TW200718688A - Fluorinated ryridine N-oxide thrombin modulators and process for N-oxidation of nitrogen containing heteroaryls - Google Patents

Fluorinated ryridine N-oxide thrombin modulators and process for N-oxidation of nitrogen containing heteroaryls

Info

Publication number
TW200718688A
TW200718688A TW095113865A TW95113865A TW200718688A TW 200718688 A TW200718688 A TW 200718688A TW 095113865 A TW095113865 A TW 095113865A TW 95113865 A TW95113865 A TW 95113865A TW 200718688 A TW200718688 A TW 200718688A
Authority
TW
Taiwan
Prior art keywords
oxidation
nitrogen containing
ryridine
fluorinated
oxide
Prior art date
Application number
TW095113865A
Other languages
English (en)
Chinese (zh)
Inventor
Kevin Kreutter
Tian-Bao Lu
Yu-Kai Lee
Christopher Teleha
Mark Player
Xizhen Zhu
Original Assignee
Janssen Pharmaceutica Nv
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of TW200718688A publication Critical patent/TW200718688A/zh

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/89Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/58Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems with hetero atoms directly attached to the ring nitrogen atom
    • C07D215/60N-oxides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW095113865A 2005-04-20 2006-04-19 Fluorinated ryridine N-oxide thrombin modulators and process for N-oxidation of nitrogen containing heteroaryls TW200718688A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US67313105P 2005-04-20 2005-04-20
US11/385,056 US7262210B2 (en) 2005-04-20 2006-03-21 Fluorinated pyridine N-oxide thrombin modulators and process for N-oxidation of nitrogen containing heteroaryls

Publications (1)

Publication Number Publication Date
TW200718688A true TW200718688A (en) 2007-05-16

Family

ID=36685688

Family Applications (1)

Application Number Title Priority Date Filing Date
TW095113865A TW200718688A (en) 2005-04-20 2006-04-19 Fluorinated ryridine N-oxide thrombin modulators and process for N-oxidation of nitrogen containing heteroaryls

Country Status (12)

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

Families Citing this family (11)

* 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
EP2010493B1 (en) 2006-04-12 2016-01-27 Merck Sharp & Dohme Corp. Pyridyl amide t-type calcium channel antagonists
AU2008317353B2 (en) 2007-10-24 2014-08-07 Merck Sharp & Dohme Llc 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
CA2947987A1 (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
EP3368036B1 (en) * 2015-10-29 2022-07-20 Merck Sharp & Dohme LLC Macrocyclic pyridine-n-oxide derivatives as 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
JP7138702B2 (ja) 2017-09-22 2022-09-16 ベクトン・ディキンソン・アンド・カンパニー カテーテルロック溶液としての使用のための4%クエン酸三ナトリウム溶液
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
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
AU643140B2 (en) 1991-05-31 1993-11-04 Sumitomo Pharmaceuticals Company, Limited Leukotriene B4 antagonist
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
WO1997024122A1 (en) 1995-12-29 1997-07-10 Smithkline Beecham Corporation Vitronectin receptor antagonists
CN1299282A (zh) 1998-03-10 2001-06-13 史密丝克莱恩比彻姆公司 玻连蛋白受体拮抗剂
MXPA03004458A (es) 2000-11-20 2005-01-25 Pharmacia Corp Arilpiridinas y heteroarilpiridinas sustituidas utiles para inhibicion selectiva de la cascada de coagulacion.
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
EP1613319B1 (en) 2003-04-10 2009-06-03 Ortho-McNeil Pharmaceuticals, Inc. Substituted phenyl acetamides and their use as protease inhibitors
US7662987B2 (en) 2003-07-15 2010-02-16 Xenoport, Inc. Methods for synthesis of acyloxyalkyl compounds

Also Published As

Publication number Publication date
CA2605480A1 (en) 2006-11-02
JP2008536918A (ja) 2008-09-11
US7262210B2 (en) 2007-08-28
EP1879864A1 (en) 2008-01-23
US20060241148A1 (en) 2006-10-26
BRPI0610506A2 (pt) 2010-06-29
MX2007013198A (es) 2008-03-24
AU2006240423A1 (en) 2006-11-02
CN101228129A (zh) 2008-07-23
KR20080004554A (ko) 2008-01-09
WO2006115652A1 (en) 2006-11-02
PE20061399A1 (es) 2007-02-05

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