CN103140479B - 制造嘧啶衍生物的方法 - Google Patents
制造嘧啶衍生物的方法 Download PDFInfo
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- CN103140479B CN103140479B CN201180047753.2A CN201180047753A CN103140479B CN 103140479 B CN103140479 B CN 103140479B CN 201180047753 A CN201180047753 A CN 201180047753A CN 103140479 B CN103140479 B CN 103140479B
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- 0 CCN(CCOC)*1=NC(*C)=C(*)C*1(C)* Chemical compound CCN(CCOC)*1=NC(*C)=C(*)C*1(C)* 0.000 description 3
- UOTUSCSUVVKJNJ-UHFFFAOYSA-N CC(Nc(nc1)cc(C(F)(F)F)c1Br)=O Chemical compound CC(Nc(nc1)cc(C(F)(F)F)c1Br)=O UOTUSCSUVVKJNJ-UHFFFAOYSA-N 0.000 description 1
- RWGBXAQMUBGGKQ-UHFFFAOYSA-N Nc1nccc(C(F)(F)F)c1 Chemical compound Nc1nccc(C(F)(F)F)c1 RWGBXAQMUBGGKQ-UHFFFAOYSA-N 0.000 description 1
- KZNICNPSHKQLFF-UHFFFAOYSA-N O=C(CC1)NC1=O Chemical compound O=C(CC1)NC1=O KZNICNPSHKQLFF-UHFFFAOYSA-N 0.000 description 1
- PCLIMKBDDGJMGD-UHFFFAOYSA-N O=C(CCC1=O)N1Br Chemical compound O=C(CCC1=O)N1Br PCLIMKBDDGJMGD-UHFFFAOYSA-N 0.000 description 1
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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/72—Nitrogen atoms
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/04—Esters of boric acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Pyridine Compounds (AREA)
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510157366.4A CN104945373A (zh) | 2010-10-01 | 2011-09-29 | 制造嘧啶衍生物的方法 |
| CN201510156027.4A CN104987321A (zh) | 2010-10-01 | 2011-09-29 | 制造嘧啶衍生物的方法 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38872110P | 2010-10-01 | 2010-10-01 | |
| US61/388,721 | 2010-10-01 | ||
| US201161494915P | 2011-06-09 | 2011-06-09 | |
| US61/494,915 | 2011-06-09 | ||
| PCT/US2011/053808 WO2012044727A2 (en) | 2010-10-01 | 2011-09-29 | Manufacturing process for pyrimidine derivatives |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510157366.4A Division CN104945373A (zh) | 2010-10-01 | 2011-09-29 | 制造嘧啶衍生物的方法 |
| CN201510156027.4A Division CN104987321A (zh) | 2010-10-01 | 2011-09-29 | 制造嘧啶衍生物的方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103140479A CN103140479A (zh) | 2013-06-05 |
| CN103140479B true CN103140479B (zh) | 2015-04-08 |
Family
ID=44773179
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201180047753.2A Active CN103140479B (zh) | 2010-10-01 | 2011-09-29 | 制造嘧啶衍生物的方法 |
| CN201510156027.4A Pending CN104987321A (zh) | 2010-10-01 | 2011-09-29 | 制造嘧啶衍生物的方法 |
| CN201510157366.4A Pending CN104945373A (zh) | 2010-10-01 | 2011-09-29 | 制造嘧啶衍生物的方法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510156027.4A Pending CN104987321A (zh) | 2010-10-01 | 2011-09-29 | 制造嘧啶衍生物的方法 |
| CN201510157366.4A Pending CN104945373A (zh) | 2010-10-01 | 2011-09-29 | 制造嘧啶衍生物的方法 |
Country Status (30)
| Country | Link |
