CA2552550A1 - Piperidine derivatives as gcs inhibitors - Google Patents
Piperidine derivatives as gcs inhibitors Download PDFInfo
- Publication number
- CA2552550A1 CA2552550A1 CA002552550A CA2552550A CA2552550A1 CA 2552550 A1 CA2552550 A1 CA 2552550A1 CA 002552550 A CA002552550 A CA 002552550A CA 2552550 A CA2552550 A CA 2552550A CA 2552550 A1 CA2552550 A1 CA 2552550A1
- Authority
- CA
- Canada
- Prior art keywords
- compound
- alkyl
- phenyl
- optionally substituted
- disease
- 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.)
- Abandoned
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- 235000010199 sorbic acid Nutrition 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 239000001593 sorbitan monooleate Substances 0.000 description 1
- 235000011069 sorbitan monooleate Nutrition 0.000 description 1
- 229940035049 sorbitan monooleate Drugs 0.000 description 1
- 238000001228 spectrum Methods 0.000 description 1
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- 230000000707 stereoselective effect Effects 0.000 description 1
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- 238000003756 stirring Methods 0.000 description 1
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- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
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- 238000010189 synthetic method Methods 0.000 description 1
- 239000002278 tabletting lubricant Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical compound C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 229940071127 thioglycolate Drugs 0.000 description 1
- CWERGRDVMFNCDR-UHFFFAOYSA-M thioglycolate(1-) Chemical compound [O-]C(=O)CS CWERGRDVMFNCDR-UHFFFAOYSA-M 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 229940100611 topical cream Drugs 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 229940100615 topical ointment Drugs 0.000 description 1
- 230000002110 toxicologic effect Effects 0.000 description 1
- 231100000759 toxicological effect Toxicity 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
- C07D211/40—Oxygen atoms
- C07D211/44—Oxygen atoms attached in position 4
- C07D211/46—Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Pulmonology (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Child & Adolescent Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Oncology (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0400812.4 | 2004-01-14 | ||
| GBGB0400812.4A GB0400812D0 (en) | 2004-01-14 | 2004-01-14 | Novel compounds |
| PCT/GB2005/000071 WO2005068426A1 (en) | 2004-01-14 | 2005-01-11 | Piperidine derivatives as gcs inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2552550A1 true CA2552550A1 (en) | 2005-07-28 |
Family
ID=31726188
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002552550A Abandoned CA2552550A1 (en) | 2004-01-14 | 2005-01-11 | Piperidine derivatives as gcs inhibitors |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20080234324A1 (https=) |
| EP (1) | EP1709000A1 (https=) |
| JP (1) | JP2007517846A (https=) |
| CN (1) | CN1910150A (https=) |
| AU (1) | AU2005205221A1 (https=) |
| BR (1) | BRPI0506843A (https=) |
| CA (1) | CA2552550A1 (https=) |
| GB (1) | GB0400812D0 (https=) |
| IL (1) | IL176823A0 (https=) |
| WO (1) | WO2005068426A1 (https=) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0100889D0 (en) | 2001-01-12 | 2001-02-21 | Oxford Glycosciences Uk Ltd | Compounds |
| US7994198B2 (en) | 2002-07-17 | 2011-08-09 | Actelion Pharmaceuticals Ltd. | Piperidinetriol derivatives as inhibitors of glycosylceramidsynthase |
