KR20080004554A - 불소화 피리딘 ｎ―옥사이드 트롬빈 모듈레이터 및 질소를함유하는 헤테로아릴의 ｎ―산화 방법 - Google Patents

불소화 피리딘 ｎ―옥사이드 트롬빈 모듈레이터 및 질소를함유하는 헤테로아릴의 ｎ―산화 방법 Download PDF

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Publication number
KR20080004554A
KR20080004554A KR1020077025219A KR20077025219A KR20080004554A KR 20080004554 A KR20080004554 A KR 20080004554A KR 1020077025219 A KR1020077025219 A KR 1020077025219A KR 20077025219 A KR20077025219 A KR 20077025219A KR 20080004554 A KR20080004554 A KR 20080004554A
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South Korea
Prior art keywords
compound
mammal
pyridin
temperature
fluoro
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.)
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KR1020077025219A
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English (en)
Korean (ko)
Inventor
케빈 크레우터
티안바오 루
유 카이 리
크리스토퍼 텔레하
마크 플레이어
크시첸 주
Original Assignee
얀센 파마슈티카 엔.브이.
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Publication of KR20080004554A publication Critical patent/KR20080004554A/ko
Withdrawn legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/14—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
    • A61P27/02—Ophthalmic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Psychology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (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)
  • Quinoline Compounds (AREA)
  • Pyridine Compounds (AREA)
KR1020077025219A 2005-04-20 2006-03-21 불소화 피리딘 ｎ―옥사이드 트롬빈 모듈레이터 및 질소를함유하는 헤테로아릴의 ｎ―산화 방법 Withdrawn KR20080004554A (ko)

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
KR20080004554A true KR20080004554A (ko) 2008-01-09

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ID=36685688

Family Applications (1)

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KR1020077025219A Withdrawn KR20080004554A (ko) 2005-04-20 2006-03-21 불소화 피리딘 ｎ―옥사이드 트롬빈 모듈레이터 및 질소를함유하는 헤테로아릴의 ｎ―산화 방법

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
ES2566481T3 (es) 2006-04-12 2016-04-13 Merck Sharp & Dohme Corp. Antagonistas del canal de calcio de tipo T de piridil amida
RU2010120671A (ru) 2007-10-24 2011-11-27 Мерк Шарп Энд Домэ Корп. (Us) Гетероциклические фениламидные антагонисты кальциевых каналов т-типа
US9884822B2 (en) 2012-02-09 2018-02-06 Arch Chemicals, Inc. Process for the preparation of 1-hydroxy-6-substituted pyridones
KR20170005871A (ko) * 2014-05-28 2017-01-16 머크 샤프 앤드 돔 코포레이션 인자 XIa 억제제
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
CA2998902C (en) * 2015-10-29 2024-03-26 Merck Sharp & Dohme Corp. Macrocyclic compounds 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
CA3076366C (en) 2017-09-22 2023-05-16 Becton, Dickinson And Company 4% trisodium citrate solution for use as a catheter lock solution
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
WO2022164735A1 (en) * 2021-01-28 2022-08-04 Merck Sharp & Dohme Llc 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
EP0516069B1 (en) 1991-05-31 1996-04-24 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
TR199801255T2 (xx) 1995-12-29 1998-10-21 Smithkline Beecham Corporation Vitronektin resept�r antagonistleri.
OA12189A (en) 1998-03-10 2006-05-09 Smithkline Beecham Corp Vitronectin receptor antagonists.
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

Also Published As

Publication number Publication date
WO2006115652A1 (en) 2006-11-02
TW200718688A (en) 2007-05-16
JP2008536918A (ja) 2008-09-11
US7262210B2 (en) 2007-08-28
EP1879864A1 (en) 2008-01-23
BRPI0610506A2 (pt) 2010-06-29
AU2006240423A1 (en) 2006-11-02
MX2007013198A (es) 2008-03-24
US20060241148A1 (en) 2006-10-26
CN101228129A (zh) 2008-07-23
CA2605480A1 (en) 2006-11-02
PE20061399A1 (es) 2007-02-05

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Date Code Title Description
PA0105 International application

Patent event date: 20071031

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
PC1203 Withdrawal of no request for examination
WITN Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid