BRPI0519054A2 - fenil metanonas bi e tricÍclicas substituÍdas como inibidores de transportador i de glicina (glyt-1) para o tratamento de doenÇa de alzheimer - Google Patents
fenil metanonas bi e tricÍclicas substituÍdas como inibidores de transportador i de glicina (glyt-1) para o tratamento de doenÇa de alzheimerInfo
- Publication number
- BRPI0519054A2 BRPI0519054A2 BRPI0519054-1A BRPI0519054A BRPI0519054A2 BR PI0519054 A2 BRPI0519054 A2 BR PI0519054A2 BR PI0519054 A BRPI0519054 A BR PI0519054A BR PI0519054 A2 BRPI0519054 A2 BR PI0519054A2
- Authority
- BR
- Brazil
- Prior art keywords
- lower alkyl
- halogen
- glyt
- alzheimer
- inhibitors
- Prior art date
Links
- 208000024827 Alzheimer disease Diseases 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 102000010726 Glycine Plasma Membrane Transport Proteins Human genes 0.000 title 1
- 108010063380 Glycine Plasma Membrane Transport Proteins Proteins 0.000 title 1
- HUMNYLRZRPPJDN-UHFFFAOYSA-N benzaldehyde Chemical class O=CC1=CC=CC=C1 HUMNYLRZRPPJDN-UHFFFAOYSA-N 0.000 title 1
- 125000002619 bicyclic group Chemical group 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 229910052736 halogen Inorganic materials 0.000 abstract 6
- 150000002367 halogens Chemical group 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 150000002431 hydrogen Chemical class 0.000 abstract 3
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 abstract 2
- 239000004471 Glycine Substances 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000000926 neurological effect Effects 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Neurosurgery (AREA)
- Medicinal Chemistry (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
FENIL METANONAS BI E TRICÍCLICAS SUBSTITUIDAS COMO INIBIDORES DE TRANSPORTADOR I DE GLICINA (GLYT-1) PARA O TRATAMENTO DE DOENÇA DE ALZHEIMER. A presente invenção refere-se a compostos da fórmula geral I em que ou R¹ é um heterociclo não aromático, ou é OR' ou N(R")~ 2~; é alquila inferior, alquila inferior substituida com halogênio ou é - (CH~ 2~)~ n~-cicIoaIquila; R" é alquila inferior; R² é NO~ 2~, CN ou SO~ 2~R"; Rü é hidrogênio, halogênio, alquila inferior, alcóxi inferior, ou alquila inferior substituida com halogênio; R^ 4^ é hidrogênio, alquila inferior, fenila substituída com halogênio ou CF~ 3~, ou é um heterociclo aromático de cinco ou seis membros; R^ 5^/R^ 6^ são hidrogênio, halogênio, alquila inferior, alcóxi inferior, ou são alquila inferior ou alcóxi inferior, substituído com halogênio; R^ 7^ é hidrogênio ou alquila inferior; n é 0, ou 2; e a sais de adição de ácido farmaceuticamente ativos para tratamento de distúrbios neurológicos e neuropsiquiátricos.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP04106597 | 2004-12-15 | ||
PCT/EP2005/012994 WO2006063709A1 (en) | 2004-12-15 | 2005-12-05 | Bi- and tricyclic substituted phenyl methanones as glycine transporter i (glyt-1) inhibitors for the treatment of alzheimer’s disease |
Publications (1)
Publication Number | Publication Date |
---|---|
BRPI0519054A2 true BRPI0519054A2 (pt) | 2008-12-23 |
Family
ID=35841863
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BRPI0519054-1A BRPI0519054A2 (pt) | 2004-12-15 | 2005-12-05 | fenil metanonas bi e tricÍclicas substituÍdas como inibidores de transportador i de glicina (glyt-1) para o tratamento de doenÇa de alzheimer |