| AU2003246942B2 (en) | 2002-07-17 | 2009-06-25 | Idorsia Pharmaceuticals Ltd | Piperidinetriol derivatives as inhibitors of glycosylceramide synthase |
| GB0313677D0 (en) | 2003-06-13 | 2003-07-16 | Oxford Glycosciences Uk Ltd | Novel compound |
| GB0313678D0 (en) | 2003-06-13 | 2003-07-16 | Oxford Glycosciences Uk Ltd | Novel compounds |
| EP1811991B1 (en) | 2004-11-10 | 2018-11-07 | Genzyme Corporation | Treatment of type 2 diabetes using inhibitors of glycosphingolipid synthesis |
| SI2032134T1 (sl) | 2006-05-09 | 2015-10-30 | Genzyme Corporation | Postopki zdravljenja bolezni zamaščenih jeter, ki obsegajo inhibicijo sintezo glukosfingolipida |
| EP2594564B1 (en) | 2007-05-31 | 2016-09-28 | Genzyme Corporation | 2-acylaminopropanol-type glucosylceramide synthase inhibitors |
| CN101888840A (zh) | 2007-10-05 | 2010-11-17 | 简詹姆公司 | 使用脑酰胺衍生物治疗多囊性肾疾病的方法 |
| CA2731685A1 (en) | 2008-07-28 | 2010-02-04 | Genzyme Corporation | Glucosylceramide synthase inhibition for the treatment of collapsing glomerulopathy and other glomerular disease |
| EP3078373A1 (en) | 2008-10-03 | 2016-10-12 | Genzyme Corporation | 2-acylaminopropanol-type glucosylceramide synthase inhibitor |
| WO2010091164A1 (en) | 2009-02-06 | 2010-08-12 | Exelixis, Inc. | Inhibitors of glucosylceramide synthase |
| WO2010091104A1 (en) | 2009-02-06 | 2010-08-12 | Exelixis, Inc. | Glucosylceramide synthase inhibitors |
| KR101987736B1 (ko) | 2011-03-18 | 2019-06-11 | 젠자임 코포레이션 | 글루코실세라마이드 합성효소 억제제 |
| MA37975B2 (fr) | 2012-09-11 | 2021-03-31 | Genzyme Corp | Inhibiteurs de synthase de glucosylcéramide |
| MX365464B (es) | 2013-03-15 | 2019-06-04 | Genzyme Corp | Prodecimiento para preparar inhibidores de la glucosilceramida sintasa. |
| JO3713B1 (ar) | 2013-03-15 | 2021-01-31 | Genzyme Corp | أشكال ملح (s)-كوينوكليدين-3-يل(2-(2-(4-فلوروفينيل)ثيازول-4-يل)بروبان-2-يل)كارباميت |
| JP6537500B2 (ja) | 2013-09-20 | 2019-07-03 | ビオマリン プハルマセウトイカル インコーポレイテッド | 疾患治療用のグルコシルセラミドシンターゼ阻害剤 |
| FR3011468B1 (fr) * | 2013-10-04 | 2015-12-04 | Inventiva | Utilisation de l'odiparcil dans le traitement d'une mucopolysaccharidose |
| HRP20181197T1 (hr) | 2013-10-29 | 2018-11-30 | Biomarin Pharmaceutical Inc. | Derivati n-(1-hidroksi-3-(pirolidinil)propan-2-il)pirolidin-3-karboksamida kao inhibitori glukozilceramid sintaze |
| US20170333435A1 (en) | 2014-11-06 | 2017-11-23 | Lysosomal Therapeutics Inc. | Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders |
| US20180185368A1 (en) | 2014-11-06 | 2018-07-05 | Lysosomal Therapeutics Inc. | Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders |
| EP4406616A3 (en) | 2014-11-06 | 2024-11-06 | Bial-R&D Investments, S.A. | Substituted pyrazolo(1,5-a)pyrimidines and their use in the treatment of medical disorders |
| CN107635980A (zh) | 2015-03-11 | 2018-01-26 | 生物马林药物股份有限公司 | 用于治疗疾病的葡糖神经酰胺合酶抑制剂 |
| CA3020305A1 (en) | 2016-04-06 | 2017-10-12 | Lysosomal Therapeutics Inc. | Imidazo [1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| EP3440081A4 (en) | 2016-04-06 | 2019-09-18 | Lysosomal Therapeutics Inc. | PYRROLO [1,2-A] PYRIMIDINYL-CARBOXAMIDE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDER |
| AU2017246455B2 (en) | 2016-04-06 | 2021-09-30 | Bial - R&D Investments, S.A. | Pyrazolo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| EP3452045A1 (en) * | 2016-05-04 | 2019-03-13 | Lysosomal Therapeutics Inc. | Methods of treatment and combination therapies using gcase activator heterobicyclic and related compounds |
