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Eluteaduste valdkonna intellektuaalse omandi kaitse. Patendiotsing, patendinõudlus.
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Eluteaduste valdkonna intellektuaalse omandi kaitsePatendiotsing, patendinõudlus
Margus Sarap, Euroopa patendivolinik17.aprill 2013, Tartu Biotehnoloogia Park
Biotehnoloogia erisused?
4/2/2013 2Margus Sarap, 2013
Mittepatenditavad:
bioloogilisi meetodeid
bioloogilise aine, taime või looma saamiseks
välja arvatud mikrobioloogilised meetodid mikroorganismide saamiseks
leiutised, mida saab kasutada ainult ühe kindla taimesordi või loomatõu puhul
NB! Bioloogilise aine, taime või looma saamise olemuselt bioloogiline meetod on meetod, mis täielikult põhineb looduslikul nähtusel, nagu ristamine ja selektsioon.
Biotehnoloogia erisused?
4/2/2013 3Margus Sarap, 2013
NB!
Ühe ja sama patenditaotlusega saab taotleda patendikaitset ainult ühele leiutisele või ühtse leiundusliku mõttega seotud leiutiste kombinatsioonile
Biotehnoloogia erisused?
4/2/2013 4Margus Sarap, 2013
Biotehnoloogia erisused?
1. A fluorescent probe for determining protein kinase activity with the general formula (I):
(X-Y-Z)-L-F (I),wherein
X-Y-Z is a bisubstrate-analog inhibitor of a protein kinase, in which X is a compound that binds to the ATP-binding pocket of the kinase and;
Z is a compound that binds to the protein/peptide-binding domain of the kinase;
Y is a an organic tether that connects X and Z and permits simultaneous binding of X and Z to the active site of the kinase;
F is a fluorescent dye which optical characteristics are changed in the course of the binding of (X-Y-Z)-L-F to the kinase;
L is a linker (between the bisubstrate-analog inhibitor XYZ and fluorescent label F) formed of a hydrocarbon chain, of other type of organic molecule or of part of organic molecule; may be omitted in the probe and F directly bound to inhibitor XYZ.
4/2/2013 5Margus Sarap, 2013
Biotehnoloogia erisused?
1. A fluorescent probe for a protein kinase selected from the group consisting of:
2. A kit comprising a fluorescent probe of claim 1. 3. A bisubstrate-analog inhibitor of a basophilic protein kinase selected from the group
consisting of:
4. A method for determining the fraction of an active binding form of a protein kinase in a sample containing a fluorescent probe of claim 1 ...
NO
N
N
OHOHN
NH2O
N
O
N+
-OOC
O
NH
O
NH-(D-Arg)6-(D-Lys)-C(=O)-NH2NH
N
S OO
HNNH
O
NH-(D-Arg)6-D-Lys(5-TAMRA)-C(O)NH2 NO
N
N
OHOH
N
NH2
O
O
NH-(D-Arg)6-(D-Lys)-C(=O)-NH2
NNO
O2N
NH
NH
NO
N
N
OHOHN
NH2O
N
O
N+
-OOC
O
NH
O
NH-(D-Arg)6-(D-Lys)-C(=O)-NH2NH
N
S OO
HNNH
O
NH-(D-Arg)6-D-Lys(5-TAMRA)-C(O)NH2 NO
N
N
OHOH
N
NH2
O
O
NH-(D-Arg)6-(D-Lys)-C(=O)-NH2
NNO
O2N
NH
NH
4/2/2013 6Margus Sarap, 2013
patent US8,158,376
Patendidokumendi ülesehitus?
•Leiutiskirjeldus – specification–Pealkiri - Title–Tehnika valdkond – Technical Field–Tehnika tase – Background Art–Leiutise olemus – Summary of invention–Jooniste loetelu – Brief description od drawings–Teostusnäi(de)ted – Description of embodiments–Viited – Recitation list–Patendinõudlus - Claims–Lühikokkuvõte - Abstract–Joonised - Drawings
9.12.2011 7Sarap ja Partnerid, ©2011
Patendidokumendi erinevate osade tähendus?
Kõige tähtsam – patendinõudlus
tehnilise lahenduse (leiutise) kaitseulatus
sõltumatu punkt
sõltuvad punktid
9.12.2011 8Sarap ja Partnerid, ©2011
Patendidokumendi erinevate osade tähendus?
