AR031512A1 - Formas de sal de amida de acido 3-(4-bromo-2,6-difluoro-benciloxi)-5-[3-(4-pirrolidin-1-ilbutil)ureido]isotiazol-4-carboxilico y metodo de produccion - Google Patents
Formas de sal de amida de acido 3-(4-bromo-2,6-difluoro-benciloxi)-5-[3-(4-pirrolidin-1-ilbutil)ureido]isotiazol-4-carboxilico y metodo de produccionInfo
- Publication number
- AR031512A1 AR031512A1 ARP010105484A ARP010105484A AR031512A1 AR 031512 A1 AR031512 A1 AR 031512A1 AR P010105484 A ARP010105484 A AR P010105484A AR P010105484 A ARP010105484 A AR P010105484A AR 031512 A1 AR031512 A1 AR 031512A1
- Authority
- AR
- Argentina
- Prior art keywords
- forms
- ureido
- bromo
- ilbutil
- isotiazol
- Prior art date
Links
- 150000003839 salts Chemical class 0.000 title abstract 3
- 241000670727 Amida Species 0.000 title 1
- 239000002253 acid Substances 0.000 title 1
- 238000004519 manufacturing process Methods 0.000 title 1
- -1 hemicitrate Chemical compound 0.000 abstract 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 abstract 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 abstract 2
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 abstract 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-L L-tartrate(2-) Chemical compound [O-]C(=O)[C@H](O)[C@@H](O)C([O-])=O FEWJPZIEWOKRBE-JCYAYHJZSA-L 0.000 abstract 2
- PJXPORIRXYJDLD-UHFFFAOYSA-N 3-[(4-bromo-2,6-difluorophenyl)methoxy]-5-(4-pyrrolidin-1-ylbutylcarbamoylamino)-1,2-thiazole-4-carboxylic acid Chemical compound S1N=C(OCC=2C(=CC(Br)=CC=2F)F)C(C(=O)O)=C1NC(=O)NCCCCN1CCCC1 PJXPORIRXYJDLD-UHFFFAOYSA-N 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical class CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000003463 hyperproliferative effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
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
- C07D275/02—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings
- C07D275/03—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- 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
- 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
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Vascular Medicine (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La presente se refiere a las formas de sal hidrocloruro, hidrobromuro, hemicitrato, acetato, p-tosilato, L-tartrato, hemisuccinato y mesilato de amida de ácido 3-(4-bromo-2,6-difluorobenciloxi)-5-[3-(4-pirrolidin-1-ilbutil)ureído]isotiazol-4-carboxílico que tienen la formula (1). La presente también se refiere a composiciones farmacéuticas que contienen las sales hidrocloruro, hidrobromuro, hemicitrato, acetato, p-tosilato, L-tartrato, hemisuccinato y mesilato de formula (1). La presente se refiere además a métodos para tratar enfermedades hiperproliferativas, tales como cánceres en mamíferos, especialmente seres humanos, por administracion de las sales anteriores, y a los métodos para preparar las formas cristalinas de las sales anteriores.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25351300P | 2000-11-28 | 2000-11-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR031512A1 true AR031512A1 (es) | 2003-09-24 |
Family
ID=22960587
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010105484A AR031512A1 (es) | 2000-11-28 | 2001-11-26 | Formas de sal de amida de acido 3-(4-bromo-2,6-difluoro-benciloxi)-5-[3-(4-pirrolidin-1-ilbutil)ureido]isotiazol-4-carboxilico y metodo de produccion |
Country Status (49)
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA60365C2 (uk) * | 1998-06-04 | 2003-10-15 | Пфайзер Продактс Інк. | Похідні ізотіазолу, спосіб їх одержання, фармацевтична композиція та спосіб лікування гіперпроліферативного захворювання у ссавця |
| ME00275B (me) | 1999-01-13 | 2011-02-10 | Bayer Corp | ω-KARBOKSIARIL SUPSTITUISANI DIFENIL KARBAMIDI KAO INHIBITORI RAF KINAZE |
| JP2002534468A (ja) | 1999-01-13 | 2002-10-15 | バイエル コーポレイション | p38キナーゼ阻害剤としてのω−カルボキシアリール置換ジフェニル尿素 |
