HUP0302671A2 - Indol-3-il-származékok, eljárás az előállításukra, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények - Google Patents

Indol-3-il-származékok, eljárás az előállításukra, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények

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Publication number
HUP0302671A2
HUP0302671A2 HU0302671A HUP0302671A HUP0302671A2 HU P0302671 A2 HUP0302671 A2 HU P0302671A2 HU 0302671 A HU0302671 A HU 0302671A HU P0302671 A HUP0302671 A HU P0302671A HU P0302671 A2 HUP0302671 A2 HU P0302671A2
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HU
Hungary
Prior art keywords
het
nhr6
conh
hal
group
Prior art date
Application number
HU0302671A
Other languages
English (en)
Inventor
Simon Goodman
Rudolf Gottschlich
Matthias Wiesner
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Merck Patent 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.)
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Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of HUP0302671A2 publication Critical patent/HUP0302671A2/hu

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

A találmány szerinti vegyületek (I) általános képletében A és Bjelentése egymástól függetlenül O, S, NH, NR7, CO, CONH, NHCO vagyközvetlen kötés, X jelentése adott esetben R4 vagy R5 csoporttalmonoszubsztituált 1vagy 2 szénatomos alkiléncsoport vagy közvetlenkötés, R1 jelentése H, Z vagy -(CH2)o-Ar, R2 jelentése H, R' vagy -C(O)Z, R3 jelentése -NHR6, -NR6-C(=NR6)-NHR6, -C(=NR6)-NHR6, -NR6-C(=NR9)-NHR6, -C(=NR9)-NHR6 vagy Het1, R4 és R5 jelentése egymástólfüggetlenül H, oxocsoport; R7, -(CH2)o-Ar, -C(O)-(CH2)o-Ar, -C(O)-(CH2)o-R7, -C(O)-(CH2)o-Het, Het, NHR6, NHAr, NH-Het, CONH-R7, CONH-(CH2)o-Ar, CONH-(CH2)o-Het, OR7, OAr, OR6 vagy O-Het, R6 jelentése H,-C(O)R7, -C(O)-Ar, -C(O)-Het, R7, COOR7, COO-(CH2)o-Ar, COO-(CH2)o-Het, SO2-Ar, SO2R7 vagy SO2-Het, R7 jelentése 1-10 szénatomosalkilcsoport vagy 3-10 szénatomos cikloalkilcsoport, R8 jelentése Hal,NO2, CN, Z, -(CH2)o-Ar, COOR1, OR1, CF3, OCF3, SO2R1, NHR1, N(R1)2,NH-C(O)R1, NHCOOR1, COOH, COOZ vagy C(O)R1, R9 jelentése CN vagy NO2,Z jelentése 1-6 szénatomos alkilcsoport; Ar jelentése adott esetbenegy vagy több R8 csoporttal szubsztituált Hal jelentése fluoratom,klóratom, brómatom vagy jódatom, Het jelentése telített, részben vagyegészen telítetlen mono- vagy biciklusos, 5-10 tagú heterociklusoscsoport, amely 1 vagy 2 nitrogénatomot és/vagy 1 vagy 2 kénatomot vagyoxigénatomot tartalmaz, és amely adott esetben 1 vagy 2 R8 csoporttalszubsztituálva lehet, Het1 jelentése telített, részben vagy egészentelítetlen; mono- vagy biciklusos, 5-10 tagú heterociklusos csoport,amely 1-4 nitrogénatomot tartalmaz, és amely adott esetben 1 vagy 2Hal, R7, OR7, CN, NHZ, oxocsoport vagy NO2 szubsztituensselszubsztituálva lehet, n értéke 0, 1 vagy 2, m értéke 0, 1, 2, 3, 4, 5vagy 6, o értéke 0, 1 vagy 2, valamint ezek fiziológiailagalkalmazható sói és szolvátjai. A találmány kiterjed a fentivegyületek előállítására és gyógyszerként történő alkalmazására. Ó
HU0302671A 2000-02-11 2001-01-05 Indol-3-il-származékok, eljárás az előállításukra, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények HUP0302671A2 (hu)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10006139A DE10006139A1 (de) 2000-02-11 2000-02-11 Indol-3-yl-Derivate
PCT/EP2001/000084 WO2001058893A2 (de) 2000-02-11 2001-01-05 Indol-3-yl-derivate und deren verwendung als integrin-inhibitoren

