NOUVEAUX DERIVES DE L'INDOLE, LEUR PREPARATION A TITRE DE MEDICAMENTS, COMPOSITIONS PHARMACEUTIQUES ET NOTAMMENT COMME INHIBITEURS DE KDR
2-(Pyrazolyl or indazolyl)-indole derivatives (I), in all possible racemic, enantiomeric or diasteroisomeric forms, their addition salts with (in)organic acids or inorganic bases are new. 2-(pyrazolyl or indazolyl)-indole derivatives of formula (I), in all possible racemic, enantiomeric or diasteroi...
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creator | BOUCHARD HERVE UGOLINI ANTONIO |
description | 2-(Pyrazolyl or indazolyl)-indole derivatives (I), in all possible racemic, enantiomeric or diasteroisomeric forms, their addition salts with (in)organic acids or inorganic bases are new. 2-(pyrazolyl or indazolyl)-indole derivatives of formula (I), in all possible racemic, enantiomeric or diasteroisomeric forms, their addition salts with (in)organic acids or inorganic bases are new. [Image] R 1>pyrazolyl or indazolyl, optionally substituted by one or more of halo, hydroxy, nitro, cyano, R 4>, OR4, SR 4>, COR 4>, OCOR 4>, COOR 4>, COOH (optionally as salt), NR 5>COR 4>, NR 5>COOR 4>, S(O) nR 4>, S(O) nOR 4>, NR5-SO 2R 4>, OS(O) nR 4>, NY 1>Y 2>, CONY 1>Y 2>, OCONY 1>Y 2>, NR5CONY 1>Y 2>, S(O) nNY 1>Y 2>or optionally substituted thienyl; R 2>, R 3>hydrogen, halo, hydroxy, nitro, cyano, R 4>, OR 4>, COR 4>, OCOR 4>, COOR 4>, COOH, NR 5>COR 4>, NR5COOR 4>, S(O) nR 4>, S(O) nOR 4>, NR 5>-SO 2R 4>, NY 1>Y 2>, CONY 1>Y 2>, NR 5>CONY 1>Y 2>, S(O) nNY 1>Y 2>or OCONY 1>Y 2>; or R 2>+ R 3>optionally substituted 4-6 membered ring optionally containing one or more heteroatoms O,N or S; n : 0-2; R 4>alkyl, alk-NY 1>Y 2>, alk-CONY 1>Y 2>, alkenyl, alkynyl, cycloalkyl, (hetero)aryl, (hetero)cycloalkylalkyl, heteroarylalkyl or aralkyl, all optionally substituted; R 5>hydrogen, alkyl, alkenyl, (hetero)cycloalkyl, (hetero)aryl, aralkyl, (hetero)cycloalkylalkyl, or heteroarylalkyl, all optionally substituted; Y 1>, Y 2>hydrogen, alkyl, alkenyl, (hetero)cycloalkyl, heterocycloalkylalkyl, (hetero)aryl, (hetero)aralkyl or (hetero)arylcarboxy, (all optionally substituted by one or more of halo, hydroxy, alkoxy, alkyl (optionally substituted by hydroxy or carboxy), cyano, nitro, trifluoromethyl, trifluoromethoxy, carboxy (optionally as salt or optionally substituted alkyl ester), Nalk-CO-alk, NHCO-alk, S(O) n-alk, NHS(O) n-alkyl, NHCO-NY 3>Y 4>, CONY 3>Y 4>, S(O) nNY 3>Y 4>, aryl, arylalkoxy, aryloxy, aryloxyalkyl, heteroaryl or heterocycloalkyl (both optionally substituted by one or more T 1>)); or NY 1>Y 2>optionally substituted ring; Y 3>, Y 4>hydrogen, aryl or alkyl (optionally substituted by one or more T 1>); T 1>halo, alkyl, carboxy (optionally as salt or ester) or amino (optionally substituted by 1 or 2 alkyl or by one phenyl (optionally substituted by a dioxol residue)); and alk : 1-6C alkyl. ACTIVITY : Cytostatic; Antiallergic; Antiasthmatic; Anticoagulant; Thrombolytic; Ophthalmological; Antipsoriatic; Antiasthmatic; Antirheumatic; Antidiabetic; Antiarteriosclerotic; A |
