PE20110807A1 - Inhibidores de cinasa akt y p70 s6 - Google Patents
Inhibidores de cinasa akt y p70 s6Info
- Publication number
- PE20110807A1 PE20110807A1 PE2011001018A PE2011001018A PE20110807A1 PE 20110807 A1 PE20110807 A1 PE 20110807A1 PE 2011001018 A PE2011001018 A PE 2011001018A PE 2011001018 A PE2011001018 A PE 2011001018A PE 20110807 A1 PE20110807 A1 PE 20110807A1
- Authority
- PE
- Peru
- Prior art keywords
- piperidin
- pirrolo
- ona
- imidazol
- pyrimidin
- Prior art date
Links
Classifications
-
- 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
- A61K31/495—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
-
- 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
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
-
- 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
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurosurgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Child & Adolescent Psychology (AREA)
- Pulmonology (AREA)
- Biomedical Technology (AREA)
- Oncology (AREA)
- Reproductive Health (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE PIPERIDINA DE FORMULA (I) DONDE X ES F, Cl, CF3, CN O H; Y ES F, H O Cl; R1 Y R2 SON CADA UNO H, ALQUILO(C1-C4) O CH2CH2OH, O R1 Y R2 JUNTO CON EL ATOMO DE N AL QUE ESTAN UNIDOS FORMAN UN ANILLO DE PIRROLIDINA O AZETIDINA; R3 ES H U OH; R6 ES H, O R6 Y R2 JUNTO CON EL ATOMO DE N AL CUAL R2 ESTA UNIDO FORMAN UN ANILLO DE PIPERIDINA; R7 Y R8 SON CADA UNO H O CH3, O R7 Y R1 JUNTO CON EL ATOMO DE N AL CUAL R1 ESTA UNIDO FORMAN UN ANILLO DE PIRROLIDINA; W ES C=O, C=CH-R9, ENTRE OTROS, DONDE R9 ES 2-TIAZOLILO, 4-PIRIDILO, 2-METIL-4-TIAZOLILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 4-{4-[4-(4-FLUORO-3-TRIFLUOROMETIL-FENIL)-1-(2-METILAMINO-ETIL)-1H-IMIDAZOL-2-IL]-PIPERIDIN-1-IL}-5,7-DIHIDRO-PIRROLO[2,3-d]PIRIMIDIN-6-ONA; 4-{4-[1-(2-AMINO-ETIL)-4-(4-FLUORO-3-TRIFLUOROMETIL-FENIL)-1H-IMIDAZOL-2-IL]-PIPERIDIN-1-IL}-5,7-DIHIDRO-PIRROLO[2,3-d]PIRIMIDIN-6-ONA; 4-{4-[4-(4-FLUORO-3-TRIFLUOROMETIL-FENIL)-1-((R)-1-METIL-PIPERIDIN-3-IL)-1H-IMIDAZOL-2-IL]-PIPERIDIN-1-IL}-5,7-DIHIDRO-PIRROLO[2,3-d]PIRIMIDIN-6-ONA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE CINASA P70 S6 Y AKT SIENDO UTILES EN EL TRATAMIENTO DE GLIOBLASTOMA MULTIFORME
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11327308P | 2008-11-11 | 2008-11-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20110807A1 true PE20110807A1 (es) | 2011-10-31 |
Family
ID=41402451
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2011001018A PE20110807A1 (es) | 2008-11-11 | 2009-11-03 | Inhibidores de cinasa akt y p70 s6 |
Country Status (37)
| Country | Link |
|---|---|
| US (1) | US8148387B2 (es) |
| EP (1) | EP2358710B1 (es) |
| JP (1) | JP5432275B2 (es) |
| KR (1) | KR101334460B1 (es) |
| CN (1) | CN102216302B (es) |
| AR (1) | AR074072A1 (es) |
| AU (1) | AU2009314324B2 (es) |
| BR (1) | BRPI0921916A2 (es) |
| CA (1) | CA2743019C (es) |
| CO (1) | CO6382114A2 (es) |
| CR (1) | CR20110240A (es) |
| CY (1) | CY1113409T1 (es) |
| DK (1) | DK2358710T3 (es) |
| DO (1) | DOP2011000129A (es) |
| EA (1) | EA018947B1 (es) |
| EC (1) | ECSP11011048A (es) |
| ES (1) | ES2391704T3 (es) |
| HK (1) | HK1158203A1 (es) |
| HN (1) | HN2011001247A (es) |
| HR (1) | HRP20120738T1 (es) |