|---|---|
| US (3) | US9181215B2 (https=) |
| EP (2) | EP2621908A2 (https=) |
| JP (3) | JP5998145B2 (https=) |
| KR (2) | KR20180123586A (https=) |
| CN (3) | CN103140479B (https=) |
| AR (1) | AR083213A1 (https=) |
| AU (4) | AU2011308856B2 (https=) |
| BR (1) | BR112013007123B1 (https=) |
| CA (1) | CA2813333C (https=) |
| CL (2) | CL2013000850A1 (https=) |
| CO (1) | CO6700837A2 (https=) |
| DK (1) | DK3040333T3 (https=) |
| EC (1) | ECSP13012596A (https=) |
| ES (1) | ES2699951T3 (https=) |
| GT (1) | GT201300080A (https=) |
| HU (1) | HUE041326T2 (https=) |
| IL (3) | IL225113A (https=) |
| LT (1) | LT3040333T (https=) |
| MX (1) | MX354482B (https=) |
| MY (1) | MY160785A (https=) |
| NZ (1) | NZ608285A (https=) |
| PE (1) | PE20140002A1 (https=) |
| PH (2) | PH12013500579A1 (https=) |
| PL (1) | PL3040333T3 (https=) |
| PT (1) | PT3040333T (https=) |
| RU (2) | RU2576619C2 (https=) |
| SG (1) | SG188439A1 (https=) |
| SI (1) | SI3040333T1 (https=) |
| TW (1) | TWI540133B (https=) |
| WO (1) | WO2012044727A2 (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103635189B (zh) | 2011-07-01 | 2016-05-04 | 诺华股份有限公司 | 用于治疗癌症的含有cdk4/6抑制剂和pi3k抑制剂的联合治疗 |
| KR20140069235A (ko) | 2011-09-27 | 2014-06-09 | 노파르티스 아게 | 돌연변이체 idh의 억제제로서의 3-피리미딘-4-일-옥사졸리딘-2-온 |
| UY34632A (es) | 2012-02-24 | 2013-05-31 | Novartis Ag | Compuestos de oxazolidin- 2- ona y usos de los mismos |
| PL2912030T3 (pl) * | 2012-10-23 | 2017-02-28 | Novartis Ag | Ulepszony sposób wytwarzania 5-(2,6-di-4-morfolinylo-4-pirymidynylo)-4- trifluorometylopirydyno-2-aminy |
| US9296733B2 (en) | 2012-11-12 | 2016-03-29 | Novartis Ag | Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases |
| EP2970240B1 (en) | 2013-03-14 | 2018-01-10 | Novartis AG | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh |
| US9318944B2 (en) | 2013-04-29 | 2016-04-19 | Rockwell Automation Technologies, Inc. | Methods and apparatus for active front end filter capacitor degradation detection |
| US9294005B2 (en) | 2013-10-01 | 2016-03-22 | Rockwell Automation Technologies, Inc. | Method and apparatus for detecting AFE filter capacitor degradation |
| NZ718487A (en) * | 2013-10-16 | 2020-01-31 | Shanghai Yingli Pharm Co Ltd | Fused heterocyclic compound, preparation method therefor, pharmaceutical composition, and uses thereof |
| RU2688665C2 (ru) * | 2014-04-22 | 2019-05-22 | Университет Базель | Новый способ получения производных триазина, пиримидина и пиридина |
| CN105085476B (zh) * | 2014-11-24 | 2018-03-09 | 苏州晶云药物科技有限公司 | 5‑[2,6‑二(4‑吗啉基)‑4‑嘧啶基]‑4‑(三氟甲基)‑2‑吡啶胺二盐酸盐的晶型及其制备方法 |
| AU2015366357B2 (en) * | 2014-12-17 | 2018-07-19 | Shanghai Haiyan Pharmaceutical Technology Co. Ltd. | 2-morpholin-4,6-disubstituted pyrimidine derivative, and preparation method and pharmaceutical use thereof |
| US9481665B2 (en) * | 2015-03-13 | 2016-11-01 | Yong Xu | Process for preparing PI3K inhibitor buparsilib |
| EP3273959A1 (en) | 2015-03-25 | 2018-01-31 | Novartis Ag | Pharmaceutical combinations |
| CN105001151B (zh) * | 2015-08-28 | 2017-07-14 | 苏州明锐医药科技有限公司 | 布帕尼西中间体及其制备方法 |
| CN106543140A (zh) * | 2015-09-21 | 2017-03-29 | 苏州晶云药物科技有限公司 | 5-[2,6-二(4-吗啉基)-4-嘧啶基]-4-(三氟甲基)-2-吡啶胺盐酸盐的晶型及其制备方法 |
| PL3978500T3 (pl) * | 2015-12-16 | 2024-03-11 | Genentech, Inc. | Sposób wytwarzania tricyklicznych związków inhibitorów pi3k |
| CN106905294A (zh) * | 2016-07-08 | 2017-06-30 | 苏州科睿思制药有限公司 | 5‑[2,6‑二(4‑吗啉基)‑4‑嘧啶基]‑4‑(三氟甲基)‑2‑吡啶胺的晶型及其制备方法 |
| CN107793394A (zh) * | 2017-08-03 | 2018-03-13 | 上海厚璞生物科技有限公司 | 一种生产选择性pi3k抑制剂的系列关键中间体 |
| CN110016142B (zh) * | 2019-04-30 | 2021-08-03 | 合肥工业大学 | 一种含嘧啶硼酸结构的硅油及其制备方法 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101389622A (zh) * | 2006-01-20 | 2009-03-18 | 诺瓦提斯公司 | 用作pi-3激酶抑制剂的嘧啶衍生物 |
| WO2009066084A1 (en) * | 2007-11-21 | 2009-05-28 | F. Hoffmann-La Roche Ag | 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors |
| WO2010130779A2 (en) * | 2009-05-15 | 2010-11-18 | Novartis Ag | COMBINATION OF A PBOSPBOINOSITKLE 3-KSπASE INHIBITOR AND AN ANTIDIABETIC COMPOUND |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6124476A (en) | 1998-04-17 | 2000-09-26 | Symyx Technologies, Inc. | Catalyst ligands, catalyst compositions, catalyst metal complexes and processes for cross-coupling aromatic boron compounds with aromatic halogens or perfluoroalkylsulfonates |
| CN1735598A (zh) * | 2002-11-11 | 2006-02-15 | 拜耳医药保健股份公司 | 作为ip受体拮抗剂的苯基或杂芳基氨基烷烃衍生物 |
| US7423148B2 (en) | 2002-11-21 | 2008-09-09 | Chiron Corporation | Small molecule PI 3-kinase inhibitors and methods of their use |
| MX2009002046A (es) | 2006-08-24 | 2009-03-06 | Astrazeneca Ab | Derivados de morfolino pirimidina utiles en el tratamiento de trastornos proliferativos. |
| WO2008098058A1 (en) | 2007-02-06 | 2008-08-14 | Novartis Ag | Pi 3-kinase inhibitors and methods of their use |
-
2011
- 2011-09-29 EP EP11767362.4A patent/EP2621908A2/en not_active Withdrawn
- 2011-09-29 US US13/825,880 patent/US9181215B2/en active Active
- 2011-09-29 SI SI201131619T patent/SI3040333T1/sl unknown
- 2011-09-29 AR ARP110103595A patent/AR083213A1/es unknown
- 2011-09-29 CN CN201180047753.2A patent/CN103140479B/zh active Active
- 2011-09-29 PT PT16151719T patent/PT3040333T/pt unknown
- 2011-09-29 LT LTEP16151719.8T patent/LT3040333T/lt unknown
- 2011-09-29 ES ES16151719T patent/ES2699951T3/es active Active
- 2011-09-29 CN CN201510156027.4A patent/CN104987321A/zh active Pending
- 2011-09-29 PH PH1/2013/500579A patent/PH12013500579A1/en unknown
- 2011-09-29 CN CN201510157366.4A patent/CN104945373A/zh active Pending
- 2011-09-29 MY MYPI2013000811A patent/MY160785A/en unknown
