CY1116775T1 - Παραγωγα πυριμιδονης ως αναστολεις της ιστικης τρανσγλουταμινασης - Google Patents
Παραγωγα πυριμιδονης ως αναστολεις της ιστικης τρανσγλουταμινασηςInfo
- Publication number
- CY1116775T1 CY1116775T1 CY20151100722T CY151100722T CY1116775T1 CY 1116775 T1 CY1116775 T1 CY 1116775T1 CY 20151100722 T CY20151100722 T CY 20151100722T CY 151100722 T CY151100722 T CY 151100722T CY 1116775 T1 CY1116775 T1 CY 1116775T1
- Authority
- CY
- Cyprus
- Prior art keywords
- transglutaminase
- pyrimidone derivatives
- inhibitors
- viral
- pyrimidone
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/10—Tetrapeptides
- C07K5/1021—Tetrapeptides with the first amino acid being acidic
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
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- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
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- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/10—Spiro-condensed systems
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- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
- C07K1/06—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using protecting groups or activating agents
- C07K1/061—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using protecting groups or activating agents using protecting groups
- C07K1/068—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using protecting groups or activating agents using protecting groups for heterocyclic side chains
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- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
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- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
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- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/081—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
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- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0819—Tripeptides with the first amino acid being acidic
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- C—CHEMISTRY; METALLURGY
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- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/10—Tetrapeptides
- C07K5/1002—Tetrapeptides with the first amino acid being neutral
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- C07—ORGANIC CHEMISTRY
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- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/10—Tetrapeptides
- C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
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- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Crystallography & Structural Chemistry (AREA)
- Dermatology (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Psychology (AREA)
- Ophthalmology & Optometry (AREA)
- Analytical Chemistry (AREA)
- Hematology (AREA)
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- Diabetes (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Η εφεύρεση αφορά παράγωγα πυριμιδόνης του γενικού τύπου (Ι) ως αναστολείς για την ιστική τρανσγλουταμινάση, μεθόδους για την παραγωγή των παραγώγων πυριμιδόνης, φαρμακευτικές συνθέσεις που περιέχουν αυτά τα παράγωγα πυριμιδόνης, καθώς και την χρήση τους για προφύλαξη και αντιμετώπιση νόσων που σχετίζονται με την ιστική τρανσγλουταμινάση.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP12176776.8A EP2687511A1 (de) | 2012-07-17 | 2012-07-17 | Pyridinonderivate als Gewebetransglutaminaseinhibitoren |
US201261741871P | 2012-07-30 | 2012-07-30 | |
EP13737220.7A EP2797892B1 (de) | 2012-07-17 | 2013-07-12 | Pyridinonderivate als gewebetransglutaminaseinhibitoren |
Publications (1)
Publication Number | Publication Date |
---|---|
CY1116775T1 true CY1116775T1 (el) | 2017-03-15 |
Family
ID=46516598
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CY20151100722T CY1116775T1 (el) | 2012-07-17 | 2015-08-18 | Παραγωγα πυριμιδονης ως αναστολεις της ιστικης τρανσγλουταμινασης |
Country Status (20)
Country | Link |
---|---|
US (1) | US9434763B2 (el) |
EP (2) | EP2687511A1 (el) |
JP (1) | JP6236445B2 (el) |
CN (1) | CN104603109B (el) |
AU (1) | AU2013292149B2 (el) |
CA (1) | CA2878796C (el) |
CY (1) | CY1116775T1 (el) |
DK (1) | DK2797892T3 (el) |
ES (1) | ES2543956T3 (el) |
HR (1) | HRP20150829T1 (el) |
HU (1) | HUE027051T2 (el) |
IL (1) | IL236707B (el) |
IN (1) | IN2015DN01151A (el) |
PL (1) | PL2797892T3 (el) |
PT (1) | PT2797892E (el) |
RS (1) | RS54153B1 (el) |
RU (1) | RU2652987C2 (el) |
SI (1) | SI2797892T1 (el) |
SM (1) | SMT201500208B (el) |
WO (1) | WO2014012858A1 (el) |
Families Citing this family (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP3543235A1 (en) | 2015-08-05 | 2019-09-25 | ratiopharm GmbH | Crystalline form and acetic acid adduct of palbociclib |
WO2019201432A1 (en) | 2018-04-17 | 2019-10-24 | Zedira Gmbh | Inhibitors of blood coagulation factor xiii |
TWI825144B (zh) | 2018-08-10 | 2023-12-11 | 美商思達利醫藥公司 | 第二型轉麩醯胺酸酶(tg2)抑制劑 |
CN113544130B (zh) * | 2019-05-31 | 2024-01-09 | 西藏海思科制药有限公司 | 一种btk抑制剂环衍生物及其制备方法和药学上的应用 |
SI3965741T1 (sl) * | 2020-04-24 | 2023-10-30 | Dr. Falk Pharma Gmbh | Sistemska formulacija piridinonskega derivata za celiakijo |
MX2022013344A (es) * | 2020-04-24 | 2022-11-30 | Dr Falk Pharma Gmbh | Formulacion sistemica de un derivado de la piridinona para las enfermedades relacionadas con la tg2. |
EP3900706A1 (en) * | 2020-04-24 | 2021-10-27 | Dr. Falk Pharma Gmbh | Systemic formulation of a pyridinone derivate for coeliac disease |
EP3900707A1 (en) * | 2020-04-24 | 2021-10-27 | Dr. Falk Pharma Gmbh | Systemic formulation of a pyridinone derivate for tg2-related diseases |
WO2023110138A1 (en) * | 2021-12-17 | 2023-06-22 | Zedira Gmbh | Inhibitors of transglutaminases |
HRP20241524T1 (hr) | 2021-06-30 | 2025-01-03 | Zedira Gmbh | Inhibitori transglutaminaza |
CN117616011A (zh) * | 2021-06-30 | 2024-02-27 | 策迪拉有限公司 | 转谷氨酰胺酶的抑制剂 |
AU2022301517A1 (en) | 2021-06-30 | 2023-12-14 | Zedira Gmbh | Inhibitors of transglutaminases |
US20240383856A1 (en) | 2021-06-30 | 2024-11-21 | Zedira Gmbh | Inhibitors of transglutaminases |
WO2023072368A1 (en) * | 2021-10-25 | 2023-05-04 | Dr. Falk Pharma Gmbh | Oral formulation of a pyridinone derivate and use thereof in prophylaxis and/or treatment of intestinal fibrosis |
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US5021440A (en) * | 1989-07-31 | 1991-06-04 | Merck & Co., Inc. | Imidazole compounds and their use as transglutaminase inhibitors |
CA2268381A1 (en) * | 1996-10-11 | 1998-04-23 | Cor Therapeutics, Inc. | Selective factor xa inhibitors |
AR032318A1 (es) * | 2000-04-13 | 2003-11-05 | Pharmacia Corp | Compuesto derivado halogenado del acido 2-amino-5,6 heptenoico; composicion farmaceutica que lo comprende y su uso en la fabricacion de un medicamento util como inhibidor de la oxido nitrico sintetasa |