| IL (1) | IL211940A (es) |
| JO (1) | JO2822B1 (es) |
| MA (1) | MA32776B1 (es) |
| MX (1) | MX2011005000A (es) |
| MY (1) | MY161461A (es) |
| NZ (1) | NZ592062A (es) |
| PA (1) | PA8846901A1 (es) |
| PE (1) | PE20110807A1 (es) |
| PL (1) | PL2358710T3 (es) |
| PT (1) | PT2358710E (es) |
| RS (1) | RS52520B (es) |
| SI (1) | SI2358710T1 (es) |
| TN (1) | TN2011000207A1 (es) |
| TW (1) | TWI422587B (es) |
| UA (1) | UA100190C2 (es) |
| WO (1) | WO2010056563A1 (es) |
| ZA (1) | ZA201102549B (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2448927T3 (pl) | 2009-07-02 | 2014-09-30 | Sanofi Sa | Nowe pochodne (6-okso-1,6-dihydro-pirymidyn-2-ylo)-amidu, ich wytwarzanie i ich zastosowanie farmaceutyczne jako inhibitorów fosforylacji AKT |
| EP2491032B1 (en) * | 2009-10-23 | 2014-04-16 | Eli Lilly and Company | Akt inhibitors |
| HUE026323T2 (en) | 2011-04-07 | 2016-05-30 | Bayer Ip Gmbh | Imidazopyridazines as AKT kinase inhibitors |
| JP5695800B2 (ja) * | 2011-07-09 | 2015-04-08 | 山東軒竹医薬科技有限公司 | ジペプチジルペプチダーゼ−ｉｖ阻害剤の塩の結晶形ｉ、及びその製造方法並びにその応用 |
| ES2646759T3 (es) | 2011-09-12 | 2017-12-15 | Merck Patent Gmbh | Derivados de aminopirimidina para uso como moduladores de la actividad de la quinasa |
| DK2755965T3 (en) * | 2011-09-12 | 2017-09-25 | Merck Patent Gmbh | PRESENT UNKNOWN IMIDAZOLAMINES AS MODULATORS OF KINASE ACTIVITY |
| AU2013344549B2 (en) | 2012-11-16 | 2018-03-08 | Xiaoling Chen | Novel imidazol-piperidinyl derivatives as modulators of kinase activity |
| JP6386467B2 (ja) * | 2012-11-16 | 2018-09-05 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | キナーゼ活性のモジュレーターとしての新規複素環式誘導体 |
| ES2746756T3 (es) * | 2013-03-11 | 2020-03-06 | Merck Patent Gmbh | Derivados de 6-[4-(1H-imidazol-2-il)piperidin-1-il]pirimidin-4-amina como moduladores de la actividad cinasa |
| US9434714B2 (en) * | 2014-02-11 | 2016-09-06 | Merck Patent Gmbh | Pyrimidine imidazole amines as modulators of kinase activity |
| TW201718574A (zh) | 2015-08-12 | 2017-06-01 | 美國禮來大藥廠 | Ｃｇｒｐ受體拮抗劑 |
| WO2017200087A1 (ja) * | 2016-05-20 | 2017-11-23 | 大鵬薬品工業株式会社 | 新規５Ｈ－ピロロ［２，３－ｄ］ピリミジン－６（７Ｈ）－オン誘導体 |
| US20230148417A1 (en) * | 2020-03-17 | 2023-05-11 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Fused bicyclic derivative, preparation method therefor, and pharmaceutical use thereof |
| CN113444110B (zh) * | 2020-03-25 | 2023-05-12 | 江苏恒瑞医药股份有限公司 | 四氢吡咯并吡唑类衍生物、其制备方法及其在医药上的应用 |
| CA3231865A1 (en) | 2021-09-17 | 2023-03-23 | Tingting SHANG | Fused bicyclic derivative, pharmaceutically acceptable salt, crystal form thereof and preparation method therefor |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8076338B2 (en) | 2004-04-23 | 2011-12-13 | Exelixis, Inc. | Kinase modulators and methods of use |
| MY179032A (en) | 2004-10-25 | 2020-10-26 | Cancer Research Tech Ltd | Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors |
| US7994172B2 (en) | 2004-12-28 | 2011-08-09 | Exelixis, Inc. | [1H-pyrazolo[3, 4-D]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (P70s6k, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases |
| US7423043B2 (en) * | 2005-02-18 | 2008-09-09 | Lexicon Pharmaceuticals, Inc. | 4-Piperidin-1-yl-7H-pyrrolo[2,3-d]pyrimidine compounds |
| WO2007003960A1 (en) | 2005-06-30 | 2007-01-11 | Prosidion Limited | Gpcr agonists |
| EP3719018A1 (en) | 2006-04-25 | 2020-10-07 | Astex Therapeutics Ltd | Purine and deazapurine derivatives as pharmaceutical compounds |
| JP2009536620A (ja) | 2006-04-25 | 2009-10-15 | アステックス、セラピューティックス、リミテッド | 医薬組み合わせ物 |
| WO2008012635A2 (en) | 2006-07-26 | 2008-01-31 | Pfizer Products Inc. | Amine derivatives useful as anticancer agents |
| AR064416A1 (es) * | 2006-12-21 | 2009-04-01 | Cancer Rec Tech Ltd | Derivados de purina, piridina y pirimidina condensadas con heterociclos, moduladores de pka y/o pkb, composiciones farmaceuticas que los contienen, y usos para el tratamiento de enfermedades hiperproliferativas. |
| UA99284C2 (ru) | 2007-05-11 | 2012-08-10 | Елі Ліллі Енд Компані | ИНГИБИТОРЫ р70 S6-КИНАЗЫ |
-
2009
- 2009-10-28 AR ARP090104158A patent/AR074072A1/es unknown
- 2009-10-29 TW TW098136731A patent/TWI422587B/zh not_active IP Right Cessation
- 2009-10-29 PA PA20098846901A patent/PA8846901A1/es unknown
- 2009-10-29 JO JO2009400A patent/JO2822B1/en active
- 2009-11-03 CN CN2009801449532A patent/CN102216302B/zh active Active
- 2009-11-03 DK DK09744896.3T patent/DK2358710T3/da active
- 2009-11-03 PE PE2011001018A patent/PE20110807A1/es not_active Application Discontinuation
- 2009-11-03 MY MYPI2011002030A patent/MY161461A/en unknown
- 2009-11-03 NZ NZ592062A patent/NZ592062A/xx not_active IP Right Cessation
- 2009-11-03 US US12/611,139 patent/US8148387B2/en active Active
- 2009-11-03 RS RS20120443A patent/RS52520B/en unknown
- 2009-11-03 CA CA2743019A patent/CA2743019C/en not_active Expired - Fee Related
- 2009-11-03 UA UAA201105367A patent/UA100190C2/ru unknown
- 2009-11-03 ES ES09744896T patent/ES2391704T3/es active Active
- 2009-11-03 WO PCT/US2009/063020 patent/WO2010056563A1/en active Application Filing
- 2009-11-03 KR KR1020117010569A patent/KR101334460B1/ko not_active IP Right Cessation
- 2009-11-03 BR BRPI0921916A patent/BRPI0921916A2/pt not_active IP Right Cessation
- 2009-11-03 SI SI200930348T patent/SI2358710T1/sl unknown
- 2009-11-03 MX MX2011005000A patent/MX2011005000A/es active IP Right Grant
- 2009-11-03 PT PT09744896T patent/PT2358710E/pt unknown
- 2009-11-03 JP JP2011536383A patent/JP5432275B2/ja active Active
- 2009-11-03 EA EA201170680A patent/EA018947B1/ru not_active IP Right Cessation
- 2009-11-03 AU AU2009314324A patent/AU2009314324B2/en not_active Ceased
- 2009-11-03 EP EP09744896A patent/EP2358710B1/en active Active
- 2009-11-03 PL PL09744896T patent/PL2358710T3/pl unknown
-
2011
- 2011-03-24 IL IL211940A patent/IL211940A/en not_active IP Right Cessation
- 2011-04-06 ZA ZA2011/02549A patent/ZA201102549B/en unknown
- 2011-04-25 TN TN2011000207A patent/TN2011000207A1/fr unknown
- 2011-05-03 HN HN2011001247A patent/HN2011001247A/es unknown
- 2011-05-06 CR CR20110240A patent/CR20110240A/es unknown
- 2011-05-09 MA MA33822A patent/MA32776B1/fr unknown
- 2011-05-09 DO DO2011000129A patent/DOP2011000129A/es unknown
- 2011-05-11 EC EC2011011048A patent/ECSP11011048A/es unknown
- 2011-05-12 CO CO11058555A patent/CO6382114A2/es active IP Right Grant
- 2011-11-24 HK HK11112734.3A patent/HK1158203A1/xx not_active IP Right Cessation
-
2012
- 2012-09-17 HR HRP20120738AT patent/HRP20120738T1/hr unknown
- 2012-10-05 CY CY20121100928T patent/CY1113409T1/el unknown
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