ES2867048T3 - Derivados deuterados de ruxolitinib - Google Patents
Derivados deuterados de ruxolitinib Download PDFInfo
- Publication number
- ES2867048T3 ES2867048T3 ES18188152T ES18188152T ES2867048T3 ES 2867048 T3 ES2867048 T3 ES 2867048T3 ES 18188152 T ES18188152 T ES 18188152T ES 18188152 T ES18188152 T ES 18188152T ES 2867048 T3 ES2867048 T3 ES 2867048T3
- Authority
- ES
- Spain
- Prior art keywords
- compound
- myelofibrosis
- therapeutic agent
- mmol
- deuterium
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
-
- 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
- A61K31/403—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 condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
-
- 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
- A61K31/435—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
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
- A61K31/5685—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone having an oxo group in position 17, e.g. androsterone
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- A61P37/02—Immunomodulators
-
- 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
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Molecular Biology (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261660428P | 2012-06-15 | 2012-06-15 | |
| US201261678795P | 2012-08-02 | 2012-08-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2867048T3 true ES2867048T3 (es) | 2021-10-20 |
Family
ID=48699982
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES18188152T Active ES2867048T3 (es) | 2012-06-15 | 2013-06-14 | Derivados deuterados de ruxolitinib |
| ES21156398T Active ES3037872T3 (en) | 2012-06-15 | 2013-06-14 | Deuterated derivatives of ruxolitinib |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES21156398T Active ES3037872T3 (en) | 2012-06-15 | 2013-06-14 | Deuterated derivatives of ruxolitinib |
Country Status (19)
| Country | Link |
|---|---|
| US (7) | US20150197525A1 (index.php) |
| EP (4) | EP3882249B1 (index.php) |
| AU (3) | AU2013274030B2 (index.php) |
| BR (1) | BR122023027277A2 (index.php) |
| CA (1) | CA2876306C (index.php) |
| DK (2) | DK3450434T3 (index.php) |
| EA (1) | EA201492287A1 (index.php) |
| ES (2) | ES2867048T3 (index.php) |
| FI (1) | FI3882249T3 (index.php) |
| HR (1) | HRP20250965T1 (index.php) |
| IN (1) | IN2014DN10670A (index.php) |
| LT (1) | LT3882249T (index.php) |
| MX (2) | MX373123B (index.php) |
| PL (2) | PL3450434T3 (index.php) |
| PT (1) | PT3882249T (index.php) |
| RS (1) | RS67061B1 (index.php) |
| SI (1) | SI3882249T1 (index.php) |
| SM (1) | SMT202500302T1 (index.php) |
| WO (1) | WO2013188783A1 (index.php) |
Families Citing this family (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LT2455382T (lt) | 2005-12-13 | 2017-02-10 | Incyte Holdings Corporation | Heteroarilu pakeisti pirolo[2,3-b]piridinai ir prolo[2,3-b]pirimidinai kaip janus kinazės inhibitoriai |
| US8765734B2 (en) | 2010-03-10 | 2014-07-01 | Incyte Corporation | Piperidin-4-yl azetidine derivatives as JAK1 inhibitors |
| WO2012177606A1 (en) | 2011-06-20 | 2012-12-27 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| EP3882249B1 (en) | 2012-06-15 | 2025-05-14 | Sun Pharmaceutical Industries, Inc. | Deuterated derivatives of ruxolitinib |
| NZ748448A (en) | 2012-11-15 | 2019-12-20 | Incyte Holdings Corp | Sustained-release dosage forms of ruxolitinib |
| EP3721873A1 (en) | 2013-08-07 | 2020-10-14 | Incyte Corporation | Sustained release dosage forms for a jak1 inhibitor |
| WO2015184087A2 (en) * | 2014-05-28 | 2015-12-03 | Institute For Myeloma & Bone Cancer Research | Anti-cancer effects of jak2 inhibitors in combination with thalidomide derivatives and glucocorticoids |
| US10865203B2 (en) | 2015-06-03 | 2020-12-15 | Uwm Research Foundation, Inc. | Ligands selective to alpha 6 subunit-containing GABAA receptors and their methods of use |