Country Status (20)
Country | Link |
---|---|
US (1) | US7375226B2 (pt) |
EP (1) | EP1828200B1 (pt) |
JP (1) | JP4709849B2 (pt) |
KR (1) | KR100883003B1 (pt) |
CN (1) | CN100586951C (pt) |
AR (1) | AR052156A1 (pt) |
AT (1) | ATE457989T1 (pt) |
AU (1) | AU2005315914B2 (pt) |
BR (1) | BRPI0519054A2 (pt) |
CA (1) | CA2590316A1 (pt) |
DE (1) | DE602005019465D1 (pt) |
ES (1) | ES2338139T3 (pt) |
IL (1) | IL183592A0 (pt) |
MX (1) | MX2007006896A (pt) |
NO (1) | NO20072833L (pt) |
NZ (1) | NZ555476A (pt) |
RU (1) | RU2007121768A (pt) |
TW (1) | TWI299041B (pt) |
WO (1) | WO2006063709A1 (pt) |
ZA (1) | ZA200705044B (pt) |
Families Citing this family (50)
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US7485637B2 (en) * | 2005-01-04 | 2009-02-03 | Hoffmann-La Roche Inc. | Benzoyl-tetrahydropiperidine derivatives |
RU2338537C2 (ru) * | 2006-01-25 | 2008-11-20 | Сергей Олегович Бачурин | СРЕДСТВО ДЛЯ ЛЕЧЕНИЯ ШИЗОФРЕНИИ НА ОСНОВЕ ГИДРИРОВАННЫХ ПИРИДО(4,3-b)ИНДОЛОВ (ВАРИАНТЫ), ФАРМАКОЛОГИЧЕСКОЕ СРЕДСТВО НА ЕГО ОСНОВЕ И СПОСОБ ЕГО ПРИМЕНЕНИЯ |
DK2134710T3 (da) | 2007-03-12 | 2020-05-18 | Intra Cellular Therapies Inc | Syntese af gamma-carboliner, der er kondenseret med substitueret heterocyklus |
JP5554319B2 (ja) | 2008-04-01 | 2014-07-23 | アボット ゲーエムベーハー ウント カンパニー カーゲー | テトラヒドロイソキノリン類、それを含む医薬組成物および治療におけるそれの使用 |
KR20110120885A (ko) | 2009-02-06 | 2011-11-04 | 바스프 에스이 | 개선된 내후성을 갖는 스티렌 공중합체 및 폴리아미드 기재 열가소성 성형 조성물 |
TW201038569A (en) * | 2009-02-16 | 2010-11-01 | Abbott Gmbh & Co Kg | Heterocyclic compounds, pharmaceutical compositions containing them, and their use in therapy |
AR075442A1 (es) | 2009-02-16 | 2011-03-30 | Abbott Gmbh & Co Kg | Derivados de aminotetralina, composiciones farmaceuticas que las contienen y sus usos en terapia |
US8846743B2 (en) | 2010-08-13 | 2014-09-30 | Abbott Laboratories | Aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy |
US8883839B2 (en) | 2010-08-13 | 2014-11-11 | Abbott Laboratories | Tetraline and indane derivatives, pharmaceutical compositions containing them, and their use in therapy |
US9051280B2 (en) | 2010-08-13 | 2015-06-09 | AbbVie Deutschland GmbH & Co. KG | Tetraline and indane derivatives, pharmaceutical compositions containing them, and their use in therapy |
US9045459B2 (en) | 2010-08-13 | 2015-06-02 | AbbVie Deutschland GmbH & Co. KG | Phenalkylamine derivatives, pharmaceutical compositions containing them, and their use in therapy |
US8877794B2 (en) | 2010-08-13 | 2014-11-04 | Abbott Laboratories | Phenalkylamine derivatives, pharmaceutical compositions containing them, and their use in therapy |
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EP2780328A1 (en) | 2011-11-18 | 2014-09-24 | Abbvie Deutschland GmbH & Co. KG | N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives, pharmaceutical compositions containing them, and their use in therapy |
WO2013091773A1 (en) * | 2011-12-22 | 2013-06-27 | Merck Patent Gmbh | Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators |
US9365512B2 (en) | 2012-02-13 | 2016-06-14 | AbbVie Deutschland GmbH & Co. KG | Isoindoline derivatives, pharmaceutical compositions containing them, and their use in therapy |
JP6114814B2 (ja) | 2012-03-16 | 2017-04-12 | ヴァイティー ファーマシューティカルズ,インコーポレイテッド | 肝臓xレセプターモジュレーター |
HRP20161690T1 (hr) * | 2012-03-16 | 2017-02-24 | Vitae Pharmaceuticals, Inc. | Modulatori jetrenog receptora x |
US9428506B2 (en) | 2012-04-14 | 2016-08-30 | Intra-Cellular Therapies, Inc. | Substituted pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalines for the treatment of nervous system disorders |
US9656955B2 (en) | 2013-03-15 | 2017-05-23 | Abbvie Inc. | Pyrrolidine derivatives, pharmaceutical compositions containing them, and their use in therapy |
US9650334B2 (en) | 2013-03-15 | 2017-05-16 | Abbvie Inc. | Pyrrolidine derivatives, pharmaceutical compositions containing them, and their use in therapy |
EP2968320B1 (en) | 2013-03-15 | 2020-11-11 | Intra-Cellular Therapies, Inc. | Organic compounds |
CA2924689A1 (en) | 2013-10-17 | 2015-04-23 | AbbVie Deutschland GmbH & Co. KG | Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy |
JP2016533375A (ja) | 2013-10-17 | 2016-10-27 | アッヴィ・ドイチュラント・ゲー・エム・ベー・ハー・ウント・コー・カー・ゲー | アミノテトラリン誘導体およびアミノインダン誘導体、これらを含有する医薬組成物、および治療におけるこれらの使用 |
KR102372145B1 (ko) | 2013-12-03 | 2022-03-07 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 신규한 방법 |
RU2728787C2 (ru) | 2014-04-04 | 2020-07-31 | Интра-Селлулар Терапиз, Инк. | Органические соединения |
WO2015154030A1 (en) | 2014-04-04 | 2015-10-08 | Intra-Cellular Therapies, Inc. | Organic compounds |
ES2863471T3 (es) | 2016-01-26 | 2021-10-11 | Intra Cellular Therapies Inc | Compuestos de piridopirroloquinoxalina, sus composiciones y usos |
EP3407889B1 (en) | 2016-03-25 | 2021-05-19 | Intra-Cellular Therapies, Inc. | Organic compounds and their use in treating or preventing central nervous system disorders |
WO2017172795A1 (en) | 2016-03-28 | 2017-10-05 | Intra-Cellular Therapies, Inc. | Novel compositions and methods |
EP3436455A4 (en) | 2016-03-28 | 2019-09-04 | Intra-Cellular Therapies, Inc. | NOVEL SALTS AND CRYSTALS |
JP6997718B2 (ja) | 2016-03-28 | 2022-01-18 | イントラ-セルラー・セラピーズ・インコーポレイテッド | 新規共結晶 |
CN110072518B (zh) | 2016-10-12 | 2021-10-26 | 细胞内治疗公司 | 无定形固体分散体 |
WO2018126140A1 (en) | 2016-12-29 | 2018-07-05 | Intra-Cellular Therapies, Inc. | Organic compounds |
EP3562484B1 (en) | 2016-12-29 | 2021-08-25 | Intra-Cellular Therapies, Inc. | Pyrido[3',4':4,5]pyrrolo[1,2,3-de]quinoxaline derivatives useful in the treatment of cns disorders |
RU2767410C2 (ru) | 2017-03-24 | 2022-03-17 | Интра-Селлулар Терапиз, Инк. | Новые композиции и способы |
KR20200033307A (ko) | 2017-07-26 | 2020-03-27 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 유기 화합물 |
CA3071137A1 (en) | 2017-07-26 | 2019-01-31 | Intra-Cellular Therapies, Inc. | Prodrugs of substituted heterocycle fused gamma-carbolines |
CA3102848A1 (en) | 2018-06-06 | 2019-12-12 | Intra-Cellular Therapies, Inc. | Novel salts and crystals |
MX2020013335A (es) | 2018-06-08 | 2021-05-27 | Intra Cellular Therapies Inc | Metodos novedosos. |
JP7483671B2 (ja) | 2018-06-11 | 2024-05-15 | イントラ-セルラー・セラピーズ・インコーポレイテッド | 置換ヘテロ環縮合ガンマ-カルボリン類合成 |
WO2020047241A1 (en) | 2018-08-29 | 2020-03-05 | Intra-Cellular Therapies, Inc. | Novel compositions and methods |
BR112021003838A2 (pt) | 2018-08-31 | 2021-05-18 | Intra-Cellular Therapies, Inc. | métodos novos |
