JP6318156B2 - キナーゼをモジュレートするための化合物および方法、ならびにその指標 - Google Patents
キナーゼをモジュレートするための化合物および方法、ならびにその指標 Download PDFInfo
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- JP6318156B2 JP6318156B2 JP2015531206A JP2015531206A JP6318156B2 JP 6318156 B2 JP6318156 B2 JP 6318156B2 JP 2015531206 A JP2015531206 A JP 2015531206A JP 2015531206 A JP2015531206 A JP 2015531206A JP 6318156 B2 JP6318156 B2 JP 6318156B2
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- 0 C*1(C)C(C=C**2)=C2C=C1 Chemical compound C*1(C)C(C=C**2)=C2C=C1 0.000 description 12
- DDZGQYREBDXECY-UHFFFAOYSA-N c1n[nH]c2nccnc12 Chemical compound c1n[nH]c2nccnc12 DDZGQYREBDXECY-UHFFFAOYSA-N 0.000 description 2
- INFXCZTYGOHFJO-UHFFFAOYSA-N C=CNc1c(cc[nH]2)c2ncn1 Chemical compound C=CNc1c(cc[nH]2)c2ncn1 INFXCZTYGOHFJO-UHFFFAOYSA-N 0.000 description 1
- DYTCGOMSQHOVMS-UHFFFAOYSA-N CC1=[I]C=Nc2c1ccc(NCCOC)c2 Chemical compound CC1=[I]C=Nc2c1ccc(NCCOC)c2 DYTCGOMSQHOVMS-UHFFFAOYSA-N 0.000 description 1
- DNFBJBRWITZICO-WKBXPBOGSA-N CCC1OC=C/C1=N/C=C\N Chemical compound CCC1OC=C/C1=N/C=C\N DNFBJBRWITZICO-WKBXPBOGSA-N 0.000 description 1
- XKNMFSNLEDMBHK-UHFFFAOYSA-N C[N+](C(CC1)=CC=C1N)(O)[OH2+] Chemical compound C[N+](C(CC1)=CC=C1N)(O)[OH2+] XKNMFSNLEDMBHK-UHFFFAOYSA-N 0.000 description 1
- KBSRYRNFSYDEHY-UHFFFAOYSA-N Ic1c(cccc2)c2ncn1 Chemical compound Ic1c(cccc2)c2ncn1 KBSRYRNFSYDEHY-UHFFFAOYSA-N 0.000 description 1
- CSJOLXDFFYCGDZ-UHFFFAOYSA-N Ic1c(cn[nH]2)c2ncn1 Chemical compound Ic1c(cn[nH]2)c2ncn1 CSJOLXDFFYCGDZ-UHFFFAOYSA-N 0.000 description 1
- UREDQPSRDVZQFV-UHFFFAOYSA-N Ic1c2[s]ccc2ncn1 Chemical compound Ic1c2[s]ccc2ncn1 UREDQPSRDVZQFV-UHFFFAOYSA-N 0.000 description 1
- MDANCFSZYMOGEV-GUSUVPGTSA-N N/C=C\N=C1\OC=NC1=[IH] Chemical compound N/C=C\N=C1\OC=NC1=[IH] MDANCFSZYMOGEV-GUSUVPGTSA-N 0.000 description 1
- COJABJBCLBJEBG-UHFFFAOYSA-N Nc1nccnc1N=N Chemical compound Nc1nccnc1N=N COJABJBCLBJEBG-UHFFFAOYSA-N 0.000 description 1
- HFTVJMFWJUFBNO-UHFFFAOYSA-N c1c[nH]c2nccnc12 Chemical compound c1c[nH]c2nccnc12 HFTVJMFWJUFBNO-UHFFFAOYSA-N 0.000 description 1
- JJTNLWSCFYERCK-UHFFFAOYSA-N c1c[nH]c2ncncc12 Chemical compound c1c[nH]c2ncncc12 JJTNLWSCFYERCK-UHFFFAOYSA-N 0.000 description 1
- YJSKZIATOGOJEB-UHFFFAOYSA-N c1c[s]c2nccnc12 Chemical compound c1c[s]c2nccnc12 YJSKZIATOGOJEB-UHFFFAOYSA-N 0.000 description 1
- DLHRAOSKUZJSEB-UHFFFAOYSA-N c1cnc2[o]nnc2n1 Chemical compound c1cnc2[o]nnc2n1 DLHRAOSKUZJSEB-UHFFFAOYSA-N 0.000 description 1
- HXTBYLZGLRCHTM-UHFFFAOYSA-N c1n[o]c2nccnc12 Chemical compound c1n[o]c2nccnc12 HXTBYLZGLRCHTM-UHFFFAOYSA-N 0.000 description 1
- ZKAMEFMDQNTDFK-UHFFFAOYSA-N c1nc2nccnc2[nH]1 Chemical compound c1nc2nccnc2[nH]1 ZKAMEFMDQNTDFK-UHFFFAOYSA-N 0.000 description 1
- PUZFXDRHCPIYCB-UHFFFAOYSA-N c1nc2nccnc2[o]1 Chemical compound c1nc2nccnc2[o]1 PUZFXDRHCPIYCB-UHFFFAOYSA-N 0.000 description 1
- HEIZPACCIHXHKV-UHFFFAOYSA-N c1nc2nccnc2[s]1 Chemical compound c1nc2nccnc2[s]1 HEIZPACCIHXHKV-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/74—Quinazolines; Hydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D401/02—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 containing two hetero rings
- C07D401/12—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 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Enzymes And Modification Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261697761P | 2012-09-06 | 2012-09-06 | |
| US61/697,761 | 2012-09-06 | ||
| US201361775347P | 2013-03-08 | 2013-03-08 | |
| US61/775,347 | 2013-03-08 | ||
| PCT/US2013/058320 WO2014039714A2 (en) | 2012-09-06 | 2013-09-05 | Compounds and methods for kinase modulation, and indications therefor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015529224A JP2015529224A (ja) | 2015-10-05 |
| JP2015529224A5 JP2015529224A5 (https=) | 2017-04-27 |
| JP6318156B2 true JP6318156B2 (ja) | 2018-04-25 |
Family
ID=50237764
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015531206A Active JP6318156B2 (ja) | 2012-09-06 | 2013-09-05 | キナーゼをモジュレートするための化合物および方法、ならびにその指標 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US10227357B2 (https=) |
| EP (1) | EP2892534B8 (https=) |
| JP (1) | JP6318156B2 (https=) |
| CN (1) | CN104981247A (https=) |
| AU (1) | AU2013312477B2 (https=) |
| CA (1) | CA2883894C (https=) |
| ES (1) | ES2889757T3 (https=) |
| MX (1) | MX2015002887A (https=) |
| WO (1) | WO2014039714A2 (https=) |
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| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| WO2009012283A1 (en) | 2007-07-17 | 2009-01-22 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| WO2009143018A2 (en) | 2008-05-19 | 2009-11-26 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
| ES2627911T3 (es) | 2009-11-18 | 2017-08-01 | Plexxikon, Inc. | Derivados de N-[2-fluoro-3-(4-amino-7H-pirrolo[2,3-d]pirimidin-5-carbonil)-fenil]-4-bencenosulfonamida como moduladores de la proteína quinasa Raf para el tratamiento del cáncer |
| BR112012015745A2 (pt) | 2009-12-23 | 2016-05-17 | Plexxikon Inc | compostos e métodos para a modulação de quinase, e indicações dos mesmos |
| TWI510487B (zh) | 2010-04-21 | 2015-12-01 | Plexxikon Inc | 用於激酶調節的化合物和方法及其適應症 |
| ES2617339T3 (es) | 2010-12-16 | 2017-06-16 | Calchan Limited | Derivados de pirrolopirimidina inhibidores de ASK1 |
| US9624213B2 (en) | 2011-02-07 | 2017-04-18 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| JP6113151B2 (ja) | 2011-05-17 | 2017-04-12 | プレキシコン インコーポレーテッドPlexxikon Inc. | キナーゼ調節およびその適応症 |
| US9358235B2 (en) | 2012-03-19 | 2016-06-07 | Plexxikon Inc. | Kinase modulation, and indications therefor |
| MX365640B (es) | 2012-12-21 | 2019-06-10 | Plexxikon Inc | Compuestos y metodos para la modulacion de quinasas y sus indicaciones. |
| AR095202A1 (es) * | 2013-03-11 | 2015-09-30 | Merck Patent Gmbh | Heterociclos como moduladores de la actividad quinasa |
| US20140303121A1 (en) | 2013-03-15 | 2014-10-09 | Plexxikon Inc. | Heterocyclic compounds and uses thereof |
