BICYCLIC HETEROAROMATIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS

Opisana suheteroaromatična jedinjenja formule (I): Opisana suheteroaromatična jedinjenja formule (I):         ili njegova so ili solvat; gde Y je CR1 i V je N; ili Y je CR1i V je CR2; R1 predstavlja grupu CH3SO2CH2CH2NHCH2-Ar-,gde Ar se bira između furana i tiazola, od kojih svaki može biti opcionos...

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Hauptverfasser: Smith, Kathryn Jane, Carter, Malcolm Clive, Lackey, Karen Elizabeth, Cockerill, George Stuart, Guntrip, Stephen Barry
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Carter, Malcolm Clive
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Guntrip, Stephen Barry
description Opisana suheteroaromatična jedinjenja formule (I): Opisana suheteroaromatična jedinjenja formule (I):         ili njegova so ili solvat; gde Y je CR1 i V je N; ili Y je CR1i V je CR2; R1 predstavlja grupu CH3SO2CH2CH2NHCH2-Ar-,gde Ar se bira između furana i tiazola, od kojih svaki može biti opcionosupstituisan sa jednim ili dva halo, C1-4 alkil ili C1-4aloksigrupama; R2 je vodonik ili C1-4 alkoksi; ili R2je halo; R3 se bira iz grupe koju čine benzil-, halo-, dihalo- itrihalobenzil, benzoil, piridilmetil, piridilmetoksi, fenoksi, benziloksi,halo-, dihalo- i trihalobenziloksi i benzensulfonil; R4 je halo iliC1-4 alkoksi ili nije prisutan; gde ili (a) R3predstavlja 3-fluorobenziloksi; ili njegova so ili solvat; gde Y je CR 1 i V je N; ili Y je CR 1 i V je CR 2 ; R 1 predstavlja grupu CH 3 SO 2 CH 2 CH 2 NHCH 2 -Ar-,gde Ar se bira između furana i tiazola, od kojih svaki može biti opcionosupstituisan sa jednim ili dva halo, C 1-4 alkil ili C 1-4 aloksigrupama; R 2 je vodonik ili C 1-4 alkoksi; ili R 2 je halo; R 3 se bira iz grupe koju čine benzil-, halo-, dihalo- itrihalobenzil, benzoil, piridilmetil, piridilmetoksi, fenoksi, benziloksi,halo-, dihalo- i trihalobenziloksi i benzensulfonil; R 4 je halo iliC 1-4 alkoksi ili nije prisutan; gde ili (a) R 3 predstavlja 3-fluorobenziloksi; i/ili (b) R4 se bira od halo i supstituent je u položaju 3fenil prstena; i halo predstavlja fluoro, hloro ili bromo, kao i njihovodobijanje, farmaceutski preparati koji ih sadrže i njihova upotreba u medicini. i/ili (b) R 4 se bira od halo i supstituent je u položaju 3fenil prstena; i halo predstavlja fluoro, hloro ili bromo, kao i njihovodobijanje, farmaceutski preparati koji ih sadrže i njihova upotreba u medicini. Compounds of formula (I) and salts or solvates thereof are disclosed wherein Y is CR and V is N; or Y is CR and V is CR ; R represents CH3SO2CH2CH2NHCH2-Ar-, wherein Ar is furan or thiazole, each of which may optionally be substituted by one or two halo, C1-4 alkyl or C1-4 alkoxy groups; R is hydrogen C1-4 alkoxy or halo; R is benzyl, halo-, dihalo- or trihalobenzyl, benzoyl, pyridylmethyl, pyridylmethoxy, phenoxy, benzyloxy, halo-, dihalo- or trihalobenzyloxy or benzenesulphonyl; R is halo or C1-4 alkoxy or is not present; and wherein either (a) R represents 3-fluorobenzyloxy; and/or (b) R is halo and is substituted in the 3-position of the phenyl ring; and wherein halo represents fluoro, chloro or bromo. Processes for the preparation of the compounds, pharmaceutical
