PE20030593A1 - DERIVADOS DE INDOL COMO INHIBIDORES DEL FACTOR Xa - Google Patents

DERIVADOS DE INDOL COMO INHIBIDORES DEL FACTOR Xa

Info

Publication number
PE20030593A1
PE20030593A1 PE2002001105A PE2002001105A PE20030593A1 PE 20030593 A1 PE20030593 A1 PE 20030593A1 PE 2002001105 A PE2002001105 A PE 2002001105A PE 2002001105 A PE2002001105 A PE 2002001105A PE 20030593 A1 PE20030593 A1 PE 20030593A1
Authority
PE
Peru
Prior art keywords
alkyl
aryl
heteroaryl
halogen
inhibitors
Prior art date
Application number
PE2002001105A
Other languages
English (en)
Inventor
Melanie Essrich
Hans Matter
David William Will
Kurt Ritter
Volkmar Wehner
Marc Nazare
Original Assignee
Sanofi Aventis Deutschland
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 Sanofi Aventis Deutschland filed Critical Sanofi Aventis Deutschland
Publication of PE20030593A1 publication Critical patent/PE20030593A1/es

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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
    • 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
    • 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
    • A61P9/08—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
    • C04—CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
    • C04B—LIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
    • C04B35/00—Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/622—Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/626—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
    • C04B35/63—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
    • C04B35/632—Organic additives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/22—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an aralkyl radical 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • 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

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Ceramic Engineering (AREA)
  • Manufacturing & Machinery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Inorganic Chemistry (AREA)
  • Structural Engineering (AREA)
  • Materials Engineering (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

SE REFIERE A DERIVADOS DE INDOL DE FORMULA I DONDE R0 ES ARILO, HETEROARILO OPCIONALMENTE SUSTITUIDO CON R8; R8 ES HALOGENO, NO2, CN, CONH2, OH, NH2, OCF3, ARILO, ALQUILO; Q ES UN ENLACE, CO, NR10CO, SO2 ALQUILENO-CO-NR10, NR10CONR10, ENTRE OTROS; R1 ES H, ALQUILO, HETEROARILO; R2 ES ENLACE, ALQUILENO; R1 Y R7 FORMAN UN GRUPO CICLICO; R1-N-R2-V PUEDE FORMAR UN GRUPO CICLICO; R14 ES HALOGENO, OH, =O, ALQUILO, ALCOXI, ENTRE OTROS; V ES RESTO CICLICO, ARILO, HETEROARILO; G ES ENLACE, (CH2)m-NR10-SO2-NR10-(CH2)n, (CH2)m, (CH2)m-CH(OH)-(CH2)n, (CH2)m-O-(CH2)n, ENTRE OTROS; n Y m SON 0-6; R10 ES H, PERFLUOROALQUILO, ALQUILO; M ES H, ALQUILO, CONR11R12, (CH2)mNR10, ARILO, ENTRE OTROS; R11 Y R12 SON H, ALQUILO, ARILO, HETEROARILO; R3, R4, R5, R6, R7 SON H, HALOGENO, ALQUILO, PERFLUOROALQUILO, O-ALQUILO, NO2, CN, OH, FENILOXI, BENCILOXI, COOR11, ENTRE OTROS. SON COMPUESTOS PREFERIDOS (1-ISOPROPIL-PIPERIDIN-4-IL)-AMIDA DEL ACIDO 1-[5-(5-CLORO-TIOFEN-2-IL)-ISOXAZOL-3-ILMETIL]-1H-INDOL-2-CARBOXILICO; (1-ISOPROPIL-PIPERIDIN-4-IL)-AMIDA DEL ACIDO 1-[5-(5-CLORO-TIOFEN-2-IL)-ISOXAZOL-3-ILMETIL]-1H-INDOL-2-CARBOXILICO; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS SON INHIBIDORES DE LOS FACTORES Xa, VIIa DE LAS ENZIMAS DE LA COAGULACION O PARA INFLUIR EN LA COAGULACION DE SANGRE O EN FIBRINOLISIS Y PUEDE SER UTIL PARA EL TRATAMIENTO DE TRASTORNOS CARDIOVASCULARES, ENFERMEDAES TROMBOEMBOLICAS, RESTENOSIS
PE2002001105A 2001-11-22 2002-11-19 DERIVADOS DE INDOL COMO INHIBIDORES DEL FACTOR Xa PE20030593A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP01127809A EP1314733A1 (en) 2001-11-22 2001-11-22 Indole-2-carboxamides as factor Xa inhibitors

Publications (1)

Publication Number Publication Date
PE20030593A1 true PE20030593A1 (es) 2003-08-21

Family

ID=8179313

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2002001105A PE20030593A1 (es) 2001-11-22 2002-11-19 DERIVADOS DE INDOL COMO INHIBIDORES DEL FACTOR Xa

Country Status (31)

Country Link
US (3) US6906084B2 (es)
EP (2) EP1314733A1 (es)
JP (1) JP4664592B2 (es)
KR (2) KR100954508B1 (es)
CN (1) CN1283638C (es)
AR (1) AR037656A1 (es)
AU (1) AU2002351918B2 (es)
BR (1) BR0214396A (es)
CA (1) CA2467374C (es)
CO (1) CO5580764A2 (es)
EC (1) ECSP045115A (es)
HK (1) HK1070352A1 (es)
HR (1) HRP20040453A2 (es)
HU (1) HUP0402063A3 (es)
IL (2) IL162105A0 (es)
MA (1) MA27350A1 (es)
ME (1) MEP43008A (es)
MX (1) MXPA04004797A (es)
MY (1) MY131516A (es)
NO (1) NO327466B1 (es)
NZ (1) NZ533044A (es)
OA (1) OA12727A (es)
PE (1) PE20030593A1 (es)
PL (1) PL210986B1 (es)
RS (1) RS40404A (es)
RU (1) RU2299881C2 (es)
TN (1) TNSN04091A1 (es)
TW (1) TWI291950B (es)
UA (1) UA78731C2 (es)
WO (1) WO2003044014A1 (es)
ZA (1) ZA200402945B (es)

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