BRPI0606905A2 - derivados de quinazolina tendo atividade inibitória de tirosina cinase e composição farmacêutica contendo-os - Google Patents
derivados de quinazolina tendo atividade inibitória de tirosina cinase e composição farmacêutica contendo-osInfo
- Publication number
- BRPI0606905A2 BRPI0606905A2 BRPI0606905-3A BRPI0606905A BRPI0606905A2 BR PI0606905 A2 BRPI0606905 A2 BR PI0606905A2 BR PI0606905 A BRPI0606905 A BR PI0606905A BR PI0606905 A2 BRPI0606905 A2 BR PI0606905A2
- Authority
- BR
- Brazil
- Prior art keywords
- optionally substituted
- hydrogen atom
- substituted alkyl
- tyrosine kinase
- pharmaceutical composition
- Prior art date
Links
- 230000002401 inhibitory effect Effects 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 title 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 title 1
- 125000002294 quinazolinyl group Chemical class N1=C(N=CC2=CC=CC=C12)* 0.000 title 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 7
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Chemical compound OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 abstract 2
- 102000001301 EGF receptor Human genes 0.000 abstract 1
- 108060006698 EGF receptor Proteins 0.000 abstract 1
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical class N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
-
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
- C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
DERIVADOS DE QUINAZOLINA TENDO ATIVIDADE INIBITóRIA DE TIROSINA CINASE E COMPOSIçãO FARMACêUTICA CONTENDO-OS. A presente invenção refere-se a um composto que inibe tanto a tirosina cinase do receptor EGF quanto a tirosina cinase HER2. Composto representado pela fórmula geral (I): em que R^ x^ é um grupo representado pela fórmula: em que R^ 1^ é um átomo de hidrogênio, alquila opcionalmente substituida, etc.; Z é -O-, -N(R^ 10^)-, etc.; R^ 10^ é um átomo de hidrogênio, alquila, etc.; R^ 2^ é um átomo de hidrogênio, alquila opcionalmente substituida, etc.; R^ 18^ é um átomo de hidrogênio, alquila opcionalmente substituida, etc.; R^ 19^ é alquila opcionalmente substituida, etc.; W^ 1^ e um grupo contendo nitrogênio não aromático opcionaímente substituído; R^ 17^ é um átomo de hidrogênio, alquila opcionalmente substituida, etc.; R^ 3^ e R^ 4^ são independentemente um átomo de hidrogênio, alquila opcionalmente substituida, etc.; X é -O-, -S-, ou -N(R^ 12^)-, etc.; R^ 2^ é um átomo de hidrogênio, alquila, etc.; e A é fenila opcionalmente tendo um substituinte, etc., seu saí farmaceuticamente aceitável, ou um solvato do mesmo.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2005-047383 | 2005-02-23 | ||
| JP2005047383 | 2005-02-23 | ||
| JP2005156828 | 2005-05-30 | ||
| JP2005-156828 | 2005-05-30 | ||
| PCT/JP2006/303125 WO2006090717A1 (ja) | 2005-02-23 | 2006-02-22 | チロシンキナーゼ阻害作用を有するキナゾリン誘導体 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BRPI0606905A2 true BRPI0606905A2 (pt) | 2009-07-28 |
| BRPI0606905B1 BRPI0606905B1 (pt) | 2021-06-01 |
Family
ID=36927355
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0606905-3A BRPI0606905B1 (pt) | 2005-02-23 | 2006-02-22 | Derivados de quinazolina tendo atividade inibitória de tirosina cinase e composição farmacêutica que os compreende |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US8202879B2 (pt) |
| EP (1) | EP1854789B1 (pt) |
| JP (1) | JP4137174B2 (pt) |
| KR (1) | KR100910333B1 (pt) |
| CN (1) | CN101163684B (pt) |
| AU (1) | AU2006216266C1 (pt) |
| BR (1) | BRPI0606905B1 (pt) |
| CA (1) | CA2599328C (pt) |
| DK (1) | DK1854789T3 (pt) |
| ES (1) | ES2431843T3 (pt) |
| NO (1) | NO343403B1 (pt) |
