CN107849010B - 作为nr2b nmda受体拮抗剂的3,3‐二氟哌啶氨基甲酸酯杂环化合物 - Google Patents
作为nr2b nmda受体拮抗剂的3,3‐二氟哌啶氨基甲酸酯杂环化合物 Download PDFInfo
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- CN107849010B CN107849010B CN201680042502.8A CN201680042502A CN107849010B CN 107849010 B CN107849010 B CN 107849010B CN 201680042502 A CN201680042502 A CN 201680042502A CN 107849010 B CN107849010 B CN 107849010B
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- pharmaceutically acceptable
- acceptable salt
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- 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
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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
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- A—HUMAN NECESSITIES
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- 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
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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
- A61K31/435—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
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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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines 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
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- 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
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- 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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- 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
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- 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
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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
- A61P25/24—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
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- 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
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- Health & Medical Sciences (AREA)
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- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562169107P | 2015-06-01 | 2015-06-01 | |
| US62/169,107 | 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 |
|---|---|
| CN107849010A CN107849010A (zh) | 2018-03-27 |
| CN107849010B true CN107849010B (zh) | 2021-11-09 |
Family
ID=57441824
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201680042502.8A Active CN107849010B (zh) | 2015-06-01 | 2016-05-31 | 作为nr2b nmda受体拮抗剂的3,3‐二氟哌啶氨基甲酸酯杂环化合物 |
Country Status (17)
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2017002775A (es) | 2014-09-15 | 2017-08-10 | Rugen Holdings (Cayman) Ltd | Derivados de pirrolopirimidina como antagonistas del receptor de n-metil-d-aspartato (nmda), subunidad nr2b. |
| US10221182B2 (en) | 2015-02-04 | 2019-03-05 | Rugen Holdings (Cayman) Limited | 3,3-difluoro-piperidine derivatives as NR2B NMDA receptor antagonists |
| CA2987606C (en) | 2015-06-01 | 2024-02-20 | Rugen Holdings (Cayman) Limited | 3,3-difluoropiperidine carbamate heterocyclic compounds as nr2b nmda receptor antagonists |
| 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 |
| WO2018098128A1 (en) | 2016-11-22 | 2018-05-31 | 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 |
| IL297333B2 (en) | 2020-04-17 | 2025-09-01 | Honeybrains Llc | Preparations and methods for treating neuropsychiatric disorders |
| CN117159541B (zh) * | 2023-09-20 | 2026-05-26 | 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 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1798744A (zh) * | 2003-06-04 | 2006-07-05 | 麦克公司 | 作为nmda/nr2b拮抗剂的3-氟-哌啶化合物 |
| WO2012123312A1 (en) * | 2011-03-11 | 2012-09-20 | Glaxo Group Limited | Pyrido[3,4-b]pyrazine derivatives as syk inhibitors |
| WO2013156614A1 (en) * | 2012-04-20 | 2013-10-24 | Ucb Pharma S.A. | Methods for treating parkinson's disease |
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| DE3717867A1 (de) | 1987-05-26 | 1988-12-15 | Schiepe Stapelautomaten Gmbh | Stapelvorrichtung |
| IL122649A (en) | 1995-08-11 | 2001-08-26 | Pfizer | (1s, 2s) - 1- (4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanol methanesulfonate trihydrate, its use in the preparation of medicaments and pharmaceutical compositions comprising same |
| 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 |
| MXPA03007621A (es) | 2001-02-23 | 2003-12-04 | Merck & Co Inc | Antagonistas nr2b de n-metil-d-aspartato no arilheterociclicos n-sustituidos. |
| US7592360B2 (en) | 2003-06-04 | 2009-09-22 | Merck & Co., Inc. | 3-fluoro-piperidines as NMDA/NR2B antagonists |
| WO2005102390A2 (en) | 2004-04-22 | 2005-11-03 | Pfizer Japan, Inc. | Combinations comprising alpha-2-delta ligands and nmda receptor antagonists |
