CR20190212A - 1,2,4-triazolonas 2,4,5-trisustituidas - Google Patents
1,2,4-triazolonas 2,4,5-trisustituidasInfo
- Publication number
- CR20190212A CR20190212A CR20190212A CR20190212A CR20190212A CR 20190212 A CR20190212 A CR 20190212A CR 20190212 A CR20190212 A CR 20190212A CR 20190212 A CR20190212 A CR 20190212A CR 20190212 A CR20190212 A CR 20190212A
- Authority
- CR
- Costa Rica
- Prior art keywords
- compounds
- useful
- preparing
- pharmaceutical compositions
- triazolones
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- 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]
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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 ring carbon atoms
- C07D249/12—Oxygen or sulfur atoms
-
- 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
- C07D403/12—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 chain containing hetero atoms as chain links
-
- 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
- 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
- C07D413/12—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 chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
La presente invención proporciona compuestos de triazolona de la fórmula general en donde R1, R2, R3, R4 y R5 son como se definen en la presente, métodos de preparación de dichos compuestos, compuestos intermedios útiles para preparar dichos compuestos, composiciones farmacéuticas y combinaciones que comprenden dichos compuestos y el uso de dichos compuestos para preparar composiciones farmacéuticas para el tratamiento o la profilaxis de enfermedades, en particular de trastornos hiperproliferativos, como un único agente o en combinación con otros ingredientes activosThe present invention provides triazolone compounds compounds of general formula (I) : in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2016/103643 | 2016-10-27 | ||
| US201762569296P | 2017-10-06 | 2017-10-06 | |
| PCT/EP2017/077252 WO2018077923A1 (en) | 2016-10-27 | 2017-10-25 | 2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of dhodh |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CR20190212A true CR20190212A (es) | 2019-06-24 |
Family
ID=60164720
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CR20190212A CR20190212A (es) | 2016-10-27 | 2017-10-25 | 1,2,4-triazolonas 2,4,5-trisustituidas |
Country Status (26)
| Country | Link |
|---|---|
| US (4) | US10815215B2 (es) |
| EP (1) | EP3532468B1 (es) |
| JP (1) | JP7084389B2 (es) |
| KR (1) | KR20190084954A (es) |
| CN (2) | CN110023302B (es) |
| AU (1) | AU2017351688B2 (es) |
| BR (1) | BR112019008458A2 (es) |
| CA (1) | CA3041643A1 (es) |
| CL (1) | CL2019001160A1 (es) |
| CO (1) | CO2019004137A2 (es) |
| CR (1) | CR20190212A (es) |
| CU (1) | CU24572B1 (es) |
| DO (1) | DOP2019000110A (es) |
| EC (1) | ECSP19030002A (es) |
