PE20061399A1 - N-oxido de piridina fluorados moduladores de la trombina y procesos para la n-oxidacion de heteroarilos nitrogenados - Google Patents

N-oxido de piridina fluorados moduladores de la trombina y procesos para la n-oxidacion de heteroarilos nitrogenados

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Publication number
PE20061399A1
PE20061399A1 PE2006000404A PE2006000404A PE20061399A1 PE 20061399 A1 PE20061399 A1 PE 20061399A1 PE 2006000404 A PE2006000404 A PE 2006000404A PE 2006000404 A PE2006000404 A PE 2006000404A PE 20061399 A1 PE20061399 A1 PE 20061399A1
Authority
PE
Peru
Prior art keywords
oxide
fluorates
nitrogenated
heteroaryls
pyridine
Prior art date
Application number
PE2006000404A
Other languages
English (en)
Inventor
Kreutter Kevin
Tianbao Lu
Christopher Teleha
Xizhen Zhu
Mark Player
Yu Kai Lee
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 PE20061399A1 publication Critical patent/PE20061399A1/es

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    • 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

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Materials For Medical Uses (AREA)

Abstract

REFERIDA A UN COMPUESTO N-OXIDO DE FORMULA I. UNO DE LOS COMPUESTOS PREFERIDOS ES EL DICLORHIDRATO DE 2-[3-CIANO-6-(2,2-DIFLUORO-2-PIRIDIN-2-IL-ETILAMINO)-5-FLUORO-1-OXI-PIRIDIN-2-IL]-N-(3-FLUORO-PIRIDIN-2-ILMETIL)-ACETAMIDA, ENTRE OTROS, TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES DE LA TROMBINA Y SON UTILES PARA INHIBIR LA FORMACION DE TROMBOS O INHIBIR LA FORMACION DE FIBRINA, PARA INHIBIR LA FORMACION DE TROMBOS O INHIBIR LA FORMACION DE EMBOLOS
PE2006000404A 2005-04-20 2006-04-18 N-oxido de piridina fluorados moduladores de la trombina y procesos para la n-oxidacion de heteroarilos nitrogenados PE20061399A1 (es)

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
PE20061399A1 true PE20061399A1 (es) 2007-02-05

Family

ID=36685688

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2006000404A PE20061399A1 (es) 2005-04-20 2006-04-18 N-oxido de piridina fluorados moduladores de la trombina y procesos para la n-oxidacion de heteroarilos nitrogenados

Country Status (12)

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

Families Citing this family (10)

* 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
PL2010493T3 (pl) 2006-04-12 2016-08-31 Merck Sharp & Dohme Pirydyloamidy jako antagoniści kanałów wapniowych typu t
WO2009054984A1 (en) 2007-10-24 2009-04-30 Merck & Co., Inc. Heterocycle phenyl amide t-type calcium channel antagonists
WO2013119928A1 (en) * 2012-02-09 2013-08-15 Arch Chemicals, Inc. Process for the preparation of 1-hydroxy-6-substituted pyridones
CN106413710A (zh) * 2014-05-28 2017-02-15 默沙东公司 因子XIa抑制剂
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
WO2017074832A1 (en) * 2015-10-29 2017-05-04 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
TW201808908A (zh) 2016-08-22 2018-03-16 美商默沙東藥廠 因子XIa抑制劑
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

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.
DE59305738D1 (de) 1992-11-29 1997-04-17 Hoechst Ag Verfahren zur Herstellung von halogenierten Benzoesäuren
CZ203798A3 (cs) 1995-12-29 1998-12-16 Smithkline Beecham Corporation Antagonista vitronektinového receptoru, farmaceutický přípravek s jeho obsahem, způsob a použití
BR9908636A (pt) 1998-03-10 2002-01-08 Smithkline Beecham Corp Antagonistas de receptor vitronectina
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
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
US7662987B2 (en) 2003-07-15 2010-02-16 Xenoport, Inc. Methods for synthesis of acyloxyalkyl compounds

Also Published As

Publication number Publication date
TW200718688A (en) 2007-05-16
WO2006115652A1 (en) 2006-11-02
CN101228129A (zh) 2008-07-23
MX2007013198A (es) 2008-03-24
EP1879864A1 (en) 2008-01-23
AU2006240423A1 (en) 2006-11-02
US20060241148A1 (en) 2006-10-26
BRPI0610506A2 (pt) 2010-06-29
KR20080004554A (ko) 2008-01-09
CA2605480A1 (en) 2006-11-02
US7262210B2 (en) 2007-08-28
JP2008536918A (ja) 2008-09-11

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