| PL (1) | PL1854789T3 (pt) |
| PT (1) | PT1854789E (pt) |
| RU (1) | RU2414457C2 (pt) |
| TW (1) | TWI372147B (pt) |
| WO (1) | WO2006090717A1 (pt) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2414457C2 (ru) * | 2005-02-23 | 2011-03-20 | Сионоги Энд Ко., Лтд. | Производные хиназолина, обладающие ингибирующей активностью в отношении тирозинкиназы |
| CN101003514A (zh) * | 2006-01-20 | 2007-07-25 | 上海艾力斯医药科技有限公司 | 喹唑啉衍生物、其制备方法及用途 |
| US7547781B2 (en) | 2006-09-11 | 2009-06-16 | Curis, Inc. | Quinazoline based EGFR inhibitors containing a zinc binding moiety |
| MX2009002585A (es) | 2006-09-11 | 2009-08-24 | Curis Inc | Inhibidores e egfr a base de quinolina que contienen porcion de enlace de zinc. |
| WO2010053572A2 (en) | 2008-11-07 | 2010-05-14 | Massachusetts Institute Of Technology | Aminoalcohol lipidoids and uses thereof |
| TWI466872B (zh) | 2008-12-25 | 2015-01-01 | Shionogi & Co | 喹唑啉衍生物之製造方法 |
| EP2691443B1 (en) | 2011-03-28 | 2021-02-17 | Massachusetts Institute of Technology | Conjugated lipomers and uses thereof |
| EA032088B1 (ru) | 2011-10-27 | 2019-04-30 | Массачусетс Инститьют Оф Текнолоджи | Аминокислотные производные, функционализованные на n-конце, способные образовывать микросферы, инкапсулирующие лекарственное средство |
| CN103288756B (zh) * | 2012-02-29 | 2016-04-20 | 江苏先声药物研究有限公司 | 一种喹唑啉中间体的甲醇溶剂合物及其制备方法 |
| AU2014244426B2 (en) | 2013-03-14 | 2019-02-28 | Convergene Llc | Methods and compositions for inhibition of bromodomain-containing proteins |
| US9951051B2 (en) * | 2014-05-29 | 2018-04-24 | Shionogi & Co., Ltd. | Process for producing alkynylketone derivative |
| JP6334065B2 (ja) * | 2015-07-29 | 2018-05-30 | 塩野義製薬株式会社 | キナゾリン誘導体の塩またはその結晶およびそれらの製造方法 |
| MX2018004109A (es) | 2015-10-05 | 2018-09-27 | Univ Columbia | Activadores de flujo autofágico y fosfolipasa d y depuración de acumulaciones de proteína que incluyen tau y tratamiento de proteinopatías. |
| ES3011058T3 (en) * | 2015-11-25 | 2025-04-07 | Convergene Llc | Bicyclic bet bromodomain inhibitors and uses thereof |
| US20180030403A1 (en) | 2016-07-28 | 2018-02-01 | Bobban Subhadra | Devices, systems and methods for the production of humanized gut commensal microbiota |
| US10953016B2 (en) | 2017-01-30 | 2021-03-23 | Shionogi & Co., Ltd. | Solid dosage form containing quinazoline derivative |
| WO2020219168A1 (en) | 2019-04-24 | 2020-10-29 | Convergene, Llc | Small molecule bromodomain inhibitors and uses thereof |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK0584222T3 (da) | 1991-05-10 | 1998-02-23 | Rhone Poulenc Rorer Int | Bis-mono- og bicycliske aryl- og heteroarylforbindelser, som inhiberer EGF- og/eller PDGF-receptor-tyrosinkinase |
| NZ243082A (en) | 1991-06-28 | 1995-02-24 | Ici Plc | 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof |
| AU661533B2 (en) | 1992-01-20 | 1995-07-27 | Astrazeneca Ab | Quinazoline derivatives |
| GB9323290D0 (en) * | 1992-12-10 | 1994-01-05 | Zeneca Ltd | Quinazoline derivatives |
| ATE446955T1 (de) * | 1995-03-30 | 2009-11-15 | Pfizer Prod Inc | Chinazolinone derivate |
| GB9624482D0 (en) * | 1995-12-18 | 1997-01-15 | Zeneca Phaema S A | Chemical compounds |
| GB9603095D0 (en) * | 1996-02-14 | 1996-04-10 | Zeneca Ltd | Quinazoline derivatives |
| ATE227283T1 (de) * | 1996-07-13 | 2002-11-15 | Glaxo Group Ltd | Kondensierte heterozyklische verbindungen als protein kinase inhibitoren |
| EP1218356A1 (en) | 1999-09-21 | 2002-07-03 | AstraZeneca AB | Quinazoline compounds and pharmaceutical compositions containing them |
| RU2276151C2 (ru) * | 2000-06-06 | 2006-05-10 | Астразенека Аб | Хиназолиновые производные для лечения опухолей |