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fullrecord <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_ME00757B</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>ME00757B</sourcerecordid><originalsourceid>FETCH-epo_espacenet_ME00757B3</originalsourceid><addsrcrecordid>eNrjZHB38nSOdPbxdFbwcA1xDfJ3DPL3dQwBcp39fQP8Q_1cghUcgxUCgvxDXD39FEIig_yDPf1cFbw9_RyDXRU8_Tw8nTxD_IOCeRhY0xJzilN5oTQ3g6yba4izh25qQX58anFBYnJqXmpJvK-rgYG5qbmTMSF5ALj-K2k</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>BICYCLIC HETEROAROMATIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS</title><source>esp@cenet</source><creator>Smith, Kathryn Jane ; Carter, Malcolm Clive ; Lackey, Karen Elizabeth ; Cockerill, George Stuart ; Guntrip, Stephen Barry</creator><creatorcontrib>Smith, Kathryn Jane ; Carter, Malcolm Clive ; Lackey, Karen Elizabeth ; Cockerill, George Stuart ; Guntrip, Stephen Barry</creatorcontrib><description>Opisana suheteroaromatična jedinjenja formule (I): Opisana suheteroaromatična jedinjenja formule (I):         ili njegova so ili solvat; gde Y je CR1 i V je N; ili Y je CR1i V je CR2; R1 predstavlja grupu CH3SO2CH2CH2NHCH2-Ar-,gde Ar se bira između furana i tiazola, od kojih svaki može biti opcionosupstituisan sa jednim ili dva halo, C1-4 alkil ili C1-4aloksigrupama; R2 je vodonik ili C1-4 alkoksi; ili R2je halo; R3 se bira iz grupe koju čine benzil-, halo-, dihalo- itrihalobenzil, benzoil, piridilmetil, piridilmetoksi, fenoksi, benziloksi,halo-, dihalo- i trihalobenziloksi i benzensulfonil; R4 je halo iliC1-4 alkoksi ili nije prisutan; gde ili (a) R3predstavlja 3-fluorobenziloksi; ili njegova so ili solvat; gde Y je CR 1 i V je N; ili Y je CR 1 i V je CR 2 ; R 1 predstavlja grupu CH 3 SO 2 CH 2 CH 2 NHCH 2 -Ar-,gde Ar se bira između furana i tiazola, od kojih svaki može biti opcionosupstituisan sa jednim ili dva halo, C 1-4 alkil ili C 1-4 aloksigrupama; R 2 je vodonik ili C 1-4 alkoksi; ili R 2 je halo; R 3 se bira iz grupe koju čine benzil-, halo-, dihalo- itrihalobenzil, benzoil, piridilmetil, piridilmetoksi, fenoksi, benziloksi,halo-, dihalo- i trihalobenziloksi i benzensulfonil; R 4 je halo iliC 1-4 alkoksi ili nije prisutan; gde ili (a) R 3 predstavlja 3-fluorobenziloksi; i/ili (b) R4 se bira od halo i supstituent je u položaju 3fenil prstena; i halo predstavlja fluoro, hloro ili bromo, kao i njihovodobijanje, farmaceutski preparati koji ih sadrže i njihova upotreba u medicini. i/ili (b) R 4 se bira od halo i supstituent je u položaju 3fenil prstena; i halo predstavlja fluoro, hloro ili bromo, kao i njihovodobijanje, farmaceutski preparati koji ih sadrže i njihova upotreba u medicini. Compounds of formula (I) and salts or solvates thereof are disclosed wherein Y is CR and V is N; or Y is CR and V is CR ; R represents CH3SO2CH2CH2NHCH2-Ar-, wherein Ar is furan or thiazole, each of which may optionally be substituted by one or two halo, C1-4 alkyl or C1-4 alkoxy groups; R is hydrogen C1-4 alkoxy or halo; R is benzyl, halo-, dihalo- or trihalobenzyl, benzoyl, pyridylmethyl, pyridylmethoxy, phenoxy, benzyloxy, halo-, dihalo- or trihalobenzyloxy or benzenesulphonyl; R is halo or C1-4 alkoxy or is not present; and wherein either (a) R represents 3-fluorobenzyloxy; and/or (b) R is halo and is substituted in the 3-position of the phenyl ring; and wherein halo represents fluoro, chloro or bromo. Processes for the preparation of the compounds, pharmaceutical formulations of the compounds, the use of the compounds in therapy, and methods of treatment of inter alia cancer and malignant tumours by administration of the compounds is also disclosed.