Publications (1)

Publication Number Publication Date
HUP0302671A2 true HUP0302671A2 (hu) 2003-12-29

Family

ID=7630611

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0302671A HUP0302671A2 (hu) 2000-02-11 2001-01-05 Indol-3-il-származékok, eljárás az előállításukra, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények

Country Status (28)

Country Link
US (1) US6743810B2 (hu)
EP (1) EP1254133B9 (hu)
JP (1) JP4938194B2 (hu)
KR (1) KR20020073585A (hu)
CN (1) CN1214026C (hu)
AR (1) AR027398A1 (hu)
AT (1) ATE293620T1 (hu)
AU (2) AU2001231664C1 (hu)
BR (1) BR0108154A (hu)
CA (1) CA2399813C (hu)
CO (1) CO5261548A1 (hu)
CZ (1) CZ20022616A3 (hu)
DE (2) DE10006139A1 (hu)
EC (1) ECSP013923A (hu)
ES (1) ES2240400T3 (hu)
HK (1) HK1051863A1 (hu)
HU (1) HUP0302671A2 (hu)
IL (1) IL151154A0 (hu)
MX (1) MXPA02007732A (hu)
NO (1) NO20023770D0 (hu)
NZ (1) NZ521260A (hu)
PE (1) PE20011125A1 (hu)
PL (1) PL356427A1 (hu)
PT (1) PT1254133E (hu)
RU (1) RU2257380C2 (hu)
SK (1) SK11152002A3 (hu)
WO (1) WO2001058893A2 (hu)
ZA (1) ZA200207273B (hu)

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PL1667668T3 (pl) * 2003-10-01 2008-10-31 Merck Patent Gmbh Antagoniści integryny alfavbeta3 oraz alfavbeta6 jako czynniki przeciwzwłóknieniowe
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Also Published As

Publication number Publication date
US20030045728A1 (en) 2003-03-06
ES2240400T3 (es) 2005-10-16
ATE293620T1 (de) 2005-05-15
EP1254133A2 (de) 2002-11-06
US6743810B2 (en) 2004-06-01
JP4938194B2 (ja) 2012-05-23
ZA200207273B (en) 2003-12-10
PL356427A1 (en) 2004-06-28
PT1254133E (pt) 2005-09-30
SK11152002A3 (sk) 2003-01-09
AU2001231664C1 (en) 2006-10-05
CA2399813A1 (en) 2001-08-16
AR027398A1 (es) 2003-03-26
KR20020073585A (ko) 2002-09-27
AU3166401A (en) 2001-08-20
CN1214026C (zh) 2005-08-10
AU2001231664B2 (en) 2006-02-23
JP2003530319A (ja) 2003-10-14
HK1051863A1 (en) 2003-08-22
EP1254133B9 (de) 2005-09-07
DE50105955D1 (de) 2005-05-25
EP1254133B1 (de) 2005-04-20
CA2399813C (en) 2010-03-09
CZ20022616A3 (cs) 2002-10-16
MXPA02007732A (es) 2002-10-11
NO20023770L (no) 2002-08-09
WO2001058893A3 (de) 2002-04-18
RU2002123332A (ru) 2004-01-10
WO2001058893A2 (de) 2001-08-16
CN1398264A (zh) 2003-02-19
RU2257380C2 (ru) 2005-07-27
PE20011125A1 (es) 2001-11-07
CO5261548A1 (es) 2003-03-31
ECSP013923A (es) 2002-09-27
NO20023770D0 (no) 2002-08-09
IL151154A0 (en) 2003-04-10
NZ521260A (en) 2004-02-27
BR0108154A (pt) 2003-01-21
DE10006139A1 (de) 2001-08-16

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