CA2605480A1 - Fluorinated pyridine n-oxide thrombin modulators and process for n-oxidation of nitrogen containing heteroaryls - Google Patents

Fluorinated pyridine n-oxide thrombin modulators and process for n-oxidation of nitrogen containing heteroaryls Download PDF

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Publication number
CA2605480A1
CA2605480A1 CA002605480A CA2605480A CA2605480A1 CA 2605480 A1 CA2605480 A1 CA 2605480A1 CA 002605480 A CA002605480 A CA 002605480A CA 2605480 A CA2605480 A CA 2605480A CA 2605480 A1 CA2605480 A1 CA 2605480A1
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CA
Canada
Prior art keywords
compound
mammal
pyridin
oxide
temperature
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.)
Abandoned
Application number
CA002605480A
Other languages
English (en)
French (fr)
Inventor
Kevin Kreutter
Tianbao Lu
Yu Kai Lee
Christopher Teleha
Mark Player
Xizhen Zhu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Janssen Pharmaceutica NV
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2605480A1 publication Critical patent/CA2605480A1/en
Abandoned legal-status Critical Current

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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

  • 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)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (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)
  • Quinoline Compounds (AREA)
  • Pyridine Compounds (AREA)
CA002605480A 2005-04-20 2006-03-21 Fluorinated pyridine n-oxide thrombin modulators and process for n-oxidation of nitrogen containing heteroaryls Abandoned CA2605480A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US67313105P 2005-04-20 2005-04-20
US60/673,131 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 (1)

Publication Number Publication Date
CA2605480A1 true CA2605480A1 (en) 2006-11-02

Family

ID=36685688

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002605480A Abandoned CA2605480A1 (en) 2005-04-20 2006-03-21 Fluorinated pyridine n-oxide thrombin modulators and process for n-oxidation of nitrogen containing heteroaryls

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)

* Cited by examiner, † Cited by third party
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
BRPI0710487A2 (pt) * 2006-04-12 2012-06-05 Merck & Co Inc composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, uso de um composto ou um sal farmaceuticamente aceitácel do mesmo e, método para tratar ou controlar a epilepsia e a dor e para o tratamento ou prevenção de um distúrbio do sono em um paciente.
BRPI0818244A2 (pt) 2007-10-24 2015-06-16 Merck Sharp & Dohme Composto, composição farmacêutica, uso de um composto, e, método para tratamento de um distúrbio ou doença
US9884822B2 (en) 2012-02-09 2018-02-06 Arch Chemicals, Inc. Process for the preparation of 1-hydroxy-6-substituted pyridones
RU2016150410A (ru) * 2014-05-28 2018-06-28 Мерк Шарп И Доум Корп. Ингибиторы фактора xia
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
CN108430471B (zh) * 2015-10-29 2021-07-09 默沙东公司 因子XIa抑制剂
TW201808908A (zh) 2016-08-22 2018-03-16 美商默沙東藥廠 因子XIa抑制劑
CN111278476B (zh) 2017-09-22 2023-01-17 贝克顿·迪金森公司 用作导管封管液的4%柠檬酸三钠溶液
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
KR20230137378A (ko) * 2021-01-28 2023-10-04 머크 샤프 앤드 돔 엘엘씨 인자 xia 억제제

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
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.
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
HUP0101143A3 (en) 1998-03-10 2002-12-28 Smithkline Beecham Corp Pyridin-carboxylic acid derivatives as vitronectin receptor antagonists, process for producing them and pharmaceutical compositions containing them
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
JP2006522809A (ja) * 2003-04-10 2006-10-05 3−ディメンショナル ファーマシューティカルズ, インコーポレイテッド 置換フェニルアセトアミおよびプロテアーゼインヒビターとしてのその使用
WO2005010011A2 (en) * 2003-07-15 2005-02-03 Xenoport, Inc. Methods of synthesis of acyloxyalkyl compounds

Also Published As

Publication number Publication date
MX2007013198A (es) 2008-03-24
US7262210B2 (en) 2007-08-28
KR20080004554A (ko) 2008-01-09
PE20061399A1 (es) 2007-02-05
US20060241148A1 (en) 2006-10-26
TW200718688A (en) 2007-05-16
WO2006115652A1 (en) 2006-11-02
EP1879864A1 (en) 2008-01-23
BRPI0610506A2 (pt) 2010-06-29
CN101228129A (zh) 2008-07-23
AU2006240423A1 (en) 2006-11-02
JP2008536918A (ja) 2008-09-11

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Legal Events

Date Code Title Description
FZDE Discontinued