| US11364226B2 (en) | 2017-06-30 | 2022-06-21 | Cinrx Pharma, Llc | Deuterated domperidone compositions, methods, and preparation |
| JP7296185B2 (ja) | 2016-02-04 | 2023-06-22 | シンリックス ファーマ、エルエルシー | 重水素化ドンペリドン組成物及び疾患の治療方法 |
| AU2017217806A1 (en) * | 2016-02-12 | 2018-08-16 | Vertex Pharmaceuticals (Europe) Limited | Deuterium-modified CFTR modulators |
| HUE068643T2 (hu) * | 2016-05-04 | 2025-01-28 | Sun Pharmaceutical Ind Inc | Hajhullási rendellenességek kezelése deuterált JAK-inhibitorokkal |
| EP3554485B9 (en) | 2016-12-14 | 2023-09-27 | Biora Therapeutics, Inc. | Treatment of a disease of the gastrointestinal tract with a jak inhibitor and devices |
| US12478612B2 (en) | 2017-06-30 | 2025-11-25 | Cindome Pharma, Inc. | Deuterated domperidone compositions, methods, and preparation |
| EP3713545A1 (en) | 2017-11-22 | 2020-09-30 | Dauntless 1, Inc. | Therapeutic compound formulations |
| EP3713660A1 (en) | 2017-11-22 | 2020-09-30 | Dauntless 1, Inc. | Membrane emulsification device for microsphere creation |
| US11179412B2 (en) * | 2017-12-04 | 2021-11-23 | University of Pittsburgh—of the Commonwealth System of Higher Education | Methods of treating conditions involving elevated inflammatory response |
| US10596161B2 (en) | 2017-12-08 | 2020-03-24 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| EP3762424A1 (en) | 2018-03-08 | 2021-01-13 | Novartis AG | Use of an anti-p-selectin antibody |
| MA52655A (fr) | 2018-03-30 | 2021-02-17 | Incyte Corp | Biomarqueurs pour maladie cutanée inflammatoire |
| PT3773593T (pt) | 2018-03-30 | 2024-06-25 | Incyte Corp | Tratamento da hidradenite supurativa com inibidores de jak |
| MX2020010815A (es) | 2018-04-13 | 2020-12-11 | Incyte Corp | Biomarcadores para enfermedad de injerto contra hospedero. |
| WO2020039401A1 (en) | 2018-08-24 | 2020-02-27 | Novartis Ag | Treatment comprising il-1βeta binding antibodies and combinations thereof |
| WO2020163653A1 (en) * | 2019-02-06 | 2020-08-13 | Concert Pharmaceuticals, Inc. | Process for preparing enantiomerically enriched jak inhibitors |
| SG11202109563WA (en) | 2019-03-05 | 2021-09-29 | Incyte Corp | Jak1 pathway inhibitors for the treatment of chronic lung allograft dysfunction |
| WO2020191041A2 (en) | 2019-03-19 | 2020-09-24 | Incyte Corporation | Biomarkers for vitiligo |
| WO2020210125A1 (en) | 2019-04-10 | 2020-10-15 | University Of Notre Dame Du Lac | Deuterated antimicrobial compounds |
| EP3963843A4 (en) | 2019-05-02 | 2023-01-25 | INTEL Corporation | QUALITY OF SERVICE (QOS) IN INFORMATION CENTRIC NETWORKING (ICN) |
| WO2020236950A1 (en) | 2019-05-21 | 2020-11-26 | Dauntless 1, Inc. | Therapeutic microsphere formulations containing charged polymers |
| CN114423786A (zh) | 2019-09-16 | 2022-04-29 | 诺华股份有限公司 | 高亲和力的、配体阻断性、人源化的抗T细胞免疫球蛋白结构域和粘蛋白结构域3（TIM-3）IgG4抗体用于治疗骨髓纤维化的用途 |
| TW202123941A (zh) | 2019-09-16 | 2021-07-01 | 瑞士商諾華公司 | Ｍｄｍ２抑制劑用於治療骨髓纖維化之用途 |
| CA3156007A1 (en) | 2019-09-27 | 2021-04-01 | Disc Medicine, Inc. | METHODS OF TREATING MYELOFIBROSE AND ASSOCIATED CONDITIONS |
| WO2021072098A1 (en) | 2019-10-10 | 2021-04-15 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| US12203942B2 (en) | 2019-10-10 | 2025-01-21 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| US11992490B2 (en) | 2019-10-16 | 2024-05-28 | Incyte Corporation | Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP) |
| JP7518900B2 (ja) | 2019-10-16 | 2024-07-18 | インサイト・コーポレイション | 皮膚エリテマトーデス及び扁平苔癬（ｌｐ）の治療のためのｊａｋ１阻害剤の使用 |
| CN116059192B (zh) | 2019-11-13 | 2024-10-29 | 润佳（苏州）医药科技有限公司 | 同位素富集的3-氨基-1-丙磺酸及其衍生物的用途 |
| IL293085A (en) | 2019-11-22 | 2022-07-01 | Incyte Corp | Combination therapy comprising an alk2 inhibitor and a jak2 inhibitor |
| KR20230012539A (ko) | 2020-05-13 | 2023-01-26 | 디스크 메디슨, 인크. | 골수섬유증을 치료하기 위한 항-헤모주벨린 (hjv) 항체 |
