JPWO2019201752A5 - - Google Patents
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- JPWO2019201752A5 JPWO2019201752A5 JP2020555045A JP2020555045A JPWO2019201752A5 JP WO2019201752 A5 JPWO2019201752 A5 JP WO2019201752A5 JP 2020555045 A JP2020555045 A JP 2020555045A JP 2020555045 A JP2020555045 A JP 2020555045A JP WO2019201752 A5 JPWO2019201752 A5 JP WO2019201752A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- heterocyclyl
- pharmaceutical composition
- fibrosis
- 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.)
- Pending
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- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 4
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 4
- 206010016654 Fibrosis Diseases 0.000 claims 3
- 101000694615 Homo sapiens Membrane primary amine oxidase Proteins 0.000 claims 3
- 102100027159 Membrane primary amine oxidase Human genes 0.000 claims 3
- 208000019425 cirrhosis of liver Diseases 0.000 claims 3
- 239000003112 inhibitor Substances 0.000 claims 3
- 208000030159 metabolic disease Diseases 0.000 claims 3
- 201000009104 prediabetes syndrome Diseases 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 208000004930 Fatty Liver Diseases 0.000 claims 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 2
- 208000002705 Glucose Intolerance Diseases 0.000 claims 2
- 206010019708 Hepatic steatosis Diseases 0.000 claims 2
- 229940123518 Sodium/glucose cotransporter 2 inhibitor Drugs 0.000 claims 2
- 230000001476 alcoholic effect Effects 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 239000008280 blood Substances 0.000 claims 2
- 210000004369 blood Anatomy 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 208000010706 fatty liver disease Diseases 0.000 claims 2
- 230000004761 fibrosis Effects 0.000 claims 2
- 239000008103 glucose Substances 0.000 claims 2
- 208000006454 hepatitis Diseases 0.000 claims 2
- 231100000283 hepatitis Toxicity 0.000 claims 2
- -1 isooxazolyl Chemical group 0.000 claims 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 2
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- QKDRXGFQVGOQKS-CRSSMBPESA-N (2s,3r,4r,5s,6r)-2-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-6-methylsulfanyloxane-3,4,5-triol Chemical compound C1=CC(OCC)=CC=C1CC1=CC([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](SC)O2)O)=CC=C1Cl QKDRXGFQVGOQKS-CRSSMBPESA-N 0.000 claims 1
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 206010002388 Angina unstable Diseases 0.000 claims 1
- 208000031104 Arterial Occlusive disease Diseases 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 208000031229 Cardiomyopathies Diseases 0.000 claims 1
- 208000002177 Cataract Diseases 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- JVHXJTBJCFBINQ-ADAARDCZSA-N Dapagliflozin Chemical compound C1=CC(OCC)=CC=C1CC1=CC([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)=CC=C1Cl JVHXJTBJCFBINQ-ADAARDCZSA-N 0.000 claims 1
- 208000002249 Diabetes Complications Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 206010012655 Diabetic complications Diseases 0.000 claims 1
- 208000008960 Diabetic foot Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 206010056340 Diabetic ulcer Diseases 0.000 claims 1
- 206010018429 Glucose tolerance impaired Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 208000029523 Interstitial Lung disease Diseases 0.000 claims 1
- WHSOLWOTCHFFBK-ZQGJOIPISA-N Luseogliflozin Chemical compound C1=CC(OCC)=CC=C1CC1=CC([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)S2)O)=C(OC)C=C1C WHSOLWOTCHFFBK-ZQGJOIPISA-N 0.000 claims 1
