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PE20040925A1 - DERIVADOS DE PIRAZOL COMO INHIBIDORES DEL FACTOR Xa - Google Patents

DERIVADOS DE PIRAZOL COMO INHIBIDORES DEL FACTOR Xa

Info

Publication number
PE20040925A1
PE20040925A1 PE2004000015A PE2004000015A PE20040925A1 PE 20040925 A1 PE20040925 A1 PE 20040925A1 PE 2004000015 A PE2004000015 A PE 2004000015A PE 2004000015 A PE2004000015 A PE 2004000015A PE 20040925 A1 PE20040925 A1 PE 20040925A1
Authority
PE
Peru
Prior art keywords
members
thiofen
mono
alkylene
compounds
Prior art date
Application number
PE2004000015A
Other languages
English (en)
Inventor
Marc Nazare
Wolkmar Wehner
David William Will
Hans Matter
Original Assignee
Aventis Pharma Gmbh
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
Priority claimed from EP02028915A external-priority patent/EP1433788A1/en
Priority claimed from EP03011308A external-priority patent/EP1479678A1/en
Application filed by Aventis Pharma Gmbh filed Critical Aventis Pharma Gmbh
Publication of PE20040925A1 publication Critical patent/PE20040925A1/es

Links

Classifications

    • 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
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • 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
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Surgery (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA I, DONDE R0 ES UN HETEROCICLILO MONO O BICICLICO DE 4 A 15 MIEMBROS QUE CONTIENE DE 1 A 4 HETEROATOMOS DE N, S Y O, OPCIONALMENTE SUSTITUIDO; UN HETEROCICLILO SELECCIONADO DE BENZOIMIDAZOLILO, 1,3-BENZODIOXOLILO, BENZOFURANILO, BENZOXAZOLILO, ENTRE OTROS, UN ARILO MONO O BICICLICO DE 6 A 14 MIEMBROS, OPCIONALMENTE SUSTITUIDO POR R8; Q ES UN ENLACE DIRECTO, -ALQUILENO(C0-C2)-C(O)-NR10-, -NR10-C(O)-NR10-, -NR10-C(O)-, -SO2-, ENTRE OTROS; R1 ES H, ALQUILO(C1-C4), ALQUILENO(C1-C3)-C(O)-NH-R0, ENTRE OTROS; R2 ES UN ENLACE DIRECTO O ALQUILENO (C1-C4), O R1 Y R3 JUNTOS FORMARIAN UN GRUPO CICLICO DE 6 A 8 MIEMBROS CON 1 A 4 HETEROATOMOS DE N, S Y O; V ES UN RESTO CICLICO DE 3 A 7 MIEMBROS, ARILO DE 6 A 14 MIEMBROS O HETEROCICLILO MONO O BICICLICO DE 4 A 15 MIEMBROS OPCIONALMENTE SUSTITUIDO POR R14; G ES UN ENLACE DIRECTO, -(CH2)m-NR10-SO2-NR10-(CH2)n-, -(CH2)m-CH(OH)-(CH2)n, -(CH2)m, ENTRE OTROS; M ES H, -ALQUILO(C1-C8), -C(O)-N(R11)-R12-, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (1-ISOPROPIL-PIPERIDIN-4-IL)-AMIDA DEL ACIDO 2-[5-(5-CLORO-TIOFEN-2-IL)-ISOXAZOL-3-ILMETIL]-5-TIOFEN-2-IL-2H-PIRAZOL-3-CARBOXILICO, (1-ISOPROPIL-PIPERIDIN-4-IL)-AMIDA DEL ACIDO 1-[5-(5-CLORO-TIOFEN-2-IL)-ISOXAZOL-3-ILMETIL]-5-TIOFEN-2-IL-1H-PIRAZOL-3-CARBOXILICO, ENTRE OTROS. ESTOS COMPUESTOS SON INHIBIDORESS REVERSIBLES DE LAS ENZIMAS DE COAGULACION SANGUINEA FACTOR Xa(FXa) Y/O FACTOR VIIa Y SON ADECUADOS PARAEL TRATAMIENTO DE ENFERMEDADES TROMBOEMBOLICAS Y REESTENOSIS
PE2004000015A 2002-12-23 2004-01-05 DERIVADOS DE PIRAZOL COMO INHIBIDORES DEL FACTOR Xa PE20040925A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP02028915A EP1433788A1 (en) 2002-12-23 2002-12-23 Pyrazole-derivatives as factor Xa inhibitors
EP03011308A EP1479678A1 (en) 2003-05-19 2003-05-19 Pyrazole-derivatives as factor xa inhibitors

Publications (1)

Publication Number Publication Date
PE20040925A1 true PE20040925A1 (es) 2004-12-24

Family

ID=32683809

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2004000015A PE20040925A1 (es) 2002-12-23 2004-01-05 DERIVADOS DE PIRAZOL COMO INHIBIDORES DEL FACTOR Xa

Country Status (13)

Country Link
EP (1) EP1581523B1 (es)
JP (1) JP4585448B2 (es)
AR (1) AR042648A1 (es)
AT (1) ATE444292T1 (es)
AU (1) AU2003292218A1 (es)
BR (1) BR0317659A (es)
CA (1) CA2511321A1 (es)
DE (1) DE60329529D1 (es)
IL (1) IL169323A0 (es)
MX (1) MXPA05006200A (es)
PE (1) PE20040925A1 (es)
TW (1) TW200505914A (es)
WO (1) WO2004056815A1 (es)

