JP2008536918A5 - - Google Patents
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- JP2008536918A5 JP2008536918A5 JP2008507677A JP2008507677A JP2008536918A5 JP 2008536918 A5 JP2008536918 A5 JP 2008536918A5 JP 2008507677 A JP2008507677 A JP 2008507677A JP 2008507677 A JP2008507677 A JP 2008507677A JP 2008536918 A5 JP2008536918 A5 JP 2008536918A5
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- JP
- Japan
- Prior art keywords
- temperature
- compound
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- 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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- WJKHJLXJJJATHN-UHFFFAOYSA-N triflic anhydride Chemical compound FC(F)(F)S(=O)(=O)OS(=O)(=O)C(F)(F)F WJKHJLXJJJATHN-UHFFFAOYSA-N 0.000 claims 14
- 238000000034 method Methods 0.000 claims 13
- 150000001875 compounds Chemical class 0.000 claims 11
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 10
- 239000004480 active ingredient Substances 0.000 claims 7
- 230000015572 biosynthetic process Effects 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 239000002904 solvent Substances 0.000 claims 7
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 6
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims 6
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims 5
- 241000124008 Mammalia Species 0.000 claims 4
- 208000007536 Thrombosis Diseases 0.000 claims 4
- 239000008280 blood Substances 0.000 claims 4
- 210000004369 blood Anatomy 0.000 claims 4
- VTIIJXUACCWYHX-UHFFFAOYSA-L disodium;carboxylatooxy carbonate Chemical compound [Na+].[Na+].[O-]C(=O)OOC([O-])=O VTIIJXUACCWYHX-UHFFFAOYSA-L 0.000 claims 4
- 125000006575 electron-withdrawing group Chemical group 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 4
- 229940045872 sodium percarbonate Drugs 0.000 claims 4
- 238000001308 synthesis method Methods 0.000 claims 4
- 230000002194 synthesizing effect Effects 0.000 claims 4
- AQLJVWUFPCUVLO-UHFFFAOYSA-N urea hydrogen peroxide Chemical compound OO.NC(N)=O AQLJVWUFPCUVLO-UHFFFAOYSA-N 0.000 claims 4
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 3
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 3
- 102000009123 Fibrin Human genes 0.000 claims 2
- 108010073385 Fibrin Proteins 0.000 claims 2
- BWGVNKXGVNDBDI-UHFFFAOYSA-N Fibrin monomer Chemical compound CNC(=O)CNC(=O)CN BWGVNKXGVNDBDI-UHFFFAOYSA-N 0.000 claims 2
- 206010047249 Venous thrombosis Diseases 0.000 claims 2
- 239000003146 anticoagulant agent Substances 0.000 claims 2
- 238000007887 coronary angioplasty Methods 0.000 claims 2
- 229950003499 fibrin Drugs 0.000 claims 2
- 239000000463 material Substances 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 238000001356 surgical procedure Methods 0.000 claims 2
- RUIZBQQGWNBRFH-UHFFFAOYSA-N 1-oxidopyrazin-1-ium Chemical compound [O-][N+]1=CC=NC=C1 RUIZBQQGWNBRFH-UHFFFAOYSA-N 0.000 claims 1
- -1 2,2-difluoro-2-pyridin-2-yl-ethylamino Chemical group 0.000 claims 1
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010003178 Arterial thrombosis Diseases 0.000 claims 1
- 206010053567 Coagulopathies Diseases 0.000 claims 1
- 206010051055 Deep vein thrombosis Diseases 0.000 claims 1
- 206010014824 Endotoxic shock Diseases 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- GIIWGCBLYNDKBO-UHFFFAOYSA-N Quinoline 1-oxide Chemical compound C1=CC=C2[N+]([O-])=CC=CC2=C1 GIIWGCBLYNDKBO-UHFFFAOYSA-N 0.000 claims 1
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 1
- 206010040070 Septic Shock Diseases 0.000 claims 1
- 108090000190 Thrombin Proteins 0.000 claims 1
- 208000007814 Unstable Angina Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 1
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 1
- 229940127219 anticoagulant drug Drugs 0.000 claims 1
- 229940127218 antiplatelet drug Drugs 0.000 claims 1
- 230000017531 blood circulation Effects 0.000 claims 1
- 208000015294 blood coagulation disease Diseases 0.000 claims 1
- 206010008118 cerebral infarction Diseases 0.000 claims 1
- 208000026106 cerebrovascular disease Diseases 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 210000004351 coronary vessel Anatomy 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000003527 fibrinolytic agent Substances 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 238000003384 imaging method Methods 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 125000006514 pyridin-2-ylmethyl group Chemical group [H]C1=C([H])C([H])=C([H])C(=N1)C([H])([H])* 0.000 claims 1
- ILVXOBCQQYKLDS-UHFFFAOYSA-N pyridine N-oxide Chemical compound [O-][N+]1=CC=CC=C1 ILVXOBCQQYKLDS-UHFFFAOYSA-N 0.000 claims 1
- 150000003230 pyrimidines Chemical class 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 229960004072 thrombin Drugs 0.000 claims 1
- 229960000103 thrombolytic agent Drugs 0.000 claims 1
- 230000002537 thrombolytic effect Effects 0.000 claims 1
- 201000005665 thrombophilia Diseases 0.000 claims 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-N triflic acid Chemical compound OS(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US67313105P | 2005-04-20 | 2005-04-20 | |
| PCT/US2006/010581 WO2006115652A1 (en) | 2005-04-20 | 2006-03-21 | Fluorinated pyridine n-oxide thrombin modulators and process for n-oxidation of nitrogen containing heteroaryls |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008536918A JP2008536918A (ja) | 2008-09-11 |
| JP2008536918A5 true JP2008536918A5 (enExample) | 2009-05-07 |
Family
ID=36685688
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008507677A Withdrawn JP2008536918A (ja) | 2005-04-20 | 2006-03-21 | フッ素置換ピリジンｎ−オキサイド系トロンビンモジュレーターおよび窒素含有ヘテロアリールのｎ−オキサイド化方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US7262210B2 (enExample) |
| EP (1) | EP1879864A1 (enExample) |
| JP (1) | JP2008536918A (enExample) |
| KR (1) | KR20080004554A (enExample) |
| CN (1) | CN101228129A (enExample) |
| AU (1) | AU2006240423A1 (enExample) |
| BR (1) | BRPI0610506A2 (enExample) |
| CA (1) | CA2605480A1 (enExample) |
| MX (1) | MX2007013198A (enExample) |
| PE (1) | PE20061399A1 (enExample) |
| TW (1) | TW200718688A (enExample) |
| WO (1) | WO2006115652A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7829584B2 (en) * | 2006-03-21 | 2010-11-09 | Janssen Pharmaceutica Nv | Pyridines and pyridine N-oxides as modulators of thrombin |
| US7875636B2 (en) | 2006-04-12 | 2011-01-25 | Merck Sharp & Dohme Corp. | Pyridyl amide T-type calcium channel antagonists |
| KR20100072266A (ko) | 2007-10-24 | 2010-06-30 | 머크 샤프 앤드 돔 코포레이션 | 헤테로사이클 페닐 아미드 ｔ-형 칼슘 채널 길항제 |
| US9884822B2 (en) | 2012-02-09 | 2018-02-06 | Arch Chemicals, Inc. | Process for the preparation of 1-hydroxy-6-substituted pyridones |
| WO2015183709A1 (en) * | 2014-05-28 | 2015-12-03 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| CN105037280B (zh) * | 2015-06-23 | 2017-09-29 | 西安近代化学研究所 | 一种 2,6‑二氨基‑3,5‑二硝基吡嗪‑1‑氧化物的合成方法 |