| GE (1) | GEP20217248B (es) |
| IL (1) | IL266214B (es) |
| JO (1) | JOP20190094A1 (es) |
| MX (1) | MX2019005009A (es) |
| NI (1) | NI201900041A (es) |
| PE (1) | PE20191005A1 (es) |
| PH (1) | PH12019500932A1 (es) |
| TN (1) | TN2019000136A1 (es) |
| TW (1) | TW201827414A (es) |
| UA (1) | UA123688C2 (es) |
| UY (1) | UY37461A (es) |
| WO (1) | WO2018077923A1 (es) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JOP20190094A1 (ar) * | 2016-10-27 | 2019-04-25 | Broad Inst Inc | مركبات 1، 2، 4-تريازولون تحمل ثلاثة بدائل عند المواقع 2، 4، 5 مفيدة كمثبطات لديهيدروجيناز ثنائي هيدرو أوروتات (dhodh) |
| US10968216B2 (en) | 2016-10-27 | 2021-04-06 | Bayer Aktiengesellschaft | 4,5-annulated 1,2,4-triazolones |
| TW201945346A (zh) | 2018-04-10 | 2019-12-01 | 德商拜耳廠股份有限公司 | 2,4,5-三取代的1,2,4-***酮之製備方法 |
| EP3553052A1 (en) * | 2018-04-10 | 2019-10-16 | Bayer AG | 5-oxo-4,5-dihydro-1h-1,2,4-triazol derivatives for the treatment of cancer |
| WO2019197269A1 (en) * | 2018-04-11 | 2019-10-17 | Bayer Aktiengesellschaft | Combinations of copanlisib with triazolone derivatives and their use in the treatment of cancer |
| JP7126556B2 (ja) | 2018-09-28 | 2022-08-26 | 富士フイルム株式会社 | シタラビンを含む抗腫瘍剤、シタラビンと併用される抗腫瘍効果増強剤、抗腫瘍用キット、およびシタラビンと併用される抗腫瘍剤 |
| TW202043208A (zh) * | 2019-01-11 | 2020-12-01 | 美商健生生物科技公司 | 二氫乳清酸脫氫酶抑制劑 |
| CN113453680A (zh) * | 2019-02-07 | 2021-09-28 | 詹森生物科技公司 | 二氢乳清酸脱氢酶抑制剂 |
| TW202104207A (zh) * | 2019-04-17 | 2021-02-01 | 美商健生生物科技公司 | 二氫乳清酸脫氫酶抑制劑 |
| EP3750892A1 (en) | 2019-06-14 | 2020-12-16 | Yerevan State University | Novel 5-cyclopropyl-furo[3,4-c]pyridine-3,4(1h,5h)-dione 1,1' substituted derivatives and their uses |
| MX2022002470A (es) * | 2019-08-29 | 2022-03-22 | Janssen Biotech Inc | Inhibidores de dihidroorotato deshidrogenasa sustituidos con urea. |
| WO2021070132A1 (en) * | 2019-10-10 | 2021-04-15 | Janssen Biotech, Inc. | Bi-aryl dihydroorotate dehydrogenase inhibitors |
| CN114222732B (zh) * | 2019-10-28 | 2023-04-04 | 南京明德新药研发有限公司 | 一种尿酸促排剂及其合成方法和其在医药上的应用 |
| CN115427109A (zh) * | 2020-02-04 | 2022-12-02 | 詹森生物科技公司 | 作为二氢乳清酸脱氢酶抑制剂的杂环化合物 |
| ES2929379T3 (es) | 2020-05-20 | 2022-11-28 | Inst Nat Sante Rech Med | Métodos para el tratamiento de infecciones por coronavirus |
| WO2021240424A1 (en) | 2020-05-29 | 2021-12-02 | Janssen Biotech, Inc. | Indazole and benzoisoxazole dihydroorotate dehydrogenase inhibitors |
| US20230257362A1 (en) * | 2020-05-29 | 2023-08-17 | Medshine Discovery Inc. | Triazolone compound |
| WO2021240429A1 (en) | 2020-05-29 | 2021-12-02 | Janssen Biotech, Inc. | Benzofuran and benzopyran dihydroorotate dehydrogenase inhibitors |
| WO2021240423A1 (en) * | 2020-05-29 | 2021-12-02 | Janssen Biotech, Inc. | Dihydroorotate dehydrogenase inhibitors |
| CN116804004A (zh) * | 2020-07-14 | 2023-09-26 | 南京征祥医药有限公司 | 作为dhodh抑制剂的化合物 |
| CN111773214B (zh) * | 2020-07-17 | 2021-04-20 | 中国人民解放军军事科学院军事医学研究院 | 2,4,5-三取代的1,2,4-***酮在制备抗病毒药物中的用途 |
| EP3960170A1 (en) | 2020-08-25 | 2022-03-02 | Bayer AG | Dosing schedule for a method of treatment with dhodh inhibitors |
| GB2598624A (en) * | 2020-09-07 | 2022-03-09 | Lorico Aurelio | Use of triazole analogues for inhibition of a tripartite VOR protein complex in multicellular organisms |
| CN116249702A (zh) * | 2020-09-28 | 2023-06-09 | 微境生物医药科技(上海)有限公司 | 用作dhodh抑制剂的1,2,4-***酮衍生物 |
| WO2022070071A1 (en) * | 2020-09-30 | 2022-04-07 | Janssen Biotech, Inc. | Dihydroorotate dehydrogenase inhibitors |
| WO2022070069A1 (en) * | 2020-09-30 | 2022-04-07 | Janssen Biotech, Inc. | Dihydroorotate dehydrogenase inhibitors |
| WO2022167402A1 (en) | 2021-02-02 | 2022-08-11 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods of therapy comprising administering a therapeutically effective combination comprising a dhodh inhibitor and an idh inhibitor |
| WO2023280181A1 (zh) * | 2021-07-05 | 2023-01-12 | 微境生物医药科技(上海)有限公司 | 用作dhodh抑制剂的1,2,4-***酮衍生物及其制备方法和用途 |
| WO2023093812A1 (zh) * | 2021-11-26 | 2023-06-01 | 南京明德新药研发有限公司 | 三氮唑酮类化合物的晶型及其应用 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US4098896A (en) | 1975-09-29 | 1978-07-04 | Chevron Research Company | 1-Halohydrocarbylthio-3-hydrocarbylthio-4-substituted-1,2,4-delta2 -triazolidin-5-ones |
| DE3936623A1 (de) | 1989-11-03 | 1991-05-08 | Bayer Ag | Sulfonylaminocarbonyltriazolinone mit ueber schwefel gebundenen substituenten |
| DE3709574A1 (de) | 1987-03-24 | 1988-10-06 | Bayer Ag | Substituierte triazolinone |
| DE3936622A1 (de) | 1989-11-03 | 1991-05-08 | Bayer Ag | Halogenierte sulfonylaminocarbonyltriazolinone |
| DE3934081A1 (de) | 1989-10-12 | 1991-04-18 | Bayer Ag | Sulfonylaminocarbonyltriazolinone |
| DE4110795A1 (de) | 1991-04-04 | 1992-10-08 | Bayer Ag | Sulfonylaminocarbonyltriazolinone mit ueber sauerstoff gebundenen substituenten |
| DE3916208A1 (de) | 1989-05-18 | 1990-11-22 | Bayer Ag | Substituierte triazolone |
| DE4342190A1 (de) | 1993-12-10 | 1995-06-14 | Bayer Ag | Verfahren und neue Zwischenprodukte zur Herstellung von Triazolinonen |
| DE4433968A1 (de) | 1994-09-23 | 1996-03-28 | Bayer Ag | Verfahren zur Herstellung von Alkoxytriazolinonen |
| DE19627901A1 (de) | 1996-07-11 | 1998-01-15 | Bayer Ag | Substituierte aromatische Carbonylverbindungen und ihre Derivate |
| US6444613B1 (en) | 1999-03-12 | 2002-09-03 | Hoechst Schering Agrevo Gmbh | Defoliant |
| WO2010077686A1 (en) | 2008-12-08 | 2010-07-08 | Sirtris Pharmaceuticals, Inc. | Isoindolinone and related analogs as sirtuin modulators |
| US20100184815A1 (en) | 2008-12-19 | 2010-07-22 | Luehr Gary W | Agonists of peroxisome proliferator activated receptor-alpha |
| KR101796483B1 (ko) | 2010-09-01 | 2017-11-10 | 바이엘 인텔렉쳐 프로퍼티 게엠베하 | Ｎ-(테트라졸-5-일)- 및 ｎ-(트리아졸-5-일)아릴카복사미드 및 제초제로서의 그의 용도 |