| WO2017192931A1 (en) | 2016-05-05 | 2017-11-09 | Lysosomal Therapeutics Inc. | SUBSTITUTED IMDAZO[1,2-α]PYRIDINES, SUBSTITUTED IMIDAZO[1,2-α]PYRAZINES, RELATED COMPOUNDS, AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS |
| KR102530515B1 (ko) | 2016-05-05 | 2023-05-09 | 비알 - 알&디 인베스트먼츠, 에스.에이. | 치환된 이미다조[1,2-b]피리다진, 치환된 이미다조[1,5-b]피리다진, 관련 화합물, 및 의학적 장애의 치료에서의 그의 용도 |
| CN114040762A (zh) | 2019-02-04 | 2022-02-11 | 建新公司 | 使用葡糖神经酰胺合酶(gcs)的抑制剂治疗纤毛疾病 |
| CN113645969A (zh) | 2019-02-04 | 2021-11-12 | 建新公司 | 用于治疗与溶酶体贮积症相关的症状和病症的方法 |
| EP3966199B1 (en) | 2019-05-10 | 2026-03-18 | Alectos Therapeutics Inc. | Non-lysosomal glucosylceramidase inhibitors and uses thereof |
| US20230002380A1 (en) | 2019-11-15 | 2023-01-05 | Yuhan Corporation | Novel compounds having inhibitory activity against glucosylceramide synthase or pharmaceutically acceptable salt thereof, processes for preparing the same, and pharmaceutical compositions comprising the same |
| AU2020384066B2 (en) | 2019-11-15 | 2025-10-30 | Green Cross Corporation | Novel derivatives having 2,3-dihydro-1H-indene or 2,3-dihydrobenzofuran moiety or pharmaceutically acceptable salt thereof and pharmaceutical compositions comprising the same |
| JP2023512366A (ja) | 2020-02-03 | 2023-03-27 | ジェンザイム・コーポレーション | リソソーム蓄積性疾患と関連する神経学的症状を処置するための方法 |
| FR3109523B1 (fr) * | 2020-04-23 | 2023-11-17 | Univ Grenoble Alpes | Nouveaux composés chaperons pharmacologiques de l’alpha-glucosidase acide humaine et leur utilisation thérapeutique |
| EP4142878B1 (en) | 2020-04-28 | 2024-06-26 | The Regents of The University of Michigan | Pyridine inhibitors of glucosylceramide synthase and therapeutic methods using the same |
| PH12022552955A1 (en) | 2020-05-07 | 2024-02-26 | Alectos Therapeutics Inc | Non-lysosomal glucosylceramidase inhibitors and uses thereof |
| AU2021311131B2 (en) | 2020-07-24 | 2026-02-19 | Genzyme Corporation | Pharmaceutical compositions comprising venglustat |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2086413A1 (en) * | 1990-06-29 | 1991-12-30 | Yohji Ezure | Piperidine derivatives |
| PT1030839E (pt) * | 1997-11-10 | 2004-05-31 | Searle & Co | Utilizacao de iminoacucares para tratar a resistencia a multifarmacos |
| GB0100889D0 (en) * | 2001-01-12 | 2001-02-21 | Oxford Glycosciences Uk Ltd | Compounds |
-
2004
- 2004-01-14 GB GBGB0400812.4A patent/GB0400812D0/en not_active Ceased
-
2005
- 2005-01-11 BR BRPI0506843-6A patent/BRPI0506843A/pt not_active IP Right Cessation
- 2005-01-11 JP JP2006548389A patent/JP2007517846A/ja active Pending
- 2005-01-11 WO PCT/GB2005/000071 patent/WO2005068426A1/en not_active Ceased
- 2005-01-11 CA CA002552550A patent/CA2552550A1/en not_active Abandoned
- 2005-01-11 US US10/586,188 patent/US20080234324A1/en not_active Abandoned
- 2005-01-11 AU AU2005205221A patent/AU2005205221A1/en not_active Abandoned
- 2005-01-11 EP EP05701841A patent/EP1709000A1/en not_active Withdrawn
- 2005-01-11 CN CNA2005800023093A patent/CN1910150A/zh active Pending
-
2006
- 2006-07-13 IL IL176823A patent/IL176823A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2007517846A (ja) | 2007-07-05 |
| BRPI0506843A (pt) | 2007-06-12 |
| US20080234324A1 (en) | 2008-09-25 |
| IL176823A0 (en) | 2006-10-31 |
| GB0400812D0 (en) | 2004-02-18 |
| CN1910150A (zh) | 2007-02-07 |
| WO2005068426A1 (en) | 2005-07-28 |
| AU2005205221A1 (en) | 2005-07-28 |
| EP1709000A1 (en) | 2006-10-11 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |