CN101228129A - 氟代吡啶n-氧化物凝血酶调节剂和含氮杂芳基化合物的n-氧化方法 - Google Patents

氟代吡啶n-氧化物凝血酶调节剂和含氮杂芳基化合物的n-氧化方法 Download PDF

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Publication number
CN101228129A
CN101228129A CNA2006800219864A CN200680021986A CN101228129A CN 101228129 A CN101228129 A CN 101228129A CN A2006800219864 A CNA2006800219864 A CN A2006800219864A CN 200680021986 A CN200680021986 A CN 200680021986A CN 101228129 A CN101228129 A CN 101228129A
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compound
mammal
oxide
amount
temperature
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Chinese (zh)
Inventor
K·克罗伊特尔
T·卢
Y·K·李
C·特尔哈
M·普莱尔
X·朱
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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    • 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
    • C07D213/89—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 with hetero atoms directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • 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
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • C07D215/58—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems with hetero atoms directly attached to the ring nitrogen atom
    • C07D215/60—N-oxides
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    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
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    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • 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
    • C07D401/14—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 three or more hetero rings

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  • Chemical & Material Sciences (AREA)
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  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
CNA2006800219864A 2005-04-20 2006-03-21 氟代吡啶n-氧化物凝血酶调节剂和含氮杂芳基化合物的n-氧化方法 Pending CN101228129A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US67313105P 2005-04-20 2005-04-20
US60/673,131 2005-04-20

Publications (1)

Publication Number Publication Date
CN101228129A true CN101228129A (zh) 2008-07-23

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ID=36685688

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CNA2006800219864A Pending CN101228129A (zh) 2005-04-20 2006-03-21 氟代吡啶n-氧化物凝血酶调节剂和含氮杂芳基化合物的n-氧化方法

Country Status (12)

Country Link
US (1) US7262210B2 (OSRAM)
EP (1) EP1879864A1 (OSRAM)
JP (1) JP2008536918A (OSRAM)
KR (1) KR20080004554A (OSRAM)
CN (1) CN101228129A (OSRAM)
AU (1) AU2006240423A1 (OSRAM)
BR (1) BRPI0610506A2 (OSRAM)
CA (1) CA2605480A1 (OSRAM)
MX (1) MX2007013198A (OSRAM)
PE (1) PE20061399A1 (OSRAM)
TW (1) TW200718688A (OSRAM)
WO (1) WO2006115652A1 (OSRAM)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106413710A (zh) * 2014-05-28 2017-02-15 默沙东公司 因子XIa抑制剂
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

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007109459A2 (en) * 2006-03-21 2007-09-27 Janssen Pharmaceutica, Nv Pyridines and pyridine n-oxides as modulators of thrombin
ES2566481T3 (es) 2006-04-12 2016-04-13 Merck Sharp & Dohme Corp. Antagonistas del canal de calcio de tipo T de piridil amida
CA2701594C (en) 2007-10-24 2014-02-18 Merck Sharp & Dohme Corp. Heterocycle phenyl amide t-type calcium channel antagonists
US9884822B2 (en) 2012-02-09 2018-02-06 Arch Chemicals, Inc. Process for the preparation of 1-hydroxy-6-substituted pyridones
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
MX387515B (es) * 2015-10-29 2025-03-18 Merck Sharp & Dohme Llc Inhibidores de factor xia.
EP3500556B1 (en) 2016-08-22 2023-08-02 Merck Sharp & Dohme LLC Pyridine-1-oxide derivatives and their use as factor xia inhibitors
WO2019060697A1 (en) 2017-09-22 2019-03-28 Becton, Dickinson And Company 4% TRISODIC CITRATE SOLUTION FOR USE AS A CATHETER LOCK SOLUTION
CA3206548A1 (en) * 2021-01-28 2022-08-04 John S. Debenham Factor xia inhibitors

Family Cites Families (13)

* Cited by examiner, † Cited by third party
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
TW204343B (OSRAM) 1991-05-31 1993-04-21 Sumitomo Pharmaceutics Co Ltd
FR2686084B1 (fr) 1992-01-10 1995-12-22 Bioprojet Soc Civ Nouveaux derives de l'imidazole, leur preparation et leurs applications therapeutiques.
EP0600317B1 (de) 1992-11-29 1997-03-12 Hoechst Aktiengesellschaft Verfahren zur Herstellung von halogenierten Benzoesäuren
CN1209060A (zh) 1995-12-29 1999-02-24 史密丝克莱恩比彻姆公司 玻连蛋白受体拮抗剂
DZ2741A1 (fr) 1998-03-10 2003-09-08 Smithkline Beecham Corp Composés nouveaux antagonistes des récepteurs de vitronectine procédé pour leur préparation et compositions.
JP2004517074A (ja) 2000-11-20 2004-06-10 ファルマシア・コーポレーション 凝血カスケードを選択的に阻害するのに有用な置換された多環アリールおよびヘテロアリールピリジン類
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
DE602004021365D1 (de) * 2003-04-10 2009-07-16 Ortho Mcneil Pharm Inc Substituierte phenylacetamide und ihre anwendung als protease inhibitoren
US7662987B2 (en) 2003-07-15 2010-02-16 Xenoport, Inc. Methods for synthesis of acyloxyalkyl compounds

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106413710A (zh) * 2014-05-28 2017-02-15 默沙东公司 因子XIa抑制剂
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

Also Published As

Publication number Publication date
EP1879864A1 (en) 2008-01-23
MX2007013198A (es) 2008-03-24
AU2006240423A1 (en) 2006-11-02
WO2006115652A1 (en) 2006-11-02
CA2605480A1 (en) 2006-11-02
TW200718688A (en) 2007-05-16
US20060241148A1 (en) 2006-10-26
BRPI0610506A2 (pt) 2010-06-29
KR20080004554A (ko) 2008-01-09
JP2008536918A (ja) 2008-09-11
PE20061399A1 (es) 2007-02-05
US7262210B2 (en) 2007-08-28

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