CA3108553A1 (en) | 2018-08-31 | 2020-03-05 | Intra-Cellular Therapies, Inc. | Novel methods |
EP3898581A4 (en) | 2018-12-17 | 2022-08-17 | Intra-Cellular Therapies, Inc. | SYNTHESIS OF FUSED GAMMA-CARBOLINES WITH SUBSTITUTED HETEROCYCLES |
CN113227045B (zh) | 2018-12-17 | 2024-04-26 | 细胞内治疗公司 | 取代的杂环稠合的γ-咔啉的合成 |
CN114072150A (zh) | 2019-07-07 | 2022-02-18 | 细胞内治疗公司 | 新方法 |
JP7261942B2 (ja) | 2019-12-11 | 2023-04-20 | イントラ-セルラー・セラピーズ・インコーポレイテッド | 有機化合物 |
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WO2005023261A1 (en) * | 2003-09-09 | 2005-03-17 | F. Hoffmann-La Roche Ag | 1-benzoyl-piperazine derivatives as glycine uptake inhibitors for the treatment of psychoses |
-
2005
- 2005-12-05 EP EP05823127A patent/EP1828200B1/en active Active
- 2005-12-05 AU AU2005315914A patent/AU2005315914B2/en not_active Ceased
- 2005-12-05 NZ NZ555476A patent/NZ555476A/en not_active IP Right Cessation
- 2005-12-05 DE DE602005019465T patent/DE602005019465D1/de active Active
- 2005-12-05 CN CN200580042730A patent/CN100586951C/zh not_active Expired - Fee Related
- 2005-12-05 KR KR1020077013440A patent/KR100883003B1/ko not_active Expired - Fee Related
- 2005-12-05 ES ES05823127T patent/ES2338139T3/es active Active
- 2005-12-05 BR BRPI0519054-1A patent/BRPI0519054A2/pt not_active IP Right Cessation
- 2005-12-05 MX MX2007006896A patent/MX2007006896A/es active IP Right Grant
- 2005-12-05 WO PCT/EP2005/012994 patent/WO2006063709A1/en active Application Filing
- 2005-12-05 CA CA002590316A patent/CA2590316A1/en not_active Abandoned
- 2005-12-05 JP JP2007545891A patent/JP4709849B2/ja not_active Expired - Fee Related
- 2005-12-05 RU RU2007121768/04A patent/RU2007121768A/ru not_active Application Discontinuation
- 2005-12-05 AT AT05823127T patent/ATE457989T1/de active
- 2005-12-08 US US11/297,597 patent/US7375226B2/en not_active Expired - Fee Related
- 2005-12-12 TW TW094143890A patent/TWI299041B/zh not_active IP Right Cessation
- 2005-12-13 AR ARP050105207A patent/AR052156A1/es not_active Application Discontinuation
-
2007
- 2007-05-31 IL IL183592A patent/IL183592A0/en unknown
- 2007-06-04 NO NO20072833A patent/NO20072833L/no not_active Application Discontinuation
- 2007-06-07 ZA ZA200705044A patent/ZA200705044B/xx unknown
Also Published As
Publication number | Publication date |
---|---|
TWI299041B (en) | 2008-07-21 |
AU2005315914B2 (en) | 2011-03-03 |
KR100883003B1 (ko) | 2009-02-12 |
WO2006063709A1 (en) | 2006-06-22 |
JP4709849B2 (ja) | 2011-06-29 |
DE602005019465D1 (de) | 2010-04-01 |
IL183592A0 (en) | 2007-09-20 |
NZ555476A (en) | 2009-09-25 |
MX2007006896A (es) | 2007-06-26 |
ES2338139T3 (es) | 2010-05-04 |
JP2008523126A (ja) | 2008-07-03 |
AU2005315914A1 (en) | 2006-06-22 |
CA2590316A1 (en) | 2006-06-22 |
ZA200705044B (en) | 2008-09-25 |
EP1828200A1 (en) | 2007-09-05 |
US7375226B2 (en) | 2008-05-20 |
CN100586951C (zh) | 2010-02-03 |
AR052156A1 (es) | 2007-03-07 |
TW200634017A (en) | 2006-10-01 |
EP1828200B1 (en) | 2010-02-17 |
KR20070086196A (ko) | 2007-08-27 |
RU2007121768A (ru) | 2009-01-27 |
ATE457989T1 (de) | 2010-03-15 |
US20060128713A1 (en) | 2006-06-15 |
NO20072833L (no) | 2007-07-17 |
CN101076532A (zh) | 2007-11-21 |
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