| US8124630B2 (en) | 1999-01-13 | 2012-02-28 | Bayer Healthcare Llc | ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
| PT1478358E (pt) | 2002-02-11 | 2013-09-11 | Bayer Healthcare Llc | Tosilato de sorafenib para o tratamento de doenças caracterizadas por angiogénese anormal |
| US20030216396A1 (en) | 2002-02-11 | 2003-11-20 | Bayer Corporation | Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors |
| CA2493701A1 (en) * | 2002-07-25 | 2004-02-05 | Pfizer Products Inc. | Isothiazole derivatives useful as anticancer agents |
| BR0313593A (pt) * | 2002-08-19 | 2005-07-12 | Pfizer Prod Inc | Terapia de combinação para doenças hiperproliferativas |
| DK1636585T3 (da) | 2003-05-20 | 2008-05-26 | Bayer Pharmaceuticals Corp | Diarylurinstoffer med kinasehæmmende aktivitet |
| PT1663978E (pt) | 2003-07-23 | 2008-02-15 | Bayer Pharmaceuticals Corp | Omega-carboxiaril difenil ureia substituída por flúor para o tratamento e a prevenção de doenças e estados patológicos |
| CA2543201C (en) * | 2003-10-27 | 2010-12-21 | Merck & Co., Inc. | ((ir, 3s)-3-isopropyl-3-{ [3-(trifluoromethyl)-7, 8-dihydro-1, 6-naphthyridin-6 (5h)-yl] carbonyl} cyclopentyl) [(3s, 4s)-3-methoxytetrahydro-2h-pyran-4-yl] amine succinate salt, composition thereof, and its use in the treatment of inflammatory diseases |
| EP1694686A1 (en) | 2003-12-19 | 2006-08-30 | Takeda San Diego, Inc. | Kinase inhibitors |
| WO2005102327A1 (en) * | 2004-04-20 | 2005-11-03 | Pfizer Products Inc. | Dosage forms and methods of treatment using vegfr inhibitors |
| MXPA06012394A (es) | 2004-04-30 | 2007-01-31 | Bayer Pharmaceuticals Corp | Derivados de pirazolilurea sustituidos utiles en el tratamiento de cancer. |
| TW200538104A (en) * | 2004-05-17 | 2005-12-01 | Pfizer Prod Inc | Phenyl derivatives for the treatment of abnormal cell growth |
| EP1778669A2 (en) | 2004-08-18 | 2007-05-02 | Takeda San Diego, Inc. | Kinase inhibitors |
| DE602005023333D1 (de) | 2004-10-15 | 2010-10-14 | Takeda Pharmaceutical | Kinaseinhibitoren |
| US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| ZA200810017B (en) | 2006-06-16 | 2010-04-28 | Lundbeck & Co As H | 1- [2- (2, 4-Dimethylphenylsulfanyl) -phenyl] piperazine as a compound with combined serotonin Reuptake, 5-HT3 and 5-HT1A activity for the treatment of cognitive impairment |
| US7932390B2 (en) | 2006-06-29 | 2011-04-26 | Hoffman-La Roche Inc. | Substituted thieno[3,2-C]pyridine carboxylic acid derivatives |
| EA200970361A1 (ru) | 2006-10-09 | 2010-02-26 | Такеда Фармасьютикал Компани Лимитед | Ингибиторы киназы |
| MX2010001636A (es) | 2007-08-14 | 2010-03-15 | Hoffmann La Roche | Derivados de pirazolo[3,4-d]-pirimidina como agentes antiproliferativos. |
| WO2011073521A1 (en) | 2009-12-15 | 2011-06-23 | Petri Salven | Methods for enriching adult-derived endothelial progenitor cells and uses thereof |
| SG187592A1 (en) | 2010-07-23 | 2013-03-28 | Univ Boston | Anti-despr inhibitors as therapeutics for inhibition of pathological angiogenesis and tumor cell invasiveness and for molecular imaging and targeted delivery |
| TR201901462T4 (tr) | 2013-03-14 | 2019-02-21 | Panoptica Inc | Gözün posterior segmentine ilaç uygulanması için oküler formülasyonlar. |
| AU2015317531B2 (en) * | 2014-09-17 | 2020-11-19 | Panoptica, Inc. | Ocular formulations for drug-delivery and protection of the anterior segment of the eye |
| AU2023416218A1 (en) * | 2022-12-28 | 2025-07-10 | Beyang Therapeutics Co., Ltd. | Protein tyrosine kinase inhibitor and medical use thereof |
| WO2026002142A1 (zh) * | 2024-06-27 | 2026-01-02 | 苏州必扬医药科技有限公司 | 一种蛋白酪氨酸激酶抑制剂的半琥珀酸盐晶型 |
| WO2026002133A1 (zh) * | 2024-06-27 | 2026-01-02 | 苏州必扬医药科技有限公司 | 一种蛋白酪氨酸激酶抑制剂的盐型 |
| WO2026002126A1 (zh) * | 2024-06-27 | 2026-01-02 | 苏州必扬医药科技有限公司 | 一种蛋白酪氨酸激酶抑制剂及其眼用制剂 |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA60365C2 (uk) * | 1998-06-04 | 2003-10-15 | Пфайзер Продактс Інк. | Похідні ізотіазолу, спосіб їх одержання, фармацевтична композиція та спосіб лікування гіперпроліферативного захворювання у ссавця |
