PE20011125A1 - Derivados de indol-3-ilo como inhibidores de la integrina - Google Patents

Derivados de indol-3-ilo como inhibidores de la integrina

Info

Publication number
PE20011125A1
PE20011125A1 PE2001000143A PE2001000143A PE20011125A1 PE 20011125 A1 PE20011125 A1 PE 20011125A1 PE 2001000143 A PE2001000143 A PE 2001000143A PE 2001000143 A PE2001000143 A PE 2001000143A PE 20011125 A1 PE20011125 A1 PE 20011125A1
Authority
PE
Peru
Prior art keywords
indol
nhr6
het
ilo
nr6c
Prior art date
Application number
PE2001000143A
Other languages
English (en)
Inventor
Simon Goodman
Matthias Wiesner
Rudolf Gottschlich
Original Assignee
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.)
Filing date
Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of PE20011125A1 publication Critical patent/PE20011125A1/es

Links

Classifications

    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • 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
    • 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
    • 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
    • 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

Abstract

SE REFIERE A DERIVADOS DE INDOL-3-ILO DE FORMULA I DONDE A Y B SON O, S, NH; NR7, CO, CONH, NHCO, ENLACE; X ES ALQUILENO SUSTITUIDO CON R4 O R5; R1 ES H, Z, (CH2)o-Ar, R2 ES H, R7, COZ; R3 ES NHR6, -NR6C(=NR6)NHR6, C(=NR6)-NHR6, NR6C(=NR9)-NHR6, HET1; R4 Y R5 SON H, OXO, R7, (CH2)o-Ar, CO(CH2)oAr, O-HET, ENTRE OTROS; R6 ES H, COR7, CO-Ar, CO-HET; ENTRE OTROS; R7 ES ALQUILO C1-C10, CICLOALQUILO C3-C10; R8 ES Hal, NO2, CN, Z, (CH2)o-Ar, ENTRE OTROS; R9 ES CN, NO2 ; Z ES ALQUILO C1-C6; Ar ES ARILO; HAL ES F, Cl, Br, I; HET ES MONO O BICICLO DE 5-10 MIEMBROS; HET1 ES BICICLOHETEROCICLO CON 5-10 MIEMBROS; n ES 0-2; m ES 0-6; o ES 0-2. SON COMPUESTOS PREFERIDOS ACIDO 3-FENIL-3-{6-[3-(PIRIDIN-2-IL-AMINO)-PROPOXI]-1H-INDOL-3-IL}-PROPIONICO; ACIDO 3-FENIL-3-{6-[4-(PIRIDIN-2-IL-AMINO)-BUTOXI]-1H-INDOL-3-IL}-PROPIONICO, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. EL COMPUESTO I ES UN INHIBIDOR DE INTEGRINA av, ß3, ß5 CON LIGANDOS Y PUEDE SER UTIL PARA TRATAMIENTO DE TROMBOSIS, INFARTO DEL MIOCARDIO, ENFERMEDAD CARDIACA CORONARIA, ARTERIOESCLEROSIS, INFLAMACION, RESTENOSIS, ARTRITIS REUMATICA
PE2001000143A 2000-02-11 2001-02-09 Derivados de indol-3-ilo como inhibidores de la integrina PE20011125A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10006139A DE10006139A1 (de) 2000-02-11 2000-02-11 Indol-3-yl-Derivate

Publications (1)

Publication Number Publication Date
PE20011125A1 true PE20011125A1 (es) 2001-11-07

Family

ID=7630611

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2001000143A PE20011125A1 (es) 2000-02-11 2001-02-09 Derivados de indol-3-ilo como inhibidores de la integrina

Country Status (28)

Country Link
US (1) US6743810B2 (es)
EP (1) EP1254133B9 (es)
JP (1) JP4938194B2 (es)
KR (1) KR20020073585A (es)
CN (1) CN1214026C (es)
AR (1) AR027398A1 (es)
AT (1) ATE293620T1 (es)
AU (2) AU2001231664C1 (es)
BR (1) BR0108154A (es)
CA (1) CA2399813C (es)
CO (1) CO5261548A1 (es)
CZ (1) CZ20022616A3 (es)
DE (2) DE10006139A1 (es)
EC (1) ECSP013923A (es)
ES (1) ES2240400T3 (es)
HK (1) HK1051863A1 (es)
HU (1) HUP0302671A2 (es)
IL (1) IL151154A0 (es)
MX (1) MXPA02007732A (es)
NO (1) NO20023770L (es)
NZ (1) NZ521260A (es)
PE (1) PE20011125A1 (es)
PL (1) PL356427A1 (es)
PT (1) PT1254133E (es)
RU (1) RU2257380C2 (es)
SK (1) SK11152002A3 (es)
WO (1) WO2001058893A2 (es)
ZA (1) ZA200207273B (es)