- 2011-09-29 JP JP2013531796A patent/JP5998145B2/ja active Active
- 2011-09-29 EP EP16151719.8A patent/EP3040333B1/en active Active
- 2011-09-29 MX MX2013003507A patent/MX354482B/es active IP Right Grant
- 2011-09-29 CA CA2813333A patent/CA2813333C/en active Active
- 2011-09-29 RU RU2013120326/04A patent/RU2576619C2/ru active
- 2011-09-29 BR BR112013007123-0A patent/BR112013007123B1/pt active IP Right Grant
- 2011-09-29 PL PL16151719T patent/PL3040333T3/pl unknown
- 2011-09-29 RU RU2015150728A patent/RU2015150728A/ru unknown
- 2011-09-29 KR KR1020187032263A patent/KR20180123586A/ko not_active Ceased
- 2011-09-29 NZ NZ608285A patent/NZ608285A/en not_active IP Right Cessation
- 2011-09-29 SG SG2013016837A patent/SG188439A1/en unknown
- 2011-09-29 WO PCT/US2011/053808 patent/WO2012044727A2/en not_active Ceased
- 2011-09-29 KR KR1020137011172A patent/KR20130119928A/ko not_active Ceased
- 2011-09-29 PE PE2013000654A patent/PE20140002A1/es active IP Right Grant
- 2011-09-29 HU HUE16151719A patent/HUE041326T2/hu unknown
- 2011-09-29 DK DK16151719.8T patent/DK3040333T3/da active
- 2011-09-29 AU AU2011308856A patent/AU2011308856B2/en not_active Ceased
- 2011-09-30 TW TW100135673A patent/TWI540133B/zh active
-
2013
- 2013-03-07 IL IL225113A patent/IL225113A/en unknown
- 2013-03-22 CO CO13057091A patent/CO6700837A2/es unknown
- 2013-03-22 GT GT201300080A patent/GT201300080A/es unknown
- 2013-03-28 CL CL2013000850A patent/CL2013000850A1/es unknown
- 2013-04-30 EC ECSP13012596 patent/ECSP13012596A/es unknown
-
2014
- 2014-06-19 IL IL233282A patent/IL233282A/en unknown
-
2015
- 2015-02-24 AU AU2015200938A patent/AU2015200938B2/en not_active Ceased
- 2015-02-24 AU AU2015200936A patent/AU2015200936A1/en not_active Abandoned
- 2015-03-30 IL IL238046A patent/IL238046A/en not_active IP Right Cessation
- 2015-04-27 CL CL2015001088A patent/CL2015001088A1/es unknown
- 2015-05-06 US US14/705,013 patent/US9359326B2/en not_active Expired - Fee Related
- 2015-07-20 PH PH12015501585A patent/PH12015501585A1/en unknown
- 2015-10-23 AU AU2015246141A patent/AU2015246141B2/en not_active Ceased
- 2015-12-17 JP JP2015246501A patent/JP2016128414A/ja active Pending
- 2015-12-17 JP JP2015246502A patent/JP2016106091A/ja active Pending
-
2016
- 2016-05-06 US US15/147,986 patent/US9452994B2/en not_active Expired - Fee Related
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101389622A (zh) * | 2006-01-20 | 2009-03-18 | 诺瓦提斯公司 | 用作pi-3激酶抑制剂的嘧啶衍生物 |
| WO2009066084A1 (en) * | 2007-11-21 | 2009-05-28 | F. Hoffmann-La Roche Ag | 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors |
| WO2010130779A2 (en) * | 2009-05-15 | 2010-11-18 | Novartis Ag | COMBINATION OF A PBOSPBOINOSITKLE 3-KSπASE INHIBITOR AND AN ANTIDIABETIC COMPOUND |
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