| EP2675440B1 (en) | 2011-02-14 | 2020-03-25 | Merck Sharp & Dohme Corp. | Cathepsin cysteine protease inhibitors |
| CN103006645A (zh) * | 2011-09-27 | 2013-04-03 | 华东理工大学 | 2-氨基苯并噻唑衍生物作为dhodh抑制剂的应用 |
| TWI568722B (zh) * | 2012-06-15 | 2017-02-01 | 葛蘭馬克製藥公司 | 作爲ｍＰＧＥＳ－１抑制劑之***酮化合物 |
| US20160251341A1 (en) | 2015-02-27 | 2016-09-01 | Verseon Corporation | Substituted triazole compounds as serine protease inhibitors |
| CN106543139B (zh) | 2015-09-17 | 2020-03-17 | 沈阳中化农药化工研发有限公司 | 一种***酮类化合物及其用途 |
| JOP20190094A1 (ar) | 2016-10-27 | 2019-04-25 | Broad Inst Inc | مركبات 1، 2، 4-تريازولون تحمل ثلاثة بدائل عند المواقع 2، 4، 5 مفيدة كمثبطات لديهيدروجيناز ثنائي هيدرو أوروتات (dhodh) |
-
2017
- 2017-06-16 JO JOP/2019/0094A patent/JOP20190094A1/ar unknown
- 2017-10-25 KR KR1020197011905A patent/KR20190084954A/ko not_active Application Discontinuation
- 2017-10-25 CU CU2019000045A patent/CU24572B1/es unknown
- 2017-10-25 CN CN201780066589.7A patent/CN110023302B/zh active Active
- 2017-10-25 CN CN202210811374.6A patent/CN115557907A/zh active Pending
- 2017-10-25 TN TNP/2019/000136A patent/TN2019000136A1/en unknown
- 2017-10-25 WO PCT/EP2017/077252 patent/WO2018077923A1/en unknown
- 2017-10-25 UA UAA201905676A patent/UA123688C2/uk unknown
- 2017-10-25 US US16/345,168 patent/US10815215B2/en active Active
- 2017-10-25 GE GEAP201715096A patent/GEP20217248B/en unknown
- 2017-10-25 CR CR20190212A patent/CR20190212A/es unknown
- 2017-10-25 PE PE2019000896A patent/PE20191005A1/es unknown
- 2017-10-25 MX MX2019005009A patent/MX2019005009A/es unknown
- 2017-10-25 JP JP2019522859A patent/JP7084389B2/ja active Active
- 2017-10-25 AU AU2017351688A patent/AU2017351688B2/en not_active Expired - Fee Related
- 2017-10-25 BR BR112019008458A patent/BR112019008458A2/pt not_active IP Right Cessation
- 2017-10-25 CA CA3041643A patent/CA3041643A1/en active Pending
- 2017-10-25 EP EP17788234.7A patent/EP3532468B1/en active Active
- 2017-10-27 TW TW106137255A patent/TW201827414A/zh unknown
- 2017-10-27 UY UY0001037461A patent/UY37461A/es not_active Application Discontinuation
-
2019
- 2019-04-23 IL IL266214A patent/IL266214B/en unknown
- 2019-04-25 PH PH12019500932A patent/PH12019500932A1/en unknown
- 2019-04-26 EC ECSENADI201930002A patent/ECSP19030002A/es unknown
- 2019-04-26 CL CL2019001160A patent/CL2019001160A1/es unknown
- 2019-04-26 CO CONC2019/0004137A patent/CO2019004137A2/es unknown
- 2019-04-26 DO DO2019000110A patent/DOP2019000110A/es unknown
- 2019-04-26 NI NI201900041A patent/NI201900041A/es unknown
-
2020
- 2020-08-18 US US16/996,721 patent/US11130745B2/en active Active
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2021
- 2021-08-20 US US17/407,951 patent/US11713304B2/en active Active
-
2023
- 2023-04-20 US US18/137,281 patent/US20230365524A1/en active Pending
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