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2001
- 2001-11-19 ES ES01982663T patent/ES2271086T3/es not_active Expired - Lifetime
- 2001-11-19 UA UA2003054858A patent/UA74221C2/uk unknown
- 2001-11-19 BR BR0115621-7A patent/BR0115621A/pt not_active Application Discontinuation
- 2001-11-19 AU AU2002214204A patent/AU2002214204B2/en not_active Ceased
- 2001-11-19 IL IL15537101A patent/IL155371A0/xx unknown
- 2001-11-19 HU HU0302553A patent/HUP0302553A3/hu unknown
- 2001-11-19 EE EEP200300247A patent/EE200300247A/xx unknown
- 2001-11-19 KR KR1020057022534A patent/KR20050116401A/ko not_active Abandoned
- 2001-11-19 CA CA002430065A patent/CA2430065C/en not_active Expired - Lifetime
- 2001-11-19 WO PCT/IB2001/002193 patent/WO2002044158A1/en not_active Ceased
- 2001-11-19 YU YU36403A patent/YU36403A/sh unknown
- 2001-11-19 EA EA200300424A patent/EA005859B1/ru not_active IP Right Cessation
- 2001-11-19 MX MXPA03004714A patent/MXPA03004714A/es active IP Right Grant
- 2001-11-19 DE DE60123461T patent/DE60123461T2/de not_active Expired - Lifetime
- 2001-11-19 DK DK01982663T patent/DK1337521T3/da active
- 2001-11-19 PT PT01982663T patent/PT1337521E/pt unknown
- 2001-11-19 NZ NZ525788A patent/NZ525788A/en unknown
- 2001-11-19 EP EP01982663A patent/EP1337521B1/en not_active Expired - Lifetime
- 2001-11-19 CN CNB018193285A patent/CN1231474C/zh not_active Expired - Fee Related
- 2001-11-19 SK SK586-2003A patent/SK5862003A3/sk unknown
- 2001-11-19 SI SI200130630T patent/SI1337521T1/sl unknown
- 2001-11-19 DO DO2001000288A patent/DOP2001000288A/es unknown
- 2001-11-19 AU AU1420402A patent/AU1420402A/xx active Pending
- 2001-11-19 AT AT01982663T patent/ATE340786T1/de not_active IP Right Cessation
- 2001-11-19 JP JP2002546528A patent/JP2004514714A/ja not_active Withdrawn
- 2001-11-19 AP APAP/P/2001/002358A patent/AP2001002358A0/en unknown
- 2001-11-19 OA OA1200300137A patent/OA12532A/en unknown
- 2001-11-19 HR HR20030408A patent/HRP20030408A2/hr not_active Application Discontinuation
- 2001-11-19 PL PL01362079A patent/PL362079A1/xx not_active Application Discontinuation
- 2001-11-19 KR KR10-2003-7007057A patent/KR20030059275A/ko not_active Ceased
- 2001-11-19 CZ CZ20031315A patent/CZ20031315A3/cs unknown
- 2001-11-19 GE GE5216A patent/GEP20053652B/en unknown
- 2001-11-26 AR ARP010105484A patent/AR031512A1/es not_active Application Discontinuation
- 2001-11-26 MY MYPI20015382A patent/MY136686A/en unknown
- 2001-11-26 PE PE2001001179A patent/PE20020591A1/es not_active Application Discontinuation
- 2001-11-26 UY UY27039A patent/UY27039A1/es not_active Application Discontinuation
- 2001-11-27 TW TW090129315A patent/TWI287542B/zh active
- 2001-11-27 US US09/993,640 patent/US6831091B2/en not_active Expired - Lifetime
- 2001-11-27 GT GT200100237A patent/GT200100237A/es unknown
- 2001-11-27 TN TNTNSN01167A patent/TNSN01167A1/fr unknown
- 2001-11-27 HN HN2001000268A patent/HN2001000268A/es unknown
- 2001-11-27 SV SV2001000748A patent/SV2002000748A/es unknown
- 2001-11-27 PA PA20018533801A patent/PA8533801A1/es unknown
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2003
- 2003-04-14 IS IS6788A patent/IS6788A/is unknown
- 2003-04-22 BG BG107752A patent/BG107752A/bg unknown
- 2003-04-24 CR CR6963A patent/CR6963A/es not_active Application Discontinuation
- 2003-04-30 ZA ZA200303341A patent/ZA200303341B/en unknown
- 2003-05-13 MA MA27158A patent/MA26960A1/fr unknown
- 2003-05-27 NO NO20032388A patent/NO325187B1/no unknown
- 2003-05-28 EC EC2003004628A patent/ECSP034628A/es unknown
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2006
- 2006-11-13 CY CY20061101645T patent/CY1106240T1/el unknown
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2007
- 2007-10-29 JP JP2007279951A patent/JP4971946B2/ja not_active Expired - Lifetime
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