredient –
improve the solubility /
hedging of the main product /
protection against workarounds
P17 -P19, 2009-2013:
new polymorphs of the drug
better pharmaceutical processing / stability
patent strategy Pharma
life cycle-ex

57. 57
20yrs// ICIC
Heidelberg 2016
Hoock-PATON
patent strategy Pharma
life cycle-ex
P1 Markush
-Formel, FR/BE/ZA
P3 DE-Anmeldung
def.Strukturen + allg.
Wirkung
P2 Ausl. Zusatzanmeldung
definierte Strukturen
BE-Zusatzanmeldung zu P1
P4 DE Prioanm.
neue Salzform Mischung v.
Polymorphen,Arzneimittel
P4NDE-Nachanmeldung
P5 DE-Prio Neues
Verfahren Herstell-
ungreineresProdukt, PbP
P6 Herstellung-2
Zwischenstufe PbP
P5NEP Nachanmeldung
P7 DE-Prio
Med.Indikation II
P7NEP-Nachanmeldung
P8 DE-Prio:
Kombinationsprodukt 1
P9 Formulierung I
P8N
P9N
P10 Indikation II (ZNS)
P11 reinesPolymorph +
Herstellung+ PbP
P11N-EP
P12 Indikation Tierarznei +
transdermal Formulierung
P13 Injektformulierung
P13N
P14 Orale Formulierung 1/d
P14N
P15 neue Salzformen,
Formulierungen
P16 spez. Salz, Formulierung
P17-P19 neue polymorphe
Formen
.09.1965
.08.1967
.07.1969
.06.1971
.05.1973
.04.1975
.03.1977
.02.1979
.01.1981
.12.1982
.11.1984
.10.1986
.09.1988
.08.1990
.07.1992
.06.1994
.05.1996
.04.1998
.03.2000
.02.2002
.01.2004
.12.2005
.11.2007
.10.2009
.09.2011
.08.2013
.07.2015
.06.2017

58. patent strategy Pharma
life cycle-ex
P1 Markush
-Formel, FR/BE/ZA
P3 DE-Anmeldung
def.Strukturen + allg.
Wirkung
P2 Ausl. Zusatzanmeldung
definierte Strukturen
BE-Zusatzanmeldung zu P1
P4 DE Prioanm.
neue Salzform Mischung v.
Polymorphen,Arzneimittel
P4NDE-Nachanmeldung
P5 DE-Prio Neues
Verfahren Herstell-
ungreineresProdukt, PbP
P6 Herstellung-2
Zwischenstufe PbP
P5NEP Nachanmeldung
P7 DE-Prio
Med.Indikation II
P7NEP-Nachanmeldung
P8 DE-Prio:
Kombinationsprodukt 1
P9 Formulierung I
P8N
P9N
P10 Indikation II (ZNS)
P11 reinesPolymorph +
Herstellung+ PbP
P11N-EP
P12 Indikation Tierarznei +
transdermal Formulierung
P13 Injektformulierung
P13N
P14 Orale Formulierung 1/d
P14N
P15 neue Salzformen,
Formulierungen
P16 spez. Salz, Formulierung
P17-P19 neue polymorphe
Formen
.09.1965
.08.1967
.07.1969
.06.1971
.05.1973
.04.1975
.03.1977
.02.1979
.01.1981
.12.1982
.11.1984
.10.1986
.09.1988
.08.1990
.07.1992
.06.1994
.05.1996
.04.1998
.03.2000
.02.2002
.01.2004
.12.2005
.11.2007
.10.2009
.09.2011
.08.2013
.07.2015
.06.2017
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Sales (Mio €) KATADOLON