</description><language>eng</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&amp;date=20080605&amp;DB=EPODOC&amp;CC=ME&amp;NR=00757B$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,777,882,25545,76296</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20080605&amp;DB=EPODOC&amp;CC=ME&amp;NR=00757B$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>Smith, Kathryn Jane</creatorcontrib><creatorcontrib>Carter, Malcolm Clive</creatorcontrib><creatorcontrib>Lackey, Karen Elizabeth</creatorcontrib><creatorcontrib>Cockerill, George Stuart</creatorcontrib><creatorcontrib>Guntrip, Stephen Barry</creatorcontrib><title>BICYCLIC HETEROAROMATIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS</title><description>Opisana suheteroaromatična jedinjenja formule (I): Opisana suheteroaromatična jedinjenja formule (I):         ili njegova so ili solvat; gde Y je CR1 i V je N; ili Y je CR1i V je CR2; R1 predstavlja grupu CH3SO2CH2CH2NHCH2-Ar-,gde Ar se bira između furana i tiazola, od kojih svaki može biti opcionosupstituisan sa jednim ili dva halo, C1-4 alkil ili C1-4aloksigrupama; R2 je vodonik ili C1-4 alkoksi; ili R2je halo; R3 se bira iz grupe koju čine benzil-, halo-, dihalo- itrihalobenzil, benzoil, piridilmetil, piridilmetoksi, fenoksi, benziloksi,halo-, dihalo- i trihalobenziloksi i benzensulfonil; R4 je halo iliC1-4 alkoksi ili nije prisutan; gde ili (a) R3predstavlja 3-fluorobenziloksi; ili njegova so ili solvat; gde Y je CR 1 i V je N; ili Y je CR 1 i V je CR 2 ; R 1 predstavlja grupu CH 3 SO 2 CH 2 CH 2 NHCH 2 -Ar-,gde Ar se bira između furana i tiazola, od kojih svaki može biti opcionosupstituisan sa jednim ili dva halo, C 1-4 alkil ili C 1-4 aloksigrupama; R 2 je vodonik ili C 1-4 alkoksi; ili R 2 je halo; R 3 se bira iz grupe koju čine benzil-, halo-, dihalo- itrihalobenzil, benzoil, piridilmetil, piridilmetoksi, fenoksi, benziloksi,halo-, dihalo- i trihalobenziloksi i benzensulfonil; R 4 je halo iliC 1-4 alkoksi ili nije prisutan; gde ili (a) R 3 predstavlja 3-fluorobenziloksi; i/ili (b) R4 se bira od halo i supstituent je u položaju 3fenil prstena; i halo predstavlja fluoro, hloro ili bromo, kao i njihovodobijanje, farmaceutski preparati koji ih sadrže i njihova upotreba u medicini. i/ili (b) R 4 se bira od halo i supstituent je u položaju 3fenil prstena; i halo predstavlja fluoro, hloro ili bromo, kao i njihovodobijanje, farmaceutski preparati koji ih sadrže i njihova upotreba u medicini. Compounds of formula (I) and salts or solvates thereof are disclosed wherein Y is CR and V is N; or Y is CR and V is CR ; R represents CH3SO2CH2CH2NHCH2-Ar-, wherein Ar is furan or thiazole, each of which may optionally be substituted by one or two halo, C1-4 alkyl or C1-4 alkoxy groups; R is hydrogen C1-4 alkoxy or halo; R is benzyl, halo-, dihalo- or trihalobenzyl, benzoyl, pyridylmethyl, pyridylmethoxy, phenoxy, benzyloxy, halo-, dihalo- or trihalobenzyloxy or benzenesulphonyl; R is halo or C1-4 alkoxy or is not present; and wherein either (a) R represents 3-fluorobenzyloxy; and/or (b) R is halo and is substituted in the 3-position of the phenyl ring; and wherein halo represents fluoro, chloro or bromo. Processes for the preparation of the compounds, pharmaceutical formulations of the compounds, the use of the compounds in therapy, and methods of treatment of inter alia cancer and malignant tumours by administration of the compounds is also disclosed.</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>eNrjZHB38nSOdPbxdFbwcA1xDfJ3DPL3dQwBcp39fQP8Q_1cghUcgxUCgvxDXD39FEIig_yDPf1cFbw9_RyDXRU8_Tw8nTxD_IOCeRhY0xJzilN5oTQ3g6yba4izh25qQX58anFBYnJqXmpJvK-rgYG5qbmTMSF5ALj-K2k</recordid><startdate>20080605</startdate><enddate>20080605</enddate><creator>Smith, Kathryn Jane</creator><creator>Carter, Malcolm Clive</creator><creator>Lackey, Karen Elizabeth</creator><creator>Cockerill, George Stuart</creator><creator>Guntrip, Stephen Barry</creator><scope>EVB</scope></search><sort><creationdate>20080605</creationdate><title>BICYCLIC HETEROAROMATIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS</title><author>Smith, Kathryn Jane ; Carter, Malcolm Clive ; Lackey, Karen Elizabeth ; Cockerill, George Stuart ; Guntrip, Stephen