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fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_FR2854159B1</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>FR2854159B1</sourcerecordid><originalsourceid>FETCH-epo_espacenet_FR2854159B13</originalsourceid><addsrcrecordid>eNqNzbEOgjAUhWEWB6O-w91ccEAl0bHQS7iRtlhuiRshpk5GSfAlfGup8QGc_uXLOfPorY1rUbgLSLTUYjMVqjVpaSqMoUJnobZYCyuYjAYBTGwxKIWScqFQcxNDblRtGgqmgboUVokcHdPZTZPIoA0LFWyQCoF0SRnxNP99PEm7jGa3_j761a-LCArkvNz44dn5ceiv_uFfXWG3h3SfpMcs2f1BPhvdPl4</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>NOUVEAUX DERIVES DE L'INDOLE, LEUR PREPARATION A TITRE DE MEDICAMENTS, COMPOSITIONS PHARMACEUTIQUES ET NOTAMMENT COMME INHIBITEURS DE KDR</title><source>esp@cenet</source><creator>BOUCHARD HERVE ; UGOLINI ANTONIO</creator><creatorcontrib>BOUCHARD HERVE ; UGOLINI ANTONIO</creatorcontrib><description>2-(Pyrazolyl or indazolyl)-indole derivatives (I), in all possible racemic, enantiomeric or diasteroisomeric forms, their addition salts with (in)organic acids or inorganic bases are new. 2-(pyrazolyl or indazolyl)-indole derivatives of formula (I), in all possible racemic, enantiomeric or diasteroisomeric forms, their addition salts with (in)organic acids or inorganic bases are new. [Image] R 1>pyrazolyl or indazolyl, optionally substituted by one or more of halo, hydroxy, nitro, cyano, R 4>, OR4, SR 4>, COR 4>, OCOR 4>, COOR 4>, COOH (optionally as salt), NR 5>COR 4>, NR 5>COOR 4>, S(O) nR 4>, S(O) nOR 4>, NR5-SO 2R 4>, OS(O) nR 4>, NY 1>Y 2>, CONY 1>Y 2>, OCONY 1>Y 2>, NR5CONY 1>Y 2>, S(O) nNY 1>Y 2>or optionally substituted thienyl; R 2>, R 3>hydrogen, halo, hydroxy, nitro, cyano, R 4>, OR 4>, COR 4>, OCOR 4>, COOR 4>, COOH, NR 5>COR 4>, NR5COOR 4>, S(O) nR 4>, S(O) nOR 4>, NR 5>-SO 2R 4>, NY 1>Y 2>, CONY 1>Y 2>, NR 5>CONY 1>Y 2>, S(O) nNY 1>Y 2>or OCONY 1>Y 2>; or R 2>+ R 3>optionally substituted 4-6 membered ring optionally containing one or more heteroatoms O,N or S; n : 0-2; R 4>alkyl, alk-NY 1>Y 2>, alk-CONY 1>Y 2>, alkenyl, alkynyl, cycloalkyl, (hetero)aryl, (hetero)cycloalkylalkyl, heteroarylalkyl or aralkyl, all optionally substituted; R 5>hydrogen, alkyl, alkenyl, (hetero)cycloalkyl, (hetero)aryl, aralkyl, (hetero)cycloalkylalkyl, or heteroarylalkyl, all optionally substituted; Y 1>, Y 2>hydrogen, alkyl, alkenyl, (hetero)cycloalkyl, heterocycloalkylalkyl, (hetero)aryl, (hetero)aralkyl or (hetero)arylcarboxy, (all optionally substituted by one or more of halo, hydroxy, alkoxy, alkyl (optionally substituted by hydroxy or carboxy), cyano, nitro, trifluoromethyl, trifluoromethoxy, carboxy (optionally as salt or optionally substituted alkyl ester), Nalk-CO-alk, NHCO-alk, S(O) n-alk, NHS(O) n-alkyl, NHCO-NY 3>Y 4>, CONY 3>Y 4>, S(O) nNY 3>Y 4>, aryl, arylalkoxy, aryloxy, aryloxyalkyl, heteroaryl or heterocycloalkyl (both optionally substituted by one or more T 1>)); or NY 1>Y 2>optionally substituted ring; Y 3>, Y 4>hydrogen, aryl or alkyl (optionally substituted by one or more T 1>); T 1>halo, alkyl, carboxy (optionally as salt or ester) or amino (optionally substituted by 1 or 2 alkyl or by one phenyl (optionally substituted by a dioxol residue)); and alk : 1-6C alkyl. ACTIVITY : Cytostatic; Antiallergic; Antiasthmatic; Anticoagulant; Thrombolytic; Ophthalmological; Antipsoriatic; Antiasthmatic; Antirheumatic; Antidiabetic; Antiarteriosclerotic; Anorectic; Antiparkinsonian; Antidepressant; Neuroleptic; Nootropic; Neuroprotective; Analgesic; Immunomodulator; Antiangiogenic; Vulnerary; Osteopathic. No details of tests for these activities are given. MECHANISM OF ACTION : Inhibition of protein kinases, particularly vascular endothelial growth factor receptor 2 (KDR) and focal adhesion kinase (FAK), and insulin-like growth factor 1 receptor.</description><language>fre</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><creationdate>2008</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20080111&DB=EPODOC&CC=FR&NR=2854159B1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,778,883,25547,76298</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20080111&DB=EPODOC&CC=FR&NR=2854159B1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>BOUCHARD HERVE</creatorcontrib><creatorcontrib>UGOLINI ANTONIO</creatorcontrib><title>NOUVEAUX DERIVES DE L'INDOLE, LEUR PREPARATION A TITRE DE MEDICAMENTS, COMPOSITIONS PHARMACEUTIQUES ET NOTAMMENT COMME INHIBITEURS DE KDR</title><description>2-(Pyrazolyl or indazolyl)-indole derivatives (I), in all possible racemic, enantiomeric or diasteroisomeric forms, their addition salts with (in)organic acids or inorganic bases are new. 2-(pyrazolyl or indazolyl)-indole derivatives of formula (I), in all possible racemic, enantiomeric or diasteroisomeric forms, their addition salts with (in)organic acids or inorganic bases are new. [Image] R 1>pyrazolyl or indazolyl, optionally substituted by one or more of halo, hydroxy, nitro, cyano, R 4>, OR4, SR 4>, COR 4>, OCOR 4>, COOR 4>, COOH (optionally as salt), NR 5>COR 4>, NR 5>COOR 4>, S(O) nR 4>, S(O) nOR 4>, NR5-SO 2R 4>, OS(O) nR 4>, NY 1>Y 2>, CONY 1>Y 2>, OCONY 1>Y 2>, NR5CONY 1>Y 2>, S(O) nNY 1>Y 2>or optionally substituted thienyl; R 2>, R 3>hydrogen, halo, hydroxy, nitro, cyano, R 4>, OR 4>, COR 4>, OCOR 4>, COOR 4>, COOH, NR 5>COR 4>, NR5COOR 4>, S(O) nR 4>, S(O) nOR 4>, NR 5>-SO 2R 4>, NY 1>Y 2>, CONY 1>Y 2>, NR 5>CONY 1>Y 2>, S(O) nNY 1>Y 2>or OCONY 1>Y 2>; or R 2>+ R 3>optionally substituted 4-6 membered ring optionally containing one or more heteroatoms O,N or S; n : 0-2; R 4>alkyl, alk-NY 1>Y 2>, alk-CONY 1>Y 2>, alkenyl, alkynyl, cycloalkyl, (hetero)aryl, (hetero)cycloalkylalkyl, heteroarylalkyl or aralkyl, all optionally substituted; R 5>hydrogen, alkyl, alkenyl, (hetero)cycloalkyl, (hetero)aryl, aralkyl, (hetero)cycloalkylalkyl, or heteroarylalkyl, all optionally substituted; Y 1>, Y 2>hydrogen, alkyl, alkenyl, (hetero)cycloalkyl, heterocycloalkylalkyl, (hetero)aryl, (hetero)aralkyl or (hetero)arylcarboxy, (all optionally substituted by one or more of halo, hydroxy, alkoxy, alkyl (optionally