BRPI0607088A2 - derivados de tetrahidrofurano heterocìclico tetracìclico como inibidores de 5ht2 no tratamento de distúrbios cns - Google Patents
derivados de tetrahidrofurano heterocìclico tetracìclico como inibidores de 5ht2 no tratamento de distúrbios cnsInfo
- Publication number
- BRPI0607088A2 BRPI0607088A2 BRPI0607088-4A BRPI0607088A BRPI0607088A2 BR PI0607088 A2 BRPI0607088 A2 BR PI0607088A2 BR PI0607088 A BRPI0607088 A BR PI0607088A BR PI0607088 A2 BRPI0607088 A2 BR PI0607088A2
- Authority
- BR
- Brazil
- Prior art keywords
- treatment
- tetrahydrofuran derivatives
- inhibitors
- receptors
- tetracyclic heterocyclic
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- -1 heterocyclic tetrahydrofuran derivatives Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 102000049773 5-HT2A Serotonin Receptor Human genes 0.000 abstract 1
- 102000006902 5-HT2C Serotonin Receptor Human genes 0.000 abstract 1
- 102000040125 5-hydroxytryptamine receptor family Human genes 0.000 abstract 1
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 abstract 1
- 102000004980 Dopamine D2 Receptors Human genes 0.000 abstract 1
- 108090001111 Dopamine D2 Receptors Proteins 0.000 abstract 1
- 108050004812 Dopamine receptor Proteins 0.000 abstract 1
- 102000015554 Dopamine receptor Human genes 0.000 abstract 1
- 101150104779 HTR2A gene Proteins 0.000 abstract 1
- 101150013372 Htr2c gene Proteins 0.000 abstract 1
- 125000000815 N-oxide group Chemical group 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 208000028017 Psychotic disease Diseases 0.000 abstract 1
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical class C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000002526 effect on cardiovascular system Effects 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000000966 norepinephrine reuptake Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
-
- 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
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- 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
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/22—Anxiolytics
-
- 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
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
- C07D491/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Gynecology & Obstetrics (AREA)
- Diabetes (AREA)
- Child & Adolescent Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Anesthesiology (AREA)
- Addiction (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Nutrition Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
DERIVADOS DE TETRAHIDROFURANO HETEROCìCLICO TETRACICLICO COMO INIBIDORES DE 5HT2 NO TRATAMENTO DE DISTúRBIOS CNS. A presente invenção refere-se a novos derivados de tetrahidrofurano heterocíclico tetracíclico substituidos com afinidades de ligação por receptores de serotonina, em particular receptores 5-HT2A e 5-HT2ç e por receptores de dopamina, em particular receptores de dopamina D2 e com propriedades de inibição da recaptação de norepinefrina, composições farmacêuticas compreendendo os compostos de acordo com a invenção, o uso dos mesmos como um medicamento, em particular para a prevenção e/ou tratamento de uma série de distúrbios psiquiátricos e neurológicos, em particular determinados distúrbios psicóticos, cardiovasculares e gastrocinéticos e processos para sua produção. Os compostos de acordo com a invenção podem ser representados pela Fórmula geral (1): e compreendem também os sais de adição de base ou ácido farmaceuticamente aceitáveis dos mesmos, as formas estereoquimicamente isoméricas dos mesmos, a forma de N-óxido dos mesmos e pró-fármacos dos mesmos, em que todos os substituintes são definido conforme na reivindicação 1.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05100547 | 2005-01-27 | ||
