AR075777A1 - Derivados de benzotiazina, su preparacion y aplicacion como farmacos para la inhibicion de 11beta-hidroxiesteroide deshidrogenasa tipo i (11betahsd1) - Google Patents
Derivados de benzotiazina, su preparacion y aplicacion como farmacos para la inhibicion de 11beta-hidroxiesteroide deshidrogenasa tipo i (11betahsd1)Info
- Publication number
- AR075777A1 AR075777A1 ARP100100618A ARP100100618A AR075777A1 AR 075777 A1 AR075777 A1 AR 075777A1 AR P100100618 A ARP100100618 A AR P100100618A AR P100100618 A ARP100100618 A AR P100100618A AR 075777 A1 AR075777 A1 AR 075777A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- substituted
- unsubstituted
- halogen
- ocf3
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
- C07D275/04—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
- C07D275/06—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to the ring sulfur atom
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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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/5415—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
-
- 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
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- 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
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D279/02—1,2-Thiazines; Hydrogenated 1,2-thiazines
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Ophthalmology & Optometry (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Biomedical Technology (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Cosmetics (AREA)
Abstract
Derivados de benzotiazina que tienen la capacidad de inhibir 11beta-HSD1, no solo en el nivel enzimático, sino además, en el nivel celular. Reivindicacion 1: Compuestos que tienen la formula general (1): donde: R1 representa: Hidrogeno; alquilo C1-6; COR5; SO2R5; CO(CH2)mR6; CO(CH2)mOR6; (CH2)mR6; (CH2)mCONR7R8; (CH2)nNR7R8; (CH2)nOR6; CHR7OR9; (CH2)mR10; m representa: 1 a 6; n representa: 2 a 6; R2 representa: un fenilo sustituido con uno o más grupos seleccionados de un halogeno, alquilo C1-6, CN, OH, CF3, OCF3, SMe, COMe, CMe(OH)CF3, CH(OH)CF3, COOR7, CONR7R11; un naftilo, 1,2,3,4-tetrahidro-naftaleno, bifenilo, fenilo, piridina o un heterociclo diferente de indol, en el caso donde R1, R4 y R'4 representan un hidrogeno, o bien no sustituido o sustituido con uno o más grupos seleccionados de un halogeno o alquilo C1-6, CN, OH, CF3, OCF3, OMe, SMe; un cicloalquilo, o bien no sustituido o sustituido con OH, CONH2, SO2Me, SO2NH2; alquilo C1-6 arilo o cicloalquil arilo; condicion: - el grupo R2 siempre está unido al carbonilo a través de un átomo de carbono; - cuando R2 es un fenilo, el sustituyente COOR7 nunca está en la posicion 4 en relacion con el carbonilo; R3 representa: metilo o etilo; R4 y R'4, idénticos o diferentes, representan: hidrogeno; halogeno; alquilo C1-6; CN; CF3; OCF3; SMe; OMe; NR7R8; SO2Me; R5 representa: alquilo C1-6; fenilo, o bien no sustituido o sustituido con uno o más grupos seleccionados de halogeno, alquilo C1-6, CN, OH, CF3, OCF3, SMe; un naftilo, o bien no sustituido o sustituido con uno o más grupos seleccionados de halogeno o alquilo C1-6, CN, OH, CF3, OCF3, SMe; un cicloalquilo, o bien no sustituido o sustituido con un CONH2, SO2Me, SO2NH2; heteroarilo, o bien no sustituido o sustituido con uno o más grupos seleccionados de halogeno, alquilo C1-6, CN, OH, CF3, OCF3, SMe; R6 representa: hidrogeno; alquilo C1-6 fenilo, o bien no sustituido o sustituido con uno o más grupos seleccionados de halogeno, alquilo C1-6, CN, OH, CF3, OCF3, SMe; un naftilo o heterociclo, o bien no sustituido o sustituido con uno o más grupos seleccionados de halogeno o alquilo C1-6, CN, OH, CF3, OCF3, SMe; un cicloalquilo, o