US7265093B2 (en) * | 2002-05-14 | 2007-09-04 | The Board Of Trustees Of The Leland Stanford Junior University | Drug therapy for Celiac Sprue |
US7605150B2 (en) * | 2002-05-14 | 2009-10-20 | The Board Of Trustees Of The Leland Stanford Junior University | Drug therapy for Celiac Sprue |
PE20050159A1 (es) * | 2003-05-27 | 2005-04-19 | Vertex Pharma | Derivados de acido 3-[2-(3-amino-2-oxo-2h-piridin-1-il)-acetilamino]-4-oxo-pentanoico como inhibidores de caspasa |
DE502005006161D1 (de) | 2004-08-11 | 2009-01-15 | N Zyme Biotec Gmbh | Fluoreszenzbasierende kinetische bestimmung der aktivität von transglutaminasen |
DE102006052755A1 (de) * | 2006-11-08 | 2008-05-15 | N-Zyme Biotec Gmbh | Michaelsysteme als Transglutaminaseinhibitoren |
JP2013180955A (ja) * | 2012-02-29 | 2013-09-12 | Toray Ind Inc | 組織トランスグルタミナーゼ阻害剤並びにカルコン誘導体及びその医薬用途 |
-
2012
- 2012-07-17 EP EP12176776.8A patent/EP2687511A1/de not_active Withdrawn
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2013
- 2013-07-12 WO PCT/EP2013/064789 patent/WO2014012858A1/de active Application Filing
- 2013-07-12 PT PT137372207T patent/PT2797892E/pt unknown
- 2013-07-12 HU HUE13737220A patent/HUE027051T2/en unknown
- 2013-07-12 CN CN201380045325.5A patent/CN104603109B/zh active Active
- 2013-07-12 US US14/415,374 patent/US9434763B2/en active Active
- 2013-07-12 RS RS20150508A patent/RS54153B1/en unknown
- 2013-07-12 AU AU2013292149A patent/AU2013292149B2/en active Active
- 2013-07-12 RU RU2015104969A patent/RU2652987C2/ru active
- 2013-07-12 JP JP2015522048A patent/JP6236445B2/ja active Active
- 2013-07-12 ES ES13737220.7T patent/ES2543956T3/es active Active
- 2013-07-12 SI SI201330058T patent/SI2797892T1/sl unknown
- 2013-07-12 CA CA2878796A patent/CA2878796C/en active Active
- 2013-07-12 EP EP13737220.7A patent/EP2797892B1/de active Active
- 2013-07-12 DK DK13737220.7T patent/DK2797892T3/en active
- 2013-07-12 PL PL13737220T patent/PL2797892T3/pl unknown
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- 2015-02-12 IN IN1151DEN2015 patent/IN2015DN01151A/en unknown
- 2015-08-03 HR HRP20150829TT patent/HRP20150829T1/hr unknown
- 2015-08-18 CY CY20151100722T patent/CY1116775T1/el unknown
- 2015-09-02 SM SM201500208T patent/SMT201500208B/xx unknown
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RU2015104969A (ru) | 2016-09-10 |
EP2797892B1 (de) | 2015-05-27 |
AU2013292149B2 (en) | 2016-11-24 |
JP6236445B2 (ja) | 2017-11-22 |
RU2652987C2 (ru) | 2018-05-04 |
WO2014012858A1 (de) | 2014-01-23 |
PL2797892T3 (pl) | 2015-10-30 |
SI2797892T1 (sl) | 2015-09-30 |
US20150203535A1 (en) | 2015-07-23 |
JP2015529645A (ja) | 2015-10-08 |
CN104603109B (zh) | 2017-07-28 |
US9434763B2 (en) | 2016-09-06 |
EP2687511A1 (de) | 2014-01-22 |
AU2013292149A1 (en) | 2015-02-05 |
CN104603109A (zh) | 2015-05-06 |
IL236707B (en) | 2018-12-31 |
RS54153B1 (en) | 2015-12-31 |
EP2797892A1 (de) | 2014-11-05 |
HRP20150829T1 (hr) | 2015-09-11 |
IN2015DN01151A (el) | 2015-06-26 |
PT2797892E (pt) | 2015-09-18 |
IL236707A0 (en) | 2015-02-26 |
CA2878796C (en) | 2018-10-23 |
DK2797892T3 (en) | 2015-07-20 |
SMT201500208B (it) | 2015-10-30 |
CA2878796A1 (en) | 2014-01-23 |
HUE027051T2 (en) | 2016-08-29 |
ES2543956T3 (es) | 2015-08-26 |
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