| PCT/EP2006/050444 WO2006079637A1 (en) | 2005-01-27 | 2006-01-25 | Heterocyclic tetracyclic tetrahydrofuran derivatives as 5ht2 inhibitors in the treatment of cns disorders |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0607088A2 true BRPI0607088A2 (pt) | 2009-08-04 |
Family
ID=34938591
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0607088-4A BRPI0607088A2 (pt) | 2005-01-27 | 2006-01-25 | derivados de tetrahidrofurano heterocìclico tetracìclico como inibidores de 5ht2 no tratamento de distúrbios cns |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US7915249B2 (pt) |
| EP (1) | EP1846415B1 (pt) |
| JP (1) | JP4937141B2 (pt) |
| KR (1) | KR101332218B1 (pt) |
| CN (1) | CN101107254B (pt) |
| AU (1) | AU2006209397B2 (pt) |
| BR (1) | BRPI0607088A2 (pt) |
| CA (1) | CA2595170C (pt) |
| EA (1) | EA013595B1 (pt) |
| ES (1) | ES2391780T3 (pt) |
| MX (1) | MX2007009092A (pt) |
| NZ (1) | NZ556272A (pt) |
| WO (1) | WO2006079637A1 (pt) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE602004000260T2 (de) | 2003-07-22 | 2006-08-24 | Arena Pharmaceuticals, Inc., San Diego | Diaryl- und arylheteroarylharnstoffderivate als modulatoren des 5-ht2a-serotoninrezeptors, die sich zur prophylaxe und behandlung von damit im zusammenhang stehenden erkrankungen eignen |
| SA05260357B1 (ar) | 2004-11-19 | 2008-09-08 | ارينا فارماسيتو تيكالز ، أنك | مشتقات 3_فينيل_بيرازول كمعدلات لمستقبل سيروتينين 5_ht2a مفيدة في علاج الاضطرابات المتعلقه به |
| SG171681A1 (en) | 2006-05-18 | 2011-06-29 | Arena Pharm Inc | Crystalline forms and processes for the preparation of phenyl-pyrazoles useful as modulators of the 5-ht2a serotonin receptor |
| JP5406018B2 (ja) | 2006-05-18 | 2014-02-05 | アリーナ ファーマシューティカルズ， インコーポレイテッド | ５−ｈｔ２ａセロトニンレセプターに関連する障害の処置に有用な５−ｈｔ２ａセロトニンレセプターのモジュレーターとしての１級アミン、およびその誘導体 |
| CA2646076C (en) | 2006-05-18 | 2015-06-30 | Arena Pharmaceuticals, Inc. | Ethers, secondary amines and derivatives thereof as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto |
| TWI415845B (zh) | 2006-10-03 | 2013-11-21 | Arena Pharm Inc | 用於治療與５-ｈｔ2ａ血清素受體相關聯病症之作為５-ｈｔ2ａ血清素受體之調節劑的吡唑衍生物 |
| JP5393677B2 (ja) | 2007-08-15 | 2014-01-22 | アリーナ ファーマシューティカルズ， インコーポレイテッド | ５−ＨＴ２Ａセロトニン受容体に関連した障害の治療のための５−ＨＴ２Ａセロトニン受容体のモジュレーターとしてのイミダゾ［１，２−ａ］ピリジン誘導体 |
| KR20100137473A (ko) * | 2008-02-19 | 2010-12-30 | 아돌로 코포레이션 | 동통 치료를 위한 벨록세핀, 이의 거울상이성질체, 및 이의 유사체 |
| US20110021538A1 (en) | 2008-04-02 | 2011-01-27 | Arena Pharmaceuticals, Inc. | Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor |
| US9126946B2 (en) | 2008-10-28 | 2015-09-08 | Arena Pharmaceuticals, Inc. | Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)urea and crystalline forms related thereto |
| CA2741731A1 (en) | 2008-10-28 | 2010-06-03 | Arena Pharmaceuticals, Inc. | Compositions of a 5-ht2a serotonin receptor modulator useful for the treatment of disorders related thereto |
| WO2011075596A1 (en) | 2009-12-18 | 2011-06-23 | Arena Pharmaceuticals, Inc. | Crystalline forms of certain 3-phenyl-pyrazole derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto |
| WO2015066344A1 (en) | 2013-11-01 | 2015-05-07 | Arena Pharmaceuticals, Inc. | 5-ht2c receptor agonists and compositions and methods of use |
| US10022355B2 (en) | 2015-06-12 | 2018-07-17 | Axovant Sciences Gmbh | Diaryl and arylheteroaryl urea derivatives as modulators of the 5-HT2A serotonin receptor useful for the prophylaxis and treatment of REM sleep behavior disorder |
| BR112018000728A2 (pt) | 2015-07-15 | 2018-09-04 | Axovant Sciences Gmbh | resumo método para a profilaxia e/ou tratamento de alucinações visuais em um sujeito com necessidade do mesmo |
| WO2020249689A1 (en) | 2019-06-12 | 2020-12-17 | Nouryon Chemicals International B.V. | Process for the production of peroxyesters |
| EP3983369B1 (en) | 2019-06-12 | 2023-08-02 | Nouryon Chemicals International B.V. | Process for the production of diacyl peroxides |