| DK2970265T3 (en) | 2013-03-15 | 2018-10-01 | Plexxikon Inc | HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF |
| WO2014160521A1 (en) | 2013-03-15 | 2014-10-02 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
| DE102013008118A1 (de) | 2013-05-11 | 2014-11-13 | Merck Patent Gmbh | Arylchinazoline |
| CN105228983A (zh) | 2013-05-30 | 2016-01-06 | 普莱希科公司 | 用于激酶调节的化合物及其适应症 |
| SI3057969T1 (sl) | 2013-10-17 | 2018-10-30 | Blueprint Medicines Corporation | Sestavki, uporabni za zdravljenje motenj, povezanih s KIT |
| WO2015058129A1 (en) | 2013-10-17 | 2015-04-23 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| SI3077395T1 (en) * | 2013-12-05 | 2018-03-30 | Pfizer Inc. | Pyrrolo(2,3-d)pyrimidinyl, pyrrolo(2,3-b)pyrazinyl and pyrrolo(2,3-d)pyridinyl acrylamides |
| US9771369B2 (en) | 2014-03-04 | 2017-09-26 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| GB201410816D0 (en) * | 2014-06-17 | 2014-07-30 | Ucb Biopharma Sprl And Katholieke Universiteit Leuven | Therapeutic agents |
| ES2774177T3 (es) | 2014-09-15 | 2020-07-17 | Plexxikon Inc | Compuestos heterocíclicos y usos de estos |
| TWI735416B (zh) | 2014-10-06 | 2021-08-11 | 美商維泰克斯製藥公司 | 囊腫纖維化症跨膜傳導調節蛋白之調節劑 |
| WO2016164641A1 (en) | 2015-04-08 | 2016-10-13 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| JP6530826B2 (ja) | 2015-05-06 | 2019-06-12 | プレキシコン インコーポレーテッドPlexxikon Inc. | キナーゼを修飾する1h−ピロロ[2,3−b]ピリジン誘導体の合成 |
| LT3292123T (lt) | 2015-05-06 | 2020-12-28 | Plexxikon Inc. | Junginio, moduliuojančio kinazes, kietos formos |
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| US10829484B2 (en) | 2015-07-28 | 2020-11-10 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| US9708333B2 (en) | 2015-08-12 | 2017-07-18 | Incyte Corporation | Fused bicyclic 1,2,4-triazine compounds as TAM inhibitors |
| WO2017035366A1 (en) | 2015-08-26 | 2017-03-02 | Incyte Corporation | Pyrrolopyrimidine derivatives as tam inhibitors |
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| CN105311585A (zh) * | 2015-12-08 | 2016-02-10 | 李朝彬 | 一种治疗肝硬化的中药组合物 |
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| KR102483020B1 (ko) | 2016-03-28 | 2023-01-04 | 인사이트 코포레이션 | Tam 저해제로서의 피롤로트리아진 화합물 |
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| EP3558991A2 (en) | 2016-12-23 | 2019-10-30 | Plexxikon Inc. | Compounds and methods for cdk8 modulation and indications therefor |
| JP2020511467A (ja) | 2017-03-20 | 2020-04-16 | プレキシコン インコーポレーテッドPlexxikon Inc. | ブロモドメインを阻害する4−(1−(1,1−ジ(ピリジン−2−イル)エチル)−6−(3,5−ジメチルイソオキサゾール−4−イル)−1H−ピロロ[3,2−b]ピリジン−3−イル)安息香酸の結晶形 |
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| AU2018279646B2 (en) | 2017-06-08 | 2023-04-06 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
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| MX2015002887A (es) | 2015-07-06 |
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| US10227357B2 (en) | 2019-03-12 |
| AU2013312477A1 (en) | 2015-04-02 |
| EP2892534B1 (en) | 2021-08-04 |
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