- 206010054805 Macroangiopathy Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000021908 Myocardial disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000036110 Neuroinflammatory disease Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010033307 Overweight Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 208000031481 Pathologic Constriction Diseases 0.000 claims 1
- 208000001280 Prediabetic State Diseases 0.000 claims 1
- 208000032056 Radiation Fibrosis Syndrome Diseases 0.000 claims 1
- GSINGUMRKGRYJP-VZWAGXQNSA-N Remogliflozin Chemical compound C1=CC(OC(C)C)=CC=C1CC1=C(C)N(C(C)C)N=C1O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 GSINGUMRKGRYJP-VZWAGXQNSA-N 0.000 claims 1
- 208000034189 Sclerosis Diseases 0.000 claims 1
- 208000007718 Stable Angina Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- ZXOCGDDVNPDRIW-NHFZGCSJSA-N Tofogliflozin Chemical compound O.C1=CC(CC)=CC=C1CC1=CC=C(CO[C@@]23[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O3)O)C2=C1 ZXOCGDDVNPDRIW-NHFZGCSJSA-N 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 208000007814 Unstable Angina Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 230000005856 abnormality Effects 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- 229960001713 canagliflozin Drugs 0.000 claims 1
- VHOFTEAWFCUTOS-TUGBYPPCSA-N canagliflozin hydrate Chemical compound O.CC1=CC=C([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)C=C1CC(S1)=CC=C1C1=CC=C(F)C=C1.CC1=CC=C([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)C=C1CC(S1)=CC=C1C1=CC=C(F)C=C1 VHOFTEAWFCUTOS-TUGBYPPCSA-N 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 229960003834 dapagliflozin Drugs 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 230000002526 effect on cardiovascular system Effects 0.000 claims 1
- 229960003345 empagliflozin Drugs 0.000 claims 1
- OBWASQILIWPZMG-QZMOQZSNSA-N empagliflozin Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1C1=CC=C(Cl)C(CC=2C=CC(O[C@@H]3COCC3)=CC=2)=C1 OBWASQILIWPZMG-QZMOQZSNSA-N 0.000 claims 1
- 208000030533 eye disease Diseases 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 206010061989 glomerulosclerosis Diseases 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 208000013403 hyperactivity Diseases 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 201000004332 intermediate coronary syndrome Diseases 0.000 claims 1
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 1
- 229950000991 ipragliflozin Drugs 0.000 claims 1
- AHFWIQIYAXSLBA-RQXATKFSSA-N ipragliflozin Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1C1=CC=C(F)C(CC=2SC3=CC=CC=C3C=2)=C1 AHFWIQIYAXSLBA-RQXATKFSSA-N 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 230000003902 lesion Effects 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 229950004397 luseogliflozin Drugs 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 230000000291 postprandial effect Effects 0.000 claims 1
- 229940126844 remogliflozin Drugs 0.000 claims 1
- 201000002793 renal fibrosis Diseases 0.000 claims 1
- 229950005268 sotagliflozin Drugs 0.000 claims 1
- 208000037804 stenosis Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 229950006667 tofogliflozin Drugs 0.000 claims 1
- 231100000331 toxic Toxicity 0.000 claims 1
- 230000002588 toxic effect Effects 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP18167739.4 | 2018-04-17 | ||
| EP18167739 | 2018-04-17 | ||
| PCT/EP2019/059341 WO2019201752A1 (en) | 2018-04-17 | 2019-04-11 | Pharmaceutical composition, methods for treating and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021520394A JP2021520394A (ja) | 2021-08-19 |
| JP2021520394A5 JP2021520394A5 (https=) | 2022-04-12 |
| JPWO2019201752A5 true JPWO2019201752A5 (https=) | 2022-04-12 |
Family
ID=62017227