| EP3983368B1 (en) | 2019-06-12 | 2023-08-02 | Nouryon Chemicals International B.V. | Process for the production of diacyl peroxides |
| EP3983340B1 (en) * | 2019-06-12 | 2023-08-02 | Nouryon Chemicals International B.V. | Method for isolating carboxylic acid from an aqueous side stream |
| JP7335362B2 (ja) | 2019-06-12 | 2023-08-29 | ヌーリオン ケミカルズ インターナショナル ベスローテン フェノーツハップ | 過酸化ジアシルを生成するためのプロセス |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH615928A5 (pt) | 1975-06-18 | 1980-02-29 | Sandoz Ag | |
| CS200271B1 (cs) | 1979-02-08 | 1980-09-15 | Miroslav Rajsner | Derivát 4,5-dihydrothieno (2,3-b)-l-benzothiepinu a jeho eoli |
| CS217949B1 (cs) | 1981-08-14 | 1983-01-28 | Miroslav Protiva | Derivát 4,5-dihydrothieno(2,3-b)-1-benzothiepinu a jeho soli |
| PL158223B1 (en) | 1989-06-09 | 1992-08-31 | Method for mnufacturing 4-(1-methyl-4-pirperidilidene)-9,10-dihydro--benso(4,5) cyclohepta (1,2) thiophen-10-on | |
| CN1082963C (zh) * | 1996-04-12 | 2002-04-17 | 詹森药业有限公司 | 异噁唑烷衍生物 |
| ES2196328T3 (es) * | 1996-04-12 | 2003-12-16 | Janssen Pharmaceutica Nv | Derivados de tetrahidrofurano tetraciclicos sustituidos. |
| UA52778C2 (uk) | 1997-10-10 | 2003-01-15 | Янссен Фармацевтика Н.В. | Галогенозаміщені тетрациклічні похідні тетрагідрофурану, спосіб їх отримання та композиція на їх основі |
| UA79248C2 (en) | 2001-11-09 | 2007-06-11 | Janssen Pharmaceutica Nv | Mandelate salts of substituted tetracyclic tetrahydrofuran derivatives |
| KR20050044329A (ko) | 2001-12-07 | 2005-05-12 | 얀센 파마슈티카 엔.브이. | 트랜스-융합된3,3ａ,8,12ｂ-테트라히드로-2Ｈ-디벤조[3,4:6,7]시클로헵타[1,2-ｂ]푸란 유도체의 제조 |
| JP4912320B2 (ja) * | 2004-12-07 | 2012-04-11 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 置換された四環式テトラヒドロピラン、ピロリジンおよびテトラヒドロチオフェン誘導体 |
-
2006
- 2006-01-25 CA CA2595170A patent/CA2595170C/en not_active Expired - Fee Related
- 2006-01-25 EP EP06704282A patent/EP1846415B1/en not_active Expired - Lifetime
- 2006-01-25 EA EA200701583A patent/EA013595B1/ru not_active IP Right Cessation
- 2006-01-25 US US11/814,432 patent/US7915249B2/en not_active Expired - Fee Related
- 2006-01-25 AU AU2006209397A patent/AU2006209397B2/en not_active Ceased
- 2006-01-25 BR BRPI0607088-4A patent/BRPI0607088A2/pt not_active IP Right Cessation
- 2006-01-25 NZ NZ556272A patent/NZ556272A/en not_active IP Right Cessation
- 2006-01-25 MX MX2007009092A patent/MX2007009092A/es active IP Right Grant
- 2006-01-25 WO PCT/EP2006/050444 patent/WO2006079637A1/en not_active Ceased
- 2006-01-25 KR KR1020077019160A patent/KR101332218B1/ko not_active Expired - Fee Related
- 2006-01-25 ES ES06704282T patent/ES2391780T3/es not_active Expired - Lifetime
- 2006-01-25 JP JP2007552640A patent/JP4937141B2/ja not_active Expired - Fee Related
- 2006-01-25 CN CN2006800032542A patent/CN101107254B/zh not_active Expired - Fee Related
-
2011
- 2011-02-16 US US13/028,596 patent/US8404729B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| AU2006209397A1 (en) | 2006-08-03 |
| JP4937141B2 (ja) | 2012-05-23 |
| US8404729B2 (en) | 2013-03-26 |
| EA013595B1 (ru) | 2010-06-30 |
| US20110144094A1 (en) | 2011-06-16 |
| KR101332218B1 (ko) | 2013-11-25 |
| WO2006079637A1 (en) | 2006-08-03 |
| MX2007009092A (es) | 2007-09-12 |
| ES2391780T3 (es) | 2012-11-29 |
| EP1846415B1 (en) | 2012-08-01 |
| CN101107254A (zh) | 2008-01-16 |
| AU2006209397B2 (en) | 2011-04-07 |
| CN101107254B (zh) | 2010-12-08 |
| CA2595170C (en) | 2014-08-05 |
| EP1846415A1 (en) | 2007-10-24 |
| US7915249B2 (en) | 2011-03-29 |
| US20080108599A1 (en) | 2008-05-08 |
| KR20070098938A (ko) | 2007-10-05 |
| JP2008528548A (ja) | 2008-07-31 |
| CA2595170A1 (en) | 2006-08-03 |
| EA200701583A1 (ru) | 2008-04-28 |
| WO2006079637A8 (en) | 2007-08-16 |
| NZ556272A (en) | 2009-12-24 |
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