Barry</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_ME00757B3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</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>Smith, Kathryn Jane</creatorcontrib><creatorcontrib>Carter, Malcolm Clive</creatorcontrib><creatorcontrib>Lackey, Karen Elizabeth</creatorcontrib><creatorcontrib>Cockerill, George Stuart</creatorcontrib><creatorcontrib>Guntrip, Stephen Barry</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>Smith, Kathryn Jane</au><au>Carter, Malcolm Clive</au><au>Lackey, Karen Elizabeth</au><au>Cockerill, George Stuart</au><au>Guntrip, Stephen Barry</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>BICYCLIC HETEROAROMATIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS</title><date>2008-06-05</date><risdate>2008</risdate><abstract>Opisana suheteroaromatična jedinjenja formule (I): Opisana suheteroaromatična jedinjenja formule (I):         ili njegova so ili solvat; gde Y je CR1 i V je N; ili Y je CR1i V je CR2; R1 predstavlja grupu CH3SO2CH2CH2NHCH2-Ar-,gde Ar se bira između furana i tiazola, od kojih svaki može biti opcionosupstituisan sa jednim ili dva halo, C1-4 alkil ili C1-4aloksigrupama; R2 je vodonik ili C1-4 alkoksi; ili R2je halo; R3 se bira iz grupe koju čine benzil-, halo-, dihalo- itrihalobenzil, benzoil, piridilmetil, piridilmetoksi, fenoksi, benziloksi,halo-, dihalo- i trihalobenziloksi i benzensulfonil; R4 je halo iliC1-4 alkoksi ili nije prisutan; gde ili (a) R3predstavlja 3-fluorobenziloksi; ili njegova so ili solvat; gde Y je CR 1 i V je N; ili Y je CR 1 i V je CR 2 ; R 1 predstavlja grupu CH 3 SO 2 CH 2 CH 2 NHCH 2 -Ar-,gde Ar se bira između furana i tiazola, od kojih svaki može biti opcionosupstituisan sa jednim ili dva halo, C 1-4 alkil ili C 1-4 aloksigrupama; R 2 je vodonik ili C 1-4 alkoksi; ili R 2 je halo; R 3 se bira iz grupe koju čine benzil-, halo-, dihalo- itrihalobenzil, benzoil, piridilmetil, piridilmetoksi, fenoksi, benziloksi,halo-, dihalo- i trihalobenziloksi i benzensulfonil; R 4 je halo iliC 1-4 alkoksi ili nije prisutan; gde ili (a) R 3 predstavlja 3-fluorobenziloksi; i/ili (b) R4 se bira od halo i supstituent je u položaju 3fenil prstena; i halo predstavlja fluoro, hloro ili bromo, kao i njihovodobijanje, farmaceutski preparati koji ih sadrže i njihova upotreba u medicini. i/ili (b) R 4 se bira od halo i supstituent je u položaju 3fenil prstena; i halo predstavlja fluoro, hloro ili bromo, kao i njihovodobijanje, farmaceutski preparati koji ih sadrže i njihova upotreba u medicini. Compounds of formula (I) and salts or solvates thereof are disclosed wherein Y is CR and V is N; or Y is CR and V is CR ; R represents CH3SO2CH2CH2NHCH2-Ar-, wherein Ar is furan or thiazole, each of which may optionally be substituted by one or two halo, C1-4 alkyl or C1-4 alkoxy groups; R is hydrogen C1-4 alkoxy or halo; R is benzyl, halo-, dihalo- or trihalobenzyl, benzoyl, pyridylmethyl, pyridylmethoxy, phenoxy, benzyloxy, halo-, dihalo- or trihalobenzyloxy or benzenesulphonyl; R is halo or C1-4 alkoxy or is not present; and wherein either (a) R represents 3-fluorobenzyloxy; and/or (b) R is halo and is substituted in the 3-position of the phenyl ring; and wherein halo represents fluoro, chloro or bromo. Processes for the preparation of the compounds, pharmaceutical formulations of the compounds, the use of the compounds in therapy, and methods of treatment of inter alia cancer and malignant tumours by administration of the compounds is also disclosed.</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 BICYCLIC HETEROAROMATIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS
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