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020555045A Pending JP2021520394A (ja) | 2018-04-17 | 2019-04-11 | 医薬組成物、処置方法及びその使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20210113561A1 (https=) |
| EP (1) | EP3781166A1 (https=) |
| JP (1) | JP2021520394A (https=) |
| CN (1) | CN111989103A (https=) |
| AU (1) | AU2019254371A1 (https=) |
| WO (1) | WO2019201752A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK3873600T5 (da) | 2018-10-29 | 2024-03-18 | Boehringer Ingelheim Int | Pyridinylsulfonamidderivater, farmaceutiske sammensætninger og anvendelser deraf |
| US12213970B2 (en) | 2018-10-29 | 2025-02-04 | Boehringer Ingelheim International Gmbh | Pyridinyl sulfonamide derivatives, pharmaceutical compositions and uses thereof |
| CN113893256A (zh) * | 2020-07-06 | 2022-01-07 | 诺未科技(北京)有限公司 | 化合物或其可药用盐、二聚体或三聚体在制备治疗癌症的药物中的应用 |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE264337T1 (de) | 1999-08-31 | 2004-04-15 | Kissei Pharmaceutical | Glucopyranosyloxypyrazol-derivate, diese enthaltende arzneimittel und zwischenprodukte zu deren herstellung |
| US6515117B2 (en) | 1999-10-12 | 2003-02-04 | Bristol-Myers Squibb Company | C-aryl glucoside SGLT2 inhibitors and method |
| PH12000002657B1 (en) | 1999-10-12 | 2006-02-21 | Bristol Myers Squibb Co | C-aryl glucoside SGLT2 inhibitors |
| AU2002223127A1 (en) | 2000-11-30 | 2002-06-11 | Kissei Pharmaceutical Co., Ltd. Intellectual Property | Glucopyranosyloxybenzyl benzene derivatives, medicinal compositions containing the same and intermediates in the production thereof |
| PL209375B1 (pl) | 2000-12-28 | 2011-08-31 | Kissei Pharmaceutical | Pochodne glukopiranozyloksypirazolu, kompozycja farmaceutyczna zawierająca takie pochodne i zastosowanie tych pochodnych do wytwarzania kompozycji farmaceutycznej |
| JP4490109B2 (ja) | 2002-03-22 | 2010-06-23 | キッセイ薬品工業株式会社 | グルコピラノシルオキシベンジルベンゼン誘導体の結晶 |
| DE10231370B4 (de) | 2002-07-11 | 2006-04-06 | Sanofi-Aventis Deutschland Gmbh | Thiophenglycosidderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zur Herstellung dieser Arzneimittel |
| ES2567571T3 (es) | 2003-03-14 | 2016-04-25 | Astellas Pharma Inc. | Derivados de C-glucósido y sales de los mismos |
| LT2896397T (lt) | 2003-08-01 | 2017-11-27 | Mitsubishi Tanabe Pharma Corporation | Nauji junginiai, turintys inhibitorinį aktyvumą prieš nuo natrio priklausomą gliukozės transporterį |
| ATE557013T1 (de) | 2004-03-16 | 2012-05-15 | Boehringer Ingelheim Int | Glucopyranosyl-substituierte benzol-derivate, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung |
| TW200637839A (en) | 2005-01-07 | 2006-11-01 | Taisho Pharmaceutical Co Ltd | 1-thio-d-glucitol derivatives |
| TW200637869A (en) | 2005-01-28 | 2006-11-01 | Chugai Pharmaceutical Co Ltd | The spiroketal derivatives and the use as therapeutical agent for diabetes of the same |
| UA91546C2 (uk) | 2005-05-03 | 2010-08-10 | Бьорінгер Інгельхайм Інтернаціональ Гмбх | КРИСТАЛІЧНА ФОРМА 1-ХЛОР-4-(β-D-ГЛЮКОПІРАНОЗ-1-ИЛ)-2-[4-((S)-ТЕТРАГІДРОФУРАН-3-ІЛОКСИ)-БЕНЗИЛ]-БЕНЗОЛУ, СПОСІБ ЇЇ ОДЕРЖАННЯ ТА ЇЇ ЗАСТОСУВАННЯ ПРИ ПРИГОТУВАННІ ЛІКАРСЬКИХ ЗАСОБІВ |
| US7772191B2 (en) | 2005-05-10 | 2010-08-10 | Boehringer Ingelheim International Gmbh | Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives and intermediates therein |
| WO2007093610A1 (en) | 2006-02-15 | 2007-08-23 | Boehringer Ingelheim International Gmbh | Glucopyranosyl-substituted benzonitrile derivatives, pharmaceutical compositions containing such compounds, their use and process for their manufacture |
| JP5230613B2 (ja) | 2006-05-23 | 2013-07-10 | テラコス・インコーポレイテッド | グルコース輸送体阻害剤およびその使用方法 |
