CONDENSED HETEROARYLS AND THEIR APPLICATION
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to field of organic chemistry, namely to novel heterocyclic compounds of formula(1) and/or to their pharmaceutically acceptable salts, where Arepresents CH; Aand Aindependently represent CRor N; Aand Atogether with ring B represent 5-member...
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| creator | SU VEHJGO CHZHAN VEHJKHAN JAN KHAJBIN |
| description | FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to field of organic chemistry, namely to novel heterocyclic compounds of formula(1) and/or to their pharmaceutically acceptable salts, where Arepresents CH; Aand Aindependently represent CRor N; Aand Atogether with ring B represent 5-membered heteroaryl or heterocycle, with said 5-membered heteroaryl or heterocycle being selected fromwhere t represents 1 or 2; and Ris independently selected from H, C-Calkyl, C-aryl, C-C-membered cycloalkyl, C(O)NRR, -OR, heteroaryl, representing pyridine, and heterocycle, representing piperidine and tetrahydropyran; and each of said alkyl, aryl, cycloalkyl, heteroaryl and heterocycle can be substituted with one group, independently selected from C-Calkyl, possibly substituted with one substituent, selected from -CONMe, C-membered cycloalkyl, -CN, -OMe, -pyridine, tetrahydropyran, -CO-morpholine, -CO-pyrrolidine, (3-methyl)oxetane; -OH; -C(O)R; -CN; -C(O)NRR; -NRR; -OR; -S(O)R; halogen, and substituted with one group -COMe heterocycle, representing piperidine, on condition that when Arepresents CR, Aand Atogether with ring B are selected from structure (3), (5) or (6);represents single bond or double bond; Rrepresents heteroaryl, representing 6-membered or 9-10-membered aromatic mono- or bicyclic ring, containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulphur; possibly substituted with one or two groups, independently selected from Calkyl, Calkinyl, -NRR, -NRS(O)R, -OR, halogen, halogenalkyl; Ris independently selected from H; each R, R, R, R, and Ris independently selected from H; C-Calkyl, possibly substituted with one substituent, selected from -OH, -OMe, -CN, -NH, -NMe, C-cycloalkyl; C-Calkenyl; Calkinyl; Caryl, possibly substituted with one or more substituents, selected from fluorine or methyl group; C-membered cycloalkyl, possibly substituted with one substituent, selected from -OH and -CN; halogenalkyl; heteroaryl, representing pyridine; and substituted with one methyl group heterocycle, representing piperidine, or Rand Rtogether with atom (atoms) which they are bound to form 5-6-membered heterocyclic ring, representing pyrrolidine or morpholine; and in each case n is independently equal 2. Invention also relates to particular compounds, pharmaceutical composition, based on claimed compounds; method of inhibiting PI3K and/or mTOR activity and to application of claimed compounds.EFFECT: novel compounds, useful for inhibiting PI3K and/or mTOR act |
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| fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_RU2552114C2</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>RU2552114C2</sourcerecordid><originalsourceid>FETCH-epo_espacenet_RU2552114C23</originalsourceid><addsrcrecordid>eNrjZNB29vdzcfULdnVR8HANcQ3ydwyK9AlWcPRzUQjxcPUMUnAMCPDxdHYM8fT342FgTUvMKU7lhdLcDApuriHOHrqpBfnxqcUFicmpeakl8UGhRqamRoaGJs5GxkQoAQA5fCS0</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>CONDENSED HETEROARYLS AND THEIR APPLICATION</title><source>esp@cenet</source><creator>SU VEHJGO ; CHZHAN VEHJKHAN ; JAN KHAJBIN</creator><creatorcontrib>SU VEHJGO ; CHZHAN VEHJKHAN ; JAN KHAJBIN</creatorcontrib><description>FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to field of organic chemistry, namely to novel heterocyclic compounds of formula(1) and/or to their pharmaceutically acceptable salts, where Arepresents CH; Aand Aindependently represent CRor N; Aand Atogether with ring B represent 5-membered heteroaryl or heterocycle, with said 5-membered heteroaryl or heterocycle being selected fromwhere t represents 1 or 2; and Ris independently selected from H, C-Calkyl, C-aryl, C-C-membered cycloalkyl, C(O)NRR, -OR, heteroaryl, representing pyridine, and heterocycle, representing piperidine and tetrahydropyran; and each of said alkyl, aryl, cycloalkyl, heteroaryl and heterocycle can be substituted with one group, independently selected from C-Calkyl, possibly substituted with one substituent, selected from -CONMe, C-membered cycloalkyl, -CN, -OMe, -pyridine, tetrahydropyran, -CO-morpholine, -CO-pyrrolidine, (3-methyl)oxetane; -OH; -C(O)R; -CN; -C(O)NRR; -NRR; -OR; -S(O)R; halogen, and substituted with one group -COMe heterocycle, representing piperidine, on condition that when Arepresents CR, Aand Atogether with ring B are selected from structure (3), (5) or (6);represents single bond or double bond; Rrepresents heteroaryl, representing 6-membered or 9-10-membered aromatic mono- or bicyclic ring, containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulphur; possibly substituted with one or two groups, independently selected from Calkyl, Calkinyl, -NRR, -NRS(O)R, -OR, halogen, halogenalkyl; Ris independently selected from H; each R, R, R, R, and Ris independently selected from H; C-Calkyl, possibly substituted with one substituent, selected from -OH, -OMe, -CN, -NH, -NMe, C-cycloalkyl; C-Calkenyl; Calkinyl; Caryl, possibly substituted with one or more substituents, selected from fluorine or methyl group; C-membered cycloalkyl, possibly substituted with one substituent, selected from -OH and -CN; halogenalkyl; heteroaryl, representing pyridine; and substituted with one methyl group heterocycle, representing piperidine, or Rand Rtogether with atom (atoms) which they are bound to form 5-6-membered heterocyclic ring, representing pyrrolidine or morpholine; and in each case n is independently equal 2. Invention also relates to particular compounds, pharmaceutical composition, based on claimed compounds; method of inhibiting PI3K and/or mTOR activity and to application of claimed compounds.EFFECT: novel compounds, useful for inhibiting PI3K and/or mTOR activity have been obtained.15 cl, 16 ex
Изобретение относится к области органической химии, а именно к новым гетероциклическим соединениям формулы (1) и/или к их фармацевтически приемлемым солям, где Апредставляет СН; Аи Анезависимо представляют собой СRили N; Аи Асовместно с кольцом В представляют собой 5-членный гетероарил или гетероцикл, причем указанный 5-членный гетероарил или гетероцикл выбран изгде t представляет собой 1 или 2; иRнезависимо выбран из Н, С-Салкила, С-арила, С-С-членного циклоалкила, C(O)NRR, -OR, гетероарила, представляющего собой пиридин, и гетероцикла, представляющего собой пиперидин и тетрагидропиран; и каждый из вышеуказанных алкила, арила, циклоалкила, гетероарила и гетероцикла может быть замещен одной группой, независимо выбранной из С-Салкила, возможно замещенного одним заместителем, выбранным из -CONMe, С-членного циклоалкила, -CN, -ОМе, -пиридина, тетрагидропирана, -СО-морфолина, -СО-пирролидина, (3-метил)оксетана; -ОН; -C(O)R; -CN; -C(O)NRR; -NRR; -OR; -S(O)R; галогена; и замещенного одной группой -СОМе гетероцикла, представляющего собой пиперидин; при условии, что когда Апредставляет собой CR, Аи Асовместно с кольцом В выбраны из структуры (3), (5) или (6);представляет собой одинарную связь или двойную связь; Rпредставляет собой гетероарил, представляющий собой 6-членное или 9-10-членное ароматическое моно- или бициклическое кольцо, содержащее 1-3 гетероатома, выбранных из азота, кислорода и серы, возможно замещенный одной или двумя группами, независимо выбранными из Салкила, Салкинила, -NRR, -NRS(O)R, -OR, галогена, галогеналкила; Rнезависимо выбран из Н; каждый R, R, R, R, и Rнезависимо выбран из Н; С-Салкила, возможно замещенного одним заместителем, выбранным из -ОН, -ОМе, -CN, -NH, -N</description><language>eng ; rus</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>2015</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=20150610&DB=EPODOC&CC=RU&NR=2552114C2$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20150610&DB=EPODOC&CC=RU&NR=2552114C2$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>SU VEHJGO</creatorcontrib><creatorcontrib>CHZHAN VEHJKHAN</creatorcontrib><creatorcontrib>JAN KHAJBIN</creatorcontrib><title>CONDENSED HETEROARYLS AND THEIR APPLICATION</title><description>FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to field of organic chemistry, namely to novel heterocyclic compounds of formula(1) and/or to their pharmaceutically acceptable salts, where Arepresents CH; Aand Aindependently represent CRor N; Aand Atogether with ring B represent 5-membered heteroaryl or heterocycle, with said 5-membered heteroaryl or heterocycle being selected fromwhere t represents 1 or 2; and Ris independently selected from H, C-Calkyl, C-aryl, C-C-membered cycloalkyl, C(O)NRR, -OR, heteroaryl, representing pyridine, and heterocycle, representing piperidine and tetrahydropyran; and each of said alkyl, aryl, cycloalkyl, heteroaryl and heterocycle can be substituted