substituted by hydroxy or carboxy), cyano, nitro, trifluoromethyl, trifluoromethoxy, carboxy (optionally as salt or optionally substituted alkyl ester), Nalk-CO-alk, NHCO-alk, S(O) n-alk, NHS(O) n-alkyl, NHCO-NY 3>Y 4>, CONY 3>Y 4>, S(O) nNY 3>Y 4>, aryl, arylalkoxy, aryloxy, aryloxyalkyl, heteroaryl or heterocycloalkyl (both optionally substituted by one or more T 1>)); or NY 1>Y 2>optionally substituted ring; Y 3>, Y 4>hydrogen, aryl or alkyl (optionally substituted by one or more T 1>); T 1>halo, alkyl, carboxy (optionally as salt or ester) or amino (optionally substituted by 1 or 2 alkyl or by one phenyl (optionally substituted by a dioxol residue)); and alk : 1-6C alkyl. ACTIVITY : Cytostatic; Antiallergic; Antiasthmatic; Anticoagulant; Thrombolytic; Ophthalmological; Antipsoriatic; Antiasthmatic; Antirheumatic; Antidiabetic; Antiarteriosclerotic; Anorectic; Antiparkinsonian; Antidepressant; Neuroleptic; Nootropic; Neuroprotective; Analgesic; Immunomodulator; Antiangiogenic; Vulnerary; Osteopathic. No details of tests for these activities are given. MECHANISM OF ACTION : Inhibition of protein kinases, particularly vascular endothelial growth factor receptor 2 (KDR) and focal adhesion kinase (FAK), and insulin-like growth factor 1 receptor.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><subject>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2008</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNzbEOgjAUhWEWB6O-w91ccEAl0bHQS7iRtlhuiRshpk5GSfAlfGup8QGc_uXLOfPorY1rUbgLSLTUYjMVqjVpaSqMoUJnobZYCyuYjAYBTGwxKIWScqFQcxNDblRtGgqmgboUVokcHdPZTZPIoA0LFWyQCoF0SRnxNP99PEm7jGa3_j761a-LCArkvNz44dn5ceiv_uFfXWG3h3SfpMcs2f1BPhvdPl4</recordid><startdate>20080111</startdate><enddate>20080111</enddate><creator>BOUCHARD HERVE</creator><creator>UGOLINI ANTONIO</creator><scope>EVB</scope></search><sort><creationdate>20080111</creationdate><title>NOUVEAUX DERIVES DE L'INDOLE, LEUR PREPARATION A TITRE DE MEDICAMENTS, COMPOSITIONS PHARMACEUTIQUES ET NOTAMMENT COMME INHIBITEURS DE KDR</title><author>BOUCHARD HERVE ; UGOLINI ANTONIO</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_FR2854159B13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>fre</language><creationdate>2008</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><topic>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</topic><toplevel>online_resources</toplevel><creatorcontrib>BOUCHARD HERVE</creatorcontrib><creatorcontrib>UGOLINI ANTONIO</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>BOUCHARD HERVE</au><au>UGOLINI ANTONIO</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>NOUVEAUX DERIVES DE L'INDOLE, LEUR PREPARATION A TITRE DE MEDICAMENTS, COMPOSITIONS PHARMACEUTIQUES ET NOTAMMENT COMME INHIBITEURS DE KDR</title><date>2008-01-11</date><risdate>2008</risdate><abstract>2-(Pyrazolyl or indazolyl)-indole derivatives (I), in all possible racemic, enantiomeric or diasteroisomeric forms, their addition salts with (in)organic acids or inorganic bases are new. 2-(pyrazolyl or indazolyl)-indole derivatives of