MX2017015370A - Compuestos heterociclicos de 3,3-difluorpiperidina carbamato como antagonistas del receptor de n-metil-d-aspartato (nmda) nr2b. - Google Patents
Compuestos heterociclicos de 3,3-difluorpiperidina carbamato como antagonistas del receptor de n-metil-d-aspartato (nmda) nr2b.Info
- Publication number
- MX2017015370A MX2017015370A MX2017015370A MX2017015370A MX2017015370A MX 2017015370 A MX2017015370 A MX 2017015370A MX 2017015370 A MX2017015370 A MX 2017015370A MX 2017015370 A MX2017015370 A MX 2017015370A MX 2017015370 A MX2017015370 A MX 2017015370A
- Authority
- MX
- Mexico
- Prior art keywords
- difluoropiperidine
- receptor antagonists
- heterocyclic compounds
- nmda receptor
- nr2b
- Prior art date
Links
- -1 3,3-difluoropiperidine carbamate heterocyclic compounds Chemical class 0.000 title 1
- 229940127523 NMDA Receptor Antagonists Drugs 0.000 title 1
- 108010054200 NR2B NMDA receptor Proteins 0.000 title 1
- 150000005829 chemical entities Chemical class 0.000 abstract 3
- 102000034527 Retinoid X Receptors Human genes 0.000 abstract 2
- 108010038912 Retinoid X Receptors Proteins 0.000 abstract 2
- 230000008485 antagonism Effects 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 208000015114 central nervous system disease Diseases 0.000 abstract 1
- 208000037765 diseases and disorders Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
Classifications
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- 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
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring 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
- A61K31/435—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
-
- 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
- A61K31/4545—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
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
- A61K31/495—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
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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
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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
- A61P25/04—Centrally acting analgesics, e.g. opioids
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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
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
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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
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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
- A61P25/24—Antidepressants
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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
- A61P25/28—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
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- 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
- 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
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Se describen entidades químicas de la Fórmula (I): donde R1 y Z son como se definen en esta solicitud, como antagonistas selectivos de receptor subtipo NR2B. Además, se describen composiciones farmacéuticas que comprenden una entidad química de la Fórmula (I), y métodos de tratamiento de diversas enfermedades y trastornos asociados con el antagonismo de NR2B, por ejemplo, enfermedades y trastornos del SNC, tales como depresión, mediante la administración de una entidad química de la Fórmula (I).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562169107P | 2015-06-01 | 2015-06-01 | |
| PCT/US2016/035098 WO2016196513A1 (en) | 2015-06-01 | 2016-05-31 | 3,3-difluoropiperidine carbamate heterocyclic compounds as nr2b nmda receptor antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2017015370A true MX2017015370A (es) | 2018-03-15 |
| MX380424B MX380424B (es) | 2025-03-12 |
Family
ID=57441824
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2017015370A MX380424B (es) | 2015-06-01 | 2016-05-31 | Compuestos heterociclicos de 3,3-difluorpiperidina carbamato como antagonistas del receptor de n-metil-d-aspartato (nmda) nr2b. |
Country Status (17)
| Country | Link |
|---|---|
| US (4) | US10584127B2 (es) |
| EP (1) | EP3303323B1 (es) |
| JP (1) | JP6876625B2 (es) |
| KR (1) | KR102613179B1 (es) |
| CN (1) | CN107849010B (es) |
| AR (1) | AR104837A1 (es) |
| AU (1) | AU2016270677B2 (es) |
| BR (1) | BR112017025023B1 (es) |
| CA (1) | CA2987606C (es) |
| DK (1) | DK3303323T3 (es) |
| ES (1) | ES2784398T3 (es) |
| IL (1) | IL255937B (es) |
| MX (1) | MX380424B (es) |
| RU (1) | RU2735277C2 (es) |
