PE20050325A1 - DERIVADOS DE PIRROLO[3,4-c]PIRAZOL ACTIVOS COMO INHIBIDORES DE QUINASA, PROCESO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS COMPRENDEN - Google Patents
DERIVADOS DE PIRROLO[3,4-c]PIRAZOL ACTIVOS COMO INHIBIDORES DE QUINASA, PROCESO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS COMPRENDENInfo
- Publication number
- PE20050325A1 PE20050325A1 PE2004000657A PE2004000657A PE20050325A1 PE 20050325 A1 PE20050325 A1 PE 20050325A1 PE 2004000657 A PE2004000657 A PE 2004000657A PE 2004000657 A PE2004000657 A PE 2004000657A PE 20050325 A1 PE20050325 A1 PE 20050325A1
- Authority
- PE
- Peru
- Prior art keywords
- pirazole
- pirrolo
- derivatives
- phenylethanoyl
- tetrahydropyrrolo
- Prior art date
Links
Classifications
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- 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
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- 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
- A61P25/28—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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- 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
- 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
- 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)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Urology & Nephrology (AREA)
- Neurology (AREA)
- Vascular Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Cardiology (AREA)
- Transplantation (AREA)
- Communicable Diseases (AREA)
- Hospice & Palliative Care (AREA)
- Virology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Oncology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
SE REFIERE A DERIVADOS DEL COMPUESTO PIRROLO[3,4-c]PIRAZOL DE FORMULA I, EN DONDE R ES H o METILO; R1 ES HIDROXI, ALQUILO o ALCOXI C1-C3 DE CADENA RECTA O RAMIFICADA; R2 ES H o HALOGENO; X ES UN GRUPO DIVALENTE SELECCIONADO DE METILENO (-CH2-), FLUOROMETILENO (-CHF-), UN HETEROATOMO SELECCIONADO DE OXIGENO (-O-), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-{5-[(2R)-2-METOXI-2-FENILETANOIL]-1,4,5,6-TETRAHIDROPIRROLO[3,4-c]PIRAZOL-3-IL}-4-(4-METILPIPERAZIN-1-IL)BENZAMIDA; N-{5-[(2R)-2-METOXI-2-FENILETANOIL]-1,4,5,6-TETRAHIDROPIRROLO[3,4-c]PIRAZOL-3-IL}-4-(4-ETILPIPERAZIN-1-IL)BENZAMIDA; N-{5-[(2R)-2-METOXI-2-FENILETANOIL]-1,4,5,6-TETRAHIDROPIRROLO[3,4-c]PIRAZOL-3-IL}-4-(4-ISOPROPILPIPERAZIN-1-IL)BENZAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCESO PARA PREPARAR DICHOS COMPUESTOS Y UNA COMPOSICION FARMACEUTICA. ADEMAS SE REFIERE A UN METODO PARA TRATAR TRASTORNOS PROLIFERATIVOS CELULARES OCASIONADOS POR UNA ACTIVIDAD DE PROTEINQUINASA ALTERADA Y/O ASOCIADOS CON LA MISMA
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US48581403P | 2003-07-09 | 2003-07-09 |
Publications (1)
Publication Number | Publication Date |
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PE20050325A1 true PE20050325A1 (es) | 2005-05-17 |
Family
ID=34062099
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2004000657A PE20050325A1 (es) | 2003-07-09 | 2004-07-08 | DERIVADOS DE PIRROLO[3,4-c]PIRAZOL ACTIVOS COMO INHIBIDORES DE QUINASA, PROCESO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS COMPRENDEN |
Country Status (42)
Families Citing this family (31)
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US7541354B2 (en) * | 2000-08-10 | 2009-06-02 | Pfizer Italia S.R.L. | Bicyclo-pyrazoles |
WO2005030776A1 (en) * | 2003-09-23 | 2005-04-07 | Vertex Pharmaceuticals Incorporated | Pyrazolopyrrole derivatives as protein kinase inhibitors |
EP1694686A1 (en) * | 2003-12-19 | 2006-08-30 | Takeda San Diego, Inc. | Kinase inhibitors |
JP2007533753A (ja) * | 2004-04-23 | 2007-11-22 | タケダ サン ディエゴ インコーポレイテッド | インドール誘導体及びキナーゼ阻害剤としてのその使用 |
EP1778669A2 (en) * | 2004-08-18 | 2007-05-02 | Takeda San Diego, Inc. | Kinase inhibitors |
WO2006044687A2 (en) * | 2004-10-15 | 2006-04-27 | Takeda San Diego, Inc. | Kinase inhibitors |
EA011815B1 (ru) | 2005-01-10 | 2009-06-30 | Пфайзер Инк. | Пирролопиразолы в качестве сильнодействующих ингибиторов киназы |
US8119655B2 (en) * | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
TW200808311A (en) * | 2006-03-30 | 2008-02-16 | Nerviano Medical Sciences Srl | Use of a kinase inhibitor for the treatment of particular resistant tumors |
WO2008017465A1 (en) * | 2006-08-10 | 2008-02-14 | F. Hoffmann-La Roche Ag | Bicyclic lactam derivatives, their manufacture and use as pharmaceutical agents |
EP2223925A1 (en) * | 2006-10-09 | 2010-09-01 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
SG158147A1 (en) | 2006-10-09 | 2010-01-29 | Takeda Pharmaceutical | Kinase inhibitors |
DE602007008949D1 (de) * | 2006-11-03 | 2010-10-14 | Nerviano Medical Sciences Srl | Verfahren zur verabreichung einer antitumoralen verbindung |
AR071780A1 (es) * | 2008-05-15 | 2010-07-14 | Nerviano Medical Sciences Srl | Derivados de carbamoilo de carbonilamino-pirazoles biciclicos como profarmacos |
JP5518062B2 (ja) * | 2008-07-24 | 2014-06-11 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | オーロラキナーゼ阻害剤および抗悪性腫瘍剤を含む治療用組み合わせ |
CN102105148B (zh) * | 2008-07-24 | 2013-04-10 | 内尔维阿诺医学科学有限公司 | 包含aurora激酶抑制剂和抗肿瘤药的治疗组合 |
US20100022553A1 (en) * | 2008-07-24 | 2010-01-28 | Nerviano Medical Sciences S.R.L. | Therapeutic Combination Comprising an Aurora Kinase Inhibitor and Imatinib |
WO2010074724A1 (en) | 2008-12-22 | 2010-07-01 | Millennium Pharmaceuticals, Inc. | Combination of aurora kinase inhibitors and anti-cd20 antibodies |
WO2013088257A1 (en) | 2011-12-12 | 2013-06-20 | Dr. Reddy's Laboratories Ltd. | Substituted heterocyclic compounds as tropomyosin receptor kinase a (trka) inhibitors |
CN104072498B (zh) * | 2013-03-26 | 2016-12-28 | 沈阳药科大学 | (R)‑N‑[5‑(2‑甲氧基‑2‑苯基乙酰基)‑1,4,5,6‑四氢吡咯并[3,4‑c]吡唑‑3‑基]‑4‑(4‑甲基哌嗪‑1‑基)苯甲酰胺的合成方法 |
US10335494B2 (en) | 2013-12-06 | 2019-07-02 | Millennium Pharmaceuticals, Inc. | Combination of aurora kinase inhibitors and anti-CD30 antibodies |
US9394305B2 (en) | 2014-06-23 | 2016-07-19 | Dr. Reddy's Laboratories Ltd. | Substituted imidazo[1,2-a]pyridine compounds as tropomyosin receptor kinase a (TrkA) inhibitors |
JP6787314B2 (ja) | 2015-06-15 | 2020-11-18 | 宇部興産株式会社 | 置換ジヒドロピロロピラゾール誘導体 |
WO2017015316A1 (en) | 2015-07-21 | 2017-01-26 | Millennium Pharmaceuticals, Inc. | Administration of aurora kinase inhibitor and chemotherapeutic agents |
CN107337674B (zh) * | 2016-04-29 | 2019-09-20 | 江苏吉贝尔药业股份有限公司 | 用于dpp-iv抑制剂的四氢吡喃胺衍生物、其药物组合物和制剂以及用途 |
US11874276B2 (en) | 2018-04-05 | 2024-01-16 | Dana-Farber Cancer Institute, Inc. | STING levels as a biomarker for cancer immunotherapy |
WO2021041532A1 (en) | 2019-08-26 | 2021-03-04 | Dana-Farber Cancer Institute, Inc. | Use of heparin to promote type 1 interferon signaling |
CN113563346A (zh) * | 2021-08-19 | 2021-10-29 | 守恒(厦门)医疗科技有限公司 | 吡咯[3,4-c]并吡唑二酰胺类衍生物及其在抗肿瘤药物中的应用 |
WO2023196959A1 (en) | 2022-04-07 | 2023-10-12 | Eli Lilly And Company | Process for making a kras g12c inhibitor |
WO2023196887A1 (en) | 2022-04-08 | 2023-10-12 | Eli Lilly And Company | Method of treatment including kras g12c inhibitors and aurora a inhibitors |
US20240108618A1 (en) | 2022-06-30 | 2024-04-04 | Eli Lilly And Company | Kras g12c inhibitor dosing regimens |
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FR2717380B1 (fr) * | 1994-03-15 | 1996-04-26 | Oreal | Compositions cosmétiques contenant un mélange synergétique de polymères conditionneurs. |
GB9911053D0 (en) | 1999-05-12 | 1999-07-14 | Pharmacia & Upjohn Spa | 4,5,6,7-tetrahydroindazole derivatives process for their preparation and their use as antitumour agents |
DE19932144A1 (de) * | 1999-07-09 | 2001-01-11 | Basf Ag | Mikrokapselzubereitungen und Mikrokapseln enthaltende Wasch- und Reinigungsmittel |
US6387900B1 (en) | 1999-08-12 | 2002-05-14 | Pharmacia & Upjohn S.P.A. | 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents |
PL353455A1 (en) | 1999-08-12 | 2003-11-17 | Pharmacia Italia S.P.A. | 3(5)-amino-pyrazole derivatives, process for their preparation and their use as antitumor agents |
US7541354B2 (en) | 2000-08-10 | 2009-06-02 | Pfizer Italia S.R.L. | Bicyclo-pyrazoles |
FR2815032B1 (fr) | 2000-10-10 | 2003-08-08 | Pf Medicament | Nouveaux derives d'aminophenyle piperazine ou d'amino phenyle piperide inhibiteurs de proteines prenyl transferase ainsi que leurs preparations |
MXPA03004644A (es) | 2000-11-27 | 2003-09-05 | Pharmacia Italia Spa | Derivados de fenilacetamdia-pirazol y su uso como agentes antitumorales. |
JP2004519486A (ja) | 2001-01-26 | 2004-07-02 | フアルマシア・イタリア・エツセ・ピー・アー | クロマン誘導体、その製造方法及びその抗腫瘍剤としての使用 |
JP4542338B2 (ja) | 2001-09-26 | 2010-09-15 | ファイザー イタリア ソシエタ ア レスポンサビリタ リミタータ | キナーゼ阻害因子として活性なアミノインダゾール誘導体、それらの製造方法及びそれらを含有する医薬組成物 |
MXPA05000947A (es) | 2002-07-25 | 2005-05-16 | Pharmacia Italia Spa | Biciclo-pirazoles activos como inhibidores de cinasa, procedimiento para su preparacion y composiciones farmaceuticas que los contienen. |
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2004
- 2004-07-01 US US10/882,493 patent/US7141568B2/en active Active
- 2004-07-08 SI SI200431502T patent/SI1644376T1/sl unknown
- 2004-07-08 PL PL04763132T patent/PL1644376T3/pl unknown
- 2004-07-08 GE GEAP20049209A patent/GEP20084395B/en unknown
- 2004-07-08 TW TW093120474A patent/TWI343382B/zh not_active IP Right Cessation
- 2004-07-08 BR BRPI0411868A patent/BRPI0411868B8/pt not_active IP Right Cessation
- 2004-07-08 AT AT04763132T patent/ATE480540T1/de active
- 2004-07-08 RS YUP-2006/0004A patent/RS20060004A/sr unknown
- 2004-07-08 DE DE602004029045T patent/DE602004029045D1/de not_active Expired - Lifetime
- 2004-07-08 RS RS20060004A patent/RS52155B/en unknown
- 2004-07-08 AP AP2006003480A patent/AP2214A/xx active
- 2004-07-08 WO PCT/EP2004/007515 patent/WO2005005427A1/en active Search and Examination
- 2004-07-08 AU AU2004255347A patent/AU2004255347B2/en not_active Ceased
- 2004-07-08 KR KR1020067000310A patent/KR101075711B1/ko active IP Right Grant
- 2004-07-08 ME MEP-519/08A patent/MEP51908A/xx unknown
- 2004-07-08 EP EP04763132A patent/EP1644376B1/en not_active Expired - Lifetime
- 2004-07-08 CN CNB2004800195930A patent/CN100564380C/zh not_active Expired - Fee Related
- 2004-07-08 ES ES04763132T patent/ES2349780T3/es not_active Expired - Lifetime
- 2004-07-08 PT PT04763132T patent/PT1644376E/pt unknown
- 2004-07-08 NZ NZ544514A patent/NZ544514A/xx not_active IP Right Cessation
- 2004-07-08 MX MXPA06000362A patent/MXPA06000362A/es active IP Right Grant
- 2004-07-08 DK DK04763132.0T patent/DK1644376T3/da active
- 2004-07-08 CA CA2531759A patent/CA2531759C/en not_active Expired - Fee Related
- 2004-07-08 EA EA200600209A patent/EA009462B1/ru not_active IP Right Cessation
- 2004-07-08 JP JP2006518148A patent/JP4728232B2/ja not_active Expired - Fee Related
- 2004-07-08 PE PE2004000657A patent/PE20050325A1/es not_active Application Discontinuation
- 2004-07-09 DO DO2004000949A patent/DOP2004000949A/es unknown
- 2004-07-09 GT GT200400133A patent/GT200400133A/es unknown
- 2004-07-09 PA PA20048606201A patent/PA8606201A1/es unknown
- 2004-07-09 MY MYPI20042753A patent/MY139072A/en unknown
- 2004-07-09 GT GT200400133AK patent/GT200400133AA/es unknown
- 2004-07-09 HN HN2004000232A patent/HN2004000232A/es unknown
- 2004-07-12 AR ARP040102447A patent/AR050045A1/es active IP Right Grant
- 2004-08-07 UA UAA200601248A patent/UA81682C2/ru unknown
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2005
- 2005-12-22 IS IS8192A patent/IS2843B/is unknown
- 2005-12-22 EC EC2005006246A patent/ECSP056246A/es unknown
- 2005-12-29 IL IL172923A patent/IL172923A/en active IP Right Grant
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2006
- 2006-01-03 ZA ZA200600095A patent/ZA200600095B/en unknown
- 2006-01-05 CR CR8171A patent/CR8171A/es unknown
- 2006-01-06 NO NO20060113A patent/NO332361B1/no not_active IP Right Cessation
- 2006-01-09 TN TNP2006000009A patent/TNSN06009A1/fr unknown
- 2006-01-09 MA MA28721A patent/MA28064A1/fr unknown
- 2006-08-11 US US11/503,256 patent/US7582628B2/en not_active Expired - Lifetime
- 2006-09-15 HK HK06110252.6A patent/HK1089769A1/xx not_active IP Right Cessation
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2010
- 2010-10-18 CY CY20101100924T patent/CY1110832T1/el unknown
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