formula (I), in all possible racemic, enantiomeric or diasteroisomeric forms, their addition salts with (in)organic acids or inorganic bases are new. [Image] R 1>pyrazolyl or indazolyl, optionally substituted by one or more of halo, hydroxy, nitro, cyano, R 4>, OR4, SR 4>, COR 4>, OCOR 4>, COOR 4>, COOH (optionally as salt), NR 5>COR 4>, NR 5>COOR 4>, S(O) nR 4>, S(O) nOR 4>, NR5-SO 2R 4>, OS(O) nR 4>, NY 1>Y 2>, CONY 1>Y 2>, OCONY 1>Y 2>, NR5CONY 1>Y 2>, S(O) nNY 1>Y 2>or optionally substituted thienyl; R 2>, R 3>hydrogen, halo, hydroxy, nitro, cyano, R 4>, OR 4>, COR 4>, OCOR 4>, COOR 4>, COOH, NR 5>COR 4>, NR5COOR 4>, S(O) nR 4>, S(O) nOR 4>, NR 5>-SO 2R 4>, NY 1>Y 2>, CONY 1>Y 2>, NR 5>CONY 1>Y 2>, S(O) nNY 1>Y 2>or OCONY 1>Y 2>; or R 2>+ R 3>optionally substituted 4-6 membered ring optionally containing one or more heteroatoms O,N or S; n : 0-2; R 4>alkyl, alk-NY 1>Y 2>, alk-CONY 1>Y 2>, alkenyl, alkynyl, cycloalkyl, (hetero)aryl, (hetero)cycloalkylalkyl, heteroarylalkyl or aralkyl, all optionally substituted; R 5>hydrogen, alkyl, alkenyl, (hetero)cycloalkyl, (hetero)aryl, aralkyl, (hetero)cycloalkylalkyl, or heteroarylalkyl, all optionally substituted; Y 1>, Y 2>hydrogen, alkyl, alkenyl, (hetero)cycloalkyl, heterocycloalkylalkyl, (hetero)aryl, (hetero)aralkyl or (hetero)arylcarboxy, (all optionally substituted by one or more of halo, hydroxy, alkoxy, alkyl (optionally substituted by hydroxy or carboxy), cyano, nitro, trifluoromethyl, trifluoromethoxy, carboxy (optionally as salt or optionally substituted alkyl ester), Nalk-CO-alk, NHCO-alk, S(O) n-alk, NHS(O) n-alkyl, NHCO-NY 3>Y 4>, CONY 3>Y 4>, S(O) nNY 3>Y 4>, aryl, arylalkoxy, aryloxy, aryloxyalkyl, heteroaryl or heterocycloalkyl (both optionally substituted by one or more T 1>)); or NY 1>Y 2>optionally substituted ring; Y 3>, Y 4>hydrogen, aryl or alkyl (optionally substituted by one or more T 1>); T 1>halo, alkyl, carboxy (optionally as salt or ester) or amino (optionally substituted by 1 or 2 alkyl or by one phenyl (optionally substituted by a dioxol residue)); and alk : 1-6C alkyl. ACTIVITY : Cytostatic; Antiallergic; Antiasthmatic; Anticoagulant; Thrombolytic; Ophthalmological; Antipsoriatic; Antiasthmatic; Antirheumatic; Antidiabetic; Antiarteriosclerotic; Anorectic; Antiparkinsonian; Antidepressant; Neuroleptic; Nootropic; Neuroprotective; Analgesic; Immunomodulator; Antiangiogenic; Vulnerary; Osteopathic. No details of tests for these activities are given. MECHANISM OF ACTION : Inhibition of protein kinases, particularly vascular endothelial growth factor receptor 2 (KDR) and focal adhesion kinase (FAK), and insulin-like growth factor 1 receptor.</abstract><oa>free_for_read</oa></addata></record> |
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subjects | CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS |
title | NOUVEAUX DERIVES DE L'INDOLE, LEUR PREPARATION A TITRE DE MEDICAMENTS, COMPOSITIONS PHARMACEUTIQUES ET NOTAMMENT COMME INHIBITEURS DE KDR |
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