CO6700852A2 - Derivados de bencimidazol como inhibidores de cinasa pi3 - Google Patents
Derivados de bencimidazol como inhibidores de cinasa pi3Info
- Publication number
- CO6700852A2 CO6700852A2 CO13090997A CO13090997A CO6700852A2 CO 6700852 A2 CO6700852 A2 CO 6700852A2 CO 13090997 A CO13090997 A CO 13090997A CO 13090997 A CO13090997 A CO 13090997A CO 6700852 A2 CO6700852 A2 CO 6700852A2
- Authority
- CO
- Colombia
- Prior art keywords
- suitably
- diseases
- relates
- benzimidazole derivatives
- cancer
- Prior art date
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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
- A61K31/535—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
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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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
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- 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]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D235/08—Radicals containing only hydrogen and carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D235/10—Radicals substituted by halogen atoms or nitro radicals
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
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- 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
- C07D401/10—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 carbon chain containing aromatic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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- 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
- C07D405/04—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 directly linked by a ring-member-to-ring-member bond
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- 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
- C07D405/10—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 aromatic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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- 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
- C07D417/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D417/10—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 carbon chain containing aromatic rings
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Esta invención se refiere al uso de derivados de bencimidazol para la modulación, notoriamente la inhibición, de la actividad o de la función de la familia de cinasa de fosfoinositida 3 OH (posteriormente en la presente las cinasas P13), adecuadamente, PI3Ka, PI3Kd, PI3Kß, y/o P13K?. Adecuadamente, la presente invención se refiere al uso de bencimidazoles en el tratamiento de uno o más estados de enfermedad seleccionados de entre: trastornos auto inmunológicos, enfermedades inflamatorias, enfermedades cardiovasculares, enfermedades neurodegenerativas, alergia, asma, pancreatitis, falla de múltiples órganos, enfermedades renales, acumulación de plaquetas, cáncer, movilidad del esperma, rechazo de trasplante, rechazo de injerto, y lesiones pulmonares. De una manera más adecuada, la presente invención se refiere a compuestos de bencimidazol selectivos de P13Kß para el tratamiento de cáncer.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US39031410P | 2010-10-06 | 2010-10-06 | |
US201161528397P | 2011-08-29 | 2011-08-29 |
Publications (1)
Publication Number | Publication Date |
---|---|
CO6700852A2 true CO6700852A2 (es) | 2013-06-28 |
Family
ID=45925614
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CO13090997A CO6700852A2 (es) | 2010-10-06 | 2013-04-08 | Derivados de bencimidazol como inhibidores de cinasa pi3 |
Country Status (37)
Country | Link |
---|---|
US (10) | US20130196990A1 (es) |
EP (2) | EP2624696B1 (es) |
JP (1) | JP5719028B2 (es) |
KR (1) | KR101594002B1 (es) |
CN (1) | CN103124496B (es) |
AR (1) | AR083296A1 (es) |
AU (1) | AU2011312594B2 (es) |
BR (1) | BR112013008259A2 (es) |
CA (1) | CA2812608C (es) |
CL (1) | CL2013000935A1 (es) |
CO (1) | CO6700852A2 (es) |
CR (1) | CR20130192A (es) |
CY (1) | CY1118792T1 (es) |
DK (1) | DK2624696T3 (es) |
DO (1) | DOP2013000059A (es) |
EA (1) | EA022623B1 (es) |
ES (2) | ES2714384T3 (es) |
HR (1) | HRP20170279T1 (es) |
HU (1) | HUE033209T2 (es) |
IL (1) | IL225140A (es) |
JO (1) | JO3194B1 (es) |