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TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
ITMI20041032A1 (it) 2004-05-24 2004-08-24 Neuroscienze S C A R L Compositi farmaceutici
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AU2005299693B2 (en) 2004-10-26 2012-07-05 Janssen Pharmaceutica, N.V. Factor Xa compounds
US7381732B2 (en) 2004-10-26 2008-06-03 Bristol-Myers Squibb Company Pyrazolobenzamides and derivatives as factor Xa inhibitors
EP1814860B1 (en) * 2004-10-29 2009-06-03 Schering Corporation Substituted 5-carboxyamide pyrazoles and [1,2,4]triazoles as antiviral agents
JP5507049B2 (ja) 2004-12-30 2014-05-28 アステックス、セラピューティックス、リミテッド 医薬品
EP1724269A1 (en) * 2005-05-20 2006-11-22 Sanofi-Aventis Deutschland GmbH Heteroaryl-carboxylic acid (sulfamoyl alkyl) amide - derivatives as factor Xa inhibitors
US8569352B2 (en) * 2005-06-27 2013-10-29 Exelixis Patent Company Llc Imidazole based LXR modulators
JP5474354B2 (ja) 2005-12-30 2014-04-16 アステックス、セラピューティックス、リミテッド 医薬化合物
JP5523829B2 (ja) 2006-06-29 2014-06-18 アステックス、セラピューティックス、リミテッド 複合薬剤
EP2238127B1 (en) * 2007-12-26 2012-08-15 Sanofi Pyrazole-carboxamide derivatives as p2y12 antagonists
EP2238128B1 (en) * 2007-12-26 2012-08-22 Sanofi Heterocyclic pyrazole-carboxamides as p2y12 antagonists
CN102056907B (zh) 2008-04-04 2014-12-31 武田药品工业株式会社 杂环衍生物及其用途
CA2722139C (en) * 2008-04-23 2017-04-11 Rigel Pharmaceuticals, Inc. Carboxamide compounds for the treatment of metabolic disorders
TWI532725B (zh) 2010-01-26 2016-05-11 賽諾菲阿凡提斯公司 經氧取代之３－雜芳醯基胺基－丙酸衍生物及其作為藥物之用途
CA2829790C (en) 2010-03-30 2018-06-05 Verseon Corporation Multisubstituted aromatic compounds as inhibitors of thrombin
TWI523844B (zh) 2011-01-26 2016-03-01 賽諾菲公司 經胺基取代之３－雜芳醯基胺基－丙酸衍生物及其作為藥物之用途
AR085013A1 (es) 2011-01-26 2013-08-07 Sanofi Aventis Derivados de acido 3-heteroaroilamino-propionico sustituidos y su uso como sustancias farmaceuticas
PT2736888E (pt) 2011-07-26 2016-02-17 Sanofi Sa Derivados do ácido 3-heteroaroilamino-propiónico e o seu uso como produtos farmacêuticos
CA2841911A1 (en) 2011-07-26 2013-01-31 Sanofi Substituted 3 - (thiazole - 4 - carbonyl) - or 3 - (thiazole - 2 - carbonyl) - aminopropionic acid derivatives and their use as pharmaceuticals
US20130123325A1 (en) 2011-11-14 2013-05-16 Sven Ruf Use of boceprevir and related compounds in atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases
US20130123276A1 (en) 2011-11-14 2013-05-16 Sven Ruf Use of telaprevir and related compounds in atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases
CA2902431A1 (en) 2013-03-15 2014-09-25 Kevin Michael Short Halogenopyrazoles as inhibitors of thrombin
EP3421036B8 (en) * 2013-03-15 2020-12-30 Verseon International Corporation Multisubstituted aromatic compounds as serine protease inhibitors
JP6357529B2 (ja) 2013-03-28 2018-07-11 サノフイ ビアリール−プロピオン酸誘導体および医薬品としてのその使用
KR20150136507A (ko) 2013-03-28 2015-12-07 사노피 바이아릴-프로피온산 유도체 및 약제로서의 그의 용도
EP2805705B1 (en) 2013-05-23 2016-11-09 IP Gesellschaft für Management mbH Packaging with one or more administration units comprising a sodium salt of (R)-3-[6-amino-pyridin-3-yl]-2-(1-cyclohexyl-1 H-imidazol-4-yl)-propionic acid
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Also Published As

Publication number Publication date
MXPA05006200A (es) 2005-08-19
EP1581523B1 (en) 2009-09-30
DE60329529D1 (de) 2009-11-12
IL169323A0 (en) 2007-07-04
AR042648A1 (es) 2005-06-29
ATE444292T1 (de) 2009-10-15
JP2006511608A (ja) 2006-04-06
AU2003292218A1 (en) 2004-07-14
WO2004056815A1 (en) 2004-07-08
TW200505914A (en) 2005-02-16
BR0317659A (pt) 2005-12-06
CA2511321A1 (en) 2004-07-08
EP1581523A1 (en) 2005-10-05
JP4585448B2 (ja) 2010-11-24

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