| BR112018008506B8 (pt) * | 2015-10-29 | 2023-12-05 | Merck Sharp & Dohme | Compostos inibidores do fator xia, composição farmacêutica e usos dos mesmos |
| US10143681B2 (en) | 2016-08-22 | 2018-12-04 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| AU2018338194B2 (en) | 2017-09-22 | 2021-07-08 | Becton, Dickinson And Company | 4% trisodium citrate solution for use as a catheter lock solution |
| CN110818629A (zh) * | 2019-12-05 | 2020-02-21 | 杭州勇诚睿生物科技有限公司 | 一种合成氟代异烟酸衍生物的方法 |
| AU2022212785A1 (en) * | 2021-01-28 | 2023-07-27 | Merck Sharp & Dohme Llc | Factor xia inhibitors |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4187379A (en) | 1978-11-13 | 1980-02-05 | Warner-Lambert Company | 3-Aryloxy-2-pyridinecarbonitrile 1-oxide compounds |
| DE3918834A1 (de) | 1989-01-26 | 1990-08-02 | Bayer Ag | Aryl- und heteroarylethanol-pyridylalkylamine, verfahren zu ihrer herstellung und ihre verwendung als leistungsfoerderer bei tieren und als mittel gegen adipositas |
| DK220890D0 (da) | 1990-09-14 | 1990-09-14 | Ole Buchardt | Fremgangsmaade til fremstilling af c-terminalt amiderede peptider |
| DE69210091T2 (de) | 1991-05-31 | 1996-10-02 | Sumitomo Pharma | Leukotrien-B4-Antagonisten |
| FR2686084B1 (fr) | 1992-01-10 | 1995-12-22 | Bioprojet Soc Civ | Nouveaux derives de l'imidazole, leur preparation et leurs applications therapeutiques. |
| DE59305738D1 (de) | 1992-11-29 | 1997-04-17 | Hoechst Ag | Verfahren zur Herstellung von halogenierten Benzoesäuren |
| TR199801255T2 (xx) | 1995-12-29 | 1998-10-21 | Smithkline Beecham Corporation | Vitronektin resept�r antagonistleri. |
| IL138245A0 (en) | 1998-03-10 | 2001-10-31 | Smithkline Beecham Corp | Vitronectin receptor antagonists |
| CA2430037A1 (en) | 2000-11-20 | 2002-05-30 | Michael S. South | Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade |
| US6610701B2 (en) | 2001-02-09 | 2003-08-26 | Merck & Co., Inc. | Thrombin inhibitors |
| US20030158218A1 (en) * | 2001-12-21 | 2003-08-21 | Nantermet Philippe G. | Thrombin inhibitors |
| US7550474B2 (en) | 2003-04-10 | 2009-06-23 | Johnson & Johnson Pharmaceuticals Research & Development, L.L.C. | Substituted phenyl acetamides and their use as protease inhibitors |
| WO2005010011A2 (en) | 2003-07-15 | 2005-02-03 | Xenoport, Inc. | Methods of synthesis of acyloxyalkyl compounds |
-
2006
- 2006-03-21 BR BRPI0610506-8A patent/BRPI0610506A2/pt not_active IP Right Cessation
- 2006-03-21 US US11/385,056 patent/US7262210B2/en not_active Expired - Fee Related
- 2006-03-21 JP JP2008507677A patent/JP2008536918A/ja not_active Withdrawn
- 2006-03-21 EP EP06739397A patent/EP1879864A1/en not_active Withdrawn
- 2006-03-21 AU AU2006240423A patent/AU2006240423A1/en not_active Abandoned
- 2006-03-21 MX MX2007013198A patent/MX2007013198A/es unknown
- 2006-03-21 CA CA002605480A patent/CA2605480A1/en not_active Abandoned
- 2006-03-21 CN CNA2006800219864A patent/CN101228129A/zh active Pending
- 2006-03-21 KR KR1020077025219A patent/KR20080004554A/ko not_active Withdrawn
- 2006-03-21 WO PCT/US2006/010581 patent/WO2006115652A1/en not_active Ceased
- 2006-04-18 PE PE2006000404A patent/PE20061399A1/es not_active Application Discontinuation
- 2006-04-19 TW TW095113865A patent/TW200718688A/zh unknown
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