EA200500248A1 - Селективные модуляторы эстрогенных рецепторов, содержащие фенилсульфонильную группу - Google Patents
Селективные модуляторы эстрогенных рецепторов, содержащие фенилсульфонильную группуInfo
- Publication number
- EA200500248A1 EA200500248A1 EA200500248A EA200500248A EA200500248A1 EA 200500248 A1 EA200500248 A1 EA 200500248A1 EA 200500248 A EA200500248 A EA 200500248A EA 200500248 A EA200500248 A EA 200500248A EA 200500248 A1 EA200500248 A1 EA 200500248A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- phenylsulphone
- group
- estrogen receptors
- receptors containing
- selective modulators
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
- C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/32—Antioestrogens
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
- C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
- C07D333/56—Radicals substituted by oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 carbon atoms of the hetero ring
- C07D333/64—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/72—Benzo[c]thiophenes; Hydrogenated benzo[c]thiophenes
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Настоящее изобретение относится к селективному модулятору эстрогенных рецепторов формулы I или его фармацевтической аддитивной соли кислоты, полезных, например, для лечения эндометриоза и/или лейомиомы/лейомиоматоза матки.Международная заявка была опубликована вместе с отчетом о международном поиске.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US39786902P | 2002-07-22 | 2002-07-22 | |
US45023303P | 2003-02-25 | 2003-02-25 | |
PCT/IB2003/003349 WO2004009086A1 (en) | 2002-07-22 | 2003-07-16 | Selective estrogen receptor modulators containing a phenylsulfonyl group |
Publications (2)
Publication Number | Publication Date |
---|---|
EA200500248A1 true EA200500248A1 (ru) | 2005-06-30 |
EA008024B1 EA008024B1 (ru) | 2007-02-27 |
Family
ID=30773044
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200500248A EA008024B1 (ru) | 2002-07-22 | 2003-07-16 | Селективные модуляторы эстрогенных рецепторов, содержащие фенилсульфонильную группу |
Country Status (25)
Country | Link |
---|---|
US (2) | US7399867B2 (ru) |
EP (1) | EP1530470B9 (ru) |
JP (2) | JP4656939B2 (ru) |
CN (1) | CN1668303B (ru) |
AT (1) | ATE433322T1 (ru) |
AU (1) | AU2003253129B2 (ru) |
BR (1) | BR0312675A (ru) |
CA (1) | CA2490580C (ru) |
CO (1) | CO5680445A2 (ru) |
CR (1) | CR7657A (ru) |
DE (1) | DE60327931D1 (ru) |
EA (1) | EA008024B1 (ru) |
EC (1) | ECSP055549A (ru) |
ES (1) | ES2326593T3 (ru) |
HK (1) | HK1078003A1 (ru) |
HR (1) | HRP20041233A2 (ru) |
IL (1) | IL165745A0 (ru) |
MX (1) | MXPA05000898A (ru) |
MY (1) | MY141879A (ru) |
NO (1) | NO20050832L (ru) |
NZ (1) | NZ537138A (ru) |
PE (1) | PE20040678A1 (ru) |
PL (1) | PL374845A1 (ru) |
TW (1) | TWI314860B (ru) |
WO (1) | WO2004009086A1 (ru) |
Families Citing this family (27)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EA008024B1 (ru) * | 2002-07-22 | 2007-02-27 | Эли Лилли Энд Компани | Селективные модуляторы эстрогенных рецепторов, содержащие фенилсульфонильную группу |
CA2512663A1 (en) * | 2003-02-25 | 2004-09-10 | Eli Lilly And Company | Crystalline non-solvated 1-(4-(2-piperidinylethoxy)phenoxy)-2-(4-methanesulfonylphenyl)-6-hydroxynaphthalene hydrochloride |
EA007978B1 (ru) * | 2003-02-25 | 2007-02-27 | Эли Лилли Энд Компани | Кристаллический несольватированный гидрохлорид 1-(4-(2-пиперидинилэтокси)фенокси)-2-(4-метансульфонилфенил)-6-гидроксинафталина |
CN1910167B (zh) * | 2004-01-22 | 2011-08-10 | 伊莱利利公司 | 用于治疗血管舒缩症状的选择性雌激素受体调节剂 |
US20070066595A1 (en) * | 2004-01-22 | 2007-03-22 | Dodge Jeffrey A | Selective estrogen receptor modulators |
UA85862C2 (ru) * | 2004-01-22 | 2009-03-10 | Елі Ліллі Енд Компані | Селективные модуляторы рецепторов эстрогена для лечения фазомоторных симптомов |
US20080227814A1 (en) * | 2004-01-29 | 2008-09-18 | Jeffrey Alan Dodge | Selective Estrogen Receptor Modulators |