Leiutiskirjeldus
leiutise olemuse avamine
tehnilise lahenduse täpne kirjeldus
9.12.2011 9Sarap ja Partnerid, ©2011
Vähiravi
Explanation of terms• Heat shock protein 90 (HSP 90)
Belongs to a class of proteins that protect cells when stressed by elevated temperatures; assists in tumour repression.
• Heat shock protein 90 inhibitor (HSP 90 inhibitor)Compounds which block the functioning of HSP 90. Examples: geldanamycin or 17-alkylamino-17-desmethoxygeldanamycin (17-AAG).
• Platinum coordination complexesPlatinum complexed with ligands. These compounds are used as chemotherapeutics. Examples: cisplatin, carboplatin, oxaliplatin.
17-AAG, R17 = alkylamino
Oxaliplatin
Allikas EPO materjalid , nõudluse tõlgendamine
LeiutisAn improved way of treating people suffering from breast cancer by injecting a platinum coordination complex and optionallyalso an HSP 90 inhibitor.The invention shows improved results by combining the two compounds. The specific combination of oxaliplatin and 17-AAG has a synergistic effect.
How can you protect it from imitation?
• "An improved way" → Compared with what? (term not clear)
• "Way of treating people" → Method of treatment of the human or animal body by therapy = excluded from patentability
• "A platinum coordination → Not a "method of treatment"; has a
complex " technical function → possible patent
Allikas EPO materjalid , nõudluse tõlgendamine
Patent Claim: "A platinum coordination complex"
How to patent this invention: claim it!
Claiming a platinum coordination complex in general means trying to get very broad protection. You already know that such complexes have been described before.
Patent Claim: "A platinum coordination complex for use in the treatment of suffering people."
This wording also does not describe what you invented.
Patent Claim: "A platinum coordination complex for use in the treatment of breast cancer."
A prior art search will show whether the invention – as claimed – is actually new.
Allikas EPO materjalid , nõudluse tõlgendamine
Tehnika taseme otsingu tulemused
The prior art search found a journal article that discloses the invention.
Cancer Treatment Reports 67(3) 235-238, 1983
"... 2 [patients] with adrenocarcinomas in the breast ... were treated
with cisplatin at a dose of 60 mg/m2 ..."
A platinum coordination complex (i.e. cisplatin) for use in the treatment
of cancer is already known from this journal article!
Allikas EPO materjalid , nõudluse tõlgendamine
Comparison of the two inventions
The invention
as claimedCancer Treatment Reports
"A platinum coordination
complex for use in the
treatment of breast cancer."
"... 2 [patients] with
adrenocarcinomas in the
breast ... were treated
with cisplatin at a dose of 60
mg/m2 ..."
"A combination of a platinum
coordination complex and an
HSP 90 inhibitor for use ..."
• New• Inventive step
(the combined use shows
improved effects)
Allikas EPO materjalid , nõudluse tõlgendamine
Not new
Leiutist kaitsev nõudlus
Claim to be filed:
"A combination of a platinum coordination complex and an HSP 90 inhibitor for use in the treatment of breast cancer."
Allikas EPO materjalid , nõudluse tõlgendamine
Sõltumatute nõudluste kasutamine kaitse täiendamiseks
The patent should include both broad and specific claims.
Broad: An independent claim (i.e. a claim stating the essential features of the invention) helps prevent the patent from being circumvented.
Specific: Dependent claims refer to an independent claim and additionally define preferred embodiments of the invention.
Independent claim
Dependent claim 1
Dependent claim 2
Allikas EPO materjalid , nõudluse tõlgendamine
Patendiametile (EPO) esitatud taotlus
CLAIM 1:"A combination of a platinum coordination complex and an HSP 90 inhibitor for use in the treatment of breast cancer."
Claim 2: "A combination according to claim 1, characterised in that the HSP 90 inhibitor is 17-AAG."
Claim 3: "A combination according to claim 1, characterised in that the platinum coordination complex is oxaliplatin."
The patent office will perform its own prior art search and thenconsider whether the invention AS CLAIMED is new and non-obvious.
Claim 4: "A combination according to claim 2, characterised in that the platinum coordination complex is oxaliplatin."
Allikas EPO materjalid , nõudluse tõlgendamine
Tehnika tase EPO otsingust
"Combination of HSP 90 inhibitor ... with anticancer agents like carboplatin or cisplatin ... to inhibit ... growth of breast cancer cells."
"Methods for enhancing the efficacy of cytotoxic agents through the use of HSP90 inhibitors"
EPO arvamus
Applicant's claim:
"A combination of a platinum
coordination complex and an HSP 90
inhibitor for use in the treatment of
breast cancer."
