JP2019532054A5 - - Google Patents
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- JP2019532054A5 JP2019532054A5 JP2019515545A JP2019515545A JP2019532054A5 JP 2019532054 A5 JP2019532054 A5 JP 2019532054A5 JP 2019515545 A JP2019515545 A JP 2019515545A JP 2019515545 A JP2019515545 A JP 2019515545A JP 2019532054 A5 JP2019532054 A5 JP 2019532054A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- fluoro
- phenyl
- chloro
- 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.)
- Pending
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- 125000000217 alkyl group Chemical group 0.000 claims description 80
- 125000001153 fluoro group Chemical group F* 0.000 claims description 36
- -1 -OH Chemical group 0.000 claims description 33
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 26
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 22
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 19
- 150000001875 compounds Chemical class 0.000 claims description 19
- 125000001424 substituent group Chemical group 0.000 claims description 19
- 150000003839 salts Chemical class 0.000 claims description 18
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 13
- 125000001072 heteroaryl group Chemical group 0.000 claims description 12
- 125000003118 aryl group Chemical group 0.000 claims description 10
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 9
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 8
- 125000001246 bromo group Chemical group Br* 0.000 claims description 7
- MWUXSHHQAYIFBG-UHFFFAOYSA-N Nitric oxide Chemical compound O=[N] MWUXSHHQAYIFBG-UHFFFAOYSA-N 0.000 claims description 6
- 239000003814 drug Substances 0.000 claims description 6
- 239000002464 receptor antagonist Substances 0.000 claims description 6
- 229940044551 receptor antagonist Drugs 0.000 claims description 6
- SBUKLPSBNFWJCU-UHFFFAOYSA-N ClIBr Chemical compound ClIBr SBUKLPSBNFWJCU-UHFFFAOYSA-N 0.000 claims description 4
- 229940125715 antihistaminic agent Drugs 0.000 claims description 4
- 239000000739 antihistaminic agent Substances 0.000 claims description 4
- 229940079593 drug Drugs 0.000 claims description 4
- 239000003112 inhibitor Substances 0.000 claims description 4
- 108090000312 Calcium Channels Proteins 0.000 claims description 3
- 102000003922 Calcium Channels Human genes 0.000 claims description 3
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims description 3
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 claims description 3
- 239000000674 adrenergic antagonist Substances 0.000 claims description 3
- 239000002170 aldosterone antagonist Substances 0.000 claims description 3
- 229940083712 aldosterone antagonist Drugs 0.000 claims description 3
- 239000002876 beta blocker Substances 0.000 claims description 3
- 229940097320 beta blocking agent Drugs 0.000 claims description 3
- 229940082638 cardiac stimulant phosphodiesterase inhibitors Drugs 0.000 claims description 3
- 239000000496 cardiotonic agent Substances 0.000 claims description 3
- 230000003177 cardiotonic effect Effects 0.000 claims description 3
- 239000002934 diuretic Substances 0.000 claims description 3
- 229940030606 diuretics Drugs 0.000 claims description 3
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims description 3
- 239000003149 muscarinic antagonist Substances 0.000 claims description 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 3
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims description 3
- 239000002571 phosphodiesterase inhibitor Substances 0.000 claims description 3
- 229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 claims description 3
- 150000003222 pyridines Chemical class 0.000 claims description 3
- 239000002461 renin inhibitor Substances 0.000 claims description 3
- 229940086526 renin-inhibitors Drugs 0.000 claims description 3
- 230000003637 steroidlike Effects 0.000 claims description 3
- PXQLVRUNWNTZOS-UHFFFAOYSA-N sulfanyl Chemical class [SH] PXQLVRUNWNTZOS-UHFFFAOYSA-N 0.000 claims description 3
- IZXIZTKNFFYFOF-UHFFFAOYSA-N 2-Oxazolidone Chemical compound O=C1NCCO1 IZXIZTKNFFYFOF-UHFFFAOYSA-N 0.000 claims description 2
- 102000003567 TRPV4 Human genes 0.000 claims description 2
- 101150098315 TRPV4 gene Proteins 0.000 claims description 2
- 102000030619 alpha-1 Adrenergic Receptor Human genes 0.000 claims description 2
- 108020004102 alpha-1 Adrenergic Receptor Proteins 0.000 claims description 2
- 239000005557 antagonist Substances 0.000 claims description 2
- 229940124599 anti-inflammatory drug Drugs 0.000 claims description 2
- 102000012740 beta Adrenergic Receptors Human genes 0.000 claims description 2
- 108010079452 beta Adrenergic Receptors Proteins 0.000 claims description 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 2
- 108091006073 receptor regulators Proteins 0.000 claims description 2
- 238000000034 method Methods 0.000 claims 19
- 125000004043 oxo group Chemical group O=* 0.000 claims 17
- 206010011224 Cough Diseases 0.000 claims 16
- 206010030113 Oedema Diseases 0.000 claims 14
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- 206010003445 Ascites Diseases 0.000 claims 6
- 208000002193 Pain Diseases 0.000 claims 6
- 208000003251 Pruritus Diseases 0.000 claims 6
- 230000000968 intestinal effect Effects 0.000 claims 6
- 208000005264 motor neuron disease Diseases 0.000 claims 6
- 206010019280 Heart failures Diseases 0.000 claims 5
- 208000004852 Lung Injury Diseases 0.000 claims 5
- 206010069363 Traumatic lung injury Diseases 0.000 claims 5
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 5
- 231100000515 lung injury Toxicity 0.000 claims 5
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 4
- 206010048962 Brain oedema Diseases 0.000 claims 4
- 206010020772 Hypertension Diseases 0.000 claims 4
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 4
- 206010069351 acute lung injury Diseases 0.000 claims 4
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 4
- 208000006752 brain edema Diseases 0.000 claims 4
- 208000013116 chronic cough Diseases 0.000 claims 4
- 230000004064 dysfunction Effects 0.000 claims 4
- 208000024827 Alzheimer disease Diseases 0.000 claims 3
- 201000001320 Atherosclerosis Diseases 0.000 claims 3
- 208000024172 Cardiovascular disease Diseases 0.000 claims 3
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 3
- 208000015943 Coeliac disease Diseases 0.000 claims 3
- 208000011231 Crohn disease Diseases 0.000 claims 3
- 208000026292 Cystic Kidney disease Diseases 0.000 claims 3
- 201000004624 Dermatitis Diseases 0.000 claims 3
- 206010012735 Diarrhoea Diseases 0.000 claims 3
- 201000009273 Endometriosis Diseases 0.000 claims 3
- 206010016807 Fluid retention Diseases 0.000 claims 3
- 208000010412 Glaucoma Diseases 0.000 claims 3
- 208000035202 High altitude pulmonary edema Diseases 0.000 claims 3
- 206010020751 Hypersensitivity Diseases 0.000 claims 3
- 206010020853 Hypertonic bladder Diseases 0.000 claims 3
- 206010062016 Immunosuppression Diseases 0.000 claims 3
- 206010021639 Incontinence Diseases 0.000 claims 3
- 206010061218 Inflammation Diseases 0.000 claims 3
- 201000010538 Lactose Intolerance Diseases 0.000 claims 3
- 208000019695 Migraine disease Diseases 0.000 claims 3
- 208000008589 Obesity Diseases 0.000 claims 3
- 208000009722 Overactive Urinary Bladder Diseases 0.000 claims 3
- 206010033645 Pancreatitis Diseases 0.000 claims 3
- 208000017442 Retinal disease Diseases 0.000 claims 3
- 206010038923 Retinopathy Diseases 0.000 claims 3
- 206010040047 Sepsis Diseases 0.000 claims 3
- 208000005392 Spasm Diseases 0.000 claims 3
- 208000006011 Stroke Diseases 0.000 claims 3
- 230000001154 acute effect Effects 0.000 claims 3
- 208000026935 allergic disease Diseases 0.000 claims 3
- 230000002491 angiogenic effect Effects 0.000 claims 3
- 208000006673 asthma Diseases 0.000 claims 3
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Chemical compound N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 claims 3
- 210000000988 bone and bone Anatomy 0.000 claims 3
- 230000001684 chronic effect Effects 0.000 claims 3
- 208000019425 cirrhosis of liver Diseases 0.000 claims 3
- 206010009887 colitis Diseases 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 230000003247 decreasing effect Effects 0.000 claims 3
- 206010012601 diabetes mellitus Diseases 0.000 claims 3
- 208000003906 hydrocephalus Diseases 0.000 claims 3
- 230000009610 hypersensitivity Effects 0.000 claims 3
- 230000001506 immunosuppresive effect Effects 0.000 claims 3
- 230000004054 inflammatory process Effects 0.000 claims 3
- 208000037805 labour Diseases 0.000 claims 3
- 201000010901 lateral sclerosis Diseases 0.000 claims 3
- 208000019423 liver disease Diseases 0.000 claims 3
- 208000030159 metabolic disease Diseases 0.000 claims 3
- 206010027599 migraine Diseases 0.000 claims 3
- 201000006417 multiple sclerosis Diseases 0.000 claims 3
- 230000003387 muscular Effects 0.000 claims 3
- 235000020824 obesity Nutrition 0.000 claims 3
- 201000008482 osteoarthritis Diseases 0.000 claims 3
- 208000020629 overactive bladder Diseases 0.000 claims 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- 230000002980 postoperative effect Effects 0.000 claims 3
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 3
- 208000002815 pulmonary hypertension Diseases 0.000 claims 3
- 230000004044 response Effects 0.000 claims 3
- 206010039083 rhinitis Diseases 0.000 claims 3
- 201000009890 sinusitis Diseases 0.000 claims 3
- 230000009885 systemic effect Effects 0.000 claims 3
- 230000005760 tumorsuppression Effects 0.000 claims 3
- 206010010774 Constipation Diseases 0.000 claims 2
- 241000282412 Homo Species 0.000 claims 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical group C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 230000001575 pathological effect Effects 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 208000007232 portal hypertension Diseases 0.000 claims 2
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical group C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims 2
- QZEQBRBATVPHSA-IFXJQAMLSA-N 4-[[(3S,4R)-1-(2,4-dichlorophenyl)sulfonyl-4-hydroxy-4-(hydroxymethyl)pyrrolidin-3-yl]methyl]-2-fluorobenzonitrile Chemical compound ClC1=C(C=CC(=C1)Cl)S(=O)(=O)N1C[C@@H]([C@@](C1)(CO)O)CC1=CC(=C(C#N)C=C1)F QZEQBRBATVPHSA-IFXJQAMLSA-N 0.000 claims 1
- ZLSYCTPUNQODSG-OXJNMPFZSA-N 4-[[(3S,4R)-1-(2-chloro-4-cyanophenyl)sulfonyl-4-hydroxy-4-(hydroxymethyl)pyrrolidin-3-yl]methyl]-2-fluorobenzonitrile Chemical compound ClC1=C(C=CC(=C1)C#N)S(=O)(=O)N1C[C@@H]([C@@](C1)(CO)O)CC1=CC(=C(C#N)C=C1)F ZLSYCTPUNQODSG-OXJNMPFZSA-N 0.000 claims 1
- QQPLUCKOAQUILN-QFBILLFUSA-N 4-[[(3S,4R)-1-[2-chloro-4-(trifluoromethyl)phenyl]sulfonyl-4-hydroxy-4-(hydroxymethyl)pyrrolidin-3-yl]methyl]benzonitrile Chemical compound ClC1=C(C=CC(=C1)C(F)(F)F)S(=O)(=O)N1C[C@@H]([C@@](C1)(CO)O)CC1=CC=C(C#N)C=C1 QQPLUCKOAQUILN-QFBILLFUSA-N 0.000 claims 1
- RDXAJICEALUQOJ-FXAWDEMLSA-N 4-[[(3S,4R)-1-[2-cyano-4-(trifluoromethyl)phenyl]sulfonyl-4-hydroxy-4-(hydroxymethyl)pyrrolidin-3-yl]methyl]-2-fluorobenzonitrile Chemical compound C(#N)C1=C(C=CC(=C1)C(F)(F)F)S(=O)(=O)N1C[C@@H]([C@@](C1)(CO)O)CC1=CC(=C(C#N)C=C1)F RDXAJICEALUQOJ-FXAWDEMLSA-N 0.000 claims 1
- QZEQBRBATVPHSA-LIRRHRJNSA-N 4-[[(3S,4S)-1-(2,4-dichlorophenyl)sulfonyl-4-hydroxy-4-(hydroxymethyl)pyrrolidin-3-yl]methyl]-2-fluorobenzonitrile Chemical compound ClC1=C(C=CC(=C1)Cl)S(=O)(=O)N1C[C@@H]([C@](C1)(CO)O)CC1=CC(=C(C#N)C=C1)F QZEQBRBATVPHSA-LIRRHRJNSA-N 0.000 claims 1
- HLJMSDGALLNUHU-KSSFIOAISA-N 4-[[(3S,4S)-4-(aminomethyl)-1-(5-chloropyridin-2-yl)sulfonyl-4-hydroxypyrrolidin-3-yl]methyl]-2-fluorobenzonitrile Chemical compound NC[C@]1([C@H](CN(C1)S(=O)(=O)C1=NC=C(C=C1)Cl)CC1=CC(=C(C#N)C=C1)F)O HLJMSDGALLNUHU-KSSFIOAISA-N 0.000 claims 1
- 208000026372 Congenital cystic kidney disease Diseases 0.000 claims 1
- 206010052139 Eye oedema Diseases 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims 1
- 229910021419 crystalline silicon Inorganic materials 0.000 claims 1
- 201000003146 cystitis Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 150000002617 leukotrienes Chemical class 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 150000003230 pyrimidines Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 230000001568 sexual effect Effects 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- UUUHXMGGBIUAPW-UHFFFAOYSA-N 1-[1-[2-[[5-amino-2-[[1-[5-(diaminomethylideneamino)-2-[[1-[3-(1h-indol-3-yl)-2-[(5-oxopyrrolidine-2-carbonyl)amino]propanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbon Chemical compound C1CCC(C(=O)N2C(CCC2)C(O)=O)N1C(=O)C(C(C)CC)NC(=O)C(CCC(N)=O)NC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C1CCCN1C(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C1CCC(=O)N1 UUUHXMGGBIUAPW-UHFFFAOYSA-N 0.000 description 4
- 102000004270 Peptidyl-Dipeptidase A Human genes 0.000 description 4
- 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 description 4
- 239000003199 leukotriene receptor blocking agent Substances 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- UCTWMZQNUQWSLP-UHFFFAOYSA-N Adrenaline Natural products CNCC(O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-UHFFFAOYSA-N 0.000 description 1
- 102000004136 Vasopressin Receptors Human genes 0.000 description 1
- 108090000643 Vasopressin Receptors Proteins 0.000 description 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 description 1
- 102000005962 receptors Human genes 0.000 description 1
- 108020003175 receptors Proteins 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662397013P | 2016-09-20 | 2016-09-20 | |
| US62/397,013 | 2016-09-20 | ||
| US201762482307P | 2017-04-06 | 2017-04-06 | |
| US62/482,307 | 2017-04-06 | ||
| PCT/IB2017/055703 WO2018055527A1 (en) | 2016-09-20 | 2017-09-20 | Trpv4 antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019532054A JP2019532054A (ja) | 2019-11-07 |
| JP2019532054A5 true JP2019532054A5 (enExample) | 2021-02-12 |
Family
ID=60117716
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019515545A Pending JP2019532054A (ja) | 2016-09-20 | 2017-09-20 | Ｔｒｐｖ４拮抗薬 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US10590077B2 (enExample) |
| EP (1) | EP3515889A1 (enExample) |
| JP (1) | JP2019532054A (enExample) |
| WO (1) | WO2018055527A1 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7106528B2 (ja) | 2016-09-20 | 2022-07-26 | グラクソスミスクライン、インテレクチュアル、プロパティー、（ナンバー２）、リミテッド | Ｔｒｐｖ４拮抗薬 |
| TW201825458A (zh) | 2016-09-20 | 2018-07-16 | 英商葛蘭素史克智慧財產（第二）有限公司 | Ｔｒｐｖ４拮抗劑 |
| JOP20210217A1 (ar) | 2019-02-15 | 2023-01-30 | Novartis Ag | طرق لعلاج ألم سطح عين |
| JP6994061B2 (ja) | 2019-02-15 | 2022-01-14 | ノバルティス アーゲー | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
| CN115427409B (zh) | 2020-04-30 | 2025-02-25 | 拉夸里亚创药株式会社 | 作为trpv4拮抗剂的嘧啶-4(3h)-酮衍生物 |
| WO2021233752A1 (en) | 2020-05-19 | 2021-11-25 | Bayer Aktiengesellschaft | Trpa1 antagonists for the treatment of diseases associated with pain and inflammation |
| CA3185968A1 (en) | 2020-07-13 | 2022-01-20 | Tony Lahoutte | Antibody fragment against folr1 |
| TW202216143A (zh) | 2020-07-16 | 2022-05-01 | 日商拉夸里亞創藥股份有限公司 | 作為眼疾病的治療藥之ｔｒｐｖ４抑制藥 |
| WO2023203135A1 (en) | 2022-04-22 | 2023-10-26 | Precirix N.V. | Improved radiolabelled antibody |
| IL318992A (en) | 2022-05-02 | 2025-04-01 | Precirix N V | Cancer treatment through advance directives |
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| GB2064336B (en) | 1979-12-06 | 1984-03-14 | Glaxo Group Ltd | Device for dispensing medicaments |
| US4778054A (en) | 1982-10-08 | 1988-10-18 | Glaxo Group Limited | Pack for administering medicaments to patients |
| ES286422Y (es) | 1982-10-08 | 1986-09-16 | Glaxo Group Limited | Dispositivo para administrar medicamentos a pacientes |
| GB2169265B (en) | 1982-10-08 | 1987-08-12 | Glaxo Group Ltd | Pack for medicament |
| AT396872B (de) | 1985-07-30 | 1993-12-27 | Glaxo Group Ltd | Gerät zur verabreichung von medikamenten in pulverform |
| SK280967B6 (sk) | 1990-03-02 | 2000-10-09 | Glaxo Group Limited | Inhalačný prístroj |
| GB9004781D0 (en) | 1990-03-02 | 1990-04-25 | Glaxo Group Ltd | Device |
| US6536427B2 (en) | 1990-03-02 | 2003-03-25 | Glaxo Group Limited | Inhalation device |
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| TW201825458A (zh) | 2016-09-20 | 2018-07-16 | 英商葛蘭素史克智慧財產（第二）有限公司 | Ｔｒｐｖ４拮抗劑 |
| JP7106528B2 (ja) | 2016-09-20 | 2022-07-26 | グラクソスミスクライン、インテレクチュアル、プロパティー、（ナンバー２）、リミテッド | Ｔｒｐｖ４拮抗薬 |
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2017
- 2017-09-20 US US16/334,410 patent/US10590077B2/en not_active Expired - Fee Related
- 2017-09-20 EP EP17784691.2A patent/EP3515889A1/en not_active Withdrawn
- 2017-09-20 WO PCT/IB2017/055703 patent/WO2018055527A1/en not_active Ceased
- 2017-09-20 JP JP2019515545A patent/JP2019532054A/ja active Pending
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