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| CA2591738A1 (en) * | 2004-12-22 | 2006-06-29 | Merck & Co., Inc. | Process for making substituted piperidines |
| CA2603876A1 (en) | 2005-04-19 | 2006-10-26 | Merck & Co., Inc. | N-alkyl-azacycloalkyl nmda/nr2b antagonists |
| 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 |
| EP2520567A3 (en) | 2006-02-23 | 2012-12-12 | Shionogi & Co., Ltd. | Nitrogen-containing heterocycle derivatives substituted with cyclic group |
| CA2662702A1 (en) * | 2006-09-07 | 2008-03-13 | Merck & Co., Inc. | Difluorinated piperidines for treatment of alzheimer's disease and related conditions |
| KR20090094338A (ko) | 2006-12-27 | 2009-09-04 | 사노피-아벤티스 | 치환된 이소퀴놀린 및 이소퀴놀리논 유도체 |
| US20110053951A1 (en) | 2008-03-27 | 2011-03-03 | Evotec Neurosciences Gmbh | Methods for treating disorders using nmda nr2b-subtype selective antagonist |
| US20100010565A1 (en) * | 2008-07-09 | 2010-01-14 | Samuel Victor Lichtenstein | Extended range wireless muscular and neural stimulation |
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| EP2519241A2 (en) | 2009-12-28 | 2012-11-07 | Afraxis, Inc. | Methods for treating autism |
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| JP6007417B2 (ja) | 2011-05-31 | 2016-10-12 | レセプトス エルエルシー | 新規glp−1受容体安定剤および調節剤 |
| EA029056B1 (ru) * | 2012-12-11 | 2018-02-28 | Такеда Фармасьютикал Компани Лимитед | Гетероциклическое соединение |
| CN105308049A (zh) | 2013-01-29 | 2016-02-03 | 阿普廷伊克斯股份有限公司 | 螺-内酰胺nmda受体调节剂及其用途 |
| JP2017500287A (ja) * | 2013-11-06 | 2017-01-05 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | Gsk−3阻害剤として有用な置換ピリジン誘導体 |
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| BR112016025910A8 (pt) | 2014-05-06 | 2021-07-13 | Univ Northwestern | uso de uma quantidade eficaz de glyx-13, uso de glyx-13 e um antagonista de nmdar e composição farmaceuticamente aceitável compreendendo os mesmos |
| US10030026B2 (en) | 2014-06-04 | 2018-07-24 | Rugen Holdings (Cayman) Limited | Difluoroethylpyridine derivatives as NR2B NMDA receptor antagonists |
| MX2017002775A (es) | 2014-09-15 | 2017-08-10 | Rugen Holdings (Cayman) Ltd | Derivados de pirrolopirimidina como antagonistas del receptor de n-metil-d-aspartato (nmda), subunidad nr2b. |
| US20180271869A1 (en) | 2014-09-22 | 2018-09-27 | Jie Liu | 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 |
| US10221182B2 (en) | 2015-02-04 | 2019-03-05 | Rugen Holdings (Cayman) Limited | 3,3-difluoro-piperidine derivatives as NR2B NMDA receptor antagonists |
| CA2987606C (en) | 2015-06-01 | 2024-02-20 | Rugen Holdings (Cayman) Limited | 3,3-difluoropiperidine carbamate heterocyclic compounds as nr2b nmda receptor antagonists |
| WO2018098128A1 (en) | 2016-11-22 | 2018-05-31 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
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2016
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- 2016-05-31 AU AU2016270677A patent/AU2016270677B2/en active Active
- 2016-05-31 BR BR112017025023-3A patent/BR112017025023B1/pt active IP Right Grant
- 2016-05-31 CN CN201680042502.8A patent/CN107849010B/zh active Active
- 2016-05-31 TW TW105117083A patent/TWI721987B/zh active
- 2016-05-31 AR ARP160101591A patent/AR104837A1/es unknown
- 2016-05-31 JP JP2017562029A patent/JP6876625B2/ja active Active
- 2016-05-31 US US15/578,460 patent/US10584127B2/en active Active
- 2016-05-31 KR KR1020177037807A patent/KR102613179B1/ko active Active
- 2016-05-31 RU RU2017142005A patent/RU2735277C2/ru active
- 2016-05-31 WO PCT/US2016/035098 patent/WO2016196513A1/en not_active Ceased
- 2016-05-31 DK DK16804257.0T patent/DK3303323T3/da active
- 2016-05-31 ES ES16804257T patent/ES2784398T3/es active Active
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2017
- 2017-11-24 ZA ZA2017/08006A patent/ZA201708006B/en unknown
- 2017-11-27 IL IL255937A patent/IL255937B/en active IP Right Grant
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2018
- 2018-08-10 US US16/100,596 patent/US10294230B2/en active Active
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2020
- 2020-03-05 US US16/810,258 patent/US11136328B2/en active Active
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2021
- 2021-10-01 US US17/491,676 patent/US20220024937A1/en not_active Abandoned
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1798744A (zh) * | 2003-06-04 | 2006-07-05 | 麦克公司 | 作为nmda/nr2b拮抗剂的3-氟-哌啶化合物 |
| WO2012123312A1 (en) * | 2011-03-11 | 2012-09-20 | Glaxo Group Limited | Pyrido[3,4-b]pyrazine derivatives as syk inhibitors |
| WO2013156614A1 (en) * | 2012-04-20 | 2013-10-24 | Ucb Pharma S.A. | Methods for treating parkinson's disease |
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