CN101128457A - 凝血酶受体拮抗剂 - Google Patents

凝血酶受体拮抗剂 Download PDF

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Publication number
CN101128457A
CN101128457A CNA2004800278261A CN200480027826A CN101128457A CN 101128457 A CN101128457 A CN 101128457A CN A2004800278261 A CNA2004800278261 A CN A2004800278261A CN 200480027826 A CN200480027826 A CN 200480027826A CN 101128457 A CN101128457 A CN 101128457A
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CN
China
Prior art keywords
compound
alkyl
pharmaceutically acceptable
solvate
salt
Prior art date
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Pending
Application number
CNA2004800278261A
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English (en)
Chinese (zh)
Inventor
S·契卡拉曼尼尔
M·V·契利亚
夏研
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Merck Sharp and Dohme LLC
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Schering Corp
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Publication of CN101128457A publication Critical patent/CN101128457A/zh
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CNA2004800278261A 2003-09-25 2004-09-23 凝血酶受体拮抗剂 Pending CN101128457A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US10/671,216 2003-09-25
US10/671,216 US7488742B2 (en) 2000-06-15 2003-09-25 Thrombin receptor antagonists

Publications (1)

Publication Number Publication Date
CN101128457A true CN101128457A (zh) 2008-02-20

Family

ID=34393462

Family Applications (1)

Application Number Title Priority Date Filing Date
CNA2004800278261A Pending CN101128457A (zh) 2003-09-25 2004-09-23 凝血酶受体拮抗剂

Country Status (21)

Country Link
US (3) US7488742B2 (https=)
EP (1) EP1663965B1 (https=)
JP (1) JP4694490B2 (https=)
KR (1) KR20060128848A (https=)
CN (1) CN101128457A (https=)
AR (1) AR045809A1 (https=)
AU (1) AU2004276327B2 (https=)
BR (1) BRPI0414592A (https=)
CA (1) CA2540163C (https=)
CO (1) CO5680428A2 (https=)
EC (1) ECSP066455A (https=)
IL (1) IL174538A0 (https=)
MX (1) MXPA06003379A (https=)
MY (1) MY143834A (https=)
NO (1) NO20061797L (https=)
PE (1) PE20050471A1 (https=)
RU (1) RU2367660C9 (https=)
SG (1) SG147466A1 (https=)
TW (1) TWI331608B (https=)
WO (1) WO2005030712A2 (https=)
ZA (1) ZA200602448B (https=)

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CN110407819A (zh) * 2019-08-02 2019-11-05 牡丹江医学院 一种作为预防外科手术并发症的凝血酶受体拮抗剂

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MX2008012574A (es) 2006-03-29 2008-10-10 Schering Corp Derivados de himbacina monociclitos y biciclicos utiles como antagonistas del receptor de trombina.
TW200812619A (en) * 2006-04-06 2008-03-16 Schering Corp TRA combination therapies
EP2007755B1 (en) * 2006-04-13 2012-06-27 Schering Corporation Fused ring thrombin receptor antagonists
CA2655720A1 (en) 2006-06-29 2008-01-10 Schering Corporation Substituted bicyclic and tricyclic thrombin receptor antagonists
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TWI343262B (en) * 2006-09-26 2011-06-11 Schering Corp Rapidly disintegrating lyophilized oral formulations of a thrombin receptor antagonist
CN101541782A (zh) * 2006-10-04 2009-09-23 先灵公司 作为凝血酶受体拮抗剂的二环和三环衍生物
WO2008079260A2 (en) * 2006-12-22 2008-07-03 Schering Corporation Disintegration promoters in solid dose wet granulation formulations
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WO2009097970A1 (de) 2008-02-05 2009-08-13 Sanofi-Aventis Triazolopyridazine als par1-inhibitoren, ihre herstellung und verwendung als arzneimittel
KR20100120139A (ko) * 2008-02-05 2010-11-12 사노피-아벤티스 Ｐａｒ１ 억제제로서의 트리아졸륨 염, 이들의 제조방법, 및 약제로서의 용도
ES2400322T3 (es) 2008-02-05 2013-04-09 Sanofi Derivados de SF5 como inhibidores de PAR-1, su preparación y utilización como medicamento
ES2437100T3 (es) 2009-06-04 2014-01-08 Merck Sharp & Dohme Corp. Metabolito activo de un antagonista de los receptores de la trombina
MX2011013091A (es) 2009-06-08 2012-01-12 Schering Corp Un antagonista del receptor de trombina y tableta con dosificacion fija de clopidogrel.
PL2558462T3 (pl) 2010-04-16 2015-03-31 Sanofi Sa Pirydylo-winylo-pirazolo-chinoliny jako inhibitory PAR1
ES2532902T3 (es) 2010-04-16 2015-04-01 Sanofi Piridil-vinil-pirroles tricíclicos como inhibidores de PAR1
US9340530B2 (en) 2012-03-06 2016-05-17 Merck Sharp & Dohme Corp. Preparation and use of bicyclic himbacine derivatives as PAR-1 receptor antagonists
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Publication number Priority date Publication date Assignee Title
CN110407819A (zh) * 2019-08-02 2019-11-05 牡丹江医学院 一种作为预防外科手术并发症的凝血酶受体拮抗剂

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US20040152736A1 (en) 2004-08-05
SG147466A1 (en) 2008-11-28
US20090076088A1 (en) 2009-03-19
CA2540163C (en) 2012-06-05
AU2004276327B2 (en) 2010-10-07
CA2540163A1 (en) 2005-04-07
BRPI0414592A (pt) 2006-11-07
WO2005030712A8 (en) 2007-12-21
ECSP066455A (es) 2006-09-18
WO2005030712A2 (en) 2005-04-07
IL174538A0 (en) 2006-08-01
US7488742B2 (en) 2009-02-10
EP1663965B1 (en) 2014-04-09
KR20060128848A (ko) 2006-12-14
JP2007523051A (ja) 2007-08-16
WO2005030712A3 (en) 2007-09-20
AU2004276327A1 (en) 2005-04-07
MXPA06003379A (es) 2006-06-08
EP1663965A2 (en) 2006-06-07
PE20050471A1 (es) 2005-08-24
US20090069383A1 (en) 2009-03-12
TW200524914A (en) 2005-08-01
NO20061797L (no) 2006-05-19
CO5680428A2 (es) 2006-09-29
TWI331608B (en) 2010-10-11
RU2367660C2 (ru) 2009-09-20
MY143834A (en) 2011-07-15
RU2367660C9 (ru) 2010-08-10
ZA200602448B (en) 2007-09-26
AR045809A1 (es) 2005-11-16
JP4694490B2 (ja) 2011-06-08
RU2006113638A (ru) 2007-11-10

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