AR039868A1 - Inhibidores selectivos de la enzima kalikreina plasmatica - Google Patents
Inhibidores selectivos de la enzima kalikreina plasmaticaInfo
- Publication number
- AR039868A1 AR039868A1 ARP030100772A ARP030100772A AR039868A1 AR 039868 A1 AR039868 A1 AR 039868A1 AR P030100772 A ARP030100772 A AR P030100772A AR P030100772 A ARP030100772 A AR P030100772A AR 039868 A1 AR039868 A1 AR 039868A1
- Authority
- AR
- Argentina
- Prior art keywords
- lower alkyl
- optionally substituted
- kalikreina
- plasmatic
- enzyme
- Prior art date
Links
- 102000004190 Enzymes Human genes 0.000 title 1
- 108090000790 Enzymes Proteins 0.000 title 1
- 229940124639 Selective inhibitor Drugs 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 13
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 abstract 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- -1 o-xylylene group Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/0606—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
-
- 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
-
- 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
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- 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
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- 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
- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Gastroenterology & Hepatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pyridine Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Compuestos de la fórmula general 1, o sales de los mismos aceptables para el uso farmacéutico, donde R1 se selecciona entre H, alquilo inferior, R4-CO, R4-O2CCH2, R5-OCO y R5-SO2; R2 se selecciona entre alquilo inferior, cicloalquilo opcionalmente sustituido con un grupo alquilo o alquiloxilo, (C5-12) cicloalquilalquilo opcionalmente sustituido con un grupo alquilo o alquiloxilo, aralquilo opcionalmente sustituido con hasta tres grupos seleccionados entre F, Cl, Br, I, OH, alquilo inferior y O-(alquilo inferior), O-bencilo, NH2, NO2, NH-acilo, CN y CF3, y aralquiloximetilo opcionalmente sustituido hasta tres grupos seleccionados entre F, Cl, Br, OH, alquilo inferior y O-(alquilo inferior); o R1 y R2 son juntos un grupo o-xilileno, opcionalmente sustituido en el anillo aromático con un grupo seleccionado entre F, Cl, Br, OH, alquilo inferior y O-(alquilo inferior); R3 se selecciona entre H, OH y O-alquilo inferior; R4 se selecciona entre H, alquilo inferior y fenilo; y R5 se selecciona entre alquilo inferior, fenilo y bencilo. Los compuestos son útiles como composiciones farmacéuticas.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0205527.5A GB0205527D0 (en) | 2002-03-08 | 2002-03-08 | Inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR039868A1 true AR039868A1 (es) | 2005-03-09 |
Family
ID=9932619
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030100772A AR039868A1 (es) | 2002-03-08 | 2003-03-06 | Inhibidores selectivos de la enzima kalikreina plasmatica |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US7649000B2 (es) |
| EP (1) | EP1483284B1 (es) |
| JP (1) | JP4330450B2 (es) |
| KR (1) | KR100974633B1 (es) |
| CN (1) | CN1274713C (es) |
| AR (1) | AR039868A1 (es) |
| AT (1) | ATE333463T1 (es) |
| AU (1) | AU2003208471B2 (es) |
| CA (1) | CA2478099C (es) |
| DE (1) | DE60306904T2 (es) |
| DK (1) | DK1483284T3 (es) |
| EG (1) | EG25482A (es) |
| ES (1) | ES2264523T3 (es) |
| GB (1) | GB0205527D0 (es) |
| HK (1) | HK1072265A1 (es) |
| IL (2) | IL163710A0 (es) |
| MX (1) | MXPA04008523A (es) |
| MY (1) | MY130830A (es) |
| NO (1) | NO332678B1 (es) |
| NZ (1) | NZ534891A (es) |
| PL (1) | PL209670B1 (es) |
| PT (1) | PT1483284E (es) |
| RU (1) | RU2301225C2 (es) |
| TW (1) | TWI283685B (es) |
| UY (1) | UY27699A1 (es) |
| WO (1) | WO2003076458A2 (es) |
| ZA (1) | ZA200406856B (es) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005095327A1 (ja) | 2004-03-31 | 2005-10-13 | Ajinomoto Co., Inc. | アニリン誘導体 |
| AU2008289005A1 (en) * | 2007-08-21 | 2009-02-26 | Genzyme Corporation | Treatment with kallikrein inhibitors |
| GB0918924D0 (en) * | 2009-10-28 | 2009-12-16 | Vantia Ltd | Azaindole derivatives |
| US9290485B2 (en) | 2010-08-04 | 2016-03-22 | Novartis Ag | N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides |
| GB2494851A (en) | 2011-07-07 | 2013-03-27 | Kalvista Pharmaceuticals Ltd | Plasma kallikrein inhibitors |
| WO2013111108A1 (en) | 2012-01-27 | 2013-08-01 | Novartis Ag | 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
| EP2807156A1 (en) | 2012-01-27 | 2014-12-03 | Novartis AG | Aminopyridine derivatives as plasma kallikrein inhibitors |
| GB201212081D0 (en) | 2012-07-06 | 2012-08-22 | Kalvista Pharmaceuticals Ltd | New polymorph |
| IL239682B (en) | 2013-01-08 | 2018-10-31 | Kalvista Pharmaceuticals Ltd | History of benzylamine and 2-(aminomethyl)pyridine |
| GB201300304D0 (en) | 2013-01-08 | 2013-02-20 | Kalvista Pharmaceuticals Ltd | Benzylamine derivatives |
| GB2510407A (en) | 2013-02-04 | 2014-08-06 | Kalvista Pharmaceuticals Ltd | Aqueous suspensions of kallikrein inhibitors for parenteral administration |
| CA2912285C (en) | 2013-05-23 | 2021-07-13 | Kalvista Pharmaceuticals Limited | Fused 6,5 or 6,6-heteroaromatic bicyclic amide derivatives and pharmaceutical compositions thereof useful as plasma kallikrein inhibitor |
| GB2517908A (en) * | 2013-08-14 | 2015-03-11 | Kalvista Pharmaceuticals Ltd | Bicyclic inhibitors |
| TWI636047B (zh) | 2013-08-14 | 2018-09-21 | 英商卡爾維斯塔製藥有限公司 | 雜環衍生物 |
| CA2920815C (en) | 2013-08-14 | 2021-09-21 | Kalvista Pharmaceuticals Limited | Inhibitors of plasma kallikrein |
| EP3062823B1 (en) * | 2013-10-28 | 2018-12-12 | BicycleRD Limited | Novel polypeptides |
| ES2945905T3 (es) | 2014-02-07 | 2023-07-10 | Exithera Pharmaceuticals Inc | Compuestos y composiciones terapéuticos |
| GB201421088D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | New enzyme inhibitors |
| GB201421083D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | Enzyme inhibitors |
| GB201421085D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | New enzyme inhibitors |
| US11180484B2 (en) | 2016-05-31 | 2021-11-23 | Kalvista Pharmaceuticals Limited | Pyrazole derivatives as plasma kallikrein inhibitors |
| GB201609603D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide |
| GB201609607D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts |
| SI3716952T1 (sl) | 2017-11-29 | 2022-04-29 | Kalvista Pharmaceuticals Limited | Farmacevtske oblike, ki obsegajo zaviralec plazemskega kalikreina |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
| BR112021008462A2 (pt) | 2018-10-30 | 2021-08-03 | Exithera Pharmaceuticals, Inc. | compostos e composições terapêuticas |
| GB201910116D0 (en) | 2019-07-15 | 2019-08-28 | Kalvista Pharmaceuticals Ltd | Treatments of hereditary angioedema |
| GB201910125D0 (en) | 2019-07-15 | 2019-08-28 | Kalvista Pharmaceuticals Ltd | Treatments of angioedema |
| EP4010333A1 (en) | 2019-08-09 | 2022-06-15 | Kalvista Pharmaceuticals Limited | Plasma kallikrein inhibitors |
| GB201918994D0 (en) | 2019-12-20 | 2020-02-05 | Kalvista Pharmaceuticals Ltd | Treatments of diabetic macular edema and impaired visual acuity |
| GB2591730A (en) | 2019-12-09 | 2021-08-11 | Kalvista Pharmaceuticals Ltd | New polymorphs |