BRPI0512395A (pt) * | 2004-06-22 | 2008-03-11 | Smithkline Beecham Corp | composto, composição farmacêutica, uso de um composto, e, métodos para o tratamento ou a profilaxia de condições ou distúrbios associadas(os) com a modulação de receptor de estrogênio seletiva, e para o tratamento ou a profilaxia relacionado(a) com condições ou distúrbios |
JP2009502935A (ja) * | 2005-07-29 | 2009-01-29 | イーライ リリー アンド カンパニー | 結晶化非溶媒和化1−(4−(2−ピペリジニルエトキシ)フェノキシ)−2−(3−ヒドロキシフェニル)−6−ヒドロキシナフタレンメタンスルホン酸塩 |
MX2011003383A (es) * | 2008-09-29 | 2011-04-21 | Lilly Co Eli | Modulador selectivo del receptor de estrogeno para el tratamiento de osteoartritis. |
DE102008057230A1 (de) | 2008-11-11 | 2010-05-12 | Bayer Schering Pharma Aktiengesellschaft | Synergistische pharmazeutische Kombination mit einem Estrogenrezeptorantagonisten und einem Progestin |
EP2406230A1 (en) | 2009-03-11 | 2012-01-18 | Pfizer Inc. | Substituted indazole amides and their use as glucokinase activators |
KR20140089402A (ko) | 2010-06-16 | 2014-07-14 | 앙도르쉐르슈 인코포레이티드 | 에스트로겐-관련 질병의 치료 또는 예방 방법 |
JP6292744B2 (ja) * | 2012-09-19 | 2018-03-14 | 富士カプセル株式会社 | 医薬品組成物 |
US9321746B2 (en) | 2013-02-19 | 2016-04-26 | Novartis Ag | Benzothiophene derivatives and compositions thereof as selective estrogen receptor degraders |
BR112021017646A2 (pt) | 2019-03-08 | 2021-11-16 | Syngenta Crop Protection Ag | Compostos de azol-amida ativos em termos pesticidas |
WO2020188027A1 (en) | 2019-03-20 | 2020-09-24 | Syngenta Crop Protection Ag | Pesticidally active azole amide compounds |
WO2020193341A1 (en) | 2019-03-22 | 2020-10-01 | Syngenta Crop Protection Ag | N-[1-(5-bromo-2-pyrimidin-2-yl-1,2,4-triazol-3-yl)ethyl]-2-cyclopropyl-6-(trifluoromethyl)pyridine-4-carboxamide derivatives and related compounds as insecticides |
UY38623A (es) | 2019-03-29 | 2020-10-30 | Syngenta Crop Protection Ag | Compuestos de diazina-amida activos como pesticidas |
MX2021012162A (es) | 2019-04-05 | 2021-11-03 | Syngenta Crop Protection Ag | Compuestos de diazina-amida activos como pesticidas. |
WO2021037614A1 (en) | 2019-08-23 | 2021-03-04 | Syngenta Crop Protection Ag | Pesticidally active pyrazine-amide compounds |
CN110526881B (zh) * | 2019-08-27 | 2020-09-22 | 河南省锐达医药科技有限公司 | 一种萘胺类化合物及其生物学可接受的盐,其制备方法和应用 |
EP4110766A1 (en) | 2020-02-27 | 2023-01-04 | Syngenta Crop Protection AG | Pesticidally active diazine-bisamide compounds |
KR20240007916A (ko) * | 2021-05-14 | 2024-01-17 | 장슈 야홍 메디텍 코퍼레이션 리미티드 | 나프탈렌 고리를 포함하는 화합물, 이를 포함하는 약학 조성물 및 이의 용도 |
EP4352050A1 (en) | 2021-06-09 | 2024-04-17 | Syngenta Crop Protection AG | Pesticidally active diazine-amide compounds |
WO2023283315A1 (en) * | 2021-07-07 | 2023-01-12 | South Dakota Board Of Regents | Compositions and methods for treatment of cervical and ovarian cancer |
WO2024042187A1 (en) | 2022-08-25 | 2024-02-29 | Sanofi | Novel substituted benzothiophene-6-carboxylic acid derivatives, processes for their preparation and therapeutic uses thereof |
Family Cites Families (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4418068A (en) * | 1981-04-03 | 1983-11-29 | Eli Lilly And Company | Antiestrogenic and antiandrugenic benzothiophenes |
EP0639567A1 (en) | 1992-05-08 | 1995-02-22 | Otsuka Pharmaceutical Factory, Inc. | Indole derivative |
US6756388B1 (en) | 1993-10-12 | 2004-06-29 | Pfizer Inc. | Benzothiophenes and related compounds as estrogen agonists |
US7501441B1 (en) | 1994-09-20 | 2009-03-10 | Eli Lilly And Company | Naphthyl compounds, intermediates, processes, compositions, and methods |
US6399634B1 (en) * | 1994-09-20 | 2002-06-04 | Eli Lilly And Company | Benzothiophene compounds, compositions, and methods |
US5552412A (en) | 1995-01-09 | 1996-09-03 | Pfizer Inc | 5-substitued-6-cyclic-5,6,7,8-tetrahydronaphthalen2-ol compounds which are useful for treating osteoporosis |