bien no sustituido o sustituido con CONH2, SO2Me, SO2NH2; R7 representa: hidrogeno, alquilo C1-6; R8 representa: hidrogeno, alquilo C1-6, fenilo, o bien no sustituido o sustituido con uno o más grupos seleccionados de halogeno, alquilo C1-6, CN, OH, CF3, OCF3, SMe; un naftilo o heterociclo, o bien no sustituido o sustituido con uno o más grupos seleccionados de halogeno, alquilo C1-6, CN, OH, CF3, OCF3, SMe; un cicloalquilo, o bien no sustituido o sustituido con CONH2, SO2Me, SO2NH2; R7 y R8 tomados juntos pueden formar un ciclo de 4 a 6 miembros con el átomo de nitrogeno al cual están unidos, que puede contener uno o más heteroátomos seleccionados de N, S u O, y que puede estar o bien no sustituido o sustituido con uno o más grupos seleccionados de alquilo C1-6, alquilo C1-6 arilo o arilo; R9 representa: COOMe, COOEt; R10 representa: halogeno, COOH, COOR7; R11 representa: hidrogeno, alquilo C1-6, alquilo C1-6 cicloalquilo, cicloalquilo, arilo, alquilo C1-6 arilo; al igual que sus estereoisomeros, sales y solvatos aceptables para uso terapéutico.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0951336A FR2942797B1 (fr) | 2009-03-03 | 2009-03-03 | Derives de benzothiazines, leur preparation et leur application a titre de medicaments |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR075777A1 true AR075777A1 (es) | 2011-04-27 |
Family
ID=40790339
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100100618A AR075777A1 (es) | 2009-03-03 | 2010-03-02 | Derivados de benzotiazina, su preparacion y aplicacion como farmacos para la inhibicion de 11beta-hidroxiesteroide deshidrogenasa tipo i (11betahsd1) |
Country Status (29)
| Country | Link |
|---|---|
| US (1) | US9187438B2 (es) |
| EP (1) | EP2403840B1 (es) |
| JP (1) | JP5650139B2 (es) |
| KR (1) | KR101701531B1 (es) |
| CN (1) | CN102341379B (es) |
| AR (1) | AR075777A1 (es) |
| AU (1) | AU2010220335B2 (es) |
| BR (1) | BRPI1010243A2 (es) |
| CA (1) | CA2753630C (es) |
| CL (1) | CL2011002171A1 (es) |
| CO (1) | CO6501175A2 (es) |
| ES (1) | ES2483516T3 (es) |
| FR (1) | FR2942797B1 (es) |
| GE (1) | GEP20135832B (es) |
| HK (1) | HK1165802A1 (es) |
| IL (1) | IL214907A (es) |
| MA (1) | MA33138B1 (es) |
| MX (1) | MX2011008942A (es) |
| MY (1) | MY160819A (es) |
| NZ (1) | NZ595276A (es) |
| PL (1) | PL2403840T3 (es) |
| RU (1) | RU2523791C2 (es) |
| SA (1) | SA110310181B1 (es) |
| SG (1) | SG174208A1 (es) |
| TN (1) | TN2011000429A1 (es) |
| TW (1) | TWI495636B (es) |
| UA (1) | UA105040C2 (es) |
| WO (1) | WO2010100139A1 (es) |
| ZA (1) | ZA201107104B (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2350077B1 (es) | 2009-06-04 | 2011-11-04 | Laboratorios Salvat, S.A. | Compuestos inhibidores de 11beta-hidroxiesteroide deshidrogenasa de tipo 1. |
| CN103271923B (zh) * | 2013-06-28 | 2014-11-26 | 安徽中医学院 | 一种苯并噻嗪衍生物的医药用途 |
| CN103275035B (zh) * | 2013-06-28 | 2014-11-26 | 安徽中医学院 | 苯并噻嗪类化合物、其制备方法及其抗肿瘤用途 |
| CN103304513B (zh) * | 2013-06-28 | 2015-02-04 | 安徽中医学院 | 一类1,2-苯并噻嗪类化合物、制备方法及其应用 |
| FR3035326B1 (fr) * | 2015-04-21 | 2017-05-12 | Pf Medicament | Utilisation de la (4-hydroxy-2-methyl-1,1-dioxido-2h-benzo[e][1,2]thiazin-3-yl)(naphtalen-2-yl)methanone dans la prevention et/ou le traitement de la steatohepatite non-alcoolique |
| CN106243046B (zh) * | 2016-08-02 | 2019-07-05 | 南京工业大学 | 一种甲基二磺隆的制备方法 |
| CN110709396A (zh) | 2017-04-06 | 2020-01-17 | 伊文蒂瓦公司 | Yap/taz-tead相互作用的新化合物抑制剂及其在治疗恶性间皮瘤中的用途 |
| EP3632908A1 (en) | 2018-10-02 | 2020-04-08 | Inventiva | Inhibitors of the yap/taz-tead interaction and their use in the treatment of cancer |
| WO2023154412A1 (en) * | 2022-02-12 | 2023-08-17 | Miralogx Llc | Anti-inflammatory compounds, pharmaceutical compositions, and treatment methods |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3591584A (en) * | 1968-08-27 | 1971-07-06 | Pfizer | Benzothiazine dioxides |