| US7919598B2 (en) | 2006-06-28 | 2011-04-05 | Bristol-Myers Squibb Company | Crystal structures of SGLT2 inhibitors and processes for preparing same |
| TWI499414B (zh) | 2006-09-29 | 2015-09-11 | Lexicon Pharmaceuticals Inc | 鈉與葡萄糖第2型共同運輸體(co-transporter 2)的抑制物與其應用方法 |
| UY30730A1 (es) | 2006-12-04 | 2008-07-03 | Mitsubishi Tanabe Pharma Corp | Forma cristalina del hemihidrato de 1-(b (beta)-d-glucopiranosil) -4-metil-3-[5-(4-fluorofenil) -2-tienilmetil]benceno |
| WO2008109591A1 (en) | 2007-03-08 | 2008-09-12 | Lexicon Pharmaceuticals, Inc. | Phlorizin analogs as inhibitors of sodium glucose co-transporter 2 |
| AR065809A1 (es) | 2007-03-22 | 2009-07-01 | Bristol Myers Squibb Co | Formulaciones farmaceuticas que contienen un inhibidor sglt2 |
| AU2008279424B2 (en) | 2007-07-26 | 2013-06-13 | Lexicon Pharmaceuticals, Inc. | Methods and compounds useful for the preparation of sodium glucose co-transporter 2 inhibitors |
| MX2010002695A (es) | 2007-09-10 | 2010-04-01 | Janssen Pharmaceutica Nv | Proceso para la preparacion de compuestos utiles como inhibidores de transportador de glucosa dependiente de sodio (sglt). |
| TW201011043A (en) | 2008-06-20 | 2010-03-16 | Chugai Pharmaceutical Co Ltd | Crystal of spiroketal derivatives and process for preparation of spiroketal derivatives |
| TWI472521B (zh) | 2008-07-17 | 2015-02-11 | Lexicon Pharmaceuticals Inc | (2s,3r,4r,5s,6r)-2-(4-氯-3-(4-乙氧苄基)苯基)-6-(甲硫)四氫-2h-哌喃-3,4,5-三醇的固體形態與其使用方法 |
| MY155418A (en) | 2008-08-28 | 2015-10-15 | Pfizer | Dioxa-bicyclo[3.2.1]octane-2,3,4-triol derivatives |
| KR101921934B1 (ko) | 2009-02-13 | 2018-11-26 | 베링거 인겔하임 인터내셔날 게엠베하 | 글루코피라노실 디페닐메탄 유도체를 포함하는 약제학적 조성물, 이들의 약제학적 용량형, 이들의 제조방법 및 환자에서의 개선된 당 조절을 위한 이들의 용도 |
| BRPI1008560B1 (pt) * | 2009-02-13 | 2021-08-31 | Boehringer Ingelheim International Gmbh | Composição farmacêutica compreendendo um inibidor de sglt2, um inibidor de dpp-iv e opcionalmente um outro agente antidiabético e usos dos mesmos |
| AP2011005795A0 (en) * | 2009-02-13 | 2011-08-31 | Boehringer Ingelheim Int | SGLT-2 inhibitor for treating type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance or hyperglycemia. |
| EP2419097B1 (en) | 2009-04-16 | 2013-09-25 | Taisho Pharmaceutical Co., Ltd. | Pharmaceutical composition comprising (1s)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-d-glucitol and metformin and uses thereof in the treatment of diabetes |
| AU2010303123B2 (en) | 2009-09-30 | 2014-02-27 | Boehringer Ingelheim International Gmbh | Method for the preparation of a crystalline form of 1-chloro-4- (Beta-D-glucopyranos-1-yl)-2-(4-((S)-tetrahydrofuran-3-yloxy)benzyl)benzene |
| JP5758900B2 (ja) | 2009-09-30 | 2015-08-05 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | グルコピラノシル置換ベンジルベンゼン誘導体の調製方法 |
| WO2014123749A1 (en) * | 2013-01-30 | 2014-08-14 | Board Of Regents Of The University Of Nebraska | Compositions and methods for treating complications associated with diabetes |
| JP2018501276A (ja) * | 2015-01-09 | 2018-01-18 | ギリアド アポロ, エルエルシー | 非アルコール性脂肪肝疾患の処置のためのacc阻害剤併用療法 |
| ES2844926T3 (es) * | 2016-05-12 | 2021-07-23 | Boehringer Ingelheim Int | Derivados de piridinilo, composiciones farmacéuticas y usos de los mismos como inhibidores de AOC3 |
-
2019
- 2019-04-11 US US17/047,708 patent/US20210113561A1/en not_active Abandoned
- 2019-04-11 AU AU2019254371A patent/AU2019254371A1/en not_active Abandoned
- 2019-04-11 CN CN201980026070.5A patent/CN111989103A/zh active Pending
- 2019-04-11 JP JP2020555045A patent/JP2021520394A/ja active Pending
- 2019-04-11 WO PCT/EP2019/059341 patent/WO2019201752A1/en not_active Ceased
- 2019-04-11 EP EP19718639.8A patent/EP3781166A1/en not_active Withdrawn
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