US5998401A (en) * | 1995-02-28 | 1999-12-07 | Eli Lilly And Company | Naphthyl compounds, intermediates, compositions, and methods |
EP0729956B1 (en) | 1995-02-28 | 2001-10-31 | Eli Lilly And Company | Benzothiophene compounds, intermediates, compositions, and methods |
US5599822A (en) | 1995-06-06 | 1997-02-04 | Eli Lilly And Company | Methods for minimizing bone loss |
ES2233982T3 (es) * | 1995-10-31 | 2005-06-16 | Eli Lilly And Company | Diaminas antitromboticas. |
IL125863A (en) * | 1996-02-22 | 2000-10-31 | Lilly Co Eli | Benzothiophenes and formulations containing same |
SK281737B6 (sk) | 1996-04-19 | 2001-07-10 | American Home Products Corporation | 2-fenylindolové zlúčeniny, farmaceutický prostriedok s ich obsahom a ich použitie |
ID19392A (id) | 1996-08-29 | 1998-07-09 | Lilly Co Eli | Senyawa naftil dan bahan pertengahan serta komposisi dan metode penggunaan |
CA2213814A1 (en) | 1996-08-29 | 1998-02-28 | Henry Uhlman Bryant | Naphthalene compounds, intermediates, formulations, and methods |
CA2213810C (en) | 1996-08-29 | 2006-06-06 | Lewis Dale Pennington | Benzo¬b|thiophene compounds, intermediates, processes, compositions and methods |
CA2214070C (en) | 1996-08-29 | 2006-03-14 | Eli Lilly And Company | Dihydronaphthalene and naphthalene compounds, intermediates, formulations, and methods |
CA2217810A1 (en) * | 1996-10-10 | 1998-04-10 | Eli Lilly And Company | 2-aryl-3-aminoaryloxynaphthyl compounds, intermediates, compositions and methods |
JPH10204082A (ja) | 1996-10-25 | 1998-08-04 | Eli Lilly & Co | 選択的エストロゲンレセプターモジュレーターとしての活性を有する置換されたベンゾ[b]チオフェン化合物 |
EA008024B1 (ru) * | 2002-07-22 | 2007-02-27 | Эли Лилли Энд Компани | Селективные модуляторы эстрогенных рецепторов, содержащие фенилсульфонильную группу |
-
2003
- 2003-07-16 EA EA200500248A patent/EA008024B1/ru not_active IP Right Cessation
- 2003-07-16 CN CN038172011A patent/CN1668303B/zh not_active Expired - Fee Related
- 2003-07-16 WO PCT/IB2003/003349 patent/WO2004009086A1/en active Application Filing
- 2003-07-16 US US10/521,896 patent/US7399867B2/en not_active Expired - Fee Related
- 2003-07-16 DE DE60327931T patent/DE60327931D1/de not_active Expired - Lifetime
- 2003-07-16 CA CA2490580A patent/CA2490580C/en not_active Expired - Fee Related
- 2003-07-16 AT AT03765254T patent/ATE433322T1/de not_active IP Right Cessation
- 2003-07-16 EP EP03765254A patent/EP1530470B9/en not_active Expired - Lifetime
- 2003-07-16 JP JP2004522648A patent/JP4656939B2/ja not_active Expired - Fee Related
- 2003-07-16 MX MXPA05000898A patent/MXPA05000898A/es active IP Right Grant
- 2003-07-16 BR BR0312675-7A patent/BR0312675A/pt not_active IP Right Cessation
- 2003-07-16 PL PL03374845A patent/PL374845A1/xx unknown
- 2003-07-16 AU AU2003253129A patent/AU2003253129B2/en not_active Ceased
- 2003-07-16 NZ NZ537138A patent/NZ537138A/en not_active IP Right Cessation
- 2003-07-16 ES ES03765254T patent/ES2326593T3/es not_active Expired - Lifetime
- 2003-07-18 PE PE2003000717A patent/PE20040678A1/es not_active Application Discontinuation
- 2003-07-18 TW TW092119725A patent/TWI314860B/zh not_active IP Right Cessation
- 2003-07-18 MY MYPI20032711A patent/MY141879A/en unknown
-
2004
- 2004-12-13 IL IL16574504A patent/IL165745A0/xx unknown
- 2004-12-30 HR HR20041233A patent/HRP20041233A2/hr not_active Application Discontinuation
-
2005
- 2005-01-18 CR CR7657A patent/CR7657A/es unknown
- 2005-01-19 EC EC2005005549A patent/ECSP055549A/es unknown
- 2005-01-20 CO CO05004232A patent/CO5680445A2/es not_active Application Discontinuation
- 2005-02-16 NO NO20050832A patent/NO20050832L/no not_active Application Discontinuation
- 2005-10-28 HK HK05109638.4A patent/HK1078003A1/xx not_active IP Right Cessation
-
2008
- 2008-04-09 US US12/100,093 patent/US7585977B2/en not_active Expired - Fee Related
-
2010
- 2010-05-11 JP JP2010109009A patent/JP5220800B2/ja not_active Expired - Fee Related
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