The invention according to claim 1
is already shown and claimed in
WO 02/15925.
EPO response:
Please amend your claims if you want your invention patented!
A platinum coordination complex
(e.g. cisplatin) and an HSP 90
inhibitor were used in
WO 02/15925 to treat breast
cancer.
Edasine analüüs
• Check the material revealed in the prior art searches:• Does the invention have any features NOT disclosed in the
prior art?• What are the advantages of the invention compared with
the prior art?
How can the claims be amended to reflect the invention in a way that it is new (considering all the prior art)?
• Did the EPO interpret any important features of the invention differently to the inventor?
Applicant's reply: amendments to the application, explanation of the relationship between the invention and the prior art
Synergism (more than additive)
Claim 2: Features of Claim 1 + HSP90 inhibitor = 17-AAG
Claim 4: Features of Claims 1 + 2 + Pt coordination complex = oxaliplatin
Cancer TreatmentReports
Improved effect (additive)
Claim 3: Features of Claim 1 +Pt coordination complex = oxaliplatin
Claim 1: Combination of HSP 90 inhibitor and Pt coordination complex
Leiutise võrdlus tehnika tasemega
Technical features of the invention
WO 02/15925
Advantages/technical result
No
No
No No
No
No
No
No
No
No
Analüüsi tulemusAlthough the individual elements of the invention are known, the combination of specific compounds is not and it produces a new, unique benefit. But you have to take into account that:
Claim 2 refers to the use of 17-AAG. To use this specific HSP 90 inhibitor is considered to be trivial, because WO 02/15925 recommends using any HSP 90 inhibitor in combination with an anticancer agent.
Claim 3 teaches the use of oxaliplatin. Again, since WO 02/15925 hints at the use of any anticancer drug, the use of oxaliplatin is also considered to be obvious.
Claim 4 describes the use of the combination of oxaliplatin and 17-AAG. It is shown in the patent application that the combination produces a synergistic (= more than additive) effect. This is not disclosed in
WO 02/15925.
Analüüsi tulemusedIf one compound is simply replaced by another without showing any unexpected or surprising effect, such a replacement is frequently considered to represent routine for an expert.
If an unexpected or surprising effect can be shown, then the invention is often considered to be inventive (i.e. the invention is not obvious for an expert working in the technical field).
The use of 17-AAG and oxaliplatin, which leads to an unexpected synergistic combination, is therefore inventive.
Invention(new + inventive)
R17 = alkylamino
The present invention provides a method for treating cancer. The
method involves the administration of an HSP90 inhibitor and a
platinum coordination complex, where the combined administration
provides a synergistic effect.
The HSP90 inhibitor for this aspect is typically 17-AAG, while the
platinum coordination complex is oxaliplatin.
17-AAG combination in SKSBr-3 cells [0093] The following table
provides CI values for combinations of 17-AAG and the platinum
complexes oxaliplatin and cisplatin in an SKBr-3 cell assay ...
EPOsse esitatud kirjeldus toetab parandusi
Differentto "Cancer Treatment…"
Differentto patentWO02/…
Supports inventive step:differenttechnical result
Väljaantud patendi nõudlus
Claim 1 as granted reads:
"Medicament comprising 17-Alkylamino-17-desmethoxygeldanamycin
(17-AAG) and oxaliplatin for use in the treatment of breast cancer
in a patient."
Response from EPO: granted!
EP1179050• 1. A method for removal of protein kinase from a liquid
containing the protein kinase by contacting the liquid with a carrier bound affinity ligand for the kinase, characterized in that the ligand is a bisubstrate inhibitor for the kinase whereas the ligand is attached to the carrier.
• 2. The method of claim 1, characterized in that the bisubstrate inhibitor comprises the structure
• C-(L) n-N• where• (a) C contains a structure inhibiting binding of the
peptide/protein substrate to the protein kinase,• (b) L is an organic linker,• (c) n is an integer 0 or 1, and• (d) N is an inhibitor competitively inhibiting binding of the
nucleoside triphosphate (NTP) to the protein kinase;• and the structure is attached to the carrier via C.• 3. The method of any one of claims 1-2, characterized in that C is
a peptide substrate consensus sequence or a pseudosubstrate consensus sequence. 4/2/2013 Margus Sarap, 2013 26
Näide
4/2/2013 Margus Sarap, 2013 27
• 1. A method for removal of protein kinase from a liquid containing the protein kinase by contacting the liquid with a carrier bound affinity ligand for the kinase, characterized in that the affinity ligand is a bisubstrate inhibitor having a structure containing
• - a moiety having the structure that is able to competitively inhibit binding of the relevant nucleotide triphosphate (NTP) and
• - a moiety having the structure that is able to competitively inhibit binding of peptide or protein substrate
• to the particular protein kinase molecule whereas the ligand is attached to the carrier.