LT (1) | LT2624696T (es) |
MA (1) | MA34591B1 (es) |
ME (1) | ME02663B (es) |
MX (1) | MX337662B (es) |
MY (1) | MY170236A (es) |
NZ (1) | NZ608069A (es) |
PE (1) | PE20140192A1 (es) |
PL (1) | PL2624696T3 (es) |
PT (1) | PT2624696T (es) |
RS (1) | RS55662B1 (es) |
SG (1) | SG188974A1 (es) |
SI (1) | SI2624696T1 (es) |
TW (1) | TWI513690B (es) |
UY (1) | UY33648A (es) |
WO (1) | WO2012047538A1 (es) |
ZA (1) | ZA201301951B (es) |
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CA2812608C (en) | 2010-10-06 | 2020-07-14 | Glaxosmithkline Llc | Benzimidazole derivatives as pi3 kinase inhibitors |
US8778937B2 (en) * | 2011-12-20 | 2014-07-15 | Glaxosmithkline Llc | Benzimidazole boronic acid derivatives as PI3 kinase inhibitors |
JP2016504409A (ja) * | 2013-01-09 | 2016-02-12 | グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー2、リミテッドGlaxosmithkline Intellectual Property No.2 Limited | 組合せ |
CA2921156A1 (en) * | 2013-09-19 | 2015-03-26 | Glaxosmithkline Llc | Combination drug therapy |
US20160287610A1 (en) * | 2013-09-19 | 2016-10-06 | GlaxoSmithKline LLCC | Combination Drug Therapy |
AU2014336775B2 (en) | 2013-10-16 | 2018-04-05 | Shanghai Yingli Pharmaceutical Co., Ltd | Fused heterocyclic compound, preparation method therefor, pharmaceutical composition, and uses thereof |
CN103910682B (zh) * | 2013-11-28 | 2016-03-02 | 大连理工大学 | 一种基于邻苯二胺环化的苯并咪唑类化合物制备方法 |
JP2017502016A (ja) * | 2013-12-20 | 2017-01-19 | バイオメッド バレー ディスカバリーズ,インコーポレイティド | 1型mek阻害剤およびerk阻害剤の組み合わせを使用するがんの処置 |
NZ726360A (en) | 2014-06-13 | 2018-04-27 | Gilead Sciences Inc | Phosphatidylinositol 3-kinase inhibitors |
JP6383810B2 (ja) | 2014-06-13 | 2018-08-29 | ギリアード サイエンシーズ, インコーポレイテッド | ホスファチジルイノシトール3−キナーゼ阻害剤としてのキナゾリノン誘導体 |
BR112016028819A2 (pt) | 2014-06-13 | 2017-08-22 | Gilead Sciences Inc | composição farmacêutica, métodos para tratar uma doença ou condição em um ser humano e para inibir a atividade de um polipeptídeo de fosfatidilinositol 3-quinase e reações imunológicas excessivas ou destrutivas ou o crescimento ou a proliferação de células cancerosas, kit, composto, sal farmaceuticamente aceitável, isômero ou mistura dos mesmos, e, uso de um composto, sal farmaceuticamente aceitável ou mistura dos mesmos. |
EP3154962B1 (en) | 2014-06-13 | 2019-08-07 | Gilead Sciences, Inc. | Phosphatidylinositol 3-kinase inhibitors |
EP3154958B1 (en) | 2014-06-13 | 2020-10-07 | Gilead Sciences, Inc. | Phosphatidylinositol 3-kinase inhibitors |
ES2760507T3 (es) | 2014-12-19 | 2020-05-14 | Janssen Pharmaceutica Nv | Derivados de imidazopiridazina enlazados a heterociclilo como inhibidores de PI3Kß |
JP6568588B2 (ja) | 2014-12-19 | 2019-08-28 | ヤンセン ファーマシューティカ エヌ.ベー. | PI3Kβ阻害剤としてのイミダゾピリダジン誘導体 |
GB201504689D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
JP6912460B2 (ja) | 2015-10-09 | 2021-08-04 | ヤンセン ファーマシューティカ エヌ.ベー. | PI3Kβ阻害剤としてのキノキサリンおよびピリドピラジン誘導体 |
EP3402795B1 (en) * | 2016-01-14 | 2019-10-30 | Bayer Pharma Aktiengesellschaft | 5-substituted 2-(morpholin-4-yl)-1,7-naphthyridines |
KR102472453B1 (ko) | 2016-06-16 | 2022-11-29 | 얀센 파마슈티카 엔.브이. | Pi3k 베타 저해제로서의 이환식 피리딘, 피라진, 및 피리미딘 유도체 |
CA3025746A1 (en) * | 2016-06-16 | 2017-12-21 | Janssen Pharmaceutica Nv | Azabenzimidazole derivatives as pi3k beta inhibitors |
WO2018013534A1 (en) * | 2016-07-11 | 2018-01-18 | Dana-Farber Cancer Institute, Inc. | Methods for treating pten deficient epithelial cancers using a combination of anti-pi3kbeta and anti-immune checkpoint agents |
TW201815787A (zh) | 2016-09-23 | 2018-05-01 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
TW201825465A (zh) | 2016-09-23 | 2018-07-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
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TW201813963A (zh) | 2016-09-23 | 2018-04-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
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BR112020001278A2 (pt) | 2017-07-28 | 2020-07-21 | Yuhan Corporation | processo aprimorado para preparar derivados de aminopirimidina |
WO2019106605A1 (en) | 2017-12-01 | 2019-06-06 | Board Of Regents, The University Of Texas System | Combination treatment for cancer |
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CN111000847B (zh) * | 2020-01-02 | 2021-03-19 | 黑龙江中医药大学 | 一种治疗肺纤维化的药物制剂及其用途 |
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