| WO2021236139A1 (en) | 2020-05-21 | 2021-11-25 | Concert Pharmaceuticals, Inc. | Novel deuterated jak inhibitor and uses thereof |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| CA3194469A1 (en) | 2020-08-12 | 2022-02-17 | Concert Pharmaceuticals, Inc. | Process for preparing enantiomerically enriched jak inhibitors |
| EP4225317A1 (en) | 2020-10-08 | 2023-08-16 | Novartis AG | Use of an erk inhibitor for the treatment of myelofibrosis |
| PE20231945A1 (es) | 2020-10-28 | 2023-12-05 | Sun Pharmaceutical Ind Inc | Regimenes para el tratamiento de los trastornos de la perdida de cabello con inhibidores de jak deuterados |
| EP4247383A1 (en) * | 2020-11-19 | 2023-09-27 | Sol-Gel Technologies Ltd. | Ruxolitinib or deuterated ruxolitinib composition and uses thereof |
| SI4255442T1 (sl) | 2020-12-04 | 2025-06-30 | Incyte Corporation | Zaviralec jak z analogom vitamina d za zdravljenje kožnih bolezni |
| TW202237083A (zh) | 2021-01-11 | 2022-10-01 | 美商英塞特公司 | 包含ｊａｋ路徑抑制劑及ｒｏｃｋ抑制劑之組合療法 |
| CN114853760B (zh) * | 2021-02-03 | 2025-12-05 | 南京正大天晴制药有限公司 | 一种芦可替尼中间体的制备方法 |
| EP4384175A1 (en) | 2021-08-11 | 2024-06-19 | Sun Pharmaceutical Industries, Inc. | Treatment of hair loss disorders with deuterated jak inhibitors |
| US20240307401A1 (en) | 2021-08-12 | 2024-09-19 | Sun Pharmaceeutical Industries, Inc. | Treatment of jak-inhibition-responsive disorders with prodrugs of jak inhibitors |
| CN113820413B (zh) * | 2021-09-17 | 2023-04-07 | 重庆华邦胜凯制药有限公司 | 高效液相色谱法分离测定磷酸芦可替尼及杂质的方法 |
| JP2025515051A (ja) | 2022-05-04 | 2025-05-13 | サン ファーマシューティカル インダストリーズ，インコーポレイテッド | 重水素化ｊａｋ阻害剤による治療のための投与レジメン |
| CN117384163A (zh) * | 2022-07-05 | 2024-01-12 | 盛世泰科生物医药技术(苏州)股份有限公司 | 一种含偕二氟基的化合物及其制备方法和用途 |
| EP4680231A1 (en) * | 2023-03-17 | 2026-01-21 | Mayo Foundation for Medical Education and Research | Use of oral jak kinase inhibitors to treat lichen planus |
| EP4683713A1 (en) | 2023-03-23 | 2026-01-28 | GlaxoSmithKline Intellectual Property (No.3) Limited | Deuterated p2x3 modulators |
| US12364699B2 (en) | 2023-10-10 | 2025-07-22 | Sun Pharmaceuticals Industries, Inc. | Method of treating hair loss disorders |
| US12247034B1 (en) | 2024-04-19 | 2025-03-11 | Sun Pharmaceutical Industries, Inc. | Crystalline form of deuruxolitinib phosphate |
| WO2025226637A1 (en) | 2024-04-22 | 2025-10-30 | Incyte Corporation | Combination therapy with an anti-colony stimulating factor 1 receptor antibody and a jak inhibitor |
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| JO2630B1 (en) | 2006-04-13 | 2012-06-17 | نوفارتيس ايه جي | Organic compounds |
| WO2008030382A1 (en) * | 2006-09-05 | 2008-03-13 | Schering Corporation | Pharmaceutical combinations for lipid management and in the treatment of atherosclerosis and hepatic steatosis |
| CL2008001709A1 (es) | 2007-06-13 | 2008-11-03 | Incyte Corp | Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras. |
| DK2740731T3 (en) * | 2007-06-13 | 2016-04-11 | Incyte Holdings Corp | CRYSTALLINE SALTS OF JANUSKINASEINHIBITOREN (R) -3- (4- (7H-pyrrolo [2,3-d] pyrimidin-4-yl) -1H-pyrazol-1-yl) -3-CYCLOPENTYLPROPANNITRIL |
| US7855204B2 (en) | 2008-01-22 | 2010-12-21 | Concert Pharmaceuticals Inc. | Derivatives of gefitinib |
| JOP20190230A1 (ar) | 2009-01-15 | 2017-06-16 | Incyte Corp | طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به |
| EP3882249B1 (en) | 2012-06-15 | 2025-05-14 | Sun Pharmaceutical Industries, Inc. | Deuterated derivatives of ruxolitinib |
| NZ748448A (en) * | 2012-11-15 | 2019-12-20 | Incyte Holdings Corp | Sustained-release dosage forms of ruxolitinib |
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2013
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- 2013-06-14 EP EP13732046.1A patent/EP2861600A1/en not_active Withdrawn
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2022
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