• 2. The method of claim 1, characterized in that the bisubstrate inhibitor for the particular protein kinase molecule comprises the structure
• C-(L) n-N• where• (a) C contains a structure inhibiting binding of the peptide or protein
substrate to the protein kinase,• (b) L is an organic linker,• (c) n is an integer 0 or 1, and• (d) N is an inhibitor competitively inhibiting binding of the nucleoside
triphosphate (NTP) to the protein kinase.• 3. The method of any one of claims 1-2, characterized in that C is a peptide
substrate consensus sequence or a pseudosubstrate consensus sequence.
• 1. A method for removal of protein kinase from a liquid containing the protein kinase by contacting the liquid with an affinity ligand for the kinase bound to a carrier insoluble in aqueous media, characterized in that the affinity ligand is a bisubstrate inhibitor having a structure containing simultaneously
• - a moiety having the structure that is able to competitively inhibit binding of the relevant nucleotide triphosphate (NTP) and
• - a non-phosphorylatable moiety having the structure that is able to competitively inhibit binding of peptide or protein substrate
• whereas both moieties target the particular protein kinase molecule whereas the ligand is attached to the carrier.
• 2. The method of claim 1, characterized in that the bisubstrate inhibitor for the particular protein kinase molecule comprises the structure
• C-(L)n-N• where• (a) C contains a structure inhibiting binding of the peptide or protein substrate to
the protein kinase,• (b) L is an organic linker,• (c) n is an integer 0 or 1, and• (d) N is an inhibitor competitively inhibiting binding of the nucleoside triphosphate
(NTP) to the protein kinase.• 3. The method of any one of claims 1-2, characterized in that C is a peptide substrate
consensus sequence or a pseudosubstrate consensus sequence.
4/2/2013 Margus Sarap, 2013 28
4/2/2013 Margus Sarap, 2013 29
Claims1. A method for removal of protein kinase from a liquid containing the protein kinase by contacting the liquid with an affinity ligand for the kinase bound to a carrier insoluble in aqueous media characterized in that the affinity ligand is a bisubstrate inhibitor having a structure containing simultaneously- a moiety having the structure that is able to competitively inhibit binding of the relevant nucleotide triphosphate (NTP) and- a non-phosphorylatable moiety having the structure that is able to competitively inhibit binding of peptide orprotein substrate whereas both moieties target the particular protein kinase molecule whereas the ligand is attached to the carrier.2. The method of claim 1, characterized in that the bisubstrate inhibitor for the particular protein kinase molecule comprises the structureC-(L)n-Nwhere(a) C contains a structure inhibiting binding of the peptide or protein substrate to the protein kinase,(b) L is an organic linker,(c) n is an integer 0 or 1, and(d) N is an inhibitor competitively inhibiting binding of the nucleoside triphosphate (NTP) to the protein kinase.3. The method of any one of claim 2, characterized in that C is a peptide substrate consensus sequence or a pseudosubstrate consensus sequence.
Nõudlused kellele
•taotleja -> võimalikult lai kaitse•Patendiameti ekspert -> tehnika tase -> kitsendamine•konkurent
• patendi vaidlustamine’• rikkumine
•rikkuja
4/2/2013 Margus Sarap, 2013 30
EE03157•1. Optiliselt puhas ühend, mida iseloomustab see,
et ühend on (-)-5-metoksü-2-{[(4-metoksü-3,5-dimetüül-2-püridinüül)metüül]sulfinüül]-H-bensimidasooli Na+-, Mg2+-, Li+-, K+- Ca2+- või N+(R)4-sool, milles R on alküülrühm 1-4 süsinikuaatomiga.
4/2/2013 Margus Sarap, 2013 31
Küsimused?-Mis on optilise puhtuse määr-tehnika tasemest tuntud Na, Mg soolad
Küsimused?
Sarap ja Partnerid PatendibürooMargus Sarappatent@patent.ee tel 747 7058Kompanii 1c, Tartu
Mikk Putkmikk.putk@patent.ee tel 53 039 088 Soo 46, Tallinn
4/2/2013 32Margus Sarap, 2013
www.patent.ee
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