with one group, independently selected from C-Calkyl, possibly substituted with one substituent, selected from -CONMe, C-membered cycloalkyl, -CN, -OMe, -pyridine, tetrahydropyran, -CO-morpholine, -CO-pyrrolidine, (3-methyl)oxetane; -OH; -C(O)R; -CN; -C(O)NRR; -NRR; -OR; -S(O)R; halogen, and substituted with one group -COMe heterocycle, representing piperidine, on condition that when Arepresents CR, Aand Atogether with ring B are selected from structure (3), (5) or (6);represents single bond or double bond; Rrepresents heteroaryl, representing 6-membered or 9-10-membered aromatic mono- or bicyclic ring, containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulphur; possibly substituted with one or two groups, independently selected from Calkyl, Calkinyl, -NRR, -NRS(O)R, -OR, halogen, halogenalkyl; Ris independently selected from H; each R, R, R, R, and Ris independently selected from H; C-Calkyl, possibly substituted with one substituent, selected from -OH, -OMe, -CN, -NH, -NMe, C-cycloalkyl; C-Calkenyl; Calkinyl; Caryl, possibly substituted with one or more substituents, selected from fluorine or methyl group; C-membered cycloalkyl, possibly substituted with one substituent, selected from -OH and -CN; halogenalkyl; heteroaryl, representing pyridine; and substituted with one methyl group heterocycle, representing piperidine, or Rand Rtogether with atom (atoms) which they are bound to form 5-6-membered heterocyclic ring, representing pyrrolidine or morpholine; and in each case n is independently equal 2. Invention also relates to particular compounds, pharmaceutical composition, based on claimed compounds; method of inhibiting PI3K and/or mTOR activity and to application of claimed compounds.EFFECT: novel compounds, useful for inhibiting PI3K and/or mTOR activity have been obtained.15 cl, 16 ex
Изобретение относится к области органической химии, а именно к новым гетероциклическим соединениям формулы (1) и/или к их фармацевтически приемлемым солям, где Апредставляет СН; Аи Анезависимо представляют собой СRили N; Аи Асовместно с кольцом В представляют собой 5-членный гетероарил или гетероцикл, причем указанный 5-членный гетероарил или гетероцикл выбран изгде t представляет собой 1 или 2; иRнезависимо выбран из Н, С-Салкила, С-арила, С-С-членного циклоалкила, C(O)NRR, -OR, гетероарила, представляющего собой пиридин, и гетероцикла, представляющего собой пиперидин и тетрагидропиран; и каждый из вышеуказанных алкила, арила, циклоалкила, гетероарила и гетероцикла может быть замещен одной группой, независимо выбранной из С-Салкила, возможно замещенного одним заместителем, выбранным из -CONMe, С-членного циклоалкила, -CN, -ОМе, -пиридина, тетрагидропирана, -СО-морфолина, -СО-пирролидина, (3-метил)оксетана; -ОН; -C(O)R; -CN; -C(O)NRR; -NRR; -OR; -S(O)R; галогена; и замещенного одной группой -СОМе гетероцикла, представляющего собой пиперидин; при условии, что когда Апредставляет собой CR, Аи Асовместно с кольцом В выбраны из структуры (3), (5) или (6);представляет собой одинарную связь или двойную связь; Rпредставляет собой гетероарил, представляющий собой 6-членное или 9-10-членное ароматическое моно- или бициклическое кольцо, содержащее 1-3 гетероатома, выбранных из азота, кислорода и серы, возможно замещенный одной или двумя группами, независимо выбранными из Салкила, Салкинила, -NRR, -NRS(O)R, -OR, галогена, галогеналкила; Rнезависимо выбран из Н; каждый R, R, R, R, и Rнезависимо выбран из Н; С-Салкила, возможно замещенного одним заместителем, выбранным из -ОН, -ОМе, -CN, -NH, -N</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>2015</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZNB29vdzcfULdnVR8HANcQ3ydwyK9AlWcPRzUQjxcPUMUnAMCPDxdHYM8fT342FgTUvMKU7lhdLcDApuriHOHrqpBfnxqcUFicmpeakl8UGhRqamRoaGJs5GxkQoAQA5fCS0</recordid><startdate>20150610</startdate><enddate>20150610</enddate><creator>SU VEHJGO</creator><creator>CHZHAN VEHJKHAN</creator><creator>JAN KHAJBIN</creator><scope>EVB</scope></search><sort><creationdate>20150610</creationdate><title>CONDENSED HETEROARYLS AND THEIR APPLICATION</title><author>SU VEHJGO ; CHZHAN VEHJKHAN ; JAN KHAJBIN</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_RU2552114C23</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; rus</language><creationdate>2015</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>SU VEHJGO</creatorcontrib><creatorcontrib>CHZHAN VEHJKHAN</creatorcontrib><creatorcontrib>JAN KHAJBIN</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>SU VEHJGO</au><au>CHZHAN VEHJKHAN</au><au>JAN