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PA8624901A1 - DERIVADOS DE BETA-AMINOACIDOS COMO INHIBIDORES DEL FACTOR Xa - Google Patents

DERIVADOS DE BETA-AMINOACIDOS COMO INHIBIDORES DEL FACTOR Xa

Info

Publication number
PA8624901A1
PA8624901A1 PA20058624901A PA8624901A PA8624901A1 PA 8624901 A1 PA8624901 A1 PA 8624901A1 PA 20058624901 A PA20058624901 A PA 20058624901A PA 8624901 A PA8624901 A PA 8624901A PA 8624901 A1 PA8624901 A1 PA 8624901A1
Authority
PA
Panama
Prior art keywords
factor
compounds
formula
vlla
invention refers
Prior art date
Application number
PA20058624901A
Other languages
English (en)
Inventor
Marc Nazare
Volkmar Wehner
Michael Wagner
Hans Matter
Matthias Urmann
Armin Bauer
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
Application filed by Aventis Pharma Gmbh filed Critical Aventis Pharma Gmbh
Publication of PA8624901A1 publication Critical patent/PA8624901A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • 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
    • 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
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C07D265/32—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C07D265/32—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
    • C07D265/33—Two oxygen atoms, in positions 3 and 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D291/00—Heterocyclic compounds containing rings having nitrogen, oxygen and sulfur atoms as the only ring hetero atoms
    • C07D291/02—Heterocyclic compounds containing rings having nitrogen, oxygen and sulfur atoms as the only ring hetero atoms not condensed with other rings
    • C07D291/06—Six-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/10—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms
    • C07D295/112—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D419/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
    • C07D419/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D419/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Cardiology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

LA PRESENTE INVENCION SE REFIERE A LOS COMPUESTOS DE LA FORMULA 1: EN LA QUE R0, R1, R2, R3, R4, R5, R6, Q, V G Y M SIGNIFICAN LO QUE SE INDICA EN LAS REIVINDICACIONES. LOS COMPUESTOS DE LA FORMULA 1 SON UNOS VALIOSOS COMPUESTOS FARMACOLOGICAMENTE ACTIVOS. MUESTRAN UN FUERTE EFECTO ANTITROMBOTICO Y SON ADECUADOS, POR EJEMPLO, EN EL TRATAMIENTO Y EN LA PROFILAXIS DE LOS TRASTORNOS CARDIOVASCULARES COMO LAS ENFERMEDADES TROMBOEMBOLICAS O LAS REESTENOSIS. SON UNOS INHIBIDORES REVERSIBLES DE LAS ENZIMAS DE LA COAGULACION SANGUINEA FACTOR XA (FXA) Y/O VllA (FVllA) Y, POR LO GENERAL, SE PUEDEN APLICAR EN LAS DOLENCIAS EN LAS QUE APARECE UNA ACTIVIDAD NO DESEADA DEL FACTOR XA Y/O DEL FACTOR VllA, O CUANDO SE PRETENDE CURAR O PREVENIR INHIBIENDO EL FACTOR XA Y/O DE FACTOR VllA. ADEMAS, LA INVENCION SE REFIERE A LOS PROCEDIMIENTOS PARA PREPARAR LOS COMPUESTOS DE LA FORMULA 1; SU USO, EN CONCRETO COMO INGREDIENTES EN LOS FARMACOS Y EN LAS PREPARACIONES FARMACEUTICAS QUE LOS COMPRENDEN.
PA20058624901A 2004-03-03 2005-03-02 DERIVADOS DE BETA-AMINOACIDOS COMO INHIBIDORES DEL FACTOR Xa PA8624901A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP04004904A EP1571154A1 (en) 2004-03-03 2004-03-03 Beta-aminoacid-derivatives as factor Xa inhibitors

Publications (1)

Publication Number Publication Date
PA8624901A1 true PA8624901A1 (es) 2005-09-28

Family

ID=34745988

Family Applications (1)

Application Number Title Priority Date Filing Date
PA20058624901A PA8624901A1 (es) 2004-03-03 2005-03-02 DERIVADOS DE BETA-AMINOACIDOS COMO INHIBIDORES DEL FACTOR Xa

Country Status (15)

Country Link
US (1) US20070179122A1 (es)
EP (2) EP1571154A1 (es)
JP (1) JP2007535497A (es)
KR (1) KR20060122950A (es)
CN (1) CN1926148A (es)
AU (1) AU2005229320A1 (es)
BR (1) BRPI0508320A (es)
CA (1) CA2559948A1 (es)
GT (1) GT200500026A (es)
IL (1) IL177470A0 (es)
PA (1) PA8624901A1 (es)
PE (1) PE20051160A1 (es)
TW (1) TW200540187A (es)
UY (1) UY28787A1 (es)
WO (1) WO2005095440A1 (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7429581B2 (en) 2002-12-23 2008-09-30 Sanofi-Aventis Deutschland Gmbh Pyrazole-derivatives as factor Xa inhibitors
EP1479675A1 (en) * 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Indazole-derivatives as factor Xa inhibitors
EP1568698A1 (en) * 2004-02-27 2005-08-31 Aventis Pharma Deutschland GmbH Pyrrole-derivatives as factor Xa inhibitors
DE102004062544A1 (de) 2004-12-24 2006-07-06 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte Pyrrolidinone, deren Herstellung und deren Verewendung als Arzneimittel
NZ587004A (en) 2008-01-04 2013-11-29 Intellikine Llc Heterocyclic containing entities, compositions and methods
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
BR112012024380A2 (pt) 2010-03-25 2015-09-15 Glaxosmithkline Llc compostos químicos
UA115767C2 (uk) 2011-01-10 2017-12-26 Інфініті Фармасьютікалз, Інк. Способи отримання ізохінолінонів і тверді форми ізохінолінонів
WO2013031930A1 (ja) * 2011-08-31 2013-03-07 味の素株式会社 イミン誘導体
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
CA2890002A1 (en) 2012-11-05 2014-05-08 Nant Holdings Ip, Llc Cyclic sulfonamide containing derivatives as inhibitors of hedgehog signaling pathway
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
CN104311537B (zh) * 2014-09-19 2016-08-24 广东东阳光药业有限公司 含有嘧啶酮乙酰基取代基吡唑类化合物及其组合物及用途
CA3028718A1 (en) 2016-06-24 2017-12-28 Infinity Pharmaceuticals, Inc. Combination therapies

Family Cites Families (21)

* Cited by examiner, † Cited by third party
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EP0673247A4 (en) * 1992-12-01 1996-05-01 Merck & Co Inc FIBRINOGEN RECEPTOR ANTAGONISTS.
CA2374650A1 (en) * 1999-05-24 2000-11-30 Penglie Zhang Inhibitors of factor xa
AU5283900A (en) * 1999-05-24 2000-12-12 Cor Therapeutics, Inc. Inhibitors of factor xa
EP1235807A1 (en) * 1999-11-24 2002-09-04 Millennium Pharmaceuticals, Inc. B-amino acid-, aspartic acid- and diaminopropionic-based inhibitors of factor xa
DE19962924A1 (de) * 1999-12-24 2001-07-05 Bayer Ag Substituierte Oxazolidinone und ihre Verwendung
DE10050723A1 (de) * 2000-10-13 2002-04-25 Merck Patent Gmbh N-Substituierte Aminosäurederivate (Faktor Xa Inhibitoren 12)
DE10063008A1 (de) * 2000-12-16 2002-06-20 Merck Patent Gmbh Carbonsäureamidderivate
EP1217000A1 (en) * 2000-12-23 2002-06-26 Aventis Pharma Deutschland GmbH Inhibitors of factor Xa and factor VIIa
DE10102322A1 (de) * 2001-01-19 2002-07-25 Merck Patent Gmbh Phenylderivate
EP1314733A1 (en) * 2001-11-22 2003-05-28 Aventis Pharma Deutschland GmbH Indole-2-carboxamides as factor Xa inhibitors
DE10254336A1 (de) * 2002-11-21 2004-06-03 Merck Patent Gmbh Carbonsäureamide
US7358268B2 (en) * 2002-12-04 2008-04-15 Sanofi-Aventis Deutschland Gmbh Imidazole derivatives as factor Xa inhibitors
US7429581B2 (en) * 2002-12-23 2008-09-30 Sanofi-Aventis Deutschland Gmbh Pyrazole-derivatives as factor Xa inhibitors
DE10300111A1 (de) * 2003-01-07 2004-07-15 Bayer Healthcare Ag Verfahren zur Herstellung von 5-Chlor-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophencarboxamid
US7317027B2 (en) * 2003-05-19 2008-01-08 Sanofi-Aventis Deutschland Gmbh Azaindole-derivatives as factor Xa inhibitors
US7223780B2 (en) * 2003-05-19 2007-05-29 Sanofi-Aventis Deutschland Gmbh Triazole-derivatives as blood clotting enzyme factor Xa inhibitors
US7741341B2 (en) * 2003-05-19 2010-06-22 Sanofi-Aventis Deutschland Gmbh Benzimidazole-derivatives as factor Xa inhibitors
EP1479677A1 (en) * 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH New indole derivatives as factor xa inhibitors
EP1479675A1 (en) * 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Indazole-derivatives as factor Xa inhibitors
DE10322469A1 (de) * 2003-05-19 2004-12-16 Bayer Healthcare Ag Heterocyclische Verbindungen
EP1568698A1 (en) * 2004-02-27 2005-08-31 Aventis Pharma Deutschland GmbH Pyrrole-derivatives as factor Xa inhibitors

Also Published As

Publication number Publication date
CA2559948A1 (en) 2005-10-13
AU2005229320A1 (en) 2005-10-13
JP2007535497A (ja) 2007-12-06
UY28787A1 (es) 2005-09-30
EP1723164A1 (en) 2006-11-22
BRPI0508320A (pt) 2007-07-24
EP1571154A1 (en) 2005-09-07
GT200500026A (es) 2006-06-09
IL177470A0 (en) 2006-12-10
US20070179122A1 (en) 2007-08-02
WO2005095440A1 (en) 2005-10-13
TW200540187A (en) 2005-12-16
PE20051160A1 (es) 2006-02-07
CN1926148A (zh) 2007-03-07
KR20060122950A (ko) 2006-11-30

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