| DE60237145D1 (de) * | 2001-02-21 | 2010-09-09 | Mitsubishi Tanabe Pharma Corp | Chinazolinderivate |
| CA2463563A1 (en) | 2001-10-12 | 2003-04-17 | Irm Llc | Kinase inhibitor scaffolds and methods for their preparation |
| WO2004026307A1 (en) | 2002-09-18 | 2004-04-01 | Pfizer Products Inc. | Triazole derivatives as transforming growth factor (tgf) inhibitors |
| WO2004069145A2 (en) | 2003-02-07 | 2004-08-19 | Dr. Reddy's Laboratories Ltd. | Anticancer compounds, process for their preparation and pharmaceutical compositions containing them |
| PA8603801A1 (es) | 2003-05-27 | 2004-12-16 | Janssen Pharmaceutica Nv | Derivados de la quinazolina |
| US20100190150A1 (en) | 2004-01-07 | 2010-07-29 | Bristol-Myers Squibb Company | Biomarkers and methods for determining sensitivity to epidermal growth factor receptor modulators |
| US8017321B2 (en) | 2004-01-23 | 2011-09-13 | The Regents Of The University Of Colorado, A Body Corporate | Gefitinib sensitivity-related gene expression and products and methods related thereto |
| RU2414457C2 (ru) * | 2005-02-23 | 2011-03-20 | Сионоги Энд Ко., Лтд. | Производные хиназолина, обладающие ингибирующей активностью в отношении тирозинкиназы |
-
2006
- 2006-02-22 RU RU2007135023/04A patent/RU2414457C2/ru active
- 2006-02-22 EP EP06714265.3A patent/EP1854789B1/en not_active Expired - Lifetime
- 2006-02-22 US US11/884,819 patent/US8202879B2/en active Active
- 2006-02-22 JP JP2007504734A patent/JP4137174B2/ja not_active Expired - Lifetime
- 2006-02-22 CA CA2599328A patent/CA2599328C/en not_active Expired - Lifetime
- 2006-02-22 AU AU2006216266A patent/AU2006216266C1/en not_active Expired
- 2006-02-22 PT PT67142653T patent/PT1854789E/pt unknown
- 2006-02-22 WO PCT/JP2006/303125 patent/WO2006090717A1/ja not_active Ceased
- 2006-02-22 DK DK06714265.3T patent/DK1854789T3/da active
- 2006-02-22 KR KR1020077019256A patent/KR100910333B1/ko not_active Expired - Lifetime
- 2006-02-22 CN CN2006800136753A patent/CN101163684B/zh not_active Expired - Lifetime
- 2006-02-22 PL PL06714265T patent/PL1854789T3/pl unknown
- 2006-02-22 ES ES06714265T patent/ES2431843T3/es not_active Expired - Lifetime
- 2006-02-22 BR BRPI0606905-3A patent/BRPI0606905B1/pt active IP Right Grant
- 2006-02-23 TW TW095106013A patent/TWI372147B/zh active
-
2007
- 2007-08-23 NO NO20074311A patent/NO343403B1/no unknown
-
2012
- 2012-01-26 US US13/359,326 patent/US8349857B2/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| AU2006216266A1 (en) | 2006-08-31 |
| TW200640880A (en) | 2006-12-01 |
| ES2431843T3 (es) | 2013-11-28 |
| AU2006216266C1 (en) | 2010-08-26 |
| AU2006216266A2 (en) | 2006-08-31 |
| CA2599328A1 (en) | 2006-08-31 |
| AU2006216266A8 (en) | 2009-04-02 |
| WO2006090717A1 (ja) | 2006-08-31 |
| JPWO2006090717A1 (ja) | 2008-07-24 |
| EP1854789B1 (en) | 2013-10-09 |
| US20120123114A1 (en) | 2012-05-17 |
| DK1854789T3 (da) | 2013-10-21 |
| AU2006216266B2 (en) | 2010-02-18 |
| US8349857B2 (en) | 2013-01-08 |
| TWI372147B (en) | 2012-09-11 |
| EP1854789A1 (en) | 2007-11-14 |
| NO20074311L (no) | 2007-11-23 |
| BRPI0606905B1 (pt) | 2021-06-01 |
| KR100910333B1 (ko) | 2009-07-31 |
| RU2414457C2 (ru) | 2011-03-20 |
| KR20070098941A (ko) | 2007-10-05 |
| NO343403B1 (no) | 2019-02-25 |
| US8202879B2 (en) | 2012-06-19 |
| US20090143414A1 (en) | 2009-06-04 |
| PL1854789T3 (pl) | 2014-03-31 |
| CN101163684A (zh) | 2008-04-16 |
| JP4137174B2 (ja) | 2008-08-20 |
| RU2007135023A (ru) | 2009-03-27 |
| CA2599328C (en) | 2012-04-17 |
| EP1854789A4 (en) | 2009-06-17 |
| PT1854789E (pt) | 2013-10-23 |
| CN101163684B (zh) | 2012-08-29 |
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