KHAJBIN</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>CONDENSED HETEROARYLS AND THEIR APPLICATION</title><date>2015-06-10</date><risdate>2015</risdate><abstract>FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to field of organic chemistry, namely to novel heterocyclic compounds of formula(1) and/or to their pharmaceutically acceptable salts, where Arepresents CH; Aand Aindependently represent CRor N; Aand Atogether with ring B represent 5-membered heteroaryl or heterocycle, with said 5-membered heteroaryl or heterocycle being selected fromwhere t represents 1 or 2; and Ris independently selected from H, C-Calkyl, C-aryl, C-C-membered cycloalkyl, C(O)NRR, -OR, heteroaryl, representing pyridine, and heterocycle, representing piperidine and tetrahydropyran; and each of said alkyl, aryl, cycloalkyl, heteroaryl and heterocycle can be substituted with one group, independently selected from C-Calkyl, possibly substituted with one substituent, selected from -CONMe, C-membered cycloalkyl, -CN, -OMe, -pyridine, tetrahydropyran, -CO-morpholine, -CO-pyrrolidine, (3-methyl)oxetane; -OH; -C(O)R; -CN; -C(O)NRR; -NRR; -OR; -S(O)R; halogen, and substituted with one group -COMe heterocycle, representing piperidine, on condition that when Arepresents CR, Aand Atogether with ring B are selected from structure (3), (5) or (6);represents single bond or double bond; Rrepresents heteroaryl, representing 6-membered or 9-10-membered aromatic mono- or bicyclic ring, containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulphur; possibly substituted with one or two groups, independently selected from Calkyl, Calkinyl, -NRR, -NRS(O)R, -OR, halogen, halogenalkyl; Ris independently selected from H; each R, R, R, R, and Ris independently selected from H; C-Calkyl, possibly substituted with one substituent, selected from -OH, -OMe, -CN, -NH, -NMe, C-cycloalkyl; C-Calkenyl; Calkinyl; Caryl, possibly substituted with one or more substituents, selected from fluorine or methyl group; C-membered cycloalkyl, possibly substituted with one substituent, selected from -OH and -CN; halogenalkyl; heteroaryl, representing pyridine; and substituted with one methyl group heterocycle, representing piperidine, or Rand Rtogether with atom (atoms) which they are bound to form 5-6-membered heterocyclic ring, representing pyrrolidine or morpholine; and in each case n is independently equal 2. Invention also relates to particular compounds, pharmaceutical composition, based on claimed compounds; method of inhibiting PI3K and/or mTOR activity and to application of claimed compounds.EFFECT: novel compounds, useful for inhibiting PI3K and/or mTOR activity have been obtained.15 cl, 16 ex
Изобретение относится к области органической химии, а именно к новым гетероциклическим соединениям формулы (1) и/или к их фармацевтически приемлемым солям, где Апредставляет СН; Аи Анезависимо представляют собой СRили N; Аи Асовместно с кольцом В представляют собой 5-членный гетероарил или гетероцикл, причем указанный 5-членный гетероарил или гетероцикл выбран изгде t представляет собой 1 или 2; иRнезависимо выбран из Н, С-Салкила, С-арила, С-С-членного циклоалкила, C(O)NRR, -OR, гетероарила, представляющего собой пиридин, и гетероцикла, представляющего собой пиперидин и тетрагидропиран; и каждый из вышеуказанных алкила, арила, циклоалкила, гетероарила и гетероцикла может быть замещен одной группой, независимо выбранной из С-Салкила, возможно замещенного одним заместителем, выбранным из -CONMe, С-членного циклоалкила, -CN, -ОМе, -пиридина, тетрагидропирана, -СО-морфолина, -СО-пирролидина, (3-метил)оксетана; -ОН; -C(O)R; -CN; -C(O)NRR; -NRR; -OR; -S(O)R; галогена; и замещенного одной группой -СОМе гетероцикла, представляющего собой пиперидин; при условии, что когда Апредставляет собой CR, Аи Асовместно с кольцом В выбраны из структуры (3), (5) или (6);представляет собой одинарную связь или двойную связь; Rпредставляет собой гетероарил, представляющий собой 6-членное или 9-10-членное ароматическое моно- или бициклическое кольцо, содержащее 1-3 гетероатома, выбранных из азота, кислорода и серы, возможно замещенный одной или двумя группами, независимо выбранными из Салкила, Салкинила, -NRR, -NRS(O)R, -OR, галогена, галогеналкила; Rнезависимо выбран из Н; каждый R, R, R, R, и Rнезависимо выбран из Н; С-Салкила, возможно замещенного одним заместителем, выбранным из -ОН, -ОМе, -CN, -NH, -N</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 | CONDENSED HETEROARYLS AND THEIR APPLICATION |
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