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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    • 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
    • C07D213/89—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
    • 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
    • C07D401/12—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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • 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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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Biomedical Technology (AREA)
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  • Pulmonology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • 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 (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)

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
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WO2007109459A2 (en) * 2006-03-21 2007-09-27 Janssen Pharmaceutica, Nv Pyridines and pyridine n-oxides as modulators of thrombin
PL2010493T3 (pl) * 2006-04-12 2016-08-31 Merck Sharp & Dohme Pirydyloamidy jako antagoniści kanałów wapniowych typu t
JP5524071B2 (ja) 2007-10-24 2014-06-18 メルク・シャープ・アンド・ドーム・コーポレーション 複素環フェニルアミドｔ型カルシウムチャネルアンタゴニスト
WO2013119928A1 (en) * 2012-02-09 2013-08-15 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
US10214512B2 (en) 2015-10-29 2019-02-26 Merck Sharp & Dohme Corp. Factor XIA inhibitors
WO2018039094A1 (en) 2016-08-22 2018-03-01 Merck Sharp & Dohme Corp. Pyridine-1-oxide derivatives and their use as factor xia inhibitors
US11045589B2 (en) 2017-09-22 2021-06-29 Becton, Dickinson And Company 4% trisodium citrate solution for use as a catheter lock solution
US12497403B2 (en) 2021-01-28 2025-12-16 Merck Sharp & Dohme Llc Factor XIa inhibitors

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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
ATE137223T1 (de) 1991-05-31 1996-05-15 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.
ES2100425T3 (es) * 1992-11-29 1997-06-16 Hoechst Ag Procedimiento para preparar acidos benzoicos halogenados.
JP2000502708A (ja) 1995-12-29 2000-03-07 スミスクライン・ビーチャム・コーポレイション ビトロネクチン受容体拮抗物質
BR9908636A (pt) 1998-03-10 2002-01-08 Smithkline Beecham Corp Antagonistas de receptor vitronectina
WO2002042272A2 (en) 2000-11-20 2002-05-30 Pharmacia Corporation 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
WO2004091613A2 (en) 2003-04-10 2004-10-28 3-Dimensional Pharmaceuticals, Inc. 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

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

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

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Open date: 20080723