JP2015509512A5 - - Google Patents
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- JP2015509512A5 JP2015509512A5 JP2014560264A JP2014560264A JP2015509512A5 JP 2015509512 A5 JP2015509512 A5 JP 2015509512A5 JP 2014560264 A JP2014560264 A JP 2014560264A JP 2014560264 A JP2014560264 A JP 2014560264A JP 2015509512 A5 JP2015509512 A5 JP 2015509512A5
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- JP
- Japan
- Prior art keywords
- het
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- atoms
- disease
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 206010028980 Neoplasm Diseases 0.000 claims description 8
- 201000011510 cancer Diseases 0.000 claims description 4
- 210000004369 blood Anatomy 0.000 claims description 3
- 239000008280 blood Substances 0.000 claims description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 2
- -1 2,3-dihydro-benzo [1,4] dioxinyl Chemical group 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 9
- 239000003814 drug Substances 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 239000012453 solvate Substances 0.000 claims 7
- 125000004432 carbon atom Chemical group C* 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 5
- 230000002265 prevention Effects 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 3
- 241000222722 Leishmania <genus> Species 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 125000002393 azetidinyl group Chemical group 0.000 claims 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 2
- 125000001070 dihydroindolyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 2
- 125000005052 dihydropyrazolyl group Chemical group N1(NCC=C1)* 0.000 claims 2
- 125000004925 dihydropyridyl group Chemical group N1(CC=CC=C1)* 0.000 claims 2
- 125000005054 dihydropyrrolyl group Chemical group [H]C1=C([H])C([H])([H])C([H])([H])N1* 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000005945 imidazopyridyl group Chemical group 0.000 claims 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000003566 oxetanyl group Chemical group 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000005493 quinolyl group Chemical group 0.000 claims 2
- 210000002784 stomach Anatomy 0.000 claims 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 2
- 125000005942 tetrahydropyridyl group Chemical group 0.000 claims 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 201000003076 Angiosarcoma Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 1
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 1
- 208000005243 Chondrosarcoma Diseases 0.000 claims 1
- 208000020406 Creutzfeldt Jacob disease Diseases 0.000 claims 1
- 208000003407 Creutzfeldt-Jakob Syndrome Diseases 0.000 claims 1
- 208000010859 Creutzfeldt-Jakob disease Diseases 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 208000007465 Giant cell arteritis Diseases 0.000 claims 1
- 208000001258 Hemangiosarcoma Diseases 0.000 claims 1
- 241000711549 Hepacivirus C Species 0.000 claims 1
- 241000701044 Human gammaherpesvirus 4 Species 0.000 claims 1
- 241000725303 Human immunodeficiency virus Species 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010024229 Leprosy Diseases 0.000 claims 1
- 206010024305 Leukaemia monocytic Diseases 0.000 claims 1
- 241000186367 Mycobacterium avium Species 0.000 claims 1
- 201000004404 Neurofibroma Diseases 0.000 claims 1
- 208000036110 Neuroinflammatory disease Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 208000025747 Rheumatic disease Diseases 0.000 claims 1
- 241000700584 Simplexvirus Species 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 206010044688 Trisomy 21 Diseases 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 206010002022 amyloidosis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 125000005879 dioxolanyl group Chemical group 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 210000000981 epithelium Anatomy 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 210000004602 germ cell Anatomy 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 230000001900 immune effect Effects 0.000 claims 1
- 210000000987 immune system Anatomy 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 210000000936 intestine Anatomy 0.000 claims 1
- 208000037906 ischaemic injury Diseases 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 210000000867 larynx Anatomy 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 201000005249 lung adenocarcinoma Diseases 0.000 claims 1
- 208000037841 lung tumor Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 210000004324 lymphatic system Anatomy 0.000 claims 1
- 201000004792 malaria Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 230000002503 metabolic effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 201000006894 monocytic leukemia Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 210000003739 neck Anatomy 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 244000045947 parasite Species 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 230000000552 rheumatic effect Effects 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 206010043207 temporal arteritis Diseases 0.000 claims 1
- 230000001732 thrombotic effect Effects 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 210000001519 tissue Anatomy 0.000 claims 1
- 201000008827 tuberculosis Diseases 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 102000004632 fms-Like Tyrosine Kinase 3 Human genes 0.000 description 8
- 108010003374 fms-Like Tyrosine Kinase 3 Proteins 0.000 description 8
- 210000004027 cell Anatomy 0.000 description 4
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 description 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 description 2
- 230000035772 mutation Effects 0.000 description 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 description 1
- 208000032800 BCR-ABL1 positive blast phase chronic myelogenous leukemia Diseases 0.000 description 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 description 1
- 208000004860 Blast Crisis Diseases 0.000 description 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 description 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 description 1
- 108091000080 Phosphotransferase Proteins 0.000 description 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 description 1
- 102000001253 Protein Kinase Human genes 0.000 description 1
- 108091005682 Receptor kinases Proteins 0.000 description 1
- 230000003213 activating effect Effects 0.000 description 1
- 230000024245 cell differentiation Effects 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 230000007012 clinical effect Effects 0.000 description 1
- 230000018109 developmental process Effects 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 210000003958 hematopoietic stem cell Anatomy 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 102000020233 phosphotransferase Human genes 0.000 description 1
- 238000010837 poor prognosis Methods 0.000 description 1
- 210000000130 stem cell Anatomy 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12001568 | 2012-03-07 | ||
| EP12001568.0 | 2012-03-07 | ||
| PCT/EP2013/000440 WO2013131609A1 (en) | 2012-03-07 | 2013-02-14 | Triazolopyrazine derivatives |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015509512A JP2015509512A (ja) | 2015-03-30 |
| JP2015509512A5 true JP2015509512A5 (enExample) | 2016-03-31 |
| JP6049768B2 JP6049768B2 (ja) | 2016-12-21 |
Family
ID=47715983
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014560264A Expired - Fee Related JP6049768B2 (ja) | 2012-03-07 | 2013-02-14 | トリアゾロピラジン誘導体 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20150051202A1 (enExample) |
| EP (1) | EP2822948B1 (enExample) |
| JP (1) | JP6049768B2 (enExample) |
| CN (1) | CN104159901B (enExample) |
| AR (1) | AR090240A1 (enExample) |
| AU (1) | AU2013230286B2 (enExample) |
| CA (1) | CA2866450C (enExample) |
| ES (1) | ES2579981T3 (enExample) |
| HK (1) | HK1203948A1 (enExample) |
| IL (1) | IL234466A (enExample) |
| TW (1) | TW201341384A (enExample) |
| WO (1) | WO2013131609A1 (enExample) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20160747A1 (es) * | 2013-06-10 | 2016-08-25 | Bayer Pharma AG | Derivados heterociclicos inhibidores de la quinasa mps-1 |
| JP6392352B2 (ja) * | 2013-12-19 | 2018-09-19 | ノバルティス アーゲー | リーシュマニア症などの寄生虫病を処置するための原生動物のプロテアソーム阻害剤としての［１，２，４］トリアゾロ［１，５−ａ］ピリミジン誘導体 |
| LT3105218T (lt) | 2014-02-13 | 2019-12-10 | Incyte Corp | Ciklopropilaminai kaip lsd1 inhibitoriai |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| WO2015123424A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| EP3392244A1 (en) | 2014-02-13 | 2018-10-24 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| WO2016007731A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyridines and imidazopyrazines as lsd1 inhibitors |
| US9758523B2 (en) | 2014-07-10 | 2017-09-12 | Incyte Corporation | Triazolopyridines and triazolopyrazines as LSD1 inhibitors |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| WO2016007736A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyrazines as lsd1 inhibitors |
| CN107108556B (zh) | 2014-11-03 | 2020-09-29 | 艾欧米制药有限公司 | 药用化合物 |
| EA201792205A1 (ru) | 2015-04-03 | 2018-02-28 | Инсайт Корпорейшн | Гетероциклические соединения как ингибиторы lsd1 |
| DK3334709T3 (da) | 2015-08-12 | 2025-02-03 | Incyte Holdings Corp | Salte af en lsd1-hæmmer |
| CA3021678A1 (en) | 2016-04-22 | 2017-10-26 | Incyte Corporation | Formulations of an lsd1 inhibitor |
| PL3498693T3 (pl) * | 2016-08-10 | 2025-03-24 | Takeda Pharmaceutical Company Limited | Związek heterocykliczny |
| WO2018119440A1 (en) | 2016-12-22 | 2018-06-28 | Calithera Biosciences, Inc. | Compositions and methods for inhibiting arginase activity |
| CA3089762A1 (en) * | 2018-01-29 | 2019-08-01 | Merck Patent Gmbh | Gcn2 inhibitors and uses thereof |
| AU2019212969B2 (en) * | 2018-01-29 | 2025-01-23 | Merck Patent Gmbh | GCN2 inhibitors and uses thereof |
| CN117304191A (zh) * | 2018-07-05 | 2023-12-29 | 因赛特公司 | 作为a2a/a2b抑制剂的稠合吡嗪衍生物 |
| US10968200B2 (en) | 2018-08-31 | 2021-04-06 | Incyte Corporation | Salts of an LSD1 inhibitor and processes for preparing the same |
| KR20220058553A (ko) * | 2019-09-05 | 2022-05-09 | 루난 파마슈티컬 그룹 코퍼레이션 | Magl 억제제 및 이의 제조 방법, 용도 |
| GB202008749D0 (en) | 2020-06-09 | 2020-07-22 | Ip2Ipo Innovations Ltd | Novel compounds |
| CN117355531A (zh) * | 2021-06-23 | 2024-01-05 | 吉利德科学公司 | 二酰基甘油激酶调节化合物 |
| CN115819425A (zh) * | 2022-12-22 | 2023-03-21 | 五邑大学 | 一种三唑并六元氮杂环-2-胺类化合物及其制备方法和应用 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9624482D0 (en) | 1995-12-18 | 1997-01-15 | Zeneca Phaema S A | Chemical compounds |
| CA2242425C (en) | 1996-02-13 | 2006-07-18 | Zeneca Limited | Quinazoline derivatives as vegf inhibitors |
| NZ331191A (en) | 1996-03-05 | 2000-03-27 | Zeneca Ltd | 4-anilinoquinazoline derivatives and pharmaceutical compositions thereof |
| GB9718972D0 (en) | 1996-09-25 | 1997-11-12 | Zeneca Ltd | Chemical compounds |
| GB9714249D0 (en) | 1997-07-08 | 1997-09-10 | Angiogene Pharm Ltd | Vascular damaging agents |
| GB9900334D0 (en) | 1999-01-07 | 1999-02-24 | Angiogene Pharm Ltd | Tricylic vascular damaging agents |
| GB9900752D0 (en) | 1999-01-15 | 1999-03-03 | Angiogene Pharm Ltd | Benzimidazole vascular damaging agents |
| BR0111230A (pt) | 2000-05-31 | 2003-06-10 | Astrazeneca Ab | Composto, e, uso e processo para a preparação do mesmo |
| EE200300015A (et) | 2000-07-07 | 2004-10-15 | Angiogene Pharmaceuticals Limited | Kolhinooli derivaadid kui angiogeneesi inhibiitorid |
| KR20030014425A (ko) | 2000-07-07 | 2003-02-17 | 앤지오젠 파마슈티칼스 리미티드 | 혈관 손상제인 콜치놀 유도체 |
| NZ545058A (en) | 2003-07-16 | 2008-05-30 | Janssen Pharmaceutica Nv | Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors |
| JP5704785B2 (ja) | 2004-07-19 | 2015-04-22 | ザ・ジョンズ・ホプキンス・ユニバーシティ | 免疫抑制のためのｆｌｔ３阻害剤 |
| WO2006075023A2 (en) | 2005-01-14 | 2006-07-20 | Janssen Pharmaceutica N.V. | Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors |
| CN101454326A (zh) * | 2006-05-31 | 2009-06-10 | 加拉帕戈斯股份有限公司 | 用于治疗变性和炎性疾病的三唑并吡嗪化合物 |
| TWI453207B (zh) * | 2008-09-08 | 2014-09-21 | Signal Pharm Llc | 胺基三唑并吡啶，其組合物及使用其之治療方法 |
| WO2010141796A2 (en) * | 2009-06-05 | 2010-12-09 | Cephalon, Inc. | PREPARATION AND USES OF 1,2,4-TRIAZOLO [1,5a] PYRIDINE DERIVATIVES |
| PH12012501381A1 (en) * | 2010-01-15 | 2012-10-22 | Janssen Pharmaceuticals Inc | Novel substituted bicyclic triazole derivatives as gamma secretase modulators |
| US20110190269A1 (en) * | 2010-02-01 | 2011-08-04 | Karlheinz Baumann | Gamma secretase modulators |
| CA2809331C (en) * | 2010-08-27 | 2018-09-25 | Merck Patent Gmbh | Triazolopyrazine derivatives |
-
2013
- 2013-02-14 EP EP13704368.3A patent/EP2822948B1/en not_active Not-in-force
- 2013-02-14 WO PCT/EP2013/000440 patent/WO2013131609A1/en not_active Ceased
- 2013-02-14 AU AU2013230286A patent/AU2013230286B2/en not_active Ceased
- 2013-02-14 CA CA2866450A patent/CA2866450C/en not_active Expired - Fee Related
- 2013-02-14 ES ES13704368.3T patent/ES2579981T3/es active Active
- 2013-02-14 CN CN201380012661.XA patent/CN104159901B/zh not_active Expired - Fee Related
- 2013-02-14 JP JP2014560264A patent/JP6049768B2/ja not_active Expired - Fee Related
- 2013-02-14 US US14/382,678 patent/US20150051202A1/en not_active Abandoned
- 2013-02-14 HK HK15104522.2A patent/HK1203948A1/xx unknown
- 2013-03-05 AR ARP130100705A patent/AR090240A1/es unknown
- 2013-03-06 TW TW102107941A patent/TW201341384A/zh unknown
-
2014
- 2014-09-04 IL IL234466A patent/IL234466A/en active IP Right Grant
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