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US20040138284A1 (en) * 2000-02-11 2004-07-15 Matthias Wiesner Indol-3-yl derivatives
US20040058915A1 (en) * 2000-08-29 2004-03-25 Khanna Ish Kumar Compounds containing a bicyclic ring system useful as alpha v beta 3 antagonists
JP5054274B2 (ja) * 2000-11-01 2012-10-24 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング 眼の疾患を治療するための方法および組成物
GB0028367D0 (en) * 2000-11-21 2001-01-03 Celltech Chiroscience Ltd Chemical compounds
KR100854424B1 (ko) * 2001-01-29 2008-08-27 3-디멘져널 파마슈티칼즈 인코오포레이티드 치환된 인돌 및 인테그린 길항제로서의 이들의 용도
US6872730B2 (en) 2001-04-27 2005-03-29 3-Dimensional Pharmaceuticals, Inc. Substituted benzofurans and benzothiophenes, methods of making and methods of use as integrin antagonists
EP1411926B1 (en) * 2001-08-01 2005-06-01 MERCK PATENT GmbH Integrin inhibitors for the treatment of eye diseases
CA2476120A1 (en) * 2002-02-14 2003-08-21 Merck Patent Gesellschaft Mit Beschraenkter Haftung Methods and compositions for the treatment of eye diseases
US20070208026A1 (en) * 2003-04-07 2007-09-06 Liu Kevin N-Containing Heteroaromatic Compounds As Modulators Of Ppars And Methods Of Treating Metabolic Disorders
US7592361B2 (en) * 2003-04-28 2009-09-22 Bayer Pharmaceuticals Corporation Indole acetic acid derivatives and their use as pharmaceutical agents
US7211588B2 (en) 2003-07-25 2007-05-01 Zentaris Gmbh N-substituted indolyl-3-glyoxylamides, their use as medicaments and process for their preparation
DE10337863A1 (de) * 2003-08-18 2005-03-17 Merck Patent Gmbh Verwendung von Chromen-4-on-Derivaten
EP1667668B1 (en) * 2003-10-01 2008-07-02 MERCK PATENT GmbH Alfavbeta3 and alfavbeta6 integrin antagonists as antifibrotic agents
JP2007536344A (ja) * 2004-05-04 2007-12-13 ノボ　ノルディスク　アクティーゼルスカブ 新規のインドール誘導体
US8003806B2 (en) * 2004-11-12 2011-08-23 OSI Pharmaceuticals, LLC Integrin antagonists useful as anticancer agents
US7777040B2 (en) 2005-05-03 2010-08-17 Cgi Pharmaceuticals, Inc. Certain substituted ureas, as modulators of kinase activity
CN102335168B (zh) * 2011-10-25 2014-04-02 合肥博太医药生物技术发展有限公司 吲哚-3-甲醇、二吲哚甲烷及其衍生物在制备治疗骨质疏松药物中的应用
AR094812A1 (es) * 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
SG11201700703XA (en) 2014-08-18 2017-03-30 Eisai R&D Man Co Ltd Salt of monocyclic pyridine derivative and crystal thereof
SG11202007591RA (en) 2018-03-28 2020-09-29 Eisai R&D Man Co Ltd Therapeutic agent for hepatocellular carcinoma

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Also Published As

Publication number Publication date
DE10006139A1 (de) 2001-08-16
EP1254133B9 (de) 2005-09-07
CZ20022616A3 (cs) 2002-10-16
AU3166401A (en) 2001-08-20
NZ521260A (en) 2004-02-27
AR027398A1 (es) 2003-03-26
IL151154A0 (en) 2003-04-10
CA2399813A1 (en) 2001-08-16
ECSP013923A (es) 2002-09-27
AU2001231664C1 (en) 2006-10-05
NO20023770D0 (no) 2002-08-09
US6743810B2 (en) 2004-06-01
HUP0302671A2 (hu) 2003-12-29
JP2003530319A (ja) 2003-10-14
CN1214026C (zh) 2005-08-10
DE50105955D1 (de) 2005-05-25
CA2399813C (en) 2010-03-09
BR0108154A (pt) 2003-01-21
CO5261548A1 (es) 2003-03-31
EP1254133B1 (de) 2005-04-20
CN1398264A (zh) 2003-02-19
WO2001058893A2 (de) 2001-08-16
US20030045728A1 (en) 2003-03-06
RU2257380C2 (ru) 2005-07-27
ZA200207273B (en) 2003-12-10
PL356427A1 (en) 2004-06-28
EP1254133A2 (de) 2002-11-06
JP4938194B2 (ja) 2012-05-23
AU2001231664B2 (en) 2006-02-23
MXPA02007732A (es) 2002-10-11
NO20023770L (no) 2002-08-09
WO2001058893A3 (de) 2002-04-18
PT1254133E (pt) 2005-09-30
RU2002123332A (ru) 2004-01-10
HK1051863A1 (en) 2003-08-22
KR20020073585A (ko) 2002-09-27
ATE293620T1 (de) 2005-05-15
SK11152002A3 (sk) 2003-01-09
ES2240400T3 (es) 2005-10-16

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