| WO2021198534A1 (en) | 2020-04-04 | 2021-10-07 | Oxurion NV | Plasma kallikrein inhibitors for use in the treatment of coronaviral disease |
| WO2022079446A1 (en) | 2020-10-15 | 2022-04-21 | Kalvista Pharmaceuticals Limited | Treatments of angioedema |
| WO2022084693A1 (en) | 2020-10-23 | 2022-04-28 | Kalvista Pharmaceuticals Limited | Treatments of angioedema |
| WO2022172006A1 (en) | 2021-02-09 | 2022-08-18 | Kalvista Pharmaceuticals Limited | Treatments of hereditary angioedema |
| WO2023002219A1 (en) | 2021-07-23 | 2023-01-26 | Kalvista Pharmaceuticals Limited | Treatments of hereditary angioedema |
| WO2023144030A1 (en) | 2022-01-31 | 2023-08-03 | Oxurion NV | Plasma kallikrein inhibitor therapy for anti-vegf sensitization |
| WO2023148016A1 (en) | 2022-02-04 | 2023-08-10 | Oxurion NV | Biomarker for plasma kallikrein inhibitor therapy response |
| LT4288036T (lt) | 2022-04-27 | 2024-09-25 | Kalvista Pharmaceuticals Limited | Farmacinės plazmos kalikreino inhibitoriaus formos |
| WO2024180100A1 (en) | 2023-02-27 | 2024-09-06 | Kalvista Pharmaceuticals Limited | New solid form of a plasma kallikrein inhibitor |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9019558D0 (en) * | 1990-09-07 | 1990-10-24 | Szelke Michael | Enzyme inhibitors |
| WO1993008211A1 (en) * | 1991-10-23 | 1993-04-29 | The Procter & Gamble Company | Tripeptide derivative anti-inflammatory agents |
| SE9301911D0 (sv) * | 1993-06-03 | 1993-06-03 | Ab Astra | New peptide derivatives |
| GB9318637D0 (en) * | 1993-09-08 | 1993-10-27 | Ferring Res Ltd | Enzyme inhibitors |
-
2002
- 2002-03-08 GB GBGB0205527.5A patent/GB0205527D0/en not_active Ceased
-
2003
- 2003-02-26 TW TW092104061A patent/TWI283685B/zh not_active IP Right Cessation
- 2003-03-03 EG EG2003030209A patent/EG25482A/xx active
- 2003-03-04 AT AT03706759T patent/ATE333463T1/de active
- 2003-03-04 PT PT03706759T patent/PT1483284E/pt unknown
- 2003-03-04 RU RU2004126610/04A patent/RU2301225C2/ru not_active IP Right Cessation
- 2003-03-04 NZ NZ534891A patent/NZ534891A/xx not_active IP Right Cessation
- 2003-03-04 AU AU2003208471A patent/AU2003208471B2/en not_active Ceased
- 2003-03-04 DE DE60306904T patent/DE60306904T2/de not_active Expired - Lifetime
- 2003-03-04 PL PL372977A patent/PL209670B1/pl unknown
- 2003-03-04 WO PCT/GB2003/000908 patent/WO2003076458A2/en active IP Right Grant
- 2003-03-04 DK DK03706759T patent/DK1483284T3/da active
- 2003-03-04 US US10/506,535 patent/US7649000B2/en active Active
- 2003-03-04 CA CA2478099A patent/CA2478099C/en not_active Expired - Lifetime
- 2003-03-04 JP JP2003574673A patent/JP4330450B2/ja not_active Expired - Fee Related
- 2003-03-04 IL IL16371003A patent/IL163710A0/xx unknown
- 2003-03-04 CN CNB038054019A patent/CN1274713C/zh not_active Expired - Fee Related
- 2003-03-04 EP EP03706759A patent/EP1483284B1/en not_active Expired - Lifetime
- 2003-03-04 KR KR1020047013816A patent/KR100974633B1/ko not_active IP Right Cessation
- 2003-03-04 MX MXPA04008523A patent/MXPA04008523A/es active IP Right Grant
- 2003-03-04 ES ES03706759T patent/ES2264523T3/es not_active Expired - Lifetime
- 2003-03-06 UY UY27699A patent/UY27699A1/es not_active Application Discontinuation
- 2003-03-06 AR ARP030100772A patent/AR039868A1/es active IP Right Grant
- 2003-03-07 MY MYPI20030803A patent/MY130830A/en unknown
-
2004
- 2004-08-24 IL IL163710A patent/IL163710A/en active IP Right Grant
- 2004-08-27 ZA ZA200406856A patent/ZA200406856B/en unknown
- 2004-09-03 NO NO20043695A patent/NO332678B1/no not_active IP Right Cessation
-
2005
- 2005-05-24 HK HK05104336A patent/HK1072265A1/xx not_active IP Right Cessation
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