| US3808205A (en) * | 1971-09-10 | 1974-04-30 | Warner Lambert Co | Process for the preparation of 4-hydroxy-3-carbamyl-2h-1,2-benzothiazine 1,1-dioxides and 4-hydroxy-3(2h)-1,2-benzothiazine carboxylate-1,1-dioxides |
| US4289879A (en) * | 1980-09-29 | 1981-09-15 | Pfizer Inc. | Synthetic method and intermediate for piroxicam |
| FR2694295B1 (fr) * | 1992-07-28 | 1994-09-02 | Adir | Nouveaux peptides dérivés de trifluoromethylcetones, leur procéde de préparation et les compositions pharmaceutiques qui les contiennent. |
| US5599811A (en) * | 1995-02-21 | 1997-02-04 | Warner-Lambert Company | Benzothiazine dioxides as endothelin antagonists |
| WO2002030914A1 (en) * | 2000-10-12 | 2002-04-18 | Dr. Reddy's Research Foundation | Salts of benzothiazine and benzoxazine derivatives and pharmaceutical compositions containing them |
| GB0224830D0 (en) * | 2002-10-24 | 2002-12-04 | Sterix Ltd | Compound |
| JP2006522747A (ja) * | 2003-04-11 | 2006-10-05 | ノボ ノルディスク アクティーゼルスカブ | 縮合１，２，４−トリアゾールの薬学的使用 |
| PL372356A1 (pl) * | 2005-01-20 | 2006-07-24 | ADAMED Sp.z o.o. | Nowe związki, pochodne kwasu 3-fenylopropionowego |
| AU2006304434B2 (en) * | 2005-10-20 | 2012-04-05 | Merck Sharp & Dohme Corp. | Triazole derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1 |
| EP1953145B1 (en) * | 2005-11-21 | 2015-11-04 | Shionogi & Co., Ltd. | Heterocyclic compound having inhibitory activity on 11-b-hydroxysteroid dehydrogenase type i |
| JP2007197369A (ja) * | 2006-01-26 | 2007-08-09 | Sankyo Co Ltd | ベンゾチアジン誘導体 |
-
2009
- 2009-03-03 FR FR0951336A patent/FR2942797B1/fr not_active Expired - Fee Related
-
2010
- 2010-03-02 MA MA34191A patent/MA33138B1/fr unknown
- 2010-03-02 KR KR1020117022812A patent/KR101701531B1/ko active IP Right Grant
- 2010-03-02 GE GEAP201012398A patent/GEP20135832B/en unknown
- 2010-03-02 ES ES10706624.3T patent/ES2483516T3/es active Active
- 2010-03-02 EP EP10706624.3A patent/EP2403840B1/en active Active
- 2010-03-02 SG SG2011063146A patent/SG174208A1/en unknown
- 2010-03-02 WO PCT/EP2010/052609 patent/WO2010100139A1/en active Application Filing
- 2010-03-02 AU AU2010220335A patent/AU2010220335B2/en not_active Ceased
- 2010-03-02 AR ARP100100618A patent/AR075777A1/es active IP Right Grant
- 2010-03-02 CA CA2753630A patent/CA2753630C/en not_active Expired - Fee Related
- 2010-03-02 NZ NZ595276A patent/NZ595276A/xx not_active IP Right Cessation
- 2010-03-02 RU RU2011139014/04A patent/RU2523791C2/ru not_active IP Right Cessation
- 2010-03-02 CN CN201080010207.7A patent/CN102341379B/zh not_active Expired - Fee Related
- 2010-03-02 JP JP2011552415A patent/JP5650139B2/ja not_active Expired - Fee Related
- 2010-03-02 MX MX2011008942A patent/MX2011008942A/es active IP Right Grant
- 2010-03-02 PL PL10706624T patent/PL2403840T3/pl unknown
- 2010-03-02 MY MYPI2011004096A patent/MY160819A/en unknown
- 2010-03-02 US US13/254,473 patent/US9187438B2/en not_active Expired - Fee Related
- 2010-03-02 SA SA110310181A patent/SA110310181B1/ar unknown
- 2010-03-02 UA UAA201111590A patent/UA105040C2/uk unknown
- 2010-03-02 BR BRPI1010243A patent/BRPI1010243A2/pt not_active Application Discontinuation
- 2010-03-03 TW TW099106123A patent/TWI495636B/zh not_active IP Right Cessation
-
2011
- 2011-08-19 TN TN2011000429A patent/TN2011000429A1/fr unknown
- 2011-08-31 IL IL214907A patent/IL214907A/en active IP Right Grant
- 2011-09-02 CL CL2011002171A patent/CL2011002171A1/es unknown
- 2011-09-29 CO CO11128125A patent/CO6501175A2/es active IP Right Grant
- 2011-09-29 ZA ZA2011/07104A patent/ZA201107104B/en unknown
-
2012
- 2012-07-06 HK HK12106611.2A patent/HK1165802A1/xx not_active IP Right Cessation
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