| TW (1) | TWI721987B (es) |
| WO (1) | WO2016196513A1 (es) |
| ZA (1) | ZA201708006B (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11201701853YA (en) | 2014-09-15 | 2017-04-27 | Rugen Holdings Cayman Ltd | Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists |
| EP3253761A4 (en) | 2015-02-04 | 2018-06-20 | Rugen Holdings (Cayman) Limited | 3,3-difluoro-piperidine derivatives as nr2b nmda receptor antagonists |
| KR102613179B1 (ko) | 2015-06-01 | 2023-12-14 | 뤼겐 홀딩스 (케이맨) 리미티드 | Nr2b nmda 수용체 길항제로서의 3,3-디플루오로피페리딘 카바메이트 헤테로사이클릭 화합물 |
| CN106986874B (zh) * | 2016-01-20 | 2019-09-24 | 西华大学 | (1H-吡唑[3,4-d]嘧啶)-4-氨基衍生物及其作为IDO抑制剂在药物制备中的用途 |
| EP3544610A1 (en) | 2016-11-22 | 2019-10-02 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
| US20210393621A1 (en) | 2018-10-26 | 2021-12-23 | The Research Foundation For The State University Of New York | Combination serotonin specific reuptake inhibitor and serotonin 1a receptor partial agonist for reducing l-dopa-induced dyskinesia |
| CN116134048A (zh) | 2020-04-17 | 2023-05-16 | Hb生物科技有限公司 | 用于治疗神经精神障碍的组合物和方法 |
| CN117159541A (zh) * | 2023-09-20 | 2023-12-05 | 南华大学 | Nat10拮抗剂在制备预防和/或治疗癫痫的药物中的应用 |
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| DE3717867A1 (de) | 1987-05-26 | 1988-12-15 | Schiepe Stapelautomaten Gmbh | Stapelvorrichtung |
| RU2140910C1 (ru) | 1995-08-11 | 1999-11-10 | Пфайзер Инк. | Тригидрат метансульфоната (1s,2s)-1-(4-гидроксифенил)-2-(4-гидрокси-4- фенилпиперидин-1-ил)-1-пропанола |
| GB9805977D0 (en) * | 1998-03-19 | 1998-05-20 | Silver Joshua D | Improvements in variable focus optical devices |
| US6476041B1 (en) | 1999-10-29 | 2002-11-05 | Merck & Co., Inc. | 1,4 substituted piperidinyl NMDA/NR2B antagonists |
| HU227197B1 (en) | 2000-10-24 | 2010-10-28 | Richter Gedeon Nyrt | Nmda receptor antagonist carboxylic acid amide derivatives and pharmaceutical compositions containing them |
| HUP0303258A3 (en) * | 2001-02-23 | 2004-06-28 | Merck & Co Inc | N-substituted nonaryl-heterocyclic nmda/nr2b antagonists and pharmaceutical compositions containing them |
| BRPI0410837A (pt) * | 2003-06-04 | 2006-06-27 | Merck & Co Inc | composto, composição farmacêutica, e, método para tratar ou prevenir uma doença ou condição |
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| JP2008536927A (ja) | 2005-04-19 | 2008-09-11 | メルク エンド カムパニー インコーポレーテッド | N−アルキル−アザシクロアルキルnmda/nr2b拮抗物質 |
| WO2007061868A2 (en) | 2005-11-17 | 2007-05-31 | Trustees Of Tufts College | Treatment of stereotypic, self-injurious and compulsive behaviors using specific serotonin reuptake inhibitors and antagonists of nmda receptors |
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| RU2009128693A (ru) * | 2006-12-27 | 2011-02-10 | Санофи-Авентис (Fr) | Замещенные производные изохинолина и изохинолинона |
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| JP2017516836A (ja) | 2014-06-04 | 2017-06-22 | リューゲン ホールディングス (ケイマン) リミテッド | Nr2bnmda受容体アンタゴニストとしてのジフルオロエチルピリジン誘導体 |
| SG11201701853YA (en) | 2014-09-15 | 2017-04-27 | Rugen Holdings Cayman Ltd | Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists |
| WO2016049048A1 (en) | 2014-09-22 | 2016-03-31 | Rugen Holdings (Cayman) Limited | Treatment of anxiety disorders and autism spectrum disorders |
| WO2016100349A2 (en) | 2014-12-16 | 2016-06-23 | Rugen Holdings (Cayman) Limited | Bicyclic azaheterocyclic compounds as nr2b nmda receptor antagonists |
| EP3253761A4 (en) | 2015-02-04 | 2018-06-20 | Rugen Holdings (Cayman) Limited | 3,3-difluoro-piperidine derivatives as nr2b nmda receptor antagonists |
| KR102613179B1 (ko) | 2015-06-01 | 2023-12-14 | 뤼겐 홀딩스 (케이맨) 리미티드 | Nr2b nmda 수용체 길항제로서의 3,3-디플루오로피페리딘 카바메이트 헤테로사이클릭 화합물 |
| EP3544610A1 (en) | 2016-11-22 | 2019-10-02 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
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2016
- 2016-05-31 KR KR1020177037807A patent/KR102613179B1/ko active Active
- 2016-05-31 RU RU2017142005A patent/RU2735277C2/ru active
- 2016-05-31 BR BR112017025023-3A patent/BR112017025023B1/pt active IP Right Grant
- 2016-05-31 AU AU2016270677A patent/AU2016270677B2/en active Active
- 2016-05-31 DK DK16804257.0T patent/DK3303323T3/da active
- 2016-05-31 ES ES16804257T patent/ES2784398T3/es active Active
- 2016-05-31 JP JP2017562029A patent/JP6876625B2/ja active Active
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- 2016-05-31 WO PCT/US2016/035098 patent/WO2016196513A1/en not_active Ceased
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2017
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2018
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